Jump to content

Propiomazine

From Wikipedia, the free encyclopedia

This is an old revision of this page, as edited by Rollie (talk | contribs) at 15:19, 1 March 2011 (Added {{Unreferenced|date=March 2011}}). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.

Propiomazine
Clinical data
Routes of
administration
Intramuscular, intravenous
ATC code
Pharmacokinetic data
Protein binding81%
Identifiers
  • 1-[10-(2-dimethylaminopropyl)-10H-phenothiazin-2-yl]propan-1-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.006.043 Edit this at Wikidata
Chemical and physical data
FormulaC20H24N2OS
Molar mass340.483 g/mol g·mol−1
3D model (JSmol)
  • O=C(c2cc1N(c3c(Sc1cc2)cccc3)CC(N(C)C)C)CC
  • InChI=1S/C20H24N2OS/c1-5-18(23)15-10-11-20-17(12-15)22(13-14(2)21(3)4)16-8-6-7-9-19(16)24-20/h6-12,14H,5,13H2,1-4H3 checkY
  • Key:UVOIBTBFPOZKGP-UHFFFAOYSA-N checkY
  (verify)

Propiomazine (Largon, Propavan, Indorm, Serentin, Indorm, Dorevane, Dorevan) is an antihistamine blocking H1 receptors. It is used to treat insomnia, and to produce sleepiness or drowsiness and to relieve anxiety before or during surgery or other procedures and in combination with analgetics also during labor. Propiomazine is a phenothiazine, but is not used as a neuroleptic because it does not block dopamine receptors well.

Mechanism of action

Propiomazine is an antagonist at types 1, 2, and 4 dopamine receptors, serotonin (5-HT) receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Propiomazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Propiomazine does not appear to block dopamine within the tubero-infundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone.

Side effects

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.

Drowsiness is a usual side effect, and propiomazine was blamed on Kerry Katona's October 2008 interview on This Morning where she was accused of being under the influence of drink or drugs, as she appeared slurred and drowsy.

References