Products
Eletriptan is commercially available in the form of film-coated tablets (Relpax, generics). It has been approved in many countries since 2000.
Structure and properties
Eletriptan (C22H26N2O2S, Mr = 382.5 g/mol) is a lipophilic methylpyrrolidinyltryptamine substituted with a sulfonylbenzene. It is present in drugs as eletriptan hydrobromide, a white powder that is readily soluble in water.
Effects
Eletriptan (ATC N02CC06) has vasoconstrictive, anti-inflammatory, and analgesic properties. The effects are due to highly potent and selective agonism at 5-HT1B/1D/1F receptors.
Indications
For acute treatment of migraine attacks with or without aura.
Dosage
According to the SmPC. The drug is taken only when a migraine headache occurs. It is ineffective against aura and it is not suitable for migraine prophylaxis. When using it, the deep maximum daily dose and the time interval between individual doses should be observed.
Contraindications
- Hypersensitivity
- Renal insufficiency
- Severe hepatic insufficiency
- Certain cardiovascular diseases / vascular diseases.
Eletriptan must not be combined with ergotamine, ergotamine derivatives, or with other 5-HT1 receptor agonists / triptans. Refer to the drug label for complete precautions.
Interactions
Eletriptan is metabolized primarily by CYP3A4 and is a substrate of P-glycoprotein at the blood–brain barrier. CYP3A4 inhibitors may therefore lead to a significant increase in concentrations. CYP2D6 is involved in biotransformation to a lesser extent. In combination with serotonergic drugs, serotonin syndrome may be possible in rare cases. Ergotamine or ergotamine analogs such as dihydroergotamine may cause an increase in blood pressure and are contraindicated.
Adverse effects
The most commonly observed adverse effects include drowsiness, stiffness, numbness, fatigue, throat tightness, warm sensation, flushing, dry mouth, nausea, chest symptoms, and weakness.
