Save up -80% on Eletriptan
|Note: this is a drug discount program, not an insurance plan.|
|RX BIN: 015558||RX PCN: HT||Group ID: DDN6600||Card Holder ID: DDN6600|
|Pharmacists and Patients support.|
2019 Price of Relpax
|$57.51||6 tablets/40 mg|
|price without discount in nearest pharmacy. Price may vary.|
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Eletriptan volume of distribution
The volume of distribution of eletriptan following IV administration is 138L. Plasma protein binding is moderate and approximately 85%.
Discount Cards 16,000+
Clients Benefit 29%
Total savings $4,735,080
What is Eletriptan
Eletriptan is a second generation triptan drug developed by Pfizer Inc for the treatment of migraine headaches. (Wikipedia)
Eletriptan 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.
Dosage forms of Eletriptan
Humans and other mammals
Indication of Eletriptan
For the acute treatment of migraine with or without aura in adults.
Toxicity of Eletriptan
Based on the pharmacology of the 5-HT1B/1D agonists, hypertension or other more serious cardiovascular symptoms could occur on overdose.
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What is Relpax?
Relpax is referred to selective serotonin receptor agonists of types 5-HT1B and 5-HT1D-receptors located in cerebral vessels, on the neurons of the nucleus and on the endings of the nervus trigeminus, respectively. In addition to impaired excretion of algogenic substances from nerve endings, Relpax causes vasoconstriction of the cranial vessels. The drug helps to increase the threshold sensitivity of the trigeminal nerve by blocking its spinal nuclei. Clinically, the effect of Relpax is manifested by a decrease in the pulsation of the cerebral vessels, the elimination of pain syndrome.
Relpax, unlike other representatives of triptans, lacks the ability to interact with muscarinic, dopamine, alpha, beta-adrenergic and opioid receptors. After oral administration of Relpax tablets, the active ingredient is immediately absorbed through the intestinal wall, and then binds to plasma proteins by 85%. Tmax after oral pills averaged 1.5 hours. The metabolism of eletriptan, the active ingredient of Relpax, is carried out in the liver by CYP3A4 cytochrome P450. Excretion of metabolites is carried out by the kidneys and gastrointestinal tract.
Relpax should be taken as early as possible, however, the drug is effective at a later stage of a migraine attack. The recommended starting dose is 40 mg. If migraine headache resumes within 24 hours, then Relpax® can be prescribed again in the same dose. If a second dose is needed, it should be taken no earlier than 2 hours after the first dose. The daily dose should not exceed 160 mg.