Eletriptan, sold under the brand nameRelpax and used in the form of eletriptan hydrobromide, is a second-generationtriptanmedication intended for treatment ofmigraineheadaches.[3][4] It is used as anabortive medication, blocking a migraine attack which is already in progress. Eletriptan is marketed and manufactured byPfizer Inc.
Eletriptan was approved by the USFood and Drug Administration (FDA) in December 2002, for the acute treatment of migraine with or withoutaura in adults.[5] It is available only byprescription in the United States, Canada and Australia. It is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. It is available in 20 mg and 40 mg strengths. But unfortunately for unknown reasons this product is hardly available in Germany if at all.
Eletriptan is believed to reduce swelling of the blood vessels surrounding the brain. This swelling is associated with the head pain of a migraine attack. Eletriptan blocks the release of substances from nerve endings that cause more pain and other symptoms like nausea, and sensitivity to light and sound. It is thought that these actions contribute to relief of symptoms by eletriptan.
Eletriptan has no significant affinity or pharmacological activity atadrenergicα1,α2, orβ;dopaminergicD1 orD2;muscarinic; oropioid receptors. Eletriptan could be efficiently co-administered with nitric oxide synthase (NOS's) inhibitors for the treatment of NOS-dependent diseases (US patent US 2007/0254940).
Two theories have been proposed to explain the efficacy of 5-HT1 receptor agonists in migraine. One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache. The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.
Eletriptan is contraindicated in patients with various diseases of the heart and circulatory system, such as angina pectoris, severe hypertension, andheart failure, as well as in patients that have had a stroke or heart attack. This is due to the unusual side effect of coronary vasoconstriction due to serotonin 5HT1B antagonism, which can precipitate aheart attack in those already at risk. It is also contraindicated in severerenal orhepatic impairment due to its extensive liver metabolism throughCYP3A4.[8]
Strong inhibitors of the liver enzyme CYP3A4, such aserythromycin andketoconazole, significantly increase blood plasma concentration of eletriptan and should be separated by at least 72 hours.Ergot alkaloids, such asdihydroergotamine, add to the drug's hypertensive effect and should be separated by at least 24 hours.[8]
It is sold in the United States, Canada, Australia, and the United Kingdom under the brand name Relpax,[2][9][1] and in several other countries under the brand name Relert.[citation needed]
In the US, Relpax is marketed byViatris after Upjohn was spun off from Pfizer.[10][11][12]
N
Y (what is this?) (verify)