USMLE Pharm Flashcards
1
Q
Abciximab
A
Monoclonal antibody to fibrin receptor (glycoprotein IIb/IIIa) on platelets. Used to prevent clotting after coronary angioplasty
2
Q
Acetaminophen
A
Antipyretic analgesic: very weak cyclooxygenase inhibitor; not anti inflammatory. Less toxic than aspirin but more dangerous in overdose (causes hepatic necrosis antidote: acetylcysteine)
3
Q
Acetazolamide, dorzolamide
A
Carbonic anhydrase inhibitor diuretic: produces a NaHCO3 diuresis, results in bicarbonate depletion, and therefore has self limited action. Used in glaucoma and mountain sickness. Dorzolamide is a topical analog for glaucoma
4
Q
Acetylcholine
A
Cholinomimetic prototype: transmitter in CNS, ENS, all ANS ganglia, parasympathetic postganglionic synapses, sympathetic postganglionic fibers to sweat glands, and some skeletal muscle vasodilator synapses
5
Q
Acyclovir
A
Antiviral: inhibits DNA synthesis in herpes simplex and varicella zoster. Requires activation by viral thymidine kinase (TK strains are resistant). Tox: behavioral effects and nephrotoxicity (crystalluria), but not myelosuppression
6
Q
Adenosine
A
Antiarrhythmic: unclassified (“Group V”); parenteral only. Hyperpolarizes AV nodal tissue, blocks conduction for 10 15 sec. Used for nodal reentry arrhythmias
7
Q
Allopurinol
A
Antigout: inhibitor of xanthine oxidase; reduces production of uric acid
8
Q
Albuterol, metaproterenol, terbutaline
A
Important beta2 agonists; used mainly for asthma.
9
Q
Alprazolam
A
Benzodiazepine sedative hypnotic: widely used in anxiety states, selectivity for panic attacks and phobias; possible antidepressant actions. Tox: psychologic and physical dependence, additive effects with other CNS depressants
10
Q
Alteplase (rt PA)
A
Thrombolytic: human recombinant tissue plasminogen activator. Used in acute MI to recanalize the occluded coronary. Occasionally used in pulmonary embolism, stroke. Tox: bleeding
11
Q
Amiloride
A
K+ sparing diuretic: blocks Na+ channels in cortical collecting tubules
12
Q
Aminoglutethimide
A
Nonsteroid inhibitor of steroid synthesis: reduces conversion of cholesterol to the hormone precursor, pregnenolone. Used in metastatic breast cancer
13
Q
Amiodarone
A
Group IA and III antiarrhythmic: broad spectrum, blocks sodium, potassium, calcium channels, beta receptors. High efficacy and very long half life (weeks months). Tox: deposits in tissues; hypo or hyperthyroidism; pulmonary fibrosis
14
Q
Amitriptyline
A
Tricyclic antidepressant: blocks reuptake of norepinephrine and serotonin. Tox: atropine like, postural hypotension, sedation; cardiac arrhythmias in overdose, additive effects with other CNS depressants
15
Q
Amoxicillin
A
Penicillin: wider spectrum than pen G with activity similar to ampicillin but greater oral bioavailability; less adverse effects on GI tract than ampicillin. Susceptible to penicillinases unless used with clavulanic acid. Tox: penicillin allergy
16
Q
Amphetamine
A
Indirectly acting sympathomimetic: displaces stored catecholamines in nerve endings. Marked CNS stimulant actions; high abuse liability. Tox: psychosis, HTN, MI, seizures
17
Q
Amphotericin B
A
Antifungal: polyene drug of choice for most systemic mycoses; binds to ergosterol to disrupt fungal cell membrane permeability. Tox: chills and fever, hypokalemia, hypotension, nephrotoxicity (dose limiting, possibly less with liposomal forms)
18
Q
Ampicillin
A
Penicillin: wider spectrum than pen G, susceptible to penicillinases unless used with sulbactam. Activity similar to pen G, plus E coli, H influenzae, P mirabilis, Shigella. Synergy with aminoglycosides versus enterococci and listeria. Tox: penicillin allergy; more adverse effects on GI tract than other penicillins; maculopapular skin rash
19
Q
Anistreplase (APSAC)
A
Thrombolytic: bacterial streptokinase complexed with human plasminogen. Longer acting in body than other thrombolytics (rt PA, streptokinase, urokinase). Tox: bleeding, allergy to streptococcal protein
20
Q
Aspirin
A
NSAID prototype: inhibits cyclooxygenase (COX) I and II irreversibly. Potent antiplatelet agent as well as antipyretic analgesic anti inflammatory drug
21
Q
Atenolol
A
Beta1 selective blocker: low lipid solubility, less CNS effect; used for HTN. (Note mnemonic for beta1 selective blockers: their names start with A through M. [Exceptions: carteolol & labetalol are not selective])
22
Q
Atropine
A
Muscarinic cholinoceptor blocker prototype: lipid soluble, CNS effects. Tox: “red as a beet, dry as a bone, mad as a hatter,” urinary retention, mydriasis
23
Q
Azithromycin
A
Antibiotic: similar to erythromycin, but greater activity versus chlamydia and streptococci; long half life due to tissue accumulation. Tox: GI distress, but no inhibition of drug metabolism
24
Q
Baclofen
A
GABA analog, orally active: spasmolytic; activates GABAB receptors in the spinal cord
25
Benztropine
Centrally acting antimuscarinic prototype for parkinsonism
26
Bethanechol
Muscarinic agonist: choline ester with good resistance to cholinesterase; used for atonic bowel or bladder
27
Botulinum
Toxin: enzyme produced by Clostridium botulinum; interacts with fusion/docking proteins to block release of acetylcholine vesicles
28
Bromocriptine
Ergot derivative: dopamine agonist in CNS; inhibits prolactin release. Used in parkinsonism and hyperprolactinemia. Tox: CNS, dyskinesias, hypotension
29
Bupivacaine
Long acting amide local anesthetic prototype: greater CV toxicity than most local anesthetics
30
Buspirone
Anxiolytic: atypical drug that interacts with 5HT1A receptors; slow onset. Minimal potentiation of CNS depressants including ethanol; negligible abuse liability
31
Captopril
ACE inhibitor prototype: used in HTN, diabetic renal disease, and CHF. Tox: hyperkalemia, fetal renal damage, cough ("sore throat")
32
Carbachol
Nonselective muscarinic and nicotinic agonist: choline ester with good resistance to cholinesterase; used for glaucoma (not a first line drug)
33
Carbamazepine
Anticonvulsant: tricyclic derivative used for tonic clonic and partial seizures; blocks Na+ channels in neuronal membranes. Drug of choice for trigeminal neuralgia; back up drug in mania. Tox: CNS depression, hematotoxic, induces liver drug metabolizing enzymes
34
Cefazolin
First generation cephalosporin prototype: bactericidal beta lactam inhibitor of cell wall synthesis. Active against gram positive cocci, E coli, K pneumoniae, but does not enter CSF. Tox: potential allergy; partial cross reactivity with penicillins
35
Cefoxitin
Second generation cephalosporin: active against a wide spectrum of gram negative bacteria including anaerobes (B fragilis). Does not enter the CNS
36
Ceftriaxone
Third generation cephalosporin: active against resistant bacteria including gonococci, H influenzae, and other gram negative organisms. Crosses the blood brain barrier
37
Celecoxib, rofecoxib
First COX II selective NSAIDs. Reduced GI toxicity
38
Chloramphenicol
Antibiotic: broad spectrum agent; inhibits protein synthesis (50S); uses restricted to back up drug for bacterial meningitis, infections due to anaerobes, Salmonella. Tox: reversible myelosuppression, aplastic anemia, gray baby syndrome
39
Chloroquine
Antimalarial: blood schizonticide used for treatment and as a chemosuppressant where P falciparum is susceptible. Tox: GI distress and skin rash at low doses; peripheral neuropathy, skin lesions, auditory and visual impairment, quinidine like myocardial depression at high doses
40
Chlorpheniramine
Antihistamine H1 blocker prototype: Tox: sedation, antimuscarinic
41
Chlorpromazine
Phenothiazine antipsychotic drug prototype: blocks most dopamine receptors in the CNS. Tox: atropine like, EPS dysfunction, hyperprolactinemia, postural hypotension, sedation, seizures (in overdose), additive effects with other CNS depressants
42
Cholestyramine, colestipol
Bile acid binding resins: sequester bile acids in gut and divert more cholesterol from the liver to bile acids instead of circulating lipoproteins. Tox: constipation, bloating; interfere with absorption of some drugs
43
Cimetidine
H2 blocker prototype: used in acid peptic disease. Tox: inhibits hepatic drug metabolism; antiandrogen effects. Less toxic analogs: ranitidine, famotidine, nizatidine
44
Ciprofloxacin
Fluoroquinolone antibiotic: bactericidal inhibitor of topoisomerases; active against many gram negative rods including E coli, H influenzae, Campylobacter, Enterobacter, Pseudomonas, Shigella. Tox: CNS dysfunction, GI distress, superinfection, collagen damage (avoid in children and pregnant women). Interactions: caffeine, theophylline, warfarin
45
Cisplatin
Platinum containing alkylating cancer chemotherapeutic agent. Used for several solid tumors (eg, testes, lung). Carboplatin is similar.
46
Clindamycin
Lincosamide antibiotic: bacteriostatic inhibitor of protein synthesis (50S); active against gram positive cocci, B fragilis. Tox: GI distress, pseudomembranous colitis
47
Clomiphene
Estrogen partial agonist: synthetic used in infertility to induce ovulation
48
Clonidine
Alpha2 agonist: acts centrally to reduce SANS outflow, lowers BP. Tox: rebound HTN if stopped suddenly
49
Clozapine
Atypical antipsychotic: low affinity for dopamine D2 receptors, higher for D4 and 5 HT2A receptors; less EPS adverse effects than other antipsychotic drugs. Tox: ANS effects, agranulocytosis (infrequent but significant)
50
Cocaine
Indirectly acting sympathomimetic: blocks amine reuptake into nerve endings. Local anesthetic (ester type). Marked CNS stimulation, euphoria; high abuse liability. Tox: psychosis, cardiac arrhythmias, seizures
51
Colchicine
Microtubule assembly inhibitor: reduces mobility and phagocytosis by WBCs in gout inflamed joints; useful in acute, not chronic gout. Tox: GI, hepatic, renal damage
52
Cyclopentolate, tropicamide
Antimuscarinics for ophthalmology: shorter duration than atropine (a few hours or less); cause cycloplegia and mydriasis
53
Cyclophosphamide
Antineoplastic, immunosuppressive: cell cycle nonspecific alkylating agent. Tox: alopecia, gastrointestinal distress, hemorrhagic cystitis, myelosuppression
54
Cyclosporine
Immunosuppressant: antibiotic; inhibits interleukin 2 synthesis, suppresses T cells. Tox: HTN, hirsutism, nephrotoxicity (dose limiting), seizures (in overdose). Not a myelosuppressant
55
Dantrolene
Blocks Ca2+ release from sarcoplasmic reticulum of skeletal muscle. Used in muscle spasm (cerebral palsy, multiple sclerosis, cord injury) and in emergency treatment of hyperthermia caused by malignant hyperthermia, malignant neuroleptic syndrome, and serotonin syndrome
56
DDAVP
ADH analog: synthetic peptide used for pituitary diabetes insipidus
57
DDT
Insecticide: prevents inactivation of sodium channels, causes uncontrolled neuronal activity. Stored for years in body fat in mammals, birds, fish
58
Deferoxamine
Chelator: bacterial product; chelates iron very avidly, aluminum less so
59
Dexfenfluramine
5 HT reuptake inhibitor and receptor agonist previously used as anorexic. Tox: produced cardiac valve damage when used in combination with phentermine
60
Dexamethasone
Glucocorticoid: very potent, long acting; no mineralocorticoid activity
61
Diazepam
Benzodiazepine prototype: binds to BDZ receptors of the GABAA receptor chloride ion channel complex; facilitates the inhibitory actions of GABA by increasing frequency of channel opening. Uses: anxiety states, ethanol detoxication, muscle spasticity, status epilepticus. Tox: psychologic and physical dependence, additive effects with other CNS depressants
62
Didanosine (DDI)
Antiviral: nucleoside inhibitor of HIV reverse transcriptase. Tox: peripheral neuropathy, pancreatitis
63
Digitoxin
Cardiac glycoside: half life 168 h, excreted in the bile (partially as digoxin); subject to enterohepatic circulation. See digoxin
64
Digoxin
Cardiac glycoside prototype: positive inotropic drug for CHF, half life 40 h; renal excretion; inhibits Na+/K+ ATPase, also a cardiac parasympathomimetic. Tox: calcium overload arrhythmias, GI upset
65
Diltiazem
Calcium channel (L type) blocker prototype: like verapamil, has more depressant effect on heart than dihydropyridines (eg, nifedipine). Tox: AV block, CHF, edema, constipation
66
Dimercaprol (BAL)
Chelator (British AntiLewisite): used for arsenic, lead, and mercury poisoning
67
Dioxin (TCDD)
Toxin: byproduct of the manufacture of herbicides 2,4 D and 2,4,5 T. Tox: extremely potent carcinogen in guinea pigs; poorly documented in humans except for chloracne, a skin disorder that occurs acutely upon exposure
68
Diphenhydramine
Antihistamine H1 blocker prototype: used in hayfever, motion sickness, dystonias. Tox: antimuscarinic, anti alpha, sedative
69
Disopyramide
Group IA antiarrhythmic: used for ventricular arrhythmias. Tox: strong antimuscarinic; may cause CHF
70
Dopamine
Neurotransmitter and agonist drug at dopamine receptors: used in shock to increase renal blood flow, stimulate heart
71
Doxorubicin
Antineoplastic: anthracycline drug (cell cycle nonspecific); intercalates between base pairs to disrupt DNA functions and forms cytotoxic free radicals. Tox: cardiotoxicity, myelosuppression
72
Doxycycline
Tetracycline antibiotic: protein synthesis inhibitor (30S), more effective than other tetracyclines against bacillary dysentery. Unlike other tetracyclines, it is eliminated mainly in the feces. Tox: see tetracycline
73
Echothiophate
Organophosphate cholinesterase inhibitor: less lipid soluble than most organophosphates; used in glaucoma
74
Edetate (EDTA)
Chelating agent: used in lead poisoning. Tox: renal tubular necrosis
75
Edrophonium
Cholinesterase inhibitor: very short duration of action (15 min). Used to reverse NM blockade and as diagnostic test in myasthenia gravis
76
Enoxaparin
Low molecular weight heparin. Primary effect is anti factor X. Other low molecular weight heparin like products: dalteparin, danaparoid. Tox: bleeding
77
Ephedrine
Indirectly acting sympathomimetic: like amphetamine but less CNS stimulation, more smooth muscle effects
78
Epinephrine
Adrenoceptor agonist prototype: product of adrenal medulla, some CNS neurons. Affinity for all alpha and all beta receptors. Used in asthma; as hemostatic and adjunct with local anesthetics; drug of choice in anaphylaxis
79
Ergonovine
Ergot alkaloid: uterine effect prototype, causes prolonged uterine contraction. Used in post partum bleeding
80
Ergotamine
Ergot alkaloid: vascular effect prototype, causes prolonged vasoconstriction, uterine contraction. Used in migraine, obstetrics
81
Erythromycin
Macrolide antibiotic: inhibitor of protein synthesis (50S); activity includes gram positive cocci and bacilli, M pneumoniae, Legionella pneumophila, C trachomatis. Tox: cholestatic jaundice, inhibits liver drug metabolizing enzymes, interactions with astemizole, theophylline, terfenadine, warfarin
82
Ethacrynic acid
Loop diuretic: not a sulfa derivative. Tox: like furosemide but does not increase serum uric acid.
83
Ethanol
Sedative hypnotic: acute actions include impaired judgment, ataxia, loss of consciousness, vasodilation, and cardiovascular and respiratory depression. Chronic use leads to dependence and liver, cardiovascular, endocrine, gastrointestinal, hepatic, and nervous system pathology. Note: zero order elimination kinetics
84
Ethosuximide
Anticonvulsant: used in absence seizures; may block T type Ca2+ channels in thalamic neurons. Tox: GI distress but safe in pregnancy
85
Etidronate, pamidronate, alendronate
Bisphosphonates: reduce turnover of bone calcium. Used in Paget's disease, osteoporosis; alendronate increases bone formation. Tox: severe esophageal ulceration
86
Fexofenadine
2nd generation antihistamine; does not enter CNS, little or no sedation
87
Finasteride
Steroid inhibitor of 5 alpha reductase: inhibits synthesis of dihydrotestosterone, the active androgen in prostate. Used in BPH
88
Flecainide
Group IC antiarrhythmic prototype: used in ventricular tachycardia and rapid atrial arrhythmias with Wolff Parkinson White syndrome. Tox: arrhythmogenic, CNS excitation
89
Fluconazole
Imidazole antifungal: used for esophageal candidiasis and in coccidioidomycoses; high CSF levels provide prophylaxis versus fungal meningitis in immunosuppressed patients
90
Fludrocortisone
Synthetic corticosteroid: high mineralocorticoid and moderate glucocorticoid activity; long duration of action
91
Flumazenil
Benzodiazepine receptor antagonist: used to reverse CNS depressant effects of benzodiazepines (overdose or when used in anesthesia)
92
Fluorouracil
Antineoplastic: pyrimidine antimetabolite (cell cycle specific) causes "thymine less" cell death; used mainly for solid or superficial tumors. Tox: GI distress, myelosuppression
93
Fluoxetine
Antidepressant: serotonin selective reuptake inhibitor (SSRI) prototype. Less ANS adverse effects and cardiotoxic potential than tricyclics. Tox: CNS stimulation, seizures in overdose
94
Flutamide
Androgen receptor inhibitor: nonsteroid used in prostatic carcinoma
95
Furosemide
Loop diuretic prototype: blocks Na+/K+/2Cl transporter; high efficacy; used in acute pulmonary edema, refractory edematous states, hypercalcemia. Tox: ototoxicity, K+ wasting, hypovolemia, increased serum uric acid
96
Foscarnet
Antiviral: effective against CMV and HSV (including TK strains); Tox: electrolyte imbalance, nephrotoxicity
97
Ganciclovir
Antiviral: effective against CMV; requires bioactivation via thymidine kinase. Tox: myelosuppression, nephrotoxicity
98
Gemfibrozil, clofibrate
Antilipemics: stimulate lipoprotein lipase in peripheral tissues. Used in hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia
99
Gentamicin
Aminoglycoside prototype: bactericidal inhibitor of protein synthesis (30S); active against many aerobic gram negative bacteria. Narrow therapeutic window; dose reduction required in renal impairment. Tox: renal dysfunction, ototoxicity; once daily dosing is effective (post antibiotic effect) and less toxic
100
Glipizide, glyburide
Oral hypoglycemics: second generation, very potent. Like other sulfonylureas, act by closing K channels in pancreatic B cells, causing depolarization and release of insulin. Tox: hypoglycemia
101
Glucagon
Hormone product of pancreatic A cells. Increases blood sugar via increased cAMP
102
Guanethidine
Postganglionic sympathetic neuron blocker: enters nerve ending by means of uptake 1 and is stored in the ending (effect reversed by TCAs, cocaine). Tox: severe orthostatic hypotension, sexual dysfunction
103
Haloperidol
Antipsychotic butyrophenone: blocks brain dopamine D2 receptors. Tox: marked EPS dysfunction, hyperprolactinemia; less ANS adverse effects than phenothiazines
104
Halothane
General anesthetic prototype: inhaled halogenated hydrocarbon. Causes cardiovascular and respiratory depression and relaxes skeletal and smooth muscle. Use has decreased due to sensitization of heart to catecholamines, and occurrence (rare) of hepatitis and malignant hyperthermia
105
Heparin
Anticoagulant: large polymeric molecule with antithrombin, and anti factor X activity. Primary rapid onset, in vitro and in vivo anticoagulation. Antidote: protamine. See also enoxaparin
106
Hydralazine
Antihypertensive: arteriolar vasodilator, orally active; used in HTN, CHF. Tox: Tachycardia, salt and water retention, lupus like syndrome
107
Hydrochlorothiazide
Thiazide diuretic prototype: acts in distal convoluted tubule; blocks Na+/Cl transporter; used in HTN, CHF, chronic renal stone syndrome. Tox: increased serum lipids, uric acid, glucose; K+ wasting
108
Ibuprofen
NSAID prototype: short duration. Inhibits cyclooxygenase (both I and II) reversibly. Used in arthritis, dysmenorrhea, muscle inflammation. Tox: peptic ulcer, renal damage
109
Imipenem
Antibiotic: carbapenem beta lactam active against many aerobic and anaerobic bacteria including penicillinase producing organisms; a bactericidal inhibitor of cell wall synthesis. Used with cilastatin (which inhibits metabolism by renal dehydropeptidases). Tox: allergy (partial cross reactivity with penicillins), seizures (overdose)
110
Imipramine
Tricyclic antidepressant prototype: blocks reuptake of norepinephrine and serotonin. Tox: ANS (alpha and muscarinic) blockade, cardiac arrhythmias
111
Indinavir
Antiviral; HIV protease inhibitor used as component of combination regimens in AIDS. Tox: anemia, nephrolithiasis, inhibits P 450 drug metabolism reactions. Other protease inhibitors: ritonavir, nelfinavir, saquinavir
112
Indomethacin
NSAID prototype: highly potent. Usually reserved for acute inflammation (eg, acute gout), not chronic; neonatal patent ductus arteriosus. Tox: GI (bleeding), renal damage
113
Insulin
Hypoglycemic peptide hormone of B (beta) cells of the pancreas: stimulates transport of glucose into cells and glycogen formation; inhibits lipolysis and protein catabolism
114
Interferon γ
Important cytokine for the treatment of hepatitis B and C infection.
115
Ipodate
Antithyroid: iodine containing radiocontrast medium; also used in thyrotoxicosis. Reduces peripheral conversion of T4 to T3; may also reduce release of hormone from thyroid
116
Ipratropium
Antimuscarinic agent: aerosol for asthma, COPD. Good bronchodilator in 20 30% of patients. Not as effective as β2 agonists
117
Isoniazid
Antimycobacterial: primary drug in combination regimens for tuberculosis; used as sole agent in prophylaxis. Metabolic clearance via N acetyltransferases (genetic variability). Tox: hepatotoxicity (age dependent), peripheral neuropathy (reversed by pyridoxine), hemolysis (in G6PD deficiency)
118
Isoproterenol
Beta1, beta2 agonist catecholamine prototype: bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR. Tox: arrhythmias, angina
119
Ketoconazole
Antifungal azole prototype: active systemically; inhibits the synthesis of ergosterol. Used for C albicans, dermatophytes and for non life threatening systemic mycoses. Tox: hepatic dysfunction, inhibits steroid synthesis and P450 dependent drug metabolism
120
Labetalol
Alpha and beta blocker: used in HTN. Tox: AV block, hypotension
121
Leuprolide
GnRH analog: synthetic peptide used in pulse therapy to stimulate gonadal steroid synthesis (infertility); used in continuous or depot therapy to shut off steroid synthesis, especially in prostate carcinoma
122
Levodopa
Dopamine precursor: used in parkinsonism, usually combined with carbidopa (a peripheral inhibitor of dopamine metabolism). Tox: dyskinesias, hypotension, on off phenomena, behavioral changes
123
Lidocaine
Local anesthetic, medium duration amide prototype: highly selective use dependent Group IB antiarrhythmic; used for nerve block and post MI ischemic ventricular arrhythmias. Tox: CNS excitation
124
Lithium
Antimanic prototype: drug of choice in mania and bipolar affective disorders; blocks recycling of the phosphatidyl inositol second messenger system. Tox: tremor, diabetes insipidus, goiter, seizures (in overdose), teratogenic potential (Ebstein's malformations)
125
Lovastatin
Antilipemic HMG CoA reductase inhibitor prototype: acts in liver to reduce synthesis of cholesterol. Other statins: atorvastatin, fluvastatin, pravastatin, simvastatin. Tox: liver damage (elevated enzymes), muscle damage
126
LSD
Lysergic acid diethylamide, "Acid:" semisynthetic ergot derivative; orally active; hallucinogen
127
Malathion
Organophosphate insecticide cholinesterase inhibitor: pro drug converted to malaoxon. Less toxic in mammals and birds because metabolized to inactive products
128
Meperidine
Opioid analgesic: synthetic, equivalent to morphine in efficacy, but orally bioavailable. Strong agonist at mu opioid receptors; blocks muscarinic receptors. Tox: see morphine
129
Mestranol
Synthetic estrogen: used in many oral contraceptives
130
Metformin, phenformin
Oral biguanide hypoglycemics: mechanism not understood, different from sulfonylurea oral hypoglycemics. Some efficacy in the absence of functioning pancreatic B cells
131
Methadone
Opioid analgesic: synthetic mu agonist, equivalent to morphine in efficacy, but orally bioavailable with longer half life (used to suppress withdrawal symptoms and in maintenance programs). Tox: see morphine
132
Methotrexate
Antineoplastic, immunosuppressant: cell cycle specific drug that inhibits dihydrofolate reductase. Major dose reduction required in renal impairment. Tox: gastrointestinal distress, myelosuppression. Leucovorin rescue used to reduce toxicity after very high doses
133
Methyldopa
Antihypertensive: prodrug of methylnorepinephrine, a CNS active α2 agonist. Reduces SANS outflow from vasomotor center. Tox: positive Coombs test, hemolysis
134
Methysergide
Ergot alkaloid: used as prophylactic in migraine. Tox: retroperitoneal and subendocardial fibroplasia
135
Metoprolol
Beta1 selective blocker: used in HTN and for prevention of post MI sudden death arrhythmias
136
Metronidazole
Antiprotozoal antibiotic: drug of choice in extraluminal amebiasis and trichomoniasis; active against bacterial anaerobes including B fragilis and in antibiotic induced colitis due to C difficile. Tox: peripheral neuropathy, gastrointestinal distress, ethanol intolerance, mutagenic potential
137
Mexiletine
Group IB antiarrhythmic drug: like lidocaine but orally active
138
Mifepristone (RU 486)
Progesterone and glucocorticoid inhibitor: abortifacient, antineoplastic
139
Minoxidil
Antihypertensive: pro drug of minoxidil sulfate, a high efficacy arteriolar vasodilator. Used in HTN; topically for baldness. Tox: tachycardia, salt and water retention, pericardial effusion
140
Misoprostol
PGE1 derivative: orally active prostaglandin used to prevent peptic ulcers in patients taking NSAIDs for arthritis. Tox: diarrhea
141
Morphine
Opioid analgesic prototype: strong mu receptor agonist. Poor oral bioavailability. Effects include analgesia, constipation, emesis, sedation, respiratory depression, miosis, and urinary retention. Tolerance may be marked; high potential for psychologic and physical dependence. Additive effects with other CNS depressants
142
Nafcillin
Penicillinase resistant penicillin prototype: used for suspected or known staphylococcal infections; not active against methicillin resistant staphylococci. Tox: penicillin allergy
143
Nalbuphine
Opioid: mixed agonist antagonist analgesic that activates kappa and weakly blocks mu receptors. Effective analgesic, but with lower abuse liability and less respiratory depressant effects than most strong opioid analgesics
144
Naloxone
Opioid mu receptor antagonist: used to reverse CNS depressant effects of opioid analgesics (overdose or when used in anesthesia)
145
Neostigmine
Cholinesterase inhibitor prototype: quaternary nitrogen carbamate with little CNS effect
146
Nevirapine
Prototype nonnucleoside inhibitor of HIV reverse transcriptase (NNRTI).Others : efavirenz, delavirdine
147
Niacin
Antilipemic: reduces release of VLDL from liver into circulation. Tox: flushing
148
Nifedipine
Calcium channel blocker prototype: vasoselective (less cardiac depression); used in angina, HTN. Tox: constipation, headache
149
Nitroglycerin
Antianginal vasodilator prototype: releases NO in smooth muscle of veins, less in arteries, and causes relaxation. Standard of therapy in angina (both atherosclerotic and variant). Tox: tachycardia, orthostatic hypotension, headache
150
Norepinephrine
Adrenoceptor agonist prototype: acts at all alpha and at beta1 adrenoceptors; used as vasoconstrictor. Causes reflex bradycardia. Tox: ischemia, arrhythmias, HTN
151
Norfloxacin
Fluoroquinolone antibiotic: inhibits bacterial DNA gyrase; active against many urinary pathogens including E coli, H influenzae, Klebsiella, Enterobacter, Pseudomonas, Serratia. Tox: see ciprofloxacin
152
Norgestrel
Progestin: used in many oral contraceptives and Norplant implantable contraceptive
153
Olanzapine
Atypical antipsychotic; high affinity antagonist at 5HT2A with minimal extrapyramidal side effects; improves both positive and negative symptoms of schizophrenia
154
Omeprazole
Antiulcer: irreversible blocker of H+/K+ ATPase proton pump in parietal cells of stomach. Used in Zollinger Ellison syndrome, gastroesophageal reflux disease (GERD)
155
Ondansetron, granisetron
5 HT3 receptor blockers: very important antiemetics for cancer chemotherapy; also used post operatively to reduce vomiting
156
Paraquat
Toxic herbicide: very small oral (but not inhaled) doses cause lethal pulmonary fibrosis
157
Parathion
Organophosphate acetylcholinesterase inhibitor prototype: used as insecticide. Pro drug: converted in body to paraoxon. Other organophosphates: DFP, soman, tabun, echothiophate. Tox: "DUMBELS" mnemonic (Chapter 7)
158
Penicillamine
Chelator, immunomodulator: copper and sometimes lead, mercury, arsenic. Used in Wilson's disease and rheumatoid arthritis
159
Penicillin G
Penicillin prototype: active against common streptococci, gram positive bacilli, gram negative cocci, spirochetes, and enterococci (if used with an aminoglycoside); penicillinase susceptible. Tox: penicillin allergy
160
Phenobarbital
Long acting barbiturate prototype: used as a sedative and for tonic clonic seizures. Facilitates GABA mediated neuronal inhibition (by increasing duration of channel opening) and may block excitatory neurotransmitters. Partial renal clearance that can be increased by urinary alkalinization. Chronic use leads to induction of liver drug metabolizing enzymes and ALA synthase. Tox: psychologic and physical dependence liability; additive effects with other CNS depressants
161
Phenoxybenzamine
Alpha blocker prototype: irreversible action. Used in pheochromocytoma
162
Phentolamine
Alpha blocker prototype: reversible action. Used in pheochromocytoma
163
Phenytoin
Anticonvulsant: used for tonic clonic and partial seizures; blocks Na+ channels in neuronal membranes. Serum levels variable due to first pass metabolism and dose dependent nonlinear elimination kinetics. Tox: sedation, diplopia, gingival hyperplasia, hirsutism, respiratory depression in overdose, teratogenic potential. Drug interactions via effects on plasma protein binding or induction of hepatic metabolism
164
Physostigmine
Cholinesterase inhibitor prototype: alkaloid tertiary amine carbamate, enters eye and CNS readily. Used in glaucoma
165
Pilocarpine
Muscarinic agonist prototype: tertiary amine alkaloid. May cause paradoxical hypertension by activating excitatory muscarinic EPSP receptors in postganglionic sympathetic neurons. Used in glaucoma. Tox: muscarinic excess
166
Piroxicam
NSAID with longest duration of action (t1/2 about 40 h)
167
Pralidoxime
Acetylcholinesterase regenerator: very high affinity for phosphorus in organophosphates
168
Prazosin, terazosin, doxazosin
Alpha1 selective blockers: used in HTN. Tox: first dose orthostatic hypotension
169
Prednisone
Glucocorticoid prototype: potent, short acting; much less mineralocorticoid activity than cortisol but more than dexamethasone or triamcinolone
170
Probenecid
Uricosuric: inhibitor of renal weak acid secretion and reabsorption in S2 segment of proximal tubule; prolongs half life of penicillin, accelerates clearance of uric acid. Used in gout
171
Probucol
Antilipemic: unknown mechanism; recently withdrawn but new evidence suggests efficacy in preventing restenosis of coronaries after angioplasty.Tox: causes arrhythmias
172
Procainamide
Group IA antiarrhythmic drug: short half life; similar to quinidine but may cause lupus erythematosus
173
Propranolol
Nonselective beta blocker prototype: local anesthetic action but no partial agonist effect. Used in HTN, angina, arrhythmias, migraine, hyperthyroidism, tremor. Tox: asthma, AV block, CHF
174
Propylthiouracil
Antithyroid drug prototype: reduces iodination of tyrosine and coupling of MIT and DIT in the thyroid; orally active. Tox: rash, agranulocytosis (rare)
175
Prostacyclin
PGI2: prostaglandin vasodilator and inhibitor of platelet aggregation
176
Pyridostigmine
Cholinesterase inhibitor: long acting (8 h) quaternary carbamate; used in myasthenia gravis
177
Quinidine
Group IA antiarrhythmic prototype: used in atrial and ventricular arrhythmias. Tox: cinchonism, GI upset, thrombocytopenic purpura, arrhythmogenic
178
Quinine
Antimalarial: blood schizonticide; no effect on liver stages. Isomer of quinidine, same toxicity
179
Ranitidine
H2 blocker: like cimetidine but less inhibition of hepatic drug metabolism; no antiandrogenic effects
180
Reserpine
Antihypertensive: selective inhibitor of vesicle catecholamine/H+ antiporter; used in HTN, causes depletion of catecholamines and 5 HT from their stores. Tox: severe depression, suicide, ulcers
181
Rifampin
Antimicrobial: inhibitor of DNA dependent RNA polymerase used in drug regimens for tuberculosis and the meningococcal carrier state. Tox: hepatic dysfunction, induction of liver drug metabolizing enzymes (drug interactions), flu like syndrome with intermittent dosing
182
Risperidone, olanzapine, sertindole
Newer atypical antipsychotics. Higher potency, more blocking of 5 HT2 receptors than older antipsychotic agents. Low extrapyramidal toxicity.
183
Selegiline
MAO B inhibitor: selective inhibitor of the enzyme that metabolizes dopamine (no tyramine interactions). Used in parkinsonism as adjunct
184
Sildenafil
Viagra. Blocks phosphodiesterase that splits cGMP; enhanced smooth muscle relaxation causes erection. Important interaction with nitrates.
185
Streptokinase
Thrombolytic: protein from streptococci that accelerates plasminogen to plasmin conversion. Tox: bleeding, allergy
186
Succimer (DMSA)
Chelator: dimercaptosuccinic acid; used to chelate lead and arsenic
187
Succinylcholine
Depolarizing neuromuscular relaxant prototype: short duration (5 min) if patient has normal plasma cholinesterase (genetically determined). No antidote (compare with tubocurarine)
188
Sumatriptan, other " triptans"
5 HT1D receptor agonists: used to abort migraine attacks
189
Tamoxifen, raloxifen
Estrogen partial agonists "selective estrogen receptor modulators": used in breast carcinoma, osteoporosis
190
Tetracaine
Local anesthetic: long acting ester prototype
191
Tetracycline
Antibiotic: tetracycline prototype; bacteriostatic inhibitor of protein synthesis (30S). Broad spectrum, but many resistant organisms. Used for Lyme disease, mycoplasmal, chlamydial, rickettsial infections, chronic bronchitis, acne, cholera; a back up drug in syphilis. Tox: GI upset and superinfections (Candida, staphylococci), antianabolic actions, Fanconi's syndrome (outdated drug), photosensitivity, dental enamel dysplasia
192
Tetrodotoxin
Toxin: very potent sodium channel blocker; blocks action potential propagation in nerve, heart, and skeletal muscle. From puffer fish, California newt. Tox: paresthesias, paralysis
193
Thiazides
Diuretic prototype: block Na+/Cl transporter in distal convoluted tubule; used in HTN, CHF, chronic stone formers. Tox: K+ wasting; increased serum lipids, uric acid, and glucose
194
Thioridazine
Antipsychotic phenothiazine: blocks most dopamine receptors in the CNS. Tox: atropine like effects (marked), ECG abnormalities, postural hypotension, retinal pigmentation, sedation, additive effects with other CNS depressants (but less EPS dysfunction than other phenothiazines)
195
Thyroxine, triiodothyronine
Major hormones produced by the thyroid: stimulate metabolism, growth, and development
196
Ticarcillin
Extended spectrum penicillin active against selected gram negative bacteria including Pseudomonas aeruginosa (synergistic with aminoglycosides). Susceptible to penicillinases unless used with clavulanic acid. Tox: penicillin allergy
197
Ticlopidine, clopidogrel
Newer antiplatelet agents. Used to prevent strokes, postangioplasty occlusion.
198
Tolbutamide, tolazamide, chlorpropamide, acetohexamide
Oral hypoglycemics: older sulfonylurea group. (See glipizide.) Chlorpropamide has longest duration of action
199
Trimethoprim sulfamethoxazole
Antimicrobial drug combination: causes synergistic sequential blockade of folic acid synthesis. Active against many gram negative bacteria including Aeromonas, Enterobacter, H influenzae, Klebsiella, Moraxella, Salmonella, Serratia, Shigella. Possible back up agent for methicillin resistant staphylococci. Tox: mainly due to sulfonamide; includes hypersensitivity, hematotoxicity, kernicterus, and drug interactions due to competition for plasma protein binding
200
Tubocurarine
Nondepolarizing neuromuscular blocking agent prototype: competitive nicotinic blocker. Releases histamine and may cause hypotension. Analogues: pancuronium, atracurium, vecuronium, and other " curiums" and " curoniums." Antidote: cholinesterase inhibitor, eg, neostigmine
201
Tyramine
Indirectly acting sympathomimetic prototype: releases or displaces norepinephrine from stores in nerve endings. Usually inactive by the oral route because of high first pass effect but will cause potentially lethal hypertensive responses in patients taking MAO inhibitors
202
Valproic acid
Anticonvulsant: used in absence, clonic tonic, and myoclonic seizure states, migraine prophylactic. Tox: GI distress, hepatic necrosis (rare), teratogenic (spina bifida); inhibits drug metabolism
203
Vancomycin
Glycopeptide bactericidal antibiotic: inhibits synthesis of cell wall precursor molecules. Drug of choice for methicillin resistant staphylococci and effective in antibiotic induced colitis. Dose reduction required in renal impairment (or hemodialysis). Tox: ototoxicity, hypersensitivity, renal dysfunction (rare)
204
Verapamil
Calcium channel blocker prototype: blocks "L type" channels; cardiac depressant and vasodilator; used in HTN, angina, and arrhythmias. Tox: AV block, CHF, constipation
205
Vesamicol
Inhibitor of vesicle ACh/H+ antiporter in cholinergic nerve endings: prevents storage of ACh. No clinical applications
206
Vincristine
Antineoplastic plant alkaloid: cell cycle (M phase) specific agent; inhibits mitotic spindle formation. Tox: peripheral neuropathy. Compare with vinblastine, a congener that causes myelosuppression
207
Warfarin
Oral anticoagulant prototype: causes synthesis of nonfunctional versions of the vitamin K dependent clotting factors (II, VII, IX, X). Tox: bleeding, teratogenic. Antidote: vitamin K, fresh plasma
208
Zanamivir, oseltamivir
Neuraminidase inhibitors that can be used to reduce severity and duration of influenza symptoms. Prevents penetration of the virion.
209
Zidovudine (AZT)
Antiviral: prototype nucleoside inhibitor of HIV reverse transcriptase (NRTI). Tox: severe myelosuppression. Others: lamivudine, stavudine, didanosine, zalcitabine.
210
Zolpidem
Non benzodiazepine hypnotic, acts via the BDZ1 (omega1) receptor subtype and is reversed by flumazenil; less amnesia and muscle relaxation; lower dependence liability
211
-azole
ergosterol synthesis inhibitor (ex. ketaconazole)
212
-bendazole
antiparasitic/antihelmintic (mebendazole)
213
-cillin
peptidoglycan synthesis inhibitor (ex. penicillin)
214
-cycline
protein synthesis inhibitor (ex. tetracycline)
215
-ivir
neuraminidase inhibitor (ex. oseltamivir)
216
-navir
protease inhibitor (ex. ritonavir)
217
-ovir
DNA Polymerase inhibitor (ex. acyclovir)
218
-thromycin
macrolide antibiotic (ex. azithromycin)
219
-ane
inhalational general anesthetic (ex. halothane)
220
-azine
```
typical antipsychotic (ex. thioridazine)
- block D2 receptors --> increase in cAMP
```
221
-barbital
barbituate (ex. phenobarbitol)
- faciliatate GABA-A function by increasing duration of Cl- channel opening --> decreases neuron firing (increase duration)
222
-caine
```
local anesthetic (ex. novacaine)
- block Na+ channels by binding to specific receptors on inner portion of channel. Preferentially bind to active Na+ channels. Tertiary amines penetrate membrane in uncharged form and then bind ion channels in charged form
```
223
-etine
SSRI (ex. Fluoxetine)
| - 5-HT specific reuptake inhibitors
224
-ipramine/-triptyline
TCA (ex. Imipramine)
| - Block reuptake of NE and 5-HT
225
-triptan
5-HT IB/ID agonists (ex. sumatriptan)
226
-zepam/-zolam
Benzodiazepines (ex. Diazepam, Alprazolam)
| - Facilitate GABA-A action by increasing frequency of Cl- channel opening
227
- chol
Cholinergic agonist (ex. bethanochol)
228
-curium/-curonium
Non-depolarizing paralytic (ex. atracurium)
229
-olol
Beta blocker (ex. propranolol)
230
-stigmine
AChE Inhibitor (ex. neostigmine)
231
-terol
B2 agonist (ex. albuterol)
232
-zosin
Alpha 1 antagonist (ex. prazosin)
233
-afil
PDE-5 Inhibitor (ex. sildenafil)
234
-dipine
```
Dihydropyridine CCB (ex. Amlodipine)
- block voltage-dependent L-type channels of cardiac and smooth muscle --> reduced muscle contractility
```
235
-pril
ACE Inhibitor (ex. captropril)
236
-sartan
ANG-II receptor blocker (ex. losartan)
237
-statin
HMG-COA reductase inhibitor (ex. atorvostatin)
238
-dronate
Bisphosphonate (ex. alendronate)
| - Pyrophosphate analogs; bind hydroxyapatite in bone, inhibiting osteoclast activity
239
-glitazone
PPAR-Gamma activator (ex.rosiglitazone)
240
-prazole
Proton pump inhibitor (ex. omeprazole)
241
-prost
Prostaglandin analog (Latanoprost)
242
-tidine
H2-antagonist (ex.cimetidine)
| - reversible block of H2-receptors --> decreased H+ secretion from parietal cells
243
-tropin
Pituitary hormone (ex. somatotropin)
244
-ximab
Chimeric monoclonal antibody (ex. basiliximab)
245
-zumab
Humanized monoclonal antibody (ex. daclizumab)
246
-limus
```
Binds FKBP (ex. tracrolimus)
- blocks T cell activation by preventing IL-2 transcription
```
