abciximab - mech
Monoclonal antibody to fibrin receptor (glycoprotein IIb/IIIa) on platelets.
abciximab - use
Used to prevent clotting after coronary angioplasty
acetaminophen - mech
Antipyretic analgesic: very weak cyclooxygenase inhibitor; not anti−inflammatory.
acetazolamide, dorzolamide - mech
Carbonic anhydrase inhibitor diuretic: produces a NaHCO3 diuresis, results in bicarbonate depletion, and therefore has self−limited action.
acetazolamide, dorzolamide - use
Used in glaucoma and mountain sickness. Dorzolamide is a topical analog for glaucoma
acetylcholine - mech (sites of action)
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 - mech
Antiviral: inhibits DNA synthesis in herpes simplex and varicella zoster. Requires activation by viral thymidine kinase (TK− strains are resistant).
acyclovir - tox
Tox: behavioral effects and nephrotoxicity (crystalluria), but not myelosuppression
acyclovir - use
varicella and herpes
adenosine - mech
Antiarrhythmic: unclassified (“Group V”); parenteral only. Hyperpolarizes AV nodal tissue, blocks conduction for 10−15 sec.
adenosine - use
Used for nodal reentry arrhythmias
allopurinol - mech
Antigout: inhibitor of xanthine oxidase; reduces production of uric acid
list the three important beta2 agonists, what is their use
albuterol, metaproterenol, terbutaline
asthma
alprazolam - mech
Benzodiazepine sedative−hypnotic
alprazolam - use
widely used in anxiety states, selectivity for panic attacks and phobias; possible antidepressant actions.
alprazolam - tox
Tox: psychologic and physical dependence, additive effects with other CNS depressants
alteplase - mech
Thrombolytic: human recombinant tissue plasminogen activator.
alteplase - use
Used in acute MI to recanalize the occluded coronary. Occasionally used in pulmonary embolism, stroke.
amiloride - mech
K+−sparing diuretic: blocks Na+ channels in cortical collecting tubules
aminoglutethimide - mech
Nonsteroid inhibitor of steroid synthesis: reduces conversion of cholesterol to the hormone precursor, pregnenolone.
aminoglutethimide - use
Used in metastatic breast cancer
amiodarone - mech
Group IA and III antiarrhythmic: broad spectrum, blocks sodium, potassium, calcium channels, beta receptors. High efficacy and very long half−life (weeks−months).
amiodarone - tox
Tox: deposits in tissues; hypo− or hyperthyroidism; pulmonary fibrosis
amitriptyline - mech
Tricyclic antidepressant: blocks reuptake of norepinephrine and serotonin.
amitriptyline - tox
Tox: atropine− like, postural hypotension, sedation; cardiac arrhythmias in overdose, additive effects with other CNS depressants
amoxicillin - mech / resistance mech
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.
amphetamine - mech
Indirectly acting sympathomimetic: displaces stored catecholamines in nerve endings. Marked CNS stimulant actions; high abuse liability.
amphetamine - tox
Tox: psychosis, HTN, MI, seizures
amphotericin b - mech
Antifungal: polyene drug of choice for most systemic mycoses; binds to ergosterol to disrupt fungal cell membrane permeability.
amphotericin b - tox
Tox: chills and fever, hypokalemia, hypotension, nephrotoxicity (dose−limiting, possibly less with liposomal forms)
ampicillin - mech / spectrum
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.
ampicillin - tox
Tox: penicillin allergy; more adverse effects on GI tract than other penicillins; maculopapular skin rash
anistreplase - mech
Thrombolytic: bacterial streptokinase complexed with human plasminogen. Longer acting in body than other thrombolytics (rt−PA, streptokinase, urokinase).
aspirin - mech
NSAID prototype: inhibits cyclooxygenase (COX) I and II irreversibly. Potent antiplatelet agent as well as antipyretic analgesic anti−inflammatory drug
atenolol - mech
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 - mech
Muscarinic cholinoceptor blocker prototype: lipid soluble, CNS effects.
atropine - tox
Tox: “red as a beet, dry as a bone, mad as a hatter,” urinary retention, mydriasis
azithromycin - mech
macrolide antibiotic: similar to erythromycin, but greater activity versus chlamydia and streptococci; long half−life due to tissue accumulation.
baclofen - mech
GABA analog, orally active: spasmolytic; activates GABAB receptors in the spinal cord
benztropine - mech
Centrally acting antimuscarinic prototype for parkinsonism
benztropine - use
parkinsonism
bethanechol - mech
Muscarinic agonist: choline ester with good resistance to cholinesterase
bethanechol - use
used for atonic bowel or bladder
botulinum - mech
Toxin: enzyme produced by Clostridium botulinum; interacts with fusion/docking proteins to block release of acetylcholine vesicles
bromocriptine - mech
Ergot derivative: dopamine agonist in CNS; inhibits prolactin release.
bromocriptine - use
Used in parkinsonism and hyperprolactinemia.
bromocriptine - tox
Tox: CNS, dyskinesias, hypotension
bupivacaine - distinguishing features
Long−acting amide local anesthetic prototype: greater CV toxicity than most local anesthetics
buspirone - mech
Anxiolytic: atypical drug that interacts with 5HT1A receptors; slow onset. Minimal potentiation of CNS depressants including ethanol; negligible abuse liability
captopril - mech
ACE inhibitor prototype
captopril - use
used in HTN, diabetic renal disease, and CHF.
captopril - tox
hyperkalemia, fetal renal damage, cough (“sore throat”)
carbachol - mech
Nonselective muscarinic and nicotinic agonist: choline ester with good resistance to cholinesterase
carbachol - use
used for glaucoma (not a first−line drug)
carbamazepine - mech
Anticonvulsant: tricyclic derivative used for tonic−clonic and partial seizures; blocks Na+ channels in neuronal membranes.
carbamazepine - use
Anticonvulsant for tonic-clonic and partial seizures. Drug of choice for trigeminal neuralgia; back−up drug in mania.
carbamazepine - tox
Tox: CNS depression, hematotoxic, induces liver drug−metabolizing enzymes
cefazolin - mech
First−generation cephalosporin prototype: bactericidal beta−lactam inhibitor of cell wall synthesis.
cefazolin - use
Active against gram−positive cocci, E coli, K pneumoniae, but does not enter CSF.
cefoxitin - use
Second−generation cephalosporin: active against a wide spectrum of gram−negative bacteria including anaerobes (B fragilis). Does not enter the CNS
ceftriaxone - use
Third−generation cephalosporin: active against resistant bacteria including gonococci, H influenzae, and other gram−negative organisms. Crosses the blood−brain barrier
celecoxib, rofecoxib - mech, advantage
First COX−II−selective NSAIDs. Reduced GI toxicity
chloramphenicol - mech
Antibiotic: broad spectrum agent; inhibits protein synthesis (50S)
chloramphenicol - use
uses restricted to back− up drug for bacterial meningitis, infections due to anaerobes, Salmonella.
chloramphenicol - tox
Tox: reversible myelosuppression, aplastic anemia, gray baby syndrome
chloroquine - mech/use
Antimalarial: blood schizonticide used for treatment and as a chemosuppressant where P falciparum is susceptible.
chloroquine - tox
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 - mech
Antihistamine H1 blocker prototype
chlorpheniramine - tox
Tox: sedation, antimuscarinic
chlorpromazine - mech
Phenothiazine antipsychotic drug prototype: blocks most dopamine receptors in the CNS.
chlorpromazine - tox
Tox: atropine−like, EPS dysfunction, hyperprolactinemia, postural hypotension, sedation, seizures (in overdose), additive effects with other CNS depressants
cholestyramine, colestipol - mech
Bile acid−binding resins: sequester bile acids in gut and divert more cholesterol from the liver to bile acids instead of circulating lipoproteins.
cholestyramine, colestipol - tox
Tox: constipation, bloating; interfere with absorption of some drugs
cimetidine - mech
H2 blocker prototype
cimetidine - tox
Tox: inhibits hepatic drug metabolism; antiandrogen effects. Less toxic analogs: ranitidine, famotidine, nizatidine
ciprofloxacin - mech
Fluoroquinolone antibiotic: bactericidal inhibitor of topoisomerases
ciprofloxacin - use
active against many gram−negative rods including E coli, H influenzae, Campylobacter, Enterobacter, Pseudomonas, Shigella.
ciprofloxacin - tox
Tox: CNS dysfunction, GI distress, superinfection, collagen damage (avoid in children and pregnant women). Interactions: caffeine, theophylline, warfarin
cisplatin -mech
Platinum−containing alkylating cancer chemotherapeutic agent. Carboplatin is similar.
cisplatin - use
Used for several solid tumors (eg, testes, lung).
cisplatin - tox
nephrotoxic and acoustic nerve damage
clindamycin - mech
Lincosamide antibiotic: bacteriostatic inhibitor of protein synthesis (50S)
clindamycin - use
active against gram−positive cocci, B fragilis, MRSA
clindamycin - tox
Tox: GI distress, pseudomembranous colitis
clomiphene - mech
Estrogen partial agonist
clomiphene - use
synthetic used in infertility to induce ovulation
clonidine - mech
Alpha2 agonist: acts centrally to reduce SANS outflow
clonidine - use
HTN
clonidine - tox
Tox: rebound HTN if stopped suddenly
clozapine - mech
Atypical antipsychotic: low affinity for dopamine D2 receptors, higher for D4 and 5−HT2A receptors
clozapine - tox
less EPS adverse effects than other antipsychotic drugs. Tox: ANS effects, agranulocytosis (infrequent but significant)
cocaine - mech
Indirectly acting sympathomimetic: blocks amine reuptake into nerve endings. Local anesthetic (ester type). Marked CNS stimulation, euphoria; high abuse liability.
cocaine - tox
Tox: psychosis, cardiac arrhythmias, seizures
colchicine - mech
Microtubule assembly inhibitor: reduces mobility and phagocytosis by WBCs in gout− inflamed joints;
colchicine - use
useful in acute, not chronic gout.
colchicine - tox
Tox: GI, hepatic, renal damage
cyclopentolate, tropicamide - mech
Antimuscarinics for ophthalmology: shorter duration than atropine (a few hours or less);
cyclopentolate, tropicamide - use
ophtho - cause cycloplegia and mydriasis
cyclophosphamide - mech
Antineoplastic, immunosuppressive: cell cycle−nonspecific alkylating agent.
cyclophosphamide - tox
Tox: alopecia, gastrointestinal distress, hemorrhagic cystitis, myelosuppression
cyclosporine - mech
Immunosuppressant: antibiotic; inhibits interleukin−2 synthesis, suppresses T cells.
cyclosporine - tox
Tox: HTN, hirsutism, nephrotoxicity (dose−limiting), seizures (in overdose). Not a myelosuppressant
dantrolene - mech
Blocks Ca2+ release from sarcoplasmic reticulum of skeletal muscle.
dantrolene - use
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 - mech
ADH analog: synthetic peptide
ddavp - use
used for pituitary diabetes insipidus
ddt - mech
Insecticide: prevents inactivation of sodium channels, causes uncontrolled neuronal activity. Stored for years in body fat in mammals, birds, fish
deferoxamine - mech
Chelator: bacterial product; chelates iron very avidly, aluminum less so
dexfenfluramine - mech
5−HT reuptake inhibitor and receptor agonist previously used as anorexic.
dexfenfluramine - tox
Tox: produced cardiac valve damage when used in combination with phentermine
dexamethasone - mech
Glucocorticoid: very potent, long−acting; no mineralocorticoid activity
diazepam - mech
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.
diazepam - use
Uses: anxiety states, ethanol detoxication, muscle spasticity, status epilepticus.
diazepam - tox
Tox: psychologic and physical dependence, additive effects with other CNS depressants
didanosine (DDI) - mech
Antiviral: nucleoside inhibitor of HIV reverse transcriptase.
didanosine (DDI) - tox
Tox: peripheral neuropathy, pancreatitis
digitoxin - mech
Cardiac glycoside: half−life 168 h, excreted in the bile (partially as digoxin); subject to enterohepatic circulation. See digoxin
digoxin - mech
Cardiac glycoside prototype: positive inotropic drug for CHF, half−life 40 h; renal excretion; inhibits Na+/K+ ATPase, also a cardiac parasympathomimetic.
digoxin - tox
Tox: calcium overload arrhythmias, GI upset
diltiazem - mech
Calcium channel (L−type) blocker prototype: like verapamil, has more depressant effect on heart than dihydropyridines (eg, nifedipine).
diltiazem - tox
Tox: AV block, CHF, edema, constipation
dimercaprol (BAL) - use
Chelator (British AntiLewisite): used for arsenic, lead, and mercury poisoning
dioxin (TCDD) - tox
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 - mech
Antihistamine H1 blocker (inverse agonist) prototype
diphenhydramine - use
used in hayfever, motion sickness, dystonias.
diphenhydramine - tox
Tox: antimuscarinic, anti−alpha, sedative
disopyramide - mech
Group IA antiarrhythmic
disopyramide - use
used for ventricular arrhythmias.
disopyramide - tox
Tox: strong antimuscarinic; may cause CHF
dopamine - use
used in shock to increase renal blood flow, stimulate heart
doxorubicin - mech
Antineoplastic: anthracycline drug (cell cycle−nonspecific); intercalates between base pairs to disrupt DNA functions and forms cytotoxic free radicals.
doxorubicin - tox
Tox: cardiotoxicity, myelosuppression
doxycycline - mech / unique features
Tetracycline antibiotic: protein synthesis inhibitor (30S), more effective than other tetracyclines against bacillary dysentery. Unlike other tetracyclines, it is eliminated mainly in the feces.
echothiophate - mech
Organophosphate cholinesterase inhibitor: less lipid soluble than most organophosphates
echothiophate - use
used in glaucoma
edetate (EDTA) - use
Chelating agent: used in lead poisoning.
edetate (EDTA) - tox
Tox: renal tubular necrosis
edrophonium - mech
Cholinesterase inhibitor: very short duration of action (15 min).
edrophonium - use
Used to reverse NM blockade and as diagnostic test in myasthenia gravis
enoxaparin - mech
Low molecular weight heparin. Primary effect is anti−factor X. Other low molecular weight heparin−like products: dalteparin, danaparoid.
ephedrine - mech
Indirectly acting sympathomimetic: like amphetamine but less CNS stimulation, more smooth muscle effects
epinephrine - mech
Adrenoceptor agonist prototype: product of adrenal medulla, some CNS neurons. Affinity for all alpha and all beta receptors.
epinephrine - use
Used in asthma; as hemostatic and adjunct with local anesthetics; drug of choice in anaphylaxis
ergonovine - mech
Ergot alkaloid: uterine effect prototype, causes prolonged uterine contraction.
ergonovine - use
Used in post−partum bleeding
ergotamine - mech
Ergot alkaloid: vascular effect prototype, causes prolonged vasoconstriction, uterine contraction.
ergotamine - use
Used in migraine, obstetrics
erythromycin - mech
Macrolide antibiotic: inhibitor of protein synthesis (50S);
erythromycin - use
activity includes gram−positive cocci and bacilli, M pneumoniae, Legionella pneumophila, C trachomatis.
erythromycin - tox
Tox: cholestatic jaundice, inhibits liver drug−metabolizing enzymes, interactions with astemizole, theophylline, terfenadine, warfarin
ethacrynic acid - mech
Loop diuretic: not a sulfa derivative.
ethacrynic acid - tox
Tox: like furosemide but does not increase serum uric acid.
ethanol - tox
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 - mech
Anticonvulsant: used in absence seizures; may block T−type Ca2+ channels in thalamic neurons.
ethosuximide - tox
Tox: GI distress but safe in pregnancy
etidronate, pamidronate, alendronate - mech
Bisphosphonates: reduce turnover of bone calcium.
etidronate, pamidronate, alendronate - use
Used in Paget’s disease, osteoporosis; alendronate increases bone formation.
etidronate, pamidronate, alendronate - tox
Tox: severe esophageal ulceration (pill esophagitis)
fexofenadine - mech
2nd generation antihistamine; does not enter CNS, little or no sedation
finasteride - mech
Steroid inhibitor of 5α−reductase: inhibits synthesis of dihydrotestosterone, the active androgen in prostate.
finasteride - use
Used in BPH
flecainide - mech
Group IC antiarrhythmic prototype
flecainide - use
used in ventricular tachycardia and rapid atrial arrhythmias with Wolff−Parkinson−White syndrome.
flecainide - tox
Tox: arrhythmogenic, CNS excitation
fluconazole - mech
Imidazole antifungal
fluconazole - use
used for esophageal candidiasis and in coccidioidomycoses; high CSF levels provide prophylaxis versus fungal meningitis in immunosuppressed patients
fludrocortisone - mech
Synthetic corticosteroid: high mineralocorticoid and moderate glucocorticoid activity; long duration of action
flumazenil - use
Benzodiazepine receptor antagonist: used to reverse CNS depressant effects of benzodiazepines (overdose or when used in anesthesia)
fluorouracil - mech
Antineoplastic: pyrimidine antimetabolite (cell cycle−specific) causes “thymine−less” cell death; used mainly for solid or superficial tumors.
fluorouracil - tox
Tox: GI distress, myelosuppression
fluoxetine - mech
Antidepressant: serotonin selective reuptake inhibitor (SSRI) prototype. Less ANS adverse effects and cardiotoxic potential than tricyclics.
fluoxetine - tox
Tox: CNS stimulation, seizures in overdose
flutamide - mech
Androgen receptor inhibitor: nonsteroid
flutamide - use
used in prostatic carcinoma
furosemide - mech
Loop diuretic prototype: blocks Na+/K+/2Cl− transporter; high efficacy
furosemide - use
used in acute pulmonary edema, refractory edematous states, hypercalcemia.
furosemide - tox
Tox: ototoxicity, K+ wasting, hypovolemia, increased serum uric acid
foscarnet - use
Antiviral: effective against CMV and HSV (including TK− strains);
foscarnet - tox
Tox: electrolyte imbalance, nephrotoxicity
ganciclovir - mech/use
Antiviral: effective against CMV; requires bioactivation via thymidine kinase.
ganciclovir - tox
Tox: myelosuppression, nephrotoxicity
gemfibrozil, clofibrate - mech
Antilipemics: stimulate lipoprotein lipase in peripheral tissues.
gemfibrozil, clofibrate - tox
Used in hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia
gentamicin - mech/spectrum of activity
Aminoglycoside prototype: bactericidal inhibitor of protein synthesis (30S); active against many aerobic gram−negative bacteria. Narrow therapeutic window; dose reduction required in renal impairment.
gentamicin - tox
Tox: renal dysfunction, ototoxicity; once−daily dosing is effective (post−antibiotic effect) and less toxic
glipizide, glyburide - mech
Oral hypoglycemics: second generation, very potent. Like other sulfonylureas, act by closing K channels in pancreatic B cells, causing depolarization and release of insulin.
glipizide, glybruide - tox
hypoglycemia
glucagon - mech
Hormone product of pancreatic A cells. Increases blood sugar via increased cAMP
guanethidine - mech
Postganglionic sympathetic neuron blocker: enters nerve ending by means of uptake−1 and is stored in the ending (effect reversed by TCAs, cocaine).
guanethidine - tox
Tox: severe orthostatic hypotension, sexual dysfunction
guanethidine - use
HTN
haloperidol - mech
Antipsychotic butyrophenone: blocks brain dopamine D2 receptors.
haloperidol - tox
Tox: marked EPS dysfunction, hyperprolactinemia; less ANS adverse effects than phenothiazines
halothane - mech
General anesthetic prototype: inhaled halogenated hydrocarbon. Causes cardiovascular and respiratory depression and relaxes skeletal and smooth muscle.
halothane - tox
Use has decreased due to sensitization of heart to catecholamines, and occurrence (rare) of hepatitis and malignant hyperthermia
heparin - mech
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 - mech
Antihypertensive: arteriolar vasodilator, orally active
hydralazine - mech
HTN, CHF
hydralazine - tox
Tox: Tachycardia, salt and water retention, lupus−like syndrome
hydrochlorothiazide - mech
Thiazide diuretic prototype: acts in distal convoluted tubule; blocks Na+/Cl− transporter;
hydrochlorothiazide - use
used in HTN, CHF, chronic renal stone syndrome.
hydrochlorothiazide - tox
Tox: increased serum lipids, uric acid, glucose; K+ wasting
ibuprofen - mech
NSAID prototype: short duration. Inhibits cyclooxygenase (both I and II) reversibly.
ibuprofen - tox
Tox: peptic ulcer, renal damage
imipenem - mech/spectrum
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).
imipenem - tox
Tox: allergy (partial cross−reactivity with penicillins), seizures (overdose)