Monograph

N02CC06 - Eletriptan

Propably not porphyrinogenic

Rationale

Eletriptan is a substrate of CYP3A4, but is not an inhibitor or an inducer of CYP3A4 in vivo. Risk for gastrointestinal adverse events in the form of nausea and vomiting motivates vigilance against insufficient intake of food, especially of carbohydrate.

Chemical description

Eletriptan is a seretonin agonist.

Therapeutic characteristics

Eletriptan is indicated for the acute treatment of migraine attacks with or without aura. 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 and abdominal pain. A less common side effect is diarrhoea.

Metabolism and pharmacokinetics

In vitro studies indicate that eletriptan is metabolised by CYP3A4, which is also confirmed by clinical studies (Evans 2003 and SPC). In vitro data indicates that eletriptan is not an inhibitor of CYP1A2, CYP2C9 and CYP2C19 (Evans 2003). It is not listed as an inhibitor in vivo of any CYP enzymes, including CYP3A4 (FDA). A study showed that eletriptan is an inducer of CYP3A4 in vitro, but not in vivo. Data also indicates that it is not an inhibitor of CYP3A4 in vivo (Pichard-Garcia 2000).

IPNet drug reports

Uneventful use reported in 2 patients with acute porphyria.

References

#	Citation details	PMID
*	Scientific articles
1.	Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein. Evans DC, O Connor D,et al. Drug Metab Dispos. 2003 Jul;31(7):861-9.	12814962
2.	Human hepatocytes in primary culture predict lack of cytochrome P-450 3A4 induction by eletriptan in vivo. Pichard-Garcia L, Hyland R, et al. Drug Metab Dispos. 2000 Jan;28(1):51-7.	10611140
*	Government bodies
3.	U.S Food and Drug Administration (FDA).
*	Summary of Product Characteristics
4.	Norwegian medicines agency. Summary of Product Characteristics (SPC). Eletriptan.

Citation details

PMID

Scientific articles

Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein.

Evans DC, O Connor D,et al. Drug Metab Dispos. 2003 Jul;31(7):861-9.

12814962

Human hepatocytes in primary culture predict lack of cytochrome P-450 3A4 induction by eletriptan in vivo.

Pichard-Garcia L, Hyland R, et al. Drug Metab Dispos. 2000 Jan;28(1):51-7.

10611140

Government bodies

U.S Food and Drug Administration (FDA).

Summary of Product Characteristics

Norwegian medicines agency. Summary of Product Characteristics (SPC). Eletriptan.

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Tradenames and packages

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Netherlands

Eletriptan · Eletriptan Aurobindo 40 mg, filmomhulde tabletten · ELETRIPTAN Biogaran 20 mg filmomhulde tabletten · ELETRIPTAN Biogaran 40 mg filmomhulde tabletten · Eletriptan Viatris 20 mg, filmomhulde tabletten · Eletriptan Viatris 40 mg, filmomhulde tabletten · Relpax · Relpax 20, filmomhulde tabletten 20 mg · Relpax 40 mg, filmomhulde tabletten · Relpax 40, filmomhulde tabletten 40 mg · RELPAX 40, filmomhulde tabletten 40mg

Belgium