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.

Eletriptan is a seretonin agonist.

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.

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).

Uneventful use reported in 2 patients with acute porphyria.