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Propiomazine: Wikis

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Propiomazine
Systematic (IUPAC) name
1-[10-(2-dimethylaminopropyl)-10H-phenothiazin-2-yl]propan-1-one
Identifiers
CAS number 362-29-8
ATC code N05CM06
PubChem 4940
DrugBank APRD00339
Chemical data
Formula C 20H24N2OS 
Mol. mass 340.483 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 81%
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Intramuscular, intravenous

Propiomazine (brand names: 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 do a good job of blocking dopamine receptors.

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 the drug 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.

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