Monograph
A10BX03 - Nateglinide |
Propably not porphyrinogenic |
PNP |
Rationale
Nateglinide is metabolized by CYP2C9 and CYP3A4, but is not an inducer of inhibitor of these CYP enzymes.
Risk for gastrointestinal adverse events in the form of nausea, dyspepsia, abdominal pain and diarrhoea motivates vigilance against insufficient intake of food, especially of carbohydrate.
Chemical description
Isoprpylcyclohexyl carbonyl phenylalanine
Therapeutic characteristics
Nateglinide is indicated for the treatment of diabetes type 2 in combination with metformin where the effect of this drug is insufficient.
Common side effects that can be potentially porphyrinogenic through reduction in carbohydrate intake and that also can be confused with an acute porphyria attack are nausea, dyspepsia, abdominal pain and diarrhoea. A less common side effect is vomiting.
Hepatic exposure
Significant
Metabolism and pharmacokinetics
Nateglinide is metabolized mainly by CYP2C9 and only to a smaller degree by CYP3A4.
There is no clinically relevant effect on the pharmacokinetics of drugs metabolized by CYP2C9 or CYP3A4 (SPC). In vitro studies have also shown that the possibility of drug-drug interactions involving nateglinide as a perpetrator is low (Takanohashi 2010).
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Inhibition of human liver microsomal CYP by nateglinide.
Takanohashi T, Kubo S, et al. J Pharm Pharmacol. 2010 May;62(5):592-7. |
20609060 |
| * | Summary of Product Characteristics | |
| 2. | Norwegian medicines agency. Summary of Product Characteristics (SPC). nateglinid.
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