1
Bone and Muscle
2
Musculoskeletal
Diseases/Disorders
 Bursitis—inflammation of the small, fluid-filled
pouches between bones
 Tendonitis—inflammation of the cords of
connective tissue that attach muscle to bone
 Myalgia—muscle pain
 Rheumatoid Arthritis—an autoimmune disorder
 Osteoarthritis—caused by physical degeneration
of connective tissue
 Gout—caused by crystals of uric acid in blood
 Bone and Muscles tend to be rich in neurons that
transmit pain
3
Treatments
Gout
 Colchicine used to alter ability of phagocytes to
attack uric acid crystals
 Anti-inflammatory analgesics can be used to
reduce pain and inflammation
Inflammation
 Salicylates relieve inflammation by inhibiting the
synthesis of prostaglandin
 Topical corticosteroids treat most causes,
including chemical, mechanical, microbiological,
and immunological
4
Analgesics
 Narcotics
 MOA: bind to opiate receptors in brain and spinal cord
 Indications: Analgesia
 Main Side effects: N/V, constipation, physical and
psychological dependence. In overdose , respiratory
depression.
 See text for complete list.
 Fentanyl is available as a IV injection, patches, oral lozenges
but not as a tablet
 Oxycodone is not available as an injection only orally
 High potency opiates include fentanyl, remifentanil and
hydromorphone (Dilaudid®) . High risk of overdose
 Combination product: Tylenol with Codeine denoted as
follows



Tylenol#2 as Codeine 15 mg/APAP 300 mg
Tylenol #3 as Codeine 30 mg/APAP 300 mg
Tylenol#4 as Codeine 60 mg/APAP 300 mg
Skeletal Muscle Relaxants
 MOA: may block action of calcium in muscles
 Indications: painful muscle spasms, neurological
spinal cord injury
 Main Side Effects: Drowsiness, weakness
Generic
Brand
Cyclobenzaprine
Flexeril
Methocarbamol
Robaxin
Baclofen
Lioresal
Musculoskeletal Pharmaceuticals
 ASA (acetylsalicylic acid)
 Relieves inflammation by inhibiting the synthesis of
prostaglandin
 Salicylates are also used as analgesics and antipyretics
 NSAIDs (nonsteroidal anti-inflammatory drugs)
 Inhibit or block the enzyme that starts the reaction of
inflammation by making prostaglandin
 COX-2 inhibitors
 Block only the cyclooxygenase II that makes PGE-2, but
not C-1 (PGE-1)
 Inflammation is inhibited, but not the viscosity of the
mucosal linin
7
Non Steroidal Anti Inflammatory
Drugs
 Called the NSAIDS
 Excellent drugs for pain relief and reducing fever and inflammation
 Developed as an alternative to corticosteroids
 MOA: blocks the COX enzyme to block prostaglandin formation
 Side effects are: severe GI bleeding (possible), GI upset and gastritis, kidney
insufficiency, edema and elevated blood pressure, hyperkalemia risk
Generic
Brand
Ibuprofen
Motrin, Advil
Naproxen
Naprosyn
Ketorolac
Toradol (IV available)
Diclofenac
Voltaren
Celecoxib
Celebrex (COX2
inhibitor)
Musculoskeletal Pharmaceuticals
 Bisphosphonates—indicated for osteoporosis
 Mimic the natural organic bisphosphonate salts found
in the body
 Inhibit bone resorption and osteoclast activity
 Restore bone mass and density
 Risedronate (Actonel)
 Ibandronate (Boniva)
 SERMs (selective estrogen receptor modulators)
 Indicated for postmenopausal women
 Protective effect on bones and heart
 Raloxifene (Evista)
 Skeletal muscle relaxants—used to relax specific muscles
in the body
 Relieve pain, stiffness, and discomfort
 Block muscle contraction at the neuromuscular junction
9
10
The Respiratory System
 Divided into the upper respiratory tract and the lower
respiratory tract
 The upper respiratory tract consists of:
 Nose or nasal cavity
 Paranasal sinuses
 Pharynx and larynx
11
The Respiratory System (cont.)
 The lower
respiratory tract
consists of:
 Trachea
 Two lungs
 Two main bronchi
12
The lower respiratory tract.
13
Common Cold
 Caused by a viral infection that inflames the membranes in
nose and throat
 Antibiotics will not cure a cold or any other viral infection
 Treatment is considered symptomatic
Cough
 May be a symptom of a cold, flu, respiratory problems, or
nonrespiratory diseases
 Most likely begins with an irritation of nerves in the
respiratory tract
 Nonproductive cough treated with cough suppressant
 Productive cough treated with an expectorant
14
Allergies and Asthma
Allergies
 Caused by the immune system reacting to a substance that
does not cause disease
 Treatment may be palliative, with antihistamines and
antitussives
 Treatment may be preventive, with mast cell stabilizers
Asthma
 Chronic respiratory disease
 Characterized by inflammation of airways, tightening of
muscles around airways
 Treatment is palliative with albuterol and other
bronchodilators
15
Nasal Congestion and Rhinitis
Nasal Congestion
 Inflamed, stuffy nose
 Treatment may be palliative, to promote easier breathing
 Indications for use of decongestants are nasal and bronchial congestion
Rhinitis
 Inflammation of nasal membranes, and/or runny nose
 Common component of colds and allergies
 Treatment is considered symptomatic
 Drugs to treat include:
Generic
Brand
Oxymetazoline
Afrin Nasal Spray
Phenylephrine
NeoSynephrine Nasal
Spray
Fluticasone
Flonase (Nasal Steroid
preparation)
Mometasone
Nasonex (Nasal Steroid
preparation)
Oxymetazoline and Phenylephrine are sympathomimetic and can raise
blood pressure. They also should be used with caution in gluacoma
patients
16
Chronic Obstructive Pulmonary
Disease (COPD)
 Umbrella term for emphysema and chronic bronchitis, and asthma
 Characterized by partially blocked bronchi and bronchioles, mucus
plugging and bronchoconstriction
 Causes shortness of breath
 Treatment may be palliative, with bronchodilators
 Beta Agonist Drugs
Generic
Brand
Albuterol
Proventil
Pirbuterol
Maxair
Salmeterol
Serevent
Formoterol
Foradil
Levalbuterol
Xopenex
Albuterol and Pirbuterol and Beta 2 agonist but can cause tachycardia in
some people.
All of the above drugs are available as MDI
Formoterol is beta agonist available as a capsule
17
Drugs used for COPD
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 Anticholinergic (Antimuscarinic) Drugs
 Act on muscarinic (cholinergic) receptors as antagonists
 Results in bronchodilation
Generic
Brand
Ipratropium
Atrovent
Ipratropium + Albuterol
Combivent
Tiotropium
Spiriva
19
Steroid / Beta Agonist
 Combination products
 These products are not meant as “rescue” agents but
for chronic long term use in prevention of COPD
 Available as MDI and for Advair as dry powdered
inhaler as well
 Patients should rinse after use to prevent oral fungal
infections
Generic
Brand
Fluticasone-Salmeterol
Advair Diskus
Budesonide-Formoterol
Symbicort
20
Leukotriene antagonists
 Drugs block the action of leukotrienes on their
receptors
 Leukotrienes are potent bronchoconstrictors in COPD
 Contraindicated in patient with hepatic disease
Generic
Brand
Montelukast
Singulair
Zafirlukast
Accolate
Zileuton
Zyflo CR
21
Steroid Products for COPD or
Rhinitis
Generic
Brand
Dose Form
Beclomethasone
Beconase AQ
Nasal Inhaler
Fluticasone
Flovent ®, Flonase®
Inhaler, Nasal Product
Methylprednisolone
Medrol
Tablets
Prednisolone
Pediapred, Orapred
Oral liquid, tablet
Triamcinolone
Nasacort AQ
Nasal Inhaler
22
Mucolytic Agents
 Used to thin bronchial mucus and secretions from
COPD and other lung diseases
Generic
Brand
Special
Consideration
Acetylcysteine
Mucomyst
Used for many
lung conditions;
used for
acetaminophen
overdose; has a
horrible scent
and flavor
Dornase Alfa
Pulmozyme
Used primarily
for cystic fibrosis
23
24
The heart.
25
Anatomy of the Heart
 Composed of four chambers: two upper and two lower
 Atria—top two chambers
 Ventricles—bottom two chambers
 Septum—divides heart into right and left sides
26
Valves of the Heart
 Tricuspid valve—located between the right atrium and
the right ventricle
 Pulmonary valve—located between the right ventricle
and the pulmonary artery
 Mitral or bicuspid valve—located between the left
atrium and the left ventricle
 Aortic valve—located between the left ventricle and
the aorta
27
Layers of the Heart
 Pericardium—fluid-filled sac that surrounds and
protects the heart
 Permits free movement of the heart during contraction
 Endocardium—innermost wall layer; covers the inside
surface of the heart
 Myocardium—surrounds heart and causes chamber
contractions
28
Function of the Heart
 Provides oxygenated blood throughout the body by a
pumping mechanism
 Oxygenated blood deposits materials necessary for
growth and nourishment
 Receives from tissues the waste products resulting
from metabolism
29
Hypertension
 Sustained elevation of systemic arterial blood pressure
 Symptoms include:
 Severe headache
 Chest pain
 Irregular heartbeat
 Fatigue
• Pharmaceutical treatment includes diuretics, vasodilators,
ACE inhibitors, beta blockers, and calcium channel
blockers
30
Congestive Heart Failure
 Heart pumps out less blood than it receives
 Results in weakened and enlarged heart
 Symptoms of CHF include:
 Upright posture or leaning forward
 Anxiety and restlessness
 Cyanotic and clammy skin
 Persistent cough
 Rapid breathing
 Fast heart rate
 Edema of the lower limbs
• Pharmaceutical treatment includes cardiac glycosides,
diuretics, vasodilators, ACE inhibitors, beta-adrenergic
blockers, and phosphodiesterase inhibitors
31
Coronary Artery Disease
 Occurs when there is insufficient blood flow to the heart
 Can lead to:






Angina
Heart attack
Arrythmias
Stroke
Pulmonary embolism
Heart failure
 Early CAD is closely monitored and symptomatic relief is
given by the use of nitroglycerin and other nitrate drugs.
 NTG
 ISDN (isosorbide dinitrate)
 Once CAD has progressed to the point where a patient has
angina at rest. Two procedures can be taken
 PCI with stents
 CABG (Coronary artery bypass graft)
32
Cardiovascular Pharmaceuticals
 Antiarrhythmic drugs—restore normal rhythm
patterns but do not cure the cause of the irregular
heartbeat
 Cardiac glycosides—used to increase the force of
myocardial contraction, without causing an increase in
the consumption of oxygen
 Diuretics—used to eliminate excess sodium and water
via the urinary tract
 Vasodilators—allow more blood to exit the heart,
preventing or mitigating congestion; lower blood
pressure
33
Cardiovascular Pharmaceuticals
(cont.)
 Angiotensin-converting enzyme inhibitors (ACE
inhibitors)—lower high blood pressure; thought to
reshape the heart; prevent the body from producing
natural vasodilators
 Angiotensin II receptor blockers—similar to ACE
inhibitors; block the body’s natural vasodilators
 Beta-adrenergic blockers—used to block cells from
receiving natural vasoconstrictors
 Platelet aggregation inhibitors—reduce the ability of
the blood to coagulate
34
Cardiovascular Pharmaceuticals
(cont.)
 Anticoagulants—prevent clots from forming or
existing clots from getting bigger
 Tissue plasminogen activators—break down blood
clots by reversing the clotting order and interfering
with the synthesis of various clotting factors
 Thrombin inhibitors—inactivate bound thrombin by
binding to the enzyme and blocking its interaction
with its substrates of fibrin
 Antihyperlipidemics—help prevent the progression of
coronary artery disease by lowering plasma lipid levels
35
Cardiovascular Drugs
 Beta Blockers: drugs that block the beta receptors in
the heart which blocks attachment of norepinephrine
and results in bradycardia and reduced blood pressure.
 ACE inhibitors (angiotensin converting enzyme
inhibitor) blocks the enzyme (ACE) responsible to
converting angiotensin I to angiotensin II (ATII). ATII
is a potent vasoconstrictor in humans This drug is
important in hypertensive patients and patients with
CHF and MI. ACEI are also important in preservation
of kidney function in diabetics
 Antianginal agents: used to widen coronary arteries to
increase myocardial oxygen delivery and reduce chest
pain. Examples: nitroglycerin (NTG), and isosorbide
(Imdur®, Isordil®)
 Calcium channel blockers: blocks the entry of calcium
ions in the heart muscle and in the muscle that control
blood vessel diameter. Reduced heart rate and reduces
blood pressure. Some are used to control a type of
cardiac arrhythmia called atrial fibrillation. Examples:
Diltiazem (Tiazac®, Cardizem®), amlodipine
(Norvasc®)
 Antiarrhythmial agents: block the entry of sodium into
the heart. The drugs in this class have several
mechanisms of action. Examples: Lidocaine,
amiodarone (Cordarone®), Procainamide (Procanbid®)
 Angiotensin 2 Receptor blockers (ARB’s): similar
to ACEI except these drug works on a receptor for
ATII
 Anticoagulation agents: drugs that block the
formation of blood clots. Different mechanisms of
action. Examples: warfarin (coumadin®),
dibigatran (Pradaxa®)
 Antiplatelet agents: drugs that block the action of
platelets in the formation of a blood clot. Used in
the prevention of stroke or MI. Examples:
(Plavix®) and Aspirin (Ecotrin®)
 Cardiac glycosides: drugs used to boost the
strenght of the heart’s contraction. Example:
Digoxin (Lanoxin®)
Alpha Receptor blockers
 MOA: blocks alpha receptors on smooth muscle in the
arteries
 Indication: blood pressure control
 Side effects: edema, dizziness
 Examples
 Prazosin (Minipress)
 Terazosin (Hytrin)
 Doxazosin (Cardura)
 The following alpha blockers are used for enlarged prostate
symtom relief
 Tamsulosin (Flomax)
 Alfuzoxin (Uroxatral)
 The following drugs are both alpha and beta receptor
blockers
 Labetolol (Trandate)
 Carvedilol (Coreg)
Anticoagulants
 Do not thin out the blood
 Prevent clots from forming
 Prevent existing clots from getting bigger
 Cannot dissolve existing blood clots
40
Warfarin
 Oral drug of choice
 Works by preventing the synthesis of clotting factors II, VII, IX,
and X
 Used in the long-term prevention or management of venous
thromboembolic disorders, including:
 Deep vein thrombosis
 Pulmonary embolism
 Clotting associated with atrial fibrillation and prosthetic
heart valves
 Vitamin K may be used as an antidote when too much warfarin
has been given
 For immediate correction of bleeding: fresh frozen plasma is
required
 Testing of bleeding is required for therapy test is called INR
 For most conditions INR should be between 2-3, INR in the
range of 5 or more requires vitamin K
41
Heparin
 Parenterally administered drug of choice
 Works by inactivating clotting factors IX, X, XI,
and XII
 Used prophylactically to:
 Prevent and treat deep vein thrombosis
 Prevent and treat pulmonary embolism
 Treat thrombophlebitis
 Prevent clotting during cardiac and vascular surgery
• The only antidote for heparin overdose is protamine
sulfate
• PTT testing is required
42
Low Molecular Weight Heparins
 Drugs that a similar to heparin
 Used as IV or SubQ injections
 PTT test not required
 Protamine sulfate is antidote
Generic
Brand
Enoxaparin
Lovenox
Dalteparin
Fragmin
Tinzaparin
Innohep
43
Newer anticoagulants
 Used primarily for anticoagulation for atrial
fibrillation
 Does not required INR testing like warfarin
 Less drug interactions
 Can’t be reversed by vitamin K
Generic
Brand
Special
Consideration
Dabigatran
Pradaxa
Must be dispense
in original
container
Rivaroxaban
Xeralto
NA
Apixaban
Eliquis
NA
44
Cholesterol and Triglycerides
 HDL—high-density lipoproteins or “good” cholesterol
 LDL—low-density lipoproteins or “bad” cholesterol
 Triglycerides—a form of energy stored in adipose and muscle tissues
 Often measured to depict fat ingestion and metabolism
 Can be used to assess CAD risk factors
 Statins- drugs used to lower LDL cholesterol
Generic
Brand
Atorvastatin
Lipitor
Simvastatin
Zocor
Fluvastatin
Lescol
Rosuvastatin
Crestor
Major: Side effects are nausea, GI and a reaction called Rhabdomyolysis
and myopathy where patient experiences muscle pain and at the extreme
renal failure and hospitalization
Statins are drug interactions with medications that block the liver’s CYP450
systems: Diltiazem, amiodarone, HIV protease inhibitors, Ketoconazole
45
Generic
Brand
Simvastatin + Ezetimibe
Vytorin
Lovastatin + Niacin
Advicor
Simvastatin + Niacin
Simcor
Above medications are combination products that contain a
statin + one other drug. Exetimibe is a drug that block enteral
absorption of cholesterol. Niacin is a B vitamin used to high
doses to alter metabolism of triglycerides and raise HDL
One unique combination product is Caduet, which is a
combination of Atorvastatin and Amlodipine (calcium channel
blocker ). This product is used to treat metabolic syndrome
46
 Non Statin Antilipidemic drugs
 Other drugs that target lowing VLDL, triglycerides, and
raising HDL have a beneficially affect on coronary artery
disease
Generic
Brand
Indications
Gemfibrozil
Lopid
High VLDL
Fenofibrate
Tricor
High VLDL, low
HDL
Niacin
Niaspan
High VLDL, low
HDL
Omega 3 Fatty
acid
Lovaza
High VLDL, low
HDL
47
Drugs used in the Treatment of MI
 MI is a myocardial Infarction. Heart attacks occurs
because a arterial plaque raptures and triggers the
coagulation cascade completely occudding a coronary
artery. This cause necrosis of the heart muscle.
 If not treated MI result in death from cardiogenic shock
 Even if treat mortality is high from secondary ventricular
fibrillation
 Even if treated, patient will suffer irrevocable heart damage
resulting in CHF and/or damage to cardiac conduction
system leading to pacemaker or ICD placement
 The main goal is to relieve the blood vessel of the clot and
reestablish coronary blood flow
 Can use “clot busters” drugs or have percutaneous coronary
intervention (PCI) which the femoral artery undergo
catherization and a probe is guide to the site of occlusion
and a ballon is inflated to push aside the clot
48
Generic
Brand
Use
Aspirin
Ecotrin
To stop platelet action at
the clot
Clopidogrel
Plavix
To stop platelet action at
the clot
Ticagrelor
Brilinta
To stop platelet action at
the clot
Nitroglycerin
Various
To vasodilate coronary
artery to relieve pain
Tissue plasminogen
activator
TPA
Alteplase (Activase)
Reteplase (Retavase)
Tenecteplase (Tnkase)
Activate plasmin, a
blood protein that
opens blood clots
Heparin
N/A
A potent blood
anticoagulant that stop
further coagulation
Metoprolol
Lopressor
A beta blocker that
slows heart rate and
slows spread of
infarction
49
Drug used in the treatment of
Atrial Fibrillation
 Atrial Fibrillation is a heart rate disturbance in which the
atrium/ atria are beating extremely rapidly
 Can lead to cardiogenic shock if the rate reaches the ventricles
 Therapy is aimed blocking this rate disturbance from reaching
the ventricles (called rate control), preventing blood clots in the
heart muscle wall from forming embolus (anticoagulation), and
eventual cardioversion
 Rate control




Diltiazem
Verapamil
Beta blockers
Amiodarone
 Anticoagulation
 Warfarin
 Apixaban (Eliquis)
 Cardioversion
 Ibutilide (Tikosyn)
 High dose Amiodarone
50
Beta Blockers
 Very useful in extending the life expectancy of patients
post MI and in CHF patients
 Due to evidence from clinical trials like the
Scandinavian Timolol study and the BHAT (beta block
heart attack trial with propranolol) beta blocker are
now an important drug in the therapy of post MI
patients
Generic
Brand
Propranolol
Inderal
Metoprolol
Lopressor
Timolol
Blocadren
Atenolol
Tenormin
Carvedilol
Coreg
51
ACE Inhibitors
 Used to decrease mortality in post MI and CHF
patients
 Used with beta blockers and often in combination
with them
Generic
Brand
Captopril
Capoten
Enalapril
Vasotec
Lisinopril
Zestril, Prinivil
Benazapril
Lotensin
Ramipril
Altace
Potassium levels should be monitored
ACE inhibitors are pregnancy category X
May cause relentless coughing in some patient requiring
discontinuation due to potent edema and closure of the airway
52
ACE inhibitors combination
products
 Often ACE inhibitors are combined with diuretics to
negate the potassium loss and to synergize to lower
blood pressure more
Generic
Brand
Lisinopril + HCTZ
Prinzide
Enalapril + HCTZ
Vaseretic
Benzapril + HCTZ
Lotensin HCT
53
Angiotensin Receptor Blockers
 Similar to ACEI but works at a receptor for angiotensin
2
 If patient has angioedema to ACEI; ARB’s can be tried
 Used in MI and renal disease, HTN and CHF
Generic
Brand
Losartan
Losartan + HCTZ
Cozaar
Hyzaar
Valsartan
Valsartan + HCTZ
Diovan
Diovan HCT
Irbasartan
Irbasartan + HCTZ
Avapro
Avalide
54
The renal system.
55
The Renal System
 Composed of two kidneys, two ureters, one bladder,





and the urethra
Filtering system of the kidneys is composed of millions
of nephrons
Waste from food and drug metabolization is filtered
through the nephrons
Wastes exit the kidneys as urine via the ureters
Ureters lead to the bladder, where urine is stored until
released
The kidneys are located in the posterior abdomen just
above the waist
56
Diuretics
 Drugs that work at the kidney to help remove sodium,
water, calcium, and potassium from the body. Each
class of diuretic is named for the most part according
to its mechanism of action or the site of action in the
kidney.
 Loop Diuretics work in a section of the kidney called
the loop of henle. This is where most of the water and
sodium and potassium is lost from the body. These
drugs are used to treat edema in CHF patients and
other patient that hold on the water.
 Example(s): Furosemide (Lasix®), Torsemide
(Demadex®)
 Carbonic anhydrase inhibitors act on the proximal
tubule of the kidney by blocking the enzyme, carbonic
anhydrase which cause sodium retention and acid loss.
 Example: acetazolamide (Diamox®)
 Carbonic anhydrase inhibitor are pretty much weak
diuretics and can produce profound lose of potassium
Thiazide Diuretics
 Thiazide diuretics act on the distal convoluted tubule
to block the NaCL cotransporter in the kidney.
 Generally good diuretics
 Produce a sodium rich urine
 Example: Hydrochlorothiazide (HydroDiuril®)
Potassium Sparing diuretics
 Most of the above diuretics cause profound lose of
potassium. To circumvent this, these diuretic are
usually taken with potassium supplements.
 A class of diuretic that “spares” potassium in the body
are know and are used for many indications
 Examples are: spironolactone (aldactone®), Amiloride
(Midamor®), and the ACE inhibitors with ARB’s.
 These diuretics unlike the ones mentioned before
should not be used with a potassium supplement.
Drugs for Kidney Disorders
 Failing kidneys cause disorders relating to retention of
toxins in the blood, acidity and electrolytes
abnormalities
 Kidney disorders effects blood potassium, calcium,
phosphate levels, and levels of various hormones in
the body.
 Patients have high PTH levels
 Low vitamin D levels
 Low erythropoetin levels
 Patients have high levels of urea and other nitrogenous
toxin that causes damage to the CNS
61
 Drugs to lower patient’s potassium levels
 K binding resins


Kayexalate ® is sodium polystrene sulfonate resin and bind K
in the GI prevent absorption
In emergency situation, where life threatening hyperkalemia
exists the following is given (in a hospital ICU)
 Insulin 10 units IVP
 Calcium choride 10% 300 mg -1 gram IVP
 Albuterol USP solution
 Kayexalate 30 g orally
 Drug that lower phosphate levels
 Sevelamer (Renagel®, Renvela ®
 Lanthanum Carbonate
 Calcium Acetate (Phoslo ®)
62
 Drugs used to correct PTH levels (secondary
hyperparathyroidism)
 Calcitriol (Calcijex, Rocaltrol®)


IV form is given with dialysis
Oral capsule (Rocaltrol ) is given as maintanence tx outpatient
 Paricalitol

Zemplar ® (IV form given with dialysis)
 Drugs used to correct renal induced red blood cell
anemia
 Epogen® (Erythropoetin)
 Procit ® (erythropoetin)
 Aranesp ® (darbepoetin)
63