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Phenmetrazine
Phenmetrazine is a stimulant of the phenylmorpholine class.1 It was first synthesized in 1952 and was originally used to suppress appetite in the treatment of obesity. It was withdrawn from the market in the 1980s because of widespread misuse and concerns about addiction. It can increase heart rate and blood pressure, and some consider its addiction potential greater than that of amphetamines.
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Duration
Subjective Effects
Pharmacology
Pharmacodynamics
In rat brain synaptosome assays, phenmetrazine promotes substrate release via norepinephrine and dopamine transporters, with much weaker activity at serotonin transporters.2 Its actions at norepinephrine and dopamine transporters have also been characterized as reuptake inhibition.3 It additionally inhibits monoamine oxidase.3 Phenmetrazine is inactive at vesicular monoamine transporter 2 (VMAT2), although the significance of this finding in humans is unclear. In rodents, it raises brain dopamine levels in a dose-dependent manner.
Pharmacokinetics
Phenmetrazine is readily absorbed through the gastrointestinal tract and buccal mucosa.4 Metabolism occurs primarily in the liver through CYP3A and CYP2D6, and the drug resists metabolism by monoamine oxidase. The described metabolic pathways include deamination, subsequent oxidation, and conjugation with glucuronic acid or glycine before excretion. Its reported elimination half-life is 16-31 hours. In three adult male subjects given radiolabeled phenmetrazine hydrochloride orally, an average of 70% of the radiolabel was excreted within 24 hours;5 about 19% of that excreted amount is unchanged drug, with the remainder consisting of metabolites. Immediate-release and sustained-release formulations have similar bioavailability and timing of peak onset, while sustained-release formulations release the drug more steadily and produce lower peak plasma concentrations.
Interactions
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Harm Potential
Addiction & Dependence
Psychological
HighPhenmetrazine is considered by some to have greater addiction potential than amphetamines, and available references describe widespread misuse, abuse, and market withdrawal due to misuse and addiction concerns.
Toxicity
Overdose may cause tachycardia, arrhythmias, hypertension, and cardiovascular collapse.
Overdose includes acute central nervous system stimulation.
History & Culture
Development and medical use
Phenmetrazine emerged from Thomä and Wick's search for an appetite suppressant without the side effects associated with amphetamine. It was first synthesized in 1952, and Boehringer-Ingelheim patented it in Germany that year. Pharmacological data were published in 1954, when it also entered…
Legality
International
Phenmetrazine has approved and illicit status, and was withdrawn from the market after prior anorectic use.
Article Status
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