Indications
Inflammatory disorders including: Rheumatoid arthritis,
Osteoarthritis. Mild to moderate pain. Fever. Prophylaxis
of transient ischemic attacks and MI. Unlabeled
Use: Adjunctive treatment of Kawasaki disease.
Action
Produce analgesia and reduce inflammation and fever
by inhibiting the production of prostaglandins. Decreases
platelet aggregation. Therapeutic Effects:
Analgesia. Reduction of inflammation. Reduction of fever.
Decreased incidence of transient ischemic attacks
and MI.
Pharmacokinetics
Absorption: Well absorbed from the upper small intestine;
absorption from enteric-coated preparations
may be unreliable; rectal absorption is slow and variable.
Distribution: Rapidly and widely distributed;
crosses the placenta and enters breast milk.
Metabolism and Excretion: Extensively metabolized
by the liver; inactive metabolites excreted by the
kidneys. Amount excreted unchanged by the kidneys
depends on urine pH; as pH increases, amount excreted
unchanged increases from 2–3% up to 80%.
Half-life: 2–3 hr for low doses; up to 15–30 hr with
larger doses because of saturation of liver metabolism.
TIME/ACTION PROFILE (analgesia/fever
reduction)
ROUTE ONSET PEAK DURATION
PO 5–30 min 1–3 hr 3–6 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity to aspirin or
other salicylates; Cross-sensitivity with other NSAIDs
may exist (less with nonaspirin salicylates); Bleeding
disorders or thrombocytopenia; Pedi: May increase risk
of Reye’s syndrome in children or adolescents with viral
infections.
Use Cautiously in: History of GI bleeding or ulcer
disease; Chronic alcohol use/abuse; Severe hepatic or
renal disease; OB: Salicylates may have adverse effects
on fetus and mother and should be avoided during
pregnancy, especially during the 3rd trimester; Lactation:
Safety not established; Geri:qrisk of adverse reactions
especially GI bleeding; more sensitive to toxic levels.
Adverse Reactions/Side Effects
EENT: tinnitus. GI: GI BLEEDING, dyspepsia, epigastric
distress, nausea, abdominal pain, anorexia, hepatotoxicity,
vomiting. Hemat: anemia, hemolysis. Derm:
rash, urticaria. Misc: allergic reactions including ANAPHYLAXIS
and LARYNGEAL EDEMA.
Interactions
Drug-Drug: Mayqthe risk of bleeding with warfarin,
heparin, heparin-like agents, thrombolytic
agents, dipyridamole, clopidogrel, tirofiban, or
eptifibatide, although these agents are frequently used
safely in combination and in sequence. Ibuprofen:
may negate the cardioprotective antiplatelet effects of
low-dose aspirin. Mayqrisk of bleeding with cefotetan
and valproic acid. Mayqactivity of penicillins,
phenytoin, methotrexate, valproic acid, oral hypoglycemic
agents, and sulfonamides. Urinary
acidificationqreabsorption and mayqserum salicylate
levels. Alkalinization of the urine or the ingestion
of large amounts of antacidsqexcretion andpserum
salicylate levels. May blunt the therapeutic
response to diuretics and ACE inhibitors.qrisk of
GI irritation with NSAIDs.
Drug-Natural Products:qanticoagulant effect
and bleeding risk with arnica, chamomile, clove, feverfew,
garlic, ginger, ginkgo, Panax ginseng, and
others.
Drug-Food: Foods capable of acidifying the
urine (see Appendix K) mayqserum salicylate levels.
Route/Dosage
Pain/Fever
PO, Rect (Adults): 325–1000 mg every 4–6 hr (not
to exceed 4 g/day). Extended-release tablets—650
mg every 8 hr or 800 mg every 12 hr.
PO, Rect (Children 2–11 yr): 10–15 mg/kg/dose
every 4–6 hr; maximum dose: 4 g/day.
Inflammation
PO (Adults): 2.4 g/day initially;qto maintenance dose
of 3.6–5.4 g/day in divided doses (up to 7.8 g/day for
acute rheumatic fever).
PO (Children): 60–100 mg/kg/day in divided doses
(up to 130 mg/kg/day for acute rheumatic fever).
Prevention of Transient Ischemic Attacks
PO (Adults): 50–325 mg once daily.
Prevention of Myocardial Infarction/Antiplatelet
Effects
PO (Adults): 80–325 mg once daily. Suspected acute
MI—160 mg as soon as MI is suspected.
PO (Children): 3–10 mg/kg/day given once daily
(round dose to a convenient amount).
Kawasaki Disease
PO (Children): 80–100 mg/kg/day in 4 divided
doses until fever resolves; may be followed by maintenance
dose of 3–5 mg/kg/day as a single dose for up
to 8 wk.
Availability (generic available) A
Tablets: 81 mgOTC, 162.5 mgOTC, 325 mgOTC, 500
mgOTC, 650 mgOTC, 975 mgOTC. Chewable tablets:
80 mgOTC, 81 mgOTC. Chewing gum: 227 mgOTC.
Dispersible tablets: 325 mgOTC, 500 mgOTC. Entericcoated
(delayed-release) tablets: 80 mgOTC, 165
mgOTC, 300 mgOTC, 325 mgOTC, 500 mgOTC, 600
mgOTC, 650 mgOTC, 975 mgOTC. Extended-release tablets:
325 mgOTC, 650 mgOTC, 800 mg. Delayed-release
capsules: 325 mgOTC, 500 mgOTC. Suppositories:
60 mgOTC, 120 mgOTC, 125 mgOTC, 130 mgOTC,
150 mgOTC, 160 mgOTC, 195 mgOTC, 200 mgOTC,
300 mgOTC, 320 mgOTC, 325 mgOTC, 600 mgOTC,
640 mgOTC, 650 mgOTC, 1.2 gOTC. In combination
with: antihistamines, decongestants, cough
suppressantsOTC, opioids, and omeprazole (Yosprala).
See Appendix B.
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