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Brand Name :
Relax
Synonyms :
Eletriptan, eletriptanum
Class :
Antimigraine agents
Brand Name :
Relax
Synonyms :
Eletriptan, eletriptanum
Class :
Antimigraine agents
Dosage Forms & Strengths
Tablets
20mg
40mg
may have an increasingly adverse effect when combined with serotonin 5-HT1D receptor agonists
may have an increased risk of hypertension when combined with eletriptan
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the serotonergic effect of monoamine oxidase inhibitors
may enhance the serotonergic effect of monoamine oxidase inhibitors
may enhance the serotonergic effect of monoamine oxidase inhibitors
may enhance the serotonergic effect of monoamine oxidase inhibitors
may enhance the serotonergic effect of monoamine oxidase inhibitors
may increase the levels of serum concentration of eletriptan
may increase the levels of serum concentration of eletriptan
may increase the levels of serum concentration of eletriptan
may increase the levels of serum concentration of eletriptan
may increase the levels of serum concentration of eletriptan
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased vasoconstricting effect when combined with ergot derivatives
may enhance the concentration of serum when combined with eletriptan
may enhance the concentration of serum when combined with eletriptan
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
CYP3A4 inhibitors increase the concentration of eletriptan in serum
may enhance the serum concentration of CYP3A4 inhibitors
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increasingly adverse effect when combined with sumatriptan
serotonin 5-HT1D receptor agonists increase the serotonergic effect of MAO inhibitors
may have an increased serotonergic effect when combined with serotonergic agents
It may enhance the effect when combined with lonafarnib by affecting the P-glycoprotein efflux transporter
It may enhance the effect when combined with grapefruit by CYP3A4 metabolism
It may enhance the metabolism when combined with dexamethasone
It may diminish the effect when combined with griseofulvin by CYP3A4 metabolism
It may enhance the effect when combined with miconazole vaginal by affecting CYP3A4 metabolism
When acetohexamide is used together with eletriptan, this lead to reduction in acetohexamide’s metabolism
When encainide is used together with eletriptan, this leads to a reduction in the encainide’s metabolism
When eletriptan is used together with melitracen, this leads to enhanced risk or seriousness of CNS depression
When indisulam is used together with eletriptan, this leads to a reduction in eletriptan metabolism
eletriptan: it may decrease the metabolism of sulfamethoxazole
may enhance the serotonergic effect of serotonergic agents
may have an increased hypertensive effect when combined with droxidopa
may increase the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists
Actions and spectrum:
It binds to 5-HT1B, 5-HT1F, and 5-HT1D receptors with high affinity and has a moderate affinity to 5-HT1A, 5-HT2B, 5-HT7, and 5-HT1E and no or little affinity towards 5-HT2A, 5-HT3, 5-HT2C, 5-HT4, 5-HT6 and 5-HT5A. It shows insignificant pharmacological effects at α1, α2, or β adrenergic receptors, muscarinic or opioid receptors, and dopaminergic D1 or D2. Vasoconstriction of cranial vessels occurs due to activation of 5-HT1 receptors due to eletriptan. This action might show the effect towards relief of migraine pain.
Diarrhea
Slow, fast or uneven heart rate
Numbness
Tingling
Burning toes or feet
Severe headache
Blurred vision
Signs of stroke
Heavy feeling in legs
Symptoms of heart attack
Weakness
Dizziness
Nausea
Drowsiness
Feeling tired
Avoid using eletriptan within 24 hours after or before administration of another medicine for migraine
Do not use this medicine in case of coronary artery disease, heart disease, Wolff-Parkinson-White syndrome, hepatic impairment, heart attack or uncontrolled hypertension
Not indicated to use within 72hours after or before administration of troleandomycin, ketoconazole, ritonavir, clarithromycin, itraconazole, nefazodone, or nelfinavir
Wolff-Parkinson-White syndrome
Heart problems
Circulation problems
Headache unusual from migraine headache
Pregnancy & breastfeeding:
Pregnancy consideration:
USFDA pregnancy category: C
Breastfeeding warnings:
It should be used with caution in lactation as the drug is known to be excreted into breast milk.
Pregnancy category:
Pharmacology:
Eletriptan, an antimigraine agent, is a selective agonist of 5-HT (5-hydroxytryptamine) 1B/1D receptor. It is a second-generation triptan used for treating migraine and was developed by Pfizer.
Pharmacodynamics:
It reduced the blood flow in carotid artery in an anesthetized dog, with only a slight raise in arterial blood pressure in higher doses. In rats, it has shown inhibition of the activity of the trigeminal nerve.
Pharmacokinetics:
Absorption: It is well absorbed following oral administration. Mean bioavailability is observed to be 50% approximately. A high fat food increases the Cmax and AUC of the drug by nearly 20% to 30%.
Distribution: The volume of distribution is 138L, and approximately 85% of the drug is known to be bound to plasma proteins.
Metabolism: In vitro studies suggest that eletriptan is metabolized by the enzyme CYP3A4. The active metabolite is the N-demethylated product of eletriptan which exhibits 10% of potency of parent compound.
Elimination: This undergoes renal route of elimination. It is excreted mainly through urine and feces.
Half-life: 4 hours
It should be administered orally only after the headache is confirmed. It is not intended to treat hemiplegic or basilar migraines. If the response to initial dose is ineffective, a second dose can be taken after 12 to 24 hours.
Patient information leaflet
Generic Name:Â eletriptan
Why do we use eletriptan?
This is a selective serotonin receptor agonist. It is used to treat migraines with or without aura. It does not decrease the number of attacks or prevent headaches. It is not indicated for treating tension headaches, which cause loss of movement on one side of the body.
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