KETOPROFEN EXTENDED-RELEASE- ketoprofen capsule, extended release
Andrx Pharmaceuticals, Inc.
Rx Only
Cardiovascular Risk
NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction (MI), and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk (See �WARNINGS").
Ketoprofen extended-release capsules are contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery (See �WARNINGS").
Gastrointestinal Risk
NSAIDs cause an increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients are at greater risk for serious gastrointestinal (GI) events (See �WARNINGS").
DESCRIPTION
Ketoprofen is a nonsteroidal anti-inflammatory drug. The chemical name for ketoprofen is 2-(3-benzoylphenyl)-propionic acid with the following structural formula:
Image from Drug Label Content
Its molecular formula is C16 H14 O3 , 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).
Ketoprofen is a white or off-white, odorless, nonhygroscopic, fine to granular powder, melting at about 95�C. It is freely soluble in ethanol, chloroform, acetone, ether and soluble in benzene and strong alkali, but practically insoluble in water at 20�C.
Each ketoprofen extended-release 100 mg, 150 mg, or 200 mg capsule contains ketoprofen in the form of hundreds of coated pellets. The dissolution of the pellets is pH dependent with optimum dissolution occurring at pH 6.5-7.5. There is no dissolution at pH 1. In addition, each capsule contains the following inactive ingredients: black iron oxide, D&C Yellow 10, ethylcellulose, FD&C Blue 1, FD&C Blue 2, FD&C Red 40, gelatin, propylene glycol, shellac, starch, sucrose, talc, and titanium dioxide.
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.
