Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1    Pharmacodynamic properties
Pharmacotherapeutic category: non-steroid anti-inflammatory drug for topical use.

Ketoprofen is an inhibitor of both the cyclooxygenase and lipoxygenase pathways. Inhibition of prostaglandin synthesis provides for potent anti-inflammatory, analgesic and antipyretic effects. Lipoxygenase inhibitors appear to attenuate cell mediated inflammation and thus retard the progression of tissue destruction in inflamed joints. In addition, ketoprofen is a powerful inhibitor of bradykinin (a chemical mediator of pain and inflammation), it stabilises lysosomal membranes against osmotic damage and prevents the release of lysosomal enzymes that mediate tissue destruction in inflammatory reactions.

Pharmacokinetic Properties

5.2    Pharmacokinetic properties

After oral administration of a single dose, maximum blood concentrations are achieved within        2 hours.
Ketoprofen plasma half-life ranges from 1 to 3 hours. Plasma protein binding is 60%-90%.
Elimination is mainly by urinary route and in glucuronated form; approximately 90% of the amount administered is excreted within 24 hours.
By cutaneous route, absorption is instead very low. In fact the percutaneous application of 50- 150 mg of ketoprofen produces plasma levels of the active ingredient of 0.08-0.15 μg/mL approx. 5-8 hours after application.

Fastum gel allows the site specific topical delivery of ketoprofen with very low plasma concentrations of drug. Therapeutic levels in the affected tissues provide relief from pain and inflammation, yet will satisfactorily overcome the problem of significant systemic unwanted effects.