Ketoprofen Other names: 2-(3-Benzoylphenyl)propionic acid

Chemical formula: C₁₆H₁₄O₃  Molecular mass: 254.281 g/mol  PubChem compound: 3825

Pharmacodynamic properties

Ketoprofen is a non-steroidal anti-inflammatory drug. It has anti-inflammatory and analgesic actions.

It has the following pharmacological effects:

Anti-inflammatory:

It inhibits the development of carageenan-induced abscesses in rats at 1mg/kg, UV radiation induced erythema in guinea pigs at 6mg/kg. It is also a potent inhibitor of PGE2 and PFG2 synthesis in guinea pig and human chopped lung preparations.

Analgesic:

Ketoprofen effectively reduced visceral pain in mice caused by phenyl benzoquinone or by bradykinin following p.o. Administration at about 6 mg/kg.

Antipyretic:

Ketoprofen (2 and 6 mg/kg) inhibited hyperthermia caused by s.c injection of brewer’s yeast in rats and, at 1 mg/kg hyperthermia caused by i.v. administration of anticoagulant vaccine to rabbits.

Ketoprofen at 10 mg/kg i.v. did not affect the cardiovascular, respiratory, central nervous system or autonomic nervous systems.

Pharmacokinetic properties

Ketoprofen is slowly but completely absorbed from ketoprofen capsules. Maximum plasma concentration occurs after 6-8 hours. It declines thereafter with a half-life of about 8 hours. There is no accumulation on continued daily dosing.

Plasma and tissue levels of ketoprofen have been measured in 24 patients undergoing knee surgery. After repeated percutaneous administration of ketoprofen gel the plasma levels were about 60 fold less (9-39 ng/g) than those obtained after a single oral dose of ketoprofen (490-3300 ng/g). Tissue levels at the area of application were within the same concentration range for the gel as for the oral treatment, although the gel was associated with a considerably higher inter-individual variability.

The bioavailability of ketoprofen after topical administration has been estimated to be approximately 5% of the level obtained after an orally administered dose, based on urinary excretion data.

The protein binding in plasma is approximately 99%. Ketoprofen is excreted through the kidneys mainly as glucuronide conjugate.

Preclinical safety data

No additional data.

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