Overview
DESCRIPTION Ketoprofen is a nonsteroidal anti-inflammatory drug. The chemical name for ketoprofen is (±)- m -Benzoylhydratropic acid with the following structural formula: Its molecular formula is C 16 H 14 O 3 , with a molecular weight of 254.29. It has a pKa of 5.94 in methanol:water (3:1) and an n-octanol:water partition coefficient of 0.97 (buffer pH 7.4).
Mechanism of Action
CLINICAL PHARMACOLOGY Ketoprofen is a nonsteroidal anti-inflammatory drug with analgesic and antipyretic properties. The anti-inflammatory, analgesic, and antipyretic properties of ketoprofen have been demonstrated in classical animal and in vitro test systems. In anti-inflammatory models ketoprofen has been shown to have inhibitory effects on prostaglandin and leukotriene synthesis, to have antibradykinin activity, as well as to have lysosomal membrane-stabilizing action. However, its mode of action, like that of other nonsteroidal anti-inflammatory drugs, is not fully understood. Pharmacodynamics Ketoprofen is a racemate with only the S enantiomer possessing pharmacological activity. The enantiomers have similar concentration time curves and do not appear to interact with one another.
Indications
- INDICATIONS AND USAGE Carefully consider the potential benefits and risks of ketoprofen extended-release capsules before deciding to use ketoprofen extended-release capsules. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals (see WARNINGS ). Ketoprofen extended-release capsules are indicated for the management of the signs and symptoms of rheumatoid arthritis and osteoarthritis.
Common Doses
- 300 mg
- 200 mg
- 150 mg
- 25 mL
Dosage
DOSAGE AND ADMINISTRATION Carefully consider the potential benefits and risks of ketoprofen extended-release capsules and other treatment options before deciding to use ketoprofen extended-release capsules. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals (see WARNINGS ). After observing the response to initial therapy with ketoprofen extended-release capsules, the dose and frequency should be adjusted to suit an individual patient’s needs. Concomitant use of ketoprofen extended-release capsules is not recommended.
Black Box Warning
Cardiovascular Thrombotic Events • Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. This risk may occur early in treatment and may increase with duration of use (see WARNINGS and PRECAUTIONS ). • Ketoprofen extended-release capsules are contraindicated in the setting of coronary artery bypass graft (CABG) surgery (see CONTRAINDICATIONS and WARNINGS ).
Contraindications
- CONTRAINDICATIONS Ketoprofen extended-release capsules are contraindicated in patients who have shown hypersensitivity to ketoprofen. Ketoprofen extended-release capsules should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic reactions to ketoprofen have been reported in such patients (see WARNINGS: Anaphylactoid Reactions and PRECAUTIONS: General: Preexisting Asthma ).
Side Effects
- ADVERSE REACTIONS The incidence of common adverse reactions (above 1%) was obtained from a population of 835 ketoprofen capsules-treated patients in double-blind trials lasting from 4 to 54 weeks and in 622 ketoprofen extended-release capsules treated (200 mg/day) patients in trials lasting from 4 to 16 weeks. Minor gastrointestinal side effects predominated; upper gastrointestinal symptoms were more common than lower gastrointestinal symptoms.
Interactions
- Drug Interactions The following drug interactions were studied with ketoprofen doses of 200 mg/day. The possibility of increased interaction should be kept in mind when ketoprofen immediate-release doses greater than 50 mg as a single dose or 200 mg of ketoprofen per day are used concomitantly with highly bound drugs. ACE Inhibitors Reports suggest that NSAIDs may diminish the antihypertensive effect of ACE-inhibitors. This interaction should be given consideration in patients taking NSAIDs concomitantly with ACE-inhibitors.