Products
Benfluorex was marketed in many countries as Mediaxal (150 mg, Servier) until 1998. Today, it is no longer on the market. In France and other European countries, it was available as Mediator, among other products. Its approval was not withdrawn in France until 2009, although the risk for cardiotoxic side effects of comparable drugs such as fenfluramine had been known for more than 10 years. Benfluorex has been blamed for several thousand deaths and hospitalizations.
Structure and properties
Benfluorex (C19H20F3NO2, Mr = 351.4 g/mol) is a derivative of the slimming agent fenfluramine. It was present in drugs as racemate and benfluorex hydrochloride, a white powder that is sparingly soluble in water. It is biotransformed in the body to the active metabolite norfenfluramine.
Effects
Benfluorex (ATC A10BX06) is thought to have antidiabetic, appetite suppressant, lipid-lowering, and antiadipose properties. It increases cell sensitivity to insulin, thereby lowering blood glucose. It also increases the formation of glycogen.
Indications
Benfluorex has been used as adjunctive treatment in diabetes mellitus with obesity and as a lipid-lowering agent. It has also been used off-label as a slimming agent in nondiabetic patients.
Adverse effects
Serious possible adverse effects include valvular heart disease and pulmonary arterial hypertension.
