Pyrazidole mesilate
Pyrazidole mesilate Uses, Dosage, Side Effects, Food Interaction and all others data.
This drug is classified as a reversible inhibitor of monoamine oxidase A enzyme (also known as a RIMA drug). It was developed and is currently used as an antidepressant in Russia. Its chemical structure is similar to metralindole, and it also shares pharmacological properties with this drug.
Pyrazidole mesilate is a selective, reversible inhibitor of monoamine oxidase (MAO) subtype A (MAO-A) that is approved in several European and non-European countries for the treatment of major depression. The antidepressant efficacy and safety of pirlindole have been demonstrated in numerous studies and, supported by many years of clinical experience in the treatment of depression. Pyrazidole mesilate's efficacy and safety have also been shown in the treatment of fibromyalgia.
Pyrazidole mesilate 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.
| Trade Name | Pyrazidole mesilate |
| Generic | Pirlindole |
| Pirlindole Other Names | Pirlindol, Pirlindole, Pirlindolum |
| Type | |
| Formula | C15H18N2 |
| Weight | Average: 226.323 Monoisotopic: 226.146998588 |
| Protein binding | 97% binding to plasma proteins |
| Groups | Experimental |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
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 .
How Pyrazidole mesilate works
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 .
Toxicity
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 .
Elimination Route
Well absorbed with a bioavailability of 90% .
Half Life
0.7±0.3 in one study of healthy volunteers
Clearance
High plasma clearance (450–1000 1/h) in one study.
Elimination Route
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 .
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