PRESCRIPTION FOR

SUCCESS ON THE BOARDS

A review compiled by:

Siamak Kazemi, DO, PharmD, R. Ph.
Thomas L. Mertz, DO, PharmD, R. Ph.
Momamad Sobh, DO, BSPharm., R. Ph.
Rahul Sood, DO, BSPharm., R. Ph.

Note from Wayne A. Krueger, Ph.D. (Bradenton Campus): All four of these
Osteopathic Physicians are graduates from LECOM. Tom was in our first
PBL class, and both Siamak and Rahul were in the next class. Mo was in the
lecture-based program, but since was an outstanding and well-qualified
student (and one of my pals), he helped put together the attached set of
"PHARMACOLOGY ONE-LINERS." I am very proud of their excellent work.
Items with an * are the highest yield items.

Basic Pharmacokinetics
Time it takes for amount of drug to fall to half of its value,
constant in first order kinetics (majority of drugs)

Half-life (T1/2)

Relates the amount of drug in the body to the plasma

concentration

Volume of distribution (VD)

Plasma concentration of a drug at a given time

Cp

The ratio of the rate of elimination of a drug to its plasma

concentration

Clearance (CL)

The elimination of drug that occurs before it reaches the

systemic circulation

First pass effect

The fraction of administered dose of a drug that reaches

systemic circulation

Bioavailability (F)

When the rate of drug input equals the rate of drug elimination

Steady state

Metabolism
This step of metabolism makes drug more hydrophilic and
hence augments elimination

Different steps of Phase I

Phase I

Oxidation, reduction,
hydrolysis

Inducers of Cytochrome P450 (CYP450)

*
Inhibitors of CYP450

Barbiturates, phenytoin,
carbamazepine, and rifampin

Cimetidine, ketoconazole,
erythromycin, isoniazid and
grapefruit

Products of Phase II conjugation

Glucuronate, acetic acid,

and glutathione sulfate

Constant percentage of substrate metabolized per unit time

First order kinetics

Drug elimination with a constant amount metabolized

regardless of drug concentration

Zero order kinetics

Page 2

Target plasma concentration times (volume of distribution

divided by bioavailability)

Loading dose (Cp*(Vd/F))

Concentration in the plasma times (clearance divided by

bioavailability)

Maintenance dose
(Cp*(CL/F))

Pharmacodynamics
Strength of interaction between drug and its receptor

Affinity

Selectivity of a drug for its receptor

Specificity

Amount of drug necessary to elicit a biologic effect

Potency

Ability of drug to produce a biologic effect

Efficacy

Ability of a drug to produce 100% of the maximum response

regardless of the potency

Full agonist

Ability to produce less than 100% of the response

Partial agonist

Ability to bind reversibly to the same site as the drug and

without activating the effector system

Competitive antagonist

Ability to bind to either the same or different site as the drug

Noncompetitive antagonist

Mechanism of action (MOA) utilizes intracellular receptors

Thyroid and steroid

hormones

MOA utilizes transmembrane receptors

Insulin

MOA utilizes ligand gated ion channels

Benzodiazepines and
calcium channel blockers

Median effective dose required for an effect in 50% of the

population

ED50

Median toxic dose required for a toxic effect in 50% of the

population

TD50

Dose which is lethal to 50% of the population

LD50

Page 3

Window between therapeutic effect and toxic effect

Therapeutic index

Drug with a high margin of safety

High therapeutic index

Drug with a narrow margin of safety

Low therapeutic index

Antidotes and agents used in drug overdose

Antidote used for lead poisoning

Dimercaprol, EDTA

Antidote used for cyanide poisoning

Nitrites

Antidote used for anticholinergic poisoning

Physostigmine

Antidote used for organophosphate/anticholinesterase

poisoning

**

Antidote used for iron salt toxicity

Atropine, pralidoxime (2PAM)

Deferoxamine

Antidote used for acetaminophen (APAP) toxicity

Antidote for severe lead poisoning

N-acetylcysteine

Antidote for arsenic, mercury, and gold poisoning

Dimercaprol + CaEDTA
(edetate calcium disodium)
Dimercaprol

Antidote used in Wilson's disease (copper poisoning)

Penicillamine

Antidote used for heparin toxicity

**

Protamine Sulfate

Antidote used for warfarin toxicity

Vitamin K and Fresh frozen

plasma (FFP)

Antidote for tissue plasminogen activator (t-PA), streptokinase

**

Aminocaproic acid

Antidote used for methanol and ethylene glycol

Ethanol

Antidote used for opioid toxicity

Page 4

Naloxone (IV), naltrexone

(PO)

Antidote used for benzodiazepine toxicity

Flumazenil

Antidote used for tricyclic antidepressants (TCA)

Sodium bicarbonate

Antidote used for carbon monoxide poisoning

100% O2 and hyperbaric O2

Antidote used for digitalis toxicity

Digibind (also need to d/c

digoxin, normalize K+, and
lidocaine if pt. Is arrhythmic)

Antidote used for beta agonist toxicity (eg. Metaproterenol)

Esmolol

Antidote for methotrexate toxicity

Leucovorin

Antidote for beta-blockers and hypoglycemia

Glucagon

Antidote useful for some drug induced Torsade de pointes

Magnesium sulfate

Antidote for hyperkalemia

sodium polystyrene
sulfonate (Kayexalate)

Antidote for salicylate intoxication

Alkalinize urine, dialysis

Cancer Chemotherapy
Constant proportion of cell population killed rather than a
constant number

Log-kill hypothesis

Treatment with cancer chemotherapy at high doses every 3-4

weeks, too toxic to be used continuously

Pulse therapy

Toxic effect of anticancer drug can be lessened by rescue

agents

Rescue therapy

Drug used concurrently with toxic anticancer agents to reduce

renal precipitation of urates

Allopurinol

Pyrimidine analog that causes "Thiamine-less death" given

with leucovorin rescue

5-flouracil (5-FU)

Page 5

Drug used in cancer therapy causes Cushing-like symptoms

Prednisone

Side effect of Mitomycin

SEVERE myelosuppression

MOA of cisplatin

Alkylating agent

Common toxicities of cisplatin

Nephro and ototoxicity

Analog of hypoxanthine, needs HGPRTase for activation

6-mercaptopurine (6-MP)

Interaction with this drug requires dose reduction of 6-MP

**

Allopurinol

May protect against doxorubicin cardio-toxicity by chelating

iron

Dexrazoxane

Blows DNA (breaks DNA strands), limiting SE is pulmonary

fibrosis

Bleomycin

Bleomycin+vinblastine+etoposide+cisplatin produce almost a

100% response when all agents are used for this neoplasm

Testicular cancer

MOPP regimen used in Hodgkin's disease (HD)

Mechlorethamine+
oncovorin (vincristine)+
procarbazine, and
prednisone

ABVD regimen used for HD, but appears less likely to cause
sterility and secondary malignancies than MOPP

Adriamycin (doxorubicin)
+bleomycin, vinblastine
+dacarbazine

Regimen used for non-Hodgkin's lymphoma

COP (cyclophosphamide,
oncovin(vincristine), and
prednisone)

Regimen used for breast cancer

CMF (cyclophosphamide,
methotrexate, and
fluorouracil) and tamoxifen if
ER+

Alkylating agent, vesicant that causes tissue damage with

extravasation

Mechlorethamine

Page 6

Anticancer drug also used in RA, produces acrolein in urine

that leads to hemorrhagic cystitis

Cyclophosphamide

Prevention of cyclophosphamide induced hemorrhagic cystitis

Hydration and
mercaptoethanesulfonate
(MESNA)

Microtubule inhibitor that causes peripheral neuropathy , foot

drop (eg. ataxia), and "pins and needles" sensation

Vincristine

Binds tubulin and prevents the disassembly of microtubules

during the M phase of the cell cycle inducing mitotic arrest

**

Paclitaxel (taxol)

Toxicities include nephrotoxicity and ototoxicity, leading to a

severe interaction with aminoglycosides

Cisplatin

Agent similar to cisplatin, less nephrotoxic, but greater

myelosuppression

Carboplatin

Converts asparagine to aspartate and ammonia, denies

cancer cells of essential AA (asparagine)

L-asparaginase

Used for hairy cell leukemia ; it stimulates NK cells

Interferon alpha

Anti-androgen used for prostate cancer

Flutamide (Eulexin)

Anti-estrogen used for estrogen receptor + breast cancer

**

Tamoxifen

Newer estrogen receptor antagonist used in advanced breast

cancer

Toremifene (Fareston)

Some cell cycle specific anti-cancer drugs

Bleomycin, vinca alkaloids,

antimetabolites (eg., 5-FU, 6MP, methotrexate,
etoposide)

Some cell cycle non-specific drugs

Alkylating agents (eg.,

mechlorethamine,
cyclophosphamide),
antibiotics (doxorubicin,
daunorubicin), cisplatin,
nitrosourea

Anti-emetics used in association with anti-cancer drugs that

are 5-HT3 (serotonin receptor subtype ) antagonist

Page 7

Odansetron, granisetron,
dolasetron, palonosetron

Nitrosoureas with high lipophilicity, used for brain tumors

Carmustine (BCNU) and

lomustine (CCNU)

Alkylating agent that produces disulfiram-like reaction with

ethanol

Procarbazine

Endocrine drugs: hypothalamic and pituitary hormones

Somatostatin (SRIF) analog used for acromegaly, carcinoid,
glucagonoma and other GH producing pituitary tumors

Octreotide

Somatotropin (GH) analog used in GH deficiency (dwarfism)

Somatrem

GHRH analog used as diagnostic agent

Sermorelin

GnRH agonist used for infertility or different types of CA

depending on pulsatile or steady usage respectively

Leuprolide

GnRH antagonist with more immediate effects, used for

infertility

Ganirelix

Dopamine agonist used to treat hyperprolactinemia

Bromocriptine

Hormone inhibiting prolactin release

Dopamine

ACTH analog used for diagnosis of patients with corticosteroid

abnormality

**

Cosyntropin

Synthetic analog of ADH hormone used for diabetes insipidus

and nocturnal enuresis

Desmopressin (DDAVP)

**

L-thyroxine (T4)

Thyroid and anti-thyroid drugs

Most widely used thyroid drugs such as Synthroid and Levoxyl
contain
T3 compound less widely used

Cytomel

Anti-thyroid drugs

Thioamides, iodides,
radioactive iodine, and
ipodate

Page 8

Thioamide agents used in hyperthyroidism

Methimazole and
propylthiouracil (PTU)

Thioamide less likely to cross placenta, inhibits peripheral

conversion of T4 to T3 in high doses, and should be used with
extreme caution in pregnancy

PTU

PTU (propylthiouracil) MOA

Inhibits thyroid hormone

synthesis by blocking
iodination of the tyrosine
residues of thyroglobulin

Can be effective for short term therapy of thyroid storm, but

after several weeks of therapy causes an exacerbation of
hyperthyroidism

Iodide salts

Permanently cures thyrotoxicosis , patients will need thyroid

replacement therapy thereafter. Contraindicated in pregnancy

Radioactive iodine

Radio contrast media that inhibits the conversion of T4 to T3

Ipodate

Block cardiac adverse effects of thyrotoxicosis such as

tachycardia, inhibits the conversion of T4 to T3

Beta-blockers such as
propranolol

Adrenocorticosteroid and adrenocortical antagonists

3 zones of adrenal cortex and their products

Glomerulosa
(mineralocorticoids),
fasciculata
(glucocorticoid=GC), and
reticularis (adrenal
androgens)

Pneumonic for 3 zones of adrenal cortex

GFR

Used for Addison's disease , Congenital Adrenal Hyperplasia

(CAH) , inflammation, allergies, and asthma (as a local
inhalation)

Glucocorticoids

Short acting GC's

Cortisone and
hydrocortisone (equivalent
to cortisol)

Page 9

Intermediate acting GC's

Prednisone,
methylprednisolone,
prednisolone, and
triamcinolone

Long acting GC's

Betamethasone,
dexamethasone, and
paramethasone

Mineralocorticoids

Fludrocortisone and
deoxycorticosterone

Some side effects of corticosteroids

Osteopenia, impaired wound

healing, inc. risk of infection,
inc. appetite, HTN, edema,
PUD, euphoria, psychosis

Period of time of therapy after which GC therapy will need to

be tapered

5-7 days

Inhibitors of corticosteroids biosynthesis

Used for Cushing's syndrome (increased corticosteroid) and
sometimes for adrenal function test

Metyrapone

Inhibits conversion of cholesterol to pregnenolone therefore

inhibiting corticosteroid synthesis

Aminoglutethimide

Antifungal agent used for inhibition of all gonadal and adrenal

steroids

Ketoconazole

Antiprogestin used as potent antagonist of GC receptor

Mifepristone

Diuretic used to antagonize aldosterone receptors

Spironolactone

Common SE of spironolactone

**

Gynecomastia and
hyperkalemia

Gonadal hormones and inhibitors

Slightly increased risk of breast cancer, endometrial cancer,
heart disease (questionable), has beneficial effects on bone
loss

Estrogen

Antiestrogen drugs used for fertility and breast cancer

respectively

Clomiphene and tamoxifen

Page 10

Common SE of tamoxifen and raloxifene

Hot flashes

Selective estrogen receptor modulator (SERM) used for

prevention of osteoporosis and currently being tested for
treatment of breast cancer (Stars study)

Raloxifene

**

Non-steroidal estrogen agonist causes clear cell

adenocarcinoma of the vagina in daughters of women who
used it during pregnancy

Diethylstilbestrol (DES)

Estrogen mostly used in oral contraceptives (OC)

Ethinyl estradiol and

mestranol

Anti-progesterone used as abortifacient

Mifepristone (RU-486)

Constant low dose of estrogen and increasing dose of

progestin for 21 days (last 5 days are sugar pills or iron prep)

Combination oral
contraceptives (OC)

Oral contraceptive available in a transdermal patch

Ortho-Evra

Converted to more active form DHT by 5 alpha-reductase

Testosterone

5 alpha-reductase inhibitor used for benign prostatic

hyperplasia (BPH) and male pattern baldness

Finasteride (Proscar and

Propecia respectively)

Anabolic steroid that has potential for abuse

Nandrolone and stanozolol

Anti-androgen used for hirsutism in females

Cyproterone acetate

Drug is used with testosterone for male fertility

**

Leuprolide

Pancreatic hormones, antidiabetics, and hyperglycemics

Alpha cells in the pancreas

Produce glucagon

Beta cells in the pancreas

Produce insulin

Beta cells are found

Islets of Langerhans

Page 11

Delta cells in the pancreas

Produce Somatostatin

Product of proinsulin cleavage used to assess insulin

production

C-peptide

Exogenous insulin

Little C-peptide

Endogenous insulin

Normal C-peptide

Very rapid acting insulin, having fastest onset and shortest

duration of action

Lispro (Humalog)

Rapid acting, crystalline zinc insulin used to reverse acute

hyperglycemia

Regular (Humulin R)

Long acting insulin

Ultralente (humulin U)

Ultra long acting insulin, has over a day duration of action

Glargine (Lantus)

Major SE of insulin

Hypoglycemia

Important in synthesis of glucose to glycogen in the liver

GLUT 2

Important in muscle and adipose tissue for glucose transport

across muscles and TG storage by lipoprotein lipase activation

GLUT 4

Examples of alpha-glucosidase inhibitors (AGI)

Acarbose, miglitol

MOA of AGI's

Act on intestine, delay

absorption of glucose

SE of AGI's

Flatulence (do not use beano

to tx), diarrhea, abdominal
cramps

Alpha-glucosidase inhibitor associated with elevation of LFT's

Acarbose

Amino acid derivative for treatment of Type II diabetes

Page 12

Nateglinide

MOA of nateglinide

Stimulates rapid and

transient release of of
insulin through closure of
the ATP-sensitive K+ channel

Biguanide

Metformin

Drugs available in combination with metformin

Glyburide, glipizide, and

rosiglitazone

MOA of metformin

Decreases hepatic glucose

production and intestinal
glucose absorption;
increase insulin sensitivity

Most important potential SE of metformin

Lactic acidosis

Meglitinide

Repaglinide

MOA of repaglinide

Insulin release from

pancreas; faster and shorter
acting than sulfonylurea

First generation sulfonylurea

Chlorpropamide,
tolbutamide, tolazamide, etc.

Second generation sulfonylurea

Glyburide, glipizide,
glimepiride, etc.

MOA of both generations

Insulin release from

pancreas by modifying K+
channels

Common SE of sulfonylureas, repaglinide, and nateglinide

Hypoglycemia

Sulfonylurea NOT recommended for elderly because of very

long half life

Chlorpropamide

Thiazolidinediones

Pioglitazone, Rosiglitazone,
Troglitazone (withdrawn/d
from market)

Page 13

Reason troglitazone was withdrawn from market

Hepatic toxicity

MOA of thiazolindinediones

Stimulate PPAR-gamma
receptor to regulate CHO
and lipid metabolism

SE of Thiazolindinediones

Edema, mild anemia;

interaction with drugs that
undergo CytP450 3A4
metabolism

Hyperglycemic agent that increases cAMP and results in

glycogenolysis, gluconeogenesis, reverses hypoglycemia, also
used to reverse severe beta-blocker overdose and smooth
muscle relaxation

Glucagon

Drugs used in bone homeostasis

Available bisphosphonates

Alendronate, etidronate,
risedronate, pamidronate,
tiludronate, and zoledronic
acid

MOA of Bisphosphonates

Inhibits osteoclast bone

resorption

Only bisphosphonates available IV

Etidronate

Uses of bisphosphonates

Osteoporosis, Paget's
disease, and osteolytic bone
lesions, and hypercalcemia
from malignancy

Major SE of bisphosphonates

Chemical esophagitis

Bisphosphonates that cannot be used on continuous basis

because it caused osteomalacia

Etidronate

Used for prevention of postmenopausal osteoporosis in

women

Estrogen (HRT-Hormone
replacement therapy)

Increase bone density, also being tested for breast CA tx.

**

Page 14

Raloxifene (SERM-selective
estrogen receptor
modulator)

Used intranasally and decreases bone resorption

Calcitonin (salmon prep)

Used especially in postmenopausal women, dosage should be

1500 mg

Calcium

Vitamin given with calcium to ensure proper absorption

Vitamin D

Drugs with important actions on smooth muscle

Disease caused by excess ergot alkaloids

St. Anthony's Fire

Endogenous substances commonly interpreted as histamine,

serotonin, prostaglandins, and vasoactive peptides

Autocoids

Syndrome of hypersecretion of gastric acid and pepsin usually

caused by gastrinoma; it is associated with severe peptic
ulceration and diarrhea

Zollinger-Ellison Syndrome

Drug that causes contraction of the uterus

Distribution of histamine receptors H1, H2, and H3

Oxytocin

Smooth muscle; stomach,

heart, and mast cells; nerve
endings, CNS respectively

Prototype antagonist of H1 and H2 receptors

Diphenhydramine

1st generation antihistamine that is highly sedating

**

Diphendydramine

1st generation antihistamine that is least sedating

Chlorpheniramine or
cyclizine

2nd generation antihistamines

Fexofenadine, loratadine,
and cetirizine

Generation of antihistamine that has the most CNS effects

First generation due to being

more lipid-soluble

Major indication for H1 receptor antagonist

Use in IgE mediated allergic

reaction

Antihistamine that can be used for anxiety and insomnia and is

not addictive

hydroxyzine (Atarax)

Page 15

H1 antagonist used in motion sickness

Dimenhydrinate, meclizine,
and other 1st generation

Most common side effect of 1st generation antihistamines

Sedation

Lethal arrhythmias resulting from concurrent therapy with

azole fungals (metabolized by CYP 3A4) and these
antihistamines which inhibit the 3A4 iso-enzyme.

Terfenadine and astemizole

(have been removed from
the market)

H2 blocker that causes the most interactions with other drugs

Cimetidine

Clinical use for H2 blockers

Acid reflux disease,

duodenal ulcer and peptic
ulcer disease

Receptors for serotonin (5HT-1) are located

Mostly in the brain, and they

mediate synaptic inhibition
via increased K+
conductance

**

5HT-1D/1B agonist used for migraine headaches

Sumatriptan, naratriptan,
and rizatriptan

Triptan available in parenteral and nasal formulation

Sumatriptan

H1 blocker that is also a serotonin antagonist

Cyproheptadine

5HT2 antagonist mediate synaptic excitation in the CNS and

smooth muscle contraction

Ketanserin, cyproheptadine,
and ergot alkaloids (partial
agonist of alpha and
serotonin receptors)

Agents for reduction of postpartum bleeding

**

Oxytocin and ergonovine

Agents used in treatment of carcinoid tumor

**

Cyproheptadine

***

Ondansetron, granisetron,
dolasetron and
palonosetron

5HT-3 antagonist used in chemotherapeutic induced

emesis

Page 16

5ht-3 antagonist that has been MOST associated with QRS

and QTc prolongation and should not be used in patients with
heart disease
DOC of chemo induced nausea and vomiting

Dolasetron

**

Odansetron

Drug used in ergot alkaloids overdose, ischemia and gangrene

Nitroprusside

Reason ergot alkaloids are contraindicated in pregnancy

Uterine contractions

SE of ergot alkaloids

Hallucinations resembling
psychosis

Ergot alkaloid used as an illicit drug

LSD

Dopamine agonist used in hyperprolactinemia

Bromocriptine

Peptide causing increased capillary permeability and edema

Mediator of tissue pain, edema, inactivated by ACE, and may
be a contributing factor to the development of angioedema

Drug causing depletion of substance P (vasodilator)

Bradykinin and histamine

Bradykinin

*
*

Capsaicin

Prostaglandin E1
(misoprostol) PGE2, and
PGF2alpha

Prostaglandins that cause abortions

COX 1 is found throughout

the body and COX 2 is only
in inflammatory tissue

Difference between COX 1 and COX 2

Drug that selectively inhibits COX 2

Celecoxib, valdecoxib, and

rofecoxib

Inhibitor of lipoxygenase

Major SE of zileuton

Zileuton

Liver toxicity

Page 17

Inhibitor of leukotrienes (LTD4) receptors and used in asthma

Used in pediatrics to maintain patency of ductus arteriosis

Zafirlukast and montelukast

Approved for use in severe pulmonary HTN

PGE1 (Alprostadil)

PGI2 (epoprostenol)

Prostaglandin used in the treatment impotence

PGE1 (Alprostadil)

Irreversible, nonselective COX inhibitor

Aspirin

Class of drugs that reversibly inhibit COX

NSAIDS

Primary endogenous substrate for Nitric Oxidase Synthase

Arginine

MOA and effect of nitric oxide

*
Long acting beta 2 agonist used in asthma

Stimulates cGMP which

leads to vascular smooth
muscle relaxation
Salmeterol

Muscarinic antagonist used in asthma

Ipratropium

MOA action of cromolyn

Mast cell stabilizer

Enzyme which theophylline inhibits

Phosphodiesterase

Methylxanthine derivative used as a remedy for intermittent

claudication
Antidote for severe CV toxicity of theophylline

Pentoxifylline
Beta blockers

inhibit phospholipase A2
MOA of corticosteroids
SE of long term (>5 days) corticosteroid therapy and remedy

Adrenal suppression and

weaning slowly, respectively

**

Inhibit DNA gyrase

Antimicrobials
MOA of quinolones

Page 18

MOA of penicillin

Block cell wall synthesis by

inhibiting peptidoglycan
cross-linkage

Drug used for MRSA

Vancomycin

Vancomycin MOA

**

Blocks peptidoglycan
synthesis

Type of resistance found with vancomycin

Point mutation

Meningitis prophylaxis in exposed patients

Rifampin

Technique used to diagnose perianal itching, and the drug

used to treat it

Scotch tape technique

and mebendazole

Two toxicities of aminoglycosides

nephro and ototoxicity

DOC for Legionnaires' disease

Erythromycin

MOA of sulfonamides

Penicillins active against penicillinase secreting bacteria

Cheap wide spectrum antibiotic DOC of otitis media

Inhibit dihydropteroate
synthase
Methicillin, nafcillin, and
dicloxacillin

**

Amoxicillin

Class of antibiotics that have 10% cross sensitivity with

penicillins

Cephalosporins

PCN active against pseudomonas

Carbenicillin, piperacillin and

ticarcillin

Antibiotic causing red-man syndrome, and prevention

Vancomycin, infusion
at a slow rate and
antihistamines

Drug causes teeth discoloration

Tetracycline

Page 19

MOA of tetracycline

Decreases protein synthesis

by inhibiting 30S ribosome

Drug that causes gray baby syndrome and aplastic anemia

Chloramphenicol

Drug notorious for causing pseudomembranous colitis

Clindamycin

DOC for tx of pseudomembranous colitis

**

Treatment of resistant pseudomembranous colitis

Metronidazole

ORAL vancomycin

Anemia caused by trimethoprim

Reason fluoroquinolones are contraindicated in children and

pregnancy
DOC for giardia, bacterial vaginosis, pseudomembranous
colitis, and trichomonas

Megaloblastic anemia

Cartilage damage

Treatment for TB patients (think RIPE )

*
Metronidazole SE if given with alcohol

Metronidazole

R ifampin, I soniazid,
P yrazinamide, and
E thambutol
Disulfiram-like reaction

Common side effect of Rifampin

Orange urine discoloration

MOA of nystatin

Bind ergosterol in fungal cell

membrane

Neurotoxicity with isoniazid (INH) prevented by

Administration of Vit. B6
(pyridoxine)

Toxicity of amphotericin

Nephrotoxicity

SE seen only in men with administration of ketoconazole

Gynecomastia

Topical DOC in impetigo

Topical mupirocin
(Bactroban)

Page 20

DOC for influenza A and B

Oseltamivir or Zanamivir

DOC for RSV

Ribavirin

DOC for CMV retinitis

Ganciclovir

SE for ganciclovir

Myelosuppression

Anti-viral agents associated with Stephen Johnson syndrome

Nevirapine, amprenavir

HIV antiviral class known to have severe drug interactions by

causing inhibition of metabolism

Protease inhibitors

Antivirals that are teratogens

Delavirdine, efavirenz, and

ribavirin

Antivirals associated with neutropenia

Ganciclovir, zidovudine,
saquinavir, and interferon

HIV med used to reduce transmission during birth

AZT (zidovudine)

Drug used for African sleeping sickness

Suramin

Drug used in Chagas disease

Nifurtimox

Cephalosporins able to cross the BBB

Cefixime (2nd) and 3rd

generation

DOC for N. gonorrhea

Ceftriaxone

Cephalosporin causes kernicterus in neonates

Ceftriaxone or cefuroxime

SE of INH

Peripheral neuritis and

hepatitis

Aminoglycoside that is least ototoxic

Streptomycin

Drug used in exoerythrocytic cycle of malaria

Primaquine

Page 21

Oral antibiotic of choice for moderate inflammatory acne

Minocycline

Drug of choice for leprosy

Dapsone

DOC for herpes and its MOA

Acyclovir; activates
thymidine kinase

Anti-microbials that cause hemolysis in G6PD-deficient

patients

Sulfonamides

MOA of erythromycin

Inhibition of protein
synthesis at the 50s subunit
of ribosome

Anti-biotic frequently used for chronic UTI prophylaxis

sulfamethoxazole/
trimethoprim

Lactam that can be used in PCN allergic patients

Aztreonam

SE of imipenem

Seizures

Anti-viral with a dose limiting toxicity of pancreatitis

Didanosine

Sedative Hypnotics
Common side effect of hypnotic agents

Sedation

Occurs when sedative hypnotics are used chronically or at

high doses

Tolerance

The most common type of drug interaction of sedative

hypnotics with other depressant medications

Additive CNS depression

Benzodiazepines
Major effect of benzodiazepines on sleep at high doses

Neurologic SE of benzodiazepines

REM is decreased

Anterograde amnesia

Reason benzos are used cautiously in pregnancy

Main route of metabolism for benzodiazepines

Ability to cross the placenta

Hepatic

Page 22

Benzodiazepine that undergo extrahepatic conjugation (which

are useful in older or hepatically impaired)

Lorazepam, oxazepam, and

temazepam

MOA for benzodiazepines

increase the FREQUENCY of

GABA-mediated chloride ion
channel opening

Antidote to benzodiazepine overdose (antagonist that reverses

the CNS effects)

Flumazenil

Benzodiazepine with useful relaxant effects in skeletal muscle

spasticity of central origin

Diazepam

Benzodiazepine that has efficacy against absence seizures

and in anxiety states, such as agoraphobia

Clonazepam

Benzodiazepines that are the most effective in the treatment of

panic disorder

Alprazolam and Clonazepam

Benzodiazepine that is used for anesthesia

Midazolam

DOC for status epilepticus

Diazepam

Longer acting benzodiazepines used in the management of

withdrawal states of alcohol and other drugs

Chlordiazepoxide and
Diazepam

Agents having active metabolites, long half lives, and a high

incidence of adverse effects

Diazepam, Flurazepam,
chlordiazepoxide, and
clorazepate

Barbiturates
Barbiturates may precipitate this hematologic condition

Acute intermittent porphyria

Barbiturates decrease the effectiveness of many other drugs

via this pharmacokinetics property

Liver enzyme INDUCTION

Barbiturates MOA

Increase the DURATION of

GABA-mediated chloride ion
channels

Barbiturate used for the induction of anesthesia

Thiopental

Page 23

Alcohols
Important drug interaction with chloral hydrate

May displace coumadin from

plasma proteins

Others
Site of action for zaleplon and zolpidem

Benzodiazepine receptor
BZ1 (although are not
considered
benzodiazepines)

Good hypnotic activity with less CNS SE than most

benzodiazepines

Zolpidem, zaleplon

Agent that is a partial agonist for the 5-HT1A receptor

Buspirone

Drug of choice for generalized anxiety disorder, NOT effective

in acute anxiety

Buspirone

Alcohols
Agent that is metabolized to acetaldehyde by alcohol
dehydrogenase and microsomal ethanol-oxidizing system
(MEOS)

Ethanol

Agent with zero-order kinetics

Ethanol

Rate limiting step of alcohol metabolism

Aldehyde dehydrogenase

System that increases in activity with chronic exposure and

may contribute to tolerance

MEOS

Agent that metabolize acetaldehyde to acetate

Aldehyde dehydrogenase

Agents that inhibit aldehyde dehydrogenase

Disulfiram, metronidazole,
certain sulfonylureas and
cephalosporins

Agent used in the treatment of alcoholism, if alcohol is

consumed concurrently, acetaldehyde builds up and results in
nausea, headache, flushing, and hypotension

Disulfiram

The most common neurologic abnormality in chronic

alcoholics

Peripheral neuropathy (also

excessive alcohol use is
associated with HTN,
anemia, and MI)

Page 24

Agent that is teratogen and causes a fetal syndrome

Alcohol

Agent that competes for alcohol dehydrogenase in the case of

methanol overdose

Ethanol

Drug that inhibits alcohol dehydrogenase and is used in

ethylene glycol exposure

Fomepizole

Anti seizure Drugs

Most frequent route of metabolism

Hepatic enzymes

Mechanisms of action for Phenytoin, Carbamazepine,

Lamotrigine

Sodium blockade

MOA for benzodiazepines and barbiturates

GABA-related targets

MOA for Ethosuximide

Calcium channels

MOA for Valproic acid at high doses

Affect calcium, potassium,

and sodium channels

Drugs of choice for generalized tonic-clonic and partial

seizures

DOC for febrile seizures

Valproic acid, Phenytoin and

Carbamazepine
Phenobarbital

Drugs of choice for absence seizures

Ethosuximide and valproic

acid

Drug of choice for myoclonic seizures

Valproic acid

Drugs of choice for status epilepticus

IV diazepam (or lorazapam)

followed by phenytoin

Drugs that can be used for infantile spasms

Corticosteroids

Anti-seizure drugs used also for bipolar affective disorder

(BAD)

Valproic acid,
carbamazepine, phenytoin
and gabapentin

Page 25

Anti-seizure drugs used also for Trigeminal neuralgia

Anti-seizure drugs used also for pain of neuropathic orgin

Carbamazepine

Gabapentin

Anti-seizure agent that exhibits non-linear metabolism, highly

protein bound, causes fetal hydantoin syndrome, and
stimulates hepatic metabolism

Phenytoin

SE of phenytoin

Gingival hyperplasia,
nystagmus, diplopia and
ataxia

*
Anti-seizure agent that induces formation of liver drugmetabolism enzymes, is teratogen and can cause craniofacial
anomalies and spina bifida

Carbamazepine

Agent that inhibits hepatic metabolism, is hepatotoxic and

teratogen that can cause neural tube defects and
gastrointestinal distress

Valproic acid

Laboratory value required to be monitored for patients on

valproic acid

Serum ammonia and LFT's

SE for Lamotrigine

Stevens-Johnson syndrome

SE for Felbamate

Aplastic anemia and acute

hepatic failure

Anti-seizure medication also used in the prevention of

migraines

Valproic acid

Carbamazepine may cause

Agranulocytosis

Anti-seizure drugs used as alternative drugs for mood

stabilization

Carbamazepine, gabapentin,
lamotrigine, and valproic
acid

General Anesthetics
MOA of general anesthetics

Unclear, thought to increase

the threshold for firing of
CNS neurons

Inhaled anesthetic with a low blood/gas partition coefficient

Nitrous oxide

Page 26

Inversely related to potency of anesthetics

Minimum alveolar anesthetic

concentration (MAC)

Inhaled anesthetics metabolized by liver enzymes which has a

major role in the toxicity of these agents

Halothane and
methoxyflurane

Most inhaled anesthetics SE

Decrease arterial blood

pressure

Inhaled anesthetics are myocardial depressants

Enflurane and halothane

Inhaled anesthetic causes peripheral vasodilation

Isoflurane

Inhaled anesthetic that may sensitize the myocardium to

arrhythmogenic effects of catecholamines and has produced
h epatitis

H alothane

Inhaled anesthetics, less likely to lower blood pressure than

other agents, and has the smallest effect on respiration

Nitrous oxide

Fluoride released by metabolism of this inhaled anesthetic

may cause renal insufficiency

Methoxyflurane

Prolonged exposure to this inhaled anesthetic may lead to

megaloblastic anemia

Nitrous oxide

Pungent inhaled anesthetic which leads to high incidence of

coughing and vasospasm

Desflurane

DOC for malignant hyperthermia that may be caused by use of

halogenated anesthetics

Dantrolene

IV barbiturate used as a pre-op anesthetic

Thiopental

Benzodiazepine used adjunctively in anesthesia

Midazolam

Benzodiazepine receptor antagonist, it accelerates recovery

from benzodiazepine overdose

Page 27

Flumazenil

This produces "dissociative anesthesia ", is a cardiovascular

stimulant which may increases intracranial pressure, and
hallucinations occur during recovery
Opioid associated with awareness during surgery and postoperative recall, but still used for high-risk cardiovascular
surgeries

Ketamine

Fentanyl

State of analgesia and amnesia produced when fentanyl is

used with droperidol and nitrous oxide

Neuroleptanesthesia

Produces both rapid anesthesia and recovery, has antiemetic

activity and commonly used for outpatient surgery, may cause
marked hypotension

Propofol

Local Anesthetics
MOA of local anesthetics (LA's)

Block voltage-dependent
sodium channels

This may enhance activity of local anesthetics

Hyperkalemia

This may antagonize activity of local anesthetics

Hypercalcemia

Almost all local anesthetics have this property and sometimes

require the administration of vasoconstrictors (ex.
Epinephrine) to prolong activity

Vasodilation

Local anesthetic with vasoconstrictive property, favored for

head, neck, and pharyngeal surgery

Cocaine

Longer acting local anesthetics which are less dependent on

vasoconstrictors

Tetracaine and bupivacaine

These LA's have surface activity

Cocaine and benzocaine

Most important toxic effects of most local anesthetics

CNS toxicity

Commonly abused LA which has cardiovascular toxicity

including severe hypertension with cerebral hemorrhage,
cardiac arrhythmias, and myocardial infarction

Cocaine

Page 28

LA causing methemoglobinemia

Prilocaine

Skeletal Muscle Relaxants

Structurally related to acetylcholine, used to produce muscle
paralysis in order to facilitate surgery or artifical ventilation. Full
doses lead to respiratory paralysis and require ventilation

Neuromuscular blocking
drugs

These drugs strongly potentiate and prolong effect of

neuromuscular blockade (NMB)

Inhaled anesthetics,
especially isoflurane,
aminoglycosides, and
antiarrhythmic

These prevent the action of Ach at the skeletal muscle

endplate to produce a "surmountable blockade," effect is
reversed by cholinesterase inhibitors (ex. neostigmine or
pyridostigmine)

Nondepolarizing type
antagonists

Agent with long duration of action and is sost likely to cause

histamine release

Tubocurarine

Non-depolarizing antagonist has short duration

Mivacurium

Agent can blocking muscarinic receptors

Pancuronium

Agent undergoing Hofmann elimination (breaking down

spontaneously)

Atracurium

One depolarizing blocker that causes continuous

depolarization and results in muscle relaxation and paralysis,
xcuses muscle pain postoperatively and myoglobinuria may
occur

Succinylcholine

During Phase I these agents worsen the paralysis by

succinylcholine, but during phase II they reverse the blockade
produced by succinylcholine

Cholinesterase inhibitors

Spasmolytic drugs
Agents acting in the CNS or in the skeletal muscle, used to
reduce abnormally elevated tone caused by neurologic or
muscle end plate disease

Spasmolytic drugs

Facilitates GABA presynaptic inhibition

Diazepam

Page 29

GABA agonist in the spinal cord

Baclofen

Similar to clonidine and may cause hypotension

Tizanidine

DOC for malignant hyperthermia by acting on the

sacroplasmic reticulum or skeletal muscle

Agent used for acute muscle spasm

Dantrolene

Cyclobenzaprine

Drugs Used in Parkinsonism & Other Movement

Disorders
Antipsychotics, reserpine at high doses, and MPTP (byproduct of illicit meperidine analog) and is irreversible

Drug induced Parkinsonism

Agent used in drug therapy of Parkinson's instead of

Dopamine which has low bioavailability and does not cross the
BBB

L-dopa

This is combined with L-dopa, inhibits DOPA decarboxylase

(active only peripherally) which allows lower effective doses of
L-dopa and allows for fewer SE's (GI distress, postural
hypotension, and dyskinesias)

Carbidopa

Clinical response that may fluctuate in tx of Parkinson's dx

"On-off-phenomenon"

Anti-Parkinson's drug which increases intraocular pressure

and is contraindicated in closed angle glaucoma

Levodopa

Ergot alkaloid that is a partial agonist at D2 receptors in the

brain, used for patients who are refractory or cannot tolerate
levodopa, causes erythromelalgia

Bromocriptine

Non ergot agents used as first-line therapy in the initial

management of Parkinson's

Pramipexole and ropinirole

Enhances dopaminergic neurotransmission SE's include CNS

excitation, acute toxic psychosis and livedo reticularis

Amantadine

Inhibitor of MAO type B which metabolizes dopamine, used

adjunct to levodopa or as sole agent in newly diagnosed pt's

Selegiline

Page 30

Inhibitors of catechol-O-methyltransferase (COMT), used as

adjuncts in Parkinson's dx and cause acute hepatic failure
(monitor LFT's)

Entacapone and Tolcapone

Agent decreases the excitatory actions of cholinergic neurons.

May improve tremor and rigidity but have LITTLE effect on
bradykinesia. Atropine-like side effects

Benztropine

Agent effective in physiologic and essential tremor

Propranolol

Agents used in Huntington's Disease

Tetrabenazine (amine
depleting drug), Haloperidol
(antipsychotic)

Agents used in Tourette's dx

Haloperidol or pimozide

Chelating agent used in Wilson's disease

Penicillamine

Antipsychotics
Extrapyramidal dysfunction is more common with these
agents, which block this subtype of dopamine receptor

Older antipsychotic agents,

D2 receptors

Side effects occuring in antipsychotics that block dopamine

EPS, hyperprolactinemia,
amennorrhea, galactorrhea,
neuroleptic malignant
syndrome

Antipsychotics that reduce positive symptoms only

Older antipsychotics

Newer atypical antipsychotics that also improve some of the

negative symptoms and help acute agitation

Olanzapine, aripiprazole, and

sertindole

Antipsychotic used in the treatment of psychiatric symptoms in

patients with dementia

Risperidone

Atypical antipsychotic causing high prolactin levels

Risperidone

Newer atypical antipsychotic used for bipolar disorder, known

to cause weight gain, and adversely affect diabetes
Agent more frequently associated with extrapyramidal side
effects that can be treated with benzodiazepine,
diphenhydramine or muscarinic blocker
Drug used in neuroleptic malignant syndrome

Olanzapine
Haloperidol

*
Page 31

Dantrolene

Agents may exacerbate tardive dyskinesias (may be

irreversible and there is no treatment)
Antipsychotics having the strongest autonomic effects

Muscarinic blockers

Chlorpromazine or
Thioridazine

Antipsychotic having the weakest autonomic effects

Haloperidol

Antipsychotic that does not block muscarinic or histamine

receptors, and it prolongs the QT interval

Sertindole

Only phenothiazine not exerting antiemetic effects, can cause

visual impairment due to retinal deposits, and high doses have
been associated with ventricular arrhythmias

Thioridazine

Agent with greater affinity to 5HT2A receptor; reserved for

refractory schizophrenia, and can cause weight gain and
agranulocytosis

Anti-psychotics shown not to cause tardive dyskinesia

Clozapine

Clozapine and quetiapine

Anti-psychotics available in depot preparation

Fluphenazine and
haloperidol

Reduced seizure threshold

Low-potency typical
antipsychotics and
clozapine

Orthostatic hypotension and QT prolongation

Low potency and

risperidone

Increased risk of developing cataracts

Quetiapine

Lithium
Major route of elimination for Lithium

Kidneys

Patients being treated with lithium, who are dehydrated, or

taking diuretics concurrently, could develop

Lithium toxicity

Drug increases the renal clearance hence decreases levels of

lithium

Page 32

Theophylline

Lithium is associated with this congenital defect

Cardiac anomalies and is

contraindicated in
pregnancy or lactation

DOC for bipolar affective disorder

SE of lithium

Lithium

Tremor, sedation, ataxia,

aphasia, thyroid
enlargement, and reversible
diabetes insipidus

Antidepressants
Example of three antidepressants that are indicated for
obsessive compulsive disorder
Neurotransmitters affected by the action of antidepressants

Clomipramine, fluoxetine
and fluvoxamine
Norepinephrine and
serotonin

Usual time needed for full effect of antidepressant therapy

2 to 3 weeks

Population group especially sensitive to side effects of

antidepressants

Elderly patients

All antidepressants have roughly the same efficacy in treating

depression, agents are chosen based on these criterion

Side-effect profile and prior

pt response

Well-tolerated and are first-line antidepressants

SSRI's, bupropion, and

venlafaxine

Monoamine oxidase inhibitors (MAOI)

Most useful in patients with significant anxiety, phobic
features, hypochondriasis, and resistant depression

Monamine oxidase inhibitors

Condition will result from in combination of MAOI with tyramine

containing foods (ex. wine, cheese, and pickled meats)

Hypertensive crisis

MAOI should not be administered with SSRI's or potent TCA's

due to development of this condition

Serotonin syndrome

Tricyclic antidepressants (TCA)

Page 33

Sedation is a common side effect of these drugs, they lower

seizure threshold, uses include BAD, acute panic attacks,
phobias, enuresis, and chronic pain and their overdose can be
deadly

Tricyclic antidepressants
(TCA)

Three C's associated with TCA toxicity

Coma, Convulsions, Cardiac

problems (arrhythmias and
wide QRS)

Agents having higher sedation and antimuscarinic effects than

other TCA's

Tertiary amines

TCA used in chronic pain, a hypnotic, and has marked

antimuscarinic effects

Amitriptyline

TCA used in chronic pain, enuresis, and OCD

Imipramine

TCA with greatest sedation of this group, and marked

antimuscarinic effects, used for sleep

Doxepin

TCA used in obsessive compulsive disorder (OCD), most

significant of TCA's for risk of seizure, weight gain, and
neuropsychiatric signs and symptoms

Clomipramine

Secondary amines that have less sedation and more

excitation effect

Nortriptyline, Desipramine

Heterocyclics
Antidepressant associated with neuroleptic malignant
syndrome

Amoxapine

Antidepressant associated with seizures and cardiotoxicity

Maprotiline

Antidepressant having stimulant effects similar to SSRI's and

can increase blood pressure

Venlafaxine

Antidepressant inhibiting norepinephrine, serotonin, and

dopamine reuptake

Venlafaxine

Antidepressant also used for sleep that causes priapism

Trazodone

Antidepressant which is inhibitor of CYP450 enzymes and may

be associated with hepatic failure

Nefazodone

Page 34

Unicyclic antidepressant least likely to affect sexual

performance, used for management of nicotine withdrawal,
SE's include dizziness, dry mouth, aggravation of psychosis,
and seizures

Bupropion

Antidepressant with MOA as alpha 2 antagonist, has effects

on both 5-HT and NE, blocks histamine receptors, and is
sedating

Mirtazapine

SE of mirtazapine

Liver toxicity, increased

serum cholesterol

Selective serotonin reuptake inhibitors (SSRI)

Except for these agents all SSRI have significant inhibition of
CytP450 enzymes

Citalopram and its

metabolite escitalopram

SSRI with long T1/2 and can be administered once weekly for
maintenance, not acute tx

Fluoxetine

SSRI indicated for premenstrual dysphoric disorder

Fluoxetine (Sarafem)

Some of SSRIs' therapeutic effects beside depression

Panic attacks, social

phobias, bulimia nervosa,
and PMDD premenstrual
dysphoric disorder), OCD
Fluoxetine

SSRI's less likely to cause a withdrawal syndrome

Opioid Analgesics & Antagonists

Inhibit synaptic activity of primary afferents and spinal cord
pain transmission neurons
Activation of these receptors close Ca2+ ion channels to
inhibit neurotransmitter release and pain transmission

Ascending pathways

Activation of these receptors open K+ ion channels to cause

membrane hyperpolarization
Tolerance to all effects of opioid agonists can develop except

All opioids except this agent (which has a muscarinic blocking

action) cause pupillary constriction

Page 35

Presynaptic mu, delta, and

kappa receptors
Postsynaptic Mu receptors

Miosis, convulsions and

constipation
Meperidine

SE of these drugs include dependence, withdrawal syndrome,

sedation, euphoria, respiratory depression nausea and
vomiting, constipation, biliary spasm, increased ureteral and
bladder tone, and reduction in uterine tone

Opioid Analgesics

Strong opioid agonists

Morphine, methadone,
meperidine, and fentanyl

Opioids used in anesthesia

Morphine and fentanyl

Opioid used in the management of withdrawal states

Methadone

Opioid available trans-dermally

Fentanyl

Opioid that can be given PO, by epidural, and IV, which helps
to relieve the dyspnea of pulmonary edema

Morphine

Use of this opioid with MAOI can lead to hyperpyrexic coma,

and with SSRI's can lead to serotonin syndrome
Moderate opioid agonists

Meperidine

Weak opioid agonist, poor analgesic, its overdose can cause

severe toxicity including respiratory depression, circulatory
collapse, pulmonary edema, and seizures

Codeine, hydrocodone, and

oxycodone
Propoxyphene

Partial agonist or mixed antagonists

Partial opioid agonist, considered a strong analgesic, has a
long duration of action and is resistant to naloxone reversal

Buprenorphine

Opioid antagonist that is given IV and had short DOA

Naloxone

Opioid antagonist that is given orally in alcohol dependency

programs

Naltrexone

These agents are used as antitussive

Dextromethorphan, Codeine

These agents are used as antidiarrheal

Diphenoxylate, Loperamide

Page 36

Drugs of Abuse
Inhalant anesthetics

NO, chloroform, and diethyl

ether

Toxic to the liver, kidney, lungs, bone marrow, peripheral

nerves, and cause brain damage in animals, sudden death
has occurred following inhalation

Fluorocarbons and Industrial

solvents

Cause dizziness, tachycardia, hypotension, and flushing

Organic nitrites

Causes acne, premature closure of epiphyses, masculinization

in females, hepatic dysfunction, MI, and increases in libido and
aggression

Steroids

Readily detected markers that may assist in diagnosis of the

cause of a drug overdose include

Changes in heart rate, blood

pressure, respiration, body
temperature, sweating,
bowel signs, and pupillary
responses

Opioid Analgesics
Most commonly abused in health care professionals

Heroin, morphine,
oxycodone, meperidine and
fentanyl

This route is associated with rapid tolerance and psychologic

dependence

IV administration

Leads to respiratory depression progressing to coma and

death

Overdose of opioids

Lacrimation, rhinorrhea, yawning, sweating, weakness,

gooseflesh, nausea, and vomiting, tremor, muscle jerks, and
hyperpnea are signs of this syndrome

Abstinence syndrome

Treatment for opioid addiction

Methadone, followed by
slow dose reduction

This agent may cause more severe, rapid and intense

symptoms (abstinence syndrome) to a recovering addict
Sedative-Hypnotics

Page 37

Naloxone

Sedative-Hypnotics action

Reduce inhibition, suppress

anxiety, and produce
relaxation

Additive effects when Sedative-Hypnotics used in combination

with these agents

CNS depressants

Common mechanism by which overdose result in death

Depression of medullary and

cardiovascular centers

"Date rape drug"

Flunitrazepam (rohypnol)

The most important sign of withdrawal syndrome

Excessive CNS stimulation

(seizures)

Treatment of withdrawal syndrome involves

Long-acting sedativehypnotic or a gradual

reduction of dose, clonidine
or propranolol

These agents are CNS depressants

Ethanol, Barbiturates, and

Benzodiazepines

Stimulants
Withdrawal from this drug causes lethargy, irritability, and
headache

Caffeine

W/D from this drug causes anxiety and mental discomfort

Nicotine

Treatments available for nicotine addiction

Patches, gum, nasal spray,

psychotherapy, and
bupropion

Chronic high dose abuse of nicotine leads to

Psychotic state, overdose

causes agitation,
restlessness, tachycardia,
hyperthermia, hyperreflexia,
and seizures

Tolerance is marked and abstinence syndrome occurs

Amphetamines

Amphetamine agents

Dextroamphetamines and
methamphetamine

Page 38

These agents are congeners of Amphetamine

DOM, STP, MDA, and MDMA

"ecstasy"

Overdoses of this agent with powerful vasoconstrictive action

may result in fatalities from arrhythmias, seizures, respiratory
depression, or severe HTN (MI and stroke)

Cocaine "super-speed"

Hallucinogens
Most dangerous of the currently popular hallucinogenic drugs,
OD leads to nystagmus, marked hypertension, and seizures,
presence of both horizontal and vertical nystagmus is
pathognomonic

PCP

Removal of PCP may be aided

Urinary acidification and

activated charcoal or
continual nasogastric
suction

THC is active ingredient, SE's include impairment of judgment,

and reflexes, decreases in blood pressure and psychomotor
performance occur

Marijuana

Cholinoreceptor-Activating & Cholinesterase-Inhibiting

Drugs
Direct-Acting Cholinomimetic Agonists
Muscarinic agonists or parasympathomimetic

This agent has greater affinity for muscarinic receptors and

used for postoperative and neurogenic ileus and urinary
retention

Bethanechol

Only direct acting agent that is very lipid soluble and used in
glaucoma

Pilocarpine

These agents are used to treat dry mouth in Sjgren's

syndrome

Pilocarpine or Cevimeline

Indirect-Acting ACh Agonist, alcohol, short DOA and used in

diagnosis of myasthenia gravis

Edrophonium

Carbamate with intermediate action postoperative and

neurogenic ileus and urinary retention

Neostigmine

Page 39

Treatment of atropine overdose and glaucoma (because lipid

soluable). Enters the CNS rapidly and has a stimulant effect,
which may lead to convulsions

Physostigmine

Treatment of myasthenia gravis

Pyridostigmine

Organophosphates
Antiglaucoma organophosphate

Echothiophate

Associated with an increased incidence of cataracts in patients

treated for glaucoma

Long acting cholinesterase

inhibitors

Scabicide organophosphate

Malathion

Organophosphate anthelmintic agent with long DOA

Metrifonate

Toxicity of cholinergics

DUMBELSS (diarrhea,
urination, miosis,
bronchoconstriction,
excitation of skeletal muscle
and CNS, lacrimation,
salivation, and sweating)

The most important cause of acute deaths in cholinesterase

inhibitor toxicity

Respiratory failure

The most toxic organophosphate

Parathion

Treatment of muscarinic symptoms in organophosphate

overdose

Atropine

This agent regenerates active cholinesterase and is a

chemical antagonist used to treat organophosphate exposure

Pralidoxime

Cholinoreceptor Blockers & Cholinesterase Regenerators

Prototypical drug is atropine

Nonselective Muscarinic
Antagonists

Treat manifestations of Parkinson's disease and EPS

Page 40

Benztropine, trihexyphenidyl

Treatment of motion sickness

Scopolamine

Produce mydriasis and cycloplegia

Atropine, homatropine, and

tropicamide

Bronchodilation in asthma and COPD

Ipratropium

Reduce transient hyper GI motility

Dicyclomine,
methscopolamine

Cystitis, postoperative bladder spasms, or incontinence

Oxybutynin, dicyclomine

Toxicity of anticholinergics

Anti-DUMBBELSS

Another pneumonic for anticholinergic toxicity

"dry as a bone, red as a beet,

mad as a hatter, hot as a
hare, blind as a bat"

Atropine fever is the most dangerous effect and can be lethal

in this population group

Infants

Contraindications to use of atropine

Infants, closed angle

glaucoma, prostatic
hypertrophy

Nicotinic Antagonists
Prototype ganglion blocker

Hexamethonium

Limiting adverse effect of ganglion blockade that patients

usually are unable to tolerate

Severe hypertension

Reversal of blockade by neuromuscular blockers

Cholinesterase inhibitors

Tubocurarine is the prototype, pancuronium, atracurium,

vecuronium are newer short acting agent, produce competitive
block at end plate nicotinic receptor, causing flaccid paralysis

Nondepolarizing
Neuromuscular Blockers

Only member of depolarizing neuromuscular blocker, causes

fasciculation during induction and muscle pain after use

Succinylcholine

Page 41

Chemical antagonists that bind to the inhibitor of ACh Estrace

and displace the enzyme (if aging has not occurred)

Cholinesterase Regenerators

Used to treat patients exposed to insecticides such as

parathion

Pralidoxime

Sympathomimetics
Pneumonic for beta receptors

You have 1 heart (Beta 1)

and 2 lungs (Beta 2)

This is the drug of choice for anaphylactic shock

Epinephrine

Phenylisopropylamines that are used legitimately and abused

for narcolepsy, attention deficit disorder, and weight reduction

Amphetamines

Alpha agonist used to produce mydriasis and reduce

conjunctival itching and congestion caused by irritation or
allergy, it does not cause cycloplegia

Phenylephrine

Epinephrine and dipivefrin are used for

Glaucoma

Newer alpha 2 agonist (apraclonidine and brimonidine) treat

glaucoma

Reduce aqueous synthesis

Short acting Beta 2 agonists that is drug of choice in treatment

of acute asthma but not recommended for prophylaxis

Albuterol

Longer acting Beta 2 agonists is recommended for prophylaxis

of asthma

Salmeterol

These agents increase blood flow and may be beneficial in

treatment of acute heart failure and some types of shock

Beta1 agonists

These agents decrease blood flow or increase blood pressure,

are local decongestant, and used in therapy of spinal shock
(temporary maintenance of blood pressure which may help
maintain perfusion)

Alpha1 agonists

Shock due to septicemia or myocardial infarction is made

worse by

Page 42

Increasing afterload and

tissue perfusion declines

Often mixed with local anesthetic to

Reduce the loss from area of

injection

Chronic orthostatic hypotension can be treated with

Midodrine

Beta 2 agonist used to suppress premature labor, but cardiac

stimulatory effects may be hazardous to mother and fetus

Terbutaline

Long acting sympathomimetic, sometimes used to improve

urinary continence in children and elderly with enuresis

Ephedrine

Alpha 1 agonist toxicity

Hypertension

Beta 1 agonist toxicity

Sinus tachycardia and

serious arrhythmias

Beta 2 agonist toxicity

Skeletal muscle tremor

The selective agents loose their selectivity at

high doses

Adrenoceptor Blocker
Nonselective alpha-blocking drug, long acting and irreversible,
and used to treat pheochromocytoma. Blocks 5-HT, so
occasionaly used for carcinoid tumor. Blocks H1 and used in
mastocytosis

Phenoxybenzamine

Nonselective alpha-blocking drug, short acting and reversible,

used for rebound HTN from rapid clonidine withdrawal, and
Raynaud's phenomena

Phentolamine

Selective Alpha 1 blocker used for hypertension, BPH, may

cause first dose orthostatic hypotension

Selective Alpha 2 blocker used for impotence (controversial

effectiveness)

Prazosin, terazosin,
doxazosin
Yohimbine

Beta-Blocking Drugs
Selective B1 Receptor blockers that may be useful in treating
cardiac conditions in patients with asthma

Page 43

Acebutolol, atenolol,
esmolol, metoprolol

Combined alpha and beta blocking agents that may have

application in treatment of CHF

Labetalol and carvedilol

Beta blockers partial agonist activity (intrinsic

sympathomimetic activity) cause some bronchodilation and
may have an advantage in treating patients with asthma

Pindolol and acebutolol

This beta blocker lacks local anesthetic activity (decreases

protective reflexes and increases the risk of corneal
ulceration) and used in treating glaucoma

Timolol

This parenteral beta blocker is a short acting

Esmolol

This beta blocker is the longest acting

Nadolol

These beta blockers are less lipid soluble

Acebutolol and atenolol

This beta blocker is highly lipid soluble and may account for
side effects such as nightmares

Propranolol

Clinical uses of these agents include treatment of HTN,

angina, arrhythmias, and chronic CHF

Beta blockers

Toxicity of these agents include bradycardia, AV blockade,

exacerbation of acute CHF, signs of hypoglycemia may be
masked (tachycardia, tremor, and anxiety)

Beta blockers

Glaucoma (all agents topical except for diuretics)

Cholinomimetics that increase outflow, open trabecular
meshwork, and cause ciliary muscle contraction

Pilocarpine, carbachol,
physostigmine

Nonselective alpha agonists that increases outflow, probably

via the uveoscleral veins

Epinephrine, dipivefrin

Selective alpha agonists that decreases aqueous secretion

Apraclonidine, brimonidine

These Beta blockers decrease aqueous secretion

This diuretic decreases aqueous secretion due to lack of

HCO3- ion. Causes drowsiness and paresthesias,
alkalinization of the urine may precipitate calcium salts,
hypokalemia, acidosis

Page 44

Timolol (nonselective),
betaxolol (selective)
Acetazolamide

This agent cause increased aqueous outflow

Prostaglandin PGF2a

Antihypertensive Agents
Inhibit angiotensin-converting enzyme (ACE)

Ace inhibitors

Captopril and enalapril (-OPRIL ending) are

Ace inhibitors

SE of ACE inhibitors

Dry cough, hyperkalemia

Ace inhibitors are contraindicated in

pregnancy and with K+

Losartan and valsartan block

Angiotensin receptor

Angiotensin receptor blockers do NOT cause

Dry cough

Block L-type calcium channel

Calcium channel blockers

CCB contraindicated in CHF

CCB with predominate effect on arteriole dilation

Verapamil

Nifedipine

SE of CCB

Constipation, edema, and

headache

Reduce heart rate, contractility, and O2 demand

Beta-blockers

B-blockers that are more cardioselective

Beta C2001-selective
blockers

Cardioselective Beta 1-blockers

Beta-blockers should be used cautiously in

Atenolol, acebutolol, and

metoprolol
Asthma (bronchospastic
effects), diabetes (block
signs of hypoglycemia) and
peripheral vascular disease

Page 45

Non-selective Beta-blocker also used for migraine prophylaxis

Propranolol

SE of beta blockers

Bradycardia, SEXUAL
DYSFUNCTION, decrease in
HDL, and increase in
Triglycerols (TG)

Alpha 1selective blockers

Prazosin, terazosin and

doxazosin (-AZOSIN ending)

Non-selective Alpha1blockers use to treat pheochromocytoma

Phenoxybenzamine

For rebound HTN from rapid clonidine withdrawal

Phentolamine

A1a-selective blocker used for BPH

Tamsulosin (Flomax)

Orthostatic hypotension
(especially with first dose)
and reflex tachycardia

SE of alpha blockers

Presynaptic Alpha 2 agonist used in HTN

Clonidine, and methyldopa

SE of methyldopa

Positive Comb's test,

depression

Methyldopa is contraindicated in

Geriatrics due to its CNS

(depression) effects

SE of clonidine

Rebound HTN, sedation, dry

mouth

Ganglionic blockers formerly used in HTN

Trimethaphan, and
hexamethonium

Direct vasodilator of arteriolar smooth muscle

Hydralazine

SE of hydralazine

Arterial vasodilator that works by opening K+ channels

Page 46

Lupus-like syndrome

Minoxidil

SE of minoxidil

Hypertrichosis

IV Drug used Hypertensive Crisis

Nitroprusside

Nitroprusside vasodilates

Arteries and veins

Toxicity caused by nitroprusside and treatment

Cyanide toxicity treated with

sodium thiosulfate

Diuretics
Carbonic anhydrase inhibitor

Acetazolamide

Diuretic used for mountain sickness and glaucoma

SE of acetazolamide

MOA of loop diuretics

Acetazolamide

Paresthesias, alkalization of
the urine (which may ppt. Ca
salts), hypokalemia,
acidosis, and
encephalopathy in patients
with hepatic impairment

inhibits Na+/K+/2Clcotransport

Site of action of loop diuretics

Thick ascending limb

Hyperuricemia, hypokalemia
and ototoxicity

SE of loop (furosemide) diuretics

Aminoglycosides used with loop diuretics potentiate adverse

effect
Loops lose and thiazide diuretics retain

Ototoxicity

MOA of thiazide diuretics

Calcium

Inhibit Na+/Cl- cotransport

Site of action of thiazide diuretics

Page 47

Work at early distal

convoluted tubule

Class of drugs that may cause cross-sensitivity with thiazide

diuretics

Sulfonamides

SE of thiazide (HCTZ) diuretics

Hyperuricemia, hypokalemia
and hyperglycemia

Potassium sparing diuretics inhibit

Na+/K+ exchange

Diuretic used to treat primary aldosteronism

Spironolactone

Gynecomastia hyperkalemia,
and impotence

Mannitol

Desmopressin (DDAVP)

SE of spironolactone

Osmotic diuretic used for increased intracranial pressure

Antidiuretic hormone (ADH) agonist and antagonist

ADH agonist used for pituitary diabetes insipidus

Used for SIADH

Demeclocycline

SE of demeclocycline

Bone marrow and teeth

discoloration for children
under 8 years of age

Antiarrhythmic agents
MOA of class I A (eg. Procainamide), class IB (eg. Lidocaine),
and class IC (eg. Flecainide) antiarrhythmics

Sodium channel blockers

SE of procainamide

Lupus-like syndrome

Limiting side effect of Quinidine

Prolongs QT interval

Other side effects of Quinidine

Thrombocytopenic purpura,
and CINCHONISM

Major drug interaction with Quinidine

Increases concentration of
Digoxin

DOC for management of acute Ventricular arrhythmias

DOC for digoxin induced arrhythmias

Lidocaine

Phenytoin

Page 48

SE of phenytoin

Gingival hyperplasia

Class of anti-arrhythmics that has a pro-arrhythmic effect

(CAST trial), therefore are used as last line agents

Class IC (flecainide,
propafenone, moricizine)

Class II antiarrhythmics are

B-blockers

Antiarrhythmic that exhibits Class II and III properties

Sotalol

Side effect of sotalol

prolongs QT and PR interval

Used intravenously for acute arrhythmias during surgery

Esmolol

Anti-arrhythmics that decrease mortality

B-blockers

MOA of class III antiarrhythmics

Potassium channel blockers

Class III antiarrhythmic that exhibits properties of all 4 classes

Amiodarone

Specific pharmacokinetic characteristic of amiodarone

Prolonged half-life, up to six

weeks

Antiarrhythmic effective in most types of arrhythmia

Amiodarone

SE of Amiodarone

Dysfunction,
photosensitivity, skin (blue
smurf syndrome), Pulmonary
fibrosis, thyroid and corneal
deposits

MOA of class IV antiarrhythmics

Calcium channel blockers

Life threatening cardiac event that prolong QT leads to

Agent to treat torsades de pointes

Torsades de pointes

Magnesium sulfate

Page 49

Drug used supraventricular arrhythmias

Digoxin

DOC for paroxysmal supraventricular tachycardia (PSVT)

Adenosine

Adenosine's MOA

Activates acetylcholine
sensitive K+ channels in SA
and AV node

Anti-arrhythmic with 15 second duration of action

Adenosine

Vasodilators and treatment of angina

MOA of sildenafil (Viagra)

Inhibits phosphodiesterase5, enhancing effects of nitric

oxide-activated increases in
cGMP

Drugs used in the management of angina

Aspirin, Nitrates, CCB, and

Beta blockers

Aspirin reduces mortality in unstable angina by

Platelet aggregation
inhibition

MOA of nitrates

Relax vascular smooth

muscle, at low doses dilate
veins and at high doses
dilate arterioles

Nitrate used for acute anginal attacks

Nitroglycerin sublingual
tablets

Nitrate used to prevent further attacks

Oral and transdermal forms

of nitroglycerin

Nitrate free intervals are needed due to

Tolerance

SE of nitrates

Postural hypotension, reflex

tachycardia, hot flashes, and
throbbing headache due to
meningeal artery dilation

CCB are DOC for

Prinzmetal's angina

Beta blockers are used for which type of anginal attack

Classic

Page 50

Drugs used to treat CHF

MOA of Cardiac glycosides (eg. digoxin)

Indirectly increase
intracellular calcium and
cardiac contractility by
inhibit Na+/K+ ATPase

Digoxin is used in

Atrial fibrillation and CHF

Digoxin toxicity can be precipitated by

Hypokalemia

Antidote for digoxin toxicity

Digibind

Phosphodiesterase inhibitors that increase mortality and have

been found to have NO beneficial effects

Amrinone and milrinone

SE of amrinone

Thrombocytopenia

Beta 1 agonists used in acute CHF

Dobutamine and dopamine

Diuretics work in CHF by

Reducing preload

Beta blockers work in CHF by

Reducing progression of
heart failure (never use in
acute heart failure)

Agent used in CHF that is a selective alpha and nonselective

beta blocker

Carvedilol

Agent used in acutely decompensated CHF resembling

natriuretic peptide

Nesiritide (Natrecor)

Drugs used in coagulation disorders

Vitamin K dependent anticoagulant

Warfarin (PT)

Warfarin is contraindicated in

Pregnancy

Anticoagulant of choice in pregnancy

Heparin

Heparin (PTT) increases activity of

*
Page 51

Antithrombin 3

Route of administration of warfarin

Oral

Routes of administration of heparin

IM (only LMW) and IV

SE of both warfarin and heparin

Bleeding

SE of heparin

Heparin induced
thrombocytopenia (HIT)

Alternative anticoagulant used if HIT develops

Lepirudin

Antidote to reverse actions of warfarin

Vitamin K or fresh frozen

plasma

Antidote to reverse actions of heparin

Protamine sulfate

MOA of aspirin

Irreversibly blocking
cyclooxygenase

Agent used to treat MI and to reduce incidence of subsequent

MI

Aspirin

SE of Aspirin

GI bleeding

Antiplatelet drug reserved for patients allergic to aspirin

Ticlopidine

SE for ticlopidine

Neutropenia and
agranulocytosis

Effective in preventing TIA's

Clopidogrel and ticlopidine

Prevents thrombosis in patients with artificial heart valve

Dipyridamole

Block glycoprotein IIb/IIIa involved in platelet cross-linking

Abciximab, tirofiban and

eptifibatide

MOA of thrombolytics

Lyse thrombi by catalyzing

the formation of plasmin
which binds fibrin

Page 52

Thrombolytics are used for

Pulmonary embolism and

DVT

Thrombolytic that can cause allergic reaction

Streptokinase

Thrombolytic used for acute MI and ischemic (non

hemorrhagic) CVA

Tissue plasmin activator

SE of tPA

Cerebral hemorrhage

Antidote for thrombolytics

Aminocaproic acid

Agents used in anemias and hematopoietic growth

factors
Agent to treat hypochromic microcytic anemias

Ferrous sulfate

Chelating agent used in acute iron toxicity

Deferoxamine

Agent for pernicious anemia

Cyanocobalamin (Vit B12)

Agent used for neurological deficits in megaloblastic anemia

Vitamin B12

Agent used for megaloblastic anemia (but does NOT reverse

neurologic symptoms) and decrease neural tube defects
during pregnancy

Folic acid

Agent used for anemias associated with renal failure

Erythropoietin

Agent used neutropenia especially after chemotherapy

G-CSF (filgrastim) and GMCSF (sargramostim)

Treatment of patients with prior episodes of thrombocytopenia

after a cycle of cancer chemotherapy

Interleukin 11 (oprelvekin)

Antihyperlipidemics
Decrease intestinal absorption of cholesterol

Bile acid-binding resins

Cholestyramine and colestipol are

Bile acid-binding resins

Page 53

Major nutritional side effect of bile acid-binding resins

Impair absorption of fat

soluble vitamin absorption
(A,D,E,K)
inhibits HMG COA reductase

MOA of lovastatin (STATIN)

HMG CoA reductase inhibitors are contraindicated in

Drug or foods (grapefruit juice) that increase statin effect

Pregnancy

SE of HMG COA reductase inhibitors

Inhibit Cytochrome P450 3A4

Rhabdomyolysis and
Hepatotoxicity

Monitoring parameter to obtain before initiation of STATINS

LFT's

Decreases liver triglycerol synthesis

Niacin

SE of niacin

Cutaneous flush

Cutaneous flush and be reduced by pretreatment with

Fibrates (gemfibrozil) increase activity of

Aspirin

Lipoprotein lipase

Most common SE of fibrates

Nausea

Fibrates are contraindicated in

Pregnancy

Concurrent use of fibrates and statins increases risk of

Rhabdomyolysis

New class of drugs that works by inhibiting absorption of

intestinal cholesterol and can be given concurrently with the
Statins

Ezetimibe (Zetia)

NSAIDS and DMARDS

MOA of NSAIDS

inhibit prostaglandin
synthesis by inhibiting cyclooxygenase (cox)

Page 54

Difference between aspirin and other NSAIDS

Aspirin irreversibly inhibits

cyclooxygenase

Four main actions of NSAIDS

Anti-inflammatory,
analgesia, antipyretic and
antiplatelet activity

Agent used for closure of patent ductus arteriosus

Indomethacin

Aspirin is contraindicated in children with viral infection

Potential for development of

Reye's syndrome

SE of salicylates

Tinnitus, GI bleeding

NSAID also available as an ophthalmic preparation

Diclofenac

NSAID available orally, IM and ophthalmically

Ketoralac

NSAID that is used for acute condition, such as pre-op

anesthesia and has limited duration (<5 days) of use due to
nephrotoxicity

Ketoralac

Newer NSAIDs that selectively inhibit COX-2

Celecoxib and rofecoxib

COX 2 inhibitors may have reduced risk of

Gastric ulcers and GI

Bleeding

COX 2 inhibitors should be used cautiously in pts with

Pre-existing cardiac or renal

disease

Acetaminophen only has

SE of acetaminophen

Antipyretic and analgesic

activity
Hepatotoxicity

Antidote for acetaminophen toxicity

N-acetylcysteine

Rheumatic disease

Drugs-Modifying Anti-Rheumatic Agents (DMARDS)

DMARDs are slow acting drugs for

Page 55

MOA of gold salts

Alter activity of
macrophages and suppress
phagocytic activity of PMNs

SE of gold salts

Dermatitis of the mouth

aplastic anemia and
agranulocytosis

Causes bone marrow suppression

Methotrexate

SE of penicillamine

Aplastic anemia and renal

Interferes with activity of T-lymphocytes

Hydroxychloroquine

Anti-malarial drug used in rheumatoid arthritis (RA)

Hydroxychloroquine

SE of hydroxychloroquine

Retinal destruction and

dermatitis

MOA of Leflunomide (newer agent)

Inhibiting Dihydroorotate
Dehydrogenase which leads
to decreased pyrimidine
synthesis

Proteins that prevent action of tumor necrosis factor alpha

(TNF-alpha)

Infliximab and etanercept

Anti-rheumatic agent also used for ulcerative colitis

Sulfasalazine

Drugs used in Gout

NSAID used in gout

Indomethacin

NSAID contraindicated in gout

Aspirin

SE of phenylbutazone

Aplastic anemia and

agranulocytosis

MOA of Colchicine (used in acute gout)

Selective inhibitor of
microtubule assembly

Page 56

SE of colchicine

Kidney and liver toxicity

Agent used to treat chronic gout by increasing uric acid

secretion

Probenecid

Allopurinol treats chronic gout by inhibiting

Page 57

Xanthine oxidase