Drug

Name

Heparin
and Low
Molecular
Weight
Heparins
Oral Anti-
coagulant

Drug Classes

Fibrino-
lytics

Desai

Anticoagulants

Antiplatelet
Drugs

Aspirin
Clopidogrel/
Ticlopidine
Eptifibatide/
Abciximab/
Tirofiban

Acts as a catalyst and activates ATIII to rapidly inhibit

clotting factors IIa (thrombin) and Xa.

LMWH

Too small to bind/inactivate thrombin (IIa). But can

bind to ATIII and inactivate factor Xa.

Warfarin

Competitive inhibitor of Vit. K epoxide reductase, which

activates factors II, VII, IX, and X.

Streptokinase

Binds to plasminogen and converts it to active plasmin.

Systemic plasmin formation.

t-PA

Activates fibrin bound plasminogen. Theoretically acts

at site of clot formation.

Drug Classes

Antiobesity

-lactams

Cell Wall

Crosses placenta teratogenic.

Dissolve clots after myocardial infarction,

deep vein thrombosis, massive pulmonary
emboli.

Bleeding, allergic reactions, hypotension,

fever.

Safest ad only hypocholesterolemic drug

recommended in children.

Carbapenems

Vancomycin

Given with statins leads to myopathy.

Given with statins leads to myopathy.
Flushing, dyspepsia, hepatotoxicity, and
avoid in pregnancy.
Not used in patients with
hypertriglyceridemia. Interfere absorption
of fat soluble vitamins. Bloating and
dyspepsia.

Reduce LDL with diet (10%) or drugs (20-

60%). Generally safe.

Major CV risk factor.

Prevent absorption of dietary fats by 30%.

Bloating, oily spotting, and fecal urgency.

Prevent absorption of Vit. A, D, E, K.

Allergic reactions and GI upset. Dont use

during pregnancy.

Nephrotoxicity. Dont use during

pregnancy.

Tetra-
cyclines

Maximal activity against rapidly dividing

bacteria. Treat infections caused by gram-
positive organisms.
See PCN. 4th gen. crosses BBB to treat
meningitis. 3rd gen. enters CSF.
See PCN.
See PCN. Strong activity against gram-
negative.
Active against gram-positive.
Topical use for gram-positive and certain
gram-negative.

Tetracyclines

Bind to 30S ribosomes to prevent aminoacyl-tRNA

attachment. Enter gram-positive by energy-dependent
process.

Rickettsial diseases: Rocky Mountain spotted

fever, typhus. Plague. Low dose: acne.

Bind to developing teeth and bone. Dont

use during pregnancy.

Macro-
lides

Inhibit synthesis of bacterial cell wall.. No -lactam

nucleus.

Hepatotoxicity and myopathy. Dont use

during pregnancy or breast feeding.

Erythromycin

Block peptide bond formation. Block translocation of

ribosome.

Mycoplasma pneumoniae. Streptococcal

upper respiratory tract infection. Legionella.

Dont use during pregnancy.

Amino-
glycosides

Bacitracin

Cleared unchanged by kidney avoid in

renal failure. Safety in pregnancy not
evaluated.

Prevent DVT or PE. Prevent

thromboembolism

Binds negatively charged bile acids. Liver must

synthesize new bile acids using cholesterol. Increase in
LDL receptors removes cholesterol from plasma.

Cephalosporins

Hemorrhage. Heparin-induced
thrombocytopenia.

Streptomycin/
Gentamicin/
Neomycin

Cause misreading of mRNA so that wrong amino acid is

added. Bind to 16S rRNA prevent release of growing
protein.

Combine with penicillin for synergy.

Ineffective against anaerobic bacteria/fungi.

Toxicity is dose-related. Dont use during

pregnancy.

Chloram-
phenicols

Protein Synthesis

Increased bleeding.

Venous thrombosis and pulmonary

embolism. Anticoagulation during pregnancy
(doesnt cross placenta).
Prevent venous thromboembolism. Treat
venous thrombosis, pulmonary embolism,
and unstable angina.

Resins

Monobactams

Chloramphenicol

Bacteriostatic. Prevent aminoacyl-tRNA binding to

mRNA codon. Block peptide bond formation.

Widely used in low income countries.

Effective against wide variety of organisms.

Rare but serious aplastic anemia. Dont use

during pregnancy.

Combination of both block 2 consecutive

steps: bactericidal.

Dont use during pregnancy.

Hypersensitivity, Stevens-Johnson
syndrome.

Urinary tract infection.

Carcinogenicity and mutagenicity. GI

effects. Hypersensitivity.

Inhibit DNA topoisomerase. Bind to enzyme-DNA

complex blocks DNA synthesis.

Second-line drug for tuberculosis.

GI effects, CNS agitations, and damage to

growing cartilage.

Bactericidal cationic detergents with both lipophilic and

lipophobic groups disrupt cell membranes.

Pseudomonas aeruginosa and Acinetobacter

baumannii.

Nephrotoxicity and neurotoxicity.

Inhibition of mycobacterial DNA-dependent RNA

polymerase.

First-line drugs for tuberculosis.

Orange discoloration in secretions. GI

upset, hepatotoxicity, hypersensitivity,
rash.
Hepatotoxicity, peripheral neuropathy,
CNS effects.

Folate Antagonists
Nitrofurans
Nucleic Acid
Modification

During or after coronary artery procedures

like angioplasty.

Best agent to increase HDL, by reducing their

clearance in liver.

Penicillins (PCN)

Fluoro-
quinolones

Cytoplasmic
Membrane
Anti-
tuberculosis

Severe neutropenia, hemorrhage.

Increases lipoprotein lipase activity removes

chylomicrons and VLDL triglycerides from blood.

Orlistat

Antibacterial

Gastrointestinal bleeding.

Niacin

Prevents absorption of dietary cholesterol from

intestines.
Inhibit pancreatic and intestinal lipases. Inhibit
breakdown of dietary fat.
Inhibit synthesis of bacterial cell walls. Bacteriostatic.

Cephalosporins: only few enter CSF in sufficient
concentration.

Carbapenems: Highly resistant to beta-lactamases.

Monobactams: beta-lactam ring is alone.

Adverse Effects

Used in combination with aspirin for

synergistic activity.

Most effective for hyperlipidemia, except

when LDL receptor dysfunctional.
Least used. Treat severe
hypertriglyceridemia.

Ezetimibe

Other
Antibacterial

Therapeutic Use
Prophylaxis for MI. Post MI. Prophylaxis for
TIA or post TIA.

Inhibits HMG-CoA reductase, an enzyme that catalyzes

cholesterol biosynthesis.
Activates nuclear transcription factor receptor, PPAR-,
to cause metabolic changes.

Fibrates

Sawacki

Block GpIIb-IIIa receptor for fibrinogen on platelets and

prevent platelet aggregation.

Heparin

Statins

Glyco-
peptides

Mechanism
Irreversibly inhibits platelet COX and prevents
formation of thromboxane from arachidonic acid.
Contraindicated in pregnancy and childbirth.
Block platelet purinergic P2Y receptors for ADP
increase cAMP.

Sulfamethoxazole
(sulfonamides)
Trimethoprim
Nitrofurantoin
Ciprofloxacin/
Norfloxacin (2nd),
Levofloxacin
(3rd),
Gatifloxacin/
Moxifloxacin (4th)
Colistin
(Polymyxin E)
Polymyxin B

Rifamycin

Rifampin

INH

Isoniazid

Structural analog of para-aminobenzoic acid

completely inhibits dihydropteroate synthase.
Reversible inhibition of dihydrofolate reductase.
At concentrations reached in urine, nitrofurantoin is
bactericidal. Reduce form is highly reactive.

Enter via passive diffusion, activated by bacterial

catalase, and attack multiple targets. Inhibition of
mycolic acid synthesis.

Cell Wall

Caspofungin

Cell Membrane

Polyenes

Amphotericin B

Rash, headache, dizziness, nausea.

Antifungal.

May induce or intensify subacute

cutaneous lupus erythematosus.

Binds to tubulin, interfering with microtubule function,

thus inhibiting mitosis.

Ringworm infections of skin and nails.

Diarrhea, GI sensitivity, CNS effects.

Pyrimidine
analog

Athletes foot, ringworm, candidiasis.

Nucleic
Division

High fever, renal toxicity, anemia.

Nucleic
Acid Synth.

Most widely used.

Griseofulvin

Flucytosine

(1) Converted to fluorouracil that interacts with RNA

biosynthesis disrupt protein syntheis.
(2) Inhibition of fungal DNA synthesis.

The only available antimetabolite drug with

antifungal activity.

Hypersensitivity. Dont use in pregnancy.

Oseltamivir/
Zanamivir

Inhibit neuraminidases of both influenza A and B viruses

prevent release of new virions.

Avian flu. Effective and safe for prophylaxis

and after exposure to influenza A and B.

Oseltamivir: GI discomfort and nausea.

Zanamivir: avoid if patient has respiratory
disease/asthma.

Amantadine/
Rimantadine

Block the viral membrane matrix protein M2, important

for viral uncoating.

Influenza A only. Active against some strains

of avian flu.

Recent substantial increase in resistance.

RNA
Inhibitor

Interferon

Induction of host cell enzymes that inhibit viral RNA

translation, degradation of RNA, and stimulate immune
system.

Hepatic viral infections: hepatitis B and C.

Flu-like symptoms, bone marrow

suppression, neurotoxicity, autoimmune
disorders.

DNA
Polymerase
Inhibitor

Acyclovir

Competitive inhibition of dGTP for viral DNA. Bind viral

DNA template, causing termination. Trap DNA
polymerase.

HSV1, HSV2, and VZV. Most common to treat

genital herpes infections.

Nausea, vomiting, diarrhea.

CCR5
Inhibitor

Maraviroc

CCR5 antagonist to inhibit entry.

Restricted to adults with CCR5-tropic HIV-1.

None as of yet. Long term unknown.

Used in combination therapy to treat HIV-1.

Injection site reactions, peripheral

neuropathy.

HIV.

Anemia, neutropenia, hepatotoxicity,

cardiomyopathy, myopathy.

DNA

Neuramin-
idase
Inhibitors
Viral
Uncoating
Inhibitors

Antithymocyte
globulins

Binds to gp41 and prevents conformational changes

that occur when HIV fuses with host.

Analogs of native nucleosides/nucleotides. Incorporated
by viral reverse transcriptase terminate viral DNA
elongation.
Highly selective, noncompetitive inhibitors of HIV-1
reverse transcriptase.
Inhibit HIV-1 integrase activity, preventing viral DNA
integrating with cellular DNA.
Selective, reversible inhibitors of HIV aspartyl protease,
and block viral maturation. Synergetic with NRTIs and
NNRTIs.
Most widely used. Regression of lymphoid tissue by
interfering with cell cycle. Inhibit leukocyte function,
antibody formation, and inflammatory mediators.
Preferentially suppress cell-mediated immune reactions.
Binds to cyclophilin to inhibit calcineurin. NFAT remains
inactive and cannot enter to promote cytokine synthesis.
More potent and allows lower dose of glucocorticoid.
Binds to different immunophilin: FKBP-12.
Also binds FKBP-12 to form complex with mTOR
block progression of activated T cells.
Structurally related to folate. Inhibits dihydrofolate
reductase, thus stopping production of tetrahydrofolic
acid. Decrease biosynthesis of adenine, guanine,
thymidine, depressed DNA/RNA/protein synthesis
cell death.
Depletion of T cells impaired T-cell responses.
Humoral antibody mechanism remains active.

Muromonab-CD3

Murine mAbs for the depletion of human T cells.

Pheno-
thiazines

Chlorpromazine

DA, -adrenergic, muscarinic, and histamine

antagonists.

Butyro-
phenones

Haloperidol

Blocks D1 and D2 dopamine receptors only.

Clozapine

D1, D2, 5-HT2 antagonists.

Fusion
Inhibitor
Retroviruses

Antiviral Therapy

Immunosuppressive Drugs

NRTI
NNRTIs

Schizophrenia and
Neuroleptics

Enfuvirtide
Zidovudine
(AZT)/
Lamivudine
Nevirapine/
Delavirdine

Integrase
Inhibitor

Raltegravir

Protease
Inhibitor

Saquinavir

Gluco-
corticoids

Prednisone/
Prednisolone
Cyclosporine

Cytokine
Inhibitors

Tacrolimus
Sirolimus

Cytotoxic
Drugs

Second
Generation

Methotrexate

Risperidone
Olanzapine

Mood Disorders and Mood Stabilizers

Central Nervous System Pharmacology

Hypersensitivity, hepatic effects.

Grisovin

Antibodies
and Biologic
Agents

Richardson

Itraconazole/
Fluconazole

Bind to ergosterol in cell membrane, form channels that

allow K+ and Mg2+ to leak out.

Inhibit synthesis of ergosterol by blocking 14-
demethylase.
Inhibit ergosterol biosynthesis via inhibition of Squalene
epoxidase.

Aspergillus, Candida.

Terbinafine

Liu
Immunoregulatory Agents

Azoles

Inhibit synthesis of (1,3)-D-Glucan, component of

fungal cell wall.

Allyamines

RNA Viruses

Antifungal

Sawacki cont.

Echino-
candins

MAO
inhibitors
Non-
selective
Reuptake
inhibitors

Irreversible. Non-selectively binds to both MOA-A and

MOA-B.

Moclobemide

Reversible. Competitively binds to MOA-A.

Imipramine
Amitriptyline

Inhibit both NA and serotonin reuptake: broad

spectrum. Also block muscarinic and 1 receptors.

Venlafaxine

New drug. No affinity for neurotransmitter receptors.

Paroxetine

Inhibit only serotonin uptake.

Rash can be severe, fatal hepatotoxicity.

Many drug interactions.
Resistance occurs in patients not taking
other fully active drugs.

HIV.

GI intolerance. Disturbances in glucose and

lipid metabolism. Buffalo hump.

Organ and tissue transplantation.

Inflammatory diseases. Prednisone: treat
autoimmune diseases.

Suppress pituitary-adrenal axis. Increase

risk of serious infections. Peptic ulcers.

Inhibit cytokines: Interleukins (ILs),

Interferons (IFNs), Tumor necrosis factors
(TNFs), Transforming growth factors (TGFs),
Colony-stimulating factors (CSFs), and
chemokines.

Many AEs are dose-dependent.

Nephrotoxicity, hepatotoxicity, greater risk
of infection, lymphoma.
Other AEs: hypertension, hyperkalemia,
tremor, hirsutism, glucose intolerance,
gum hyperplasia.

Doses much lower than those needed for

cancer chemotherapy.

Ulcers, low white blood count, nausea,

abdominal pain.

Acute renal transplant rejection.

Autoimmune disorders and renal, cardiac,
and hepatic transplant patients.
DA antagonists reduce positive, but not
negative, symptoms of schizophrenia.
Antihistamine, antiemetic.
Neuroleptic, antiemetic.

Halt schizophrenia. Effective on both positive

and negative symptoms.

Tranylcypromine

Fluvoxamine

Combination therapy for experienced adults

with highly resistant HIV-1 strains.

D2, 5-HT2 antagonists.

Fluoxetine

Serotonin
Reuptake
inhibitors

HIV-1 only. Lack affinity for HIV-2.

Increase levels of serotonin, NA, and DA

neurons in brain. Increase absorption of
dietary tyramine from gut into bloodstream.
Increase levels of serotonin and NA in brain
without changes in tyramine in blood.
Half life of 17 hours. Antidepressant.
Half life of 38 hours. Antidepressant.
Half life of 7 hours. Antidepressant. Treats
generalized anxiety disorder.

Half life of 3 days. Active metabolite extends
half life to over 7 days. Antidepressant. Treat
OCD.
Half life of 15 hours. Lack active metabolites.
Antidepressant. Treats GAD, OCD, and
anxiety disorders.
Half life of 24 hours. Lack active metabolites.
Antidepressant. Treats GAD, OCD, and
anxiety disorders.

Cytokine release syndrome: fatigue, fever,

chills, myalgia, headaches, nausea.
EPS, pituitary, CTZ, tardive dyskinesia,
postural hypotension, PSNS, memory,
sedation, itching, etc.
EPS, hyperprolactinemia, tardive
dyskinesia.
Little to no EPS. Bone marrow suppression
agranulocytosis and death. Weekly blood
tests required.
Little or no EPS, nor other side effects.
Very few side effects: weight gain,
dizziness, dry mouth.
Wine-cheese reactions: increased heart
rate, throbbing, and possible hypertensive
crisis.
No wine-cheese reaction.
Impaired memory, postural hypotension.
Nausea, somnolence, dry mouth.
Inhibits cytochrome P450, causing
potentially fatal drug interactions with
narcotics, -blockers, etc.

Less serious P450 related drug

interactions than fluoxetine.

Mood Disorders and Mood Stabilizers cont.

Desipramine
Noradren-
aline
Reuptake
inhibitors
Non-
selective
Release
enhancer

Maprotiline

Anticonvulsant and mood stabilizer. Treat

epilepsy and bipolar disorder.
Anxiolytic, hypnotic, anticonvulsant, muscle
relaxant. Status epilepticus or prolonged
seizures.
Hynotic. Treat: jet lag, shift work,
bereavement.

Short half life withdrawal. Does not

produce normal sleep.

Clonazepam
Ethosuximide

Increase GABA levels but also block Na+ and Ca2+

channels, and increase K+ conductance.
Increase GABA inhibition, down-regulate
benzodiazepine receptors. Up-regulate downstream NA,
5-HT, etc.
Ideal sleeping pill: short half-life, drug eliminated by
morning. Rapid onset, sleep induction within an hour or
less. Little effect on brain activity during sleep.
Block Na+ channels but also potentiate postsynaptic
effects of GABA.
Increase GABA levels.
Block Ca2+ channels.

Sedation, ataxia.
Ataxia, sedation, dizziness, headaches,
tremors.
Nausea, vomiting, gastric pain, heartburn.
Rare hepatotoxicity.
Overdose not lethal, but does potentiate
lethal actions of other compounds like
alcohols or narcotics. Tolerance.

Gabapentin

Increase GABA levels.

Lamotrigine

Block Na+ channels.

Phenobarbital

Opens Cl- channels.

Epilepsy and Anti-Convulsants

Anxiety and
Anxiolytics

Diazepam
Triazolam

Stimulants and Sympathomimetics

Central Nervous System Pharmacology cont.

Caffeine

Cocaine

Analgesics

Main action is to block Na+ channels but other things as

well.
Increase GABA levels but also block Na+ and Ca2+
channels, and increase K+ conductance.
Blocks receptors for adenosine, an inhibitory
neurotransmitter. Inhibits phosphodiesterase, leading to
increased cAMP and activates NA, DA, and other
pathways where cAMP is a second messenger.
Blocks reuptake of NA and DA.

Amphetamine
Stimulates the release and blocks reuptake of NA, DA,
and 5-HT. Inhibits MAO. Direct agonist at NA receptors.
Methylphenidate
Morphine
Codeine
Meperidine

Synthetic mu agonist. Good oral absorption.

Naloxone

Blocks all EOP receptors. Poor oral absorption.

Blocks all EOP receptors. Good oral absorption, but first
pass metabolism.

Naltrexone
Aspirin/
Ibuprofen

Rofecoxib
Acetaminophen

Stimulant Recreational Drugs

Nicotine
Caffeine

Cocaine
Ephedrine
Amphetamine

Methylphenidate

Depressant
Recreational Drugs

Predominant constituent of opium. Agonist at mu

receptors. Oral administration is poorly absorbed.
Also constituent of opium. Less potent than morphine at
mu receptors. Good oral absorption.
Synthetic mu agonist. Less respiratory depression than
morphine. Moderate oral absorption.

Methadone

Celecoxib

Drug Abuse

Richardson cont.

Valproic acid

Selective
Inhibitors
of COX II
Antipyretic
Agent

Polydipsia, tremor, nausea, GI upset.

Antidepressant. Treat epilepsy.

Phenytoin

Endorphin
Antagonists
Non-
selective
Inhibitors
of COX I/II

Bipolar disorder.
Anticonvulsant, mood stabilizer. Treat
epilepsy and bipolar disorder.
Anticonvulsant, anxiolytic.

Increase GABA levels.

Carbamazepine

Synthetic
Endorphin
Agonists

Generally mild side effects.

Gabapentin
Valproic acid

Natural
Endorphin
Agonists

Half life of 30 hours. Antidepressant.

Dry mouth, sedation, constipation,

increased appetite.

Clonazepam

Carbamazepine

Benzo-
diazepine
Anxiolytic
Benzo-
diazepine
Hypnotic

Cardiac arrhythmia, genotoxicity, breast

cancer.
Dizziness, drowsiness, fatigue, dry mouth.

Increase both noradrenaline and serotonin release.

Blocks presynaptic auto-receptors that inhibit release of
NA and serotonin. Blocks several postsynaptic serotonin
receptors.
Reduce neuronal inositol second messenger system.
Block Na+ channels but also potentiate postsynaptic
effects of GABA.
Increase GABA levels.

Mirtazapine
Lithium

Mood
Stabilizing
Agents

Selective noradrenaline reuptake inhibitors.

Nortriptyline

Half life of 38 hours. Active metabolite of

imipramine. Antidepressant.
Half life of 36 hours. Antidepressant.
Half life of 55 hours. Active metabolite of
amitriptyline. Antidepressant. Also treats
nocturnal enuresis.

Opioids
Ethanol
Marijuana
Barbiturates
Benzodiazepines

Irreversibly inhibit COX I/II reduce formation of

prostaglandins and thromboxanes.
Selective COX II inhibitors reduces various mediators
of inflammatory process, but no effect on GI mucosal
defenses or platelet aggregation.
Weak inhibition of PG formation in peripheral tissues.
Lacks anti-inflammatory actions.
Prototype nicotinic agonist.
Blocks receptors for adenosine, an inhibitory
neurotransmitter. Inhibits phosphodiesterase, leading to
increased cAMP and activates NA, DA, and other
pathways where cAMP is a second messenger.

Anticonvulsant, mood stabilizer. Treat

epilepsy and bipolar disorder.
Anticonvulsant, anxiolytic.
Anticonvulsant.
Antidepressant. Anticonvulsant. Treat
epilepsy.
Anticonvulsant. Treat epilepsy and bipolar
disorder.
Most widely used anticonvulsant worldwide.
Anticonvulsant. Treat epilepsy.
Anticonvulsant and mood stabilizer. Treat
epilepsy and bipolar disorder.
Half life of 5 hours.
Stimulant/sympathomimetic.
Half life of 40 minutes.
Stimulant/sympathomimetic. Local
anesthetic.
Half life of 20 hours.
Stimulant/sympathomimetic. Treat
narcolepsy and increase impulse control.
Half life of 2 hours.
Stimulant/sympathomimetic. Treat
narcolepsy, ADHD, and increase impulse
control.
Potent analgesic.
Analgesic. Good cough suppressant.
Fast acting analgesic.
Good analgesic profile, chronic pain
syndrome. Used in addiction treatment
programs.
Used in opioid overdose.
Used in addiction treatment for
narcotics/opoids. Reduce alcohol cravings.
Analgesic. Relieve arthritis, fever. Reset
thermoregulatory mechanism in
hypothalamus.
Arthritis, acute pain, menstrual symptoms.
Arthritis, acute pain, menstrual symptoms.
Withdrawn from market.
Analgesic and anti-pyretic actions. Less GI
distress than aspirin.
Stimulant.
Half life of 5 hours.
Stimulant/sympathomimetic.

Half life of 40 minutes.

Stimulant/sympathomimetic. Local
anesthetic.
Stimulant, appetite suppressant,
-adrenergic agonist.
concentration aid.
Half life of 20 hours.
Stimulant/sympathomimetic. Treat
narcolepsy and increase impulse control.
Stimulates the release and blocks reuptake of NA, DA,
Half life of 2 hours.
and 5-HT. Inhibits MAO. Direct agonist at NA receptors.
Stimulant/sympathomimetic. Treat
narcolepsy, ADHD, and increase impulse
control.
Refer to section Endorphin Agonists.
Refer to section Endorphin Agonists.
Suppresses neuronal excitability in concentration-
Moderate ethanol consumption has health
dependent manner.
benefits, perhaps due to antioxidant action.
Active ingredient: THC. Cannabinoid receptors found in cortex, hippocampus, and other areas of brain.
Stimulation decreases formation of cAMP reduce activity of NA, DA, glutamate and other pathways.

Refer to phenobarbital.
Refer to phenobarbital.

Refer to section Anxiety and Anxiolytics.
Refer to section Anxiety and Anxiolytics.
Blocks reuptake of NA and DA.

Dizziness, ataxia, diplopia.

Dizziness, ataxia, diplopia.

Sedation, ataxia.
GI upset, nausea, vomiting, drowsiness.
Ataxia, sedation, dizziness, headaches,
tremors.
Sedation, dizziness, headache, nausea,
rash.
Sedation, hypnosis, drug interactions.
Overdose is fatal.
Nystagmus, ataxia, sedation, gingival
hyperplasia, hirsutism.
Nausea, vomiting, gastric pain, heartburn.
Rare hepatotoxicity.
High doses activate DA reward pathways
abuse potential. Insomnia. Appetite and
growth suppression by NA. Drug holidays
when therapeutic action not needed.
Tolerance, addiction.
Tolerance, addiction. Contraindicated in
those with CV problems.
Nervousness, insomnia, drowsiness.
Tolerance, addiction, withdrawal.
Constipation.
Itching, nausea, vomiting, drowsiness, dry
mouth.
May induce psychosis in the elderly.
Nausea, vomiting, sedation.
Itching, nausea, vomiting, drowsiness, dry
mouth.
Nausea, nervousness, restlessness,
trembling, vomiting
Aspirin: overdose produces lethargy,
hyperventilation (fatal acidosis in
children). Inhibiting COX I: GI
irritation/ulceration, reduced coagulation.
Sulfonamide moiety may cause allergic
reactions. Teratogenic.
Reduces PGI2 but not TBX-A2 increased
platelet stickiness and reduced
vasodilation.
In many OTC products easily overdose
liver damage.
Addiction. Withdrawal.
High doses activate DA reward pathways
abuse potential. Insomnia. Appetite and
growth suppression by NA. Drug holidays
when therapeutic action not needed.
Tolerance, addiction.
Tachycardia, flushing, nausea.
Tolerance, addiction. Contraindicated in
those with CV problems.
Nervousness, insomnia, drowsiness.
Refer to section Endorphin Agonists.
N/A
N/A
Refer to phenobarbital.
Refer to section Anxiety and Anxiolytics.

Hallucinogenic Recreational Drugs

Drug Abuse cont.

CNS Pharmacology cont.

Endocrine

Richardson cont.

Oxytocics
Tocolytics

Oxytocics and Tocolytics

Gonadal Hormones, OCP, and Inhibitors of Gonodal Function

TMA, MDA, MDMA

N/A

Phencyclidine

Dose dependent. Unsteady gait, slurred

speech, bloodshot eyes, etc.

Selective
Estrogen
Receptor
Modulator

Clomiphene

Partial agonist blocking estrogen-mediated inhibition of

FSH/LH release from anterior pituitary.

Promote increased FSH/LH, thus promoting

ovulation and fertility.

Hot flashes, abdominal discomfort, visual

blurring.

Dopamine
D2 Agonists

Bromocriptine/
Cabergoline

Bind to D2 receptors on pituitary lactotrophs and

decrease production and release of PRL. Mimics the role
of dopamine.

Hyperprolactinemia, galactorrhea
amenorrhea, loss of menstrual cycle, infertile
males, Parkinsonism, acromegaly.

Nausea, orthostatic hypotension,

headaches, vomiting.

Synthetic
Vasopressin
replace-
ment

DDAVP

Selective V2 agonist and 4000x more potent that AVP

and longer acting. No V1 mediated adverse effects of
vasoconstriction or hepatic glycogenolysis.

Neurogenic diabetes insipidus. Hemophilia A.

Von Willebrands disease.

Headaches, facial flushing, nausea,

hyponatremia, seizures.

At term: induction of labor. Preterm:

augment incomplete abortion. Postpartum:
control hemorrhage, milk letdown.

H2O intoxication, hyponatremia.

Postpartum hemorrhage and uterine atony.

Nausea, vomiting, vasoconstriction, angina.

Ergot
Alkaloids

Oxytocin
Ergonovine/
Ergometrine

Released from posterior pituitary dilates cervix,

contracts myometrium and myoepithelial cells in
breasts. Positive feedback.
Stimulates both pregnant and non-pregnant uterus by
activating 1 receptors in myometrium.

Prosta-
glandins

PGF2/PGE2

Ripening and dilation of cervix. Increase uterine

contractions.

Steroid

Mifepristone
(RU486)

Potent progesterone antagonist, glucocorticoid

antagonist.

Terbutaline

Force Ca2+ out of myometrial cells.

Nifedipine

Inhibits Ca2+ influx via L-type channels in non-vascular

muscle cells.

2 Selective
Agonist
Ca2+
Channel
Blocker
NSAIDs

Other
Contra-
ceptives

Indomethacin
Atosiban
Leuprolide
acetate/
Abarelix
Progesterone
Mini pill
Norplant
Diethylstilbestrol

Postcoital
Pill and
Aborti-
faceint
Selective
Estrogen
Receptor
Modulators
Progest-
erone
Antagonist
Androgens

Antiandrogens

Methotrexate
Fulvestrant
Tamoxifen
Clomiphene
Raloxifene

Decrease production of prostaglandins by COX

inhibition.
Inhibitor of hormones oxytocin and vasopressin.
Desensitizes and down-regulates Gn-RH receptors on
pituitary.
Uterus: endometrial secretory mucus during luteal
phase. Cervix: thick, viscous mucous plug. Negative
nitrogen balance and increased basal body temperature.
Contains only low-progesterone and no estrogen. See
above.
Parenteral progesterone. Single injection in special
implant containing progestin.
High dose of EE2 for 3-5 days along with an anti-emetic.
Cytotoxic agent for placenta. Stimulate uteral
contractions, leading to expulsion.
Steroid. Pure competitive antagonist, a derivative of
estradiol.
Non-steroidal. Partial agonist, blocks estrogen receptors
in breast.
Non-steroidal. Blocks estrogen-induced inhibition of
FSH/LH release ovulation.
Non-steroidal. Mimics estrogen effect on bone and
decreases parathormone induced bone resorption.

Mifepristone
(RU486)

Steroid. Competitive antagonist of progesterone

terminate pregnancy during first 53 days.

17-testosterone

Stimulate and control androgenic development.

Stanozol

Selective anabolic steroid with less androgenic activity.

Leuprolide
acetate

Synthesis inhibitor. Desensitize receptors to reduce

FSH/LH release.
Synthesis inhibitor. Steroid that inhibits conversion of
testosterone to DHT by inhibiting 5 reductase.
Antiandrogen. Non-steroid competes with DHT for
androgen receptors, blocking testosterone action.
Antiandrogen. Steroid that is most potent blocker of
DHT receptor.
Synthesis inhibitor: steroid that inhibits 17
hydroxylase. Antiandrogen: blocks DHT receptors in
hair follicles.

Finasteride
Flutamide
Cyproterone
Spironolactone

Reduce Gastric
Acid Secretion

Tolerance develops to hallucinogenic

action. Cross tolerance develops to drugs
sharing same mechanism of action, but not
across mechanisms.

Produces altered body image detachment

of mind from body. Induces state very
similar to psychosis. Angel dust.

Steroid
Hormone

Antiulcer Agents

Peyote cactus.
Magic mushrooms.

Various plants, jimson weed, locoweed.

Gn-RH
Antagonists

Androgens and Antiandrogens

LSD.
Increase neural activity in NA, DA, and 5-HT pathways.

Dissociative anesthetic agent. Agonist at the pcp

receptor, which modulates the NMDA glutamate
receptor.

Ideal Drug

Upper Gastrointestinal Tract

Lysergic acid
diethylamide
Mescaline
Psilocybine
Amphetamine
analogs
Atropine/
Scopolamine/
Benztropine

Reduce activity in ACh pathways.

Nona-
peptide

Gopal

Uterine contractility, migraines, peripheral

vasoconstriction. Morning glory seeds.

Ergotamines

Induction of labor. Combine with

Mifepristone to terminate pregnancy in first
trimester.
Cushing syndrome. Abortion during first 2
months.
Selective to uterus, orally effective, less toxic
on fetus.

Nausea, vomiting, uterine pain.

No long-term studies as of yet.
Tachycardia, hypotension, pulmonary
edema, hyperglycemia.

Delay premature labor.

Headache, constipation, tachycardia,

hypotension.

Dysmenorrhea, menorrhagia.

GI irritation, nephritic syndromes.

Premature labor.

Still under review.

Prostatic cancer. Endometriosis.

Flushing, headache, hot flashes.

Leuprolide: initial flare

Given as combined oral contraceptive pill or

progesterone-only pill.
For patients suffering estrogen side effects.
Implantation under skin can last up to 5
years.
Pregnancy termination.
Early management of estrogen-dependent
breast carcinoma (when Tamoxifen fails).
Early stages of estrogen-dependent breast
carcinoma.
Secondary amenorrhea, anovulatory
menstrual cycles.
Osteoporosis in postmenopausal women.

Decreased HDL, increased LDL,

thrombophlebitis. Acne, hirsutism, weight
gain.
Irregular menstrual bleeding, spotting,
headache.
Menstrual irregularities may lead to
anxiety.
Nausea, vomiting.
Nausea, abdominal pain, fatigue. Highly
teratogenic.
None listed.
Endometrial carcinoma. Enhance deep
vein thrombosis, pulmonary embolism.
Hot flushes, alopecia, headaches, multiple
pregnancy, ovarian hyperstimulation.
Deep vein thrombosis, pulmonary
embolism.

Cushings syndrome, endometriosis.

No long-term studies as of yet.

Hypogonadism, osteoporosis, trauma, post

operative convalescence, intractable anemia.

Acne, prostatic hyperplasia and

hypertrophy. Behavioral changes,
cholestatic jaundice.

Prostate cancer.

Initial flare.

Prostate cancer, hirsutism.

Impotence, gynecomastia. Teratogenic.

Prostate cancer. Flutamide combined with

leuprolide gives no initial flare.
Hirsutism. Decreased libido and aggression
in male sex offenders.

Hepatotoxic. Gynecomastia.
Hepatotoxic.

Hirsutism, primary hyperaldosteronism.

Antihypertensive, K sparing diuretic.

Gynecomastia.

H2 Receptor
Blocker

Cimetidine

Inhibits 90% of acid secretion.

Gastric/duodenal ulcers. Zollinger-Ellison

syndrome.

Confusion, somnolence, headache,

dizziness. Skin rashes, myalgia, itching.
Gynecomastia, impotence. Inhibits
CYP450.

Proton
Pump
Inhibitor

Omeprazole

Irreversible inhibitor of H+ K+ ATPase proton pump

block 98% of acid secretion.

Ulceration. Zollinger-Ellison syndrome. No

need to combine H2 blocker with PPI unless
in ZES.

Headache, diarrhea, abdominal pain,

nausea, dizziness.

NaHCO3
Al(OH)2
Ca(CO)3
Mg(OH)2

Acid neutralization.

Immediate pain relief, but short duration of

effect rebound gastric acid secretion.

Sucralfate

Stimulates PGE1 production, adsorbs pepsin, gives a

protective gel coating.

Ulcers.

Misoprostol

Mimics PGE1, enhances production of mucus and HCO3.

Bismuth chelate

Increases mucous and prostaglandin production.

Neutralize
Acids

Enhance
Mucosal
Defense

Very effective in drug-induced peptic ulcers

by NSAIDs/corticosteroids.

Eradicates H. pylori.

Systemic alkalosis, fluid retention.

Constipation, hypophosphatemia.
Hypercalcemia, nephrolithiasis.
Diarrhea, hypermagnesemia.
Constipation, dry mouth. Decreases
bioavailability of other drugs.
Diarrhea. Contraindicated in pregnancy.

Prokinetic Agents

Antiemetics

Domperidone
Non-
antiemetics

Antiemetics
Anti-
migraine

Antiemetics and Antimigraine

Dopamine
Antagonists

5-HT3
Selective
Antagonists
Cannab-
inoids
Cortico-
steroids
Substance P
Antagonists

Triptans

Ultra Rapid
Acting

Interm.
Acting

Dimenhydrinate

Long Acting

Block inhibitory presynaptic D2 receptor increase

ACh.
Activates presynaptic 5-HT4 receptors increase ACh.
Increases cholinergic transmission in gastroduodenal
region.
Activate neural and smooth muscle motilin receptors.
Increase ACh release.
Block H1 receptors and prevent peripheral stimulation
of emetic center.

Scopolamine

Block peripheral stimulation of emetic center.

Lorazepam/
Alprazolam

Prevent central cortical induced vomiting. Enhance

effectiveness of antiemetic regimens.
Non-selective DA antagonist. Act at CTZ by inhibitng
dopaminergic transmission and decrease vomiting by
inhibitng peripheral vagal and sympathetic afferents.

Phenothiazines
Metoclopramide/
Domperidone
Ondansetron (1st)
Palonesetron
(2nd)
Tetrahydro-
cannabinol
Dexamethasone

Increase gastric emptying. Relieve gastric

stasis. Prevent reflux esophagus, heart burn,
and regurgitation of gastric contents.
Decrease nausea, vomiting. Aid in
overcoming postvagotomy gastroparesis or
prior to small bowel intubation.
Motion sickness and inner dysfunctions
(Meniers disease and Labrynthitis).
Motion sickness.
Anxiety, anticipatory emesis (chemotherapy).
Not used anymore due to side effects.

D2 selective antagonists. Selective blockade of D2 CTZ

receptors.
Anticipatory emesis (chemotherapy).
Inhibit serotonin mediated responses by blocking 5-HT3
receptors involved in vomiting reflex. Most effective.

Not available.

Aprepitant

Control emesis when all other agents fail.

Feelings of well-being. Anticipatory emesis.
Control emesis in motion sickness from
mountaineering. Anticipatory emesis.
Combine with Dexamethasone and
Palonesetron for late cancer (CINV).

Selectively constrict collateral blood vessels.

Headaches, migraines.

Lispro

Analog of human insulin: B28Proline and B29Lysine are

switched to B28Lys-B29Pro.

Aspart

Analog of human insulin: B28Proline is replaced with

B28Aspartate.

Dissolve rapidly at site of administration and

enters 2x faster than regular very short
action. Immediate use before meals only.
Increasing dose only increases intensity, not
duration.
Used intravenously during emergencies.
Administered subcutaneously in ordinary
maintenance regimens.

Regular
crystalline insulin
NPH

Glargine
Detemir

Sulfonyl-
ureas

Glyburide

Miglitinides

Repaglinide

Biguanides

Crystalline zinc insulin. Rapid onset and short action.

Used alone or mixed with intermediate- or long-acting
preparations.
Neutral protamine Hagedorn insulin. Protamine: protein
isolated from rainbow trout sperm in a zinc
suspension.
Used to provide basal insulin level. Injected morning
only, or morning and evening to provide maintenance
for 12-24 hours. Withdrawn from market.
Two additional arginine residues in B-chain and one
glycine in place of A21Aspargine.
Deletion of B30 threonine and the attachment of a 14-
carbon fatty acid chain to B29Lysine.
Inhibit K+ATP channels in -cell membrane. May
increase number of functional insulin receptors in
peripheral tissues or increase insulin sensitivity.

Crosses BBB. Hyperprolactinemia,

iatrogenic Parkinsonism.
Does not cross BBB. Hyperprolactinemia.
Torsades de pointes (long QT syndrome).
Watery diarrhea (although useful in
constipation).
Drowsiness, sedation, blurred vision, dry
mouth.
Dry mouth, drowsiness, blurred vision,
tachycardia.
Drowsiness.
Acute dystonic reaction, orthostatic
hypotension, extrapyramidal side effects,
blood dyscrasias.
Metoclopramide precipitates
extrapyramidal AEs (domperidone does
not).
None listed.

Sumatriptan/
Naratriptan

Lente

Subcutaneous injection, not suitable for

intravenous use. NPH preferred when mixing
with regular insulin, because lente can retard
onset of regular insulin.

Hallucination, bulimia.
Osteoporosis, Cushingoid features,
hyperglycemia, peptic ulcers, etc.
Not available.
Mild pain, stinging/burning sensation,
feeling of heaviness or pressure in the
head. Contraindicated: angina and
peripheral vascular disease.

Hypoglycemia: tachycardia, confusion,

vertigo, diaphoresis, possible brain
damage. Treatment: prompt
administration of glucose or glucagon.

Insulin-induced immunologic
complication: formation of insulin
antibodies.

Subcutanous injection once or twice daily.

Basal insulin level may be supplemented
with injection of lispro or regular during the
day to meet required carbohydrate intake.
Hypoglycemic drug.

Drug-induced hypoglycemia, skin rash,

allergy.

Stimulate release of endogenous insulin by inhibiting

K+ATP channels in -cell membrane.

Hypoglycemic drug. Unlike sulfonylureas,

repaglinide has rapid onset and short action.
Taken before meals to control postprandial
glucose concentrations.

No effect on patients lacking -cells.

Metformin

Increase number/affinity of insulin receptors in

peripheral tissues. Reduce hepatic output. Stimulate
glucose uptake and glycolysis in skeletal muscle and
adipose tissue. Doesnt stimulate insulin release from -
cells.

First-line drug for T2DM, especially in

patients with obesity and/or hyperlipidemia.
Used alone or combine with sulfonylurea.

GI distress: nausea, diarrhea. Lactic

acidosis (rare) in patients with renal/liver
disease, alcoholism, etc.

Thiazolidin
ediones

Rosiglitazone/
Pioglitazone

Activate PPAR- in adipose tissue, skeletal muscle, and

liver. Regulates transcription of genes encoding proteins
involved in carbohydrate and lipid metabolism. Increase
GLUT4 expression.

Used alone or combined with other

antidiabetic drugs.

Edema, mile anemia. Both increase risk of

heart failure. Rosig: increase risk of MI and
death.

-
glucosidase
Inhibitor

Acarbose

Inhibits -glucosidase, slows absorption of

carbohydrates, reduces postprandial hyperglycemia.

Used alone or combined with other

antidiabetic drugs. No effect on fasting blood
sugar.

Flatulence, diarrhea, cramping.

Synthetic
Levothyroxine
(T4)

Preferred. Long half-life (7 days), oral bioavailability

80%. Orally once a day.

Replace-
ment
Therapy

Liothyronine (T3)

Faster-acting, higher oral bioavailability (95%), but

shorter half-life (1 day). More expensive.

Treatment for all forms of hypothyroidism is

replacement therapy with either T4 or T3.

Excessive doses similar to effects of

hyperthyroidism. Contraindications with
oral anticoagulants, antidiabetic drugs,
female hormones.

Thioureas

Propylthiouracil/
Methimazole

Inhibit peroxidase-catalyzed steps (iodination &

coupling).
PTU: also inhibits conversion of T4 to T3 in peripheral
tissues.

Graves disease, to induce remission or

control symptoms prior to surgery or RAI
treatment. Requires 3-4 weeks for full effect.

Skin rash (common), severe immune

reactions (rare). Contraindicated with
pregnancy crosses placenta.

Iodide Salts

Lugols solution

Inhibit iodination of tyrosine & thyroid hormone

release. Decrease size and vascularity of hyperplastic
thyroid gland.

Short-term basis to treat thyroid storm.

Prepare for thyroid surgery. Inhibit release of
thyroid hormones following RAI therapy.

Skin rashes. Other hypersensitivity

reactions.

Iodinated
Radiocon-
trast Media

Ipodate

Suppress conversion of T4 to T3 in liver, kidney, and

other peripheral tissues.

Very useful in rapidly reducing T3

concentrations in thyrotoxicosis.

Uncommon.

RAI
Therapy

Radioactive
iodine (131I)

Ablation of thyroid tissue. RAI taken up and

concentrated in thyroid gland.

Most popular method. Emit particles that

destroy thyroid tissue without endangering
other tissues.

Should not be used in pregnant or nursing

women.

Parathyroid
Hormone

Acts on membrane G-protein coupled receptor to

increase cAMP in bone and renal tube. Net effect:
increase circulating Ca2+, decrease PO4-.

Substitute for PTH replacement.

Primary/secondary parahyperthyroidism.

Vitamin D3

Functions as a true hormone. Net effect: increase

circulating Ca2+ and PO4-. Bone formation may be
increased.

Osteomalacia (Rickets).

Overdose: hypercalcemia, toxicity.

Osteo-
porosis

Insulin Preparations
Hyperthyroidism

Thyroid and Anti-Thyroid Agents

Hypothy-
roidism

Four (roughly) Major Classes of

Oral Antidiabetic Agents

Insulin and Antidiabetic Drugs

Rapid
Acting

Wu

Cisapride
Erythromycin

Anti-
histamine
Anti-
cholinergic
Benzo-
diazepines

Drugs
Affecting
Bone
Drugs in Bone
Mineral
Homeostasis

Metoclopramide

Raloxifene/
Estrogen

Inhibition of PTH-stimulated bone resorption. Inhibit

secretion of IL-6 by osteoblasts decrease osteoclast
differentiation and activation.

Alendronate

Inhibits osteoclast-mediated bone-resorption. Used in

place or in addition to estrogen.

Calcitonin

Secreted by C (clear) cells of thyroid in response to

increased plasma Ca2+ levels. Inhibits activity of
osteoclasts.

Bisphosphonates

Inhibits osteoclast-mediated bone-resorption.

Plicamycin

Cytotoxic antibiotic as potent osteoclast inhibitor.

Abnormal
Mineralization

Drugs Affecting Bone cont.

Wu cont.

Osteo-
porosis
cont.

Pagets
Disease

Prevent or delay bone loss in

postmenopausal women.
Postmenopausal or glucocorticoid-induced
osteoporosis. Prevent bone loss and decrease
fractures.
Decreases bone resorption without
disturbing mineralization. Protect during
periods of Ca2+ loss: pregnancy, lactation.
Treat Pagets disease of bone, hypercalcemia,
osteolytic bone lesions in cancer patients.
May decrease tumor burden on bone, bone
pain, and risk of fractures.
Hypercalcemia and bone resorption in
Pagets disease.

Hot flashes, leg cramps. Possible blood

clots.
Esophageal ulceration. Skin rash.
None listed.
Esophageal ulceration (oral
administration). Mild and transient
nausea, dyspepsia, constipation, diarrhea.
Hemorrhage, hepatic and renal damage,
and frequent nausea/vomiting.