Propiomazine

drugbox
IUPAC_name=1- [10-(2-dimethylaminopropyl)-10H-phenothiazin-2-yl] propan-1-one

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CAS_number=362-29-8
ATC_prefix=N05
ATC_suffix=CM06
ATC_supplemental=
PubChem=4940
DrugBank=APRD00339
C=20|H=24|N=2|O=1|S=1
molecular_weight=340.483 g/mol
bioavailability=
protein_bound=81%
metabolism=
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routes_of_administration=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.