Chemically known as eletriptan hydrobromide, it is a variant of the triptan drugs manufactured as an anti migraine treatment. It is more commonly known in the US as the marketed Relpax, though there are other brand names allocated in other regional markets.
The drug first saw action after being approved by the FDA to be safely marketed and distributed last December 26, 2002. This drug, which comes in 20 or 40-milligram strengths, is sold by prescription and should not be taken in casually to treat severe headaches or basilar forms of migraine.
The main mechanism of action of the drug is to decrease the swelling of the blood vessels surrounding the brain as evidenced by chronic migraine attacks. It also potentially ingested as a neurological suppressant that blocks the nerve endings from releasing receptor substances.
This serotonin agonist is a selective form with a high affinity to the 5-HT receptor 1B, 1D, and 1F, but has no relation to the activation or influence over adrenergic, dopaminergic, muscarinic or opioid processes.
In a more detailed look into the process of the drug over migraine, eletriptan activates the high affinity 5-HT receptors in the intracranial blood vessels. This would include the arteriovenous anastomoses that are highly affected during a migraine attack. Activation of these areas leads to vasoconstriction, and a subsequent alleviation of intracranial pressure against the walls. It is also viewed as to stopping the release of pro-inflammatory neuropeptides, which is responsible for the supposed swelling.
Eletriptan is intended for patients who suffer from migraines and extreme headaches related to nausea and light sensitivity. This drug is for immediate action against the signs and symptoms of the migraine attacks but is limited to not being able to actually lessen the chances of having such an attack. It is a prescription drug not intended for common headaches related to hunger, hormonal imbalance, or other prophylactic means as it may cause undesired effects.
Proper dosing of the drug is to take a required amount by either a single dose of any strength marketed, and under strict compliance with the physician's advice. This is done once the initial migraine attack is perceived. Ingestion may be repeated after two hours if the migraine attack returns, or if allowed by the doctor.
It is not advisable that the drug should be used more than 80 milligrams in a 24 hour period as it may cause an increased risk for side or even adverse effects. It is highly advised that strict adherence to medication regimen should be observed.
Some of the common forms of side effects include dizziness, overall weakness, fatigue, diarrhea, dry mouth, fluctuations in the heartbeat, irritability, blocked nostrils, itchiness, sleeping disorders, confusion, and overall body malaise.
There are several drug contraindications for eletriptan, among which include other triptan class drugs as these may increase the risk of contracting heart attacks. It is also contraindicated to use this drug alongside ergot medicines.
There are also indications that the drug should be avoided of being combined with these drugs within a 72-hour period: Ketoconazole, Itraconazole, Clarithromycin, Fluvoxamine, Sertraline, and other similar drugs indicated in the drug package leaflet.
It is also advised to use this drug with caution on patients who are at risk of coronary artery diseases, among which include diabetes, chronic smoking, obesity, and high level hypertension.
Eletriptan has the following structural formula:
• Molecular formula of eletriptan is C22H26N2O2S
• Chemical IUPAC Name is 3-[(1-methylpyrrolidin-2-yl)methyl]-5-(2-phenylsulfonylethyl)-1H-indole
• Molecular weight is 382.52 g/mol
• Eletriptan available : 20mg tablets, 40mg tablets
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