Pharm One Liners Flashcards by Molly Philbin

Relates the amount of drug in the body to the plasma concentration

Volume of distribution (VD)

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Plasma concentration of a drug at a given time

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

Clearance (CL)

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Hepatic metabolism of the drug before it reaches the systemic circulation

First pass effect

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The fraction of unchanged drug that reaches systemic circulation after administration

Bioavailability (F)

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

Steady state

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Different steps of Phase I

Oxidation, reduction, hydrolysis

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Name 3 Phase II conjugation reactions

Glucuronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation, water conjugation

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Constant percentage of drug metabolized per unit time

First order kinetics

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Constant amount of drug metabolized per unit time

Zero order kinetics

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Target plasma concentration times (volume of distribution divided by bioavailability)

Loading dose (Cp*(Vd/F))

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Concentration in the plasma times (clearance divided by bioavailability)

Maintenance dose (Cp*(CL/F))

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Strength of interaction between drug and its receptor

Affinity

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Selectivity of a drug for its receptor

Specificity

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Amount of drug necessary to elicit a biologic effect compared with another drug

Potency

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Ability of a drug to produce maximal response after binding to the receptor

Full agonist

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Ability to produce less than maximal response after binding to the receptor

Partial agonist

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Ability to bind reversibly to the same site as the drug and without activating the effector system

Competitive antagonist

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Ability to bind irreversibly to the active site or bind to a site distinctly separate from the agonist binding site

Noncompetitive antagonist

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Mechanism of action utilizes ligand gated ion channels

Acetylcholine, nicotine

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Dose that produces therapeutic response in 50% of the population

ED50

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Dose that is toxic to 50% of the population

TD50

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Dose that is lethal to 50% of the population

LD50

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Window between therapeutic effect and toxic effect

Therapeutic index

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Drugs that have a high margin of safety is indicated by

High therapeutic index

Drugs that have a narrow margin of safety is indicated by

Low therapeutic index

Antidote for lead poisoning

Edetate calcium disodium, succimer, or dimercaprol

Antidote for cyanide poisoning

Nitrates, thiosulfate, hydroxocobalamin

Antidotefor anticholinergic poisoning

Physostigmine

Antidote for iron salt poisoning

Deferoxamine

Antidote for arsenic, mercury, and gold poisoning

Dimercaprol, succimer

Antidote for Wilson's disease (copper poisoning)

Penicillamine

Antidote for methanol and ethylene glycol toxicity

Fomepizole, ethanol

Antidote for tricyclic antidepressants (TCA)

Sodium bicarbonate (alkalinize plasma)

Antidote for carbon monoxide poisoning

100% O2 and hyperbaric O2

Antidote for digitalis toxicity

Digibind

Antidote for beta-blocker overdose

Glucagon

Method to reduce salicylate intoxication

Sodium bicarbonate (alkalinize urine), dialysis

Muscarinic that is very lipid soluble and used in glaucoma

Pilocarpine

Muscarinic used to treat dry mouth in Sjögren's syndrome

Pilocarpine or Cevimeline

Cholinesterase inhibitor, short duration of action, used in diagnosis of myasthenia gravis

Edrophonium

Cholinesterase inhibitor, intermediate duration of action, used off-label for postoperative paralytic ileus and urinary retention

Neostigmine

Cholinesterase inhibitor, lipid soluble, indicated for atropine overdose and glaucoma

Physostigmine

Treatment of myasthenia gravis and sometimes used prophylactically for organophosphate poisoning in chemical warfare

Pyridostigmine

Organophosphate, indicated for glaucoma but not used much clinically due to long duration of action

Echothiophate

Insecticide organophosphate

Malathion, parathion

The most important cause of acute deaths in cholinesterase inhibitor toxicity

Respiratory failure

Used in treatment of muscarinic symptoms in organophosphate overdose

Atropine

Mechanism of action of atropine

Nonselective antimuscarinic

Antimuscarinic indicated for overactive bladder muscle dysfunction

Oxybutynin

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

Pneumonic for beta receptors

You have 1 heart (Beta 1) and 2 lungs (Beta 2)

Drug of choice for anaphylactic shock

Epinephrine

Indirect acting sympathomimetic, reuptake inhibitor, commonly abused, indicated for attention deficit disorder and weight reduction

Methamphetamine

Alpha agonist indicated for nasal congestion, hypotension, and mydriasis induction

Phenylephrine

Short acting beta 2 agonist, drug of choice for acute asthma

Albuterol

Longer acting beta 2 agonist, indicated for prophylaxis of asthma

Salmeterol

Its ability to increase heart rate makes it useful as adjunct therapy for acute heart failure and hypovolemia or septic shock

Beta 1 agonist

Indicated for symptomatic orthostatic hypotension

Midodrine

Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus

Terbutaline

Indirect acting sympathomimetic, improves urinary continence in children and elderly with enuresis

Ephedrine

Beta agonists used in acute congestive heart failure

Dobutamine and dopamine

Beta 1 agonist toxicity

Sinus tachycardia and serious arrhythmias

Beta 2 agonist toxicity

Skeletal muscle tremor

Irreversible, nonselective alpha-blocker indicated for pheochromocytoma

Phenoxybenzamine

Reversible, nonselective alpha blocker indicated for pheochromocytoma

Phentolamine

Blocks alpha 1 and beta receptors and indicated for the treatment of CHF

Labetalol and carvedilol

Beta blockers with partial agonist activity, can bronchodilate and may have an advantage treating patients with asthma

Pindolol and acebutolol

Short-acting beta blocker that can be given parenterally

Esmolol

Clinical uses of these agents include treatment of hypertension, angina, arrhythmias, and chronic congestive heart failure

Beta blockers

Beta-blockers should be used cautiously in

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

Beta blockers are used for this type of angina attack

Classic (exertional) angina

A nonselective beta blocker with alpha 1 blocking effect indicated for congestive heart failure

Carvedilol

This class of drugs inhibit angiotensin-converting enzyme

ACE inhibitors

Mechanism of action of calcium channel blockers

Block L-type calcium channels

Side effects of methyldopa

Positive Comb's hemolytic anemia, SLE-like syndrome, CNS depression

Side effect of clonidine

Rebound hypertension, sedation, dry mouth

Direct vasodilator of arteriolar smooth muscle by increasing cGMP and inhibit IP3-induced calcium release from the sarcoplasmic reticulum

Hydralazine

Arterial vasodilator that works by opening K+ channels

Minoxidil

Side effect of minoxidil

Hypertrichosis

IV nitrate used in hypertensive crisis

Nitroprusside

Nitroprusside vasodilates

Arteries and veins

Side effect of nitroprusside

Cyanide poisoning

Drugs used in the management of exertional (classic) angina

Nitrates, calcium channel blockers, beta blockers

Aspirin reduces mortality in unstable angina by

Inhibiting platelet aggregation

Nitrate free intervals are needed due to

Tolerance

Side effects of nitrates

Reflex tachycardia, hypotension, flushing, and throbbing headache due to meningeal artery dilation

Mechanism of action of cardiac glycosides (eg. digoxin)

Inhibit Na+/K+ ATPase and indirectly increase intracellular calcium and cardiac contractility

Indication of digoxin

Atrial fibrillation and congestive heart failure

Digoxin toxicity can be precipitated by

Hypokalemia

Phosphodiesterase (PDE3) inhibitors indicated for acute congestive heart failure; long term use is associated with increased mortality

Amrinone and milrinone

Side effect of amrinone and milrinone

Thrombocytopenia

Agent used in acutely decompensated congestive heart failure resembling natriuretic peptide

Nesiritide

Mechanism of action of class II antiarrhythmics

Beta -blockers

Mechanism of action of class IV antiarrhythmics

Calcium channel blockers

Major drug interaction with quinidine

Increases concentration of digoxin

Contraindication of disopyramide use

Heart failure

Used as last line antiarrhythmic agents due to proarrhythmic property; strongest sodium channel blocker

Class IC (flecainide, propafenone)

Anti-arrhythmic agents that decrease mortality

B-blockers

Used intravenously for acute tachycardia during and post- surgery

Esmolol

Antiarrhythmic effective in most types of arrhythmia

Amiodarone

Class III antiarrhythmic that exhibits properties of all 4 classes

Amiodarone

Antiarrhythmic that exhibits Class II and III properties

Sotalol

Side effect of sotalol

prolongs QT interval

Drug of choice for narrow complex paroxysmal supraventricular tachycardia (PSVT)

Adenosine

Mechanism of action of adenosine

Activates G-protein coupled K+ channels in atrium, SA and AV node

Anti-arrhythmic with <10 second duration of action

Adenosine

Drug of choice for early after depolarizations (Torsade)

Magnesium sulfate

HMG CoA reductase inhibitors are contraindicated in

Pregnancy

Concurrent use of fibrates and statins increases risk of

Rhabdomyolysis

Class of agents for cholestyramine, colestipol, colesevalem

Bile acid-binding resins

Major nutritional side effect of bile acid-binding resins

Impair absorption of fat soluble vitamins (A,D,E,K)

Side effect of fenofibrate and gemfibrozil

Gallstone formation

Cutaneous flush due to niacin can be reduced by pretreatment with

NSAIDs

Inhibits intestinal cholesterol absorption by inhibiting Niemann Pick C1 Like 1 (NPC1L1) Protein

Ezetimibe

Mechanism of action of aspirin

Irreversibly blocks COX1 and COX2

Agent used to treat myocardial infarction (MI) and to reduce incidence of subsequent MI

Aspirin

Antiplatelet drug reserved for patients allergic to aspirin

Ticlopidine

Side effect for ticlopidine

Neutropenia and agranulocytosis

Irreversible inhibitor of platelet P2Y12 receptors; effective in preventing transient ischemic attack

Clopidogrel and ticlopidine

Phosphodiesterase inhibitor indicated for intermittent claudication

Dipyridamole, cilostazol

Block glycoprotein IIb/IIIa involved in platelet cross-linking

Abciximab, tirofiban and eptifibatide

Route of administration of warfarin

Oral

Contraindication of warfarin

Pregnancy

Anticoagulant of choice in pregnancy

Heparin

Routes of administration of heparin

IV and SC

Side effect of both warfarin and heparin

Bleeding

Two anticoagulant used for prophylaxis and treatment of thrombosis in patients with heparin-induced thrombocytopenia

Bivalirudin, argatroban

Thrombolytic used for acute myocardial infarction and ischemic (non-hemorrhagic) cerebral vascular accident (stroke)

Alteplase

Side effect of tissue plasminogen activators

cerebral hemorrhage

Thrombolytic that can cause allergic reaction and non-selective systemic fibrinolysis

Streptokinase

Carbonic anhydrase inhibitor

Acetazolamide

Mechanism of action of loop diuretics

inhibits Na+/K+/2Cl- cotransporter

Diuretic used in hypertensive patients with renal failure

Loop diuretics (furosemide, ethacrynic acid, butmetanide)

Aminoglycosides used with loop diuretics potentiate this adverse effect

Ototoxicity

Mechanism of action of thiazide diuretics

Inhibit Na+/Cl- cotransport

Diuretic used as first line for treatment of hypertension

Thiazides

Class of drugs that may cause cross-sensitivity with thiazide diuretics

Sulfonamides

Mechanism of action of spironolactone

Inhibit mineralocorticoid (aldosterone) receptor resulting in inhibition of Na/K-ATPase and ENaC synthesis

Diuretics work in congestive failure by

Reducing preload

Agents used for syndrome of inappropriate antidiuretic hormone (SIADH) secretion

Tolvaptan and conivaptan

An early generation tetracycline that may be used for chronic persistant syndrome of inappropriate antidiuretic hormone (SIADH) secretion

demeclocycline

Side effect of demeclocycline

Stunted bone growth and teeth discoloration for children under 8 years of age

Antibacterials for optimal treatment of acute uncomplicated cystitis

Nitrofurantoin, trimethoprim-sulfamethoxazole, fosfomycin

Antibacterials for optimal treatment of acute pyelonephritis

Fluoroquinolones (ciprofloxacin, levofloxacin), trimethoprim-sulfamethoxazole

Mechanism of action of penicillin

Block cell wall synthesis by inhibiting transpeptidase and block peptidoglycan cross-linkage

Penicillins active against penicillinase secreting bacteria

Methicillin, nafcillin, and dicloxacillin

Class of antibiotics that have 10% cross sensitivity with penicillins

Cephalosporins

Penicillins active against pseudomonas

Piperacillin and ticarcillin

Beta lactam that can be used in penicillin-allergic patients

Aztreonam

Side effect of imipenem

Seizures

Drug of choice for treatment of serious pseudomembranous colitis

Oral vancomycin

Antibiotic causing red-man syndrome, and prevention

Vancomycin, can be prevented by infusion | at a slow rate and antihistamines

Drug causes teeth discoloration

Tetracycline

Mechanism of action of tetracycline

Decreases protein synthesis by binding to 30S ribosome and prevent binding of tRNA

Two toxicities of aminoglycosides

Nephro and ototoxicity

Aminoglycoside less used due to its irreversible vestibular toxicity

Streptomycin

Mechanism of action of macrolides (erythromycin, clarithromycin)

Inhibit protein synthesis by binding to 23S rRNA of 50S ribosome subunit

Drug of choice for Legionnaires' disease

Azithromycin or levofloxacin

Drug notorious for causing pseudomembranous colitis

Clindamycin

Drug that causes gray baby syndrome and aplastic anemia

Chloramphenicol

Inhibits isoleucyl tRNA and used topically for impetigo

Mupirocin

Side effect of metronidazole when given with alcohol

Disulfiram-like reaction

Neurotoxicity with isoniazid can be prevented by

Administration of Vit B6 (pyridoxine)

Side effect of isoniazid

Systemic lupus erythematosus, peripheral neuritis, hepatitis

Drug of choice for leprosy

Dapsone

Toxicity of amphotericin

Nephrotoxicity

Side effect of ketoconazole only in men

Gynecomastia

Mechanism of action of nystatin

Binds to ergosterol and creates a pore in fungal membrane

Drug used in exoerythrocytic cycle of malaria

Primaquine

Drug of choice for cytomegalovirus (CMV) treatment

Ganciclovir

Side effect of ganciclovir

Myelosuppression (neutropenia)

First line for the treatment of chronic hepatitis B virus (HBV) infections

IFN + nucleoside reverse transcriptase inhibitor (NRTI)

First line for the treatment of chronic hepatitis C virus (HCV) infections in genotype 1 patients

IFN + ribavirin + protease inhibitor (-previr)

HIV medication used to reduce mother-to-child transmission during birth

Zidovudine, nevirapine

Antivirals associated with neutropenia

Ganciclovir, zidovudine, interferon

Two nucleoside reverse transcriptase inhibitors approved for both HIV and HBV infections

Tenofovir, lamivudine

Antiviral/antiretroviral that are teratogens

Efavirenz, and ribavirin

Anti-retroviral with a dose limiting toxicity of pancreatitis and peripheral neuropathy

Didanosine

Three anti-retroviral agents associated with fatal Stephen-Johnson syndrome

Nevirapine, efavirenz, etravirine

Anti-retroviral class that causes drug interactions by causing induction of CYP enzymes

Non-nucleos(t)ide reverse transcriptase inhibitors

Class of drugs that reversibly inhibit cyclooxygenase (COX)

NSAIDS

Mechanism of action of non-steroidal antiinflammatory drugs (NSAIDS)

inhibit prostaglandin synthesis by inhibiting cyclo-oxygenase (cox)

Four main actions of NSAIDS

Anti-inflammatory, analgesia, antipyretic and antiplatelet activity

Irreversible, nonselective COX inhibitor that displays zero-order kinetics of elimination

Aspirin

The reason why aspirin is contraindicated in children with viral infection

Potential for development of Reye's syndrome

Two side effects of salicylates

Tinnitus, GI bleeding

Prostaglandin analog indicated for severe pulmonary hypertension

Epoprostenol (PGI2)

NSAID available orally, IM, IV, nasally, and ophthalmically

Ketoralac

NSAID used mostly for anesthesia and has limited duration (<5 days) due to nephrotoxicity

Ketoralac

Difference between COX 1 and COX 2

COX 1: constitutive, COX 2: inducible during inflammation

Selective COX 2 inhibitor

Celecoxib

COX 2 inhibitors may have reduced risk of

Gastric ulcers and GI Bleeding

COX 2 inhibitors should be used cautiously in patients with

Pre-existing cardiac or renal disease

Side effect of acetaminophen

Hepatotoxicity

Major side effect of zileuton that limits its use

Liver toxicity

Two leukotrienes (LTD4) receptor antagonists used in asthma

Zafirlukast and montelukast

First line drugs for acute gout

Indomethacin, naproxen

NSAID avoided in gout because low doses increases uric acid levels

Aspirin

Mechanism of action of colchicine

Inhibits microtubule assembly, decreases leukocyte migration and phagocytosis

Side effects of colchicine

Diarrhea, liver toxicity, myelosuppression

Agent used to treat chronic gout by increasing uric acid excretion through inhibition of URAT1 anion transporter

Probenecid

Recombinant uricase that enhances uric acid metabolism and indicated for gout refractory to conventional therapy

Pegloticase

A mixture of two agents with one agent active for rheumatic disease and the other for inflammatory bowel disease

Sulfasalazine

Alternative to methotrexate as 1st line for rheumatoid arthritis through inhibition of dihydroorotate dehydrogenase, which leads to decreased pyrimidine synthesis

Leflunomide

Side effect of penicillamine

Hypersensitivity (rash), nephrotoxicity, myopathy, myelosuppression

Anti-malarial drug used in rheumatoid arthritis

Hydroxychloroquine

Side effect of hydroxychloroquine

Retinopathy

Two drugs that bind and prevent action of tumor necrosis factor alpha (TNF-alpha)

Infliximab and etanercept

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

This class of agents block acetylcholine receptors at motor endplates and its effects can be reversed by cholinesterase inhibitors

Nondepolarizing blockers

Non-depolarizing neuromuscular blocker with long duration of action and is most likely to cause histamine release

Tubocurarine

Non-depolarizing neuromuscular blocker with short duration of action

Mivacurium

Two non-depolarizing blockers that undergo Hofmann elimination, which is useful for patients with renal and hepatic deficiency

Atracurium, cisatracurium

Non-depolaring neuromuscular blocker with long duration of action that can block muscarinic receptor in the heart

Pancuronium

These drugs strongly potentiate and prolong effect of neuromuscular blockers

Inhalation anesthetics (isoflurane), antibiotics (aminoglycosides, tetracyclines)

Depolarizing blocker that causes muscle relaxation and paralysis and can cause postoperative muscle pain

Succinylcholine

Two life-threatening side effects of succinylcholine

Hyperkalemia, malignant hyperthermia

During Phase I depolarizing block this class of agents enhance muscle paralysis, but during Phase II block they may reverse muscle paralysis

Cholinesterase inhibitors

Drug of choice for reversal of non-depolarizing neuromuscular blockade

Neostigmine

Enzyme which theophylline inhibits

Phosphodiesterase

Growth hormone analog used in growth hormone deficiency

Somatropin

Somatostatin analog used for acromegaly, carcinoid, glucagonoma and other growth hormone-producing pituitary tumors

Octreotide

Gonadotropin-releasing hormone analog used for infertility (pulsatile administration) or suppression of gonadotropin production (continuous administration)

Leuprolide

Competitive antagonists at gonadotropin releasing hormone receptors used to prevent LH surge during controlled ovarian hyperstimulation

Ganirelix

An isomer of T3 which may be used in myxedema coma

Liothyronine (T3)

Thioamide agents used in hyperthyroidism

Methimazole and propylthiouracil (PTU)

Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism

Iodide salts (potassium iodide)

Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy

Radioactive iodine

Used for the symptomatic treatment of thyrotoxicosis by blocking cardiac adverse effects

Beta-blockers such as propranolol and esmolol

Used for Addison's disease, congenital adrenal hyperplasia inflammation, immune suppression, and asthma

Glucocorticoids

Two short-acting glucocorticoids

Hydrocortisone (cortisol), cortisone

Four intermediate-acting glucocorticoids

Prednisone, prednisolone, methylprednisolone, and triamcinolone

Two long-acting glucocorticoids

Betamethasone, dexamethasone

Mineralocorticoids

Fludrocortisone and deoxycorticosterone

Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis

Aminoglutethimide

Antifungal agent used to inhibit adrenal and gonadal steroid synthesis

Ketoconazole

Selective inhibitor of 11-hydroxylation and interferes with cortisol and corticoterone synthesis; used for adrenal function tests and is the only adrenal-inhibiting medication that can be administered to pregnant women with Cushing's syndrome

Metyrapone

Glucoroticoid receptor antagonist that is used as an antiabortifacient due to its strong antiprogestin activity

Mifepristone (RU486)

Three rapid-acting insulin used for postprandial glycemia

Aspart, lispro, glulisine

Short-acting insulin used intravenously for ketoacidosis

Regular insulin

Two long-acting insulin preparations that provide basal glycemia control

Glargine, detemir

Major side effect of insulin

Hypoglycemia

First generation sulfonylurea that is safest for elderly diabetics due to its short half-life

Tolbutamide

First generation sulfonylurea contraindicated in elderly diabetics because of very long half-life

Chlorpropamide

Three second generation sulfonylureas

Glyburide, glipizide, glimepiride

Mechanism of action of sulfonylureas

Close K+ channels, depolarize cell, open voltage-gated Ca2+ channels, release insulin

Common side effect of first generation sulfonylureas

Disulfiram-like reactions with alcohol use

Common side effect of second generation sulfonylureas

Hypoglycemia

A meglitinide insulin secretagogue that has no sulfur in its structure and may be used in type 2 diabetics with sulfonylurea allergy

Repaglinide

A D-phenylalanine derivative insulin secretagogue that is useful for type 2 diabetics with very reduced renal function

Nateglinide

Mechanism of action of repaglinide and nateglinide

Close K+ channels, depolarize cell, open voltage-gated Ca2+ channels, release insulin

Mechanism of action of metformin

¯ gluconeogenesis, peripheral glucose uptake; increase insulin sensitivity

Two thiazolidinediones

Pioglitazone, rosiglitazone

Mechanism of action of thiazolindinediones

Activate PPAR-gamma, transcription of insulin-responsive genes, GLUT4 glucose transporter, insulin sensitivity

Side effect of thiazolindinediones

Weight gain, edema, heart failure, hepatotoxicity

Two alpha-glucosidase inhibitors

Acarbose, miglitol

Mechanism of action of alpha-glucosidase inhibitors

Act on intestine, delay digestion and absorption of glucose

Side effect of alpha-glucosidase inhibitors

Flatulence , diarrhea, abdominal cramps

Amylin analog that delays gastric emptying and suppresses glucagon release

Pramlintide

Two glucagon-like polypeptide-1 (GLP-1) analogs that increase insulin secretion and suppress postprandial glucagon release

Exenatide, liraglutide

Three dipeptidyl peptidase-4 (DPP-4) inhibitors that reduce breakdown of glucagon-like polypeptide-1, resulting in increased insulin secretion and suppress postprandial glucagon release

Sitagliptin, saxagliptin, linagliptin

Bisphosphonates

Alendronate and -dronates

Mechanism of action of bisphosphonates

Inhibits osteoclast activity and prevent bone resorption

Uses of bisphosphonates

Osteoporosis, Paget's disease, hyperglycemia

Major side effects of bisphosphonates

Corrosive esophagitis, osteonecrosis of the jaw

First generation bisphosphonate when used long-term causes osteomalacia

Etidronate

Vitamin given with calcium to ensure proper absorption

Vitamin D

Its use can increase risk of endometrial and breast cancer, cause postmenopausal uterine bleeding, but can stabilize bone mineral loss

Estrogen

Antiestrogen drugs used for treatment of infertility in anovulatory women

Clomiphene

Common side effect of tamoxifen and clomiphene

Hot flushes

Two estradiol derivatives with higher oral bioavailability and longer half-lives that are primarily used as oral contraceptives

Ethinyl estradiol and mestranol

5 alpha-reductase inhibitor used for benign prostatic hyperplasia and male pattern baldness

Finasteride

Partial androgen agonist used for endometriosis and hereditary angioedema

Danazol

Androgen receptor antagonist used to treat prostate cancer

Flutamide

Androgen receptor antagonist used for hirsutism in females

Cyproterone

A class of endogenous substances that include histamine, serotonin, prostaglandins, and vasoactive peptides that work in autocrine or paracrine manner

Autacoids

Two peptide that increase capillary permeability and edema

Bradykinin and histamine

Most common side effect of 1st generation antihistamines

Sedation, anticholinergic

1st generation antihistamine that is least sedating

Chlorpheniramine

Major indication for H1 antihistamines

IgE mediated allergic reaction (allergic rhinitis, urticaria)

Antihistamine that is indicated for allergies, motion sickness, and insomnia

Diphenhydramine

Antihistamine with motion sickness as the only indication

Dimenhydrinate

Indication for H2 antagonists

Acid reflux disease, duodenal ulcer and peptic ulcer disease

Location of serotonin type-1 (5HT-1) receptors

Mostly in the brain

Ergot alkaloid indicated for migraine headaches

Ergotamine

Reason ergot alkaloids are contraindicated in pregnancy

Uterine contractions

Two side effects of ergot alkaloids

Prolonged vasospasm and hallucinations resembling psychosis

Two drugs that may be used off-label for ischemia and gangrene caused by ergot alkaloids overdose

Nitroprusside, nitroglycerin

Serotonin receptor responsible for serotonin syndrome

5HT2

Location of serotonin type-3 (5HT-3) receptors

GI tract, vomiting center of medulla

Ganglion blockers that were indicated (but not anymore) for severe hypertension

Hexamethonium, trimethaphan

Two direct-acting cholinomimetics that increase aqueous outflow through ciliary muscle contraction and opening of trabecular meshwork

Pilocarpine, carbachol

Two indirect-acting cholinomimetics that increase aqueous outflow through ciliary muscle contraction and opening of trabecular meshwork

Physostigmine, echothiophate

Nonselective alpha agonist that decreases aqueous production

Epinephrine

Selective alpha 2 agonist that decreases aqueous production

Brimonidine

Carbonic anhydrase inhibitor used to decrease aqueous humor production

Acetazolamide

Common side effect of sedative hypnotics

CNS depression

Occurs when sedative hypnotics are used long-term

Tolerance and physical dependence

Main route of metabolism for benzodiazepines

Hepatic

Useful side effect of benzodiazepines in patients undergoing stressful procedures or surgery

Anterograde amnesia

Three benzodiazepines that are metabolized only by Phase II conjugation and therefore is useful in elderly patients

Lorazepam, oxazepam, and temazepam

Two benzodiazepines that have active metabolites with long half-lives

Diazepam, chlordiazepoxide

Clinical uses of benzodiazepines

Anxiety, insomnia, alcohol detoxification, status epilepticus, spasticity

Reason why benzodiazepines are safer than barbiturates

Benzodiazepines work only in presence of GABA

Most serious side effects of barbiturates

Respiratory and cardiovascular depression

Barbiturates may precipitate this hematologic condition

Porphyria

Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetic property

Induce CYP450

Effect of benzodiazepines and barbiturates on sleep architecture

Suppress REM

Mechanism of action of zolpidem

Activates BZ1 subtype of GABAA receptor

Antiepileptic drug used as first line for trigeminal neuralgia

Carbamazepine

Antiepileptic drug that can induce CYP450, is teratogenic, and can cause diplopia, ataxia, and blood dyscrasias; follows first order kinetics of elimination

Carbamazepine

Mechanism of action of Phenytoin, Carbamazepine, Lamotrigine

Blocks sodium channels

Mechanism of action of valproic acid

Blocks sodium channels, T-type calcium channels, and increase GABA concentration

Antiepileptic drug that can cause fatal hepatotoxicity and neural tube defects

Valproic acid

Mechanism of action of Ethosuximide

Blocks T-type calcium channels

Antiepileptic drugs that may also be used for bipolar disorder

Valproic acid, carbamazepine, gabapentin

Serious side effect of lamotrigine that makes it require slow titration

Stevens-Johnson syndrome

Side effects of these drugs include nausea and vomiting, euphoria, dependence, tolerance, sedation, respiratory depression, constipation

Opioids

Strong opioid agonists

Morphine, methadone, meperidine, and fentanyl

Opioids used in anesthesia

Morphine and fentanyl

Opioid with antimuscarinic activity

Meperidine

Opioid that can cause hyperpyrexic coma with MAOI and serotonin syndrome with SSRI

Meperidine

Partial opioid agonist that has a long duration of action and is resistant to naloxone reversal

Buprenorphine

Opioids indicated for use as antitussive

Dextromethorphan, Codeine

Opioids indicated for use as antidiarrheal

Diphenoxylate, Loperamide

Directly proportional to the potency of inhalation anesthetics

Lipid solubility

Inversely proportional to the potency of inhalation anesthetics

Minimal alveolar concentration (MAC)

Inversely proportional to the rate of induction and recovery of inhalation anesthetics

Blood:gas partition coefficient

Mechanism of action of inhalation anesthetics

Potentiation of GABA at GABAA receptors; also reduce Na and Ca influx

Currently the only non-halogenated inhalation anesthetic

Nitrous oxide

Inhalation anesthetic with the most analgesic activity

Nitrous oxide

Inhalation anesthetic with the least respiratory and cardiovascular depression and therefore is used frequently as a component of balanced anesthesia

Nitrous oxide

Inhalation anesthetic that can cause fatal hepatotoxicity and cardiac arrhythmia and is no longer used in the US

Halothane

Inhalation anesthetic that is withdrawn from the market due to fatal nephrotoxicity

Methoxyflurane

Inhalation anesthetic that at high concentrations can produce CNS excitation, leading to seizures

Enflurane

Close to ideal inhalation anesthetic that exhibits rapid and smooth induction and recovery, with little organ system toxicity

Sevoflurane

Barbiturate used for the induction of anesthesia

Thiopental

A short-acting benzodiazepine commonly used adjunctively with inhalation anesthetics and opioid analgesics for a balanced anesthesia

Midazolam

Produces both rapid anesthesia and recovery, has antiemetic activity, but may cause marked hypotension

Propofol

Mechanism of action of the intravenous anesthetic that causes dissociative anesthesia

Block NMDA receptor

Side effects of dissociative anesthetic

Cardiovascular stimulation, increased cerebral blood flow, vivid dreams, hallucinations

Neuroleptanesthesia can be produced by a combination of these two agents

Fentanyl and droperidol

Mechanism of action of local anesthetics

Block voltage-gated sodium channels

This condition may necessitate larger doses of local anesthetics because the drugs become ionized and cannot penetrate the neuronal membranes

Low pH

Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors to prolong activity

Vasodilation

The only local anesthetic with vasoconstrictive property, but due to abuse potential, only occasionally used for nasal surgery

Cocaine

This type of local anesthetic is more likely to cause hypersensitivy reactions

Ester-type (local anesthetic with one "I" in name)

Local anesthetic most widely used for obstetric anesthesia but causes the most cardiac depression

Bupivacaine

Side effect of most local anesthetics

CNS excitation

Common side effect of antipsychotics, MPTP (contaminant in illicit meperidine analog), and cholinergic excess

Drug-induced Parkinsonism

Two fluctuations in clinical response associated with long-term use of dopamine precursor

"Wearing off" and "on-off-phenomenon"

Inhibits of catechol-O-methyltransferase (COMT), used as adjunct to improve motor function in Parkinson's patients with fluctuations in clinical response

Entacapone, tolcapone

Ergot type 2 dopamine receptor (D2) agonist, used as adjunct to improve motor function in Parkinson's patients with fluctuations in clinical response

Bromocriptine

Non ergot type 2 dopamine receptors (D2) agonist, used for Parkinson's and restless legs syndrome

Pramipexole and ropinirole

An antiviral that enhances dopamine release from nigrostriatal neurons

Amantadine

Two centrally-acting anticholinergics useful for tremor and rigidity but have little effect on bradykinesia in patients with Parkinson's

Benztropine, trihexylphenidyl

Drug of choice indicated for familial or essential tremors

Propranolol

Two drugs that inhibit vesicle monoamine transporter used for Huntington's

Tetrabenazine, reserpine

An antipsychotic with dopamine receptor antagonist activity used for Huntington's

Haloperidol

Three centrally-acting cholinesterase inhibitors used for Alzheimer's

Donepezil, rivastigmine, galantamine

Noncompetitive antagonist of NMDA receptors used for Alzheimer's

Memantine

Complications of the gastrointestinal system associated with chronic alcohol use

Mallory-Weiss syndrome, hepatitis, cirrhosis, pancreatitis

The most common neurologic abnormality in chronic alcoholics

Neurologic deficits (Peripheral neuropathy)

Life-threatening alcohol withdrawal syndrome that peaks at 5 days after the last drink

Delirium tremens

Inhibits aldehyde dehydrogenase and used as deterrent for alcohol use

Disulfiram

Opioid receptor antagonist used to prevent alcohol abuse

Naltrexone

Competes for alcohol dehydrogenase and is used in methanol or ethylene glycol poisoning

Fomepizole, ethanol

Most commonly abused opioids

Heroin, morphine, oxycodone

Sweating, dilated pupils, piloerection, and flu-like symptoms are symptoms of withdrawal from this class of drugs

Opioid

Opioids used for long-term maintenance from opioid withdrawal

Methadone, buprenorphine

Most widely abused sedative hypnotics

Short-acting barbiturates (pentobarbital)

Four major CNS stimulant drugs of abuse

Caffeine, nicotine, cocaine, amphetamines

CNS stimulant that acts by inhibiting reuptake of neurotransmitters; may cause pupil dilation, alter tactile sensation, irregular breathing, and cardiac toxicity

Cocaine

Amphetamine derivatives commonly abused

Methamphetamine (crystal meth), MDMA (methylenedioxymeth-amphetamine, or ecstasy)

Drug of abuse that was developed as a dissociative anesthetic; intoxication leads to both horizontal and vertical nystagmus, analgesia, psychosis, delirium, and seizures

PCP (phencyclidine, or angel dust)

Use of all antipsychotic medication in this group of patients is associated with increased risk of deaths

Elderlyl with dementia-related psychosis

Antipsychotics that repress primarily the positive symptoms of schizophrenia

Typical antipsychotics

Two low potency, typical antipsychotic drugs

Chlorpromazine, thioridazine

Typical antipsychotic associated with retinopathy and cardiac toxicity

Thioridazine

Three high potency, typical antipsychotic drugs

Haloperidol, fluphenazine, trifluoperazine

Typical antipsychotic that can also be used for Tourette syndrome

Haloperidol

Treatment for drug-induced acute extrapyramidal symptoms

Benztropine, diphenhydramine

Advantage of atypicals over typical antipsychotics

Less extrapyramidal symptoms, more effect against negative symptoms of schizophrenia

Two atypical antipsychotics that can cause weight gain

Clozapine, olanzapine

Two atypical antipsychoics that can prolong the QT interval

Risperidone, ziprasidone

Atypical antipsychotic that can increase prolactin levels and cause gynecomastia and irregular menstruation in men and women, respectively

Risperidone

Atypical antipsychotic that can also be used to treat irritability in autistic children

Aripiprazole

Tricyclic antidepressants

-iptyline, -ipramine, doxepin, amoxapine

Mechanism of action of tricyclic antidepressants

Block serotonin and norepinephrine reuptake

Common side effects of tricyclic antidepressants

Autonomic (block muscarinic and α1), sedation

Tricyclic secondary amines that produce less sedation and autonomic side effects (compared with tricyclic tertiary amines)

Nortriptyline, desipramine

Tricyclic antidepressant used for enuresis

Imipramine

Tricyclic antidepressant used in obsessive compulsive disorder

Clomipramine

Tricyclic antidepressant with antihistamine effect and is indicated for insomnia

Doxepin

Class of antidepressants that has fewer sedative and autonomic side effects than tricyclic antidepressants and indicated for panic disorder, generalized anxiety disorder, social phobias, bulimia, obsessive compulsive behavior, and post-traumatic stress disorder

Selective serotonin reuptake inhibitors (SSRI)

Four selective serotonin reuptake inhibitors

Fluoxetine, paroxetine, sertraline, citalopram

Two selective serotonin-norepinephrine reuptake inhibitors

Duloxetine, venlafaxine

Class of drugs that is most useful in patients with anxiety, hypochondriasis, and depression that is refractory to other antidepressants

Monamine oxidase inhibitors

Mechanism of action of isocarboxazid, phenelzine, and tranylcypromine

Irreversible inhibition of monoamine oxidase A and B

Mechanism of action of selegiline

Selectively inhibits monoamine oxidase B

A fatal condition that results from combination of monoamine oxidase inhibitors with tyramine-containing foods

Hypertensive crisis

Antidepressant that inhibits alpha 2, 5HT-2, and 5HT-3 receptors to increase release of norepinephrine and serotonin

Mirtazapine

Major route of elimination for Lithium

Kidneys

Antineoplastic pyrimidine analog that inhibits thymidylate synthetase

5-fluorouracil (5-FU)

Antineoplastic pyrimidine analog that inhibits DNA polymerase

Cytarabine

Serious side effect associated with cytarabine

Pancytopenia

Three antineoplastic purine analogs that inhibit purine synthesis

Azathioprine, 6-mercaptopurine, 6-thioguanine

Drug used concurrently with antineoplastics to reduce renal precipitation of urates

Allopurinol

Inhibits microtubule formation by binding to β-tubulin; dose-limiting side effect is bone marrow suppression

Vinblastine

Inhibits microtubule formation by binding to β-tubulin; dose-limiting side effect is neurotoxicity

Vincristine

Two prodrugs, that after liver bioactivation, bind to N7 nitrogen of guanine and cross-link DNA

Cyclophosphamide, ifosfamide

Serious side effect of cyclophosphamide and ifosfamide due to generation of acrolein

Hemorrhagic cystitis

Agent that is used to bind acrolein and prevent drug-induced hemorrhagic cystitis

Mesna

Akylating agent that has greater activity against myeloid cells than lymphoid cells; serious side effects include myelosuppression and pulmonary fibrosis

Busulfan

Two anthracyclines that chelate DNA, form free radicals, and cause dose-limiting cardiotoxicity

Daunorubicin, doxorubicin

DNA intercalating agent useful for treatment of solid tumors in children

Dactinomycin (actinomycin D)

Antineoplastic with G2 phase cell cycle selectivity

Bleomycin

Ribonucleotide reductase inhibitor with S phase cell cycle selectivity that is used for management of sickle cell anemia

Hydroxyurea

Platinum-derivatives that form DNA intrastrand cross-links; causes dose-limiting nephrotoxicity and ototoxicity

Cisplatin, carboplatin

Two antineoplastics that inhibit topoisomerase I

Irinotecan, topotecan

Two antineoplastics that inhibit topoisomerase II

Etoposide, teniposide

Inhibits BCR-ABL tyrosine kinase expressed by the Philadelphia chromosome in chronic myeloid leukemia

Imatinib

Inhibits BRAF kinase in melanomas with BRAF V600E mutation

Vemurafenib

Chimeric monoclonal antibody against CD20 antigen found on non-Hodgkin lymphomas and normal B lymphocytes

Rituximab

Recombinant human monoclonal antibody against vascular endothelial growth factor (VEGF)

Bevacizumab

Recombinant human monoclonal antibody against human epidermal growth factor-2 (HER2) receptor; useful for breast cancer cells that overexpress HER2

Trastuzumab

Gonadotropin-releasing hormone agonist that can be used to inhibit leutinizing hormone secretion and testosterone production in men with advanced prostate cancer

Leuprolide

Two most commonly used glucocorticoids for cancer due to their lymphotoxic effects; may cause Cushing-like symptoms

Prednisone, prednisolone

Increase activity of cytoxic cells and indicated for hairy cell leukemia

Interferon alpha-2b

Agent used for hypochromic microcytic anemias

Ferrous sulfate

Agent used for megaloblastic anemia with neurological deficits

Vitamin B12

Agent used for neutropenia associated with cancer chemotherapy and bone marrow transplantation

Filgrastim (granulocyte colony-stimualting factor) and sargramostim (granulocyte-macrophage colony-stimulating factor)

Pharm One Liners Flashcards

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