Pharm One Liners Flashcards
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)
Hepatic metabolism of the drug before it reaches the systemic circulation
First pass effect
The fraction of unchanged drug that reaches systemic circulation after administration
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination
Steady state
Different steps of Phase I
Oxidation, reduction, hydrolysis
Name 3 Phase II conjugation reactions
Glucuronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation, water conjugation
Constant percentage of drug metabolized per unit time
First order kinetics
Constant amount of drug metabolized per unit time
Zero order kinetics
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))
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 compared with another drug
Potency
Ability of a drug to produce maximal response after binding to the receptor
Full agonist
Ability to produce less than maximal response after binding to the receptor
Partial agonist
Ability to bind reversibly to the same site as the drug and without activating the effector system
Competitive antagonist
Ability to bind irreversibly to the active site or bind to a site distinctly separate from the agonist binding site
Noncompetitive antagonist
Mechanism of action utilizes ligand gated ion channels
Acetylcholine, nicotine
Dose that produces therapeutic response in 50% of the population
ED50
Dose that is toxic to 50% of the population
TD50
Dose that is lethal to 50% of the population
LD50
Window between therapeutic effect and toxic effect
Therapeutic index
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)
