Katzung Flashcards
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Abciximab
Abciximab,Monoclonal antibody to fibrin receptor (glycoprotein IIb/IIIa) on platelets. Used to prevent clotting after coronary angioplasty
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Acetaminophen
Acetaminophen,Antipyretic analgesic: very weak cyclooxygenase inhibitor; not anti−inflammatory. Less toxic than aspirin but more dangerous in overdose (causes hepatic necrosis−antidote: acetylcysteine)
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Acetazolamide dorzolamide
Acetazolamide, dorzolamide,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
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Acetylcholine
Acetylcholine,Cholinomimetic prototype: transmitter in CNS, ENS, all ANS ganglia, parasympathetic postganglionic synapses, sympathetic postganglionic fibers to sweat glands, and some skeletal muscle vasodilator synapses
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Acyclovir
Acyclovir,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
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Adenosine
Adenosine,Antiarrhythmic: unclassified (“Group V”); parenteral only. Hyperpolarizes AV nodal tissue, blocks conduction for 10−15 sec. Used for nodal reentry arrhythmias
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Allopurinol
Allopurinol,Antigout: inhibitor of xanthine oxidase; reduces production of uric acid
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Albuterol, metaproterenol, terbutaline
Albuterol, metaproterenol, terbutaline,Important β2−agonists; used mainly for asthma.
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Alprazolam
Alprazolam,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
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Alteplase (rt−PA)
Alteplase (rt−PA),Thrombolytic: human recombinant tissue plasminogen activator. Used in acute MI to recanalize the occluded coronary. Occasionally used in pulmonary embolism, stroke. Tox: bleeding
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Amiloride
Amiloride,K+−sparing diuretic: blocks Na+ channels in cortical collecting tubules
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Aminoglutethimide
Aminoglutethimide,Nonsteroid inhibitor of steroid synthesis: reduces conversion of cholesterol to the hormone precursor, pregnenolone. Used in metastatic breast cancer
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Amiodarone
Amiodarone,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
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Amitriptyline
Amitriptyline,Tricyclic antidepressant: blocks reuptake of norepinephrine and serotonin. Tox: atropine− like, postural hypotension, sedation; cardiac arrhythmias in overdose, additive effects with other CNS depressants
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Amoxicillin
Amoxicillin,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
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Amphetamine
Amphetamine,Indirectly acting sympathomimetic: displaces stored catecholamines in nerve endings. Marked CNS stimulant actions; high abuse liability. Tox: psychosis, HTN, MI, seizures
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Amphotericin B
Amphotericin B,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)
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Ampicillin
Ampicillin,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
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Anistreplase (APSAC)
Anistreplase (APSAC),Thrombolytic: bacterial streptokinase complexed with human plasminogen. Longer acting in body than other thrombolytics (rt−PA, streptokinase, urokinase). Tox: bleeding, allergy to streptococcal protein
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Aspirin
Aspirin,NSAID prototype: inhibits cyclooxygenase (COX) I and II irreversibly. Potent antiplatelet agent as well as antipyretic analgesic anti−inflammatory drug
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Atenolol
Atenolol,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])
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Atropine
Atropine,Muscarinic cholinoceptor blocker prototype: lipid soluble, CNS effects. Tox: “red as a beet, dry as a bone, mad as a hatter,” urinary retention, mydriasis
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Azithromycin
Azithromycin,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
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Baclofen
Baclofen,GABA analog, orally active: spasmolytic; activates GABAB receptors in the spinal cord
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Benztropine
Benztropine,Centrally acting antimuscarinic prototype for parkinsonism
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Bethanechol
Bethanechol,Muscarinic agonist: choline ester with good resistance to cholinesterase; used for atonic bowel or bladder
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Botulinum
Botulinum,Toxin: enzyme produced by Clostridium botulinum; interacts with fusion/docking proteins to block release of acetylcholine vesicles
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Bromocriptine
Bromocriptine,Ergot derivative: dopamine agonist in CNS; inhibits prolactin release. Used in parkinsonism and hyperprolactinemia. Tox: CNS, dyskinesias, hypotension
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Bupivacaine
Bupivacaine,Long−acting amide local anesthetic prototype: greater CV toxicity than most local anesthetics
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Buspirone
Buspirone,Anxiolytic: atypical drug that interacts with 5HT1A receptors; slow onset. Minimal potentiation of CNS depressants including ethanol; negligible abuse liability
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Captopril
Captopril,ACE inhibitor prototype: used in HTN, diabetic renal disease, and CHF. Tox: hyperkalemia, fetal renal damage, cough (“sore throat”)
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Carbachol
Carbachol,Nonselective muscarinic and nicotinic agonist: choline ester with good resistance to cholinesterase; used for glaucoma (not a first−line drug)
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Carbamazepine
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
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Cefazolin
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
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Cefoxitin
Cefoxitin,Second−generation cephalosporin: active against a wide spectrum of gram−negative bacteria including anaerobes (B fragilis). Does not enter the CNS
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Ceftriaxone
Ceftriaxone,Third−generation cephalosporin: active against resistant bacteria including gonococci, H influenzae, and other gram−negative organisms. Crosses the blood−brain barrier
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Celecoxib
Celecoxib, rofecoxib,First COX−II−selective NSAIDs. Reduced GI toxicity
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Chloramphenicol
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
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Chloroquine
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
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Chlorpheniramine
Chlorpheniramine,Antihistamine H1 blocker prototype: Tox: sedation, antimuscarinic
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Chlorpromazine
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
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Cholestyramine
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
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Cimetidine
Cimetidine,H2 blocker prototype: used in acid−peptic disease. Tox: inhibits hepatic drug metabolism; antiandrogen effects. Less toxic analogs: ranitidine, famotidine, nizatidine
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Ciprofloxacin
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
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Cisplatin
Cisplatin,Platinum−containing alkylating cancer chemotherapeutic agent. Used for several solid tumors (eg, testes, lung). Carboplatin is similar.
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Clindamycin
Clindamycin,Lincosamide antibiotic: bacteriostatic inhibitor of protein synthesis (50S); active against gram−positive cocci, B fragilis. Tox: GI distress, pseudomembranous colitis
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Clomiphene
Clomiphene,Estrogen partial agonist: synthetic used in infertility to induce ovulation
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Clonidine
Clonidine,Alpha2 agonist: acts centrally to reduce SANS outflow, lowers BP. Tox: rebound HTN if stopped suddenly
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Clozapine
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)
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Cocaine
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
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Colchicine
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
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Cyclopentolate
Cyclopentolate, tropicamide,Antimuscarinics for ophthalmology: shorter duration than atropine (a few hours or less); cause cycloplegia and mydriasis
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Cyclophosphamide
Cyclophosphamide,Antineoplastic, immunosuppressive: cell cycle−nonspecific alkylating agent. Tox: alopecia, gastrointestinal distress, hemorrhagic cystitis, myelosuppression
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Cyclosporine
Cyclosporine,Immunosuppressant: antibiotic; inhibits interleukin−2 synthesis, suppresses T cells. Tox: HTN, hirsutism, nephrotoxicity (dose−limiting), seizures (in overdose). Not a myelosuppressant
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Dantrolene
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
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DDAVP
DDAVP,ADH analog: synthetic peptide used for pituitary diabetes insipidus
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DDT
DDT,Insecticide: prevents inactivation of sodium channels, causes uncontrolled neuronal activity. Stored for years in body fat in mammals, birds, fish
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Deferoxamine
Deferoxamine,Chelator: bacterial product; chelates iron very avidly, aluminum less so
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Dexfenfluramine
Dexfenfluramine,5−HT reuptake inhibitor and receptor agonist previously used as anorexic. Tox: produced cardiac valve damage when used in combination with phentermine
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Dexamethasone
Dexamethasone,Glucocorticoid: very potent, long−acting; no mineralocorticoid activity
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Diazepam
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
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Didanosine (DDI)
Didanosine (DDI),Antiviral: nucleoside inhibitor of HIV reverse transcriptase. Tox: peripheral neuropathy, pancreatitis
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Digitoxin
Digitoxin,Cardiac glycoside: half−life 168 h, excreted in the bile (partially as digoxin); subject to enterohepatic circulation. See digoxin
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Digoxin
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
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Diltiazem
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
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Dimercaprol (BAL)
Dimercaprol (BAL),Chelator (British AntiLewisite): used for arsenic, lead, and mercury poisoning
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Dioxin (TCDD)
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
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Diphenhydramine
Diphenhydramine,Antihistamine H1 blocker prototype: used in hayfever, motion sickness, dystonias. Tox: antimuscarinic, anti−alpha, sedative
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Disopyramide
Disopyramide,Group IA antiarrhythmic: used for ventricular arrhythmias. Tox: strong antimuscarinic; may cause CHF
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Dopamine
Dopamine,Neurotransmitter and agonist drug at dopamine receptors: used in shock to increase renal blood flow, stimulate heart
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Doxorubicin
Doxorubicin,Antineoplastic: anthracycline drug (cell cycle−nonspecific); intercalates between base pairs to disrupt DNA functions and forms cytotoxic free radicals. Tox: cardiotoxicity, myelosuppression
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Doxycycline
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
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Echothiophate
Echothiophate,Organophosphate cholinesterase inhibitor: less lipid soluble than most organophosphates; used in glaucoma
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Edetate (EDTA)
Edetate (EDTA),Chelating agent: used in lead poisoning. Tox: renal tubular necrosis
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Edrophonium
Edrophonium,Cholinesterase inhibitor: very short duration of action (15 min). Used to reverse NM blockade and as diagnostic test in myasthenia gravis
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Enoxaparin
Enoxaparin,Low molecular weight heparin. Primary effect is anti−factor X. Other low molecular weight heparin−like products: dalteparin, danaparoid. Tox: bleeding
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Ephedrine
Ephedrine,Indirectly acting sympathomimetic: like amphetamine but less CNS stimulation, more smooth muscle effects
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Epinephrine
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
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Ergonovine
Ergonovine,Ergot alkaloid: uterine effect prototype, causes prolonged uterine contraction. Used in post−partum bleeding
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Ergotamine
Ergotamine,Ergot alkaloid: vascular effect prototype, causes prolonged vasoconstriction, uterine contraction. Used in migraine, obstetrics
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Erythromycin
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
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Ethacrynic acid
Ethacrynic acid,Loop diuretic: not a sulfa derivative. Tox: like furosemide but does not increase serum uric acid.
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Ethanol
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
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Ethosuximide
Ethosuximide,Anticonvulsant: used in absence seizures; may block T−type Ca2+ channels in thalamic neurons. Tox: GI distress but safe in pregnancy
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Etidronate
Etidronate, pamidronate, alendronate,Bisphosphonates: reduce turnover of bone calcium. Used in Paget’s disease, osteoporosis; alendronate increases bone formation. Tox: severe esophageal ulceration
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Fexofenadine
Fexofenadine,2nd generation antihistamine; does not enter CNS, little or no sedation
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Finasteride
Finasteride,Steroid inhibitor of 5α−reductase: inhibits synthesis of dihydrotestosterone, the active androgen in prostate. Used in BPH
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Flecainide
Flecainide,Group IC antiarrhythmic prototype: used in ventricular tachycardia and rapid atrial arrhythmias with Wolff−Parkinson−White syndrome. Tox: arrhythmogenic, CNS excitation
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Fluconazole
Fluconazole,Imidazole antifungal: used for esophageal candidiasis and in coccidioidomycoses; high CSF levels provide prophylaxis versus fungal meningitis in immunosuppressed patients
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Fludrocortisone
Fludrocortisone,Synthetic corticosteroid: high mineralocorticoid and moderate glucocorticoid activity; long duration of action
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Flumazenil
Flumazenil,Benzodiazepine receptor antagonist: used to reverse CNS depressant effects of benzodiazepines (overdose or when used in anesthesia)
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Fluorouracil
Fluorouracil,Antineoplastic: pyrimidine antimetabolite (cell cycle−specific) causes “thymine−less” cell death; used mainly for solid or superficial tumors. Tox: GI distress, myelosuppression
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Fluoxetine
Fluoxetine,Antidepressant: serotonin selective reuptake inhibitor (SSRI) prototype. Less ANS adverse effects and cardiotoxic potential than tricyclics. Tox: CNS stimulation, seizures in overdose
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Flutamide
Flutamide,Androgen receptor inhibitor: nonsteroid used in prostatic carcinoma
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Furosemide
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
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Foscarnet
Foscarnet,Antiviral: effective against CMV and HSV (including TK− strains); Tox: electrolyte imbalance, nephrotoxicity
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Ganciclovir
Ganciclovir,Antiviral: effective against CMV; requires bioactivation via thymidine kinase. Tox: myelosuppression, nephrotoxicity
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Gemfibrozil, clofibrate
Gemfibrozil, clofibrate,Antilipemics: stimulate lipoprotein lipase in peripheral tissues. Used in hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia
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Gentamicin
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
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Glipizide, glyburide
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
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Glucagon
Glucagon,Hormone product of pancreatic A cells. Increases blood sugar via increased cAMP
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Guanethidine
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
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Haloperidol
Haloperidol,Antipsychotic butyrophenone: blocks brain dopamine D2 receptors. Tox: marked EPS dysfunction, hyperprolactinemia; less ANS adverse effects than phenothiazines
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Halothane
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
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Heparin
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
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Hydralazine
Hydralazine,Antihypertensive: arteriolar vasodilator, orally active; used in HTN, CHF. Tox: Tachycardia, salt and water retention, lupus−like syndrome
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Hydrochlorothiazide
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
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Ibuprofen
Ibuprofen,NSAID prototype: short duration. Inhibits cyclooxygenase (both I and II) reversibly. Used in arthritis, dysmenorrhea, muscle inflammation. Tox: peptic ulcer, renal damage
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Imipenem
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)
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Imipramine
Imipramine,Tricyclic antidepressant prototype: blocks reuptake of norepinephrine and serotonin. Tox: ANS (alpha and muscarinic) blockade, cardiac arrhythmias
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Indinavir
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
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Indomethacin
Indomethacin,NSAID prototype: highly potent. Usually reserved for acute inflammation (eg, acute gout), not chronic; neonatal patent ductus arteriosus. Tox: GI (bleeding), renal damage
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Insulin
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
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Interferon−α
Interferon−α,Important cytokine for the treatment of hepatitis B and C infection.
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Ipodate
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
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Ipratropium
Ipratropium,Antimuscarinic agent: aerosol for asthma, COPD. Good bronchodilator in 20−30% of patients. Not as effective as β2 agonists
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Isoniazid
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)
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Isoproterenol
Isoproterenol,Beta1, beta2 agonist catecholamine prototype: bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR. Tox: arrhythmias, angina
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Ketoconazole
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
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Labetalol
Labetalol,Alpha− and beta−blocker: used in HTN. Tox: AV block, hypotension
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Leuprolide
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
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Levodopa
Levodopa,Dopamine precursor: used in parkinsonism, usually combined with carbidopa (a peripheral inhibitor of dopamine metabolism). Tox: dyskinesias, hypotension, on−off phenomena, behavioral changes
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Lidocaine
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
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Lithium
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)
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Lovastatin
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
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LSD
LSD,Lysergic acid diethylamide, “Acid:” semisynthetic ergot derivative; orally active; hallucinogen
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Malathion
Malathion,Organophosphate insecticide cholinesterase inhibitor: pro−drug converted to malaoxon. Less toxic in mammals and birds because metabolized to inactive products
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Meperidine
Meperidine,Opioid analgesic: synthetic, equivalent to morphine in efficacy, but orally bioavailable. Strong agonist at mu opioid receptors; blocks muscarinic receptors. Tox: see morphine
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Mestranol
Mestranol,Synthetic estrogen: used in many oral contraceptives
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Metformin, phenformin
Metformin, phenformin,Oral biguanide hypoglycemics: mechanism not understood, different from sulfonylurea oral hypoglycemics. Some efficacy in the absence of functioning pancreatic B cells
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Methadone
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
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Methotrexate
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
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Methyldopa
Methyldopa,Antihypertensive: prodrug of methylnorepinephrine, a CNS−active α2 agonist. Reduces SANS outflow from vasomotor center. Tox: positive Coombs test, hemolysis
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Methysergide
Methysergide,Ergot alkaloid: used as prophylactic in migraine. Tox: retroperitoneal and subendocardial fibroplasia
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Metoprolol
Metoprolol,Beta1−selective blocker: used in HTN and for prevention of post−MI sudden death arrhythmias
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Metronidazole
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
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Mexiletine
Mexiletine,Group IB antiarrhythmic drug: like lidocaine but orally active
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Mifepristone (RU 486)
Mifepristone (RU 486),Progesterone and glucocorticoid inhibitor: abortifacient, antineoplastic
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Minoxidil
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
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Misoprostol
Misoprostol,PGE1 derivative: orally active prostaglandin used to prevent peptic ulcers in patients taking NSAIDs for arthritis. Tox: diarrhea
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Morphine
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
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Nafcillin
Nafcillin,Penicillinase−resistant penicillin prototype: used for suspected or known staphylococcal infections; not active against methicillin−resistant staphylococci. Tox: penicillin allergy
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Nalbuphine
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
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Naloxone
Naloxone,Opioid mu receptor antagonist: used to reverse CNS depressant effects of opioid analgesics (overdose or when used in anesthesia)
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Neostigmine
Neostigmine,Cholinesterase inhibitor prototype: quaternary nitrogen carbamate with little CNS effect
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Nevirapine
Nevirapine,Prototype nonnucleoside inhibitor of HIV reverse transcriptase (NNRTI).Others : efavirenz, delavirdine
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Niacin
Niacin,Antilipemic: reduces release of VLDL from liver into circulation. Tox: flushing
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Nifedipine
Nifedipine,Calcium channel blocker prototype: vasoselective (less cardiac depression); used in angina, HTN. Tox: constipation, headache
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Nitroglycerin
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
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Norepinephrine
Norepinephrine,Adrenoceptor agonist prototype: acts at all alpha and at beta1 adrenoceptors; used as vasoconstrictor. Causes reflex bradycardia. Tox: ischemia, arrhythmias, HTN
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Norfloxacin
Norfloxacin,Fluoroquinolone antibiotic: inhibits bacterial DNA gyrase; active against many urinary pathogens including E coli, H influenzae, Klebsiella, Enterobacter, Pseudomonas, Serratia. Tox: see ciprofloxacin
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Norgestrel
Norgestrel,Progestin: used in many oral contraceptives and Norplant implantable contraceptive
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Olanzapine
Olanzapine,Atypical antipsychotic; high affinity antagonist at 5HT2A with minimal extrapyramidal side effects; improves both positive and negative symptoms of schizophrenia
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Omeprazole
Omeprazole,Antiulcer: irreversible blocker of H+/K+ ATPase proton pump in parietal cells of stomach. Used in Zollinger−Ellison syndrome, gastroesophageal reflux disease (GERD)
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Ondansetron, granisetron
Ondansetron, granisetron,5−HT3 receptor blockers: very important antiemetics for cancer chemotherapy; also used post−operatively to reduce vomiting
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Paraquat
Paraquat,Toxic herbicide: very small oral (but not inhaled) doses cause lethal pulmonary fibrosis
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Parathion
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)
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Penicillamine
Penicillamine,Chelator, immunomodulator: copper and sometimes lead, mercury, arsenic. Used in Wilson’s disease and rheumatoid arthritis
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Penicillin G
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
Katzung
Phenobarbital
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
Katzung
Phenoxybenzamine
Phenoxybenzamine,Alpha−blocker prototype: irreversible action. Used in pheochromocytoma
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Phentolamine
Phentolamine,Alpha−blocker prototype: reversible action. Used in pheochromocytoma
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Phenytoin
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
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Physostigmine
Physostigmine,Cholinesterase inhibitor prototype: alkaloid tertiary amine carbamate, enters eye and CNS readily. Used in glaucoma
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Pilocarpine
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
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Piroxicam
Piroxicam,NSAID with longest duration of action (t1/2 about 40 h)
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Pralidoxime
Pralidoxime,Acetylcholinesterase regenerator: very high affinity for phosphorus in organophosphates
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Prazosin, terazosin, doxazosin
Prazosin, terazosin, doxazosin,Alpha1−selective blockers: used in HTN. Tox: first−dose orthostatic hypotension
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Prednisone
Prednisone,Glucocorticoid prototype: potent, short−acting; much less mineralocorticoid activity than cortisol but more than dexamethasone or triamcinolone
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Probenecid
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
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Probucol
Probucol,Antilipemic: unknown mechanism; recently withdrawn but new evidence suggests efficacy in preventing restenosis of coronaries after angioplasty.Tox: causes arrhythmias
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Procainamide
Procainamide,Group IA antiarrhythmic drug: short half−life; similar to quinidine but may cause lupus erythematosus
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Propranolol
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
Katzung
Propylthiouracil
Propylthiouracil,Antithyroid drug prototype: reduces iodination of tyrosine and coupling of MIT and DIT in the thyroid; orally active. Tox: rash, agranulocytosis (rare)
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Prostacyclin
Prostacyclin,PGI2: prostaglandin vasodilator and inhibitor of platelet aggregation
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Pyridostigmine
Pyridostigmine,Cholinesterase inhibitor: long−acting (8 h) quaternary carbamate; used in myasthenia gravis
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Quinidine
Quinidine,Group IA antiarrhythmic prototype: used in atrial and ventricular arrhythmias. Tox: cinchonism, GI upset, thrombocytopenic purpura, arrhythmogenic
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Quinine
Quinine,Antimalarial: blood schizonticide; no effect on liver stages. Isomer of quinidine, same toxicity
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Ranitidine
Ranitidine,H2 blocker: like cimetidine but less inhibition of hepatic drug metabolism; no antiandrogenic effects
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Reserpine
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
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Rifampin
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
Katzung
Risperidone, olanzapine, sertindole
Risperidone, olanzapine, sertindole,Newer atypical antipsychotics. Higher potency, more blocking of 5−HT2 receptors than older antipsychotic agents. Low extrapyramidal toxicity.
Katzung
Selegiline
Selegiline,MAO−B inhibitor: selective inhibitor of the enzyme that metabolizes dopamine (no tyramine interactions). Used in parkinsonism as adjunct
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Sildenafil
Sildenafil,Viagra. Blocks phosphodiesterase that splits cGMP; enhanced smooth muscle relaxation causes erection. Important interaction with nitrates.
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Streptokinase
Streptokinase,Thrombolytic: protein from streptococci that accelerates plasminogen−to−plasmin conversion. Tox: bleeding, allergy
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Succimer (DMSA)
Succimer (DMSA),Chelator: dimercaptosuccinic acid; used to chelate lead and arsenic
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Succinylcholine
Succinylcholine,Depolarizing neuromuscular relaxant prototype: short duration (5 min) if patient has normal plasma cholinesterase (genetically determined). No antidote (compare with tubocurarine)
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Sumatriptan, other “− triptans”
Sumatriptan, other “− triptans”,5−HT1D receptor agonists: used to abort migraine attacks
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Tamoxifen, raloxifen
Tamoxifen, raloxifen,Estrogen partial agonists “selective estrogen receptor modulators”: used in breast carcinoma, osteoporosis
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Tetracaine
Tetracaine,Local anesthetic: long−acting ester prototype
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Tetracycline
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
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Tetrodotoxin
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
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Thiazides
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
Katzung
Thioridazine
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)
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Thyroxine, triiodothyronine
Thyroxine, triiodothyronine,Major hormones produced by the thyroid: stimulate metabolism, growth, and development
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Ticarcillin
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
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Ticlopidine, clopidogrel
Ticlopidine, clopidogrel,Newer antiplatelet agents. Used to prevent strokes, postangioplasty occlusion.
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Tolbutamide, tolazamide, chlorpropamide, acetohexamide
Tolbutamide, tolazamide, chlorpropamide, acetohexamide,Oral hypoglycemics: older sulfonylurea group. (See glipizide.) Chlorpropamide has longest duration of action
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Trimethoprim−sulfamethoxazole
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
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Tubocurarine
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
Katzung
Tyramine
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
Katzung
Valproic acid
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
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Vancomycin
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)
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Verapamil
Verapamil,Calcium channel blocker prototype: blocks “L−type” channels; cardiac depressant and vasodilator; used in HTN, angina, and arrhythmias. Tox: AV block, CHF, constipation
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Vesamicol
Vesamicol,Inhibitor of vesicle ACh/H+ antiporter in cholinergic nerve endings: prevents storage of ACh. No clinical applications
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Vincristine
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
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Warfarin
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
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Zanamivir
Zanamivir, oseltamivir,Neuraminidase inhibitors that can be used to reduce severity and duration of influenza symptoms. Prevents penetration of the virion.
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Zidovudine (AZT)
Zidovudine (AZT),Antiviral: prototype nucleoside inhibitor of HIV reverse transcriptase (NRTI). Tox: severe myelosuppression. Others: lamivudine, stavudine, didanosine, zalcitabine.
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Zolpidem
Zolpidem,Non−benzodiazepine hypnotic, acts via the BDZ1 (omega1) receptor subtype and is reversed by flumazenil; less amnesia and muscle relaxation; lower dependence liability
