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Title: Characterization of phentermine and related compounds as monoamine oxidase (MAO) inhibitors
Authors: Maher, Timothy J.
Wurtman, Richard J.
Uludağ Üniversitesi/Tıp Fakültesi/Farmakoloji ve Klinik Farmakolojisi Bölümü.
Ulus, İsmail H.
Keywords: Phentermine
Appetite-suppressant drugs
Valvular heart-disease
In-vivo microdialysis
Serotonin release
Obese patients
Weight control
Issue Date: 15-Jun-2000
Publisher: Pergamon-Elsevier Science Ltd
Citation: Ulus, İ. H. vd. (2000). "Characterization of phentermine and related compounds as monoamine oxidase (MAO) inhibitors". Biochemical Pharmacology, 59(12), 1611-1621.
Abstract: Phentermine was shown in the 1970s to inhibit the metabolism of serotonin by monoamine oxidase (MAO), but never was labeled as an MAO inhibitor; hence, it was widely used in combination with fenfluramine, and continues to be used, in violation of their labels, with other serotonin uptake blockers. We examined the effects of phentermine and several other unlabeled MAO inhibitors on MAO activities in rat lung, brain, and liver, and also the interactions of such drugs when administered together. Rat tissues were assayed for MAO-A and -B, using serotonin and beta-phenylethylamine as substrates. Phentermine inhibited serotonin-metabolizing (MAO-A activity in all three tissues with K-i values of 85-88 mu M. These potencies were similar to those of the antidepressant MAO inhibitors iproniazid and moclobemide. When phentermine was mixed with other unlabeled reversible MAO inhibitors (e.g. pseudoephedrine, ephedrine, norephedrine; estradiol benzoate), the degree of MAO inhibition was additive. The cardiac valvular lesions and primary pulmonary hypertension that have been reported to be associated with fenfluramine-phentermine use may have resulted from the intermittent concurrent blockage of both serotonin uptake and metabolism.
ISSN: 0006-2952
Appears in Collections:Web of Science

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