N05AL05 - Amisulpride |
Propably not porphyrinogenic |
PNP |
Rationale
Amisulpride is mainly excreted unchanged in urine and feces. Pharmacokinetic studies suggest the absence of inducing or inhibiting effects on hepatic microsomal enzyme activity. No clinical reports of CYP-related drug-drug interactions. Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Chemical description
Amisulpride is a substituted benzamide.
Therapeutic characteristics
Amisulpride is an atypical antipsychotic used mainly in the management of psychoses such as schizophrenia, but in some countries it has also been tried in depression. Administered orally or as an intramuscular injection. Common adverse reactions of amisulpride that can be confused with an acute porphyric attack are constipation, nausea, vomiting, anxiety, and agitation. Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Metabolism and pharmakokinetics
Absolute bioavailability of amisulpride is 48%. Amisulpride undergoes only minimal metabolic transformation (Rosenzweig, 2002; Spina, 2007). Two inactive metabolites, accounting for approximately 4% of the dose, have been identified. Most of a dose appears in the urine as unchanged drug.(Spina, 2007). Antipyrine half-life is not altered after repeated administration, which suggests the absence of inducing or inhibiting effects on hepatic microsomal enzyme activity. (Rosenzweig, 2002). Because of its negligible metabolic elimination, amisulpride is almost devoid of clinically relevant metabolic interactions (Spina, 2007). There are no clinical reports that amisulpride influences the blood concentrations of other CYP metabolized drugs. A high-carbohydrate high-fluid meal almost halves the already low oral bioavailability of this drug (Caccia, 2000).
References
- Scientific articles
- Caccia S. Biotransformation of post-clozapine antipsychotics: pharmacological implications. Clin Pharmacokinet. 2000;38(5):393-414. PMID 10843459. #2663
- Rosenzweig P, Canal M,et al. A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers. Hum Psychopharmacol. 2002;17(1):1-13. PMID 12404702. #4673
- Spina E, de Leon J. Metabolic drug interactions with newer antipsychotics: a comparative review. Basic Clin Pharmacol Toxicol. 2007;100(1):4-22. PMID 17214606. #2666
- Drug reference publications
- Sweetman SC, editor. Martindale: The complete drug reference. Amisulpride. Pharmaceutical Press 2009. #2667
- Summary of Product Characteristics
- Norwegian medicines agency. Summary of Product Characteristics (SPC). Solian. #2664
- The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Solian. #2668
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