Pharmacology Mnemonics - Flash Cards

Name: Diflunisal (Dolobid)

Class: Salicylate.

Mechanism: Inhibition of cyclooxygenase ® inhibition of prostaglandin synthesis. Also inhib. of PMN adhesion, aggregation, & activation (ramifications uncertain).

Absorption: Oral. Absorbed from stomach and upper intestine. Peak conc. 2-3 hr.

Dist.: Weak acid (pKa <5). ~90% protein binding. Vd @ albumin Vd. No CNS.

Metabolism.: 1° = liver. Phase I (oxid.) & Phase II (conjug.).

Excretion, t½: Metabolismolites in urine. Renal failure ® retention of glucuronide Metabolismolites®potential for toxic accumulation of orig. compound. t½ = 11-15 hr. Clearance decreased w/renal impairment & in the elderly.

Toxicity/S.E.s: GI—esophagitis & esophageal strictures; gastroduodenal erosions, ulceration, hemorrhage, & perforation; ileal inflammation, strictures, hemorrhage, & perforation; colon hemorrhage and exacerbation of inflammatory bowel disease. Hypersensitivity—possible cross-reaction w/aspirin. Inhib. of platelet aggregation. Kidney—Na⁺ retention, hemodynamic renal failure, interstitial nephritis. CNS—dizziness, tinnitus, headache, aseptic meningitis. Overdose—Acute is less serious than w/aspirin, but may cause Metabolismolic acidosis & seizures.

Utility: Treat pain, inflammation, dysmenorrhea, patent ductus arteriosis, acute gout.

Name: Salicylamide

Class: Salicylate

Mechanism:

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: May exacerbate acute gout attacks.

Name: Methylsalicylate (Oil of Wintergreen)

Class: Salicylate

Mechanism:

Absorption: Absorbed transdermally.

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Used in foods…may be toxic.

Utility: Used in liniments for cutaneous counterirritation.

Special Features:

Name: Acetylsalicylic Acid/Aspirin

Class: Salicylate

Mechanism: Irrevers. acetylation of cyclooxygenase ® inhib. of prostaglandin synth. ® ¯ prostaglandins, thromboxanes, & prostacyclins ® analgesia, inhib. of platelet aggregation, anti-inflammatory effects, anti-pyresis, stim. of central resp. center.

Absorption: Rapidly absorbed in stomach and upper intestine. Also absorbed through skin. pKa = 3.5, so gastric acid ® ­ absorption. Enteric coating may delay absorption.

Dist.: pH-dependent passive (non-ionic) diffusion. Active transport in renal tubules. 90% bound to albumin.

Metabolism.: Hydrolyzed by tissue/blood esterases. Conjugated in liver.

Excretion, t½: Salicylate & Metabolismolites excreted in urine. pH-dependent—30% excretion in alkaline urine, 2% in acidic urine. Low doses (600 mg) = 1^st order; t½ = 3-5 hr. High doses (4 g/d) = 0 order, t½ = 15 hr.

Utility: Analgesia—mild-mod. pain, somatic pain. No dependence or tolerance. Low efficacy for visceral pain. Anti-inflammatory—also a Mechanism of analgesia. Anti-pyresis—inhib. bacterial pyrogens in CNS; blocks hypothalamic response to IL-1. ¯ Platelet aggregation—2° to inhib. of thromboxane synth.

Toxicity/S.E.s: GI bleeding and ulceration—usu. due to high doses, but may occur w/lower doses. Painless bleeding may cause iron-deficiency anemia. Hypersensitivity—usu. in patients w/nasal polyps, asthma, or chronic urticaria ® urticaria, angioedema, hypotension. Bleeding—C/i w/severe hepatic damage, vit. K deficiency, hemophilia. Hepatotoxicity w/CT disorders. May be involved in Reye’s Synd.; not recommended for kids w/chicken pox or influenza. Pregnancy—reduced birth weight, ­ perinatal mortality, ante/post-partum hemorrhage, prolonged gestation. Renal effects—low doses ® ¯ uric acid excretion; high doses ® ­ uric acid excretion. Poisoning—acute ® resp. alkalosis (hyperventilation), Metabolismolic acidosis (fixed anion). Correlates w/plasma conc. Chronic ® higher brain conc. than in acute poisoning; greater toxicity than plasma conc. would suggest. More resistant to treatment than acute poisoning.

Drug Interactions: Alcohol ® ­ gastric bleeding. Displacement of oral hypoglycemia drugs, NSAIDS, methotrexate, phenytoin, oral anti-coagulants, & sulfonamides from protein binding sites.

Special Features: May exacerbate acute gout attacks.