Introduction to Pharmacology
Listed below are some of the terms you should be familiar with for the exam.
The list concentrates on the drugs and drug categories that will be covered on
the exam. I have tried to categorize the drugs according to the diseases that they
are prescribed for, and which systems the diseases affect. However, many
drugs can be prescribed for completely different diseases. For example, many
anti-cancer drugs are really antibiotic or antiviral. I have done the best that I can
to organize these for you, and where there are clearly more than one use, I have
put them in the “other” category. Remember that you will also need to know the
names of hormones, neurotransmitters and other compounds in the body that
these drugs work on that are not on this list.
NEURO
DRUGS FOR MOVEMENT DISORDERS
Leva-dopa (L-Dopa): commonly used for Parkinson’s disease; a chemically
modified form of dopamine that can cross the blood brain barrier where it
converts to dopamine then goes to the basal ganglia. L-dopa converts quickly
into dopamine prior to entering the brain, so high doses are required for
therapeutic effect, may be neuroprotective
Carbidopa: when combined with Leva-dopa (combo called Sinamet), it prevents
the conversion of L-dopa into dopamine so more L-dopa reaches the brain;
allows lower doses of L-dopa and less side effects
Sinemet: combination of Leva-dopa and Carbidopa (refer to two drugs); Major
side effects include nausea, abnormal muscle tone, tremors, confusion,
hallucinations, cardiac arrhythmias, hypotension and dyskinesia (PD)
Amantadine: Parkinson’s; usually given with L-Dopa to facilitate release of
endogenous dopamine (other drugs like it bromocriptine aka parlodel, pergolide
aka permax); side effects include: orthostatic hypotension, depression,
hallucinations, nausea, vomiting, confusion and insomnia
Selegiline (Deprenyl): antioxidant used for Parkinson’s; inhibit monoamine
oxidase, preventing the breakdown of dopamine; limit the level of free radicals in
the area, may be neuroprotective
Rasagiline: antioxidant used for Parkinson’s disease; approved by FDA in 2008
DRUGS FOR EPILEPSY
Barbiturates (ex. phenobarbital): used to treat epilepsy, anxiety, insomnia; bind to
the GABA receptor to open chloride channels (decrease neuronal firing); main
side effect is sense of sedation and may cause uncoordinated movements; very
low therapeutic index; best used for partial and generalized tonic-clonic seizures
Phenobarbital: barbiturate prescribed for all seizure types. Primidone is
converted into phenobarbital. See barbiturates
Benzodiazepine (ex. Diazepam aka Valium, Klonopin): drug of choice for antianxiety drugs (also insomnia, epilepsy); potentiate the effects of GABA; inhibitory
drug that hyperpolarizes the neuronal membrane; side effects: sedation, ataxia,
behavioral changes; drug dependence; safer than barbiturates; only metabolized
in the liver; signs of overdose: sleepiness, confusion, dizziness, loss of memory
Dilantin: non-sedative anti-epileptic drug on market; drug interferes with
movement of sodium across the membrane (stabilized membrane – lower neuron
firing); most effective against partial and generalized tonic clonic seizures; side
effects: dizziness, drowsiness, uncoordinated movement, blurred vision, anemia,
water retention, cardiac arrhythmias, CHF; bind quickly to albumin; only
metabolized in the liver; signs of overdose: sleepiness, confusion, blurred vision,
ataxia
Carbamazepine: used to treat epilepsy and depression; one of the tricyclic
compounds; works through sodium channels and acts on the presynaptic neuron
to inhibit synaptic transmission
Vigabatrin: designed to enhance the natural effect of GABA; used to treat partial
seizures; signs of toxicity: drowsiness, dizziness, weight gain
Ethosuximide: used for absence seizures; succinimide drug; acts on the calcium
channels and on the sodium-potassium ATPase; side effects: gastric issues,
headaches, dizziness, euphoria
Valproic acid: free fatty acid that blocks high frequency brain activity; effective
with absence and generalized tonic-clonic seizures; side effects: nausea,
vomiting, GI complaints
DRUGS FOR MULTIPLE SCLEROSIS
Betaseron: interferon best prescribed for the early diagnosed person with a form
of relapsing-remitting Multiple Sclerosis; molecule thought to inhibit immune
system from attacking itself; decreases the number and frequency of
exacerbations; injected
Novantrone (Mitoxantrone): immunosuppressant approved for relapsing-remitting
MS getting progressively worse (secondary-progressive MS); most effective in
reducing number of lesion forms on nerves; side effects: heart damage; injected
DRUGS FOR ANXIETY
Luvox, Praxil, Prozac, Zoloft: drugs prescribed for panic disorders (generalized
panic disorder and PTSD); serotonin reuptake inhibitors (block reuptake of
serotonin)
Prozac, Zoloft: see above; these can also be used as antidepressants in bipolar
disorder
DRUGS FOR INSOMNIA
Ambien: treat insomnia without harsh side effects; nonbenzodiazepine: acts on
benzodiazepine receptor (not whole receptor); affect wear off over time
Estorra: see Ambien; stays in bloodstream 6-7 hours so it is good when people
have difficulty staying asleep
Indiplon: nonbenzodiazepine used for insomnia; works fast and does not induce
sleepiness during the day
ANTI-PSYCHOTIC DRUGS
Phenothiazines, Thioxanthenes: 2 of 5 anti-psychotic classifications; block
dopamine receptors but are not specific to the limbic system alone; side effects:
tardive dyskinesia, pseudo Parkinson’s, akathisia, dyskinesia
Haldol (Haloperidol): in a different antipsychotic classification; see above; can
treat manic phase of bipolar disorder
ANTIDEPRESSANTS
Tricyclic Antidepressants: impair the reuptake of amine transmitters back into
the presynaptic terminal; neurotransmitter in the synapse longer and
overstimulation of the post-synaptic neuron; side effects: sedation, confusion,
delirium, tachycardia, dry mouth, urinary retention
MAO inhibitors: antidepressants that act on the enzymes that normally degrade
amine neurotransmitters and remove it from the synaptic cleft; allows more
neurotransmitter to remain; side effects: restlessness, irritability, agitation,
insomnia, hypertension
DRUGS FOR ALZHEIMER’S DISEASE
Aricept, Exelon, Reminyl: these help relieve cognitive symptoms of Alzheimer’s
disease; cholinesterase inhibitors prevent breakdown of acetylcholine (important
in memory and reasoning); rare side effects: nausea, vomiting, loss of appetite,
diarrhea
Memantine: treatment for AD; drug is an antagonist of the NMDA receptor on the
post-synaptic neuron. Blocks excessive glutamate (which uses NMDA receptor);
neuroprotective; moderate to severe AD; side effects: hallucinations, confusion,
dizziness and headaches
DRUGS FOR BIPOLAR DISORDER
Lithium: treatment for bipolar disorder; ion that enters the cell through neuronal
sodium channels, but doesn’t have a specific target; may decrease release of
amine neurotransmitters, increase their reuptake, or reduce production of
another messenger; side effects: metallic taste, resting hand tremor, diarrhea,
nausea/vomiting, slurred speech, dizziness, increased muscle tone, confusion
Depakote: an anticonvulsant that helps bipolar disorder, specifically the manic
phase; side effects: nausea, dizziness, vomiting, stomach pain, rash
CARDIOVASCULAR
DRUGS ACTING ON THE AUTONOMIC NERVOUS SYSTEM
Beta blockers (ex Labetolol (G), Zebeta (T), Cargard (T), Inderal (T)): block the
binding of norepinephrine to the beta adrenergic receptors (G protein) of the
heart and thus they slow the heart beat and force of contraction (antagonist to
block sympathetic activity); this also blocks the G proteins cascade of ionotropic
(K+ channels) and chronotropic (Ca+ channels) activation; only metabolized in
the liver; signs of overdose: hypotension, slowed HR; treatment: HTN, cardiac
arrhythmias; side effects: fatigue, hypotension, excessive slow heart rate and
contractility; possible increase in lipid profile and promotion of insulin
resistance/glucose intolerance; class II anti-arrhythmia drug
Labetalol: see above; has both beta blocking and alpha adrenergic-blocking
effects; decreases HR and contractility (beta) and decreases peripheral vascular
resistance (alpha)
Alpha-1 Blocker (ex. Cardura (T)): binds to and blocks alpha adrenergic
receptors of the sympathetic NS, primarily on cells of the vasculature, resulting in
increased blood flow and decreased BP; for severe or advanced stages of HTN;
positive effect on glucose and lipid metabolism unlike beta blocker; side effects:
generalized hypotension, orthostatic hypotension and reflex tachycardia
DRUGS THAT ACT DIRECTLY ON HEART AND VASCULAR SMOOTH
MUSCLE CELLS
Calcium Channel Blockers (ex. Diltiazem (G) aka Cardizem (T), Nicardipine (G),
Verapamil (G), Procardia (T)): block the voltage-gated Ca+ channels in smooth
muscle cells to allow relaxation of vessels and increase in blood flow, decrease
in BP; also blocks Ca in muscle cell so decreases chance of contraction; similar
negative iontropic effects to beta-blockers; side effects: swelling in feet/ankles,
orthostatic hypotension, headaches, nausea; should be avoided by people with
SA or AV abnormalities; can be used for certain cardiac arrhythmias (especially
Diltiazem and Verapamil); class IV anti-arrhythmia drugs
Sodium Channel Blockers (ex Lidocaine (G) aka Xylocaine (T), Norpace (T),
Tambocor (T), Quinidine (G)): first class of drugs used to treat arrhythmias; treat
atrial fibrillation or flutter, ventricular tachycardia, paroxysmal supraventricular
tachycardia; decrease membrane automaticity, slow impulse conduction through
myocardium and prolong refractory period
Potassium Channel Blockers (ex. Amidarone (G) aka Cordarone (T)): class III
anti-arrhythmia drugs; treat atrial fibrillation or flutter, paroxysmal supraventricular
tachycardia and ventricular tachycardia
Digitalis (Digoxin (G) aka Lanoxin (T)): drug prescribed for heart failure;
increases myocardial contractility by blocking the Na/K pump which drives the
Na/Ca exchange so more Ca is brought into the cell and force of contraction is
increased; slows HR and normalizes autonomic influence (decrease sympathetic,
increase parasympathetic); don’t use in combo with Ca Channel Blockers; low
therapeutic index (small margin of safety) so toxicity is common; improves left
ventricular performance during exercise (higher ejection fraction and systolic BP)
Nitroglycerine: organic nitrate that is used for angina pectoris; it dilates coronary
arteries, ameliorates myocardial ischemia, minimizes left ventricular remodeling
and reduces mortality in patients with acute MI; decrease myocardial oxygen
demand; metabolized into NO which is a vascular smooth muscle relaxant that
dilates vessels; sublingual or patches; side effects: headaches, dizziness,
orthostatic hypotension; possible tolerance; onset of action 10-45 min lasting 4-6
hours
DRUGS FOR THE RENAL SYSTEM
Diuretic: can increase the excretion of Na+ and water by the kidneys, producing a
decrease in blood volume; decrease in fluid improves dyspnea and alleviates
swelling; also reduces resistance in peripheral vessels secondary to vasodilation;
treat HTN; potential hypokalemia so take potassium supplements; 3 categories:
thiazides, loop diuretic, and K-sparing agents; side effects: fluid and electrolyte
imbalance, may effect glucose intolerance and insulin resistance
K+-sparing (ex. Aldactone (T)): work at the distal tubule
Loop diuretics (ex. Bumex (T), Lasix (T)): work at the thick ascending limb
of the Loop of Henle
Thiazides (ex. Diuril (T)): work at the distal tubule
Angiotensin-converting enzyme (ACE) inhibitors (ex. Lotensin (T), Vasotec (T),
Altace (T)): powerful drugs, most preferred for cardiac problems; prevent the
conversion of angiotensin I to angiotensin II and increases serum aldosterone
levels, results in sodium retention; decreases blood pressure and peripheral
resistance; they prevent or may reverse structural changes in large and small
vessels throughout the vascular system, leading to improved vascular
compliance; can cause allergic reaction (skin rash) or persistent dry cough
Avapro (T): like ACE inhibitor but block the receptor that angiotensin II normally
would bind; still inhibits vasoconstriction
Angiotensinogen: hormone secreted in the liver that converts to angiotensin I
Angiotensin I: molecule travels to the lungs where it meets with ACE and
converts into Angiotensin II
Angiotensin II: powerful constrictor; travels to the kidneys causing water and Na
retention and vasoconstriction of vessels
Angiotensinogen Angiotensin I  Angiotensin II  Vasoconstriction of vessel
Renin
ACE
DRUGS ACTING ON BLOOD AND BLOOD PRODUCTS
Thrombolytic agents
Streptokinase (G), Tissue plasminogen activator (G) aka Activase (T): facilitate
breakdown of clots that have been formed; intravenously administered; convert
plasminogen to plasmin; side effect: may cause hemorrhage elsewhere;
contraindicated for internal bleeding; usually for ischemic stroke, not
hemorrhagic; have 3-6 hours to administer before major cell death from ischemia
Tissue Plasminogen activator (tPA) (G): see above; first to hit the market from
Genetech and reduced mortality of pts having MI; tPA is endogenous to the
body, cloned version is activase;
Streptokinase (G): see above; bacterial protein (streptococci) not chemically
similar to tPA, but same final effect; cost way less than tPA; more adverse
reactions with this than tPA
Heparin: Anticoagulant that is naturally made in our body by mast cells; heparin
works with antithrombin III to inhibit thrombin for clot formation; given
parenterally; side effects (dose dependent): prolonged bleeding;
Aspirin: see musculoskeletal section; works through the arachidonic pathway to
block the works of platelets (responsible for thromboxane A2 production); result
is a blood thinner
Lipid-lowering drugs
Statins (ex. Lipitor (T), Crestor (T), Lovastatin (G), Zocor (T)): inhibit cholesterol
biosynthesis in the liver; decrease serum LDL and total triglyceride levels and
increase HDL; block Hydroxyl-methylglutayl-coenzyme A reductase (HMG-CoA
reductase) enzyme responsible for making cholesterol; used to prevent MI or
stroke; contraindications: combo with certain antibiotics, calcium channel
blockers and protease inhibitors; side effects: unbalance in liver enzymes,
muscle aches
Caduet: combination of amlodipine (a calcium channel blocker) and atorvastatin
aka Lipitor (HMG CoA reductase inhibitor); reduces LDL and triglycerides in the
blood and increase HDL; treat HTN or angina
Questran (T): bile acid sequestrant originally designed for obstructive liver
disease; drug works in the liver to block resorption of bile and promote excretion
of bile acid (conversion of cholesterol to bile acid); also block the HMG CoA
reductase activity; little side effect
Niaspan (T), Simcor (T): extended release form of niacin (Nicotinic acid, B3
vitamin); commonly used to increase the levels of HDL’s; inhibits the synthesis of
precursors for LDL’s; side effects: flushing or itching of skin, vomiting, diarrhea,
dry skin, increase plasma glucose
MUSCULOSKELETAL
ANALGESICS
Opiate Drugs: five classes of receptors (mu, kappa, delta, epsilon, sigma) each
distributed differently in the body and various affinities; predominately receptors
in limbic system; work in CNS and GI tract; side effects: sedation, lethargy,
inability to concentrate, mood swings, orthostatic hypotension, cough
suppression, decrease respiratory rate; good for moderate to severe pain,
constant in nature; used on schedule rather than when feel pain; tolerance and
physical dependence can occur
Morphine (G): opiate; most common strong agonist; restricted by federal
govt because of high rate of abuse
Demerol (T): synthetic opioid analgesic; strong agonist; risk for patients
with renal impairment, toxic metabolite stays in the body for long periods
of time, high levels cause seizures and convulsions.
Fentanyl (G): opiate, strong agonist; 100x stronger than morphine; slow
acting form; patches or lozenge
Codeine (G): chemically modified from morphine; 1/6 as potent as
morphine; mild to moderate opiate agonist; body converts it into morphine
when administered;
Oxycontin (T) aka Oxycodone (G): mild to moderate opiate agonist;
frequently abused; oxycontin is slow acting form
Percodan: combination of oxycodone and aspirin; mild to moderate opiate
agonist;
Hydrocodone (G), Darvon (T): other mild to moderate opiate agonists
Nalbuphine (G): mixed agonist/antagonist opiate; kappa receptor
active/mu receptors inactive; less side effects, do not depress respiration
Naloxone (G), Naltrexone (G): these drugs block the effect of opiates;
used at antidote for opioid overdose or recover from depressed respiration
from opioids
Dynorphin: opioid peptide
NSAIDS (Non-steroidal anti-inflammatory drugs): common actions: antiinflammatory, anti-pyretic (fever reducer), analgesic, anti-coagulating; should be
taken short term; potent inhibiters of enzyme cyclooxygenase which blocks the
conversion of arachadonic acid into prostaglandins and thromboxanes;
asthmatics shouldn’t take because of broncho-constriction; may increase blood
pressure; block bone healing
Aspirin (G): acetylsalicylic acid (ASA); most widely used NSAID; inhibits
the synthesis of prostaglandins; potent and effective drug; founded by
Bayer in 1800’s, traditional headaches and muscle pain; effective for OA
and RA; also used for anti-coagulant effects; side effects: gastric issues
due to prostaglandin blocking which protects stomach from gastric acid,
long term use causes liver toxicity and kidney disorders; children with flu
or chicken pox taking this could get Reye’s Syndrome
Advil (T) aka Ibuprofen (G)
Fenoprofen (G)
Naproxen (G) aka Alleve: study showed risk of cardiovascular events
Celebrex (T), Vioxx (T): COX-2 inhibitors (class of NSAID) that are specific
to COX-2 subtype enzyme; great anti-inflammatory drugs; side effects:
abdominal pain, tenderness and discomfort, nausea, blood in vomit,
bloody stools, unexplained weight loss/gain, water retention, cardiac
events, protect GI tract (unlike aspirin)
Vioxx: have a significantly higher change of cardiovascular disease if on
the drug; approved for colon cancer
Thromboxanes: one of the end products of arachadonic acid that causes
platelet aggregation; NSAIDS will block the cellular pathway to inhibit
thrombus formation
Acetaminophen (G) aka Tylenol: not a NSAID, no anti-inflammatory or anticoagulant effects; no stomach irritation or Reye’s syndrome; may cause liver
damage with long term use; absorbed rapidly in upper GI tract, has a half-life of
2 hours
LOCAL ANESTHETICS
Lidocaine (G) aka Xylocaine (T), Novacaine (T), Benzocaine (G): block the
neuronal action potential by blocking the Na+ channel on the neuron causing
pain relief; block sensation to particular area; lots of applications
ANTI-INFLAMMATORY DRUGS
Corticosteroids: common for musculoskeletal problems; drug of choice to reduce
inflammatory signals; can be used for MS; side effects: muscle wasting,
abdominal adipose tissue, decrease in cognitive function, break-down of muscle,
tendon and bone; careful administration to RA and skeletal muscle disease; see
endocrine section for more on corticosteroids
Leukotrienes: signals inflammatory process
SKELETAL MUSCLE RELAXANTS
Baclofen: muscle relaxant; binds to GABA-b receptors in the CNS; useful for MS
and SCI spasticity; allows better bladder control; has a greater effect when
placed in the subarachnoid space (intrathecally: baclofen pump); side effect:
weakness, transient drowsiness, orthostatic hypotension, confusion
(stroke/elderly)
Barbiturates: may reduce muscle spasm or tone; act on GABA receptor;
antagonistic effect on postsynaptic receptors, see Neuro section for more
Benzodiazepines: increase general CNS inhibition through GABA; low doses of
Valium can reduce muscle tone without sedation; see Neuro section
Dantrolene: commonly used and only muscle relaxant that acts directly on
skeletal muscle; binds to skeletal muscle intracellular calcium release channel,
blocking the release of calcium; side effect: muscle weakness, drowsiness,
dizziness, fatigue, diarrhea; cleared by liver, so may have some liver damage
Tizanidine: used to treat chronic spasticity associate with illness or injury (MS or
SCI); no drug dependence; can be used in combo with Dantrolene or baclofen
Botulinum Toxin (Botox): impairs the release of acetylcholine at the
neuromuscular junction; decreases spasticity if injected into the affected muscle;
side effects: food poisoning, irritation at injection site, anti-body production to
botulinum toxin; not good long term alternative
ENDOCRINE
ADRENOCORTICOSTEROIDS: produced by the adrenal cortex
Glucocorticoids: involved in control of glucose metabolism; decrease
inflammation and suppress immune system; intracellular receptors in cytoplasm
then translocated to the nucleus; used as 1.) replacement therapy (Addison’s
disease, Cushing’s syndrome), 2.) anti-inflammatory effect (inhibit enzyme
phospholipase A which blocks production of leukotrienes and other proinflammatory substances and mediators; arthritis, ulcerative colitis, Crohn’s,
systemic lupus, allergic reactions, asthma) and/or 3.) immunosuppression
(hypersensitivity to cell-mediated allergic reactions, transplant pts, leukemia,
lymphoma, autoimmune hemolytic anemia)
Cortisol (aka hydrocortisone): primary glucocorticoid in body; provides negative
feedback to hypothalamus and pituitary gland to reduce release of hormone that
stimulates cortisol synthesis and release; released in response to stress (fight of
flight); when enters mm cell, it decreases glucose uptake and increases protein
breakdown; systemically increases blood glucose and liver glycogen
Corticosteroids (ex. Prednisone (G), Prednisolone (G), Dexamethasone (G) aka
Decadron (T), Kenacort (T): drugs that are synthetic cortisol; no cure, treat
symptoms; become active in the liver, so people with liver disease may have
trouble using; side effects: no normal production of glucocorticoids (dependent),
Cushing’s syndrome, break-down of support tissue (bone, muscle, connective
tissue), nervousness and jitteriness
Mineralcorticoids: maintain fluid and electrolyte balance; primary one is
aldosterone; respond to decrease in BP and works on kidneys (increasing
sodium reabsorption); bind cortisol at low affinity
THYROID: temp regulation, growth/development, cardio & metabolic effects
Drugs for Hyperthyroidism
Iodine: will completely stop thyroid hormone production; good short term to
decrease feedback mechanism; replaced by beta blockers
Iodotope (T): also for thyroid cancer
Tapazole (T)
Drugs for Hypothyroidism
Triostat (T), Synthroid (T): drugs that increase thyroid hormone (synthetic forms
of T3 and T4, respectively)
PARATHYROID: control calcium concentrations; PTH causes bone breakdown
Calcitonin: secreted by cells in the thyroid gland; antagonist to parathyroid
hormone (PTH); stimulates bone formation and increases calcium into skeletal
storage
PANCREAS: endocrine/exocrine; responsible for glucose control
Insulin: 51 amino acid peptide that binds to insulin receptor (tyrosine kinase
receptor – alpha subunit) and moves glucose into cell; exogenous insulin used
for DM Type I; bovine, porcine or human insulin can be used; intramuscular
injections; rapid-, intermediate-, and long-acting forms of insulin; common
problem is hypoglycemia when too much insulin injected
Exubra: inhaled insulin (human form); main problem is dosing (ex. upper
respiratory tract infection); may replace injections
Oral Hypoglycemic Drugs: for type II DM; induce the release of insulin from
pancreas and increase sensitivity of peripheral tissues to insulin; side effects:
hypoglycemia, heart burn, nausea, vomiting, diarrhea, headaches, dizziness,
skin rashes, leukopenia
Diabinese (T), Glucamide (T): peak effect 3-6 hrs; duration 24-48 hrs
Glipizide (G): peak 1-3 hrs; duration 12-24 hrs
Glyburide (G): peak 4 hrs; duration 24 hrs
Metformin (G) aka Glucaphage (T): peak 4-8 hrs; duration 12-24hrs
Orinase (T): peak 1-3 hrs; duration 6-12 hrs
GPL-1 (glucagon-like peptide 1): hormone in the stomach and intestines that is
known to stimulate insulin secretion and decrease glucagon secretion; trying to
use this to develop a new drug to improve glycemic control for Type II DM
Liraglutide (G): peak 2-13 hrs; duration 24 hrs; mimic GLP1; could cause
significant increase in hypoglycemic events
Exenatide (G) aka Byetta (T): peak 2 hrs; duration 10 hrs; mimic GLP1;
could cause significant increase in hypoglycemic events
Sitagliptin (G) aka Januvia (T): peak 1-4 hrs; duration 12.4 hrs; inhibits the
enzyme that destroys GLP1; preserve islet mass and increase the
average size of islet; increase insulin secretion
PULMONARY
DRUGS FOR ASHTMA
Bronchodilators: can be used for asthma, COPD, infections and other
respiratory conditions
Albuterol (G): adrenergic bronchodilator; quick acting; for acute asthma; beta
agonist used to stimulate respiratory portion of SNS through cAMP (promotes
smooth muscle relaxation, inhibits mast cell degranulation through G protein
receptor) and cGMP (promotes smooth muscle contraction and enhance mast
cell release of histamine); assists in preventing asthma attacks from exercise; too
much can increase asthma symptoms; no depression of inflammation; inhaler
Formoterol (G), Salbutamol (T): slow acting bronchodilator; also beta agonist
(see above); prevent attacks from happening, not for acute asthma; need 12
hours to take effect; no depression of inflammation; inhaler
Glucocorticoids (ex. Beclovent (T), Budenoside (G), Cortone (T),
Dexamethasone (G), Prednisolone (G), Hydrocortisone (G)): reduce airway
inflammation and swelling, decrease chance of asthma attack; preferred long
term control mild to mod asthma; inhaler or oral; risk for OP, slow healing
wounds, muscle wasting b/c of catabolic effects; side effects: weight gain, fluid
retention, high BP, diabetes, cataracts, osteoporosis; see endocrine section
Saltropine (T): most common parasympathetic blocker; inhaler; blocks vagus
stimulation to prevent bronchoconstriction; body develops tolerance so short term
use; side effects: mental depression (low dose), high doses – delirium,
hallucination, decreased GI activity
Atrovent (T): also parasympathetic blocker, see above, fewer side effects than
saltropine (poorly absorbed)
Methylxanthine (ex. Theophylline (G)): commonly found in food and beverages;
cause reversible airway dilation by inhibiting cAMP and phosphodiesterase; side
effects: increased myocardial work load, confusion, irritability, restlessness; low
therapeutic range means high toxicity
Caffeine (G): a methylxanthine, see above; only metabolized in the liver;
signs and symptoms of overdose: nervousness, jitters, anxiety; has
intracellular receptors – quickly diffuses through cell membrane without
transporter to receptor on endoplasmic reticulum.
Cromolyn (G): mediator-release inhibitor family; can be prophylactic for chronic
asthma to prevent immediate hypersensitivity or used for acute attacks to reduce
severity; used most for persistent mild asthma; prevents influx of Ca into mast
cells and blocks release of mediators causing bronchoconstriction; nasal spray;
side effects: dry mouth/throat, airway irritation, bronchospasm
Singulair (T): blocks the formation of leukotrienes; treat mild, persistent asthma
or combo with corticosteroids can treat mod to severe asthma; categorized as an
NSAID; side effects: upset stomach, fatigue, dizziness, headache and rash
DRUGS FOR ALLERGIES
Antihistamines (ex. Benadryl (T, OTC), Claritin (T, OTC), Allegra (T, Rx), Zyrtec
(T, Rx): modulate the neural activity within CNS and regulate gastric secretions
through H1 an H2 receptors; block H1 (histamine receptor) to decrease mucosal
congestion, irritation, and discharge from allergen; also used for asthma; side
effects: dizziness, drowsiness, nausea, dry mouth, muscle aches
Astelin: antihistamine; prescription nasal spray
Decongestants: specifically given to relieve congestion; nasal sprays, syrup, pill,
usually OTC, decrease the swelling from inflammation, shrink blood vessels (less
leaky); side effects: could increase BP, insomnia, irritability; used in combo with
antihistamines
Bronchodilators: see above under asthma
DRUGS FOR OBSTRUCTIVE LUNG DISEASE
Mucinex (T): expectorant used to for mucous obstructions; moving mucous and
lubricating internal lining in airway; side effects: minimal/rare, rash, urinary
retention, insomnia, hallucinations
Antitussives (ex. Tessalon (T)): suppress a cough; all opioids drugs are cough
suppressants (neuro section); act on cough center of the brain (CNS effect); any
drug with codeine for respiratory problem or infection would be antitussive
ONCOLOGY
Alkylating Drugs (ex. Cisplatin): largest group of anticancer drug used to treat
leukemias, carcinomas, and other neoplasms; induces binding within DNA
strands (cause 2 DNA strands to bind so replication and gene expression don’t
take place); kills human and cancerous cells; side effects: anemia, leukopenia,
thrombocytopenia, GI distress
Cisplatin (G): an alkylating drug (see above); primary use for bladder,
ovaries and testicles; side effect: pulmonary fibrosis, restrictive lung
disease, impaired gas exchange, peripheral neuropathy, loss of strength,
fibrosis and hard edema around a joint, cellulitis, neuronal and pulmonary
toxicity, bladder irritation
Antimetabolitic Drugs (ex. Fluorouracil, Methotrexate, Adrucil); interferes with
replication of DNA; metabolites made to be incorporated into DNA making a
nonfunctional segment, slow down activity of enzymes involved in DNA
replication; side effects: blood disorders, GI distress, skin rash, hair loss,
hepatotoxicity, CNS effects
Fluorouracil (G) aka Adrucil (T): antimetabolitic drug (see above); primary
use colon, rectium, stomach and pancreas
Methotrexate (G): antimetabolitic drug (see above); primary use acute
lymphoma leukemia, meningeal leukemia, lung, carcinoma of head and
neck, NHL; side effect: pulmonary fibrosis, restrictive lung disease,
impaired gas exchange, hair loss
Antibiotics (ex. Bleomycin, Adriamycin): harsh drugs that are inserted into the
DNA strand so DNA replication and gene expression can’t take place; side effect:
GI disorders, blood disorders, skin rash, hair loss, hepatotoxicity
Bleomycin (G): antibiotic; primary use: carcinoma of head, neck, cervical
region, skin, testicle carcinoma, Hodgkin’s disease, NHL; side effect:
pulmonary fibrosis, restrictive lung disease, impaired gas exchange
Adriamycin (T): antibiotic; primary use: acute leukemia, carcinoma of
bladder, breast, ovary, thyroid, Hodgkin’s disease, NHL; side effect: may
cause irreversible cardiac damage (cardiac toxicity), hair loss
Plant Alkaloids (Vinblastine, Vincristine): nitrogen-based compounds that
dissociate microtubules of cells involved in mitosis; cells can’t divide; side effects:
blood disorders, GI distress, hair loss, CNS/PNS neuropathies
Vinblastine: plant alkaloid; primary use: breast, testes, Hodgkin’s, nonHodgkin’s, Kaposi’s sarcoma; side effects: peripheral neuropathy, loss of
strength, fibrosis and hard edema around a joint, cellulitis
Vincristine: plant alkaloid; primary use: acute lymphotic leukemia
neuroblastoma, Wilm’s tumor, Hodgkin’s, non-Hodgkin’s lymphoma,
Ewing’s sarcoma; side effect: peripheral neuropathy, weakness and
paresthesia distally, hair loss
Mylotarg (T): antibodies to proteins that bind only to cancer cells; CD33 antibody
given to treat people with relapsed acute myeloid leukemia
IMMUNOLOGY
ANTIBACTERIAL AGENTS (ANTIBIOTICS)
Penicillin (G): most widely prescribed and effective class of antibiotics because it
treats a broad spectrum of infectious agents; Tx gram positive bacteria
(streptococci, meningococci, enterococci, group A beta hemolytic and staph
infections); administered orally, intramuscularly, intrathecally; few side effects:
hypersensitivity to drug, allergic reactions, seizures, epigastric distress, vomiting,
colitis, rashes and pain; toxicity: convulsions
Amoxicillin: Extended-spectrum Penicillin; commonly used to treat peptic
ulcers; prescribed for pneumonia, strep and staph infections, and
prevention of rheumatic fever
Vancomycin (G): effective with treating gram positive bacteria; drug of choice for
severe staph infections or when other antibiotics are ineffective; hinder bacterial
cell-wall synthesis; intervention for sepsis or endocarditis caused by methicillinresistant staphylococci; poor GI absorption; administered: capsule, powder form,
nasal inhaler or IV; side effects: skin rash, nausea, vomitting; resistance has
become major clinical problem;
Tetracycline: inhibit bacterial protein synthesis of ribosomes; wide spectrum of
activity; inhibit both gram positive and gram negative bacteria (ex. Chlamydiae,
mycoplasmas, rickettsiae, protozoa, amebas); administered: tablets, capsules,
topical solution, IV; few side effects: nausea, vomiting, diarrhea, sore throat,
hoarseness, inflammatory lesions, local venous thrombosis; not for pregnant
women or children (deformities); commonly prescribed for peptic ulcers
Chloramphenicol: binds to ribosome’s responsible for protein production in
bacteria; broad spectrum against aerobic/anaerobic gram positive and negative
bacteria; fairly toxic: usually only Rx for rickettsial infection, typhus and Rocky
Mountain Spotted Fever; administered: orally; Side effects: GI problems; Toxic to
infants: “Gray Baby Syndrome” (grey color, vomiting, flaccidity, and shock)
Macrolides (ex. Erythromycin): inhibit protein synthesis; used for diphtheria,
erthrasma, genital chlamydia and H influenza; substitute for penicillin; side
effects: anorexia, nausea, vomiting and diarrhea, liver toxicity possible
Erythromycin: destroyed in stomach acid, given in coated tablet form or IV
Aminoglycosides (ex. Gentamycin, Kanamycin, Neomycin): family of drugs that
block protein synthesis; rely only on the kidneys for excretion
Kanamycin, Neomycin: treat gram negative rods (E Coli, Proteus,
Enterobacter Aerogenes, Klebsiella pneumonia); bind onto ribosome
subunits and inhibit protein synthesis; administered: capsules, injections;
side effects: headaches, confusion, vertigo, hearing loss; toxicity: tinnitus,
extreme vertigo, decreased renal clearance, increased BUN
Gentamycin: gram negative; treat: Pseudomonas Earuginosa, proteus, E
Coli, Klebsiella pneumonia, enterobacter aerogenes; administered:
intramuscular or IV; side effects: renal functional impairment; Not for
pregnant women
Sulfonamides (ex. Sulfadiazine (T)): treat bacterial infections (mostly UTI),
diabetes mellitus, edema and gout; inhibit bacterial folic acid synthesis;
administered: tablets, oral suspensions, injections; side effects: nausea,
vomiting, mental confusion; capable of toxicity: anemia, leukopenia;
contraindications: kidney irritation or damage, pregnancy, bone marrow
depression
Isoniazid: first line of defense to treat active tuberculosis (Mycobacterium
tuberculosis) in combo with other agents; tuberculosis difficult to treat because a
myobacteria (dont respond to antibacterial agents, replicate slowly, develop drug
resistance); preventative tx to people exposed to TB; block synthesis of bacterial
cell walls and interfere with cell metabolism; administered: tablets, syrup,
injections; side effects: nausea, vomiting, fever, rashes, stomach pain,
weakness, loss of appetite, headaches; toxicity: blurred vision, eye pain, diff
breathing, seizures; contraindications: liver disease/damage, alcholic
ANTIVIRAL AGENTS
Acyclovir: inhibits DNA synthesis (doesn’t harm host because it requires a viral
protein to activate it, attacks only cells with virus); treat: herpes simplex virus,
vericell-zoster virus; administered: oral, IV, topically; side effects: nausea,
diarrhea, tolerated well
Azidothymidine aka AZT (ex. Epivir): reverse transcriptase inhibitor; first drug
designed for HIV (slow rate of progression and prolong survival, viral resistance
quickly); administered: IV, oral; strict time regiment; side effects:
myelosuppression, GI problems, headaches, myopathies;
Indinavir (ex. Ritonavir): inhibitor of protease specific to HIV-1; used in combo
with reverse transcriptase inhibitors (more effective with combo); side effects:
kidney problems, hyperbilirubinemia, nausea, diarrhea
Ritonavir: protease inhibitor; interacts with many drugs (problem); not
useful for HIV since on multiple meds
Interferon: endogenous proteins (cytokine) inserted into cell membrane after viral
infection; block viral entrance into healthy cells (“fools” virus the cell is already
infected); artificially administered; success rate not great; Tx: hep B/C, Kaposi’s
sarcoma; side effects: GI problems, anemia, weakness, fever
ANTIFUNGAL AGENTS
Amphotericin: attacks the unique lipids in fungi compromising the stability of the
fungus; administered: orally, topically, IV; broad spectrum of antiviral activity:
Crytococcus neofomans, candida albican, histoplasma capsulatum, blastomyces
dermatitidis; resistance and toxicity likely: renal impairment/failure; side effects
IV: fever, headache, vomiting, nausea, muscle spasm
Flucytosine: inhibit DNA/RNA synthesis; narrow spectrum: Cryptococcus
neofomans, some Candida; rare resistance; typically used in combo with other
antifungals; oral admin; side effects: bone marrow toxicity, anemia
Azole (ex. Ketoconazoles (G), Diflucan (T)): new category of antifungals that bind
to cytochrome P450 enzyme; fight fungal infections on systemic level or topically;
broad spectrum (Candida, Blastomycosis, histoplasmosis, Cryptococcus
neofomans); Tx amphotericin-resistant fungi; few side effects: minor GI problems
DRUGS TO BOOST THE IMMUNE SYSTEM
Cytokines (ex. Actimmune, Roferon, Interferon (Betaseron)): endogenous
proteins that have regulatory capacities within the immune system; extra
amounts can produce severe side effects
GASTROINTESTINAL
ACID REDUCING DRUGS
Antacids (ex. Di-gel, Maalox, Mylanta, Rolaids, Tums): attempt to neutralize
excess stomach acid (heart burn or acid reflux); for minor GI discomforts;
common side effect is constipation; aluminum containing associated with
constipation and magnesium with diarrhea
H2 Receptor Antagonists (ex. Tagamet (T), Pepcid AC (T), Zantac (T)): decrease
the amount of stomach acid by preventing histamine-activated release of acid
under resting conditions and food stimulation; acute and long term care of ulcers;
over the counter= peptic ulcers, prescription= reflux disorder; side effects:
headaches, dizziness, mild/transient GI complaints
Tagamet: more drug interactions if taken in combo, see above
Pepcid AC: only Maximum strength Pepcid AC has enough active ingredient to
treat/heal peptic ulcers, see above
Proton-Pump Inhibitors (PPI) (ex. Prilosec, Prevacid, Nexium): directly act on the
proton pump to block hydrogen and the production of acid; 90% more effective
than H2 receptor antagonists; can use antibiotics combo (H. pylori can cause
peptic ulcers); side effects: headache, diarrhea, constipation, abdominal pain,
nausea, rash; typically prescription except Prilosec OTC
Gastrozepin (T): most common acetylcholine receptor antagonist for GI problems
inhibits gastric secretion at doses below those needed to affect the CNS; relaxes
esophageal sphincter; less effective than H2 blockers reducing acid, but good
long term healing ulcers; rarely used; side effects: urinary retention, confusion,
constipation, dry mouth
LAXATIVES: drug of choice when no obstructions in GI tract
Citrucel (T) (generic -Methylcellulose): bulk forming lax; absorbs water and swells
in lower GI; stretches stimulate peristalsis; side effects: distended, painful
abdomen
Dulcolax (T), Ex-Lax (T), Senna (G): stimulant lax: these activate peristalsis by
unknown means, but thought it increases fluid accumulation in small intestines;
side effects: stomach pain, cramping, diarrhea
Amitiza (T), Fleets enema (T): hyperosmotic lax; these produce gradients that
draw water into the bowel and small intestines=excretion; side effects: stomach
pain, gas, cramps
Amitiza: see above; frequently used for irritable bowel syndrome, diverticulitis
and chronic constipation
Colace (T): lubricant and stool softener; brings water into fecal mass and easy
elimination; short-term basis for constipation; side effects uncommon: stomach
cramp
ANTIDIARRHEA AGENTS
Kaopectate (T): stool thickener; compound carries pectin which thickens stool,
should not be taken more than 2 days since it can kill normal bacteria in GI
ANTI-SPASMODIC DRUGS
Imodium (T): opiate that produces a general decrease in GI motility; thought to
produce local effect on gut wall; slow travel allows water to be removed from
stool=firm stool; not taken for more than 3 days; side effects: nausea, abdominal
pain, dry mouth, constipation, drowsiness, fatigue, dizziness
OTHER
Aldosterone: mineralcorticoid responsible for maintaining electrolyte balance;
responds to low blood pressure; works in kidneys by increasing sodium
reabsorption
Antioxidants: ex. Vitamin E, selegiline, rasagiline; control the synthesis of
elimination of free radicals (lower the bodies concentration of free radicals); used
to treat Parkinson’s (body loses defense against radicals or has increase in
production)
Calcium channel blockers: bind to voltage-gated calcium channels in arteries (i.e.
smooth muscle in coronary arteries); inhibits calcium into cell and the drug blocks
the interaction between actin and myosin (contractile elements); the cell is
encouraged to relax/increase in diameter, decrease local blood pressure,
increase blood flow to that region.
Interferon: cytokine thought to inhibit the immune system from attacking itself;
antiviral, anticancer, boost immune system
Pharmacokinetics: study of the factors that are involved in getting the drug to its
target in the body; the mechanisms and regulatory processes that determine how
drugs are transported throughout the body comprise the study of
pharmacokinetics
Pharmacodynamics: the study of the mechanisms of action of the drug, the
therapeutic and toxicologic effects, and the chemical structure-activity
relationships; the study of what the drug does when it gets to the target molecule