Pirlindole

322.42

226.32

DTXSID8048230

2933990090

79.71000

3.84390

1.29 g/cm3

145

422.6ºC at 760 mmHg

209.4ºC

0.0168 None

Store at RT

IRRITANT

Short-acting selective and reversible monoamine oxidase A inhibitors, such as pirlindole, are commonly well-tolerated during an overdose. When taken alone, the clinical course is usually well-tolerated and benign. Deaths from an overdose of this medication have more commonly observed during interactions with tyramine-rich foods tricyclic antidepressants (TCAs), or sympathomimetic drugs, and selective serotonin reuptake inhibitors (SSRIs). The clinical course of adverse effects from these conditions includes agitation, extreme tremor, followed by seizures and hyperthermia. Deaths occurred 3-16 hours after ingestion, after intractable seizure and/or hyperthermia and its sequelae, such as disseminated intravascular coagulation (DIC) and multi-organ failure.

97% binding to plasma proteins

For the treatment of major depression. It is being studied in the treatment of fibromyalgia pain syndrome. One study determined that the effect of pirlindole on sensorimotor performance while driving a motor vehicle shows many similarities to that of placebo. The drug appears to stimulate the central nervous system, rather than exhibit a sedative effect, like many antidepressants. Because of its selective, reversible inhibition of monoamine oxidase (MAO-A) and short half-life, unpleasant "cheese effects" are avoided. This refers to the effects of consuming tyramine-rich foods, such as cheese while medicated with monoamine oxidase inhibitors, leading to severe headaches and hypertension. of The available evidence supports pirlindole as a safe and effective treatment option for the management of depression and fibromyalgia syndrome.

Pirlindole regulates that metabolism of norepinephrine and catecholamines, leading to relief of depressive symptoms. The prevention of breakdown of these neuromodulators is thought to elevate mood.

Mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions. Several MONOAMINE OXIDASE INHIBITORS are useful as antidepressants apparently as a long-term consequence of their modulation of catecholamine levels. The tricyclic compounds useful as antidepressive agents (ANTIDEPRESSIVE AGENTS, TRICYCLIC) also appear to act through brain catecholamine systems. A third group (ANTIDEPRESSIVE AGENTS, SECOND-GENERATION) is a diverse group of drugs including some that act specifically on serotonergic systems. (See all compounds classified as Antidepressive Agents.)|A chemically heterogeneous group of drugs that have in common the ability to block oxidative deamination of naturally occurring monoamines. (From Gilman, et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p414) (See all compounds classified as Monoamine Oxidase Inhibitors.)|Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)

Well absorbed with a bioavailability of 90%.|Mainly renal, with 0.4-0.5% being excreted in the urine as unchanged drug in healthy males. Renal excretion was the main route of elimination of the metabolites in man.|High plasma clearance (450–1000 1/h) in one study.

The drug is metabolized significantly through the hepatic system. From studies in dogs and rats, pirlindole has a bioavailability of between 20 and 30% due to the hepatic first-pass effect on this medication. The rat eliminates mainly unconjugated drug while the dog eliminates mostly conjugated drug.

0.7±0.3 in one study of healthy volunteers

This drug is a selective and reversible inhibitor of monoamine oxidase A (also known as MAO-A). Its main mechanism of action is selective and reversible inhibition of monoamine oxidase A. Its secondary mechanism of action is the inhibition effect of noradrenaline and 5-hydroxytryptamine reuptake.

1,10-trimethylene-8-methyl-1,2,3,4-tetrahydropyrazino(1,2-a)indole