Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2018 Publisher: A/S GEA Farmaceutisk Fabrik, Edvard Thomsens Vej 14, 2300, Copenhagen S, Denmark
Pharmacotherapeutic group: Antiinflammatory and antirheumatic products
ATC code: M01AG02
NSAID with anti-inflammatory, analgesic, and antipyretic effects. Tolfenamic acid is a prostaglandin synthesis inhibitor and a leukotriene synthesis inhibitor.
Tolfenamic acid is absorbed quickly and almost completely after oral administration.
Hepatic first pass metabolism is as low as 15% (bioavailability 85%). Maximum plasma concentrations are reached after about 1-1½ hours. The half-life in plasma is about 2 hours. Tolfenamic acid is extensively bound to plasma proteins (99%). It is metabolised in the liver and tolfenamic acid as well as the metabolites is conjugated with glucuronic acid. About 90% of a given dose of tolfenamic acid is excreted in the urine as glucuronic acid conjugates, and about 10% is excreted in the faeces. Enterohepatic circulation exists.
The therapeutic index for tolfenamic acid is high, and gastrointestinal ulceration and kidney changes have only been seen with oral doses approximately 6-10 times the maximum therapeutic dose recommended for tolfenamic acid. In human volunteers, tolfenamic acid did not affect renal function.
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