Katzung Flashcards
1
Q
Katzung
Abciximab
A
Abciximab,Monoclonal antibody to fibrin receptor (glycoprotein IIb/IIIa) on platelets. Used to prevent clotting after coronary angioplasty
2
Q
Katzung
Acetaminophen
A
Acetaminophen,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
Katzung
Acetazolamide dorzolamide
A
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
4
Q
Katzung
Acetylcholine
A
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
5
Q
Katzung
Acyclovir
A
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
6
Q
Katzung
Adenosine
A
Adenosine,Antiarrhythmic: unclassified (“Group V”); parenteral only. Hyperpolarizes AV nodal tissue, blocks conduction for 10−15 sec. Used for nodal reentry arrhythmias
7
Q
Katzung
Allopurinol
A
Allopurinol,Antigout: inhibitor of xanthine oxidase; reduces production of uric acid
8
Q
Katzung
Albuterol, metaproterenol, terbutaline
A
Albuterol, metaproterenol, terbutaline,Important β2−agonists; used mainly for asthma.
9
Q
Katzung
Alprazolam
A
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
10
Q
Katzung
Alteplase (rt−PA)
A
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
11
Q
Katzung
Amiloride
A
Amiloride,K+−sparing diuretic: blocks Na+ channels in cortical collecting tubules
12
Q
Katzung
Aminoglutethimide
A
Aminoglutethimide,Nonsteroid inhibitor of steroid synthesis: reduces conversion of cholesterol to the hormone precursor, pregnenolone. Used in metastatic breast cancer
13
Q
Katzung
Amiodarone
A
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
14
Q
Katzung
Amitriptyline
A
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
15
Q
Katzung
Amoxicillin
A
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
16
Q
Katzung
Amphetamine
A
Amphetamine,Indirectly acting sympathomimetic: displaces stored catecholamines in nerve endings. Marked CNS stimulant actions; high abuse liability. Tox: psychosis, HTN, MI, seizures
17
Q
Katzung
Amphotericin B
A
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)
18
Q
Katzung
Ampicillin
A
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
19
Q
Katzung
Anistreplase (APSAC)
A
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
20
Q
Katzung
Aspirin
A
Aspirin,NSAID prototype: inhibits cyclooxygenase (COX) I and II irreversibly. Potent antiplatelet agent as well as antipyretic analgesic anti−inflammatory drug
21
Q
Katzung
Atenolol
A
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])
22
Q
Katzung
Atropine
A
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
23
Q
Katzung
Azithromycin
A
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
24
Q
Katzung
Baclofen
A
Baclofen,GABA analog, orally active: spasmolytic; activates GABAB receptors in the spinal cord
25
# Katzung
Benztropine
Benztropine,Centrally acting antimuscarinic prototype for parkinsonism
26
# Katzung
Bethanechol
Bethanechol,Muscarinic agonist: choline ester with good resistance to cholinesterase; used for atonic bowel or bladder
27
# Katzung
Botulinum
Botulinum,Toxin: enzyme produced by Clostridium botulinum; interacts with fusion/docking proteins to block release of acetylcholine vesicles
28
# Katzung
Bromocriptine
Bromocriptine,Ergot derivative: dopamine agonist in CNS; inhibits prolactin release. Used in parkinsonism and hyperprolactinemia. Tox: CNS, dyskinesias, hypotension
29
# Katzung
Bupivacaine
Bupivacaine,Long−acting amide local anesthetic prototype: greater CV toxicity than most local anesthetics
30
# Katzung
Buspirone
Buspirone,Anxiolytic: atypical drug that interacts with 5HT1A receptors; slow onset. Minimal potentiation of CNS depressants including ethanol; negligible abuse liability
31
# Katzung
Captopril
Captopril,ACE inhibitor prototype: used in HTN, diabetic renal disease, and CHF. Tox: hyperkalemia, fetal renal damage, cough ("sore throat")
32
# Katzung
Carbachol
Carbachol,Nonselective muscarinic and nicotinic agonist: choline ester with good resistance to cholinesterase; used for glaucoma (not a first−line drug)
33
# Katzung
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
34
# Katzung
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
35
# Katzung
Cefoxitin
Cefoxitin,Second−generation cephalosporin: active against a wide spectrum of gram−negative bacteria including anaerobes (B fragilis). Does not enter the CNS
36
# Katzung
Ceftriaxone
Ceftriaxone,Third−generation cephalosporin: active against resistant bacteria including gonococci, H influenzae, and other gram−negative organisms. Crosses the blood−brain barrier
37
# Katzung
Celecoxib
Celecoxib, rofecoxib,First COX−II−selective NSAIDs. Reduced GI toxicity
38
# Katzung
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
39
# Katzung
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
40
# Katzung
Chlorpheniramine
Chlorpheniramine,Antihistamine H1 blocker prototype: Tox: sedation, antimuscarinic
41
# Katzung
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
42
# Katzung
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
43
# Katzung
Cimetidine
Cimetidine,H2 blocker prototype: used in acid−peptic disease. Tox: inhibits hepatic drug metabolism; antiandrogen effects. Less toxic analogs: ranitidine, famotidine, nizatidine
44
# Katzung
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
45
# Katzung
Cisplatin
Cisplatin,Platinum−containing alkylating cancer chemotherapeutic agent. Used for several solid tumors (eg, testes, lung). Carboplatin is similar.
46
# Katzung
Clindamycin
Clindamycin,Lincosamide antibiotic: bacteriostatic inhibitor of protein synthesis (50S); active against gram−positive cocci, B fragilis. Tox: GI distress, pseudomembranous colitis
47
# Katzung
Clomiphene
Clomiphene,Estrogen partial agonist: synthetic used in infertility to induce ovulation
48
# Katzung
Clonidine
Clonidine,Alpha2 agonist: acts centrally to reduce SANS outflow, lowers BP. Tox: rebound HTN if stopped suddenly
49
# Katzung
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)
50
# Katzung
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
51
# Katzung
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
52
# Katzung
Cyclopentolate
Cyclopentolate, tropicamide,Antimuscarinics for ophthalmology: shorter duration than atropine (a few hours or less); cause cycloplegia and mydriasis
53
# Katzung
Cyclophosphamide
Cyclophosphamide,Antineoplastic, immunosuppressive: cell cycle−nonspecific alkylating agent. Tox: alopecia, gastrointestinal distress, hemorrhagic cystitis, myelosuppression
54
# Katzung
Cyclosporine
Cyclosporine,Immunosuppressant: antibiotic; inhibits interleukin−2 synthesis, suppresses T cells. Tox: HTN, hirsutism, nephrotoxicity (dose−limiting), seizures (in overdose). Not a myelosuppressant
55
# Katzung
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
56
# Katzung
DDAVP
DDAVP,ADH analog: synthetic peptide used for pituitary diabetes insipidus
57
# Katzung
DDT
DDT,Insecticide: prevents inactivation of sodium channels, causes uncontrolled neuronal activity. Stored for years in body fat in mammals, birds, fish
58
# Katzung
Deferoxamine
Deferoxamine,Chelator: bacterial product; chelates iron very avidly, aluminum less so
59
# Katzung
Dexfenfluramine
Dexfenfluramine,5−HT reuptake inhibitor and receptor agonist previously used as anorexic. Tox: produced cardiac valve damage when used in combination with phentermine
60
# Katzung
Dexamethasone
Dexamethasone,Glucocorticoid: very potent, long−acting; no mineralocorticoid activity
61
# Katzung
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
62
# Katzung
Didanosine (DDI)
Didanosine (DDI),Antiviral: nucleoside inhibitor of HIV reverse transcriptase. Tox: peripheral neuropathy, pancreatitis
63
# Katzung
Digitoxin
Digitoxin,Cardiac glycoside: half−life 168 h, excreted in the bile (partially as digoxin); subject to enterohepatic circulation. See digoxin
64
# Katzung
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
65
# Katzung
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
66
# Katzung
Dimercaprol (BAL)
Dimercaprol (BAL),Chelator (British AntiLewisite): used for arsenic, lead, and mercury poisoning
67
# Katzung
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
68
# Katzung
Diphenhydramine
Diphenhydramine,Antihistamine H1 blocker prototype: used in hayfever, motion sickness, dystonias. Tox: antimuscarinic, anti−alpha, sedative
69
# Katzung
Disopyramide
Disopyramide,Group IA antiarrhythmic: used for ventricular arrhythmias. Tox: strong antimuscarinic; may cause CHF
70
# Katzung
Dopamine
Dopamine,Neurotransmitter and agonist drug at dopamine receptors: used in shock to increase renal blood flow, stimulate heart
71
# Katzung
Doxorubicin
Doxorubicin,Antineoplastic: anthracycline drug (cell cycle−nonspecific); intercalates between base pairs to disrupt DNA functions and forms cytotoxic free radicals. Tox: cardiotoxicity, myelosuppression
72
# Katzung
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
73
# Katzung
Echothiophate
Echothiophate,Organophosphate cholinesterase inhibitor: less lipid soluble than most organophosphates; used in glaucoma
74
# Katzung
Edetate (EDTA)
Edetate (EDTA),Chelating agent: used in lead poisoning. Tox: renal tubular necrosis
75
# Katzung
Edrophonium
Edrophonium,Cholinesterase inhibitor: very short duration of action (15 min). Used to reverse NM blockade and as diagnostic test in myasthenia gravis
76
# Katzung
Enoxaparin
Enoxaparin,Low molecular weight heparin. Primary effect is anti−factor X. Other low molecular weight heparin−like products: dalteparin, danaparoid. Tox: bleeding
77
# Katzung
Ephedrine
Ephedrine,Indirectly acting sympathomimetic: like amphetamine but less CNS stimulation, more smooth muscle effects
78
# Katzung
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
79
# Katzung
Ergonovine
Ergonovine,Ergot alkaloid: uterine effect prototype, causes prolonged uterine contraction. Used in post−partum bleeding
80
# Katzung
Ergotamine
Ergotamine,Ergot alkaloid: vascular effect prototype, causes prolonged vasoconstriction, uterine contraction. Used in migraine, obstetrics
81
# Katzung
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
82
# Katzung
Ethacrynic acid
Ethacrynic acid,Loop diuretic: not a sulfa derivative. Tox: like furosemide but does not increase serum uric acid.
83
# Katzung
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
84
# Katzung
Ethosuximide
Ethosuximide,Anticonvulsant: used in absence seizures; may block T−type Ca2+ channels in thalamic neurons. Tox: GI distress but safe in pregnancy
85
# Katzung
Etidronate
Etidronate, pamidronate, alendronate,Bisphosphonates: reduce turnover of bone calcium. Used in Paget's disease, osteoporosis; alendronate increases bone formation. Tox: severe esophageal ulceration
86
# Katzung
Fexofenadine
Fexofenadine,2nd generation antihistamine; does not enter CNS, little or no sedation
87
# Katzung
Finasteride
Finasteride,Steroid inhibitor of 5α−reductase: inhibits synthesis of dihydrotestosterone, the active androgen in prostate. Used in BPH
88
# Katzung
Flecainide
Flecainide,Group IC antiarrhythmic prototype: used in ventricular tachycardia and rapid atrial arrhythmias with Wolff−Parkinson−White syndrome. Tox: arrhythmogenic, CNS excitation
89
# Katzung
Fluconazole
Fluconazole,Imidazole antifungal: used for esophageal candidiasis and in coccidioidomycoses; high CSF levels provide prophylaxis versus fungal meningitis in immunosuppressed patients
90
# Katzung
Fludrocortisone
Fludrocortisone,Synthetic corticosteroid: high mineralocorticoid and moderate glucocorticoid activity; long duration of action
91
# Katzung
Flumazenil
Flumazenil,Benzodiazepine receptor antagonist: used to reverse CNS depressant effects of benzodiazepines (overdose or when used in anesthesia)
92
# Katzung
Fluorouracil
Fluorouracil,Antineoplastic: pyrimidine antimetabolite (cell cycle−specific) causes "thymine−less" cell death; used mainly for solid or superficial tumors. Tox: GI distress, myelosuppression
93
# Katzung
Fluoxetine
Fluoxetine,Antidepressant: serotonin selective reuptake inhibitor (SSRI) prototype. Less ANS adverse effects and cardiotoxic potential than tricyclics. Tox: CNS stimulation, seizures in overdose
94
# Katzung
Flutamide
Flutamide,Androgen receptor inhibitor: nonsteroid used in prostatic carcinoma
95
# Katzung
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
96
# Katzung
Foscarnet
Foscarnet,Antiviral: effective against CMV and HSV (including TK− strains); Tox: electrolyte imbalance, nephrotoxicity
97
# Katzung
Ganciclovir
Ganciclovir,Antiviral: effective against CMV; requires bioactivation via thymidine kinase. Tox: myelosuppression, nephrotoxicity
98
# Katzung
Gemfibrozil, clofibrate
Gemfibrozil, clofibrate,Antilipemics: stimulate lipoprotein lipase in peripheral tissues. Used in hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia
99
# Katzung
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
100
# Katzung
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
101
# Katzung
Glucagon
Glucagon,Hormone product of pancreatic A cells. Increases blood sugar via increased cAMP
102
# Katzung
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
103
# Katzung
Haloperidol
Haloperidol,Antipsychotic butyrophenone: blocks brain dopamine D2 receptors. Tox: marked EPS dysfunction, hyperprolactinemia; less ANS adverse effects than phenothiazines
104
# Katzung
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
105
# Katzung
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
106
# Katzung
Hydralazine
Hydralazine,Antihypertensive: arteriolar vasodilator, orally active; used in HTN, CHF. Tox: Tachycardia, salt and water retention, lupus−like syndrome
107
# Katzung
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
108
# Katzung
Ibuprofen
Ibuprofen,NSAID prototype: short duration. Inhibits cyclooxygenase (both I and II) reversibly. Used in arthritis, dysmenorrhea, muscle inflammation. Tox: peptic ulcer, renal damage
109
# Katzung
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)
110
# Katzung
Imipramine
Imipramine,Tricyclic antidepressant prototype: blocks reuptake of norepinephrine and serotonin. Tox: ANS (alpha and muscarinic) blockade, cardiac arrhythmias
111
# Katzung
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
112
# Katzung
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
113
# Katzung
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
114
# Katzung
Interferon−α
Interferon−α,Important cytokine for the treatment of hepatitis B and C infection.
115
# Katzung
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
116
# Katzung
Ipratropium
Ipratropium,Antimuscarinic agent: aerosol for asthma, COPD. Good bronchodilator in 20−30% of patients. Not as effective as β2 agonists
117
# Katzung
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)
118
# Katzung
Isoproterenol
Isoproterenol,Beta1, beta2 agonist catecholamine prototype: bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR. Tox: arrhythmias, angina
119
# Katzung
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
120
# Katzung
Labetalol
Labetalol,Alpha− and beta−blocker: used in HTN. Tox: AV block, hypotension
121
# Katzung
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
122
# Katzung
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
123
# Katzung
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
124
# Katzung
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)
125
# Katzung
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
126
# Katzung
LSD
LSD,Lysergic acid diethylamide, "Acid:" semisynthetic ergot derivative; orally active; hallucinogen
127
# Katzung
Malathion
Malathion,Organophosphate insecticide cholinesterase inhibitor: pro−drug converted to malaoxon. Less toxic in mammals and birds because metabolized to inactive products
128
# Katzung
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
129
# Katzung
Mestranol
Mestranol,Synthetic estrogen: used in many oral contraceptives
130
# Katzung
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
131
# Katzung
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
132
# Katzung
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
133
# Katzung
Methyldopa
Methyldopa,Antihypertensive: prodrug of methylnorepinephrine, a CNS−active α2 agonist. Reduces SANS outflow from vasomotor center. Tox: positive Coombs test, hemolysis
134
# Katzung
Methysergide
Methysergide,Ergot alkaloid: used as prophylactic in migraine. Tox: retroperitoneal and subendocardial fibroplasia
135
# Katzung
Metoprolol
Metoprolol,Beta1−selective blocker: used in HTN and for prevention of post−MI sudden death arrhythmias
136
# Katzung
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
137
# Katzung
Mexiletine
Mexiletine,Group IB antiarrhythmic drug: like lidocaine but orally active
138
# Katzung
Mifepristone (RU 486)
Mifepristone (RU 486),Progesterone and glucocorticoid inhibitor: abortifacient, antineoplastic
139
# Katzung
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
140
# Katzung
Misoprostol
Misoprostol,PGE1 derivative: orally active prostaglandin used to prevent peptic ulcers in patients taking NSAIDs for arthritis. Tox: diarrhea
141
# Katzung
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
142
# Katzung
Nafcillin
Nafcillin,Penicillinase−resistant penicillin prototype: used for suspected or known staphylococcal infections; not active against methicillin−resistant staphylococci. Tox: penicillin allergy
143
# Katzung
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
144
# Katzung
Naloxone
Naloxone,Opioid mu receptor antagonist: used to reverse CNS depressant effects of opioid analgesics (overdose or when used in anesthesia)
145
# Katzung
Neostigmine
Neostigmine,Cholinesterase inhibitor prototype: quaternary nitrogen carbamate with little CNS effect
146
# Katzung
Nevirapine
Nevirapine,Prototype nonnucleoside inhibitor of HIV reverse transcriptase (NNRTI).Others : efavirenz, delavirdine
147
# Katzung
Niacin
Niacin,Antilipemic: reduces release of VLDL from liver into circulation. Tox: flushing
148
# Katzung
Nifedipine
Nifedipine,Calcium channel blocker prototype: vasoselective (less cardiac depression); used in angina, HTN. Tox: constipation, headache
149
# Katzung
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
150
# Katzung
Norepinephrine
Norepinephrine,Adrenoceptor agonist prototype: acts at all alpha and at beta1 adrenoceptors; used as vasoconstrictor. Causes reflex bradycardia. Tox: ischemia, arrhythmias, HTN
151
# Katzung
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
152
# Katzung
Norgestrel
Norgestrel,Progestin: used in many oral contraceptives and Norplant implantable contraceptive
153
# Katzung
Olanzapine
Olanzapine,Atypical antipsychotic; high affinity antagonist at 5HT2A with minimal extrapyramidal side effects; improves both positive and negative symptoms of schizophrenia
154
# Katzung
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)
155
# Katzung
Ondansetron, granisetron
Ondansetron, granisetron,5−HT3 receptor blockers: very important antiemetics for cancer chemotherapy; also used post−operatively to reduce vomiting
156
# Katzung
Paraquat
Paraquat,Toxic herbicide: very small oral (but not inhaled) doses cause lethal pulmonary fibrosis
157
# Katzung
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)
158
# Katzung
Penicillamine
Penicillamine,Chelator, immunomodulator: copper and sometimes lead, mercury, arsenic. Used in Wilson's disease and rheumatoid arthritis
159
# Katzung
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
160
# 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
161
# Katzung
Phenoxybenzamine
Phenoxybenzamine,Alpha−blocker prototype: irreversible action. Used in pheochromocytoma
162
# Katzung
Phentolamine
Phentolamine,Alpha−blocker prototype: reversible action. Used in pheochromocytoma
163
# Katzung
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
164
# Katzung
Physostigmine
Physostigmine,Cholinesterase inhibitor prototype: alkaloid tertiary amine carbamate, enters eye and CNS readily. Used in glaucoma
165
# Katzung
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
166
# Katzung
Piroxicam
Piroxicam,NSAID with longest duration of action (t1/2 about 40 h)
167
# Katzung
Pralidoxime
Pralidoxime,Acetylcholinesterase regenerator: very high affinity for phosphorus in organophosphates
168
# Katzung
Prazosin, terazosin, doxazosin
Prazosin, terazosin, doxazosin,Alpha1−selective blockers: used in HTN. Tox: first−dose orthostatic hypotension
169
# Katzung
Prednisone
Prednisone,Glucocorticoid prototype: potent, short−acting; much less mineralocorticoid activity than cortisol but more than dexamethasone or triamcinolone
170
# Katzung
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
171
# Katzung
Probucol
Probucol,Antilipemic: unknown mechanism; recently withdrawn but new evidence suggests efficacy in preventing restenosis of coronaries after angioplasty.Tox: causes arrhythmias
172
# Katzung
Procainamide
Procainamide,Group IA antiarrhythmic drug: short half−life; similar to quinidine but may cause lupus erythematosus
173
# Katzung
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
174
# 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)
175
# Katzung
Prostacyclin
Prostacyclin,PGI2: prostaglandin vasodilator and inhibitor of platelet aggregation
176
# Katzung
Pyridostigmine
Pyridostigmine,Cholinesterase inhibitor: long−acting (8 h) quaternary carbamate; used in myasthenia gravis
177
# Katzung
Quinidine
Quinidine,Group IA antiarrhythmic prototype: used in atrial and ventricular arrhythmias. Tox: cinchonism, GI upset, thrombocytopenic purpura, arrhythmogenic
178
# Katzung
Quinine
Quinine,Antimalarial: blood schizonticide; no effect on liver stages. Isomer of quinidine, same toxicity
179
# Katzung
Ranitidine
Ranitidine,H2 blocker: like cimetidine but less inhibition of hepatic drug metabolism; no antiandrogenic effects
180
# Katzung
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
181
# Katzung
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
182
# 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.
183
# Katzung
Selegiline
Selegiline,MAO−B inhibitor: selective inhibitor of the enzyme that metabolizes dopamine (no tyramine interactions). Used in parkinsonism as adjunct
184
# Katzung
Sildenafil
Sildenafil,Viagra. Blocks phosphodiesterase that splits cGMP; enhanced smooth muscle relaxation causes erection. Important interaction with nitrates.
185
# Katzung
Streptokinase
Streptokinase,Thrombolytic: protein from streptococci that accelerates plasminogen−to−plasmin conversion. Tox: bleeding, allergy
186
# Katzung
Succimer (DMSA)
Succimer (DMSA),Chelator: dimercaptosuccinic acid; used to chelate lead and arsenic
187
# Katzung
Succinylcholine
Succinylcholine,Depolarizing neuromuscular relaxant prototype: short duration (5 min) if patient has normal plasma cholinesterase (genetically determined). No antidote (compare with tubocurarine)
188
# Katzung
Sumatriptan, other "− triptans"
Sumatriptan, other "− triptans",5−HT1D receptor agonists: used to abort migraine attacks
189
# Katzung
Tamoxifen, raloxifen
Tamoxifen, raloxifen,Estrogen partial agonists "selective estrogen receptor modulators": used in breast carcinoma, osteoporosis
190
# Katzung
Tetracaine
Tetracaine,Local anesthetic: long−acting ester prototype
191
# Katzung
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
192
# Katzung
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
193
# Katzung
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
194
# 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)
195
# Katzung
Thyroxine, triiodothyronine
Thyroxine, triiodothyronine,Major hormones produced by the thyroid: stimulate metabolism, growth, and development
196
# Katzung
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
197
# Katzung
Ticlopidine, clopidogrel
Ticlopidine, clopidogrel,Newer antiplatelet agents. Used to prevent strokes, postangioplasty occlusion.
198
# Katzung
Tolbutamide, tolazamide, chlorpropamide, acetohexamide
Tolbutamide, tolazamide, chlorpropamide, acetohexamide,Oral hypoglycemics: older sulfonylurea group. (See glipizide.) Chlorpropamide has longest duration of action
199
# Katzung
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
200
# Katzung
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
201
# 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
202
# 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
203
# Katzung
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)
204
# Katzung
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
205
# Katzung
Vesamicol
Vesamicol,Inhibitor of vesicle ACh/H+ antiporter in cholinergic nerve endings: prevents storage of ACh. No clinical applications
206
# Katzung
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
207
# Katzung
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
208
# Katzung
Zanamivir
Zanamivir, oseltamivir,Neuraminidase inhibitors that can be used to reduce severity and duration of influenza symptoms. Prevents penetration of the virion.
209
# Katzung
Zidovudine (AZT)
Zidovudine (AZT),Antiviral: prototype nucleoside inhibitor of HIV reverse transcriptase (NRTI). Tox: severe myelosuppression. Others: lamivudine, stavudine, didanosine, zalcitabine.
210
# Katzung
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
