Product Information
Registration Status: ActiveSTEMETIL INJECTION 12.5mg/ML is approved to be sold in Singapore with effective from 1988-05-19. It is marketed by SANOFI-AVENTIS SINGAPORE PTE LTD, with the registration number of SIN01382P.
This product contains Prochlorperazine 12.5mg/ml in the form of INJECTION. It is approved for INTRAMUSCULAR use.
This product is manufactured by AVENTIS PHARMA in ITALY, and DAGENHAM in UNITED KINGDOM.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
A phenothiazine antipsychotic used principally in the treatment of nausea; vomiting; and vertigo. It is more likely than chlorpromazine to cause extrapyramidal disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612)
Indication
For the symptomatic management of psychotic disorders, short term management of nonpsychotic anxiety in patients with generalized anxiety disorder, and for the control of severe nausea and vomiting of various causes.
Mechanism of Action
The mechanism of action of prochlorperazine has not been fully determined, but may be primarily related to its antidopaminergic effects. Prochlorperazine blocks the D2 somatodendritic autoreceptor, resulting in the blockade of postsynaptic dopamine receptors in the mesolimbic system and an increased dopamine turnover. Prochlorperazine also has anti-emetic effects, which can be attributed to dopamine blockade in the chemoreceptor trigger zone. Prochlorperazine also blocks anticholinergic and alpha-adrenergic receptors, the blockade of alpha(1)-adrenergic receptors resulting in sedation, muscle relaxation, and hypotension.
Pharmacokinetics
- Absorption
- Rapidly absorbed following oral administration
- Distribution
- Metabolism
- Hepatic. Undergoes metabolism in the gastric mucosa and on first pass through the liver, CYP2D6 and/or CYP3A4.
- Elimination
Toxicity
Symptoms of central nervous system depression to the point of somnolence or coma. Agitation and restlessness may also occur. Other possible manifestations include convulsions, EKG changes and cardiac arrhythmias, fever and autonomic reactions such as hypotension, dry mouth and ileus; LD50=400mg/kg (orally in mice)
Active Ingredient/Synonyms
2-Chloro-10-(3-(1-methyl-4-piperazinyl)propyl)-phenothiazine | 2-Chloro-10-(3-(4-methyl-1-piperazinyl)propyl)phenothiazine | 3-Chloro-10-(3-(1-methyl-4-piperazinyl)propyl)phenothiazine | 3-Chloro-10-(3-(4-methyl-1-piperazinyl)propyl)phenothiazine | Capazine | Chlormeprazine | Chloro-3 (N-methylpiperazinyl-3 propyl)-10 phenothiazine | Chloropernazine | Emetiral | N-(gamma-(4'-Methylpiperazinyl-1')propyl)-3-chlorophenothiazine | Prochlorperazin | Prochlorpérazine | Prochlorperazinum | Prochlorpermazine | Prochlorpromazine | Procloperazine | Proclorperazina | Prochlorperazine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.