Product Information
Registration Status: ActiveRELPAX TABLET 40mg is approved to be sold in Singapore with effective from 2002-01-14. It is marketed by PFIZER PTE LTD, with the registration number of SIN11767P.
This product contains Eletriptan 40mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by R-Pharm Germany GmbH (Illertissen) in ITALY, andPfizer Italia S.r.l. in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Eletriptan is a second generation triptan drug developed by Pfizer Inc for the treatment of migraine headaches.
Indication
For the acute treatment of migraine with or without aura in adults.
Mechanism of Action
Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors. Two theories have been proposed to explain the efficacy of 5-HT 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.
Pharmacokinetics
- Absorption
- Well absorbed after oral administration with a mean absolute bioavailability of approximately 50%.
- Distribution
- * 138 L
- Metabolism
- In vitro studies indicate that eletriptan is primarily metabolized by cytochrome P-450 enzyme CYP3A4. The N-demethylated metabolite of eletriptan is the only known active metabolite.
- Elimination
Clearance
* Renal cl=3.9 L/h
Toxicity
Based on the pharmacology of the 5-HT1B/1D agonists, hypertension or other more serious cardiovascular symptoms could occur on overdose.
Active Ingredient/Synonyms
Eletriptanum | Eletriptan |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.