Levomepromazine

Levomepromazine

Basics

Levomepromazine, also known as methotrimeprazine, is a phenothiazine neuroleptic. It is a low-potency antipsychotic (about half as potent as chlorpromazine) with potent analgesic, hypnotic, and antiemetic properties used primarily in palliative care. As is typical of phenothiazine antipsychotics, levomepromazine is a "dirty drug," meaning that it exerts its effects by blocking a variety of receptors, including adrenergic receptors, dopamine receptors, histamine receptors, muscarinic acetylcholine receptors, and serotonin receptors. This is the reason for the high number of possible side effects.

Effect

Pharmacodynamics

The antipsychotic effect of methotrimeprazine is largely due to its antagonism at dopamine receptors in the brain. In addition, binding to 5HT2 receptors may also play a role. It also interacts with a variety of other receptors. However, these additional interactions are undesirable and can therefore result in many side effects.

Pharmacokinetics

Methotrimeprazine has incomplete oral bioavailability because it undergoes significant first-pass metabolism in the liver. Oral bioavailability is approximately 50 to 60%. Methotrimeprazine is metabolized in the liver and degraded to a sulfoxide, a glucuronide, and a demethyl moiety. The half-life is approximately 20 hours.

Toxicity

Side effects

The most common side effect is akathisia. Levomepromazine has marked sedative and anticholinergic/sympatholytic effects (dry mouth, hypotension, sinus tachycardia, night sweats) and may cause weight gain. These side effects usually preclude prescribing the drug in the doses needed for complete remission of schizophrenia, so it must be combined with a stronger antipsychotic. In any case, blood pressure and ECG should be monitored regularly.
Eine seltene, aber lebensbedrohliche Nebenwirkung ist das neuroleptische maligne Syndrom (NMS). Zu den Symptomen von NMS gehören Muskelsteifheit, Krämpfe und Fieber.

Toxicological data

LD50 (rat, oral): 1100 mg-kg-1

Chemical & physical properties

ATC Code N05AA02
Formula C19H24N2OS
Molar Mass (g·mol−1) 328,47
Physical State solid
PKS Value 9,19
CAS Number 60-99-1
PUB Number 3916
Drugbank ID DB01403

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 201

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

The content of this page is an automated and high-quality translation from DeepL. You can find the original content in German here.

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