Eletriptan (Relpax ® trade name, manufacturer, Pfizer) is a drug from the group of triptans, which is used for acute treatment of migraine. It is an agonist at the serotonin receptor subtype 5-HT1B/1D. Eletriptan was patented in 1992 by Pfizer.
Drugs approved for the acute treatment of Eletriptan in migraine include tablets with 20 or 40mg Eletriptanhydrochlorid.
Eletriptan should not be used with known hypersensitivity to the drug. The drug should not be used in patients with heart attack, suspected ischemic heart disease, coronary vasospasm (Prinzmetal angina), peripheral blood vessel diseases, and moderate to severe or uncontrolled high blood pressure.
In known severe liver or kidney dysfunction or transient ischemic attacks medical history should detail that Eletriptan should not be used as well. Eletriptan should not be used simultaneously with ergot alkaloids and their derivatives (for example ergotamine or dihydroergotamine), since an increased risk of vasospasm is present.
Use during pregnancy and lactation
Since there are no sufficient experience on the use of eletriptan in pregnant women, eletriptan should be used during pregnancy with caution and under strict indications. Animal studies have revealed no evidence of embryotoxic or teratogenic effects. Eletriptan occurs principally in breast milk, and again, about 0.02% of the total dose of 80mg when the drug is administered can be present in breast milk.
Despite the small amount of eletriptan in breast milk, breastfeeding mothers should use with caution. Possible effects on the infant can be minimized by interruption of breastfeeding with pumping and discarding breast milk for at least 24 hours after taking eletriptan.
Mechanism of action (pharmacodynamics)
Eletriptan is a selective agonist of serotonin receptor subtype 5-HT1B/1D-Rezeptoren. Eletriptan also shows a relevant affinity for 5-HT1F receptors. Eletriptan leads to a reduction of the distribution of blood vessel dilating pain and triggers inflammatory mediators, such as serotonin, calcitonin gene-related peptide (CGRP) and substance P.