Propiomazine

Medical uses

Propiomazine has been used in the treatment of insomnia.

Side effects

Drowsiness is a usual side effect. Rare, serious side effects include convulsions (seizures); difficult or unusually fast breathing; fast or irregular heartbeat or pulse; fever (high); high or low blood pressure; loss of bladder control; muscle stiffness (severe); unusual increase in sweating; unusually pale skin; and unusual tiredness or weakness.

Pharmacology

Pharmacodynamics

Propiomazine is an antagonist of the dopamine D1, D2, and D4 receptors, the serotonin 5-HT2A and 5-HT2C receptors, the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5 receptors, α1-adrenergic receptor, and histamine H1 receptor.

The antipsychotic effect of propiomazine is thought to be due to antagonism of the dopamine D2 receptor and serotonin 5-HT2A receptor, with greater activity at the 5-HT2A receptor than at the D2 receptor. This may explain the lack of extrapyramidal effects with propiomazine. Propiomazine does not appear to block dopamine within the tuberoinfundibular pathway, which may explain its lower incidence of hyperprolactinemia than with typical antipsychotics or risperidone.

Chemistry

Propiomazine, also known as 10-(2-dimethylaminopropyl)-2-propionylphenothiazine or as propionylpromethazine, is a phenothiazine derivative and is structurally related to promethazine. The compound is provided medically as the hydrochloride and maleate salts.

Society and culture

Brand names

Propiomazine has been sold under the brand names Dorevan, Dorévane, Indorm, Largon, Phenoctyl, Propavan, Propial, and Serentin.

Availability

In 2000, propiomazine continued to be marketed only in Sweden.

References

References

1. Anvisa. (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial". [[Diário Oficial da União]].
2. "Propiomazine".
3. https://pubchem.ncbi.nlm.nih.gov/compound/Propiomazine#:~:text=Unknown%2C%20but%20most%20likely%20hepatic%20as%20with%20other%20phenothiazines
4. https://fass.se/health/product/19600628000017/fass-text#:~:text=Latenstiden%20till%20klinisk%20effekt%20kan%20variera%20mellan%2030%2D60%C2%A0minuter
5. (1997). "A comparison of zopiclone and propiomazine as hypnotics in outpatients: a multicentre, double-blind, randomized, parallel-group comparison of zopiclone and propiomazine in insomniacs". Curr Med Res Opin.
6. (6 December 2012). "Concise Dictionary of Pharmacological Agents: Properties and Synonyms". Springer Science & Business Media.
7. "NCI Thesaurus".
8. (2001). "Organic-chemical Drugs and Their Synonyms: An International Survey, Volume 3". Wiley-VCH.
9. Swiss Pharmaceutical Society. (2000). "Index Nominum 2000: International Drug Directory". Taylor & Francis.