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Phendimetrazine (Bontril): Techincal information: Half-life, blood concentration, metabolism
Monday, February 13, 2006 9:13 am Email this article
This article contains techincal information for the diet drug phendimetrazine (Bontril) including the half-life of the drug, time to achieve peak levels in the blood, blood concentrations after a single dose, etc. Lipolysis: Phendimetrazine has a minor effect on releasing fat from fat cells
Phendimetrazine has a minor effect on lipolysis (releasing fat from fat cells) based on an in vitro study, that is a study done in a test tube. (Holmes et al, 1975)
The same study found that diethylpropion had a minor effect on lipolysis, whereas amphetamine, fenfluramine and cholorphentermine significantly stimulated lipolysis. (Holmes et al, 1975)
Time to reach peak blood levels: 1-2 hours
Phendimetrazine reaches peak blood levels 1-2 hours after oral administration. (Beckett and Raisi, 1996)
Blood levels: 70 ng/ml after 35 mg dose
Blood concentrations are 70 ng/ml after an oral dose of 35 mg. (Rudolph et al, 1983)
Half-life: 2 hours for immediate release, 9 hours for sustained-release
Phendimetrazine has an elimination half-life of about 2 hours for the immediate-release form (Beckett and Raisi, 1996; Rudolph et al, 1983) and 9 hours for the sustained-release form. (Muller et al, 1975)
Absorption: Completely absorbed
An oral dose of phendimetrazine is absorbed completely in the gastrointestinal tract. (Beckett and Raisi, 1996)
The drug was recovered in the urine as 30 percent unchanged, 30 percent as phenmetrazine, and 20 percent as the N-oxide. (Beckett and Raisi, 1996)
Metabolites include ephedrine
Apparently a small amount of phendimetrazine is metabolized into norephedrine, cathine, ephedrine and pseudoephedrine. (Cui et al, 1990)
Sustained-release vs immediate-release
The amount of drug and metabolites recovered in the urine was similar after a single dose of sustained-release phendimetrazine compared to three doses of immediate-release given four hours apart. (Beckett and Raisi, 1996)
Markowitz GS; Tartini A; D’Agati VD. Acute interstitial nephritis following treatment with anorectic agents phentermine and phendimetrazine. Clinical Nephrology, 1998 Oct, 50(4):252-4.
Rostagno C; Caciolli S; Felici M; Gori F; Neri Serneri GG. Dilated cardiomyopathy associated with chronic consumption of phendimetrazine. American Heart Journal, 1996 Feb, 131(2):407-9.
Young RE. Comparative study of phenmetrazine and phendimetrazine in the management of obesity. Curr Ther Res 1961 Aug;3(8):350-4.
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