Trade Names:Ketoprofen- Capsules 50 mg- Capsules 75 mg- Capsules, extended-release 100 mg- Capsules, extended-release 150 mg- Capsules, extended-release 200 mgAPO-Keto (Canada)APO-Keto-E (Canada)APO-Keto SR (Canada)
Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.
Immediate-release form is released in the stomach; T max is 0.5 to 2 h. Sustained-release form is released in the small intestine; T max is 6 to 7 h. Bioavailability is approximately 90%. Food does not change AUC, but the rate of absorption for either form is slowed.
More than 99% protein bound, mainly to albumin. Vd is 0.1 L/kg.
Metabolic pathway is glucuronide conjugation. The metabolite is acylglucuronide, which can be converted back to the parent drug. There are no known active metabolites.
Oral immediate release t ½ is 2 to 4 h. Sustained-release t ½ is approximately 5.4 h. Cl is approximately 0.08 L/kg/h.
Within 30 min.
Persisted for up to 6 h.
Plasma and renal Cl are reduced and the unbound fraction increases.Hypoalbuminemia and Renal Function Impairment
Patients with these conditions may be at greater risk of adverse reactions due to increased fractions of free drug. Give these patients lower doses of the drug and monitor them closely.
Treatment of rheumatoid arthritis and osteoarthritis.Immediate-release form only
Treatment of mild to moderate pain and primary dysmenorrhea.OTC Use
Temporary relief of minor aches and pains associated with common cold, headache, toothache, muscular aches, backache, minor arthritis pain, menstrual cramps, and reduction of fever.
Treatment of juvenile rheumatoid arthritis, sunburn, migraine prophylaxis.
Patients in whom aspirin, iodides, or any NSAID have caused allergic-type reactions.
PO 75 mg 3 times daily or 50 mg 4 times daily; do not exceed 300 mg/day.Maintenance dose
Reduce initial dosage to 75 to 150 mg/day in elderly or disabled patients or those with renal function impairment.Sustained-release
PO 200 mg once daily can be used in patients already stabilized on that dose.Mild to Moderate Pain, Primary DysmenorrheaAdults
PO 25 to 50 mg every 6 to 8 h as needed; do not exceed 300 mg/day.OTC UseAdults
PO 12.5 mg with a full glass of liquid every 4 to 6 h. If pain or fever persists after 1 h, follow with 12.5 mg. Do not exceed 25 mg in a 4- to 6-h period or 75 mg in a 24-h period. Use the smallest effective dose.Children
PO Do not give to children younger than 16 yr of age unless directed by a health care provider.Mild To Severe Renal Function Impairment
Maximum recommended total daily dose is 150 mg. In patients with more severe renal function impairment (GFR less than 25 mL/min or end-stage renal impairment), the max total daily dose should not exceed 100 mg.Hepatic Function Impairment
For patients with impaired hepatic function and serum albumin concentration less than 3.5 g/dL, the max initial total daily dose should be 100 mg.
Store at room temperature in tightly closed, light-resistant container.
Increased risk of gastric erosion and bleeding.Aspirin
Additive GI toxicity.Cyclosporine
Nephrotoxicity of both agents may be increased.Lithium
Serum lithium levels may be increased.Methotrexate
Increased methotrexate levels.
May prolong bleeding time.
Peripheral edema; fluid retention; CHF.
Headache; dizziness; lightheadedness; drowsiness; vertigo.
Visual disturbances; stomatitis.
Peptic ulcer; GI bleeding; dyspepsia; nausea; diarrhea; constipation; abdominal pain; flatulence; anorexia; vomiting.
Bronchospasm; laryngeal edema; rhinitis; dyspnea.
Category B .
Excreted in breast milk.
Safety and efficacy not established.
Increased risk of adverse reactions.
Hypersensitivity may occur; use caution in aspirin-sensitive individuals because of possible cross-sensitivity.
Lower doses may be necessary.
Avoid sustained-release product.
Bleeding, ulceration or perforation can occur at any time, with or without warning symptoms.
Acute renal insufficiency, interstitial nephritis, hyperkalemia, hyponatremia and renal papillary necrosis may occur.
Drowsiness, dizziness, confusion, disorientation, lethargy, numbness, vomiting, gastric irritation, nausea, abdominal pain, headache, tinnitus, convulsions, acute renal failure.
Copyright © 2009 Wolters Kluwer Health.