Running head: PERSONAL DRUGS
1
Personal Drugs
Ashley Peczkowski
Wright State University
PERSONAL DRUGS
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First Diagnosis: Left Ventricular Heart Failure in a Renal Patient
A 45 year old male presents as a new patient to your cardiology practice. He has not seen
a cardiologist since he was hospitalized three years ago for acute myocardial infarction (MI). The
patient has expressed concern for increased leg swelling over the past week and a weight gain of
three pounds. His history includes diabetes, end stage chronic kidney disease requiring
hemodialysis, and MI. An in office echocardiogram shows a dilated left ventricle with a 40%
ejection fracture (EF). Upon completion of history and physical his diagnosis is left ventricular
heart failure (LVHF) with fluid overload. Laboratory tests have been ordered, including lipid
panel, basic metabolic panel, complete blood count, B-type natriuretic peptide (BNP), and a
urinalysis. Results are pending. Other tests ordered include an electrocardiogram (ECG) and
chest x-ray. An in office blood glucose test was 152, blood pressure was 167/93 and his weight
and height are 167 pounds (75.9 kilograms), five foot nine inches. Finally, he is set up to receive
an additional hemodialysis treatment today for removal of excess fluid.
I. Definition of Diagnosis
Heart failure is defined by the Heart Failure Society of America (2013) as a syndrome,
not a diagnosis, which can be caused by cardiac impairment. This can result from myocardial
muscle dysfunction or destruction and is represented by either left ventricular dilation or
hypertrophy or both (Albert et al., 2010). According to the 2009 heart failure guidelines, there
are four different stages of heart failure. The first two stages (A and B) are not considered heart
failure but rather at risk patients and include those with a history of hypertension (HTN),
pervious MI, diabetes (DM), left ventricular (LV) remodeling and other pre heart failure (HF)
diseases. The final two stages (C and D) are for those patients who have diagnosed heart failure.
PERSONAL DRUGS
3
Stage C includes those with known structural cardiac deficits, shortness of breath (SOB), fatigue,
and reduced tolerance for exercise. The final stage, stage D, are for patients who have maxed out
on medical therapy and need specialized interventions such as hospice, heart transplant, or
permanent mechanical support (Abraham et al., 2009).
Diagnosis criteria are not exact and can depend on a variety of findings or symptoms. An
echocardiogram is the most common tool used to diagnosis HF. A comprehensive 2-dimensional
echocardiogram with Doppler flow studies can determine EF, structural abnormalities,
ventricular wall thickness, wall motion, valvular abnormalities, and pericardial abnormalities
(Abraham et al., 2009). The typical findings of a HF patient are an EF of 40 percent or less;
however, the patient may still have HF with a higher EF (Heart Failure Society of America,
2002). Left ventricular dilation, hypertrophy, reduced EF, and symptoms such as fatigue, SOB,
fluid retention, reduced exercise tolerance, palpations, and cough are all evaluated when
diagnosing LVHF.
II. Therapeutic Objectives
Treatment objectives for patients with LVHF include life style changes, risk factor
management, starting ACE inhibitors, Beta blockers, and insertion of a pacemaker/ defibrillator
for appropriate patients. Life style changes such as smoking cessation, regular exercise, reduced
alcohol use, and illicit drug use should be encouraged. The treatment goals according to the
Heart Failure Practice Guidelines for 2010 are: HTN patients with renal insufficiency and ≤ one
g/day of proteinuria need to sustain a blood pressure of 130/85, have a limited sodium diet,
reduced BMI to < 30(Albert et al., 2010), and obtain management of hyperlipidemia (HDL >
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PERSONAL DRUGS
50mg/dL and LDL < 100mg/dL) and diabetes (A1C < 7%) (American Diabetes Association,
2011).
While HF is considered a progressive disease, it is important to stabilize myocardial
dysfunction and improve remodeling. These outcomes are obtained by medication therapy
through ACE inhibitors, beta-blockers, and diuretics. ACE inhibitors are given to those with
increased risk of developing HF such as those with coronary artery disease, diabetes, peripheral
vascular disease, or stroke. Beta blockers are given for those individuals who have suffered from
a previous MI and diuretics are given to those with fluid overload and functioning kidneys
(Albert et al., 2010). For those individuals with severe kidney impairment requiring
hemodialysis, fluid overload should be treated with dialysis and ACE inhibitors should be
avoided (Abraham et al., 2009).
An implantable cardioverter-defibrillator (ICD) should be considered for those patients
with sustained ventricular arrhythmias, cardiac arrest, or unexplained syncope to prevent sudden
death. An ICD is contraindicated in those individuals with progressive decompensated HF
because death is expected. Only in cases of planned cardiac transplant should the ICD then be
considered (Abraham et al., 2009).
III. Inventory of Effective Drug Groups: Oral
Drug
Angiotensin II
Receptor
Blockers (ARBs)
Candesartan
(Atacand®),
Eprosartan
Efficacy
Pharmacodynamics:
ARBs selective
inhibition of angiotensin
II by competitive
antagonism of receptors.
Displacement of
angiotensin II from
Safety
Side effects:
Common:
Hyperkalemia,
hypotension, dizziness,
headache, drowsiness,
diarrhea, metallic taste,
and rash.
Suitability
This medication can
be given with or
without food. Avoid
alcohol use (Lexicomp, 2013).
Contraindications:
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PERSONAL DRUGS
(Teventen®),
Irbesartan
(Avapro®),
Losartan
(Cozaar®),
Olmesartan
(Benicar®),
Telmisartan
(Micardis®),
Valsartan
(Diovan®) (Lexicomp, 2013)
AngiotensinConverting
Enzyme (ACE)
angiotensin I receptor to
produce vasodilation,
prohibit aldosterone
release, catecholamine
release, arginine
vasopressin release,
water intake and reduce
hypertrophic response
(Barraras & GurkTurner, 2003).
Pharmacokinetics
Absorption: Rapid
Metabolism: Absorption
via ester hydrolysis with
intestinal wall, hepatic
CYP2C9 and 3A4.
Extensive first pass
effect
Excretion: Urine and
feces (Clinical
Pharmacology, 2013)
Pharmacodynamics:
Prevents conversion of
angiotensin I to
Rare:
Kidney impairment,
hepatic impairment,
angioedema, and
leukocytosis (Lexicomp, 2013).
Monitor: Supine BP,
CNS changes,
hyperglycemia,
electrolytes, serum
creatinine, BUN,
urinalysis, hypotension,
tachycardia, and CBC
(Lexi-comp, 2013).
Substrate CYP2C9
(minor), Inhibits
CYP2C8 (moderate),
(weak), CYP2C19
(weak), CYP2D6
(weak), CYP3A4
(weak), CYP2C9
(weak), (moderate) and
SLCO1B1 (Lexi-comp,
2013).
Side effects:
Common: Orthostatic
effects, hypotension,
Hypersensitivity to
ARBs or formulary
components.
Concomitant use of
aliskiren in diabetic
patients (Lexi-comp,
2013).
Use Caution:
May not be effective
in African-American
patients. Use with
caution in
Aortic/Mitral
stenosis. Reduce dose
in hepatic
impairment, and use
with caution in renal
impairment, Bilateral
renal artery stenosis,
aortic/mitral stenosis,
oral airway surgery,
or history of
angioedema. Watch
for hyperkalemia in
renal impairment,
potassium-sparring
diuretics, potassium
supplements, and
potassium salts.
Watch for
hypotension in
volume depletion.
May cause further
renal dysfunction.
May cause worsening
Heart failure.
Diabetics should
monitor glucose
closely (Access
Medicine, 2013;
Lexi-comp, 2013).
Take on empty
stomach one hour
before or two hours
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PERSONAL DRUGS
Inhibitors
Benazepril
(Lotensin®),
Captopril
(Capoten®),
Enalapril
(Vasotec®,
Renitec®),
Fosinopril
(Monopril®),
Lisinopril
(Lisodur®,
Lopril®,
Novatec®,
Prinivil®,
Zestril®),
Perindopril
(Cpversy®,
Aceon®),
Quinapril
(Accupril®),
Ramipril
(Altace®,
Tritace®,
Ramace®,
Ramwin®),
Trandolapril
(Mavik®) (Lexicomp, 2013)
angiotensin II which in
turn dilates arterioles
and promotes excretion
of sodium and water.
(Song & White, 2002).
headache, dizziness,
cough, rash,
hyperkalemia,
weakness, and metallic
taste
Pharmacokinetics:
Absorption: Moderately
in gastrointestinal (GI)
tract
Metabolism: Rapid and
extensive hepatic via
enzymatic hydrolysis,
50%; Extensive first
pass effect. Some drugs
not metabolized
Excretion: Urine
(unchanged) and hepatic
depending on drug
(Lexi-comp, 2013).
Under certain
conditions:
Prolonged QT interval,
gout, and bradycardia
Rare: Kidney failure,
neutropenia,
angioedema, and
Steven-Johnson
syndrome (Access
Medicine, 2013; Lexicomp, 2013).
Monitor:
BUN, Serum
creatinine, Renal
function, Lithium
levels, White blood
count, Potassium, and
CBC with differential
in renal impairment or
collagen diseases
Substrate CYP2D6
(major) (Lexi-comp,
2013).
before meal. Long
term use can alter
taste due to zinc
deficiency. Avoid
potassium rich diet
(Lexi-comp, 2013).
Contraindications:
Hypersensitivity to
ACE inhibitors,
previous angioedema,
and concomitant use
of aliskiren in
diabetic patients
(Lexi-comp, 2013).
Use Caution:
Use caution with
aortic stenosis,
African Americans
with angioedema
history, cholestatic
jaundice, cough,
cardiovascular
disease, collagen
vascular diseases,
hypertrophic
cardiomyopathy,
hyperkalemia,
hypersensitivity
reactions, hepatic
impairment,
neutropenia,
agranulocytosis, renal
artery stenosis, and
renal impairment.
Dose adjustment may
be needed in renal
impairment. Concommitted use with
ARBs and renin
inhibitors may cause
hypotension,
hyperkalemia, and
increased renal
impairment. (Clinical
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PERSONAL DRUGS
Beta Blockers
Acebutolol
(Sectral®),
Atenolol
(Tenormin®),
Betaxolol
(Kerlone®,
Betoptic®),
Bisoprolol
(Zebeta®),
Carvedilol
(Coreg®, Coreg
CR®), Esmolol
(Brevibloc®),
Labetalol
(Trandate®),
Metoprolol
(Lopressor®,
Toprol-XL®),
Nadolol
(Corgard®),
Nebivolol
(Bystolic®),
Penbutolol
(Levatol®),
Pindolol
(Visken®),
Propranolol
(Inderal®, Inderal
LA®, InnoPran
XL®), Sotalol
(Betapace®,
Sorine®),
Timolol
(Betimol®,
Blocadren®,
Istalol®,
Timoptic®)
(Lexi-comp,
2013)
Pharmacodynamics:
Beta adrenoreceptor
blocker or beta
adrenoreceptor and
alpha adrenergic
blocker causing reduced
cardiac output, exercise
tachycardia, reduced
reflex orthostatic
tachycardia,
vasodilation, lower
peripheral vascular
resistance, lower renal
resistance, reduced
plasma renin activity,
increased atrial
natriuretic peptide and
in heart failure patients
it reduced pulmonary
wedge pressure, lower
pulmonary artery
pressure, increase stroke
volume, and decrease
right atrial pressure
(Lexi-comp, 2013).
Pharmacokinetics:
Absorption: Rapid and
extensive
Metabolism: Hepatic
through CYP2c9, 2D6,
3A4, and 2C19. Three
active metabolites.
Extensive first pass
effect. Plasma
concentration in elderly
and hepatic impaired are
50% and 4-7 times
higher.
Excretion: primary feces
(2-60%), some urine
(30-80%) (Lexi-comp,
2013).
Side Effects:
Common:
Fatigue, cold hands,
headache, GI distress,
constipation, diarrhea,
and dizziness.
Rare:
Shortness of breath,
insomnia, decreased
libido, and depression
(Lexi-comp, 2013).
Monitor:
Blood pressure, heart
rate, fluid balance, and
glucose
Substrate CYP2C19
(minor) and CYP2D6
(major). Inhibits
CYP2D6 (weak) (Lexicomp, 2013).
Pharmacology, 2013;
Lexi-comp, 2013)
This drug should be
given with meals to
reduce orthostatic
hypotension. Do not
crush or chew.
Bradycardia may be
more severe in
elderly (Lexi-comp,
2013).
Contraindication:
Hypersensitivity to
Beta blockers,
Decompensated
cardiac failure
requiring intravenous
inotropic therapy,
Bronchial asthma,
Bronchospastic
conditions, Av block,
Sick sinus syndrome,
Sinus node
dysfunction,
Pregnancy, Severe
bradycardia without
pacemakers,
Cardiogenic Shock,
Severe hepatic
impairment
Use Caution:
Bronchospatic
disease, Conduction
abnormality,
Diabetes, Heart
failure, Hepatic
impairment,
Mesenteric Vascular
Disease, Myasthenia
gravis, Peripheral
vascular disease,
Pheochromocytoma,
Psoriasis, Psychiatric
Disease, Renal
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PERSONAL DRUGS
impairment, and
Thyroid disease. Use
caution when taking
verapamil, diltiazem,
digoxin, or inhaled
anesthetics (Lexicomp, 2013).
Diuretic/
Anhydrase
Diuretic
Acetazolamide
(Lexi-comp,
2013)
Pharmacodynamics:
Reverses inhibition of
carbonic anhydrase
causing reduced
hydrogen ion secretion
at renal tubule and
increase excretion of
sodium, potassium,
bicarbonate, and water.
Decreased aqueous
humor and inhibits
carbonic anhydrase in
CNS to retard abnormal
and excessive discharge
(Clinical Pharmacology,
2013; Lexi-comp,
2013).
Pharmacokinetics:
Onset of Action: Two
hours
Peak Effect: Eight -18
hours
Duration: 18-24 hours
Time to Peak: three-six
hours
Excretion: Urine (70100% Unchanged)
(Lexi-comp, 2013).
Side Effects:
Common:
Taste alterations,
nausea, vomiting,
diarrhea, polyuria,
drowsiness, and
dehydration
Under Certain
Condition:
Numbness in
extremities, blurred
vision, and kidney
stones
Rare:
Acidosis and confusion
(Lexi-comp, 2013).
Monitor:
Intraocular pressure,
serum electrolytes,
CBC with differential,
growth, and glucose in
diabetics.
Inhibits CTYP3A4
(weak) (Lexi-comp,
2013).
Avoid:
Dental epinephrine
(Lexi-comp, 2013).
Give with food to
decrease GI upset.
Can cause metallic
taste (Access
Medicine, 2013).
Contraindications:
Hypersensitivity to
acetazolamide,
sulfonamides, or any
component. Hepatic
disease or
insufficiency.
Decreased sodium/
potassium levels.
Adrenocortical
insufficiency.
Cirrhosis,
hyperchloremic
acidosis. Severe renal
disease. Long term
use in non-congestive
angle-closure
glaucoma (Lexicomp, 2013)
Use Caution:
Impairment of mental
alertness, sulfa
allergy, diabetes,
hepatic impairment,
and respiratory
acidosis (Access
Medicine, 2013).
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PERSONAL DRUGS
Diuretic/
Loop Diuretics
Bumetanide
(Bumex®),
Ethacrynate
(Edecrin®),
Furosemide
(Lasix®),
Torsemide
(Demadex®)
(Lexi-comp,
2013)
Diuretics/
Potassium
Sparing Diuretic
Amiloride
Hydrochloride,
Spironolactone
Pharmacodynamics:
Inhibits reabsorption of
sodium and chloride in
ascending loop of
Henle, distal tubules,
and proximal renal
tubule. Causes excretion
of water, sodium,
chloride, magnesium,
phosphate, and calcium
(Lexi-comp, 2013).
Side Effects:
Common:
Hypokalemia,
dizziness, headache,
fatigue, constipation,
abdominal pain,
nausea, tinnitus, and
hyperglycemia.
Rare: Abnormal heart
rhythms (Lexi-comp,
2013).
Pharmacokinetics:
Absorption: Extensively
Metabolism: Partially
hepatic via CYP
Half-life: 0.5- 3.5 hours
Excretion: Urine (5081%; 20-45%
unchanged) and feces
(2%) (Lexi-comp,
2013).
Monitor:
Weight, I&O, blood
pressure, orthostasis,
serum electrolytes,
renal function, and
hearing (Clinical
Pharmacology, 2013).
Pharmacodynamics:
Blocks sodium channels
in late distal convoluted
tubule and collecting
duct. This causes
reduced intracellular
sodium decreasing
Avoid:
High dose Aspirin
(Lexi-comp, 2013).
May decrease levels
if taken with food.
Some patients may
need potassium
supplements (Lexicomp, 2013).
Contraindicated:
Anuria, Hepatic
come,
hypersensitivity to
loop diuretics or any
component, history of
severe watery
diarrhea caused by
drug and severe
electrolyte depletion
(Access Medicine,
2013).
Use Caution:
Cirrhosis, ascites,
fluid/ electrolyte loss,
diabetes, prostatic
hyperplasia, urinary
stricture, SLE
hypersensitivity
reactions,
hyperuricemia,
nephrotoxicity,
ototoxicity,
photosensitivity, sulfa
allergy, digoxin, and
with other
antihypertensive
(Lexi-comp, 2013)
Side Effects:
Avoid alcohol,
Common:
licorice, and
Dizziness, nausea, rash, potassium rich foods.
decreased libido,
Do not use salt
constipation, lethargy,
substitutes. May be
and vomiting.
taken with food if GI
Rare:
upset (Lexi-comp,
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PERSONAL DRUGS
(Aldactone®),
Triamterene
(Dyrenium®)
(Lexi-comp,
2013)
Na+/K+ATPase, leading
to potassium retention
and excretion of
calcium, magnesium,
and hydrogen ions
(Lexi-comp, 2013).
Pharmacokinetics:
Absorption: 15-25%
Metabolism: Hepatic,
multiple metabolites
Half-life: 78 minutes to
23 hours
Excretion: Urine and
feces (Lexi-comp,
2013).
Pharmacodynamics:
Inhibits sodium and
chloride reabsorption in
distal tubules, Proximal
Chlorothiazide
segment of the distal
(Diuril®)
tubule of the nephron,
Chlorthalidone
and cortical-diluting
(Hygroton®),
segment of the
Hydrochlorothiazi ascending loop of Henle
de (Hydrodiuril®, causing excretion of
Microzide®),
sodium, chloride, and
Indapamide
water. Product of
(Lozol®),
mechanism results in
Methyclothiazide diuresis. Also causes
(Enduron®),
potassium, hydrogen
Metolazone
ions, magnesium,
(Zaroxolyn®,
phosphate, and
Diuretics/
Thiazide
Diuretics
Macromastia,
confusion, StevenJohnsons syndrome,
and breast cancer
(Lexi-comp, 2013).
Monitor:
Blood pressure, serum
electrolytes, renal
function, I&O, CNS
changes, ECG changes,
rash, dehydration, and
daily weight (Lexicomp, 2013).
Side effects:
Common:
Hypokalemia,
dizziness, nausea, and
xerostomia
Rare:
Urinary retention,
sudden vision changes,
eye pain, or rash (Lexicomp, 2013)
Monitor:
Serum electrolytes,
renal function, blood
pressure, weight, and
I&O (Lexi-comp,
2013).
2013).
Contraindications:
Anuria, acute renal
insufficiency, severe
hepatic disease,
hypersensitivity to
potassium sparing
diuretics or any
component, diabetic
nephropathy, and
hyperkalemia (Lexicomp, 2013).
Use caution:
Fluid or electrolyte
loss, hyperkalemia,
diabetes,
photosensitivity,
kidney stones,
acidosis,
gynecomastia,
tumorigenic, adrenal
vein catheterization,
cirrhosis, heart
failure, and taking
potassium
supplements (Lexicomp, 2013).
Take dose in am or
early day to avoid
night time urinary
frequency. If taking
oral hypoglycemic,
watch glucose
closely. Decrease
dietary sodium and
calcium and increase
dietary potassium,
zinc, magnesium, and
riboflavin (Lexicomp, 2013).
Contraindications:
Hypersensitivity to
Thiazide diuretics or
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PERSONAL DRUGS
Diulo®,
Mykrox®) (Lexicomp, 2013).
bicarbonate loss (Lexicomp, 2013).
any component,
Sulfonamide-derived
drugs, and anuria
(Lexi-comp, 2013).
Pharmacokinetics:
Absorption: Poor
Metabolism: Not
metabolized
Half-life: 45 minutes -60
hours.
Excretion: Urine (1015%) (Clinical
Pharmacology, 2013;
Lexi-comp, 2013).
Digoxin
(Lanoxin®)
(Lexi-comp,
2013)
Pharmacodynamics:
Inhibits
sodium/potassium
APTase pump in
myocardial cells causing
increased intracellular
sodium, promoting
calcium influx creating
increased contractility
(Lexi-comp, 2013).
Pharmacokinetics:
Absorption: Passive
diffusion in upper small
intestine
Metabolism: Sugar
hydrolysis in stomach or
reduced lactone ring in
intestinal bacteria
Excretion: Urine (50-
Side Effects:
Common:
Dizziness, dyspepsia,
nausea, diarrhea,
tachycardia, or
bradycardia
Rare:
Confusion, weight
gain, vision changes,
anorexia, asthenia,
rash, or abnormal heart
conductions (Access
Medicine, 2013)
Monitor:
Heart rate, Apical
pulse, Rhythm,
Periodic ECGs,
Baseline and periodic
serum creatinine, serum
Use Caution:
Use caution with
patients who have:
Asthma, electrolyte
imbalance,
hypersensitivity
reactions, ocular
effects,
photosensitivity, sulfa
allergy, diabetes,
gout, hepatic
impairment,
hypercalcemia,
hypercholesterolemia
, renal impairment,
parathyroid disease,
and systemic lupus
erythematosus
(Access Medicine,
2013; Lexi-comp,
2013).
End stage renal
disease requires 50%
reduce in loading
dose. Needs
potassium rich diet
(Lexi-comp, 2013).
Contraindication:
Hypersensitivity to
digoxin, digitalis
forms, or any
component.
Ventricular
fibrillation (Lexicomp, 2013).
Use caution:
Proarrhythmic
effects, Accessory
bypass tract, Wolff-
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PERSONAL DRUGS
70% unchanged) (Lexicomp, 2013).
potassium, magnesium,
and
Calcium. Monitor for
signs of toxicity
including confusion
and depression. Draw
digoxin level 12-14
hours after initial dose
or 3-5 days, and then
every 5-7 days until at
steady state then 7-14
days (Lexi-comp,
2013).
Substrate of CYP3A4
(minor) (Lexicomp,
2013).
Nitrates
Isosorbide
Dinitrate,
Isosorbide
Mononitrate
(Imdur®,
Monoket®),
Nitroglycerin
(Nitro-Dur®)
(Lexi-comp,
2013)
Pharmacodynamics:
Stimulation of cyclicGMP causing vascular
smooth muscle
relaxation. More
prominent in veins.
Decreases preload thus
reducing cardiac oxygen
demand and reduced
afterload. Also improves
coronary artery dilation.
Nitroglycerin form free
radical nitric oxide
which works on the
smooth muscle and
increases guanosine 3’5’
monophosphate causing
smooth muscle
relaxation, reduces
Side effects:
Common:
Headache, flushing,
dizziness, upset
stomach, vomiting,
hypotension, and
arrhythmias
Rare:
Fainting, restlessness,
blurry vision, dry
mouth, and rash
(Access Medicine,
2013).
Monitor:
Blood pressure, heart
rate, GI disturbances,
volume depletion,
hypotension, right
Parkinson-White
syndrome, Acute MI
(6 months or less),
Atrioventricular
block, Beri beri heart
disease, electrolyte
imbalance, Heart
failure, Low EF,
Cardiomyopathy,
Constrictive
pericarditis, Amyloid
heart disease, Sinus
rhythm, No HF
symptoms,
Hypermetabolic
states, Hypertrophic
Cardiomyopathy,
Renal impairment,
Sinus nodal disease,
and Thyroid disease.
Reduce digoxin with
Amiodarone,
propafenone,
quinidine, and
verapamil (Clinical
Pharmacology,
2013).
Allow for nitrate free
intervals. Dose
alternate timing.
Alcohol can
exacerbate
hypotension (Lexicomp, 2013).
Contraindications:
Hypersensitivity to
Nitrates or any
component, Organic
nitrates, and
Concurrent use of
phosphodiesterase-5
inhibitors. Severe
pericardial effusion,
Severe anemia,
increased Intracranial
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PERSONAL DRUGS
cardiac oxygen demand,
decreased preload,
reduced afterload,
dilates coronary arteries,
and improves collateral
flow (Clinical
Pharmacology, 2013)
ventricular infarction,
and tolerance (Lexicomp, 2013).
Substrate CYP3A4
(major) (Lexi-comp,
2013).
Pharmacokinetics:
Absorption: 50%
through mucous
membranes in GI tract
Metabolism: Extensive
hepatic via liver
reductase enzyme.
Extensive first pass
effect. Nonhepatic
metabolism via red
blood cells and vascular
walls.
Excretion: urine and
feces (Lexi-comp,
2013).
pressure,
Hypotension,
Extreme Bradycardia,
Tachycardia in the
absence of heart
failure, and Right
ventricular infarction
(Lexi-comp, 2013).
Use caution:
Hypotension,
Bradycardia, Inferior
wall MI, Intracranial
pressure increase,
Hypertrophic
cardiomyopathy,
PDE-5 inhibitors,
Extended release:
Acute MI or Acute
HF, Sublingual: acute
anginal episode, and
Tolerance: Overcome
by short nitrate
absence (Lexi-comp,
2013).
IV. Effective Drug Classification: Beta Blocker Oral
Drug Name
Beta Blockers
Acebutolol
(Sectral®)
(Lexi-comp,
2013)
Efficacy
Onset: One to two
hours
Duration: 12-24
hours
Absorption: Oral
40%
Protein binding:
~26%%
Metabolism:
Extensive first pass
effect to equipotent
and cardioselective diacetolol
metabolite.
Bioavailability:
40%
Safety
Drug interactions:
Floctafenine, and
Methacholine
(Lexi-comp,
2013).
Increase
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents,
Suitability
-Teach diabetics
about possible
altered glucose.
-Taper over two
weeks when
discontinuing.
-Serum levels
slightly increased
with food intake.
-Check pulse
prior to taking
drug.
-Bradycardia may
be more severe in
elderly.
-Geriatrics may
Cost
Acebutolo
l HCL
oral:
200mg
(100):
$100.73
400mg
(100):
$133.97
Sectral ®
oral:
200mg
(100)L
$399.19
400mg
14
PERSONAL DRUGS
Half-life: Parent
drug: Three to four
hours; Metabolite:
Eight to 13 hours
Peak time: Two to
four hours
Excretion: primary
feces (50- 60%),
some urine (3040%) (Clinical
Pharmacology,
2013; Lexi-comp,
2013).
Aripiprazole,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Ergot derivatives,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
(Lexi-comp,
2013).
need reduced
dose.
-Do not stop drug
abruptly.
-Do not stop prior
to surgery.
-Avoid herbs with
hypertensive
properties and
hypotensive
properties
(Access
Medicine, 2013;
Lexi-comp,
2013).
(100)
$530.75
(Lexicomp,
2013)
-Teach diabetics
about possible
Atenolol
oral:
Decrease
Effect/Toxicity:
Beta2-agnosits and
Theophylline
derviatives (Lexicomp, 2013).
Avoid:
Beta2-angonist,
Dong quai,
Yohimbe,
Ginseng,
Bosutinib,
Floctafenine,
Methacholine,
Pomalidomide,
Topotecan, and
VinCRIStine
(Lexi-comp,
2013).
Beta Blockers
Onset: One to two
hours
Weak inhibitor of
CYP2D6
substrates (Lexicomp, 2013).
Drug interactions:
Floctafenine, and
15
PERSONAL DRUGS
Atenolol
(Tenormin®)
(Lexi-comp,
2013)
Peak effect: 2-4
hours
Duration: 12-24
hours
Absorption: Rapid
and incomplete
Distribution: Does
not cross blood
brain barrier
Protein binding: 616%
Metabolism:
Limited hepatic
Peak time: 2-4
hours
Excretion: Feces
(50%) and Urine
(40%) (Lexi-comp,
2013).
Methacholine
(Lexi-comp, 2013)
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Ergot derivatives,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab and
Sulfonylureas
(Lexi-comp,
2013).
altered glucose.
-Taper over two
weeks when
discontinuing.
-May decrease
concentration
when taken with
food.
-Check pulse
prior to taking
drug.
-Geriatrics may
need reduced
dose.
-Do not stop drug
abruptly.
-Do not stop prior
to surgery.
-Decreased HDL
levels.
-Avoid herbs with
hypertensive
properties and
hypotensive
properties
(Access
Medicine, 2013;
Lexi-comp,
2013).
25mg
(100):
$81.75
50mg
(100):
$84.60
100mg
(30):
$42.62
-Geriatrics may
bradycardia more
Betaxolol
HCL oral:
Tenormin
® oral:
25mg
(100):
$184.99
50mg
(30):
$41.06
100mg
(30):
$92.07
(Lexicomp,
2013)
Decreased
Effect/Toxicity:
Beta2-agnosits and
Theophylline
derviatives (Lexicomp, 2013)
Avoid:
Dong quai,
Ephedra,
Yohimbe, Ginseng
and Garlic (Lexicomp, 2013).
Beta Blockers
Onset: 1-1.5 hours
Absorption:
Drug interactions:
Floctafenine, and
16
PERSONAL DRUGS
Betaxolol
(Kerlone®,
Betoptic) (Lexicomp, 2013)
~100%
Metabolism:
Hepatic to multiple
metabolism
Protein Binding:
~50%
Bioavailability:
89%
Half-life: 14-22
hours, prolonged
with hepatic or
renal disease
Peak time:1.5-6
hours
Excretion: Urine
(Lexi-comp, 2013).
Methacholine
(Clinical
Pharmacology,
2013).
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents,
Aripiprazole,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Ergot derivatives,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
(Lexi-comp,
2013).
Decreased
Effect/Toxicity:
Beta2-agonists and
theophylline
derivatives (Lexicomp, 2013).
Avoid:
Herbs with
antihypertensive
effects (Lexicomp, 2013).
frequently.
-Taper down over
two week when
stopping drug.
-Do not stop for
surgery.
-May take with
meals.
-Diabetics should
watch glucose
closely.
-Do not abruptly
stop. Can cause
tachycardia and
hypertension.
-Do not stop for
surgery (Access
Medicine, 2013).
10mg
(100):
$123.00
20mg
(100):
$186.00
Kerlone®
oral:
10mg
(100):
$156.89
20mg
(100):
$235.25
(Lexicomp,
2013)
17
PERSONAL DRUGS
Beta Blockers
Bisoprolol
(Zebeta®)
(Lexi-comp,
2013)
Onset: 1-2 hours
Absorption: Rapid
and almost
complete
Distribution:
Widely; heart,
liver, lungs and
saliva; does cross
the blood-brain
barrier
Protein binding:
~30%
Metabolism:
Hepatic Extensive
first pass effect.
Bioavailability:
~80%
Half-life: 9-36
hours depending
on renal and liver
function
Peak time: 2-4
hours
Excretion: Urine
(50% unchanged
drug), and feces
(2%) (Lexi-comp,
2013).
Increases
metabolism of
CYP1A2 (major)
and CYP2D6
(minor) substrates.
Inhibits CYP2D6
weak affect (Lexicomp, 2013).
Drug interactions:
Floctafenine,
Conivaptan, and
Methacholine
(Lexi-comp, 2013)
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensive,
Antipsychotic
agents,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Ergot derivatives,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
(Lexi-comp,
2013).
Drug may
decrease:
Beta2-agnosits and
-Treatment for
anaphylaxis may
be ineffective or
have undesirable
effects.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Can be given
without regard to
meals.
-Watch glucose in
diabetic patients.
-Teach patients to
monitor
orthostatic
hypotension
(Access
Medicine, 2013).
Bisoprolol
Fumarate
oral: 5mg
(30):
$36.59
10mg
(30):
$36.59
Zebeta®
oral: 5mg
(30):
$117.78
10mg
(30):
$144.60
(Lexicomp,
2013)
18
PERSONAL DRUGS
Theophylline
derviatives (Lexicomp, 2013).
Avoid:
Herbs with
antihypertensive
properties (Lexicomp, 2013).
Beta Blockers
Carvedilol
(Coreg, Coreg
CR) (Lexicomp, 2013)
Onset: 1-2 hours
Peak: ~1-2 hours
Absorption: Rapid
and extensive
Protein binding:
>98 to albumin
Metabolism:
Extensively
hepatic via
CYP2C9, 2D6,
3A4, and 2C19 in
to three different
metabolites; First
pass effect; Plasma
concentration in
geriatrics and
cirrhotic patient
Bioavailability:
Immediate release:
25-35%; Extended
release: 85%
Half-life: 7-10
hours depending
on renal and liver
function
Peak time: 5 hours
Excretion:
Primarily feces
(Lexi-comp, 2013).
Increases
metabolism of
substrate CYP2D6
(minor) and
CYP3A4 (major)
(Lexi-comp,
2013).
Drug interactions:
Beta2-Agonists,
Bosutinib,
Floctafenine,
Methacholine,
pomalidomide,
topotecan, and
vincristine (Lexicomp, 2013).
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents, bosutinib,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
cholchine,
cyclosporine,
daigatran,
etexilate, digoxin,
-given with food
to prevent
orthostatic
hypotension.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Can be given
without regard to
meals.
-Watch glucose in
diabetic patients.
-Teach patients to
monitor
orthostatic
hypotension.
-Assess blood
pressure and
pulse rate before
giving (Access
Medicine, 2013).
Coreg
CR® oral:
10mg
(30):
$175.36
20mg
(30):
$174.76
40mg
(30):
$175.36
80mg
(30):
$174.76
Carvedilol
oral:
3.125mg
(100):
$213.40
6.25mg
(100):
$213.40
12.5mg
(100):
$213.40
25mg
(100):
$213.40
19
PERSONAL DRUGS
Ergot derivatives,
everolimus,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine, pglycoprotein/ABC
B1 substrates,
pomalidamide,
prucalapride,
RiTuximab,
rivaroxaban,
Sulfonylureas,
topotencan, and
vincristine (Lexicomp, 2013).
Drug may
decrease:
Beta2-agnosits and
Theophylline
derviatives (Lexicomp, 2013).
Avoid:
Herbs with
antihypertensive
properties or
hypotensive
properties (Lexi
comp, 2013).
Increases
metabolism of
substrate CYP1A2
(minor), CYP2C9
(minor), CYP2D6
(major), CYP2E1
(minor), CYP3A4
(minor), and Pglycoprotein.
Inhibits
metabolism of P-
Coreg®
oral:
3.125mg
930):
$96.21
6.25mg
(30):
$89.71
12.5mg
(30):
$91.75
25mg
(30)L
$89.11
(Lexicomp,
2013)
20
PERSONAL DRUGS
Beta Blockers
Labetalol
(Trandate®)
(Lexi-comp,
2013)
Onset: 20 minutes2 hours
Peak: 1-4 hours
Absorption:
Complete
Distribution: Can
cross the bloodbrain barrier
Protein binding:
50%
Metabolism:
Hepatic primarily
via glucuronide
conjugation;
extensive first pass
effect
Bioavailability:
25%; increased in
elderly, hepatic
impairment, and
cimetidine use
Half-life: 6-8 hours
Peak time: 1-2
hours
Excretion: Urine
(Lexi-comp, 2013).
glycoprotein.
(Lexi-comp,
2013).
Drug interactions:
Beta2-agonists,
Floctafenine, and
Methacholine
(Lexi-comp,
2013).
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Ergot derivatives,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
(Lexi-comp,
2013).
Drug may
decrease:
Beta2-agnosits and
Theophylline
derviatives (Lexicomp, 2013).
Avoid:
-Treatment for
anaphylaxis may
be ineffective or
have undesirable
effects.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Serum levels
increased with
food intake.
-Watch glucose in
diabetic patients.
-Teach patients to
monitor
orthostatic
hypotension.
-Not removed by
dialysis.
-Bradycardia
more common in
elderly (Access,
Medicine, 2013).
Labetalol
HCL oral:
100mg
(100):
$51.31
200mg
(100):
$72.79
300mg
(100):
$96.83
Trandate®
oral:
100mg
(100):
$64.87
200mg
(100):
$126.14
300mg
(100):
$127.78
(Lexicomp,
2013).
21
PERSONAL DRUGS
Beta Blockers
Metoprolol
(Lopressor,
Toprol-XL)
(Lexi-comp,
2013)
Onset: 1-2 hours
Duration: Variable
depending on dose
Absorption: Rapid
and complete
Protein binding:
~10% to albumin
Metabolism:
Extensively
hepatic via
CYP2D6;
Extensive first pass
effect.
Bioavailability:
~50%
Half-life: 3-4 hours
Excretion: Urine
(Lexi-comp, 2013).
Herbs with
antihypertensive
properties (Lexicomp, 2013).
Drug interactions:
Floctafenine, and
Methacholine
(Lexi-comp,
2013).
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents,
aripiprazole,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Ergot derivatives,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
Lexi-comp, 2013).
-Treatment for
anaphylaxis may
be ineffective or
have undesirable
effects.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Food can
increased
absorption. Give
immediate release
with food.
Regular release
can be given
without regard to
meals.
-Watch glucose in
diabetic patients
-Teach patients to
monitor
orthostatic
hypotension
-May need to
dose down in
elderly due to
bradycardia
(Access
Medicine, 2013).
Metoprolo
l
Succinate
ER oral:
25mg
(100):
$105.38
50mg
(100):
$105.38
100mg
(100):
$158.35
200mg
(100):
$251.95
Toprol
XL® oral:
25mg
(100):
$143.46
50mg
(30):
$44.39
100mg
(30):
$66.13
200mg
(30):
$97.96
Drug may
decrease:
Beta2-agnosits and
Theophylline
derviatives (Lexicomp, 2013).
Lopressor
® oral:
50mg
(30):
$43.02
100mg
(30):
$63.29
Avoid:
Metoprolo
22
PERSONAL DRUGS
Herbs with
antihypertensive
properties (Lexicomp, 2013).
Beta Blockers
Nadolol
(Corgard®)
(Lexi-comp,
2013).
Duration: 17-24
hour
Absorption: 3040%
Protein binding:
30%
Metabolism: Not
metabolized
Half-life: 10-24
hours depending
on renal and liver
function
Peak time: 2-4
hours
Excretion: Urine
(unchanged drug)
(Lexi-comp, 2013).
Increases
metabolism of
substrate
CYP2C19 (minor)
and CYP2D6
(major). Inhibits
metabolism of
CYP2D6 (weak)
(Lexi-comp,
2013).
Drug interactions:
Beta2-agonists
Floctafenine, and
Methacholine
(Lexi-comp,
2013).
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Ergot derivatives,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
(Lexi-comp,
l Tartrate
oral:
25mg
(100):
$24.25
50mg
(100):
$55.50
100mg
(100):
$80.10
(Lexicomp,
2013).
-Treatment for
anaphylaxis may
be ineffective or
have undesirable
effects.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Bradycardia may
be seen more in
elderly.
-Can be given
without regard to
meals.
-Watch glucose in
diabetic patients.
-Teach patients to
monitor
orthostatic
hypotension
(Access
Medicine, 2013).
Corgard®
oral:
20mg
(100):
$384.04
40mg
(30):
$78.48
80mg
(100):
$617.29
Nadolol
oral:
20mg
(100):
$92.49
40mg
(100):
$108.15
80mg
(100):
$142.30
(Lexicomp,
2013).
23
PERSONAL DRUGS
2013).
Drug may
decrease:
Beta2-agnosits and
Theophylline
derviatives (Lexicomp, 2013).
Avoid:
Herbs with
antihypertensive
properties (Lexicomp, 2013).
Beta Blockers
Nebivolol
(Bystolic®)
(Lexi-comp,
2013)
Absorption: Rapid
Protein binding:
~98% mostly to
albumin
Metabolism:
Hepatic via
glucuronidation
and CYP2D6;
Extensive first pass
effect.
Bioavailability:
~12%
Half-life: 10-12
hours
Peak time: 1.5-4
hours
Excretion: Urine
(38%), and feces
(44%) (Lexi-comp,
2013).
Increases
metabolism of
substrate Pglycoprotein
(Lexi-comp,
2013).
Drug interactions:
Floctafenine, and
Methacholine
(Lexi-comp,
2013).
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Ergot derivatives,
Fingolimod,
Hypotensive
agents, Insulin,
-Treatment for
anaphylaxis may
be ineffective or
have undesirable
effects.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Can be given
without regard to
meals.
-Watch glucose in
diabetic patients.
-Teach patients to
monitor
orthostatic
hypotension.
-Watch
bradycardia in
geriatrics (Access
Medicine, 2013).
Bystolic®
oral:
2.5mg
(100):
$267.44
5mg
(100):
$267.44
10mg
(100):
$267.44
20mg
(30):
$81.49
(Lexicomp,
2013).
24
PERSONAL DRUGS
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
(Lexi-comp,
2013).
Drug may
decrease:
Beta2-agnosits and
Theophylline
derviatives (Lexicomp, 2013).
Avoid:
Herbs with
antihypertensive
properties (Lexicomp, 2013).
Beta Blockers
Penbutolol
(Levatol®)
(Lexi-comp,
2013)
Onset: 1.3-3 hours
Duration: >20
hours
Absorption:
~100%
Protein binding:
80-98%
Metabolism:
Hepatic –oxidation
and conjugation
Bioavailability:
~100%
Half-life: 5 hours
Peak time: 2-3
hours
Excretion: Urine
(Lexi-comp, 2013).
Increases
metabolism of
substrate CYP2D6
(minor) (Lexicomp, 2013).
Drug interactions:
Beta2-agonists,
Floctafenine, and
Methacholine
(Lexi-comp,
2013).
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents,
Bupivacaine,
Cardiac
-Treatment for
anaphylaxis may
be ineffective or
have undesirable
effects.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Can be given
without regard to
meals.
-Teach patients to
monitor
orthostatic
hypotension
(Access
Medicine, 2013).
Levatol®
oral:
20mg
(100):
$406.80
(Lexicomp,
2013).
25
PERSONAL DRUGS
glycosides,
Cholinergic
agonists,
Ergot derivatives,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
(Lexi-comp,
2013).
Beta Blockers
Pindolol
(Visken®)
(Lexi-comp,
2013)
Absorption: Rapid;
50-95%
Protein binding:
40%
Metabolism:
Hepatic 60-65% to
conjugates
Half-life: 3-4 hours
Peak time: ~1hour
Excretion: Urine
(35-40%
unchanged drug),
and feces (6-9%)
(Lexi-comp, 2013).
Drug may
decrease:
Beta2-agnosits and
Theophylline
derviatives.
(Lexi-comp,
2013).
Drug interactions:
Bet2-agonists,
Floctafenine, and
Methacholine
(Lexi-comp,
2013).
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents, aripirazole,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Ergot derivatives,
-Treatment for
anaphylaxis may
be ineffective or
have undesirable
effects.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Can be given
without regard to
meals.
-Watch glucose in
diabetic patients.
-Teach patients to
monitor
orthostatic
hypotension.
-Half-life is ten
time longer in
cirrhosis patients
(Access
Pindolol
oral:
5mg
(100):
$103.75
10mg
(100):
$141.36
(Lexicomp,
2013).
26
PERSONAL DRUGS
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
(Lexi-comp,
2013).
Medicine, 2013).
Drug may
decrease:
Beta2-agnosits and
Theophylline
derviatives (Lexicomp, 2013).
Avoid:
Herbs with
antihypertensive
properties (Lexicomp, 2013).
Beta Blockers
Propranolol
(Inderal®,
Inderal LA®,
InnoPran XL®)
(Lexi-comp,
2013)
Onset: 1-2 hours
Duration:6-12
hours Absorption:
Rapid and
complete
Protein binding:
~90%
Metabolism:
Hepatic via
CYP2D6 and
CYP1A2 to 4hydroxypropranolo
l and inactive
Increases
metabolism of
substrate CYP2D6
(minor). Inhibits
metabolism of
CYP2D6 (weak)
(Lexi-comp,
2013).
Drug interactions:
Beta2-agonists,
bosutinib,
Floctafenine,
Methacholine,
pomalidomide,
topotecan, and
vincristine (Lexicomp, 2013).
Increased
Effect/Toxicity:
Alpha/Beta-
-Treatment for
anaphylaxis may
be ineffective or
have undesirable
effects.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Teach patients to
monitor
orthostatic
Inderal
LA® oral:
60mg
(30):
$56.35
80 mg
(30):
$65.39
120 mg
(100):
$247.03
160 mg
(100):
27
PERSONAL DRUGS
compounds;
Extensive first pass
effect.
Bioavailability:
~25%
Half-life: 3-6 hours
Peak time: 1-4
hours
Excretion: Urine
(Lexicomp, 2013).
agonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents,
aripiprazole,
bosutinib,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Dabigatran,
etexilate, Ergot
derivatives,
everolimus,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine, pglycoprotein/ABC
B1 substrates,
pomalidomide,
prucalopride,
RiTuximab,
rizatriptan,
Sulfonylureas,
topotecan,
vincristine, and
zolmitriptan (Lexicomp, 2013).
Drug may
decrease:
Beta2-agnosits,
lacidipina, and
Theophylline
derviatives (Lexicomp, 2013).
Avoid:
hypotension.
-Not dialyzable.
-Bradycardia seen
in hepatic
impairment
patients.
-Smoking
decreases serum
plasma levels.
-Alcohol can
increase or
decrease plasma
levels.
-Give medication
on empty stomach
(Access
Medicine, 2013).
$322.78
InnoPran
XL® oral:
80 mg
(30):
$80.00
120 mg
(30):
$80.00
Propranol
ol HCL
ER oral:
60 mg
(100):
$132.59
80 mg
(100):
$154.89
120 mg
(100):
$192.09
160 mg
(100):
$251.47
Propranol
ol HCL
oral:
10mg
(100):
$33.53
20mg
(100):
$36.30
40mg
(100):
$60.07
60mg
(100):
$121.83
80mg
(100):
$63.39
(Lexi-
28
PERSONAL DRUGS
Herbs with
antihypertensive
properties (Lexicomp, 2013).
Beta Blockers
Sotalol
(Betapace®,
Sorine®) (Lexicomp, 2013).
Increases
metabolism of
substrate Cyp1A2
(major), CYP2C19
(minor) CYP2D6
(major) and
CYP3A4 (major).
Inhibits
metabolism of
CYP1A2 (weak)
(Lexi-comp,
2013).
Onset: 1-2 hours
Drug interactions:
Duration:8-16
Beta2-agonists,
hours
Floctafenine,
Absorption:
floctafenine, QT
Decreased 20-30% prolonging agents,
when given with
ivabradine,
meals
Methacholine,
Protein binding:
mifepristone, and
none
propafenone
Metabolism: none
(Lexi-comp,
Bioavailability: 90- 2013).
100%
Half-life: 12 hours Increased
Peak time: 2.5-4
Effect/Toxicity:
hours
Alpha/BetaExcretion: Urine
agonists, Alpha1(Lexi-comp, 2013). blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents,
Bupivacaine,
Cardiac
glycosides,
Cholinergic
agonists,
Ergot derivatives,
Fingolimod, QT
comp,
2013).
-Treatment for
anaphylaxis may
be ineffective or
have undesirable
effects.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Do not give with
meals.
-Watch glucose in
diabetic patients.
-Teach patients to
monitor
orthostatic
hypotension.
-Dialysis removes
drug. Give dose
post dialysis.
-Closely monitor
QT intervals.
-Do not give to
elderly (BEERS
criteria) (Lexicomp, 2013)
Betapace
AF® oral:
80mg
(60):
$259.50
120mg
(60):
$346.25
160mg
(60):
$433.07
Betapace
® oral:
80mg
(100):
$473.45
120mg
(100):
$631.76
160mg
(100):
$789.65
Sorine®
oral:
80mg
(100):
$260.89
29
PERSONAL DRUGS
prolonging agents,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
(Lexi-comp,
2013).
120mg
(100):
$346.39
160mg
(100):
$430.98
240mg
(100):
$559.97
Drug may
decrease:
Beta2-agnosits and
Theophylline
derviatives (Lexicomp, 2013).
Avoid:
Ephedra (Lexicomp, 2013).
Beta Blockers
Timolol
(Betimol,
Blocadren,
Istalol,
Timoptic) (Lexicomp, 2013)
Onset: 1545minutes
Duration:~4 hours
Absorption: Rapid
and almost
complete
Protein binding:
60%
Metabolism:
Hepatic via
CYP2D6;
Extensive first pass
effect.
Bioavailability:
50%
Half-life: 2-2.7
hours
Peak time: 1-2
hours
Drug interactions:
Beta2-agonists,
Floctafenine, and
Methacholine
(Lexi-comp, 2013)
Increased
Effect/Toxicity:
Alpha/Betaagonists, Alpha1blockers, Alpha2agnosist,
Amifostine,
Antihypertensives,
Antipsychotic
agents,
Bupivacaine,
Cardiac
glycosides,
-Treatment for
anaphylaxis may
be ineffective or
have undesirable
effects.
-Do not abruptly
stop.
-Do not stop prior
to non-cardiac
surgery.
-Can be given
without regard to
meals (Access
Medicine, 2013).
Sotalol
HCL oral:
80mg
(100):
$234.72
120mg
(100):
$322.35
160mg
(100):
$403.00
240mg
(100):
$55.59
(Lexicomp,
2013).
Timolol
Maleate
oral:
5mg
(100):
$63.66
10mg
(100):
$78.75
20mg
(100):
$145.30
(Lexicomp,
2013).
30
PERSONAL DRUGS
Excretion: Urine
Cholinergic
(Lexi-comp, 2013). agonists,
Ergot derivatives,
Fingolimod,
Hypotensive
agents, Insulin,
Lidocaine,
Mepivacaine,
Methacholine,
Midodrine,
RiTuximab, and
Sulfonylureas
(Lexi-comp,
2013).
Drug may
decrease:
Beta2-agnosits and
Theophylline
derviatives (Lexicomp, 2013).
Increases
metabolism of
substrate CYP2D6
(major).inhibits
metabolism of
CYP2D6 (weak)
(Lexi-comp,
2013).
V. Drug of Choice: Carvedilol
The recommended therapy for treating HTN and controlling HF in hemodialysis patient
is the use of beta blockers (Abbott, Agodoa, Bakris, Taylor, & Trespalacios, 2004). There are
several different beta blockers for use of HF but only Carvedilol was mentioned by name by the
American Heart Association (AHA, 2008). Carvedilol is unique compared to the other beta
blockers because it is beta blocker and an alpha blocker. This drug has a slight inverse agonist
action and has a reduced negative chronotropic and inotropic effect. Carvedilol has shown to
PERSONAL DRUGS
31
improve EF, reduce HF symptoms, increase stroke volume, stroke work, cardiac output,
improved insulin sensitivity and adrenergic activity. The overall effect of Carvedilol is a
reduction in mortality from all causes (DiNicolantonio, Fares, Lavie, Menezes, & O’Keefe,
2012).
An Advanced Nurse Practitioner (APN) with a current certificate to prescribe (CTP) can
prescribe Carvedilol according to the Ohio Board of Nursing Formulary (Ohio Board of Nursing,
2013). When giving a beta blocker, such as Carvedilol, close initial monitoring and follow up
are necessary. While guidelines encourage an ACE inhibitor and a beta blocker for HF patients,
those with severe renal impairment are only given beta blockers (Abbott et al., 2004). Carvedilol
is given as 3.125 mg twice daily for two weeks and then increased to 6.25 mg twice daily if
tolerated. Every two weeks the dose should be double as tolerated until the highest dose with the
maximal benefit is reached. For this patient the recommended maximum dose is 25 mg twice
daily. This medication should be given with food to help reduce the risk of hypotension. Close
monitoring of the patients heart rate and blood pressure are needed to find optimum therapy
dosage until goal is achieved. Blood test including renal studies, BUN, and liver function tests
should be performed before each dose increase and then yearly when optimum dose is found.
Carvedilol should be taken every day for the rest of the patient’s life unless hospice or change in
diagnosis is made. This drug has a slight risk for increasing renal impairment. Carvedilol is
metabolized in the liver and should not be given to those with liver impairment. This drug costs
from $14.99 to $25.99 for 30 tablets depending on strength (Access Medicine, 2013).
32
PERSONAL DRUGS
Second Diagnosis: Acute Clavicle Fracture
A 23 year old Caucasian male presents to the emergency department complaining of right
clavicle pain after falling off a stage. He states he was moving the stage set when he backed up
into the curtain and fell off the stage catching himself with his right arm. He is in good health.
He is a college student at the local community college and is majoring in stage manager
assistant. After history and physical assessment and X-rays of the right shoulder, he is diagnosed
with acute right clavicle fracture non-displaced.
I. Definition of Diagnosis
Acute clavicle fracture is one of the most common fractures seen in young active adults,
accounting for 2.6% to 4% of all total fractures (Andriolo, Belloti, Faloppa, Gomes dos Santos,
& Lenza, 2010). The Allman’s method classifies clavicle fractures into three sub groups which
are: Group I- mid shaft fractures, Group II- Lateral fractures, and Group III- medial fractures.
Group I (midshaft factures) account for up to 81% of all clavicle fractures and are usually
displaced resulting in the need for surgery (Farsetti, Gumina, Postacchini, & Postacchini, 2010).
Clavicle fractures results from a fall with an out stretched hand or from direct trauma. For nondisplaced factures conservative treatment is best (Andriolo et al., 2010).
II. Therapeutic Objectives
The choice of treatment for a non-displaced clavicle fracture is placement of the arm in a
sling or placing the back in a figure eight bandage. One or both of these treatments can be used
to achieve stabilization of the fracture. It is recommended that the patient be immobilized for
two to six weeks for adequate healing. Some patients may need arm stretching exercises after,
however, this incident is low (Adriolol et al., 2010).
33
PERSONAL DRUGS
The second focused treatment should be pain control. Only 28-85% of all patients with a
facture receive analgesic prescription and of that only 17-64% received an opioid. This statistic
leaves a large number of patients who have an acute painful injury without or with poorly
controlled pain management (Castelluccio et al., 2010). Patients without proper pain control and
immobilization are generally more dissatisfied with their care (Farsetti, Gumina, Postacchini, &
Postacchini, 2010).
III. Inventory of Effective Drug Groups Oral
Drug
Non-Steroidal
AntiInflammatory
Drugs/
Acetic Acid
Derivatives
Indomethacin,
Tolmetin,
Sulindac,
Etodolac,
Ketorolac,
Diclofenac
(Valtaren®),
Nabumetone
(Lexi-comp,
2013)
Efficacy
Pharmacodynamics:
Inhibits
cyclooxygenase 1
and 2 enzyme
causing decreased
prostaglandin
precursors. This
causes an
antipyretic,
analgesic, and antiinflammatory effect
(Clincial
Pharmacology,
2013).
Pharmacokinetics:
Absorption:
Immediate release
Metabolism: Hepatic
Excretion: Urine
(60-80%) and feces
(9-33%) (Lexicomp, 2013).
Safety
Side Effects:
Common:
Dyspepsia, stomach
ulcers, anemia, and GI
bleeding
Rare:
MI, heart failure, and
hypertension
Very Rare:
Kidney and liver
impairment (Lexicomp, 2013).
Monitor:
Pain response,
inflammation, weight,
edema, renal function,
confusion, GI effects,
CBC, Liver function,
and bruising (Access
Medicine, 2013).
Substrate: CYP1A2
(minor), CYP2B6
(minor), CYP2C19
(minor), CYP2C8
(minor), CYP2C9
(minor), CYP2D6
(minor). Inhibits:
CYP1A2 (weak)
Suitability
Contraindications:
Hypersensitivity to
NSAIDs or any
component,
perioperative setting for
CABG, advanced renal
impairment, and history
of proctitis or rectal
bleeding (Lexi-comp,
2013).
Use Caution:
Anaphylactoid
reactions,
cardiovascular events,
CNS effects, GI events,
hematologic effects,
hyperkalemia, skin
reactions, visual
impairments, asthma,
CABG, depression,
hepatic impairment,
hypertension,
parkinsonism,
photosensitivity
reaction, and renal
impairment (Lexicomp, 2013).
34
PERSONAL DRUGS
Non-Steroidal
AntiInflammatory
Drugs/
Cox-2 Selective
Celecoxib
(Celebrex) (Lexicomp, 2013)
Pharmacodynamics:
Inhibits
prostaglandin
synthesis by
decreasing enzyme
cyclooxygenase-2.
This causes an
antipyretic,
analgesic, and antiinflammatory effect
(Clinical
Pharmacology,
2013; Lexicomp,
2013).
CYP2C19 (weak),
CYP2E1 (weak),
CYP3A4 (weak),
CYP2C9 (weak),
UGT1A6 (Lexi-comp,
2013).
Side Effects:
Common:
GI upset, diarrhea, gas,
dizziness, nervousness,
headache, runny nose,
sore throat, and skin
rash
Rare:
Chest pain, weakness,
SOB, vision problems,
melena, coughing up
blood, weight gain,
oliguria, nausea,
stomach pain, anorexia,
jaundice, sever skin
reaction, and
ecchymosis (Lexicomp, 2013).
Contraindications:
Advanced renal
disease,
hypersensitivity to
celecoxib,
sulfonamides, aspirin,
NSAIDs, or any
component, and
perioperative CABG
surgery (Lexi-comp,
2013)
Use Caution:
Anaphylactiod
reactions,
Pharmacokinetics:
cardiovascular events,
Absorption: Not
GI events, hematologic
reported
events, skin reactions,
Metabolism: Hepatic
asthma, CABG,
via CYP2C9
Monitor:
corticosteroidExcretion: Feces
CBC, occult blood loss, dependent disease,
(60%), urine (30%)
liver function, renal
cytochrome P450
(Lexi-comp, 2013).
function, pain
isoenzyme 2C9
response, blood
deficiency, hepatic
pressure, weight gain,
impairment, and renal
bruising, and GI effects impairment (Lexi(Clinical
comp, 2013).
Pharmacology, 2013).
Non-Steroidal
AntiInflammatory
Drugs/
Enolic Acid
Pharmacodynamics:
Inhibits
cyclooxygenase 1
and 2 enzymes
which cause
Substrate: CYP 2C9
(major), CYP3A4
(monitor). Inhibits:
CYP2C8 (moderate),
CYP2D6 (moderate)
(Lexi-comp, 2013).
Side Effects:
Common:
GI upset, diarrhea,
bloating, flatulence,
dizziness, nervousness,
Contraindications:
Severe renal
impairment, severe
hepatic impairment,
hypersensitivity or
35
PERSONAL DRUGS
(Oxicam)
Derivatives
Piroxicam,
Meloxicam
(Mobic®) (Lexicomp, 2013).
Non-Steroidal
AntiInflammatory
Drugs/
Fenamic Acid
Derivatives
(Fenamates)
Mefenamic acid
(Ponstel®),
Meclofenamate
(Lexi-comp,
2013)
decreased
prostaglandin
precursors. This
causes antipyretic,
analgesic, and antiinflammatory
response (Lexicomp, 2013).
headache, rhinitis, sore
throat, and skin rash
Rare:
Chest pain, weakness,
headache, pruritus,
severe rash, anorexia,
bleeding, constipation,
confusion, anxiety,
depression,
Pharmacokinetics:
somnolence,
Protein Binding:
perforation, vomiting,
99%
anemia, increased
Metabolism: Heptaic bleeding time, tinnitus,
via CYP2C9
micturition, flu-like
Half-life: 50 hours
symptoms, falls, and
Peak Time: Three to angina (Clinical
five hours
Pharmacology, 2013).
Excretion: Urine and
feces (Lexi-comp,
Monitor:
2013).
Periodic: Occult blood
loss, CBC, BMP, liver
function tests, and eye
exams (Access
Medicine, 2013).
Pharmacodynamics:
Inhibits
cyclooxygenase 1
and 2 enzymes
which cause
decreased
prostaglandin
precursors. This
causes antipyretic,
analgesic, and antiinflammatory
response (Clinical
Pharmacology,
2013; Lexi-comp,
2013).
Substrate: CYP3A4
(minor), CYP2C9
(major). Inhibits:
CYP2C9 (weak) (Lexicomp, 2013).
Side Effects:
Common:
Headache, dizziness,
itching, abdominal
cramps, heartburn,
nausea, vomiting,
diarrhea, constipation,
dyspepsia, gastritis,
and bleeding
Rare:
Nervousness, itching,
fluid retention, LFTs
increase, and tinnitus
(Lexi-comp, 2013)
Monitor:
asthma reaction to
piroxicam, aspirin,
NSAIDs, or any
component,
perioperative CABG
surgery, and severe
heart failure (Access
Medicine, 2013).
Use Caution:
Anaphylactiod
reactions,
cardiovascular events,
CNS events, GI events,
hematologic events,
skin reactions,
hyperkalemia, serum
sickness, asthma,
CABG, hepatic
impairment,
hypertension, and renal
impairment (Lexicomp, 2013).
Contraindications:
Hypersensitivity to
mefenamic acid,
aspirin, NSAIDs, or
other components,
perioperative CABG
surgery, GI ulcerations,
and renal disease (Lexicomp, 2013).
Use Caution:
Anaphylactoid
reactions,
cardiovascular effects,
CNS effects, GI events,
hematologic effects,
36
PERSONAL DRUGS
Non-Steroidal
AntiInflammatory
Drugs/
Propionic Acid
Derivatives
Ibuprofen
(Motrin®)
(Children’s
Motrin®),
Naproxen
(Aleve®,
Midol®),
Oxaprozin
(Daypro®),
Fenoprofen
(Nalfon®),
Ketoprofen,
Nuprin,
Flurbiprofen
(Lexi-comp,
2013)
Non-Steroidal
AntiInflammatory
Drugs/
Pharmacokinetics:
Absorption: Rapid
Metabolism: Hepatic
via CYP2C9
Excretion: Urine
(52-70%) and feces
(20-30%) (Lexicomp, 2013).
Pharmacodynamics:
Inhibits
cyclooxygenase 1
and 2 enzymes
which cause
decreased
prostaglandin
precursors. This
causes antipyretic,
analgesic, and antiinflammatory
response (Lexicomp, 2013).
Pharmacokinetics:
Absorption: Rapid
Metabolism: hepatic
via oxidation
Excretion: Urine,
some feces (Lexicomp, 2013).
Pharmacodynamics:
Irreversibly inhibits
cyclooxygenase 1
and 2 enzymes by
Renal function and
dehydration (Lexicomp, 2013).
Substrate: CYP2C9
(minor). Inhibits:
CYP2C9 (weak) (Lexicomp, 2013).
Side Effects:
Common:
dizziness, headache,
rash, itching, heartburn,
nausea, abdominal
pain, anorexia, and
constipation
Rare:
Edema, nervousness,
fluid retention,
dyspepsia, vomiting,
weakness, tremor, and
tinnitus (Access
Medicine, 2013).
hyperkalemia, skin
reactions, asthma,
hepatic impairment,
hypertension, and renal
impairment (Lexicomp, 2013).
Contraindications:
Severe hepatic
impairment, anuria,
oliguria,
hypersensitivity to
NAIDS or any
component, asthma,
urticarial, allergic type
response, and
perioperative CABG
surgery (Lexi-comp,
2013)
Monitor:
CBC, chemistry
profile, occult blood
loss, liver function
tests, pain response,
inflammation, weight
gain, edema, bleeding,
GI effects, confusion,
blood pressure, urine
output, and eye exams
(Access Medicine,
2013).
Use Caution:
Anaphylactoid reaction,
cardiovascular events,
CNS effects, GI events,
hematologic effects,
hyperkalemia,
ophthalmic events, skin
reactions, aseptic
meningitis, asthma,
CABG surgery, hepatic
impairment,
hypertension, and renal
impairment (Lexicomp, 2013).
Substrate: CYP1A2
(minor), CYP2C19
(minor), CYP2C9
(minor). Inhibits
CYP2C9 (weak) (Lexicomp, 2013).
Side Effects:
Common:
Diarrhea, headache,
abdominal pain,
Contraindications:
Hypersensitivity to
salicylate, NSAIDs, or
any component,
37
PERSONAL DRUGS
Salicylates
Acetylsalicylic
acid (Aspirin®),
Choline
Magnesium
Salicylate,
Sulfasalazine,
Diflunisal,
Salsalate (Lexicomp, 2013)
acetylation causing
decreased
prostaglandin
precursors
(thromboxane A2).
This causes an
antipyretic,
analgesic, and antiinflammatory effect
(Lexi-comp, 2013).
Pharmacokinetics:
Absorption: Rapid,
stomach and small
intestines
Metabolism:
hydrolyzed in GI
mucosa, red blood
cells, synovial fluid,
and blood. Hepatic
conjunction.
Excretion: Urine
(Lexi-comp, 2013).
Opioids/
Esters of
Morphine
Dihydrocodeine
(Synalgos®)
(Lexi-comp,
2013)
nausea, and rhinitis
Rare:
Hypotension,
tachycardia,
dysrhythmias, edema,
rash, angioedema,
urticarial, acidosis,
gastric erosions,
bleeding, hepatitis,
weakness, asthma,
bronchospasm, and
Reye’s syndrome
(Access Medicine,
2013).
Monitor:
Bleeding disorders,
dehydration, GI
diseases, asthma, renal
function, and hepatic
function (Lexi-comp,
2013).
Substrate: CYP2C9
(minor) (Lexi-comp,
2013).
Pharmacodynamics: Side Effects:
Bind to opiate
Common:
receptors in CNS,
Lightheadedness,
inhibiting ascending dizziness, drowsiness,
pain pathways
sedation, puritus, skin
altering pain
reactions, nausea,
response. Suppresses vomiting, constipation,
cough by direct
hypotension, and
action in medulla
respiratory depression.
(Lexi-comp, 2013).
Rare:
Palpitations,
Pharmacokinetics:
bradycardia, increased
Absorption: Not
ICP, biliary tract
reported
spasm, urinary tract
Metabolism: Hepatic spasm, and miosis
Excretion: Urine
(Lexi-comp, 2013).
unchanged
(Lexi-comp, 2013).
Monitor:
Respiratory and CNS
effects (Lexi-comp,
asthma, rhinitis, nasal
polyps, bleeding
disorders, and children
less than 26 years of
age (Lexi-comp, 2013)
Use Caution:
Salicylate sensitivity,
tinnitus, upper GI
events, bleeding
disorders, dehydration,
ethanol use, hepatic
impairment, renal
impairment, alteplase,
NSAIDs, elderly,
children, and surgery
patients (Lexi-comp,
2013).
Contraindications:
Hypersensitivity to
dihsrdocodeine or any
component, and
pregnancy (Access
Medicine, 2013).
Use Caution:
CNS depression,
phenanthrene
hypersensitivity,
salicylate sensitivity,
tinnitus, abdominal
conditions, adrenal
insufficiency, biliary
tract impairment,
bleeding disorders,
CNS depression/ coma,
drug abuse, ethanol use,
GI diseases, head
38
PERSONAL DRUGS
2013).
Pharmacodynamics:
Opioids/
Opioid Alkaloids Bind to opiate
receptors in CNS,
Codeine ,
inhibiting ascending
Morphine
pain pathways
(Kadian®, MS
altering pain
Contin®) (Lexiresponse. Suppresses
comp, 2013)
cough by direct
action in medulla
(Lexi-comp, 2013).
Side Effects:
Common:
Weight loss,
constipation, diarrhea,
nausea, vomiting,
abdominal pain,
anorexia, flushing,
headache, dizziness
confusion, insomnia,
and abnormal dreams
Rare:
Pharmacokinetics:
Apnea, bradycardia,
Absorption: GI 50% stiffness, seizure,
Metabolism: Hepatic clammy skin,
via UGT2B7,
confusion, weakness,
UGT2B4,
SOB, tachycardia, and
CYP2D6,and
bleeding (Access
CYP3A4;
Medicine, 2013).
conjugated with
glucuronic acid
Monitor:
Excretion: Urine
Pain relief, respiratory
(90%) and feces
and mental status,
(Lexi-comp, 2013).
blood pressure, and
heart rate (Clinical
Pharmacology, 2013).
Substrate: CYP2D6
(major) (Lexi-comp,
2013).
Opioids/
Semisynthetic
Opioids:
Hydrocodone
(Lortab®,
Vicodin®,
Lorcet®),
Hydromorphone
Pharmacodynamics:
Blocks pain
reception in the
cerebral cortex by
binding to receptor
molecules in the
synapses preventing
pain impulses to
Side Effects:
Common;
Hypotension,
drowsiness, faint
feeling, dizziness,
weakness, and ill
feeling
Infrequent:
trauma, hepatic
impairment, prostatic
hyperplasia, renal
impairment, respiratory
diseases, and thyroid
dysfunction (Lexicomp, 2013).
Contraindications:
Hypersensitivity to
codeine or any
component, respiratory
depression,
acute/severe asthma,
hypercarbia, or
paralytic ileus (Lexicomp, 2013)
Use Caution:
CNS depression,
constipation,
hypotension,
phenanthrene
hypersensitivity,
respiratory depression,
abdominal conditions,
adrenal insufficiency,
biliary tract
impairment, CND
depression/coma, drug
abuse, GI obstruction,
head trauma, hepatic
impairment, obesity,
prostatic hyperplasia,
renal impairment,
respiratory disease,
seizure disorder, and
thyroid dysfunction
(Lexi-comp, 2013).
Contraindications:
Hypersensitivity to
semisynthetic opioids,
acetaminophen, or any
component, CNS
depression, GI
obstruction, and severe
respiratory depression
39
PERSONAL DRUGS
(Dilaudid®),
Oxycodone
(Oxycontin®,
Roxicodone®),
Oxymorphone
(Opana®) (Lexicomp, 2013)
higher centers in the
brain. Mu and Kapa
are two of the
receptor sites that
are bound (Lexicomp, 2013).
Pharmacokinetics:
Absorption: Not
reported
Metabolism:
Hepatic: Odemethyation via
CYP2D6 to
hydromorphone; Ndemethylation via
CYP3A4 to
norhydrocodone;
and 40% other nonCYP pathways; via
glucuronidation
Excretion: Urine
(Lexi-comp, 2013).
Opioids/
Synthetic
Opioids/
Anilidopiperidin
es
FentanylLozenge (Lexicomp, 2013)
Pharmacodynamics:
Increased pain
threshold, alters pain
reception, and
inhibits ascending
pain pathways by
blocking many
receptor cites (Lexicomp, 2013).
Bradycardia,
bronchospasm,
tachycardia, SOB,
confusion, vision
problems, dry mouth,
nervous ness, anxious,
and addiction
Rare:
Depression, tinnitus,
hypertension, hepatitis,
itching, hallucinations,
rash,
thrombocytopenia,
nightmares, and
insomnia (Lexi-comp,
2013)
Monitor:
Pain relief, respiratory
and mental status,
blood pressure, liver
disease, ethanol abuse,
falls, and withdrawal
(Access Medicine,
2013).
Substrates: CYP2D6
(minor), CYP3A4
(major) (Lexi-comp,
2013).
Side Effects:
Common:
Bradycardia, CNS
depression, confusion,
fatigue, headache,
sedation, constipation,
nausea, vomiting,
weakness, dyspnea,
and diaphoresis.
Rare:
Edema, xerstomia, and
miosis (Access
Medicine, 2013).
Pharmacokinetics:
Absorption: rapid
buccal, 50% saliva,
and slow GI
Metabolism: Hepatic Monitor:
via CYP3A4
Respiratory and
(Lexi-comp, 2013)
Use Caution:
CNS depression,
hepatotoxicity,
hypersensitivity/anaphy
lactic reactions,
constipation,
hypotension,
phenanthrene
hypersensitivity,
respiratory depression,
abdominal conditions,
adrenal insufficiency,
biliary tract
impairment, G6PD
deficiency, CYP3A4
inhibitors, CNS
depression/coma,
delirium tremens, drug
abuse, GI obstruction,
head trauma, hepatic
impairment, ethanol
use, obesity, prostatic
hyperplasia, psychosis,
renal impairment,
respiratory disease,
seizure disorder, and
thyroid dysfunction
(Lexi-comp, 2013).
Contraindications:
Severe renal or hepatic
impairment and
hypersensitivity to
fentanyl or any
component (Lexi-comp,
2013)
Use Caution:
CNS depression, opioid
agonist toxicities,
respiratory depression,
allergic rhinitis,
bradycardia, drug
abuse, head trauma,
hepatic impairment,
40
PERSONAL DRUGS
Excretion: Urine
(75%), Feces (9%)
(Lexi-comp, 2013).
Opioids/
Synthetic
Opioids/
Diphenylpropyla
mine
deriveratives
Methadone
(Dolophine®)
(Lexi-comp,
2013)
cardiovascular status,
blood pressure, pain
relief, heart rate, signs
of misuse, abuse, or
addiction (Access
Medicine, 2013).
Substrate: CYP3A4
(major). Inhibits:
CTP3A4 (weak) (Lexicomp, 2013).
Pharmacodynamics: Side Effects:
Binds to receptor
Common:
sites preventing
Hypotension, dizziness
ascending pain
drowsiness, dysphoria
pathways and
and weakness
altering pain
Rare:
perception (LexiArrhythmias,
comp, 2013)
bradycardia, agitation,
confusion, rash,
Pharmacokinetics:
decreased libido,
Absorption: Rapid in anorxia, constipation,
stomach
impotence,
Metabolism: Hepatic thrombocytopenia,
via CYP3A4,
vision problems,
CPY2B6, and
respiratory depression,
CYP2C19
and death (Lexi-comp,
Excretion: Urine
2013)
(Lexi-comp, 2013).
Monitor:
Dependence need, QT,
blood pressure, CNS
and respiratory status,
sedation, and falls
(Access Medicine,
2013).
Substrate: CYP2B6
(major), CYP2C19
(minor), CYP2C9
(minor), CYP2D6
(minor), CYP3A4
(major). Inhibits:
CYP2D6 (moderate),
CYP3A4 (weak) (Lexicomp, 2013).
oral mucositis, renal
impairment, respiratory
disease, CNS
depressants, CYP3A4
inhibitors, and MOA
inhibitors (Lexi-comp,
2013).
Contraindications:
Severe liver disease,
hypersensitivity to
methadone or any
component, respiratory
depression, asthma,
hypercarbia, paralytic
ileus, or selegiline use
(Lexi-comp, 2013)
Use Caution:
CNS depression,
hypotension, QT
prolongation,
respiratory depression,
abdominal conditions,
anxiety disorders,
adreal insufficiency,
drug abuse, depression,
head injury, renal
impairment, and seizure
disorder (Lexi-comp,
2013).
41
PERSONAL DRUGS
Opioids/
Synthetic
Opioids/
Others
Tramadol
(Ultram®),
Tapentadol
(Nucynta®)
(Lexi-comp,
2013)
Opioids/
Synthetic
Opioids/
Morphinan
Derivatives
Levorphanol
(Lexi-comp,
2013)
Pharmacodynamics:
Inhibits reuptake of
norepinephrine and
serotonin modifying
ascending pain
pathways while
binding to u-opiate
receptors blocking
ascending pain
pathways which
alters response to
pain (Lexi-comp,
2013).
Side Effects:
Common:
Flushing, dizziness,
headache, insomnia,
constipation, nausea,
vomiting, weakness,
and hypotension
Rare:
Chest pain, anxiety,
confusion, and vertigo
(Lexi-comp, 2013).
Monitor:
Pain relief, respiratory
Pharmacokinetics:
rate, blood pressure,
Absorption: Rapid
pulse, sings of
and complete
tolerance, abuse, or
Metabolism: Hepatic suicide (Access
via CYP3A4 and
Medicine, 2013).
CYP2B6,
glucuronidation, and Substrates: CYP2B6
sulfation
(minor), CYP2D6
Excretion: Urine
(major), CYP3A4
(Lexi-comp, 2013).
(major), CYP2C9
(minor) (Lexi-comp,
2013).
Pharmacodynamics: Side Effects:
Alters perception of Common:
pain by interacting
Hypotension, CNS
with opioid
depression, drowsiness,
receptors in the CNs nausea, vomiting,
and other tissues
constipation, and
(Lexi-comp, 2013).
weakness
Rare:
Pharmacokinetics:
Palpitation,
Absorption: Not
bradycardia, shock,
reported
nervousness, headache,
Metabolism: Hepatic anorexia, coma,
Excretion: Urine
convulsion,
(Lexi-comp, 2013).
hallucinations,
diplopia, apnea,
cyanosis, and
dependence (Lexicomp, 2013).
Monitor:
Contraindications:
Hypersensitivity to
tramadol, opioids, or
any component,
intoxication, hypnotics,
analgesics, opioids,
psychotropic drugs,
asthma, hypercapnia,
and respiratory
depression (Lexi-comp,
2013).
Use Caution:
Anaphylactoid
reactions, CNS
depression, seizures,
abdominal conditions,
drug abuse, ethanol use,
head trauma, hepatic or
renal impairment,
respiratory disease, or
suicide risk (Lexicomp, 2013).
Reduce dose with renal
or hepatic impairment.
Contraindications:
Hypersensitivity to
levorphanol or any
component (Lexi-comp,
2013).
Use Caution:
CNS depression,
hypotension,
phenanthrene
hypersensitivity,
abdominal conditions,
adrenal insufficiency,
biliary tract
impairment, drug
abuse, head trauma,
obesity, respiratory
disease, or thyroid
42
PERSONAL DRUGS
Opioids/
Synthetic
Opioids/
Phenylpiperdine
Meperidine
(Demerol®)
(Lexi-comp,
2013)
Pharmacodynamics:
Binds to opioid
receptors in the
ascending pathways
altering perception
of pain and
depressing the CNS
(Lexi-comp, 2013).
Pharmacokinetics:
Absorption: Erratic
and highly variable
Metabolism:
Hepatic; hydrolyzed
Excretion: Urine
(Lexi-comp, 2013).
Pharmacodynamics:
Inhibit synthesis of
(Tylenol®) (Lexi- prostaglandins in the
comp, 2013)
CNS. In the
peripheral it blocks
pain impulse
generation. Inhibits
hypothalamus heatregulating center to
produce antipyresis
(Lexi-comp, 2013).
Acetaminophen
Pharmacokinetics:
Absorption:
Pain relief, respiratory
and mental status, and
blood pressure (Lexicomp, 2013).
Side Effects:
Common:
Pre-syncope, fatigue,
blurred vision,
confusion, vertigo,
nausea, and
constipation
Rare:
Bradycardia, arrest,
hypotension, shock,
delirium, anorexia,
ileus, dyspnea, and
dependence (Lexicomp, 2013)
disease (Lexi-comp,
2013).
Contraindications:
Hypersensitivity to
meperidine or any
component, respiratory
depression, and the use
of a MAO inhibitor
within the last 14 days
(Access Medicine,
2013).
Use Caution:
CNS depression, CNS
events, hypotension,
abdominal conditions,
adrenal insufficiency,
Monitor:
biliary tract
Pain relief, respiratory impairment, coma,
and metal status, blood delirium, drug abuse,
pressure, CNS
head trauma, hepatic
depression, seizure,
impairment, obesity,
and respiratory
pheochromocytoma,
depression (Lexi-comp, prostatic hyperplasia,
2013)
psychoses, renal
impairment, respiratory
depression, sickle-cell
disease, tachycardia,
and thyroid dysfunction
(Lexi-comp, 2013)
Side Effects:
Contraindications:
Common:
Hypersensitivity to
Nausea, confusion,
acetaminophen or any
dyspepsia, jaundice,
component, severe
anorexia, asthenia, and hepatic impairment,
rash
and liver disease (LexiRare:
comp, 2013).
Anemia, neutropenia,
ammonia increase,
Use Caution:
nephropathy, and
Hepatotoxicity,
hypersensitivity
anaphylactic reactions,
(Clinical
ethanol use, G6PD
Pharmacology, 2013;
deficiency, hepatic
Lexi-comp, 2013)
impairment,
43
PERSONAL DRUGS
Variable; Primarily
in small intestine
Metabolism:
Primarily hepatic to
sulfate and
glucuronide
conjugates; small
amount by CYP2E1
Excretion: Urine
(Lexi-comp, 2013).
Monitor:
Serum APAP levels,
liver function tests,
pain relief, and
temperature (Lexicomp, 2013).
hypovolemia, and renal
impairment (Lexicomp, 2013).
Substrate: CYP1A2
(minor), CYP2A6
(minor), CYP2C9
(minor), CYP2D6
(minor), CYP2E1
(minor), CYP3A4
(minor). Inhibits:
CYP3A4 (weak) (Lexicomp, 2013).
IV. Effective Drug Classification: Opioid/Semisynthetic Opioids Oral
Drug Name
Opioids/
Semisynthet
ic Opioids
Hydrocodon
e (Lortab®,
Vicodin®,
Lorcet®)
(Lexi-comp,
2013)
Efficacy
Hydrocodone:
Onset of Action:
Ten to 20
minutes
Duration: Four to
eight hours
Metabolism:
Hepatic: Odemethyation via
CYP2D6 to
hydromorphone;
N-demethylation
via CYP3A4 to
norhydrocodone;
N-demethylation
via CYP#A$ to
norhydrocodone
and ~40% other
non-CYP
pathways
including 6ketosteroid
reduction to 6alpha-hydrocol
and 6-beta-
Safety
Drug
Interactions:
Azelastine,
conivptan,
paraldehyde,
MAO
inhibitors, and
pimozide (Lexicomp, 2013).
Increased
Effect/ Toxicity:
Alcohol,
alvimopan,
aripiprazole,
azelastine,
busulfan, CNS
depressants,
dasatinib,
desmopressin,
imatinib,
lomitapide,
metyrosine,
mipomersen,
mirtazapine,
Suitability
-CYP2D6 poor or
extensive metabolizers
may have varied
effects and toxicity.
-Do not abruptly stop
in chronic use. May
cause withdrawal.
-High potential of
abuse.
-Avoid fatty meals.
-Take one before
eating or two hours
after eating.
-May cause
constipation.
(Access Medicine,
2013; Lexi-comp,
2013).
Cost
Hydrogesic®
oral
(capsules): 5500mg (100):
$25.00
Lortab® oral
(elixir) 7.5500mg/15ml:
(473ml):
$220.50
Hycet® oral
(solution):
7.5-325/15ml
(473ml):
$227.77
Hydrocodone
acetaminoph
en oral
(solution):
7.5325mg/5ml
44
PERSONAL DRUGS
hydrocol
Half-life: 3.3 -4.4
hours
Excretion: Urine
(Lexi-comp,
2013).
paraldehyde,
pimozide,
pramipexole,
prilocaine,
ropinirole,
rotigotine,
SSRIs,
Acetaminophen:
sorafenib,
Onset of action:
thiazide
less than one hour diuretics,
Duration: Four to vitamin K
six hours
antagonists, and
Absorption:
zolpidem (LexiPrimarily small
comp, 2013).
intestine; varies
by dose
Decrease
Protein binding:
Effect/ Toxicty:
Ten to 25%
Pegvisomant,
Metabolism:
Ammonium
Hepatic to sulfate chloride,
and glucuronide
anticonvulsants,
conjugates; small barbiturates,
amount CYP2E1: carbamazepine,
substrate of
cholestyrmine
CYP1A2 (minor), resin, mixed
CYP2A6 (minor), agonist/
CYP2C9 (minor), antagonist
CYP2D6 (minor), opioids,
CYP2E1 (minor), peginterferon
CYP3A4 (minor); alfa-2b,
inhibits CYP3A4 rifampin, St
(weak).
Johns wort,
Half-life: ~2
tocilizumab,
hours
and quinidine
Peak Time:
(Lexi-comp,
Immediate
2013).
Excretion: Urine
(Lexi-comp,
Avoid:
2013).
More than three
alcoholic
beverages,
MAO
inhibitors, other
sedatives, and
herbs (valerian,
St John’s wort,
(473ml):
$139.77
7.5500mg/15ml
(471ml):
%58.12
Liquicet®
oral
(solution):
10500mg/15ml
(473ml):
$201.03
Zamicet®
oral
(solution) 10325mg/15ml
(473ml):
$173.12
Zolivt® oral
(solution):
10300mg/15ml
(473ml):
$92.40
Co-Gesic®
oral (tablets):
5-500mg
(100):
$137.58
Hydrocodone
acetaminoph
en oral
(tablets): 2.5500mg (40):
$21.28
5-300mg
(100):
$191.04
5-325mg
45
PERSONAL DRUGS
SAMe, and
kava kava)
(Lexi-comp,
2013).
(100): $54.22
5-500mg
(30): $26.65
5-500mg
(30): $26.65
7.5-300mg
(100):
$214.27
7.5-325mg
(100): $61.85
7.5-500mg
(100): $57.21
7.5-650mg
(100): $69.50
7.5-750mg
(100): $48.92
10-300mg
(100):
$276.44
10-325mg
(100): $83.00
10-500mg
(100): $70.10
10-650mg
(60): $713.80
10-660mg
(100): $71.50
10-750mg :
(100): $11.55
Lorcet®
10/650
(tablets): 10650mg (20):
$45.12
Lorcet® plus
oral (tablets):
7.5-650mg
(100):
$130.45
Lortab® oral
(tablets):
5-500mg
(100):
46
PERSONAL DRUGS
$103.45
7.5-500mg
(12): $13.32
10-500mg
(100):
$138.80
Maxidone®
oral:10750mg (100):
$216.85
Opioids/
Semisynthet
ic Opioids
Hydromorph
one
(Dilaudid®)
(Lexi-comp,
2013)
Onset of Action:
15 to 30 minutes
Duration: Three
to 13 hours
Absorption:
Delayed and
variable
Protein Binding:
Eight to 19%
Metabolism:
Hepatic: via
glucuronidation
Half-life: Two 11 hours
Peak Time: Less
than an hour to 16
hours
Excretion: Urine
(Lexi-comp,
2013).
Drug
Interactions:
Azelastine,
paraldehyde,
and MAO
inhibitors
(Access
Medicine,
2013).
Increase Effect/
Toxicity:
Alcohol,
alvimopan,
azelastine, CNS
depressants,
desmopressin,
metyrosine,
mirtazapine,
paraldehyde,
pramipexole,
ropinirole,
rotigotine,
SSRIs,
-Do not crush, chew,
dissolve or inject
medication.
-May be taken with or
without food.
-Alcohol can increase,
-Does not have a
histamine reaction.
-Do not abruptly stop
in chronic use.
-High potential of
abuse. (Lexi-comp,
2013).
Norco® oral
(tablets):
5-325mg
(15): $33.00
7.5-325mg
(30): $70.56
10-325mg
(30): $59.53
(Lexi-comp,
2013).
Dilaudid-5®
oral (liquid):
1mg/ml
(473ml):
$239.66
Hydromorph
one HCL
oral (liquid):
1mg/ml
(473ml):
$189.12
Hydromorph
one HCL
rectal
(suppository)
: 3mg (6):
$73.60
Exaglo® oral
(24 hour
tablet): 8mg
(100):
47
PERSONAL DRUGS
sorafenib,
thiazide
diuretics,
zolpidem,
Amphetamines,
antipsychotic
agents,
droperidol,
hydroxyzine,
magnesium
sulfate, MAO
inhibitors,
perampanel,
probenecid,
sodium oxybate,
and
succinylcholine
(Access
Medicine,
2013).
$1154.06
Dilaudid®
oral (tablets):
2mf (100):
$109.27
4mg (100):
$178.38
8mg (100):
$132.00
(Lexi-comp,
2013).
Decreased
Effect/Toxicity:
Pegvisomant,
Ammonium
chloride, and
mixed agonist/
antagonist
opioids (Access
Medicine,
2013).
Opioids/
Semisynthet
ic Opioids
Oxycodone
Onset of Action:
ten to 15 minutes
Peak Effect: 0.5-1
hour
Duration: Three
Avoid:
MAO
inhibitors, other
sedatives, and
herbs (valerian,
gotu kola, and
kava kava)
(Lexi-comp,
2013).
Drug
Interactions:
Azelastine,
conivptan, and
paraldehyde
-Use of CYP3A4
inhibitors with
oxycodone can result
in increased effects.
-Do not moisten,
Oxycodone
HCL oral
(capsules):
5mg (60):
$48.99
48
PERSONAL DRUGS
(Oxycontin®
,
Roxicodone
®) (Lexicomp, 2013)
to 12 hours
Protein Binding:
~45%
Metabolism:
Hepatic: via
CYP3A4 to
noroxycodone,
noromorphone,
and apla/betanoroxycodol.
CYP2D6 to
oxymorphone,
alpha/betaoxymorphol.
Substrates of
CTP2D6 (minor)
and CYP3A4
(major)
Half-life: Two -~
five hours
Excretion: Urine
(Lexi-comp,
2013).
(Lexi-comp,
2013).
Increased
Effect/Toxicity:
Alcohol,
alvimopan,
azelastine, CNS
depressants,
desmopressin,
metyrosine,
mirtazapine,
paraldehyde,
pramipexole,
ropinirole,
rotigotine,
SSRIs, thiazide
diuretics,
zolpidem,
Amphetamines,
antipsychotic
agents,
conivaptan,
dasatinib,
droperidol,
hydroxyzine,
magnesium
sulfate,
perampanel,
sodium oxybate,
and
succinylcholine
(Lexi-comp,
2013).
Increased
Effect/ Toxicity:
Pegvisomant,
Ammonium
chloride, mixed
agonist/
antagonist
opioids,
rifampin, St
Johns Wort, and
tocilizumab
dissolve, cut, crush,
break, or chew.
-Drink full glass of
water with pills.
-Laxatives should be
given to avoid
constipation.
-Do not abruptly stop
in chronic use.
-High potential of
abuse.
(Lexi-comp, 2013).
Oxycodone
HCL oral
(concentrate)
:
20mg/ml
(30ml):
$221.88
Oxycontin®
oral (12 hour
tablet):
10mg (20):
$61.95
15mg (60):
$209.46
20mg (20):
$100.42
30mg 960):
$407.50
40mg (30):
$280.43
60mg (30):
$395.91
80mg (60):
$1022.37
Oxecta® oral
(tablets):
5mg (100):
$320.40
7.5mg (100):
$320.40
Oxycodone
HCL oral
(tablets):
5mg (100):
$47.94
10mg (100):
$62.50
15mg (100):
$75.79
20mg (90):
$99.00
30mg (100):
49
PERSONAL DRUGS
(Lexi-comp,
2013).
Onset of Action:
Five to ten
minutes
Duration: Three
Oxymorphon to six hours
e (Opana®)
Protein Binding:
(Lexi-comp, ten to 12 %
2013)
Metabolism:
Hepatic: via
glucuronidation
Half-life: Seven
to 11hours
Excretion: Urine
(Lexi-comp,
2013).
Opioids/
Semisynthet
ic Opioids
Avoid:
MAO
inhibitors, other
sedatives, and
herbs (valerian,
St John’s wort,
and kava kava)
(Lexi-comp,
2013).
Drug
Interactions:
Azelastine,
paraldehyde,
and MAO
inhibitors (Lexicomp, 2013).
Increased
Effect/ Toxicity:
Alcohol,
alvimopan,
azelastine, CNS
depressants,
desmopressin,
metyrosine,
mipomersen,
paraldehyde,
pramipexole,
ropinirole,
rotigotine,
SSRIs,
sorafenib,
thiazide
diuretics,
zolpidem,
Amphetamines,
antipsychotic
agents,
droperidol,
hydroxyzine,
magnesium
sulfate, MAO
inhibitors,
$143.90
Roxicodone
® oral
(tablets):
15mg (100):
$175.10
30mg (90):
$278.65
(Lexi-comp,
2013).
-Do not abruptly stop
in chronic use.
-High potential of
abuse. –Do not break,
crush, dissolve, or
chew.
-Use safety measures
to prevent falls.
-Use laxatives to
prevent constipation.
-Avoid fatty meals.
-Take one before
eating or two hours
after eating.
(Lexi-comp, 2013).
Opana® ER
oral (12 hour
tablet):
5mg (60):
$143.56
7.5.mg (60):
$209.60
10mg (60):
$275.66
15mg (600:
$382.28
20mg (60):
$488.93
30mg (60):
$703.73
40mg (60):
$918.54
Oxymorphon
e HCL ER
oral (tablets):
7.5mg (100):
$283.52
15mg (60):
$565.00
Opana® oral
(tablets):
5mg (56):
$215.14
10mg (100):
$534.93
Oxymorphon
50
PERSONAL DRUGS
perampanel,
sodium oxybate,
and
succinylcholine
(Lexi-comp,
2013).
Deceased
Effect/Toxicity:
Pegvisomant,
Ammonium
chloride, and,
mixed agonist/
antagonist
opioids (Lexicomp, 2013).
e HCL oral
(tablets):
5mg (100):
$294.61
10mg (100):
$534.93
(Lexi-comp,
2013).
Avoid:
Alcoholic
beverages,
MAO
inhibitors, other
sedatives, and
herbs (valerian,
St John’s Wort,
and kava kava)
(Lexi-comp,
2013).
V. Drug of Choice: Hydrocodone-Acetaminophen Oral
Hydrocodone-Acetaminophen is the drug of choice for many emergency departments for
treating simple acute clavicle fractures in young healthy adults. Opioids such as hydrocodone
act in preventing the transmission of the pain receptive neurons by blocking the mu receptors.
Among the opioids the most common prescribed are oxycodone and hydrocodone. When
compared to each other, both have the same pain control effectiveness and similar side effects.
Only hydrocodone showed an increase in constipation and therefore should not be given to the
PERSONAL DRUGS
51
elderly or those with constipation difficulties. A stool softener should be prescribed in
combination with the hydrocodone (Black, Buderer, Marco, Plewa, & Roberts, 2008).
Hydrocodone-acetaminophen is a relatively safe opioid for the treatment of moderate to
severe pain. Thorough review of the patient’s history and physical is needed because this drug
has the potential for abuse. This drug is most commonly dosed as hydrocodone 5mg and
acetaminophen 500mg, one to two tablets by mouth every four to six hours as needed for pain for
a maximum of seven days. Hydrocodone is a cheap medicine only costing $11.99 for thirty pills
in generic form. The patient should be well educated on the proper use of taking this medication
such as , do not take while driving, use with alcohol or other sedatives, and do not take with
other forms of Tylenol as this may cause the patient to exceed their daily limit. Side effects of
this medication are vast and should be discussed with the patient. Have the patient follow up in
two weeks to ensure adequate healing (Access Medicine, 2013). An Advance Practice Nurse can
prescribe this medication only with a valid Certificate to Prescribe (CPT) and they can only write
for a seven day maximum in the hospital setting (Ohio Board of Nursing, 2013).
PERSONAL DRUGS
52
Third Diagnosis: New on Set of Epilepsy after an Subdural Hematoma
A 32 year old man develops new onset of tonic-clonic seizures one month after suffering
a stable subdural hematoma (SDH) from a fall. He was witnessed to have seizure like activity
this morning while getting dressed for work. He is an otherwise healthy individual who works as
an accountant. While being admitted to the hospital, staff witnessed a tonic-clonic seizure. Head
computed tomography (CT) showed a resolving subdural hematoma without any ischemia. After
a through history and physical he is diagnosed with new onset of generalized tonic-clonic
seizures after a stable SDH.
I. Definition of Diagnosis
A subdural hematoma is caused by tearing of a vein in minor head injuries. It is
associated with a low risk a seizure development and therefore patients are not routinely placed
on anti-convulsant afterward. The seizure itself is caused by abnormal excessive or synchronous
neuronal activity in the brain. A generalized tonic-clonic seizure is defined by being bilaterally
distributed across both hemispheres causing loss of consciousness with ridged motor movement.
The seizure is abrupt, without warning, and absent of any aura. The tonic-clonic seizure,
characterized by its name, has two parts with tonic being sustained muscle contraction (10-20
seconds) followed by clonic, which is recurrent contractions of the muscle (30 seconds). This
type of seizure is serious because of the increased risk of death if it were to be sustained (status
epilepticus). The patient can experience: Incontinence, elevated blood pressure, increased heart
rate, mydriasis, apnea, cyanosis, or death. The post ictal phase of recovery is characterized by
lethargy and confusion. Based on the reasoning of the seizure a CT, Magnetic Resonance
53
PERSONAL DRUGS
Imaging (MRI), or Electroencephalography (EEG) may be needed for evaluation along with
blood work (Bruni, 2008).
II. Therapeutic Objectives
Therapeutic objectives for new set of seizures after an acute SDH is the same as any other
seizure in that the goal is to remain seizure free, remain side effect free, have easy drug
convenience, low cost, and aim for low dose mono-therapy drug treatment (Dobrin, 2012).
Treatment for seizures post SDH is with Valproic acid; however, more recently providers are
choosing Levetiracetam due to its lower side effect profile. Drug choice should be chosen on
effectiveness and minimalizing side effects to ensure the best quality of life for the patient. Once
the patient is stabilized intense education of condition, medication, and changes in daily living
are needed (Kumlien & Zelano, 2011).
III. Inventory of Effective Drug Groups Oral
Drug
Efficacy
Safety
Suitability
Anti-epileptic/
Barbiturate
Pharmacodynamics:
Depresses the sensory
cortex, decreases motor
activity, alters
cerebellar function and
causes sedation. In high
doses this drug has anticonvulsant activity
(Lexi-comp, 2013).
Side Effects:
Common: Pre-syncope,
fatigue, blurred vision,
illogical thinking, an
dizziness
Rare: bradycardia,
nausea, vomiting, rash,
laryngospasm, and
constipation (Access
Medicine, 2013).
Contraindications:
Hypersensitivity to
barbiturates or any
component, hepatic
impairment, dyspnea,
airway obstruction,
porphyria, intraarterial administration,
subcutaneous
administration, drug
addiction, and
nephritic patients
(Lexi-comp, 2013).
Phenobarbital
PO (Lexi-comp,
2013)
Pharmacokinetics:
Absorption: 70-90%
Metabolism: Hepatic
via hydroxylation and
glucuronide conjunction
Excretion: Urine (50%
unchanged drug) (Lexicomp, 2013).
Monitor:
Vitamin D levels,
phenobarbital levels,
mental status, CBC,
LFTs, and seizure
activity (Access
Medicine, 2013).
Use Caution:
CNS depression,
hypotension,
paradoxical response,
54
PERSONAL DRUGS
Substrate: CYP2C19
(major), CYP2C9
(minor); Induces:
CYP1A2 (strong),
CYP2A6 (strong),
CYP2B6 (strong),
CYP2C9 (strong),
CYP3A4 (strong)
(Lexi-comp, 2013).
Side Effects
Anticonvulsant Pharmacodynamics
Stabilizes neuronal
Common: Suicidal
/
membranes and reduced ideation, rash, nausea,
Hydantoin
seizure activity by
vomiting, ataxia,
Ethotoin
increasing efflux or
fatigue, headache,
(Paganone®)
decreasing influx of
insomnia, drowsiness.
sodium ions in the
Rare: Chest pain,
Phenytoin
motor cortex. This
numbness, and diplopia
(Dilantin®,
prolongs refractory
(Clinical
Phenytek®)
period (Lexi-comp,
Pharmacology, 2013).
(Lexi-Comp,
2013)
2013)
Monitoring:
Pharmacokinetics:
CBC,EEG, LFT’s,
Absorption: Slow
Suicidality, trough
Metabolism: Hepatic;
concentrations, and
undergoes enterohepatic depression (Clinical
recirculation
Pharmacology, 2013).
Excretion: Urine (Lexicomp, 2013).
Substrate: CYP2C19
(major), CYP2C9
(major), CYP3A4
(minor), Induces:
CYP2B6 (strong),
CYP2C19 (strong),
CYP2C8 (strong),
CYP2C9 (strong),
CYP3A49 strong)
InhibitsCYP2C19
(weak) (Lexi-Comp,
2013)
Side Effects:
Anticonvulsant Pharmacodynamics
Binds to KCNQ
Common: Dizziness,
/
voltage-gated
potassium
fatigue, confusion,
Neuronal
channels stabilizing
vertigo, tremors,
Potassium
channels in open
diplopia, attention
Channel
formation and
disturbance, balance
Opener
respiratory depression,
depression, hepatic
impairment,
hypoadrenalism, renal
impairment, substance
abuse, with sedatives,
and in elderly (Lexicomp, 2013).
Contraindications:
Hematologic disease,
hypersensitivity to
hydatoin or any
component, hepatic
disease, and suicidal
ideation (Lexi-comp,
2013).
Use Caution:
Blood dyscrasias,
bone effects,
cardiovascular events,
skin reactions,
hypoabluminemia,
hypothyroidism,
porphyria, seizures,
Asian ancestry, and
elderly (Lexi-comp,
2013).
Contraindications:
No contraindications.
Use Caution:
CNS effects,
neuropsychiatric
55
PERSONAL DRUGS
Ezogabine
(Potiga®)
(Lexi-Comp,
2013)
enhancing M-current.
This regulates
epileptiform activity.
Alterations of GABAmediated currents are
also a suspected
mechanism (Lexicomp, 2013).
Pharmacokinetics:
Absorption: Rapid
Metabolism:
Glucuronidation via
UGT1A4, UGT1A4,
UGT1A9, UTG1A1 and
acetylation via NAT2
Excretion: Urine 85%,
Feces
(Lexi-Comp, 2012).
Anticonvulsant Pharmacodynamics
Increases seizure
/
threshold and
Succinmide
suppresses paroxysmal
Ethosuximide
spike and wave pattern
(Zarontin®),
in the motor cortex
Methsuximide
(Access Medicine,
(Celontin®)
2013; Lexi-comp,
(Lexi-Comp,
2013).
2013)
Pharmacokinetics:
Absorption: Rapidly
through GI tract
Metabolism: Hepatic
Excretion: Urine
(Slowly) and small
amount through feces
(Lexi-comp, 2013).
Anticonvulsant Pharmacodynamics
disturbance, memory
impairment
Rare: Alopecia,
appetite increase,
coma, hallucination,
liver enzyme increase,
malaise, muscle
spasms, and syncope
(Lexi-comp, 2013).
disorders, QT
prolongation, suicidal
ideas, urinary
retention, and hepatic
or renal impairment
(Lexi-comp, 2013).
Monitoring:
Seizures, electrolytes,
bilirubin, ALT, SAT,
creatinine, QT interval,
urinary retention,
sedation, and
behavioral changes
(Lexi-Comp, 2013).
Side Effects:
Common: Abdominal
pain, agitation,
dizziness, elevated
hepatic enzymes,
fatigue, headache,
drowsiness, ataxia,
aplastic anemia, rash,
nightmares, vomiting
Rare: Agranulocytosis,
vaginal bleeding,
paranoid psychosis, and
myopia (Access
Medicine, 2013).
Monitoring:
CBC, LFT’s,
Urinalysis, seizures,
trough serum, platelets,
and rash (Access
Medicine, 2013).
Substrate: CYP3A4
(major) (Lexi-comp,
2013)
Side Effects:
Contraindications:
Succinimide
hypersensitivity or any
component (Access
Medicine, 2013).
Use Caution:
Blood dyscrasias,
CNS depression, skin
reactions, SLE, suicide
ideas, hepatic
impairment, renal
impairment, with
sedatives, and watch
for withdrawal when
stopping (Lexi-comp,
2013).
Contraindications:
56
PERSONAL DRUGS
/ Triazole
Derivatives
Rufinamide
(Banzel®)
(Lexi-Comp,
2013)
Exact mechanism
unknown but it
prolongs the inactive
state of sodium
channels limiting
repetitive firing of
sodium –dependent
action which reduces
convulsions (Clinical
Pharmacology, 2013;
Lexi-comp, 2013).
Pharmacokinetics:
Absorption: Slow and
extensive; increased
with food.
Metabolism:
Carboxylesterasemediated hydrolysis of
the carboxylamide
group CGP 47292,
weak inhibitor of
CYP2E1 and weak
inducer of CYP3A4
Excretion: Urine 85%
(Lexi-Comp, 2013).
Anticonvulsant Pharmacodynamics:
Decrease production of
/
aqueous humor inhibits
Miscellaneous
carbonic anhydrase in
Acetazolamide
CNS to slow abnormal
(Diamox®,
and excessive discharge
Serquels®)
(Lexi-comp, 2013).
(Lexi-Comp,
2013)
Pharmacokinetics:
Absorption: Rapidly
absorbed from GI tract
Metabolism: Not
reported
Excretion: Urine
Metabolism: no
(Lexi-Comp, 2013)
Common: QT
shortening, headache,
vomiting, fatigue,
dizziness, nausea,
ataxia, rash, anemia,
tremor, diplopia
Rare: AV block, BBB
block, hematuria,
incontinence, and
lymphadenopathy
(Clinical
Pharmacology, 2013).
Monitoring:
Suicidal ideations,
seizure, serum levels of
anticonvulsants
(Clinical
Pharmacology, 2013).
Patients with familial
short QT syndrome,
hypersensitivity to
triazole and
derivatives (Lexicomp, 2013).
Use Caution:
Abnormal cardiac
conductions, CNS
effects, rash, suicidal
ideas, and hepatic
impairment (Lexicomp, 2013).
Inhibits: CYP2E1
(weak); Induces
CYP3A4
(weak/moderate) (LexiComp, 2013)
Side Effects:
Common: nausea,
xerostomia, and
diarrhea
Rare: Flushing, ataxia,
confusion, fatigue,
electrolyte imbalance,
parenthesis, and
myopia (Lexi-comp,
2013).
Contraindications:
Adrenal insufficiency,
hepatic disease, renal
disease, hypokalemia,
electrolyte imbalance,
hypersensitivity
sulfonamide,
acetazolamide or any
component (Lexicomp, 2013).
Monitoring:
Intraocular pressure,
serum electrolytes,
CBC, growth in
pediatric patients,
blood glucose (Lexicomp, 2013).
Use Caution:
CNS effects, sulfa
allergy, diabetes,
hepatic impairment,
respiratory acidosis,
aspirin use, and
elderly (Lexi-comp,
57
PERSONAL DRUGS
2013).
Inhibits CYP3A4
(Lexi-comp, 2013)
Anticonvulsant Pharmacodynamics
Depresses activity in
/
the nucleus ventralis of
Miscellaneous
the thalamus or
Carbamazepine decreases synaptic
(Carbatrol®,
transmission or
Epitol®,
decreases temporal
Equetro®,
stimulation by limiting
Tegretol®
influx of sodium ions
(Lexi-Comp,
across cell membranes
2013)
(Lexi-comp, 2013)
Pharmacokinetics:
Absorption: Slow
Metabolism: Hepatic
via CYP3A4
Excretion: Urine
(Lexi-comp, 2013)
Anticonvulsant Pharmacodynamics
Allows for increased
/
availability of gammaMiscellaneous
aminobutyric acid
Divalproex,
(GABA) to brain
Valproic Acid
neurons and enhances
(Depakote®)
the action of GABA or
(Lexi-comp,
mimics its action at
2013)
receptor sites (Access
Medicine, 2013; Lexicomp, 2013).
Pharmacokinetics:
Absorption: Not
Side Effects:
Common: Diplopia,
ataxia, drowsiness, GI
upset, hyponatremia,
Rare: leucopenia, rash
and hepatic dysfunction
(Lexi-comp, 2013)
Monitoring:
CBC, platelets, serum
iron, LFT’s. renal
panel, serum
carbamazepine levels,
thyroid functions, and
suicidality (Access
Medicine, 2013).
Substrate: CYP2C8
(minor), CYP3A4
(major); Induces
CYP1A2 (strong),
CYP2B6 (strong),
CYP2C19 (strong),
CYP2C8 (strong),
CYP2C9 (strong), pglycoprotein
(Lexi-Comp, 2013).
Side Effects:
Common: Nausea,
vomiting, GI upset,
abdominal pain,
heartburn, weight gain,
hair loss (Access
Medicine, 2013).
Monitoring:
Liver panel, CBC,
platelets, PT/PTT,
serum ammonia, serum
valproate levels, and
suicidality (Access
Contraindications;
Hypersensitivity to
carbamazepine and
tricyclic
antidepressants or any
component, bone
marrow depression,
MAO inhibitors, or
use of nefazodone
(Lexi-comp, 2013).
Use Caution:
Blood dyscrasia, CNS
depression, skin
reactions,
Hyponatremia,
anticholinergic
sensitivity,
cardiovascular disease,
hepatic impairment,
renal impairment, and
drug abuse (LexiComp, 2013).
Contraindications:
Hypersensitivity to
Valproic acid,
divalproex, derivatives
of any component,
hepatic disease, or
cycle disorders (Lexicomp, 2013).
Use Caution:
Hepatic disease,
pancreatitis,
pregnancy, CNS
depression,
58
PERSONAL DRUGS
reported
Metabolism: extensive
hepatic via glucuronide
and mitochondrial betaoxidation
Excretion: Urine
(Lexi-comp, 2013).
Anticonvulsant Pharmacodynamics
Mechanism unknown,
/
weak inhibitory effects
Miscellaneous
on GABA,
Felbamate
benzodiazepine receptor
(Felbatol®)
binding, and activity at
(Lexi-Comp,
MK-801 receptor
2013)
binding site of the
NMDA receptor
complex (Lexi-comp,
2013).
Pharmacokinetics:
Absorption: Rapid and
almost complete
Metabolism: Not
reported
Excretion: Urine
(Lexi-comp, 2013)
Medicine, 2013).
Substrate: CYP2A6,
2B6, 2C9, 2C19, 2E1
(minor); Inhibits:
CYP2C9, 2C19, 2D6,
3A4 (weak); induces
CYP2A6 (weak) (Lexicomp, 2013)
Side Effects:
Common: drowsiness,
dizziness, blurred
vision, fever, insomnia,
fatigue, nervousness,
nausea, vomiting,
anorexia, and dry
mouth
Rare:
Aplastic anemia,
hepatitis, insomnia,
fever, fatigue,
nervousness, and
purpura (Lexi-comp,
2013).
hypothermia, suicidal
ideas,
thrombocytopenia, and
acute head trauma
(Lexi-comp, 2013).
Contraindications:
Hypersensitivity to
drug or any
component, blood
dyscrasia, or hepatic
dysfunction (LexiComp, 2013).
Use Caution:
Aplastic anemia,
hepatic failure, renal
impairment, and
suicide ideas (Lexicomp, 2013).
Monitoring:
AST, ALT,
hematological
evaluation before
therapy and frequently
during therapy, and
suicidality (Lexi-comp,
2013).
Substrates: CYP2E1
(minor), CYP3A4
(major); Inhibits
CYP2C19 (weak);
Induces CYP3A4
(weak/moderate) (LexiComp, 2013).
Anticonvulsant Pharmacodynamics
Modify release of
/
GABA, GABA sites
Miscellaneous
Side Effects:
Common: Dizziness,
fatigue, ataxia, fever,
Contraindications:
Hypersensitivity to
gabapentin or any
59
PERSONAL DRUGS
GABA
Derivatives:
Gabapentin
(Gralise®,
Neurontin®)
Gabapentin
Enacarbil
(Horizant®)
(Lexi-comp,
2013)
throughout brain
correspond to presence
of calcium channels
such as alpha-2-delta-1
subunits this releases
excitatory
neurotransmitters which
assist with
epileptogenesis and
nociception (Clinical
Pharmacology, 2013;
Lexi-comp, 2013).
Pharmacokinetics:
Absorption: variable,
small bowel by Lamino transport system
Metabolism: Does not
induce hepatic enzymes
Excretion: Urine
(Lexi-comp, 2013).
diarrhea, leucopenia,
tremor, weakness,
increased appetite.
Rare: Cushingoid
appearance,
encephalopathy,
erythema multiform,
facial paralysis, fecal
incontinence,
glaucoma, glycosuria,
hearing loss, heart
block, hematuria,
hemiplegia,
hemorrhage, hepatitis,
hepatomegaly,
myoclonus,
lymphadenopathy,
lymphocytosis, MI,
migraine, nephrosis,
nerve palsy, nonHodgkin's lymphoma
(Clinical
Pharmacology, 2013).
component (Lexicomp, 2013).
Use Caution:
CNS depression,
suicidal thoughts,
renal impairment,
seizure disorder, and
sedative use (Lexicomp, 2013).
Monitoring:
Suicidality and drug
levels
(Lexi-Comp, 2013)
Anticonvulsant Pharmacodynamics:
Enhances slow
/
inactivation of voltage
Miscellaneous
gated sodium channels,
Lacosamide
with stabilization of
(Vimpat®)
hyperexcitability
(Lexi-Comp,
neuronal membranes
2013)
and inhibition of
neuronal firing (Access
Medicine, 2013; Lexicomp, 2013).
Side Effects:
Common: Dizziness,
headache, nausea, and
diplopia
Rare: syncope,
vomiting, tremor,
weakness, nystagmus,
and tremor (Access
Medicine, 2013).
Contraindications:
Hypersensitivity to
drug, MI, atrial flutter,
AV block,
bradycardia, heart
failure, suicidal,
pregnancy, renal
failure (Lexi-comp,
2013)
Monitoring:
EKG prior to therapy,
Pharmacokinetics:
CBC, and suicidal
Absorption: Completely ideas (Lexi-Comp,
Metabolism: Hepatic
2013)
Inhibits
CYP2C19(weak)
Use caution:
Hepatic failure, renal
failure, CNS
depression,
depression, abnormal
heart conductions, and
sedative use (Lexi-
60
PERSONAL DRUGS
Excretion: Urine and
feces
(Lexi-Comp, 2013)
Anticonvulsant Pharmacodynamics:
Triazine derivative
/
inhibits release of
Miscellaneous
glutamate and inhibits
Lamotrigine
voltage-sensitive
(Lamictal®)
sodium channels and
(Lexi-Comp,
stabilizes neuronal
2013)
membranes. This also
has a weak inhibitory
effect on 5-HT3
receptor (Lexi-comp,
2013).
Pharmacokinetics:
Absorption: Rapid and
complete
Metabolism: Hepatic
and renal
Excretion: Urine 94%
and feces (Lexi-comp,
2013).
Anticonvulsant Pharmacodynamics
Inhibition of voltage/
dependent N-type
Miscellaneous
calcium channels,
Levetiracetam
facilitation of GABA
(Keppra®)
inhibitory transmission
(Lexi-Comp,
through negative
2013)
modulators, reduced
rectifier potassium
current, and binging to
synaptic proteins to
reduce neural discharge
(Clinical
Pharmacology, 2013;
Lexi-comp, 2013).
Pharmacokinetics:
Absorption: Rapid,
complete
Metabolism: Not
comp, 2013)
Side Effects:
Common: pre-syncope,
fatigue, blurred vision,
illogic thinking,
dizziness, imbalance,
headache, and nausea
Rare:
Abdominal pain, acne,
agitation, anorexia,
anxiety, agitation, back
pain, edema, rash,
weakness, dry skin
(Lexi-comp, 2013).
Contraindications:
Hypersensitivity to
drug and component
(Lexi-comp, 2013).
Use Caution:
Aseptic meningitis,
blood dyscrasia, CNS
depression, skin
reaction, suicidal
thoughts and hepatic
and renal impairment
(Lexi-comp, 2013).
Monitoring:
Serum levels, LFTs,
BMP, reactions,
seizures, suicide ideas,
depression, an behavior
(Lexi-comp, 2013)
Side Effects:
Common: pre-syncope,
fatigue, blurred vision,
illogical thinking,
imbalance, headache,
mood changes,
rhinorrhea, pharyngitis,
asthenia, nausea, and
emotional imbalance
Rare: anorexia,
weakness, cough,
infection, facial edema,
confusion, bruising,
dehydration,
leukopenia, neck pain,
diplopia, ear pain, and
albuminuria (Access
Medicine, 2013).
Monitoring:
Contraindications:
None (Lexi-comp,
2013)
Use Caution:
CNS effects skin
reactions, hematologic
effect, hypertension,
psychiatric disorders,
renal impairment, and
sedative use (Lexicomp, 2013)
61
PERSONAL DRUGS
extensive; mainly
through enzyme
hydrolysis
Excretion: Unchanged
in urine (Lexi-comp,
2013).
Anticonvulsant Pharmacodynamics:
Decreases acetylcholine
/
in motor nerves
Miscellaneous
reducing transmission
Magnesium
(Lexi-comp, 2013).
Sulfate (Lexicomp, 2013)
Pharmacokinetics:
Absorption: Not
reported
Metabolism: Not
reported
Excretion: Urine (Lexicomp, 2013).
Anticonvulsant Pharmacodynamics
Blocks voltage/
sensitive sodium
Miscellaneous
channels stabilizing
Oxcarbazepine
hyper excited neuronal
(Trileptal®)
membranes inhibiting
(Lexi-Comp,
firing and decreasing
2013)
propagation of impulses
(Lexi-comp, 2013).
Suicidality (Lexi-comp,
2013)
Side effects:
Common: hypotension,
and diarrhea
Rare: angina,
tachycardia, dizziness,
asthenia, vision
changes, illogical
thinking, flushing and
rash (Lexi-comp,
2013).
Monitoring:
Respiratory rate, deep
tendon reflexes, and
renal function (Lexicomp, 2013).
Side Effects:
Common: Dizziness,
somnolence, headache,
ataxia, fatigue, vertigo,
nausea, tremor,
abnormal gait, rash,
weight gain, and
constipation
Rare: aggressiveness,
alopecia, anxiety,
Pharmacokinetics:
aplastic anemia,
Absorption: Complete
dysphagia, hemiplegia,
Metabolism: Hepatic to palpitations, and
10-monohydroxy
xerophthalmia (Leximetabolite then
comp, 2013).
glucuronidated to 10,11
dihydroxy metabolite
Monitoring:
Induces
Serum sodium CNS
CYP3A4(strong)
depression, serum
Excretion: Urine 95%,
levels, seizures, and
feces
suicidality (Lexi-comp,
(Lexi-Comp, 2013)
2013).
Contraindications:
Hypersensitivity to
drug or components,
heart block and
myocardial damage
(Lexi-comp, 2013).
Use Caution:
Neuromuscular
disease, renal
impairment, and with
aluminum use (Lexicomp, 2013).
Contraindications:
Hypersensitivity to
Oxcarbazepine or any
component (Lexicomp, 2013)
Use Caution:
Blood dyscrasias,
CNS effects, skin
reactions,
Hyponatremia,
suicidal ideas, sedative
use, and oral
contraceptives (Lexicomp, 2013).
62
PERSONAL DRUGS
Induces: CYP3A4
(Lexi-Comp, 2013)
Anticonvulsant Pharmacodynamics:
The exact mechanism
/
of action is unknown
Miscellaneous
but is thought to have a
Perampanel
noncompetitive
(Lexi-comp,
antagonist of the
2013)
AMPA glutamate
receptor on
postsynaptic neurons
(Lexi-comp, 2013).
Pharmacokinetics:
Absorption: Rapid and
complete
Metabolism: Extensive
via oxidation mediated
by CYP3A5 and
sequential
glucuronidation
Excretion: Feces (48%)
and urine (22%) (Lexicomp, 2013).
Anticonvulsant Pharmacodynamics:
Stimulates the
/
hypothalamus and
Miscellaneous
releases norepinephrine
Phenetermine,
while blocking neuronal
Topiramate
voltage dependent
(Qsymia®)
sodium channels,
(Lexi-comp,
enhancing GABA
2013)
activity, antagonizes
AMPA glutamate
receptors, and weakly
inhibits carbonic
anhydrase (Lexi-comp,
2013).
Pharmacokinetics:
Absorption: Well
absorbed
Side Effects:
Common: Dizziness,
somnolence, headache,
fatigue, irritability,
weight gain, and
nausea
Rare: Ataxia, anxiety,
hypersomnia, mood
changes Hyponatremia,
arthralgia, parenthesis,
and diplopia (Lexicomp, 2013).
Contraindications:
None reported (Lexicomp, 2013).
Use Caution:
Neuropsychiatric
disorders, CNS
effects, suicidal
thoughts, hepatic
impairment, renal
impairment, fall risk,
and withdrawal (Lexicomp, 2013).
Monitoring:
Seizure activity,
suicidality, and weight
(Lexi-comp, 2013).
Substrate: CYP3A4;
Induces CYP3A4
(Lexi-comp, 2013).
Side Effects:
Common: Somnolence,
headache, constipation,
fatigue, irritability,
weight gain, and
nausea
Rare: Ataxia, dizziness,
anxiety, hypersomnia,
mood changes
Hyponatremia,
arthralgia, parenthesis,
and diplopia (Lexicomp, 2013).
Monitoring:
Seizure activity,
suicidality, resting
heart rate, serum
Contraindications:
Hypersensitivity or
idiosyncrasy to drug
or any component,
hyperthyroidism,
glaucoma, MAO
inhibitor use, or
pregnancy (Lexicomp, 2013).
Use Caution:
Cardiovascular effect,
CNS effects,
glaucoma,
hyperthermia,
hypokalemia,
hypotension,
metabolic acidosis,
63
PERSONAL DRUGS
Metabolism: hepatic via
hydroxylation,
hydrolysis, and
glucuronidation
Excretion: Mainly urine
(Lexi-comp, 2013).
bicarbonate, potassium,
glucose, serum
creatinine, blood
pressure, glaucoma,
symptoms of acidosis,
and weight (Lexicomp, 2013).
renal calculus, suicidal
thoughts, renal
impairment, Diabetes,
hepatic impairment,
and withdrawal (Lexicomp, 2013).
Inhibits: CYPC19
(weak); Induces
(CYP3A4
(weak/moderate) (Lexicomp, 2013).
Anticonvulsant Pharmacodynamics:
Binds to aplh2-delta
/
subunit of calcium
Miscellaneous
channels inhibiting
Pregabalin
excitatory
(Lyrica®)
neurotransmitter release
(Lexi-comp,
(Lexi-comp, 2013).
2013)
Pharmacokinetics:
Absorption: Not
reported
Metabolism: Nagligible
Excretion: Mainly urine
(Lexi-comp, 2013).
Side Effects:
Common: Edema,
dizziness, Somnolence,
headache, constipation,
fatigue, weight gain,
and nausea
Rare: Ataxia, drunken
feeling, anxiety,
hypersomnia, mood
changes, hyponatremia,
arthralgia, parenthesis,
and diplopia (Lexicomp, 2013).
Monitoring:
Seizure activity,
suicidality, myopathy,
ocular disturbances,
skin integrity, and
weight (Lexi-comp,
2013).
Anticonvulsant Pharmacodynamics
Decreases neuron
/
excitability and raises
Miscellaneous
seizure threshold (LexiPrimidone
comp, 2013).
(Mysoline®)
(Lexi-Comp,
Pharmacokinetics:
2013)
Absorption: 60-80%
Metabolism: Hepatic to
Phenobarbital by
Side Effects:
Common: Pre-syncope,
fatigue, blurred vision,
illogical thinking,
dizziness, and nausea
Rare: Ataxia, vertigo,
anorexia, impotence,
agranulocytosis, and
diplopia (Lexi-comp,
2013).
Contraindications:
Hypersensitivity to
drug or any
component (Lexicomp, 2013).
Use Caution:
Angioedema, CNS
effects,
hypersensitivity,
peripheral edema,
platelet count, PR
interval,
rhabdomyolysis,
Visual disturbances,
weight gain,
cardiovascular disease,
suicidal thoughts,
renal impairment,
tumorigenic potential,
and withdrawal (Lexicomp, 2013).
Contraindications:
Hypersensitivity to
phenobarb and
porphyria (Lexi-comp,
2013)
Use caution:
CNS depression,
suicidal ideas,
depression, hepatic
64
PERSONAL DRUGS
oxidation to PEMA by
seission of the
heterocyclic ring
Excretion: Urine
(Lexi-Comp, 2013).
Monitoring:
Serum primidone and
phenobarb,
neurological status,
CBC, and behavioral
changes (Lexi-comp,
2013).
and renal impairment,
respiratory disease,
and substance abuse
(Lexi-comp, 2013).
Induces: CYP1A2
(strong), CTP2B6
(strong), CYP2C8
(strong), CYP2C9
(strong), CYP3A4
(strong) (Lexi-Comp,
2013).
Anticonvulsant Pharmacodynamics
Enhances GABA
/
uptake activity in
Miscellaneous
neurons and allows
Tiagabine
increased amount of
(Gabitril®)
GABA in postsynaptic
(Lexi-comp,
neurons (Access
2013)
Medicine, 2013; Lexicomp, 2013)
Side Effects:
Common: pre-syncope,
fatigue, blurred vision,
illogical thinking,
dizziness, nausea,
diarrhea, xerostomia,
increased appetite,
tremors, nervousness,
and anxiety
Rare: depression,
imbalance, vision
changes, eye pain,
asthenia, and rash
(Access Medicine,
2013).
Pharmacokinetics:
Absorption: Rapid;
prolonged with food
Metabolism: Hepatic
via CYP (primarily
3A4)
Excretion: Feces mainly Monitoring:
and urine (Lexi-comp,
Seizures, CBC, LFT’s,
2013).
renal functions, serum
chemistry, and
suicidality (Access
Medicine, 2013).
Contraindications:
Hypersensitivity to
Tiagabine or any
component (Lexicomp, 2013)
Use Caution:
CNS depression, skin
reactions suicidal
ideas, hepatic
impairment, with
enzyme-inducing
drugs, and with
sedatives (Lexi-comp,
2013).
Substrate: CYP3A4
(major) (Lexi-Comp,
2013)
Anticonvulsant Pharmacodynamics
/Miscellaneous Blocks neuronal
Side Effects:
Common: Somnolence,
Contraindications:
None
65
PERSONAL DRUGS
Topiramate
(Topamax)
(LexiComp,
2012)
voltage-dependent
sodium channels,
enhances GABA
activity, antagonizes
AMPA/kainite
glutamate receptors and
weakly inhibits
carbonic anhydrase
(Lexi-comp, 2013).
headache, fatigue,
sedation, rash, blurred
vision, dizziness, and
tremors.
Rare: hypotension,
infections, diaphoresis,
and paranoid reactions
(Access Medicine,
2013).
Pharmacokinetics:
Absorption: Good,
rapid
Metabolism: minor
amounts hepatic via
hydroxylation,
hydrolysis, and
glucuronidation
Excretion: Urine (Lexicomp, 2013).
Monitoring:
Seizures, hydration,
electrolytes, creatinine,
ammonia, intraocular
pressure, and suicidal
ideation (Access
Medicine, 2013).
Inhibits: CYP2C19
(weak); Induces
CYP3A4
(weak/moderate) (LexiComp, 2013).
Side Effects:
Anticonvulsant Pharmacodynamics
Common: Drowsiness,
/Miscellaneous Stabilizes neuronal
membranes and
cognitive impairment,
Zonisamide
suppresses neuronal
confusion, poor
(Zonegran®)
hypersynchronization
concentration,
(Lexi-comp,
though sodium and
Rare: anorexia,
2013)
calcium channels (Lexi- headache, irritability,
comp, 2013).
tiredness, abdominal
pain (Lexi-comp,
Pharmacokinetics:
2013).
Absorption: Not
reported
Monitoring:
Metabolism: Hepatic
Metabolic profile, renal
via CYP3A4
panel, serum
Excretion: Urine (Lexi- bicarbonate, and
comp, 2013)
suicidiality (Lexicomp, 2013).
Substrate: CYP2C19
(minor), CYP3A4
(minor) (Lexi-comp,
2013).
Use Caution:
CNS effects.
Glaucoma,
encephalopathy,
hyperthermia,
acidosis, renal
calculus, suicidal
ideas, and renal and
hepatic impairment
(Lexi-comp, 2013).
Contraindications:
Hypersensitivity of
zonisamide or
sulfonamides or any
component (Lexicomp, 2013).
Use Caution:
CNS effects, acidosis,
renal stones, suicidal
ideas, sulfonamide
reactions, and renal
and hepatic
impairment (Lexicomp, 2013).
66
PERSONAL DRUGS
IV. Effective Drug Classification: Levetiracetam Oral
Drug Name
Levetiracetam
(Keppra®)
(Lexi-comp,
2013)
Efficacy
Absorption:
Rapid and
complete
Protein Binding:
<10%
Metabolism: Not
Extensive.
Mainly by
enzymatic
hydrolysis
Half-life: ~6-8
hours; increased
in renal
dysfunction
Peak Time: ~1
hour to ~4 hours
Excretion: Urine
(Lexi-comp,
2013).
V. Drug of Choice: Levetiracetam
Safety
Drug Interactions:
Azelastine and
paraldehyde (Lexicomp, 2013)
Suitability
-This drug can
be given to
children and
hemodialysis
patients.
Increased
-Monitor for
Effect/Toxicity:
behavioral
Alcohol,
changes and
azelastine,
suicidal ideas.
buprenorphine,
-Do not stop
CNS depressants,
abruptly due to
methotrimeprazine, the possibility
metyrosine,
increased seizure
mirtazapine,
frequency.
paraldehyde,
-May be taken
pramipexole,
without regard
ropinirole,
to meals.
rotgotine, SSRIs,
-Alcohol
zolpidem,
increases CNS
droperidol,
depression
hydroxyzine,
(Access
magnesium sulfate, Medicine, 2013;
methotrimeprazine, Lexi-comp,
perampanel, and
2013).
sodium oxybate
(Lexi-comp, 2013).
Cost
Keppra XR®
oral (24 hour
tablets)
500mg (60):
$374.36
750mg (60):
$562.13
Decreased
Effect/Toxicity:
Ketorlac (nasal and
systemic) and
mefloquine (Lexicomp, 2013).
Levetiracetam
oral (tablets)
250mg (120):
$345.04
500mg (120):
$421.71
750mg (120):
$571.31
1000mg (60):
$422.18 (Lexicomp, 2013).
Levetiracetam
ER oral (24
hour tablets)
500mg (60):
$266.82
750mg (60):
$400.64
Keppra® oral
(tablets)
250mg (60):
$206.02
500mg (30):
$145.88
750mg (120):
$1118.96
1000mg (30):
$244.36
PERSONAL DRUGS
67
Levetiracetam is quickly becoming the drug of choice for patients who develop seizure
activity after suffering an acute SDH. While traditionally it has been used for secondary line of
treatment its equal effectiveness has brought it to the forefront. Unlike Valproic acid,
Levetiracetam is a non-enzyme anti-epileptic drug with better tolerability by the patient, fewer
side effects and drug to drug interactions, and does not require therapeutic index blood sampling.
While this drug is more expensive, adherence to treatment is more likely due to the reduced side
effect profile (Ghauri, Khan, Shamim, & Zafar, 2012). The appropriate dose is 500mg oral twice
daily for two weeks that may be increased by 500mg oral every two weeks until maximum dose
of 1500mg oral twice daily is reached or seizure activity is stopped. The patient should be seen
at each dose increase and then one month after finding stabilization dose and then yearly. Doses
may have to be lowered based on creatinine clearance. As with any drug, education about side
effects is crucial along with developing goals and treatment plan with the patient. This drug is
not to be stopped abruptly due to the possible increases in seizure frequency and should be taken
until cleared by a neurologist. Avoid alcohol use with Levetiracetam. Do not break, crush, or
chew tablet. This drug costs $29.99 for 30 pills of the 500mg oral (Access Medicine, 2013). An
advance practice nurse with a current CTP may prescribe Levetiracetam (Ohio Board of Nursing,
2013).
Fourth Diagnosis: Ventilator Assisted Pneumonia in a Renal Patient
A 68 year old male has been in the intensive care unit for one week after suffering acute
respiratory failure and has been intubated since admission. He is a long time dialysis patient due
to stage four kidney disease. Over the past two days he has developed hyperthermia, increased
tracheobronchial secretions, and leukocytosis. A bronchoalveolar lavage was completed and the
sample was positive for Methicillin-resistant Staphylococcus Aureus (MRSA). Patient history
PERSONAL DRUGS
68
included renal failure and previous MRSA infection of the skin. After a complete history and
physical the patient is diagnosed with ventilator assisted pneumonia (VAP) culture positive for
MRSA.
I. Definition of Diagnosis
Ventilator assisted pneumonia is defined by new or increased pulmonary infiltrates in a
intubated patient for more than 48 hours plus two or more infective criteria including: Fever,
hypothermia, leukocytosis, purulent secretions, and reduced PaO2/FiO2. Methicillin-resistant
Staphylococcus Aureus is defined by obtaining a positive culture. Effective treatment for VAP
MRSA includes starting the correct antibiotics within 24 hours of sample collection (Bouza et
al., 2011). The Center for Disease Control (2013) also recommends non medication therapy
including raising the head of bed 30-45 degrees, extubate the patient as soon as medically
possible, always wash hands before and after care, wear clean gloves, regularly clean inside the
patients mouth, and clean or replace equipment between patient use. Contact precautions must
be maintained per hospital protocol on all MRSA positive patients. The rate of occurrence of
VAP MRSA varies greatly from hospital to hospital, patient co-morbidities, and reason for
intubation. In house mortality is around 60% but is not an independent risk factor (Bouza et al.,
2011).
II. Therapeutic Objectives
The treatment goal for patients with VAP MRSA is effective treatment with antibiotics,
reduction in mortality, and early extubation. Ventilator associated pneumonia MRSA requires
immediate treatment once infection is suspected. Until susceptibilities are known, any hospital
VAP infection should be treated with combination therapy of Vancomycin, Imipenem, and either
69
PERSONAL DRUGS
an aminoglycoside or fluoroquinolone. Once the organism has been identified as MRSA, then
therapy can be adjusted to Vancomycin or Linezolid depending on renal function. All other
antibiotics can be stopped. Prevention of VAP MRSA through good mouth care, increased
mobility of patient, and early extubation are very important and continue to be very important
once VAP MRSA is established along with antibiotic treatment (Access Medicine, 2013).
III. Inventory of Effective Drug Groups: Intravenous Administration
Aminoglycosides Pharmacodynamics:
Aminoglycosides
Amikcan,
inhibit protein synthesis
Gentamicin,
in susceptible bacteria
Kanamycin,
by binding to 30S and
Neomycin (Neo- 50S ribosomal subunits
Fradin®),
causing defective
Streptomycin,
bacterial cell membrane
Tobramycin
(Access Medicine,
(Tobi®) (Lexi2013; Lexi-comp,
comp, 2013)
2013).
Pharmacokinetics:
Absorption: Rapid
Metabolism: Not
reported
Excretion: Urine (98%)
(Lexi-comp, 2013).
Glycopeptides
Telavancin
(Vibativ®),
Vancomycin
(Vacocin®)
(Lexi-comp,
2013)
Pharmacodynamics:
Binds to D-alanyl-Dalanine portion of cell
wall precursor which
blocks glycopeptide
polymerization and
inhibits bacterial cell
wall synthesis (Lexicomp, 2013).
Side Effects:
Common: decreased
renal function,
hypotension,
hypertension,
neurotoxicity,
nephrotoxicity and
ototoxicity
Rare:
Allergic reaction,
dyspnea, eosinophilia,
nausea, diarrhea, urinary
retention, or rash
(Access Medicine,
2013).
Monitor:
Urinalysis, BUN, serum
creatinine, CBC, peak
and trough, vital signs,
temperature, weight,
I&O, and hearing tests
(Lexi-comp, 2013)
Side Effects:
Common:
Dyspepsia, nausea, site
irritation, flushing, and
hypotension
Rare:
Diarrhea, loss of
balance, tinnitus,
hearing difficulty,
Contraindications:
Hypersensitivity to
drug or component;
cross sensitivity
potential to
aminoglycosides (Lexicomp, 2013).
Use Caution:
Nephrotoxicity,
neuromuscular
blockade,
neurotoxicity,
superinfection, hearingimpairment,
hypocalcemia,
neuromuscular
disorders, renal
impairment, and with
sulfite use (Lexi-comp,
2013).
Contraindications:
Hypersensitivity to
drug or any component
(Lexi-comp, 2013).
Use Caution:
Nephrotoxicity,
neurotoxicity,
neutropenia,
70
PERSONAL DRUGS
Oxazolidinone
Linezolid
(Zyvox®) (Lexicomp, 2013)
Pharmacokinetics:
Absorption: Poor oral,
rapid IV
Metabolism: Not
reported
Excretions: IV: urine;
Oral: feces (Lexi-comp,
2013)
Pharmacodynamics:
Binds to bacterial 23S
ribosomal RNA of the
50S subunit which
prevents bacterial
protein synthesis.
Prevention of the
formation of functional
70S initiation complex
is completed (Clinical
Pharmacology, 2013;
Lexi-comp, 2013).
Pharmacokinetics:
Absorption: Rapid and
extensive
Metabolism: hepatic via
oxidation; minimally by
cytochrome P450
Excretion: Urine (80%)
and feces (9%) (Lexicomp, 2013)
Rifamycins
Pharmacodynamics
urinary retention, and
rash (Lexi-comp, 2013).
Monitor:
Renal function tests,
urinalysis, WBC, and
trough levels (Lexicomp, 2013).
Side Effects:
Common:
Anemia, headache,
nausea, and diarrhea.
Rare:
Dizziness, dyspnea,
illogical thinking,
balance problems,
hypoglycemia,
ecchymosis, bleeding,
fatigue, vision changes,
and rash (Clinical
Pharmacology, 2013).
Monitor:
CBC, platelet count, and
visual acuity with
chronic use (Lexi-comp,
2013).
Side Effects:
ototoxicity,
superinfections,
inflammatory bowel
disease, renal
impairment (Lexicomp, 2013)
Contraindications:
Hypersensitivity to
Linezolid or any
component, use of
MAO inhibitor within
the past two weeks,
uncontrolled
hypertension,
pheochromocytoma,
thyrotoxicosis, taking
sympathomimetics,
vasopressive agents,
dopaminergic agents,
have carcinoid
syndrome, taking
SSRIs, tricyclic
antidepressants,
serotonin 5-HT1b1d
receptor agonists,
meperdine, and
buspirone (Lexi-comp,
2013).
Use Caution:
Lactic acidosis,
myelosuppression,
peripheral and optic
neuropathy,
superinfection,
carcinoid syndrome,
diabetes, hypertension,
hyperthyroidism,
pheochromocytoma,
seizures, and serotonin
syndromes (Lexi-comp,
2013).
Contraindications:
71
PERSONAL DRUGS
Rifampin (Lexicomp, 2013)
Inhibits bacterial RNA
synthesis by binding to
beta subunit of DNAdependent RNA
polymerase and
blocking RNA
transcription (Lexicomp, 2013)
Pharmacokinetics:
Absorption: Well
absorbed
Metabolism: Hepatic;
undergoes
enterohepatic
recirculation
Excretion: Feces (6065%) and urine (~30%)
(Lexi-comp, 2013).
Streptogramins
Quinuprstin,
Dalfopristin
(Synercid®)
(Lexi-comp,
2013)
Pharmacodynamics
Inhibits bacterial
protein synthesis by
binding to different
sites on 50S ribosomal
subunit which inhibits
protein synthesis
(Access Medicine,
2013; Lexi-comp,
2013).
Pharmacokinetics:
Absorption: Not
reported
Metabolism:
Common:
Orange colored body
fluids, discolored
contact lenses,
dyspepsia, diarrhea,
dizziness, and flu-like
symptoms
Rare:
Nausea, anorexia,
jaundice, fatigue, and
rash (Lexi-comp, 2013).
Monitor:
Liver function tests,
CBC, mental status,
sputum culture, and
chest x-ray (Lexi-comp,
2013)
Substrate: Pglycoprotein,
SLCO1B1; Induces:
CYP1A2 (strong),
CYP2A6 (strong),
CYP2B6 (strong),
CYP2C19 (strong),
CYP2C8 (strong),
CYP2C9 (strong),
CYP3A4 (strong), Pglycoprotein (Lexicomp, 2013).
Side Effects:
Common:
Site irritation, headache,
nausea, diarrhea,
arthralgia, and myalgia
Rare:
Urine discoloration,
jaundice, fatigue,
ecchymosis, bleeding,
and rash (Access
Medicine, 2013).
Monitor:
Culture and sensitivity,
hepatic and renal
Hypersensitivity to
drug or any component,
concurrent use of
amprenavir and
saquinavir/ritonavir
(Lexi-comp, 2013)
Use Caution:
Flu-like syndrome,
hematologic effects,
hyperbilirubinemia,
hypersensitivity,
superinfection,,
alcoholism, hepatic
impairment,
meningococcal disease,
porphyria, and
hepatotoxicity
medications (Lexicomp, 2013).
Contraindications:
Hypersensitivity to
drug or component,
pristinamycin, or
vairginiamycin (Lexicomp, 2013)
Use Caution:
Arthralgias, myalgias,
hyperbilirubinemia,
phlebitis,
superinfection,
cisapride, and drugs
metabolized by
CYP3A4 (Access
72
PERSONAL DRUGS
nonenzymatic reactions
Excretion: Mainly
feces, some urine
(Access Medicine,
2013).
Pharmacodynamics
Sulfonamides
Interferes with bacterial
Sulfamethoxazole folic acid synthesis and
with
growth via dihydrofolic
Trimethoprim
acid formation and
(Bactrim®,
para-aminobenzoic acid
Septra®),
inhibition. Also inhibits
Erythromycin
the enzymes of the folic
with
acid pathway (LexiSulfisoxazole
comp, 2013).
(E.S.P.®),
Sulfadiazine,
Pharmacokinetics:
Sulfur with
Absorption: Almost
Sulfacetamide
completely
(Lexi-comp,
Metabolism: N2013).
acetylated and
glucuronidated; to
oxide and hydroxylated
metabolites
Excretion: Urine (LExicomp, 2013).
Miscellaneous
Aztreonam
(Azactam®,
Cayston®) (Lexicomp, 2013)
Pharmacodynamics:
Inhibits bacterial cell
wall synthesis by
binding to penicillinbinding proteins. This
inhibits final
transpeptidation step
inhibiting cell wall
biosynthesis (Clinical
Pharmacology, 2013;
Lexi-comp, 2013)
function, infusion site,
and for side effects
(Lexi-comp, 2013).
Medicine, 2013).
Side Effects:
Common:
Nausea, vomiting,
anorexia, rash, and
urticaria
Rare:
Life threatening
conditions, skin
reactions, fatigue, blood
dyscrasia, and
hepatotoxic reactions
(Lexi-comp, 2013).
Contraindications:
Hypersensitvitiy to
sulfa, trimethoprim,
erythromycin, or any
component,
megaloblastic anemia,
severe hepatic or renal
failure, and breastfeeding (Lexi-comp,
2013).
Monitor:
Culture and sensitivity,
CBC, potassium level,
creatinine, and BUN
(Lexi-comp, 2013).
Substrates: CYP2C9
(major), CYP2E1
(minor), CYP3A4;
inhibits: CYP2C9
(strong) (Lexi-comp,
2013).
Side Effects:
Common:
Nausea and diarrhea
Rare:
Dyspnea, site irritation,
and rash (Clinical
Pharmacology, 2013).
Monitor:
Liver function tests and
anaphylaxis (Lexi-
Use Caution:
Blood dyscrasias,
altered cardiac
conduction, myasthenia
gravis, skin reactions,
hepatic necrosis,
hyperkalemia,
hypoglycemia,
sulfonamide allergy,
superinfection,
leucovorin use, asthma,
hepatic and renal
impairment, thyroid
dysfunction, AIDS
population, elderly,
G6PD deficiency,
folate deficiency, and
slow acetylators (Lexicomp, 2013).
Contraindications:
Hypersensitivity to
drug or component
(Lexi-comp, 2013).
Use Caution:
Bronchospasms,
cephalosporin/penicillin
allergy, super infection,
and renail impairment
(Lexi-comp, 2013).
73
PERSONAL DRUGS
comp, 2013).
Pharmacokinetics:
Absorption: Well
absorbed
Metabolism: Hepatic
Excretion: Mostly urine
some feces (Lexi-comp,
2013).
Beta-lactamase
Clavulanic acid
with amoxicillin
(Augmentin®),
Clavulanic acid
with ticarcillian
(Timentin®),
Sulbactam with
ampicillin
(Unasyn®),
Tazobactam with
piperacillin
(Zosyn®) (Lexicomp, 2013)
Pharmacodynamics:
Binds and inhibits betalactamases allowing
other antibiotics to have
expanded spectrum
activity. Binds to
penicillin-binding
proteins preventing
peptidoglycan synthesis
and biosynthesis (Lexicomp, 2013)
Pharmacokinetics:
Absorption: Not
reported
Metabolism: Hepatic
Excretion: Urine (Lexicomp, 2013).
Side effects:
Common:
Diarrhea, rash, urticaria,
abdominal pain, nausea,
vomiting, vaginitis,
vaginal mycosis, and
moniliasis
Rare:
Alkaline phosphatase
increase, cholestatiic
jaundice, flatulence,
headache, hepatic
dysfunction, hepatitis,
increased ptothrombin
time, thrombocytosis,
and vasculitis (Lexicomp, 2013).
Monitor:
Infection and renal,
hepatic, and
hematologic functions
(Lexi-comp, 2013).
Cyclic
Lipopeptide
Daptomycin
(Cubin®) (Lexicomp, 2013)
Pharmacodynamics:
Bind to cell membrane
components and causes
rapid depolarization and
inhibited intracellular
synthesis of DNA,
RNA, and proteins
(Access Medicine,
2013; Lexi-comp,
2013).
Pharmacokinetics:
Absorption: Not
Side effects:
Common:
Diarrhea, vomiting,
constipations, edema,
chest pain, hypertension,
hypotension, headache,
fever, dizziness, anxiety,
rash, abdominal pain,
dyspepsia, increased
CPK, weakness, and
back pain
Rare:
Anaphylaxis, atrial
Contraindications:
Hypersensitivity to
drug or any component,
cholestatic jaundice,
hepatic dysfunction,
severe renal
impairment, and
hemodialysis (Lexicomp, 2013).
Use Caution:
Hypersensitivity,
bleeding disorders,
heart failure, seizures,
diarrhea, hepatic
effects, supreinfections,
infectious
mononucleosis, renal
impairment, and
phenylalanine products
(Lexi-comp, 2013)
Contraindications:
Hypersensitivity to
drug or component
(Lexi-comp, 2013).
Use Caution:
Eosinophilic
pneumonia,
hypersensitivity,
myopathy, peripheral
neuropathy,
superinfection, renal
impairment, and
74
PERSONAL DRUGS
reported
Metabolism: Not
reported
Excretion: Urine (78%),
feces (6%) (Lexi-comp,
2013).
Fluoroquinolone Pharmacodynamics:
Inhibits DNA-gryase,
Ciprofloxacin
topoisomerase and
(Cipro®),
relaxation of
Besifloxacin
supercoiled DNA. This
(Besivance®),
promotes breakage of
Gatifloxacin
double-stranded DNA
(Zymaid®),
(Lexi-comp, 2013).
Gemifloxacin,
Levofloxacin
Pharmacokinetics:
(Leevaquin®),
Absorption: Rapid
Moxifloxacin,
Metabolism: Partially
Norfloxacin,
hepatic
Ofloxacin (Lexi- Excretion: Urine (30comp, 2013)
87%), and feces (461%) (Lexi-comp,
2013).
Cephalosporins
Cefepime,
Ceftazidime
(Fortaz®,
Tazicef®) (Lexicomp, 2013)
Pharmacodynamics:
Binds to penicillinbinding proteins which
inhibits peptidoglycan
synthesis allowing cell
wall biosynthesis
inhibition (Lexi-comp,
2013)
Pharmacokinetics:
Absorption: Rapid and
complete
fibrillation, C-Diff,
pneumonia (Lexi-comp,
coma, hypomagnesium, 2013)
rhabdomyolysis, vertigo,
and vesiculobullous rash
(Access Medicine,
2013).
Monitor:
Infection, CPK, muscle
pain/weakness, and
eosiniphilic pneumonia
(Lexi-comp, 2013).
Side effects:
Common:
Dyspepsia, nausea, and
diarrhea
Rare:
Tachycardia, joint pain,
arthralgia, edema,
asthenia, parasthesia,
and rash (Lexi-comp,
2013).
Monitor:
CBC, renal function,
and hepatic function
(Lexi-comp, 2013).
Substrates: Pglycoprotein; inhibits:
CYP1A2 (strong),
CYP3A4 (weak) (Lexicomp, 2013).
Side effects:
Common:
Nausea, diarrhea, site
irritation, and vaginal
yeast infection
Rare:
Confusion, ecchymosis
and rash (Access
Medicine, 2013).
Monitor:
Culture and sensitivity,
Contraindications:
Hypersensitivity to
drug or any component
or use of tizanidine
(Lexi-comp, 2013)
Use Caution:
Myasthenia gravis,
tendon inflammation,
altered cardiac
conduction, CNS
effects, crystalluria,
glucose regulation,
hypersensitivity,
peripheral neuropathy,
phototoxicity,
superinfection, renal
impairment, rheumatoid
arthritis, seizures,
syphilis, and with
CYP1A2 substrates
(Lexi-comp, 2013).
Contraindications:
Hypersensitivity to
drug or any component,
cephalosporin,
penicillin or betalactams (Lexi-comp,
2013)
Use Caution:
Elevated INR,
neurotoxicity, penicillin
allergy, superinfection,
75
PERSONAL DRUGS
Carbapenem
Doripenem
(Doribax®),
Ertapenem
(Invanz®),
Impenem,
Cilastatin
(Primaxin®),
Meropenem
(Merrem®)
(Lexi-comp,
2013)
Metabolism: Minimally
hepatic
Excretion: Urine
prothrombin time, and
renal function (Lexicomp, 2013)
gastrointestinal disease,
renal impairment, and
seizure disorders (Lexicomp, 2013).
Pharmacodynamics:
Binds to penicillinbinding protein (PBP-2,
PBP-3, PBP-4), which
inhibits peptidoglycan
synthesis allowing cell
wall biosyntheisi
inhibition (Lexi-comp,
2013)
Side effects:
Common:
Headache, nausea,
diarrhea, anemia, and
vaginal yeast infection
Rare:
Dizziness, syncope, and
rash (Lexi-comp, 2013).
Contraindications:
Hypersensitivity to
drug, drug class, or any
component or betlactam antibiotics
(Lexi-comp, 2013).
Pharmacokinetics:
Absorption: Almost
complete
Metabolism: Non-CYP
mediated via hydrolysis
Excretion: Urine (70%);
feces (<1%) (Lexicomp, 2013).
Monitor:
Renal function, hepatic
fnction, and
hematologic function
(Lexi-comp, 2013).
Use Caution:
Hypersensitivity, CNS
effects, superinfection,
renal impairment,
ventilator assisted
pneumonia, and with
Valproic acid use
(Lexi-comp, 2013).
IV. Effective Drug Classification: Oxazolidinone IV
Drug Name
Linezolid
(Zyvox®)
(Lexi-comp,
2013)
Efficiency
Absorption: Rapid
and extensive
Protein Binding:
31%
Metabolism:
Hepatic via
oxidation of
morpholine ring to
aminoethoxyacetic
acid, and
hydroxyethyl
glycine;
minimally by
cytochrome P450
Half-life: Four to
five hours
Peak Time: Oral:
One to two hours
Safety
Drug Interactions:
Monoamine Oxidase;
alpha/beta agonists,
alpha1/2 agonits,
amphetamines,
anilidopiperidine opioids,
antidepressants,
atomoxatine, bezafibrate,
buprenorphine,
bupropine, buspirone,
carbamazepine, clozapine,
cyclobenzaprine,
dexmethyphenidate,
dextromethorphan,
diathylpropion,
hydromorphone, mao
inhibitors, maprotiline,
meperidine, methyldopa,
Suitability
-Give after
hemodialysis.
-Monitor for
hypoglycemia in
diabetic patients.
-Watch for
seizures in
patients with
history of
seizures.
-Oral: Can give
without regard to
meals.
-Avoid large
amounts of
tyramine foods.
-Time-dependent
kill
Cost
Zyvox®
Intravenou
s
(solution)
2mg/ml
(100ml):
$72.18
(Lexicomp,
2013).
76
PERSONAL DRUGS
Excretion: Urine
(~30% parent
drug, ~50%
metabolites; feces
(~9) (Lexi-comp,
2013).
methylene blue,
methylphenidate,
mirtazapine,
oxymorphine, pizotifen,
SSRIs,
serotonin/norepinephrine
reuptake inhibitors,
tapentadol, tetrabenazine,
tatrahydrozoline,
trazodone, tricyclic
antidepressants, and
tryptophan (Lexi-comp,
2013).
Increased Effect/ Toxicity:
Alpha/beta agonists,
alpha1/2 agonists,
amphetamines,
antidepressants,
antihypertensives,
atomoxatine, beta2
agonists, bezafibrate,
bupropion, clozapine,
dexmethylphenidate,
dextromethorphan,
diethylpropion,
doxaprem,
hydromorphine,
hypoglycemia agents,
lithium, meperidine,
methadones,
methlphenidate,
methylene blue,
methylphenidate,
metoclopramide,
mirtazapine, orthostatic
hypotension producing
agents, pizotifen,
reserpine, SSRIs,
serotonin 5-HT1D
receptor agonists,
serotonin/norepinephrine
reuptake inhibitors,
sympathomimetics,
tetrahydrozoline,
trazodone, tricyclic
characteristics.
-Best predictor of
efficacy is time
which
concentration
remains above the
MIC (Lexi-comp,
2013).
77
PERSONAL DRUGS
antidepressants,
altrtamine,
anilidopiperidine opioids,
antipsychotics,
buprenorphine, buspirone,
carbamazepine, comt
inhibitors,
cyclobenzaprine,
levodopa, mao inhibitors,
maprotiline,
oxymorphone, tapentadol,
tetrabenazine, tramadol,
and tryptophan (Lexicomp, 2013).
Decreased Effect/
Toxicity:
None known (Lexi-comp,
2013).
Avoid:
Alcohol, tyramine foods,
and large amounts of :
caffeine, tyrosine,
tryptophan, or
phenylalanine (Lexicomp, 2013).
V. Drug of Choice: Linezolid
The gold standard of treatment for VAP MRSA has always been Vancomycin but
efficacy is limited due to poor penetration in the alveolar lining fluid. Linezolid has had
comparable improvement rates and in some studies has slightly exceeded Vancomycin. In a
retrospective analysis Linezolid had a higher improved survival rate and clinical cure rate (Chan
et al., 2011).
For this patient Linezolid is chosen over Vancomycin because Vancomycin is considered
nephrotoxic and should be avoided in patients with existing renal impairment. Dosing for
PERSONAL DRUGS
78
Linezolid should be 600mg IV every 12 hours for the course of seven to 21 days based on the
patients clinical response. Since the patient is a dialysis patient, it is recommended that this drug
be given after hemodialysis or given early on dialysis days. Monitor glucose levels closely in
diabetic patient as this drug may cause hypoglycemia. Educate patient and family on potential
side effects, although rare. This drug has many drug to drug interactions and should be given
with caution and the patient monitored closely. For IV administrations give medication over 30120 minutes and prevent mixing or infusing with other drugs. Always make sure the line has
been flushed before and after administration with normal saline. Monitoring of the patient
should include weekly complete blood count and visual test if patient remains on the drug for
over three months or develops any visual symptoms (Access Medicine, 2013). This drug costs
$72.18 for 100ml dose with the concentration being two mg/ml (Lexicomp, 2013). An advance
practice nurse with a current CTP may prescribe this drug only when it has been physician
initiated or written in the standard care arrangement with the collaborating physician as a
physician consulted drug (Ohio Board of Nursing, 2013).
79
PERSONAL DRUGS
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