Tranylcypromine: A review

Atkinson, Roland; Ditman, Keith S.

doi:10.1002/cpt196565631

Cited by 65 publications

(33 citation statements)

References 35 publications

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“…This molecule had been synthesized in 1948 by Alfred Burger and William L. Yost, as an analogue of amphetamines (trans-dl-2-phenyl-cyclopropylamine sulphate) [46], but its MAOI action was not discovered until 1959, in Smith, Kline & French Laboratories [42,47]. Precisely because tranylcypromine was not, like isoniazid and iproniazid, a hydrazine derivative, its clinical interest increased enormously, as it was thought it might have a more acceptable safety profile than that of the previous MAOIs [48]. By the mid-1980s, tranylcypromine and phenelzine together accounted for over 90% of the market in MAOIs [49].…”

Section: The Saga Moves Onmentioning

confidence: 93%

Monoaminergic Neurotransmission: The History of the Discovery of Antidepressants from 1950s Until Today

López-Muñoz

Álamo²

2009

CPD

354

204

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The 1950s saw the clinical introduction of the first two specifically antidepressant drugs: iproniazid, a monoamine-oxidase inhibitor that had been used in the treatment of tuberculosis, and imipramine, the first drug in the tricyclic antidepressant family. Iproniazid and imipramine made two fundamental contributions to the development of psychiatry: one of a social-health nature, consisting in an authentic change in the psychiatric care of depressive patients; and the other of a purely pharmacological nature, since these agents have constituted an indispensable research tool for neurobiology and psychopharmacology, permitting, among other things, the postulation of the first aetiopathogenic hypotheses of depressive disorders. The clinical introduction of fluoxetine, a selective serotonin reuptake inhibitor, in the late 1980s, once again revolutionized therapy for depression, opening the way for new families of antidepressants. The present work reviews, from a historical perspective, the entire process that led to the discovery of these drugs, as well as their contribution to the development of the neuroscientific disciplines. However, all of these antidepressants, like the rest of those currently available for clinical practice, share the same action mechanism, which involves the modulation of monoaminergic neurotransmission at a synaptic level, so that the future of antidepressant therapy would seem to revolve around the search for extraneuronal non-aminergic mechanisms or mechanisms that modulate the intraneuronal biochemical pathways.

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Section: The Saga Moves Onmentioning

confidence: 93%

Monoaminergic Neurotransmission: The History of the Discovery of Antidepressants from 1950s Until Today

López-Muñoz

Álamo²

2009

CPD

354

204

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“…(ii) Aoyama (1 1) described an increase in norepinephrine and dopamine contents in infarcted and noninfarcted heart muscles of dogs treated with 15 pg/kg of nitroglycerin. Tranylcypromine was able to cause demonstrable accumulation of catecholamines in different animals in much smaller doses than used in our study (5,12).…”

Section: The Effect Of Nitroglycerin and Tranylcy-mentioning

confidence: 56%

Metabolic Effects of Nitroglycerin and Tranylcypromine in Unanesthetized Rabbits

Kypson

Hait

1971

Experimental Biology and Medicine

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Monoamine oxidase (MAO) inhibitors are compounds of different chemical structure which prevent the intracellular degradation of catecholamines and 5-hydroxytryptamine, and thus produce an accumulation of these amines in tissues such as brain (1), sympathetic ganglia (2), heart (3), and adipose tissue (4).I t is known that catecholamines regulate the rate of lipolysis and glycolysis in tissues through specific receptors. The increased availability of these amines for receptor sites following M A 0 inhibition might result in higher rates od these metabolic pathways. Increased glycolysis in rats treated with different types of M A 0 inhibitors was described by Gey and Pletscher (5). Recently, Kypson et a2. (6) demonstrated higher lipolytic activity in rats injected with pargyline and tranylcypromiae, both MA0 inhibitors.The possibility that the vasodilators of the nitrite type belong to the class of M A 0 inhibitors was suggested by Ogawa et al. ( 7 ) , who observed inhibition of MA0 activity in heart, liver, and brain of nitroglycerin-treated rats. The purpose of the present study was to compare the metabolic alterations caused by nitroglycerine with those of tranylcypromine in rabbits. Propranold, an inhibitor of beta receptors and reserpine, a catecholamine depleting agent, were used to determine whether the effects of nitroglycerin or tranylcypromine were mediated by catecholamines.Methods. Unanesthetized albino rabbits of both sexes, weighting 2.0-3.5 kg and starved for 16 hr before the experiment, were used.

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“…In patients with severe hepatic impairment, tranylcypromine and moclobemide dosages should be reduced by one-third to one-half in such patients [62,81].…”

Section: Dosage and Administrationmentioning

confidence: 98%

Clinical Applications of MAO-Inhibitors

Riederer

Lachenmayer²,

Laux³

2004

Current Medicinal Chemistry

204

115

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Monoamine oxidase inhibitors (MAO-I) have been useful in the treatment of both psychiatric and neurological disorders over centuries. Here we focus on the development of this drug treatment. Focus is given on the use of irreversible MAO-I's as well as on reversible ones. Benefit and side effects are reported for Parkinson's disease, Alzheimer's dementia, depression syndrome and panic disorders. The preclinical and clinical effects of selegiline with regard to neuroprotection are highlightened and the conclusion is drawn that there is good evidence for a clinical neuroprotective capacity based on the assumption that the 50 percent recovery of MAO-B is obtained already after a 10 days withdrawal of selegiline. There is also a focus on selegilines metabolism to amphetamine and metamphetamine. In order to avoid any such effects of metabolic compounds on the cardiovascular system Zydis Selegiline, a melt-tablet avoid of major metabolism to amphetamine and metamphetamine is described in detail. Developments in MAO-I research are discussed in detail as there are moclobemide, lacabemide, rasagiline. Interactions of MAO-I' with tricyclics and serotonin selective reuptake inhibitors (SSRI's) are described as there is mentioning of interactions of MAO-I's with other compounds in general. Tables and figures report on clinical studies and on pharmacological properties of MAO-I's.

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Tranylcypromine: A review

Cited by 65 publications

References 35 publications

Monoaminergic Neurotransmission: The History of the Discovery of Antidepressants from 1950s Until Today

Monoaminergic Neurotransmission: The History of the Discovery of Antidepressants from 1950s Until Today

Metabolic Effects of Nitroglycerin and Tranylcypromine in Unanesthetized Rabbits

Clinical Applications of MAO-Inhibitors

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