Phendimetrazine
Adipost®, Adphen®, Anorex®, Bacarate®, Bontril PDM®, Bontril Slow Release®, Delcozine®, Di-Ap-Trol®, Elphemet®, Limit®, Melfiat®, Melfiat 105®, Obepar®, Obe-Tite®, Phen-70®, Phenzine®, Plegine®, Prelu-2®, Reducto®, Rexigen Forte®, Slim-Tabs®, Statobex®, Stodex®, Trimtabs® | Bock-Arate™ | Bontril® SR | Kraft-Pleg™ | Kraft-Stat 35™ | Phendiet™ | Rapdone™
Classification:
Autonomic Agents
Sympathomimetics
Psychotropic Agents
Psychostimulants
NOTE: Phendimetratizine is a schedule C-III controlled substance.
Description: Phendimetrazine is an oral, indirect-acting, nonamphetamine sympathomimetic amine. It is used as an anoretic agent for short-term (8 to 12 weeks) adjunct in the treatment of exogenous obesity. The pharmacologic effects of phendimetrazine are similar to amphetamines. Phendimetrazine is only indicated for use as monotherapy. This drug was approved by the FDA in 1961.
Mechanism of Action: Similar to amphetamines, phendimetrazine increases the release of norepinephrine and dopamine from nerve terminals and inhibits their reuptake. Clinical effects include CNS stimulation and elevation of blood pressure. Appetite suppression is believed to occur through direct stimulation of the satiety center in the hypothalamic and limbic region.
Tolerance to the anorexiant effects of phendimetrazine usually develops within a few weeks of starting therapy. The mechanism of tolerance appears to be pharmacodynamic in nature; higher doses of phendimetrazine are required to produce the same response. When tolerance develops to the anorexiant effects, it is generally recommended that phendimetrazine be discontinued rather than the dose increased.
Pharmacokinetics: Phendimetrazine is administered orally and is readily absorbed from the gastrointestinal tract. The absorption half-life is approximately the same for both regular-release and sustained-release formulations. This indicates a similar onset of action between sustained-release and regular-release dosage forms. The duration of action for regular-release forms is about 4 hours; the duration is prolonged for sustained-release formulations. Once in the systemic circulation, some of the drug is metabolized to phenmetrazine and phendimetrazine-N-oxide. The main route of elimination for unchanged drug and metabolites is the kidneys. The average elimination half-life for regular-release forms is about 1.9 hours and 9.8 hours for sustained-release forms.
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[ Revised 3/11/2005 11:22:00 AM ]
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