02-02-12 pharm one liners

8/10/2019 02-02-12 Pharm One Liners

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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-qualifiedstudent (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.


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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 *Phase I

Different steps of Phase I Oxidation, reduction,

hydrolysis

Inducers of Cytochrome P450(CYP450)

*Barbiturates, phenytoin,

carbamazepine, and rifampin

Inhibitors of CYP450

*Cimetidine, ketoconazole,

erythromycin, isoniazid and

ra efruit

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

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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

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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 **Atropine, pralidoxime (2-

PAM)

Antidote used for iron salt toxicity Deferoxamine

Antidote used for acetaminophen (APAP) toxicity * N-acetylcysteine

Antidote for severe lead poisoning Dimercaprol + CaEDTA

(edetate calcium disodium)

Antidote for arsenic, mercury, and goldpoisoning 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*

Naloxone (IV), naltrexone

(PO)

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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)

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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, andrednisone

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

rednisone

Regimen used for breast cancer CMF (cyclophosphamide,methotrexate, and

fluorouracil) and tamoxifen if

ER+

Alkylating agent, vesicant that causes tissue damage with

extravasation

Mechlorethamine

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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 causesperipheral 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 greatermyelosuppression

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 forprostate 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, 6-

MP, methotrexate,

eto oside

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 *Odansetron, granisetron,

dolasetron, palonosetron

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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) analogused for acromegaly, carcinoid,

glucagonoma and other GH producing pituitary tumors

Octreotide

Somatotropin (GH) analogused in GH deficiency (dwarfism) Somatrem

GHRHanalogused as diagnostic agent Sermorelin

GnRHagonistused 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 analogused for diagnosis of patients with corticosteroid

abnormality **Cosyntropin

Synthetic analog of ADH hormone used for diabetes insipidus

and nocturnal enuresis *Desmopressin (DDAVP)

Thyroid and anti-thyroid drugs

Most widely used thyroid drugs such as Synthroid and Levoxyl

contain **L-thyroxine (T4)

T3 compound less widely used Cytomel

Anti-thyroid drugs Thioamides, iodides,

radioactive iodine, and

i odate

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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 th ro lobulin

Can be effective for short term therapyof 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 productsGlomerulosa(mineralocorticoids),

fasciculata

(glucocorticoid=GC), and

reticularis (adrenal

andro ens

Pneumonic for 3 zones of adrenal cortex GFR

Used forAddison'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

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Intermediate acting GC's Prednisone,

methylprednisolone,

prednisolone, and

triamcinolone

Long acting GC's Betamethasone,

dexamethasone, and

aramethasone

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

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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 inhibitorused 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

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Delta cells in the pancreas Produce Somatostatin

Product ofproinsulin 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

cram s

Alpha-glucosidase inhibitor associated with elevation of LFT's Acarbose

Amino acid derivative for treatment of Type II diabetes * Nateglinide

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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 homeostasisAvailable 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 cannotbe 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.

**Raloxifene (SERM-selective

estrogen receptor

modulator)

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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 * Oxytocin

Distribution of histamine receptors H1, H2, and H3

*

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)

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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

5HT-3 antagonist used in chemotherapeutic induced

emesis ***Ondansetron, granisetron,

dolasetron and

alonosetron

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

and QTc prolongation and should not be used in patients with

heartdisease

Dolasetron

DOC of chemo induced nausea and vomiting ** 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 Bradykinin and histamine

Mediator of tissue pain, edema, inactivated by ACE, and may

be a contributing factor to the development of angioedema *Bradykinin

Drug causing depletion of substance P (vasodilator) * Capsaicin

Prostaglandins that cause abortions

*Prostaglandin E1

(misoprostol) PGE2, and

PGF2al ha

Difference between COX 1 and COX 2

COX 1 is found throughout

the body and COX 2 is only

in inflammatory tissue

Drug that selectively inhibits COX 2 Celecoxib, valdecoxib, and

rofecoxib

Inhibitor of lipoxygenase * Zileuton

Major SE of zileuton Liver toxicity

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Inhibitor of leukotrienes (LTD4) receptors and used in asthma Zafirlukast and montelukast

Used in pediatrics to maintain patency of ductus arteriosis * PGE1 (Alprostadil)

Approved for use in severe pulmonary HTN 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

*Stimulates cGMP which

leads to vascular smooth

muscle relaxation

Long acting beta 2 agonist used in asthma 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

Pentoxifylline

Antidote for severe CV toxicity of theophylline Beta blockers

MOA of corticosteroids

inhibit phospholipase A2

SE of long term (>5 days) corticosteroid therapy and remedy

*Adrenal suppression and

weaning slowly, respectively

Antimicrobials

MOA of quinolones ** Inhibit DNA gyrase

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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*

Inhibit dihydropteroate

synthase

Penicillins active against penicillinase secreting bacteria Methicillin, nafcillin, and

dicloxacillin

Cheap wide spectrum antibiotic DOC of otitis media ** 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

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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 ofpseudomembranous colitis ** Metronidazole

Treatment of resistant pseudomembranous colitis ORAL vancomycin

Anemia caused by trimethoprim * Megaloblastic anemia

Reason fluoroquinolones are contraindicated in children and

pregnancy

Cartilage damage

DOC for giardia, bacterial vaginosis, pseudomembranous

colitis, and trichomonas *Metronidazole

Treatment for TB patients (thinkRIPE)

*R ifampin, Isoniazid,

Pyrazinamide, and

E thambutol

Metronidazole SE if given with alcohol 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)

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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, andribavirin

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

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Oral antibiotic of choice for moderate inflammatory acne Minocycline

Drug of choice for leprosy Dapsone

DOC for herpes and its MOA * Acyclovir; activatesthymidine 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 * REM is decreased

Neurologic SE of benzodiazepines Anterograde amnesia

Reason benzos are used cautiously in pregnancy*

Ability to cross the placenta

Main route of metabolism for benzodiazepines Hepatic

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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 ionchannel 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

cloraze ateBarbiturates

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

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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

benzodiaze ines

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

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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 *Valproic acid, Phenytoin and

Carbamazepine

DOC for febrile seizures 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 aba entin

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Anti-seizure drugs used also for Trigeminal neuralgia Carbamazepine

Anti-seizure drugs used also for pain of neuropathic orgin * Gabapentin

Anti-seizure agent that exhibits non-linear metabolism, highlyprotein 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 drug-

metabolism 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

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Inversely related to potency of anesthetics Minimum alveolar anesthetic

concentration (MAC)

Inhaled anesthetics metabolized by liver enzymes which has amajor role in the toxicity of these agents

Halothane andmethoxyflurane

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 toarrhythmogenic effects of catecholamines and has produced

h epatitis

Halothane

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 tomegaloblastic 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 *Flumazenil

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This produces "dissociative anesthesia ", is a cardiovascular

stimulant which may increases intracranial pressure, and

hallucinations occur during recovery

Ketamine

Opioid associated with awareness during surgery and post-

operative recall, but still used for high-risk cardiovascular

surgeries *

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

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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

antiarrh thmic

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 drugsAgents 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

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GABA agonist in the spinal cord Baclofen

Similar to clonidine and may cause hypotension Tizanidine

DOC for malignant hyperthermia by acting on thesacroplasmic reticulum or skeletal muscle * Dantrolene

Agent used for acute muscle spasm Cyclobenzaprine

Drugs Used in Parkinsonism & Other Movement

DisordersAntipsychotics, reserpine at high doses, and MPTP (by-

product 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 theBBB

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 pressureand 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

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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

anti s chotic

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

s ndrome

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

Olanzapine

Agent more frequently associated with extrapyramidal side

effects that can be treated with benzodiazepine,

diphenhydramine or muscarinic blocker

Haloperidol

Drug used in neuroleptic malignant syndrome * Dantrolene

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Agents may exacerbate tardive dyskinesias (may be

irreversible and there is no treatment)

Muscarinic blockers

Antipsychotics having the strongest autonomic effects*

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 andagranulocytosis

*

Clozapine

Anti-psychotics shown not to cause tardive dyskinesia * Clozapine and quetiapine

Anti-psychotics available in depot preparation Fluphenazine and

haloperidol

Reduced seizure threshold Low-potency typical

antipsychotics and

cloza ine

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, ortaking diuretics concurrently, could develop *

Lithium toxicity

Drug increases the renal clearance hence decreases levels of

lithium

Theophylline

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Lithium is associated with this congenital defect Cardiac anomalies and is

contraindicated in

re nanc or lactation

DOC for bipolar affective disorder * Lithium

SE of lithium

*

Tremor, sedation, ataxia,

aphasia, thyroid

enlargement, and reversible

diabetes insipidus

Antidepressants

Example of three antidepressants that are indicated for

obsessive compulsive disorder

Clomipramine, fluoxetine

and fluvoxamineNeurotransmitters affected by the action of antidepressants 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)

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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, anddopamine reuptake

Venlafaxine

Antidepressant also used for sleep that causespriapism Trazodone

Antidepressant which is inhibitor of CYP450 enzymes and may

be associated with hepatic failure

Nefazodone

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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

d s horic disorder OCDSSRI's less likely to cause a withdrawal syndrome Fluoxetine

Opioid Analgesics & Antagonists

Inhibit synaptic activity of primary afferents and spinal cord

pain transmission neurons

Ascending pathways

Activation of these receptors close Ca2+ ion channels to

inhibit neurotransmitter release and pain transmission *Presynaptic mu, delta, and

kappa receptors

Activation of these receptors open K+ ion channels to cause

membrane hyperpolarization

Postsynaptic Mu receptors

Tolerance to all effects of opioid agonists can develop except*

Miosis, convulsions and

constipation

All opioids except this agent (which has a muscarinic blocking

action) cause pupillary constriction

Meperidine

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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 helpsto 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

Meperidine

Moderate opioid agonists*

Codeine, hydrocodone, and

oxycodone

Weak opioid agonist, poor analgesic, its overdose can cause

severe toxicity including respiratory depression, circulatory

collapse, pulmonary edema, and seizures

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

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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

fentan l

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 *Naloxone

Sedative-Hypnotics

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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 sedative-hypnotic or a gradual

reduction of dose, clonidine

or ro ranolol

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

bu ro ion

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

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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, respiratorydepression, 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 nasogastricsuction

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

DrugsDirect-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 indiagnosis of myasthenia gravis

Edrophonium

Carbamate with intermediate action postoperative and

neurogenic ileus and urinary retention

Neostigmine

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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*

Benztropine, trihexyphenidyl

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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

h ertro h

Nicotinic AntagonistsPrototype 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

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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 treatmentof 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

Increasing afterload and

tissue perfusion declines

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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 cardiacstimulatory 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 inmastocytosis

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 *Prazosin, terazosin,

doxazosin

Selective Alpha 2 blocker used for impotence (controversial

effectiveness)

Yohimbine

Beta-Blocking Drugs

Selective B1 Receptor blockers that may be useful in treating

cardiac conditions in patients with asthma *Acebutolol, atenolol,

esmolol, metoprolol

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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*

Timolol (nonselective),

betaxolol (selective)

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

Acetazolamide

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This agent cause increased aqueous outflow Prostaglandin PGF2a

Antihypertensive AgentsInhibit 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 * Verapamil

CCB with predominate effect on arteriole dilation 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

*

Atenolol, acebutolol, and

meto rolol

Beta-blockers should be used cautiously in Asthma (bronchospastic

effects), diabetes (block

signs of hypoglycemia) and

peripheral vascular disease

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Non-selective Beta-blocker also used for migraine prophylaxis Propranolol

SE of beta blockers

*

Bradycardia, SEXUAL

DYSFUNCTION, decrease in

HDL, and increase in

Tri l cerols 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)

SE of alpha blockers

*Orthostatic hypotension

(especially with first dose)

and reflex tach cardia

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 * Lupus-like syndrome

Arterial vasodilator that works by opening K+ channels Minoxidil

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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 * Acetazolamide

SE of acetazolamide

*

Paresthesias, alkalization of

the urine (which may ppt. Ca

salts), hypokalemia,

acidosis, and

encephalopathy in patients

with hepatic impairment

MOA of loop diuretics inhibits Na+/K+/2Cl-

cotrans ort

Site of action of loop diuretics * Thick ascending limb

SE of loop (furosemide) diuretics

*Hyperuricemia, hypokalemia

and ototoxicity

Aminoglycosides used with loop diuretics potentiate adverse

effect

Ototoxicity

Loops lose and thiazide diuretics retain * Calcium

MOA of thiazide diuretics Inhibit Na+/Cl- cotransport

Site of action of thiazide diuretics*

Work at early distal

convoluted tubule

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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

SE of spironolactone

*Gynecomastia hyperkalemia,

and impotence

Osmotic diuretic used for increased intracranial pressure

*Mannitol

Antidiuretic hormone (ADH) agonist and antagonist

ADH agonist used for pituitary diabetes insipidus * Desmopressin (DDAVP)

Used for SIADH Demeclocycline

SE of demeclocycline Bone marrow and teeth

discoloration for children

under 8 ears of a e

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 * Lidocaine

DOC for digoxin induced arrhythmias Phenytoin

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SE of phenytoin Gingival hyperplasia

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

(CAST trial), therefore are used as lastline 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 * Torsades de pointes

Agent to treat torsades de pointes Magnesium sulfate

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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 * Antithrombin 3

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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

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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

factorsAgent 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 reverseneurologic 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 GM-

CSF (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

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Difference between aspirin and other NSAIDS Aspirin irreversibly inhibits

cyclooxygenase

Four main actions of NSAIDS Anti-inflammatory,

analgesia, antipyretic and

anti latelet activit

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

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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

a ranuloc tosis

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

s nthesis

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

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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 * Xanthine oxidase

02-02-12 pharm one liners

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