Tenuate (Diethylpropion)
Tenuate®, Tenuate Dospan® | Depletite | Durad | Radtue
Classification:
Autonomic Agents
Psychotropic Agents
NOTE: Tenuate (Diethylpropion) is a C-IV controlled substance.
Description: Tenuate (Diethylpropion) is an oral, sympathomimetic amine that is used as an anorexiant agent. It is structurally and chemically related to the amphetamines. The pharmacologic effects of Tenuate (Diethylpropion) are also similar to amphetamines. Tenuate (Diethylpropion) is utilized in the short-term (up to 12 weeks) management of obesity. Clinical trials report greater weight loss in adult obese subjects treated with dietary management and anorexiants versus patients treated with diet and placebo alone. Weight loss is generally greatest in the first weeks of therapy and decreases in succeeding weeks. Diethylpropion is recommended for short term treatment of obesity; however, longer periods of therapy, up to 25 weeks, may be safely and successfully utilized without the development of tolerance or drug dependence. Diethylpropion was approved by the FDA in 1959 and is available in both immediate-release and sustained-release tablets. It is only indicated for use as monotherapy.
Mechanism of Action: Tenuate (Diethylpropion) is a sympathomimetic amine that possesses pharmacological properties similar to amphetamine. Although the exact mechanism of action has not been established, it is thought that appetite suppression is produced by a stimulant effect on the satiety center in the hypothalamic and limbic regions of the brain. Secondary actions include CNS stimulation and blood pressure elevation. Tenuate (Diethylpropion) acts primarily on adrenergic pathways to increase the release of norepinephrine from nerve terminals and inhibit its reuptake; therefore, it is considered an indirect-acting sympathomimetic. There is evidence that Tenuate (Diethylpropion) may also provide some direct stimulation of the nerve terminal to produce the pharmacologic response.
Pharmacokinetics: Tenuate (Diethylpropion) is administered orally. The 75 mg sustained-release tablet has more gradual release characteristics than three 25 mg tablets given in a single dose, based on studies of plasma levels obtained with each dosage form. Tenuate (Diethylpropion) is rapidly absorbed from the GI tract and is extensively metabolized through a complex mechanism of N-dealkylation and reduction. N-dealkylation is thought to be responsible for metabolizing 45-55% of the dose whereas reduction accounts for 20-25% of the metabolic processes. Many of the Tenuate (Diethylpropion) metabolites are active. Tenuate (Diethylpropion) and/or its metabolites are believed to cross the blood-brain-barrier and the placenta.
Tenuate (Diethylpropion) and its metabolites are excreted mainly by the kidneys. Within 48 hours after dosing, over 75% of the dose is recovered in the urine, 3-6% as unchanged drug, and 64-67% as metabolites. The plasma half-life of the diethylpropion metabolites is approximately 4-8 hours.
Related entries
Syndicate
|
