Pharmacology Mnemonics - Flash Cards

Chromium

2008-06-04T03:58:00.001-07:00

Name: Chromium

Class:

Mechanism: Part of several metalloenzymes

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Deficiencies only in severely protein-deprived pts and pts. w/prolonged parenteral feeding.

Cobalt

2008-06-04T03:57:00.005-07:00

Name: Cobalt

Class:

Mechanism: Present in vitamin B₁₂.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: No known deficiency states.

Manganese

2008-06-04T03:57:00.003-07:00

Name: Manganese

Class:

Mechanism: Present in several enzymes, required for normal bone structure.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: No reported deficiencies. Excess limited to manganese miners.

Fluoride

2008-06-04T03:57:00.001-07:00

Name: Fluoride

Class:

Mechanism: Present in bones and teeth. Fluoridation of drinking water at 1 ppm ® ¯ dental caries by 30-40%. Hardens outer layers of tooth enamel. Makes enamel more resistant to demineralization.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Excess (> 10 ppm in water) ® fluorosis (mottling of teeth) due to excess accumulation in teeth and bones.

Selenium

2008-06-04T03:56:00.002-07:00

Name: Selenium

Class:

Mechanism: Present in glutathione peroxidase which destroys peroxides derived from unsaturated fatty acids. Probably has a close functional relationship w/vitamin E.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: RDA probably directly proportional to intake of polyunsaturated fatty acids.

Copper

2008-06-04T03:56:00.001-07:00

Name: Copper

Class:

Mechanism: Present in muscle, bone, liver, blood. In blood, almost entirely bound to ceruloplasmin. Component of many metalloenzymes such as cytochrome oxidase and tyrosinase.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Excess plasma free copper may be due to Wilson’s Disease (defective ceruloplasmin) or excessive intake.

Zinc

2008-06-04T03:55:00.000-07:00

Name: Zinc

Class:

Mechanism: Part of many metalloproteins (e.g., “zinc fingers”). Element of carbonic anhydrase.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Kids w/low Zinc often grow poorly and have a poor appetite (prob. 2° to impaired taste).

Iodine

2008-05-15T15:38:00.002-07:00

Name: Iodine

Class:

Mechanism: 80% contained in thyroglobulin.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Deficiency ® endemic goiter. Excess (>20 x RDA) ® blocked organification of iodine ® myxedema.

Vitamin B12 (Cyanocobalamin)

2008-05-15T15:38:00.001-07:00

Name: Vitamin B₁₂ (Cyanocobalamin)

Class:

Mechanism: Necessary for folate Metabolismolism and DNA synth. Maintains myelinization of spinal cord tracts.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Vegan diet ® deficiency ® megaloblastic pernicious anemia and degeneration of posterolateral spinal cord tracts. If patient is deficient in B₁₂ and folate, replace B₁₂ first to avoid irreversible neuro damage. Liver damage ® need.

Biotin

2008-05-15T15:37:00.001-07:00

Name: Biotin

Class:

Mechanism: Incorporated in coenzyme A.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Some antibiotics kill gut microbes that synthesize biotin.

Vitamin B3 (Niacin)

2008-05-15T15:36:00.000-07:00

Name: Vitamin B₃ (Niacin)

Class:

Mechanism: Incorporated into NAD and NADP.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Deficiency ® pellagra (dementia, dermatitis, diarrhea). Penicillamine, hydralazine, and isoniazid complex w/B₆ ® ¯ B₆. B₆ is a cofactor of tryptophan ® nicotinic acid conversion. Results in ¯ B₃.

Vitamin B6 (Pyridoxine)

2008-05-15T14:32:00.001-07:00

Name: Vitamin B₆ (Pyridoxine)

Class:

Mechanism: Derivatives serve as coenzymes in many intermed. rxns.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Megadose—severe (often irreversible) sensory neuropathy

Utility:

Special Features: Deficiency ® cheilosis, glossitis, dermatitis, peripheral neuropathy. Liver damage ® need. Penicillamine, hydralazine, and isoniazid complex w/B₆ ® ¯ B₆. B₆ is a cofactor of tryptophan ® nicotinic acid conversion. Results in ¯ B₃. Pregnancy ® B₆ demand.

Vitamin B1 (Thiamine)

2008-05-15T14:28:00.000-07:00

Name: Vitamin B₁ (Thiamine)

Class:

Mechanism: Coenzyme in decarboxylation rxns. Facilitates conduction of impulses in peripheral nerves.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Deficiency ® dry & wet beriberi, Wernicke-Korsakoff’s synd. RDA directly proportional to caloric intake. Deficiency common in alcoholics.

Vitamin B2 (Riboflavin)

2008-05-15T14:26:00.001-07:00

Name: Vitamin B₂ (Riboflavin)

Class:

Mechanism: Converted to coenzymes FMN and FAD.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Deficiency ® ariboflavinosis, cheilosis, stomatitis, glossitis, dermatitis, corneal vascularization.

Vitamin K

2008-05-15T14:22:00.000-07:00

Name: Vitamin K

Class:

Mechanism: Cofactor in hepatic carboxylation of procoagulants—factors II, VII, IX, and X.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Antagonize coumarin anticoagulation (min. dose = 60-100 x RDA). Infants given injxn (infant GI tract lacks microbes that produce vitamin K).

Special Features: Deficiency ® bleeding diathesis. Some antibiotics kill gut microbes that synthesize vitamin K. Bishydroxycoumarin antagonizes effects of vitamin K. Prolonged use of large dose salicylates block vitamin K actions in prothrombin synth. ® hypoprothrombinemia.

Vitamin E

2008-05-12T11:44:00.000-07:00

Name: Vitamin Vitamin

Class:

Mechanism: Fat soluble antioxidant. Scavenges free radicals. Conc. in adipose tissue.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Diarrhea, headache.

Utility: Large doses may reduce rate of buildup of atherosclerotic plaques in coronary arteries and protect against stroke and heart disease.

Special Features: RDA directly proportional to intake of polyunsaturated fatty acids. Deficiency ® spinocerebellar degeneration.

Ofloxacin (Floxin)

2008-05-12T11:43:00.000-07:00

Name: Ofloxacin (Floxin)

Class: Fluorinated quinolone

Mechanism: Inhib bact. DNA gyrase (topoisomerase II). Bactericidal.

Absorption: Oral admin.

Distrib.: Good tissue penetration.

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Usu. not severe. GI, CNS. Not for pregnant or nursing women or prepubertal children.

Utility: UTIs due to Enterobacteriaceae, Enteroccus, Staph, Pseudomonas. Infectious diarrhea.

Special Features: Broader spectrum than nonfluorinated quinolones. For diarrhea, treat until symptoms resolve, or no longer than 3 days.

Ciprofloxacin (Cipro)

2008-05-12T10:42:00.000-07:00

Name: Ciprofloxacin (Cipro)

Class: Fluorinated quinolone

Mechanism: Inhib bact. DNA gyrase (topoisomerase II). Bactericidal.

Absorption: Rapid absorption after oral admin.

Distrib.: Good tissue penetration. Poor CSF.

Metabolism.: Partial hepatic Metabolism.

Excretion, t½: Glomerular filtration, secretion. Also feces, bile, sputum. 4 hr.

Toxicity/S.E.s: Usu. not severe. GI, CNS, arthropathy. Not for pregnant or nursing women or prepubertal children.

Utility: Upper and lower UTIs, DOC for Pseudomonas UTIs. Active against aerobic gram- bacilli, H. influenzae, Neisseria. Good for several causes of infectious diarrhea, osteomyelitis, and patients w/CF.

Special Features: Broader spectrum than nonfluorinated quinolones. For diarrhea, treat until symptoms resolve, or no longer than 3 days.

Norfloxacin (Noroxin)

2008-05-12T09:42:00.000-07:00

Name: Norfloxacin (Noroxin)

Class: Fluorinated quinolone

Mechanism: Inhib bact. DNA gyrase (topoisomerase II). Bactericidal.

Absorption: Oral admin.

Distrib.: Good tissue penetration.

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Usu. not severe. GI, CNS. Not for pregnant or nursing women or prepubertal children.

Utility: UTIs due to Enterobacteriaceae, Enteroccus, Staph, Pseudomonas. Infectious diarrhea.

Special Features: Broader spectrum than nonfluorinated quinolones. For diarrhea, treat until symptoms resolve, or no longer than 3 days.

Folic Acid

2008-05-12T08:45:00.001-07:00

Name: Folic Acid

Class:

Mechanism: Essential for transfer and utilization of 1-carbon units in DNA synth.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Recommended for all premenopausal women at dose of 2 x RDA ® reduced risk of neural tube defects. Lowers homocysteine, reduces risk of heart disease. May lower risk of cervical cancer. Treat folate-responsive schizophrenia (50-150 x RDA ® ¯ buildup of urinary homocysteine ® ¯ psychiatric symptoms).

Special Features: Deficiency ® megaloblastic anemia. Alcoholism ® ¯ folate absorption. Pregnancy ® folate demand.

Vitamin A

2008-05-12T08:44:00.001-07:00

Name: Vitamin A

Class:

Mechanism: Component of visual pigment. Maintains specialized epithelia and resistance to infxn.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Megadose—teratogenic (face, head, brain, heart), thickening of the leg bones, intracranial pressure.

Utility:

Special Features: Deficiency ® night blindness, xerophthalmia, blindness, squamous metaplasia, infxn vulnerability (esp. measles). Liver damage ® need.

Vitamin C

2008-05-12T08:43:00.002-07:00

Name: Vitamin C

Class:

Mechanism:

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Diarrhea. Megadose—diarrhea, kidney stones, precipitation of sickle cell crisis, transient infertility, altered renal secretion of weak acids and bases.

Utility: Large doses may reduce rate of buildup of atherosclerotic plaques in coronary arteries and protect against stroke and heart disease.

Special Features: TB pts. probably need 2x normal amount of vitamin C.

Vitamin D

2008-05-12T08:43:00.001-07:00

Name: Vitamin D

Class:

Mechanism: Facilitates intest. absorption of Ca²⁺ and PO₄^3-, and mineralization of bone.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Megadose—hypercalcemia.

Utility:

Special Features: Quasi-vitamin—synthesized in humans. RDA inversely proportional to amount of UV light exposure. Deficiency ® rickets (kids), osteomalacia (adults).

Trimethoprim-Sulfamethoxazole (Bactrim, Septra)

2008-05-12T08:42:00.000-07:00

Name: Trimethoprim-Sulfamethoxazole (Bactrim, Septra)

Class: Antimicrobial

Mechanism: Acts on two sequential steps in synth of folic acid. PABA competitive inhib, dihydrofolate reductase inhib. Bacteriostatic.

Absorption: Oral, IV

Distrib.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Megaloblastic anemia, leukopenia, granulocytopenia (prevented by admin. of folic acid)

Utility: Uncomp. UTIs, otitis media, acute exacerbations of chronic bronchitis, various pneumonias. DOC for Travelers’ diarrhea (esp. in kids), P. carinii pneumonia, Shigella enteritis, systemic Salmonella infects, prostatitis.

Special Features: Trimethoprim = highly selective inhib. of bacterial dihydrofolate reductase. For diarrhea, treat until symptoms resolve, or no longer than 3 days.

Difenoxin-Atropine (Motofen)

2008-05-12T08:41:00.001-07:00

Name: Difenoxin-Atropine (Motofen)

Class: Opioid (Antidiarrheal)

Mechanism: Increased gastric tone ® delayed gastric emptying. tone and ¯ propulsive peristaltic waves in large intest. ® ¯ gut motility. Effects due to inhib. of ACh release by neurons in the intest. wall. Naloxone sensitive.

Absorption: Oral

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Recommended dose ® dizziness, drowsiness, mild euphoria. Excessive doses ® pronounced euphoria, potentially serious respiratory depression (may not be evident until 12-30 hr later). ¯ peristalsis ® ¯ evacuation of bacteria and toxins. Use w/great caution in kids. Potentiates effects of barbiturate, tranquilizers, alcohol, other narcotics. Hypertensive crisis w/MAOI.

Utility: Antidiarrheal.

Special Features: Difenoxin has 5x potency of diphenoxylate. Atropine included primarily to prevent drug abuse. Kids esp. sensitive to atropine toxicity.

Paregoric

2008-05-11T11:02:00.003-07:00

Name: Paregoric

Class: Opioid (Antidiarrheal)

Mechanism: Preparation of oral morphine, anise oil, benzoic acid, camphor, diluted alcohol, and glycerin. Increased gastric tone ® delayed gastric emptying. tone and ¯ propulsive peristaltic waves in large intest. ® ¯ gut motility. Effects due to inhib. of ACh release by neurons in the intest. wall. Naloxone sensitive.

Absorption: Oral

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Antidiarrheal.

Special Features:

Loperamide (Imodium)

2008-05-11T11:02:00.001-07:00

Name: Loperamide (Imodium)

Class: Opioid (Antidiarrheal) (OTC)

Mechanism: Increased gastric tone ® delayed gastric emptying. Increase tone and decreased propulsive peristaltic waves in large intest. ® decreased gut motility. Effects due to inhib. of ACh release by neurons in the intest. wall. Naloxone sensitive. Anti-secretory effect (non-naloxone sensitive).

Absorption: Oral

Dist.: 90% ® GI tract and liver. Very little CNS.

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: ¯ peristalsis ® ¯ evacuation of bacteria and toxins.

Utility: Antidiarrheal. Traveler’s Diarrhea.

Special Features: No abuse liability. Preferred anti-diarrheal of the opioids. Less potential for analgesia, respiratory depression, and addiction than other opioids. Much safer than other opioids. Longer lasting effects than diphenoxylate.

Diphenoxylate-Atropine (Lomotil)

2008-05-11T11:01:00.000-07:00

Name: Diphenoxylate-Atropine (Lomotil)

Class: Opioid (Antidiarrheal)

Absorption: Oral

Dist.:

Metabolism.:

Excretion, t½:

Utility: Antidiarrheal.

Special Features: Atropine included primarily to prevent drug abuse. Kids esp. sensitive to atropine toxicity.

Kaolin-Pectin (Kaopectate)

2008-05-11T11:00:00.002-07:00

Name: Kaolin-Pectin (Kaopectate)

Class: Antidiarrheal Drug (Hydrophilic Agent/Absorbent)

Mechanism: Kaolin + pectin. Absorb water, bacteria, virus, toxins, bile acids. Decrease fluidity of formed stool.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: May increase water and electrolyte loss. May absorb nutrients, folate, drugs.

Utility: Treat diarrhea.

Special Features: Not terribly effective.

Docusates (Colace, Doxinate)

2008-05-11T11:00:00.001-07:00

Name: Docusates (Colace, Doxinate)

Class: Laxative

Mechanism: Anionic surfactant. Becomes emulsified w/stool ® softer feces, easier passage. Requires 1-3 days for action.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: May increase intestinal absorption of other drugs. Don’t use w/lubricant oils. May be mutagenic to cultured liver cells.

Utility: Laxative. Use limited to keeping stool soft.

Special Features: Only a minimal laxative effect at recommended dosage.

Lubricant Oils (mineral oil, olive oil, etc.)

2008-05-11T09:29:00.001-07:00

Name: Lubricant Oils (mineral oil, olive oil, etc.)

Class: Laxative

Mechanism: Coat stomach contents, change consistency of stool, reduce water absorption.

Absorption: Oral, enema.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Oil absorption ® foreign body rxn. Possible lipid pneumonia. Decreased absorption of fat-soluble nutrients.

Utility: Laxative. Mineral oil enemas relieve fecal impaction.

Special Features: Seldom given orally, as better agents are available.

Lactulose (Constilac, Cephulac)

2008-05-11T09:28:00.004-07:00

Name: Lactulose (Constilac, Cephulac)

Class: Laxative (Osmotic Laxative)

Mechanism: Galactose-fructose disaccharide ® osmotic effect in small intest. In colon, Metabolism. by bacteria to lactic, formic, and acetic acids ® osmotic effect.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Not for use in pts on low galactose diets. Antacids can block fecal acidification (® ¯ effect on portal-systemic encephalopathy). Neomycin interferes w/lactulose action.

Utility: 1° use = symptomatic treatment of portal-systemic encephalopathy assoc. w/chronic liver disease. Acidified feces ® NH₄⁺ excretion. Routine purgation.

Special Features: May be preferred for elderly patients for routine purgation, but expensive.

Castor Oil

2008-05-11T09:28:00.003-07:00

Name: Castor Oil

Class: Laxative (Contact Cathartic)

Mechanism: Broken down in small intest. to ricinoleic acid (anionic surfactant) ® gut irritation ® peristalsis. ¯ small intest. absorption of electrolytes and water, speed of transit through GI tract. Effective in as little as 2 hr.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Must not be used chronically ® ¯ nutrient absorption. Violent uterine and abdominal cramping.

Utility: Laxative

Special Features: Contact cathartics are most commonly involved in prolonged cathartic abuse. Should never be used > 1 wk of regular therapy. Not recommended for initial therapy.

Anthraquinones (senna, cascara, danthron, aloe)

2008-05-11T09:28:00.001-07:00

Name: Anthraquinones (senna, cascara, danthron, aloe)

Class: Laxative (Contact Cathartic) (Anthraquinone Cathartic)

Mechanism: Emodin, an anthraquinone, stimulates peristalsis in the colon. Effects take > 6 hr. to develop.

Absorption:

Dist.: Breast milk.

Metabolism.:

Excretion, t½: Partial kidney excretion (may color urine).

Toxicity/S.E.s: Excessive catharsis. Colored urine. Not to be used by nursing mothers.

Utility: Laxative

Special Features: Activated by intestinal microflora. More complete evacuation than diphenylmethanes. Contact cathartics are most commonly involved in prolonged cathartic abuse. Should never be used > 1 wk of regular therapy. Not recommended for initial therapy.

Bisacodyl Tannex (Clysodrast)

2008-05-11T09:27:00.002-07:00

Name: Bisacodyl Tannex (Clysodrast)

Class: Laxative (Contact Cathartic) (Diphenylmethane Cathartic)

Mechanism: Act on colon ® peristalsis.

Absorption: Enema.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Fluid and electrolyte depletion, abdominal cramping, Metabolismolic acidosis or alkalosis, hypocalcemia, tetany. Tannic acid in large amounts is hepatotoxic. Use caution w/multiple enemas. Don’t use in pts. w/colonic ulcers or in kids < style=""> Don’t use > 7.5 g at a time or > 10 g over 72 hr.

Utility: Preparation of colon for surgery or X-ray.

Special Features: Indiv. effective doses vary 4-8x. Acid/base indicator ® pink/red urine.

Bisacodyl (Dulcolax)

2008-05-11T09:27:00.001-07:00

Name: Bisacodyl (Dulcolax)

Class: Laxative (Contact Cathartic) (Diphenylmethane Cathartic)

Mechanism: Act on colon ® peristalsis. Effects take at least 6 hr. to manifest.

Absorption: Oral ® 5% absorption. Enema, suppositories (can be irritating).

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Fluid and electrolyte depletion, abdominal cramping, Metabolismolic acidosis or alkalosis, hypocalcemia, tetany. Potential for atonic colon w/prolonged use.

Utility: Preparation of colon for surgery or X-ray.

Special Features: Most useful contact cathartic. Indiv. effective doses vary 4-8x. Acid/base indicator ® pink/red urine. Contact cathartics are most commonly involved in prolonged cathartic abuse. Should never be used > 1 wk of regular therapy. Not recommended for initial therapy.

Phenolphthalein (Ex-Lax)

2008-05-11T07:33:00.001-07:00

Name: Phenolphthalein (Ex-Lax)

Class: Laxative (Contact Cathartic) (Diphenylmethane Cathartic)

Mechanism: Act on colon ® peristalsis. Effects take at least 6 hr. to manifest.

Absorption: Oral ® 15% absorption

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Fluid and electrolyte depletion, abdominal cramping, ashes, osteomalacia. Potential for atonic colon w/prolonged use.

Utility: Laxative.

Special Features: Indiv. effective doses vary 4-8x. Acid/base indicator ® pink/red urine. Not effective in pts. who lack bile. Contact cathartics are most commonly involved in prolonged cathartic abuse. Should never be used > 1 wk of regular therapy. Not recommended for initial therapy.

Sodium Phosphate

2008-05-11T07:32:00.005-07:00

Name: Sodium Phosphate

Class: Laxative (Saline Cathartic)

Mechanism: Nonabsorbable ions ® osmotic pressure in bowel ® watery stools in 1-3 hr.

Absorption: Not much.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Large amount of Na⁺ (prob. for pts. on low Na⁺ diets). Potential problem of dehydration.

Utility: Acute evacuation of bowel in preparation for endoscopic exam. Elim. of drugs/toxins for suspected drug/food poisoning.

Special Features:

Magnesium Citrate

2008-05-11T07:32:00.003-07:00

Name: Magnesium Citrate

Class: Laxative (Saline Cathartic)

Mechanism: Nonabsorbable ions® osmotic pressure in bowel ® watery stools in 1-3 hr.

Absorption: Not much.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Toxic levels of Mg²⁺ may accumulate in infants, old folk, and pts. w/impaired renal fxn. Large amount of Na⁺ (prob. for pts. on low Na⁺ diets). Potential problem of dehydration.

Utility: Acute evacuation of bowel in preparation for endoscopic exam. Elim. of drugs/toxins for suspected drug/food poisoning.

Special Features:

Magnesium Hydroxide

2008-05-11T07:32:00.001-07:00

Name: Magnesium Hydroxide

Class: Laxative (Saline Cathartic)

Mechanism: Nonabsorbable ions ® osmotic pressure in bowel ® watery stools in 1-3 hr.

Absorption: Not much.

Dist.:

Metabolism.:

Excretion, t½:

Utility: Acute evacuation of bowel in preparation for endoscopic exam. Elim. of drugs/toxins for suspected drug/food poisoning.

Special Features:

Polycarbophil

2008-05-11T07:31:00.000-07:00

Name: Polycarbophil

Class: Laxative (Bulk-Forming Agent)

Mechanism: Absorbs and retains water, increases fecal volume ® rate of transit.

Absorption: Not absorbed.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Can bind other drugs ® reduced absorption. Admin. > 1 hr before or after other medication.

Utility: Laxative. Esp. useful in pts. w/alternating constipation and diarrhea (e.g., irritable bowel synd) ® ¯ fluidity of liquid stools and softening of hard stools. Also useful for pts who are on low residue diets; are postpartum; are elderly; or have diverticular disease, spastic colon, or hemorrhoids.

Special Features: Inert, hydrophilic. Introduce gradually to avoid GI impaction. Gentle agent. Requires 1/2-3 days for effect.

Magnesium Sulfate

2008-05-11T04:28:00.008-07:00

Name: Magnesium Sulfate

Class: Laxative (Saline Cathartic)

Mechanism: Nonabsorbable ions® osmotic pressure in bowel ® watery stools in 1-3 hr.

Absorption: Not much.

Dist.:

Metabolism.:

Excretion, t½:

Utility: Acute evacuation of bowel in preparation for endoscopic exam. Elim. of drugs/toxins for suspected drug/food poisoning.

Special Features:

Psyllium (Metamucil)

2008-05-11T04:28:00.007-07:00

Name: Psyllium (Metamucil)

Class: Laxative (Bulk-Forming Agent)

Mechanism: Absorbs and retains water, increases fecal volume ® rate of transit.

Absorption: Not absorbed.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Can bind other drugs ® reduced absorption. Admin. > 1 hr before or after other medication.

Special Features: Inert, hydrophilic. Introduce gradually to avoid GI impaction. Gentle agent. Requires 1/2-3 days for effect.

Methylcellulose

2008-05-11T04:28:00.005-07:00

Name: Methylcellulose

Class: Laxative (Bulk-Forming Agent)

Mechanism: Absorbs and retains water, increases fecal volume ® rate of transit.

Absorption: Not absorbed.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Can bind other drugs ® reduced absorption. Admin. > 1 hr before or after other medication.

Special Features: Inert, hydrophilic. Introduce gradually to avoid GI impaction. Gentle agent. Requires 1/2-3 days for effect.

Tetracycline (Achromycin V)

2008-05-11T04:28:00.003-07:00

Name: Tetracycline (Achromycin V)

Class: Tetracycline

Mechanism: Active uptake into bacteria ®inhib protein synth by binding to 30S ribosome. Bacteriostatic

Absorption: Oral adequate, but incomplete. Impaired by divalent cations. IM painful. IV may cause thrombophlebitis. Never intrathecal.

Distrib.: Good CSF. Conc. in liver ® enterohepatic circ. Penetrates most tissues and fluids. Crosses placenta.

Metabolism.:

Excretion, t½: filtration (1°), bile

Toxicity/S.E.s: GI — burning, discomfort, nausea, vomiting; superinfection — due to broad spectrum, candida albicans (1°), staph enterocolitis, pseudomemb. colitis; hepatotoxicity (esp. in pregnancy); renal toxicity; Fanconi synd.; perm. brown discoloration of teeth; slowing of bone growth; phototoxicity; thrombophlebitis; hematopoetic changes; rare hypersens. rxns.

Utility: gram - cocci, gram - bacilli, acid fast bacilli, chlamydiae, mycoplasma, rickettsia, spirochetes. No effect on viruses or fungi. Also used for acne, prophylaxis for Travelers’ diarrhea. H. pylori (PUD).

Special Features: Broad spectrum. Decreased effect of oral contraceptives.

Amoxicillin (Amoxil)

2008-05-11T04:28:00.001-07:00

Name: Amoxicillin (Amoxil)

Class: Penicillin (Aminopenicillin)

Mechanism: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: Acid stable. Good oral (better than ampicillin).

Distrib.: Widely distributed, little CSF unless meninges inflamed.

Metabolism.:

Excretion, t½: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile.

Toxicity/S.E.s: diarrhea (less than ampicillin), hypersensitivity (1-10%), superinfection.

Utility: More effective against gram -s (esp. Proteus, H. influenzae, E. coli, P. mirabilis). Less active than Pen. G against gram+ cocci. H. pylori (PUD).

Special Features: Broad spectrum.

Pirenzipene

2008-05-11T04:27:00.001-07:00

Name: Pirenzipene

Class: -Muscarinic Antagonist

Mechanism: M₁-inhib. ® suppression of gastrin-stimulated and basal acid secretion at doses that have a minimal effect on salivary glands, heart, and eyes.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: PUD.

Special Features:

Metronidazole (Flagyl)

2008-05-10T08:15:00.004-07:00

Name: Metronidazole (Flagyl)

Class: Nitroimidazole derivative

Mechanism: Inhib. DNA synth, degrades DNA, e- acceptor for reduced substrates.

Absorption: Complete, quick oral absorption.

Dist.: Well distrib to all tissues and fluids (including CSF)

Metabolism.: Hepatic Metabolism.

Excretion, t½:

Toxicity/S.E.s: GI, metallic taste, neurotox (vertigo), disulfiram-like effect w/alcohol, neutropenia. Not for first trimester preg (mutagenic). Not for patients w/active CNS disease or hist. of blood dyscrasias.

Utility: IV treatment of anaerobic infects. Oral for amebiasis, giardiasis, and genital infects of Trichomonas vaginalis. H. pylori (PUD).

Special Features: Antiparasitic and antibacterial activity. All anaerobic cocci and anaerobic gram- bacilli, including Bacterioides. Trichomoniasis, amebiasis, giardiasis.

Sucralfate (Carafate)

2008-05-10T08:15:00.003-07:00

Name: Sucralfate (Carafate)

Class: Cytoprotective Agent

Mechanism: Complex of aluminum hydroxide and sulfated sucrose. Forms complex gels w/mucus ® physical barrier than impairs diffusion of HCl and prevents peptic mucus degradation. Stim. prostaglandin release and secretion of mucus and bicarbonate. Inhib. acid secretion by ~50%.

Absorption: Not absorbed.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Well tolerated.

Utility: PUD

Special Features: Largely supplanted by H2RAs and PPIs. Requires acidic pH for activation. \ should not be admin. w/antacids, PPIs, or H2RAs.

Bismuth-Subsalicylate (Pepto-Bismol)

2008-05-10T08:15:00.001-07:00

Name: Bismuth-Subsalicylate (Pepto-Bismol)

Class: Cytoprotective Agent/Hydrophilic Agent/Absorbent/Antimicrobial.

Mechanism: Inhib. pepsin activity, mucus secretion, coats & protects ulcer. Antimicrobial action. May have antiinflammatory action.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Binds tetracyclines. Turns stools and tongue black. Contains salicylate ® additive effects w/aspirin, tinnitus. Don’t use w/salicylate allergy. May cause GI impaction in debilitated patients.

Utility: PUD. Traveler’s Diarrhea (at least in Mexico)—8 doses (1-2 tablets every eight hours). Prophylaxis for Traveler’s Diarrhea. General diarrhea (usu. controls diarrhea w/in 24 hr).

Special Features:

Calcium Carbonate (Tums, Rolaids)

2008-05-10T08:14:00.005-07:00

Name: Calcium Carbonate (Tums, Rolaids)

Class: Antacid

Mechanism: Weak base ® ¯ gastric acidity. pH ® ¯ peptic activity.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: PUD

Special Features: Counterproductive—Ca²⁺ stimulates gastrin release.

Misoprostol (Cytotec)

2008-05-10T08:14:00.003-07:00

Name: Misoprostol (Cytotec)

Class: Prostaglandin Analogue (PGE₁)

Mechanism: Stim. mucus and bicarbonate secretion, mucosal blood flow, cell turnover. Inhib. acid secretion.

Absorption:

Dist.:

Metabolism.:

Excretion, t½: Longer t½ than natural prostaglandins.

Toxicity/S.E.s: intest. secretion ® diarrhea. Nausea. Uterine contractions. \ c/i during pregnancy.

Utility: PUD, prevention of NSAID injury.

Special Features:

Magnesium Hydroxide (Milk of Magnesia)

2008-05-10T08:14:00.001-07:00

Name: Magnesium Hydroxide (Milk of Magnesia)

Class: Antacid

Mechanism: Weak base ® ¯ gastric acidity. pH ® ¯ peptic activity.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Diarrhea.

Utility: PUD

Special Features:

Al-Mg Hydroxides

2008-05-10T04:49:00.004-07:00

Name: Al-Mg Hydroxides

Class: Antacid

Mechanism: Weak base ® ¯ gastric acidity. pH ® ¯ peptic activity.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Al³⁺ can form insoluble complexes w/other drugs ® ¯ absorption (e.g., tetracycline).

Utility: PUD

Special Features: Comb. of constipation (Al) and laxative (Mg) effects may cancel ® rel. normal bowel function.

Omeprazole (Prilosec)

2008-05-10T04:49:00.003-07:00

Name: Omeprazole (Prilosec)

Class: Proton Pump Inhibitor

Mechanism: Irreversible inhib. of H⁺/K⁺ ATPase ® > 95% inhib. of acid secretion.

Absorption: Oral ® 30-40% bioavail. Peak plasma levels at 0.5-3.5 hr. Give prior to meals, preferably in the morning. Additional dose, if necessary, should be given later in the day.

Dist.:

Metabolism.:

Excretion, t½: 0.5-1 hr.

Toxicity/S.E.s: Rare headache, diarrhea, rash. Inhib. of cyt. P-450 requires altered doses of warfarin, phenytoin, diazepam, and cyclosporin. Inhib. of vitamin. B12 absorption.

Utility: PUD, erosive esophagitis, Zollinger-Ellison synd., GERD.

Special Features: Mismatch between pharmacokinetics & pharmacodynamics. Short t½, but actions last > 24 hr (irreversible binding). Acid inhib. ® gastrin.

Aluminum Hydroxide (Maalox)

2008-05-10T04:49:00.001-07:00

Name: Aluminum Hydroxide (Maalox)

Class: Antacid

Mechanism: Weak base ® ¯ gastric acidity. pH ® ¯ peptic activity.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Constipation. Al³⁺ can form insoluble complexes w/other drugs ® ¯ absorption (e.g., tetracycline).

Utility: PUD

Special Features:

Famotidine (Pepcid)

2008-05-10T03:27:00.004-07:00

Name: Famotidine (Pepcid)

Class: H2 Receptor Antagonist

Mechanism: Competitive inhib. of the histamine H2 receptor, but not of the H1 receptor ® inhib. of fasting and stim. acid secretion. No disruption of circadian rhythm of acid secretion. Inhib. of 80-90% of gastrin and vagal-stim. acid secretion.

Absorption: Oral ® rapid, good absorption. Single nighttime dose.

Dist.:

Metabolism.: Partial hepatic Metabolism.

Excretion, t½: Excreted intact in urine. 1.5-3 hr.

Toxicity/S.E.s: Uncommon. Diarrhea, headaches, myalgias, skin rashes. Occasional cardiac arrhythmias (more common than in other H2RAs).

Utility: PUD, Zollinger-Ellison synd., acute stress ulcers, GERD

Special Features: Potency—famotidine > ranitidine/nizatidine > cimetidine. Tachyphylaxis—50% less effective after 6 months. Rebound hypersecretion 2° to receptor upregulation and inhib. of ATPase recycling.

Nizatidine (Axid)

2008-05-10T03:27:00.003-07:00

Name: Nizatidine (Axid)

Class: H2 Receptor Antagonist

Absorption: Oral ® rapid, good absorption. Single nighttime dose.

Dist.:

Metabolism.: Partial hepatic Metabolism.

Excretion, t½: Excreted intact in urine. 1.5-3 hr.

Toxicity/S.E.s: Uncommon. Diarrhea, headaches, myalgias, skin rashes. Occasional cardiac arrhythmias.

Utility: PUD, Zollinger-Ellison synd., acute stress ulcers, GERD

Cimetidine (Tagamet)

2008-05-10T03:27:00.001-07:00

Name: Cimetidine (Tagamet)

Class: H2 Receptor Antagonist

Absorption: Oral ® rapid, good absorption. Single nighttime dose.

Dist.:

Metabolism.: Partial hepatic Metabolism.

Excretion, t½: Excreted intact in urine. 1.5-3 hr.

Toxicity/S.E.s: Uncommon. Diarrhea, headaches, myalgias, skin rashes. Large doses over prolonged periods assoc. w/impotence & gynecomastia. Inhib. cyt. P-450 ® dose adjustment with phenytoin, warfarin, & theophylline. Occasional cardiac arrhythmias.

Utility: PUD, Zollinger-Ellison synd., acute stress ulcers, GERD

Ranitidine (Zantac)

2008-05-10T03:26:00.004-07:00

Name: Ranitidine (Zantac)

Class: H2 Receptor Antagonist

Absorption: Oral ® rapid, good absorption. Single nighttime dose.

Dist.:

Metabolism.: Partial hepatic Metabolism.

Excretion, t½: Excreted intact in urine. 1.5-3 hr.

Toxicity/S.E.s: Uncommon. Diarrhea, headaches, myalgias, skin rashes. Inhib. cyt. P-450 (less than cimetidine) ® dose adjustment with phenytoin, warfarin, & theophylline. Occasional cardiac arrhythmias.

Utility: PUD, Zollinger-Ellison synd., acute stress ulcers, GERD

Magnesium

2008-05-10T03:26:00.003-07:00

Name: Magnesium

Class: Antidysrhythmic Agent

Mechanism:

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: DOC for torsades de pointes (DILQT synd). Treat pts w/digitalis-induced arrhythmia if hypomagnesemia is present.

Special Features:

Adenosine (Adrenocard)

2008-05-10T03:26:00.001-07:00

Name: Adenosine (Adrenocard)

Class: Antidysrhythmic Agent

Mechanism: High doses ® ¯ conduction velocity, refractory period, ¯ automaticity in the AV node.

Absorption: IV

Dist.:

Metabolism.:

Excretion, t½: Extremely short duration of action (15 sec.).

Toxicity/S.E.s: Low toxicity. Flushing, chest pain, hypotension, transient dyspnea, non-myocardial chest discomfort, metallic taste.

Utility: DOC for acute supraventricular tachycardia. Treat AV nodal reentry, orthodromic tachycardia.

Special Features:

Amiodarone (Cordarone)

2008-05-10T03:25:00.001-07:00

Name: Amiodarone (Cordarone)

Class: Antidysrhythmic Agent (Class III)

Mechanism: Structurally related to thyroxine. 1° effect is prolongation of action potential and refractory period. Antiarrhythmic activity and antianginal activity.

Absorption: Oral.

Dist.:

Metabolism.:

Excretion, t½: 25-110 days.

Toxicity/S.E.s: Common (>75% of pts). Interstitial pulmonary fibrosis, GI intolerance, tremor, ataxia, dizziness, depression, nightmares, hallucinations, hyper/hypothyroidism, liver toxicity, photosensitivity, periph. neuropathy, muscle weakness, blue skin (I₂), possibly irreversible hepatic dysfxn. DILQT synd., sinus bradycardia. Asympt. corneal deposits in all pts. Substantial in LDL. Phospholipidosis. Enhances effect of warfarin. conc. of digoxin, quinidine, procainamide, et. al.

Utility: Treat severe refractory supraventricular and ventricular tachyarrhythmia.

Special Features: Usefulness limited by toxicity. Full effects may take up to 6 weeks to manifest.

Sotalol (Betapace)

2008-05-06T07:43:00.005-07:00

Name: Sotalol (Betapace)

Class: Antidysrhythmic Agent (Class III)

Mechanism: Blocks rapid outward K⁺ current (delayed rectifier) ® prolonged repolarization and action potential ® effective refractory period. Little effect on rate of depolarization. L-isomer is a potent b-blocker.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Rel. low rate of adverse effects. DILQT synd., sinus bradycardia.

Utility: Long-term therapy to decrease the rate of sudden death following acute MI. Modest ability to suppress ectopic beats and ¯ O₂ demand. Strong antifibrillary effect. Prevents arrhythmia and decreases mortality in pts. w/sustained ventricular tachycardia.

Special Features:

Flecainide (Tambocor)

2008-05-06T07:43:00.003-07:00

Name: Flecainide (Tambocor)

Class: Antidysrhythmic Agent (Class IC)

Mechanism: Slow dissociation from Na⁺ channels ® marked suppression of phase 0 upstroke ® marked slowing of conduction. threshold potential ® ¯ automaticity.

Absorption: Oral.

Dist.:

Metabolism.: Minimal.

Excretion, t½: 16-20 hr.

Toxicity/S.E.s: Long-term Rx ® mortality. Dizziness, blurred vision, tremor, agitation, headache, nausea. Aggravation of preexisting arrhythmias, negative inotropy, induction of life-threatening ventricular tachycardia (CAST proarrhythmia), aggravation of CHF, infranodal conduction block.

Utility: Treat refractory ventricular arrhythmias. Suppress premature ventricular contraction. Treat AV nodal reentry, WPW-related arrhythmia.

Special Features: Class IC drugs have the highest potency as Na⁺ channel blockers

Mexiletine (Mexitil)

2008-05-06T07:43:00.001-07:00

Name: Mexiletine (Mexitil)

Class: Antidysrhythmic Agent (Class IB)

Mechanism: Shortens phase 3 repolarization. Decreases action potential duration. Inhibits arrhythmias caused by abnormal automaticity. Rapid speed of dissociation from Na⁺ channels.

Absorption: Oral

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Proarrhythmic effects, negative inotropy, infranodal conduction block. N/v, dizziness, disorientation, tremor.

Utility: Chronic treatment of ventricular arrhythmias assoc. w/previous myocardial infarction.

Special Features: Concurrent use w/quinidine may be effective at lower doses than either alone ® ¯ adverse effects of each.

Tocainide (Tonocard)

2008-05-06T07:42:00.004-07:00

Name: Tocainide (Tonocard)

Class: Antidysrhythmic Agent (Class IB)

Mechanism: Shortens phase 3 repolarization. Little change in action potential duration. Inhibits arrhythmias caused by abnormal automaticity. Rapid speed of dissociation from Na⁺ channels.

Absorption: Oral

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Proarrhythmic effects, negative inotropy, infranodal conduction block. N/v, dizziness, disorientation, tremor. Hematologic effects (agranulocytosis, bone marrow suppression, thrombocytopenia) can be fatal.

Utility: Treat ventricular tachyarrhythmias (only as a last resort).

Special Features: Concurrent use w/quinidine may be effective at lower doses than either alone ® ¯ adverse effects of each.

Lidocaine (Zylocaine)

2008-05-06T07:42:00.003-07:00

Name: Lidocaine (Zylocaine)

Class: Antidysrhythmic Agent (Class IB)

Mechanism: Shortens phase 3 repolarization. Little change in action potential duration. Inhibits arrhythmias caused by abnormal automaticity. Rapid speed of dissociation from Na⁺ channels.

Absorption: IV

Dist.:

Metabolism.: Hepatic.

Excretion, t½:

Toxicity/S.E.s: Fairly wide therapeutic index. Proarrhythmic effects, negative inotropy, infranodal conduction block. Drowsiness, slurred speech, paresthesia, agitation, confusion, convulsions, resp. depression, tinnitus, muscle twitching, psychosis, seizures. CNS toxicity if used w/tocainide or mexiletine (e.g., seizures).

Utility: DOC for sustained ventricular tachycardia. Treat ventricular arrhythmias arising during myocardial ischemia or digitalis-induced VA.

Special Features: Class IB drugs have the lowest potency as Na⁺ channel blockers.

Disopyramide (Norpace)

2008-05-06T07:42:00.001-07:00

Name: Disopyramide (Norpace)

Class: Antidysrhythmic Agent (Class IA)

Mechanism: Binds to open and inactivated Na⁺ channels and prevents Na⁺ influx ® slowing of the rapid upstroke during phase 0. Also decreases the slope of phase 4 spontaneous depolarization. Prolongs repolarization. Inhibits arrhythmias due to normal automaticity. Intermed. speed of dissociation from Na⁺ channels. Peripheral vasoconstriction. The stereoisomers have opposite effects on repolarization.

Absorption:

Dist.:

Metabolism.: Hepatic.

Excretion, t½: Urine.

Toxicity/S.E.s: Proarrhythmic effects, negative inotropy, infranodal conduction block, DILQT. Anticholinergic effects—dry mouth, urinary retention, blurred vision, constipation. N/v/d, abd. pain. Less GI intolerance than quinidine.

Utility: Alt. to procainamide or quinidine for treatment of ventricular arrhythmia.

Special Features:

Procainamide (Pronestyl)

2008-05-06T07:41:00.000-07:00

Name: Procainamide (Pronestyl)

Class: Antidysrhythmic Agent (Class IA)

Absorption: Oral. IV rarely used, as hypotension occurs w/too rapid infusion.

Dist.: Excretion, t½: Urine. 2-3 hr.

Metabolism.: Hepatic ® active Metabolismolite NAPA ( duration of action potential).

Toxicity/S.E.s: Proarrhythmic effects, negative inotropy, infranodal conduction block, DILQT. Hypotension (ganglion-blocking activity). Chronic use ® reversible SLE-like synd. Depression, hallucination, psychosis, giddiness. Less GI intolerance than quinidine. Hypersensitivity rxns—fever, agranulocytosis, Raynaud’s synd., myalgias, rashes, digital vasculitis.

Utility: Treat atrial, AV junctional, & ventricular tachyarrhythmias. Maintain sinus rhythm after direct current cardioversion of atrial flutter or fibrillation. Prevent frequent ventricular tachycardia.

Quinidine (Quinidex)

2008-04-14T13:37:00.005-07:00

Name: Quinidine (Quinidex)

Class: Antidysrhythmic Agent (Class IA)

Absorption: Oral ® rapid, nearly complete absorption.

Dist.: Metabolism.: Excretion, t½:

Toxicity/S.E.s: Proarrhythmic effects, negative inotropy, infranodal conduction block, DILQT. Cinchonism—n/v/d, tinnitus, headache, vertigo, auditory/visual disturbances. Hypotension (a-blocking activity). digoxin levels. Hypersensitivity rxns—rash, fever, angioneurotic edema, hepatitis. Reversible thrombocytopenia.

Special Features:

Tranexamic Acid (Amstat)

2008-04-14T13:37:00.003-07:00

Name: Tranexamic Acid (Amstat)

Class: Thrombolytic Agent Antagonist

Mechanism: Competitive inhib. of plasminogen activation.

Absorption: Oral.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Used for hemostasis in pts. undergoing oral surgery who are being treated w/oral anticoagulants.

Special Features:

Aminocaproic Acid (Amicar)

2008-04-14T13:37:00.001-07:00

Name: Aminocaproic Acid (Amicar)

Class: Thrombolytic Agent Antagonist

Mechanism: Lysine analog. Binds to lysine sites on plasminogen and plasmin ® blocks binding of plasmin to fibrin.

Absorption: IV (slow injxn).

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Thrombi that form during treatment are not lysed. Thrombosis may become a problem.

Utility: Treat bleeding from fibrinolytic therapy.

Special Features:

Urokinase (Abbokinase)

2008-04-14T13:36:00.003-07:00

Name: Urokinase (Abbokinase)

Class: Antithrombotic Agent (Thrombolytic Agent)

Mechanism: Urinary-type single chain plasminogen activator. Isolated from cultured human kidney cells.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Hemorrhage.

Utility: Treat acute MI (w/in 6 hr. of symptoms), massive PE, acute proximal vein thromboses, occlusion of dialysis access sites and indwelling catheters, occlusion of prosthetic heart valves.

Special Features: Best results in pts. that receive therapy < style=""> Generally non-antigenic. Does not cause allergic rxns.

Tissue Plasminogen Activator, tPA (Activase)

2008-04-14T13:36:00.001-07:00

Name: Tissue Plasminogen Activator, tPA (Activase)

Class: Antithrombotic Agent (Thrombolytic Agent)

Mechanism: Recombinant product identical to endothelial tPA. Preferentially activates plasminogen that is bound to fibrin ® greater clot specificity and potentially less systemic fibrinolysis than w/streptokinase.

Absorption: IV. Prolonged admin. necessary (generally given over 3 hr.). “Accelerated” regimen admin. over 90 min. (2/3 given w/in 1^st 30 min.)

Dist.:

Metabolism.:

Excretion, t½: Short t½.

Toxicity/S.E.s: Hemorrhage.

Utility: Treat acute MI (w/in 6 hr. of symptoms), massive PE, acute proximal vein thromboses, occlusion of dialysis access sites and indwelling catheters, occlusion of prosthetic heart valves.

Special Features: Best results in pts. that receive therapy < style=""> Expensive—several times more costly than streptokinase.

Anistreplase/APSAC (Eminase)

2008-04-11T03:18:00.005-07:00

Name: Anistreplase/APSAC (Eminase)

Class: Antithrombotic Agent (Thrombolytic Agent)

Mechanism: Acylated plasminogen-streptokinase activator complex. Plasminogen active site is protected from inactivation. Poor thrombus specificity—catalyzes conversion of circulating & fibrin-bound plasminogen—results in a systemic lytic state.

Absorption: IV. Admin. w/large loading dose to overcome plasma antibodies.

Dist.: Metabolism.:

Excretion, t½: Longer t½ than streptokinase ® sustained fibrinolytic effect.

Toxicity/S.E.s: Hemorrhage. Allergic rxns—pruritis, flushing, urticaria. Higher incidence of allergic rxns. w/readministration. Pronounced hypotension (usu. transient). Delayed fever and arthralgia.

Utility: Treat acute MI (w/in 6 hr. of symptoms), massive PE, acute proximal vein thromboses, occlusion of dialysis access sites and indwelling catheters, occlusion of prosthetic heart valves.

Special Features: Best results in pts. that receive therapy < style=""> Pts. w/antibodies can develop therapeutic resistance.

Streptokinase (Streptase)

2008-04-11T03:18:00.003-07:00

Name: Streptokinase (Streptase)

Class: Antithrombotic Agent (Thrombolytic Agent)

Mechanism: Derived from b-hemolytic streptococci. Forms a complex w/plasminogen, exposing its active site. Poor thrombus specificity—catalyzes conversion of circulating and fibrin-bound plasminogen—results in a systemic lytic state.

Absorption: IV. Admin. w/large loading dose to overcome plasma antibodies.

Dist.:

Metabolism.:

Excretion, t½:

Utility: Treat acute MI (w/in 6 hr. of symptoms), massive PE, acute proximal vein thromboses, occlusion of dialysis access sites and indwelling catheters, occlusion of prosthetic heart valves.

Special Features: Best results in pts. that receive therapy < style=""> Pts. w/antibodies can develop therapeutic resistance.

Vitamin K1 (Phytonadione)

2008-04-11T03:18:00.001-07:00

Name: Vitamin K₁ (Phytonadione)

Class: Anticoagulant Antagonist

Mechanism: Vit. K is necessary for g-carboxylation of thrombin, factors VII, IX, & X, and proteins C & S. The g-carboxylated residues are required for binding Ca²⁺, which is essential for their activity.

Absorption: Oral or SC preferred. IV admin. may cause shock or anaphylaxis.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: IV admin. may cause shock or anaphylaxis.

Utility: Reverse excessive bleeding due to warfarin—indicated for severe or continued bleeding if warfarin dosage adjustment is unsuccessful.

Special Features: Significant improvement in hemostasis may require as long as 24 hr. If immediate hemostasis is necessary, fresh frozen plasma should be infused.

Warfarin (Coumadin)

2008-04-11T03:17:00.006-07:00

Name: Warfarin (Coumadin)

Class: Antithrombotic Agent (Oral Anticoagulant)

Mechanism: Vitamin K antagonist ® ¯ g-carboxylation of thrombin, factors, VII, IX, & X, and proteins C & S ® inhib. of synth. of active coagulation factors. Does not alter organized clots.

Absorption: Oral.

Dist.: Almost completely bound (99%) to plasma proteins (mainly albumin).

Metabolism.: Microsomal enzymes in liver and kidneys.

Excretion, t½: Urine and stool.

Toxicity/S.E.s: Hemorrhage, hypersensitivity rxns., fetal toxicity. “Purple Toe” synd. (necrosis) assoc. w/protein C deficiency. During pregnancy, can cause birth defects and abortion. Many drug interactions.

Utility: Prevention of recurrent thrombotic events following acute Rx w/heparin. Valvular heart disease, prosthetic cardiac valves, AMI, atrial fibrillation.

Special Features: Max. effects require 2-7 days. Init. response may be procoagulant due to inhib. of protein C. Should have 6 day overlap w/heparin. Monitor PT.

Antithrombin III (ATnativ)

2008-04-11T03:17:00.005-07:00

Name: Antithrombin III (ATnativ)

Class: Antithrombotic Agent (Coagulation Inhibitor)

Mechanism: Prepared from pooled human plasma. Inhibits coagulation factors (thrombin, IXa, Xa, XIIa).

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Treat pts w/hereditary AT-III deficiency and neonates w/a family history of AT-III deficiency. Prophylaxis for deficient pts who are undergoing surgery or delivery at term.

Special Features:

Protamine Sulfate

2008-04-11T03:17:00.003-07:00

Name: Protamine Sulfate

Class: Anticoagulant Antagonist

Mechanism: Binds tightly to heparin and rapidly reverses its effects. Also interacts w/platelets, fibrinogen, and other plasma proteins ® anticoagulant effect.

Absorption: IV infusion—slow rate.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Treat life-threatening hemorrhage 2° to heparin use.

Special Features: Use minimal effective dose.

Enoxaparin (Lovenox)

2008-04-11T03:17:00.001-07:00

Name: Enoxaparin (Lovenox)

Class: Antithrombotic Agent (Anticoagulant) (Low Molecular Weight Heparin)

Mechanism: Catalyzes complex formation btwn. plasma antithrombin III and various serine proteases of the coagulation pathway, including thrombin and activated factors IX, X, XI, & XII. Effect primarily due to thrombin inhib. Less effect on thrombin than heparin. Prevents further clot formation and thrombus propagation. Does not alter organized clots.

Absorp.: SC ® better bioavail. than heparin. Daily SC injxn has sim. efficacy to 2-3 injxns/d of heparin.

Dist.: Metabolism.: Hepatic.

Excretion, t½: Longer t½ than heparin. ¯ t½ w/pulm. embolism. t½ w/hepatic cirrhosis or end-stage renal disease.

Toxicity/S.E.s: 1° = bleeding. Thrombocytopenia (bovine > porcine)—mild, severe (delayed onset; can occur w/heparin resistance ® thromboembolism & DIC). Long-term use ® osteoporosis. Non-teratogenic, but discontinue prior to delivery.

Utility: 1° prevention of DVT after hip replacement surgery.

Special Features: Primarily used for venous thromboses. Monitor PTT to achieve desired dose—1.5-2.5x normal PTT is therapeutic. recurrence rate if PTT < style=""> Few drug interactions. Lower rate of bleeding than w/heparin.

Heparin

2008-04-11T03:16:00.001-07:00

Name: Heparin

Class: Antithrombotic Agent (Anticoagulant)

Mechanism: Catalyzes complex formation btwn. plasma antithrombin III and various serine proteases of the coagulation pathway, including thrombin and activated factors IX, X, XI, & XII. Effect primarily due to thrombin inhib. Prevents further clot formation and thrombus propagation. Does not alter organized clots.

Absorp.: IV, continuous IV®immed. onset. SC®1-2 hr onset w/variable bioavail.

Dist.: Metabolism.: Hepatic.

Excretion, t½: Rel. short t½. ¯ t½ w/pulm. embolism. t½ w/hepatic cirrhosis or end-stage renal disease.

Utility: Symptomatic calf vein thrombi or thrombi extending above the popliteal vein, pulm. embolus, atrial fibrillation, valvular heart disease, CAD, adjunct to post-MI thrombolytic therapy. Use in general surgery for E on oral contraceptives.

Special Features: Primarily used for venous thromboses. Most widely used antithromb. agent. Monitor PTT to achieve desired dose—1.5-2.5x normal PTT is therapeutic. recurrence rate if PTT < style=""> Few drug interactions.

Abciximab (Reo-Pro)

2008-04-08T10:25:00.001-07:00

Name: Abciximab (Reo-Pro)

Class: Antithrombotic Agent (Antiplatelet Agent)

Mechanism: Monoclonal antibody to GPIIb/IIIa. Interferes w/platelet-adhesive protein interactions.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Treat high risk angioplasty pts.

Special Features:

Ticlopidine (Ticlid)

2008-04-08T10:24:00.006-07:00

Name: Ticlopidine (Ticlid)

Class: Antithrombotic Agent (Antiplatelet Agent)

Mechanism: Unknown. Through some effect on platelet membranes, blocks ADP-induced aggregation. Interacts w/membrane glycoprotein IIb/IIIa.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Diarrhea, GI cramping, rash, LDL & VLDL, leukopenia, agranulocytosis, pancytopenia.

Utility: Treat thromboses in patients unable to take aspirin. May be more effective than aspirin in 2° prevention of stroke in pts w/previous TIA.

Special Features: Several days required for effects to develop. Effects persist for several days after cessation of treatment. As effective in E as in G. Antithrombotic use is primarily for arterial thromboses.

Dipyridamole (Persantine)

2008-04-08T10:24:00.005-07:00

Name: Dipyridamole (Persantine)

Class: Antithrombotic Agent (Antiplatelet Agent)

Mechanism: Inhib. PDE in platelets ® cAMP ® inhib. of platelet activation.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Prevention of systemic embolism in pts. w/prosthetic heart valves. Admin. in combination w/warfarin.

Special Features: When used alone, ineffective for Rx of cerebral or CV thrombotic events. Not proven to be of additional benefit when admin. w/aspirin. Antithrombotic use is primarily for arterial thromboses.

Acetylsalicylic Acid (Aspirin)

2008-04-08T10:24:00.003-07:00

Name: Acetylsalicylic Acid (Aspirin)

Class: Antithrombotic Agent (Antiplatelet Agent)

Mechanism: Irrevers. acetylation of cyclooxygenase ® ¯ platelet thromboxane synth.

Absorption: Oral ® rapid absorption.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: GI hemorrhage, hemorrhagic stroke. Use w/caution in pts on long-term oral anticoagulants. Hypersensitivity rxns—generalized urticaria, bronchial asthma, laryngeal edema, bronchoconstriction, hypotension, shock—may occur in 20-25% of pts w/asthma, nasal polyps, or chronic urticaria.

Utility: Acute MI, stable/unstable angina, 2° prevention in MI survivors. TIA. 2° prevention in nondisabling ischemic stroke. Prevention of saphenous vein bypass graft occlusion. Post-coronary angioplasty. 1° MI prophylaxis (325 mg/d) adjunctive to risk factor management. Headache.

Special Features: Low dose Rx optimal—75-325 mg/d. Antithrombotic use is primarily for arterial thromboses.

Amyl Nitrate

2008-04-08T10:24:00.001-07:00

Name: Amyl Nitrate

Class: Antianginal Agent (Organonitrate)

Mechanism: Converted to NO ® activation of cytosolic guanylate cyclase ® cGMP ® activation of cGMP-dependent protein kinase ® smooth muscle relaxation ® vasodilation. Greater effect in veins & large arteries than in resistance vessels ® ¯¯ preload, ¯ afterload ® ¯ work ® ¯ O₂ demand. Inhib. of platelet fxn.

Absorption: Inhalation ® rapid onset.

Dist.:

Metabolism.: Hepatic inactivation via glutathione-organic nitrate reductase.

Excretion, t½: Renal. Short duration of action (3-5 min.).

Toxicity/S.E.s: Orthostatic hypotension, tachycardia, severe throbbing headache, dizziness, flushing, syncope. C/i w/elevated ICP.

Utility: Treat angina. Not suitable for maintenance therapy.

Special Features:

Isosorbide Dinitrate (Isordil)

2008-04-08T10:23:00.000-07:00

Name: Isosorbide Dinitrate (Isordil)

Class: Antianginal Agent (Organonitrate)

Absorption: Sublingual preferred ® complete absorption. Oral ® 1^st pass Metabolism, low bioavail. Buccal/transdermal ® slow absorption.

Dist.:

Metabolism.: 80% converted to active Metabolismolite 5-ISMN before entering systemic circulation. Hepatic inactivation via glutathione-organic nitrate reductase.

Excretion, t½: Renal. 10 min. Short duration of action (20-30 min.).

Toxicity/S.E.s: Orthostatic hypotension, tachycardia, severe throbbing headache, dizziness, flushing, syncope. C/i w/elevated ICP.

Utility: Treat angina. Subling. not suitable for maintenance therapy. Oral/buccal/transdermal for prophylaxis, but may ® tolerance

Special Features: 8+ hr. breaks necessary to avoid tolerance from slow absorp.

Nitroglycerin (Nitro-Bid)

2008-04-08T10:22:00.001-07:00

Name: Nitroglycerin (Nitro-Bid)

Class: Antianginal Agent (Organonitrate)

Absorption: Sublingual preferred. IV. Oral ® 1^st pass Metabolism, low bioavail. Buccal/transdermal ® slow absorption.

Dist.:

Metabolism.: Hepatic (glutathione-organic nitrate reductase), extra-hepatic. Plasma clearance >> C.O.

Excretion, t½: Renal. 3 min. Short duration of action (20-30 min.).

Toxicity/S.E.s: Orthostatic hypotension, tachycardia, severe throbbing headache, dizziness, flushing, syncope. C/i w/elevated ICP.

Utility: Treat angina. Subling. not suitable for maintenance therapy. IV for severe recurrent unstable angina. Oral/buccal/transdermal for prophylaxis, but may ® tolerance.

Special Features: 8+ hr. breaks necessary to avoid tolerance from slow absorp.

Probucol (Lorelco)

2008-04-08T10:21:00.000-07:00

Name: Probucol (Lorelco)

Class: Blood Lipid-Lowering Agent (Fibric Acid Derivative)

Mechanism: Stim. LDL clearance by non-receptor pathways. May reduce risk of atherogenesis w/o altering serum cholesterol levels. May block oxidation of LDL. Moderate ¯ in cholesterol, LDL, & HDL. No effect on TG or VLDL.

Absorption:

Dist.: Stored in fat.

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Generally very well tolerated (2-6% incidence). Flatulence, n/v/d, abd. pain, headache, rash. C/i in monkeys (cardiac arrhythmias). Stored in fat. \ E advised to wait 6 mo. after last dose before becoming pregnant.

Utility: Treat hyperlipidemia IIA/IIB, but prob. not drug o’ first choice. May be useful for homozygous familial hypercholesterolemia (IIA). May cause regression of xanthomas.

Special Features: ¯ in LDL takes 1-3 mo., but some pts. don’t respond. Does not further reduce LDL when used w/lovastatin.

Clofibrate (Atromid-S) mnemonic

2008-04-07T08:45:00.004-07:00

Name: Clofibrate (Atromid-S) mnemonic

Class: Blood Lipid-Lowering Agent (Fibric Acid Derivative)

Mechanism: catabolism of VLDL, in part 2° to activity of lipoprotein lipase in adipose tissue. Moderate ¯ in TG & VLDL. Zero-mild ¯ in cholesterol. Zero-mild in HDL. Mild or ¯ in LDL.

Absorption:

Dist.:

Metabolism.: Glucuronide conjugation.

Excretion, t½: Renal excretion.

Toxicity/S.E.s: Generally well tolerated. Gallstones, nausea, diarrhea, abdominal discomfort. Displaces weakly acidic drugs (T3, T4, warfarin, phenytoin) from plasma proteins. Binds cholestyramine.

Utility: Treat severe hyperlipidemia IV refractory to gemfibrozil or niacin.

Special Features: Does not appear to decrease frequency of CHD-related incidents.

Gemfibrozil (Lopid) mnemonic

2008-04-07T08:45:00.003-07:00

Name: Gemfibrozil (Lopid) mnemonic

Class: Blood Lipid-Lowering Agent (Fibric Acid Derivative)

Mechanism: catabolism of VLDL, in part 2° to activity of lipoprotein lipase in adipose tissue. Moderate ¯ in TG & VLDL. Mild ¯ in LDL and cholesterol. Moderate in HDL.

Absorption:

Dist.:

Metabolism.: Glucuronide conjugation.

Excretion, t½: Renal excretion.

Toxicity/S.E.s: Generally well tolerated. GI distress, rash, musculoskeletal pain, blurred vision, anemia, leukopenia, gallstones. Adjust dose in pts. w/renal insufficiency.

Utility: DOC for hyperlipidemia III. Better tolerated than niacin for type IV, although less effective. Decreases frequency of CHD-related incidents.

Special Features:

Nicotinic Acid (Niacin)

2008-04-07T08:45:00.001-07:00

Name: Nicotinic Acid (Niacin)

Class: Blood Lipid-Lowering Agent

Mechanism: Reduces synth. rate of VLDL. Inhib. lipolysis of TG in adipocytes. Large ¯ in TG. Moderate ¯ in cholesterol & VLDL. Mild ¯ in LDL. Zero-moderate in HDL.

Absorption:

Dist.: Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Cutaneous flushing (92%), itching (49%), rashes (20%). Reduce w/aspirin pretreatment, admin. after meals, small init. dose gradually increased in size. Pruritis, dry skin, pigmentation, hepatotoxicity, n/v, dyspepsia, peptic ulceration, urinary frequency, dysuria, gout. High doses ® hepatic/pancreatic dysfxn. Coadmin. anti-hypertensives ® dizziness, syncope. Sustained-release preparations more commonly assoc. w/hepatotoxicity, dry eyes, pigmentation, hyperglycemia.

Utility: Prob. DOC for hyperlipidemias IV and V. Very useful for III. Can be used for II. Synergy w/resins.

Special Features:

Colestipol (Colestid)

2008-04-07T08:44:00.002-07:00

Name: Colestipol (Colestid)

Class: Blood Lipid-Lowering Agent (Resin)

Mechanism: Binds bile acids in intestine ® defecation of bile acids, conversion of cholesterol to bile acids, ¯ pool of hepatic cholesterol, activity of apoB/E receptor, LDL clearance, ¯ plasma cholesterol. Moderate ¯ in cholesterol & LDL. Mild in HDL. Zero-moderate in TG & VLDL.

Absorption: Oral. No absorption.

Dist.: Metabolism.: Excretion, t½:

Toxicity/S.E.s: Flatulence, constipation, gas, n/v, steatorrhea. Supersaturation of cholesterol in bile ® gallstones, need for cholecystectomy. ¯ bile ® ¯ absorption of lipid-soluble drugs/vitamins. Binds acidic drugs. Weak stim. of VLDL synth. Do not use in pts. w/hyperTG w/o concurrent TG-lowering agent.

Utility: Treat hyperlipidemia IIA/IIB. Use alone or w/niacin, probucol, or HMG CoA reductase inhib.

Special Features: GI S.E.s reduced if taken immediately prior to meals. ½ dose + Metamucil™ ® ¯ constipation & bloating, but sim. efficacy.

Cholestyramine (Cholybar)

2008-04-07T08:44:00.001-07:00

Name: Cholestyramine (Cholybar)

Class: Blood Lipid-Lowering Agent (Resin)

Absorption: Oral. No absorption.

Dist.: Metabolism.: Excretion, t½:

Toxicity/S.E.s: Up to 50% refuse to continue Rx. Flatulence, constipation, gas, n/v, steatorrhea. Supersaturation of cholesterol in bile ® gallstones, need for cholecystectomy. ¯ bile ® ¯ absorption of lipid-soluble drugs/vitamins. Binds acidic drugs. Weak stim. of VLDL synth. Do not use in pts. w/hyperTG w/o concurrent TG-lowering agent.

Utility: Treat hyperlipidemia IIA/IIB. Use alone or w/niacin, probucol, or HMG CoA reductase inhib.

Special Features: GI S.E.s reduced if taken immediately prior to meals. ½ dose + Metamucil™ ® ¯ constipation & bloating, but sim. efficacy.

Simvastatin (Zocor)

2008-04-07T08:43:00.002-07:00

Name: Simvastatin (Zocor)

Class: Blood Lipid-Lowering Agent (HMG CoA Reductase Inhibitor)

Mechanism: Inhib. of HMG CoA reductase ® ¯ cholesterol pool, apoB/E receptor activity, LDL clearance. Large reduction of cholesterol and LDL. Little/no ¯ in TGs, little/no in HDL, no change in VLDL.

Absorption: Dist.: Metabolism.: Excretion, t½:

Toxicity/S.E.s: Common mild GI disturbances. Reversible elevations of liver enzymes in 4-7% (if AST or ALT > 3x normal, discontinue). Possible muscle damage—much more likely w/concurrent cyclosporine, gemfibrozil, niacin, or erythromycin; or if pt has hepatic disease, a severe infxn, or renal insufficiency. Continued use w/myopathy may ® severe myositis, rhabdomyolysis, or acute renal failure. Can shorten sleep period by up to 18%. C/i in kids & preg. E.

Utility: Treat hyperlipidemia IIA/IIB refractory to diet and other drugs. May not be useful for pts. w/homozygous familial hypercholesterolemia.

Special Features: Most effective drug class for lowering LDL. Probably better tolerated than other cholesterol lowering drugs. Synergistic effects w/resins and niacin. If taken once/day, take at night (peak cholesterol synth. occurs between 12:00-3:00 a.m.).

Pravastatin (Pravochol)

2008-04-07T08:43:00.001-07:00

Name: Pravastatin (Pravochol)

Class: Blood Lipid-Lowering Agent (HMG CoA Reductase Inhibitor)

Absorption: Dist.: Metabolism.: Excretion, t½:

Utility: Treat pts. w/type IIA/IIB hyperlipidemia refractory to diet and other drugs. May not be useful for pts. w/homozygous familial hypercholesterolemia.

Lovastatin (Mevacor)

2008-04-07T08:42:00.000-07:00

Name: Lovastatin (Mevacor)

Class: Blood Lipid-Lowering Agent (HMG CoA Reductase Inhibitor)

Absorption: Dist.: Metabolism.: Excretion, t½:

Utility: Treat pts. w/type IIA/IIB hyperlipidemia refractory to diet and other drugs. May not be useful for pts. w/homozygous familial hypercholesterolemia.

Losartan (Cozaar)

2008-04-04T10:17:00.003-07:00

Name: Losartan (Cozaar)

Class: Angiotensin II Antagonist

Mechanism: Competitive inhib. of angiotensin II ® smooth muscle relaxation (vasodilation), ¯ Na⁺ & H₂0, ¯ plasma volume ® ¯ BP.

Absorption: Oral.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Hyperkalemia, fetal toxicity (c/i in 2^nd & 3^rd trimesters).

Utility: Treat hypertension.

Special Features: Angioneurotic edema and dry cough of ACE inhibitors not manifested.