METHOTRIMEPRAZINE

Definition

A phenothiazine with pharmacological activity similar to that of both CHLORPROMAZINE and PROMETHAZINE. It has the histamine-antagonist properties of the antihistamines together with CENTRAL NERVOUS SYSTEM effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604)

Description

Methotrimeprazine is only found in individuals that have used or taken this drug. It is a phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604). Methotrimeprazine's antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition, its binding to 5HT2 receptors may also play a role.

Top Gene Interactions

General Information

Metabolism: Hepatic. Methotrimeprazine is metabolized in the liver and degraded to a sulfoxid-, a glucuronid- and a demethyl-moiety. Half Life: Approximately 20 hours.
Uses/Sources: For the treatment of psychosis, particular those of schizophrenia, and manic phases of bipolar disorder. As a potentiator of anesthetics: In general anesthesia where it can be used as both a pre- and post-operative sedative and analgesic. (L1857) As an anti-emetic: For the treatment of nausea and vomiting of central origin.(L1857) As a sedative: For the management of insomnia. (L1857)
Symptoms: Symptoms of overdose include convulsions, spastic movements, and coma.
Route of Exposure: Oral; parental (intramuscular). Methotrimeprazine has an incomplete oral bioavailability, because it undergoes considerable first-pass-metabolism in the liver. Oral bioavailability is approximately 50 to 60%.

Mechanism of Action

Methotrimeprazine's antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition, its binding to 5HT2 receptors may also play a role. Methotrimeprazine exerts its actions through a central adrenergic-blocking, a dopamine-blocking, a serotonin-blocking, and a anticholinergic blocking.

Target Name	Mechanism of Action	References
5-hydroxytryptamine receptor 2A 5-hydroxytryptamine receptor 2C Alpha-2A adrenergic receptor D(2) dopamine receptor D(4) dopamine receptor D(1A) dopamine receptor Alpha-2B adrenergic receptor D(1B) dopamine receptor Alpha-2C adrenergic receptor		6149771 10592235 15701205 2870716
Muscarinic acetylcholine receptor M1 Muscarinic acetylcholine receptor M2 Muscarinic acetylcholine receptor M3 Muscarinic acetylcholine receptor M4 Muscarinic acetylcholine receptor M5 5-hydroxytryptamine receptor 2B Alpha-1A adrenergic receptor D(3) dopamine receptor Histamine H1 receptor Alpha-1B adrenergic receptor Alpha-1D adrenergic receptor	Methotrimeprazine exerts its actions through a central adrenergic-blocking, a dopamine-blocking, a serotonin-blocking, and a anticholinergic blocking.	17139284 17016423 2899826