N05AL01 - Sulpiride |
Propably not porphyrinogenic |
PNP |
Rationale
Sulpiride is mainly excreted unchanged in urine and feces. Does not inhibit CYP 1A2, 2C9, 2C19, 2D6, 2E1, or 3A4. No clinical reports of CYP-related drug-drug interactions.
Chemical description
Sulpiride is a substituted benzamide.
Therapeutic characteristics
Sulpiride is a conventional antipsychotic used in the treatment of psychoses such as schizophrenia. It has also been given in the management of Tourettes syndrome, anxiety disorders, depression, vertigo, and benign peptic ulceration. Administered orally or as an intramuscular injection.
Metabolism and pharmakokinetics
Sulpiride is about 40% bound to plasma proteins and is reported to have a plasma half-life of about 8 to 9 hours. After intravenous administration
of sulpiride, 70% of the dose is recovered as unchanged drug in urine, as compared to 15% after oral administration, and the bioavailability of the oral form is 25—36%. After oral dosing of 14C-labeled sulpiride, urinary excretion of radioactivity was 27—52%, and more than 95% of the radioactivity recovered in the urine and feces is unchanged sulpiride. Sulpiride did not inhibit human CYP1A2, CYP2C9, CYP2C19,
CYP2D6, CYP2E1, or CYP3A4 at 500 mM concentration, which is 8-fold higher than the predicted free fractions (Niwa, 2005). Additionally, there are no clinical reports that sulpiride increases the blood concentrations of other CYP metabolized drugs.
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.
References
- Scientific articles
- Niwa T, Inoue S, et al. No inhibition of cytochrome P450 activities in human liver microsomes by sulpiride, an antipsychotic drug. Biol Pharm Bull. 2005;28(1):188-91. PMID 15635191. #4672
- Drug reference publications
- Sweetman SC, editor. Martindale: The complete drug reference. Sulpiride. Pharmaceutical Press 2009. #2661
- Summary of Product Characteristics
- The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Dolmatil. #2662
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