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