Tiaprofenic acid

Further Information

The effects of tiaprofenic acid on articular cartilage have been investigated in in-vitro experiments and in ex-vivo studies using different animal models of arthritis. Ex-vivo experiments on human chondrocyte cultures have also been conducted. In these experiments, tiaprofenic acid, in concentrations equivalent to the therapeutic dose, did not depress the biosynthesis of proteoglycans and did not alter the differentiation of proteoglycans secreted. The degradation of proteoglycan aggregates was inhibited. These results suggest a neutral or possibly beneficial effect of tiaprofenic acid on joint cartilage under experimental conditions. The clinical significance of these findings has been studied in a long term double-blind controlled study, in which tiaprofenic acid did not significantly increase the rate of radiological deterioration of joint space in patients with osteoarthritis of the knee.

Single dose studies: Following oral administration (max. at 90 mins). Plasma level zero at 24 hours. t_½ = 1.5–2 hours.

Repeated dose studies: Tiaprofenic acid is rapidly eliminated and there is no accumulation after repeated doses of 600mg/day in divided doses. Steady state after first day. No impairment of absorption in patients with RA undergoing long term therapy. There is no evidence of different pharmacokinetics in the elderly.

Protein Binding = 97–98%

Plasma clearance = 6 L/hour

Elimination = 60% of urine remainder in bile

Metabolites = there two main metabolites which account for about 10% of urinary excretion and have low pharmacological activity. The parent compound is excreted mostly in the form of acylglucuronide.

Not applicable.