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Active ingredient: Benzphetamine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Adrenergic Agents
  • Dopamine Agents
  • Central Nervous System Agents

Dosage Forms

  • Tablet (scored)

Brands / Synonyms

Benzfetamine; Benzylamphetamine; Didrex; Didrex

Indications

For the management of exogenous obesity as a short term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction

Pharmacology

Benzphetamine, a phenylalkylamin, is related to amphetamine both chemically and pharmacologically. It is an anorectic agent indicated in the management of exogenous obesity as a short term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction. Benzphetamine is a sympathomimetic amine with pharmacologic activity similar to the prototype drugs of this class used in obesity, the amphetamines. Actions include central nervous system stimulation and elevation of blood pressure. Tachyphylaxis and tolerance have been demonstrated with all drugs of this class in which these phenomena have been looked for.

Mechanism of Action

Although the mechanism of action of the sympathomimetic appetite suppressants in the treatment of obesity is not fully known, these medications have pharmacological effects similar to those of amphetamines. Amphetamine and related sympathomimetic medications (such as benzphetamine) are thought to stimulate the release of norepinephrine and/or dopamine from storage sites in nerve terminals in the lateral hypothalamic feeding center, thereby producing a decrease in appetite. This release is mediated by the binding of benzphetamine to centrally located adrenergic receptors.

Absorption

Readily absorbed from the gastro-intestinal tract and buccal mucosa. It Is resistant to metabolism by monoamine oxidase.

Toxicity

LD50=160 mg/kg (orally in rats). Acute overdosage may result in restlessness, tremor, tachypnea, confusion, assaultiveness, and panic states.

Biotrnasformation / Drug Metabolism

Hepatic. Benzphetamine's metabolites include amphetamine and methamphetamine.

Contraindications

DIDREX Tablets are contraindicated in patients with advanced arteriosclerosis, symptomatic cardiovascular disease, moderate to severe hypertension, hyper-thyroidism, known hypersensitivity or idiosyncrasy to sympathomimetic amines, and glaucoma. Benzphetamine should not be given to patients who are in an agitated state or who have a history of drug abuse.

Hypertensive crises have resulted when sympathomimetic amines have been used concomitantly or within 14 days following use of monoamine oxidase inhibitors. DIDREX should not be used concomitantly with other CNS stimulants.

DIDREX may cause fetal harm when administered to a pregnant woman. Amphetamines have been shown to be teratogenic and embryotoxic in mammals at high multiples of the human dose. DIDREX is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.

Drug Interactions

Hypertensive crises have resulted when sympathomimetic amines have been used concomitantly within14 days following use of monoamine oxidase inhibitors. DIDREX should not be used concomitantly with other CNS stimulants.

Amphetamines may decrease the hypotensive effect of antihypertensives. Amphetamines may enhance the effects of tricyclic antidepressants.

Urinary alkalinizing agents increase blood levels and decrease excretion of amphetamines. Urinary acidifying agents decrease blood levels and increase excretion of amphetamines.

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