Drug reference
(as′pir-in) Acuprin, Asaphen , Asatab , A.S.A. Ascriptin Enteric, Aspergum, Aspir-Low, Aspir-trin, Bayer Aspirin, Easprin, Ecotrin, Entrophen , Halfprin, Lowprin , Novasen , Rivasa , Sloprin, St. Joseph Adult, Zorpin
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Func. class.: Nonopioid analgesic, nonsteroidal antiinflammatory, antipy- retic, antiplatelet
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Chem. class.: Salicylate
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Do not confuse: Aspirin/Anacin Adult Low/Anacin-3
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ACTION: Blocks pain impulses by blocking COX-1 in CNS, reduces inflam- mation by inhibition of prostaglandin syn- thesis; antipyretic action results from vaso- dilation of peripheral vessels; decreases platelet aggregation
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USES: Mild to moderate pain or fever, including rheumatoid arthritis (RA), osteoarthritis, thromboembolic disor- ders; TIAs, rheumatic fever, post-MI, pro- phylaxis of MI, ischemic stroke, angina, acute MI, Kawasaki disease
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Unlabeled uses: Colorectal cancer pro- phylaxis, venous thromboembolism extended treatment to prevent recurrence
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CONTRAINDICATIONS: Preg- nancy, breastfeeding, children <12 yr, children with flulike symptoms, hypersen- sitivity to salicylates, tartrazine (FD&C yel- low dye #5), GI bleeding, bleeding disor- ders, vitamin K deficiency, peptic ulcer, acute bronchospasm, agranulocytosis, increased intracranial pressure, intracra- nial bleeding, nasal polyps, urticaria Precautions: Abrupt discontinuation, acet- aminophen/NSAIDs hypersensitivity, acid/ base imbalance, alcoholism, ascites, asthma, bone marrow suppression in elderly patients, dehydration, G6PD deficiency, gout, heart failure, anemia, renal/hepatic disease, pre/postoperatively, gastritis
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SIDE EFFECTS CNS: Confusion, seizures, headache, intracranial hemorrhage CV: Tachycardia, hypotension, dysrhyth- mias EENT: Tinnitus, hearing loss ENDO: Hypoglycemia, hypokalemia GI: Nausea, vomiting, GI bleeding, pan- creatitis, hepatotoxicity HEMA: Thrombocytopenia, leukopenia, DIC, increased PT, aPTT, bleeding time INTEG: Rash, urticaria, bruising SYST: Reye’s syndrome (children), ana- phylaxis, laryngeal edema, angioedema
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INTERACTIONS Increase: gastric ulcer risk—corticoste- roids, antiinflammatories, NSAIDs, alcohol Increase: bleeding—alcohol, plicamy- cin, cefamandole, thrombolytics, ticlopi- dine, clopidogrel, tirofiban, eptifibatide, anticoagulants; monitor for bleeding Increase: effects of insulin, methotrexate, thrombolytic agents, penicillins, phenyt- oin, valproic acid, oral hypoglycemics, sulfonamides; monitor for increased effects of each product Increase: salicylate levels—urinary acid- ifiers, ammonium chloride, nizatidine Increase: hypotension—nitroglycerin Decrease: effects of aspirin—antacids (high doses), urinary alkalizers, corti- costeroids; monitor for decreased effects Decrease: antihypertensive effect—ACE inhibitors, monitor B/P Decrease: effects of probenecid, spi- A ronolactone, sulfinpyrazone, sulfonyl- β-blockers, amides, NSAIDs, loop diuretics Drug/Herb Increase: risk of bleeding—feverfew, garlic, ginger, ginkgo, ginseng (Panax), horse chestnut Drug/Food Increase: risk of bleeding—fish oil (omega-3 fatty acids) • Foods that acidify urine may increase aspirin level Drug/Lab Test Increase: coagulation studies, LFTs, serum uric acid, amylase, CO2, urinary protein Decrease: serum potassium, cholesterol Interference: VMA, 5-HIAA, xylose toler- ance test, TSH, pregnancy test
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TREATMENT OF OVERDOSE: Lavage, monitor electrolytes, VS
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DOSAGE AND ROUTES Pain/fever • Adult: PO/RECT 325-1000 mg q4hr prn, max 4 g/day • Child 2-11 yr: PO 10-15 mg/kg/dose q4hr, max 4 g/day RA, osteoarthritis, other inflammatory conditions • Adult: PO 2.4 g/day in divided doses q4- 6hr, maintenance 3.6-5.4 g/day; EXTENDED RELEASE 650 mg q8hr or 800 mg q12hr; target salicylate level 150-300 mcg/mL Juvenile RA • Child: PO/RECT 90-130 mg/kg/day in divided doses, target salicylate level 150- 300 mcg/mL Thromboembolic disorders • Adult: PO 325-650 mg/day or bid Transient ischemic attacks • Adult: PO 50-325 mg/day (grade 1A) Evolving MI with ST segment elevation (STEMI) • Adult: PO 160-325 mg nonenteric, chewed and swallowed immediately, maintenance 75-162 mg daily MI, stroke prophylaxis • Adult: PO 50-325 mg/day Prevention of recurrent MI/ antiplatelet • Adult: PO 80-325 mg/day CABG • Adult: PO 325 mg/day starting 6 hr postprocedure, continue for 1 yr PTCA • Adult: PO 325 mg 2 hr before surgery, then 160-325 mg daily Prevention of colorectal cancer in those who are carriers of hereditary nonpolyposis colon cancer Lynch syndrome (unlabeled) Adult: PO 600 mg daily × 2 yr Venous thromboembolism to pre- vent recurrence (unlabeled) Adult: PO 100 mg/day
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Available forms: capsules 325 ; cap- sules extended release 162.5; tablets 81, 162.5, 325, 500, 650, 975 mg; chewable tablets 81 mg; suppository 60, 120, 150 , 160 , 200, 300, 600, 650 mg; enteric-coated tablets 81, 162 , 325, 500 mg; delayed-release tablets 81, 325, 500 mg
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Administer: PO route • Do not break, crush, or chew enteric product • Crushed or whole (regular PO prod- uct), chewable tablets may be chewed • With food or milk to decrease gastric symptoms; separate by 2 hr from enteric products • With 8 oz of water; sit upright for ½ hr after dose to facilitate product passing into stomach Rectal route • Place suppository in refrigerator for at least 30 min before removing wrapper
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Assess: • Pain: character, location, intensity; ROM before and 1 hr after administration • Fever: temperature before and 1 hr after administration • Hepatic studies: AST, ALT, bilirubin, creatinine if patient is receiving long- term therapy • Renal studies: BUN, urine creatinine; I&O ratio; decreasing output may indi- cate renal failure (long-term therapy) • Blood studies: CBC, Hct, HB, PT if pa- tient is receiving long-term therapy • Hepatotoxicity: dark urine, clay- colored stools, yellowing of skin, sclera, itching, abdominal pain, fever, diarrhea if patient is receiving long-term therapy • Allergic reactions: rash, urticaria; if these occur, product may have to be dis- continued; patients with asthma, nasal polyps, allergies: severe allergic reaction may occur • Ototoxicity: tinnitus, ringing, roaring in ears; audiometric testing needed be- fore, after long-term therapy • Salicylate level: therapeutic level 150- 300 mcg/mL for chronic inflammation • Beers: avoid chronic use in older adults; GI bleeding may occur • Pregnancy/breastfeeding: do not use in first trimester; may cause fetal harm; use only if benefits outweigh fetal risks (second/third trimester); avoid breastfeeding
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Evaluate: • Therapeutic response: decreased pain, inflammation, fever
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To report any symptoms of hepato toxicity, renal toxicity, visual changes, ototoxicity, allergic reactions, bleeding (long-term therapy) • To avoid if allergic to tartrazine • Not to exceed recommended dosage; acute poisoning may result • To read labels on other OTC prod- ucts because many contain aspirin, salicylates • That the therapeutic response takes 2 wk (arthritis) • To report tinnitus, confusion, diar- rhea, sweating, hyperventilation • To avoid alcohol ingestion; GI bleed- ing may occur • That patients who have allergies, nasal polyps, asthma may develop allergic re- actions • To discard tablets if vinegar-like smell is detected • That medication is not to be given to children or teens with flulike symptoms or chickenpox, because Reye’s syndrome may develop • To take with a full glass of water • Pregnancy/breastfeeding: to inform prescriber if pregnancy is planned or suspected; avoid breastfeeding
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PHARMACOKINETICS Enteric metabolized by liver; inactive metabolites excreted by kidneys; crosses placenta; excreted in breast milk; half- life 15-20 min, up to 30 hr in large dose; rectal products may be erratic; protein binding 90% PO: Onset 15-30 min, peak 1-2 hr, dura- tion 4-6 hr, well absorbed PO: Enteric coated: onset 10-30 min, duration 2-4 hr RECT: Onset slow, duration 4-6 hr
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• Child 2-11 yr: PO 10-15 mg/kg/dose q4hr, max 4 g/day RA, osteoarthritis, other inflammatory conditions
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• Child: PO/RECT 90-130 mg/kg/day in divided doses, target salicylate level 150- 300 mcg/mL Thromboembolic disorders
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