EPHEDRINE - ORAL side effects, medical uses, and drug interactions.

Ephedrine is the brand name of the popular prescription diet drug sibutramine hydrochloride monohydrate, which is manufactured by Abbott Laboratories. Ephedrine is administered orally in capsules, and is the first serotonin reuptake inhibitor used for the treatment of obesity.

Ephedrine is well absorbed from the GI tract (77%), but undergoes considerable first-pass metabolism reducing its bioavailability. The drug itself reaches its peak plasma level after 1 hour and has also a half-life of 1 hour. Sibutramine is metabolized by cytochrome P450 izozyme CYP3A4 resulting in 2 active primary and secondary amines (called active metabolites 1 and 2) with half-lives of 14 and 16 hours, respectively. Peak plasma concentrations of active metabolites 1 and 2 are reached after 3 to 4 hours. The following metabolic pathway mainly results in two inactive conjugated and hydroxylated metabolites (called metabolites 5 and 6). Metabolites 5 and 6 are mainly excreted in the urine.

Ephedrine (sibutramine hydrochloride monohydrate) is a prescription diet drug first marketed to the public in February 1998. Ephedrine works by altering brain chemistry to make the person using it feel full. One of the most heavily advertised drugs since its appearance on the market, it has been widely prescribed to induce and maintain weight loss. Since 1998 there have been approximately 400 adverse events reported to the FDA associated with the use of Ephedrine.

Prior to its approval for sale in the United States, clinical trials of the drug showed that it could have adverse effects on patients' heart rate and blood pressure. In fact, in October 1996, Knoll Pharmaceuticals, the company that created Ephedrine, withdrew its request for FDA approval of a 30mg dose of Ephedrine, because the drug induced heart complications. The FDA recommended that the company also withdraw their application for approval of 20mg doses. Despite these strong early warning signs the company proceeded to seek approval for and market 5mg, 10mg and 15mg doses of Ephedrine. Subsequent data shows that the average yearly weight loss for patients taking Ephedrine is only six and a half pounds greater than patients who don't take Ephedrine.

The effectiveness of Ephedrine as a diet drug has also been questioned in addition to its safety. When the FDA approved Ephedrine in November 1997, it stated that the average weight loss in Ephedrine patients over the course of one year was only 6 1/2 pounds over the placebo group.