Product Information
Registration Status: ActiveIMIGRAN TABLET 50mg is approved to be sold in Singapore with effective from 1995-10-26. It is marketed by GLAXOSMITHKLINE PTE LTD, with the registration number of SIN08419P.
This product contains Sumatriptan 50mg( Equivalent to 70mg as Succinate) in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by GLAXOSMITHKLINE PHARMACEUTICALS S.A. in POLAND.
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
A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of migraine disorders. A transdermal patch version of sumatriptan is currently in phase I trials in the U.S. under the code name NP101 (NuPathe).
Indication
For the treatment of migraine attacks with or without aura.
Mechanism of Action
The 5-HT1B and 5-HT1D receptors function as autoreceptors, which inhibit the firing of serotonin neurons and a reduction in the synthesis and release of serotonin upon activation. After sumatriptan binds to these receptors, adenylate cyclase activity is inhibited via regulatory G proteins, incrases intracellular calcium, and affects other intracellular events. This results in vasoconstriction and inhibtion of sensory nociceptive (trigeminal) nerve firing and vasoactive neuropeptide release.
Pharmacokinetics
- Absorption
- Approximately 15%
- Distribution
- * 2.7 L/kg [subcutaneous dosing]
- Metabolism
- Hepatic. In vitro studies with human microsomes suggest that sumatriptan is metabolized by monoamine oxidase (MAO), predominantly the A isoenzyme.
- Elimination
Clearance
* 1200 mL/min [Following a 6-mg SC injection]
Toxicity
Symptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation.
Active Ingredient/Synonyms
(3-[2-(dimethylamino)Ethyl]-1H-indol-5-yl)-N-methylmethanesulfonamide | 1-[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]-N-methyl-methanesulfonamide | 3-(2-(dimethylamino)Ethyl)-N-methyl-1H-indole-5-methanesulfonamide | 3-[2-(dimethylamino)Ethyl]-N-methylindole-5-methanesulfonamide | NP101 | Sumatran | Sumatriptan | Sumatriptán | Sumatriptan Succinate | Sumatriptanum | Sumax | triptan | Sumatriptan |
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.