Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Eletriptan (Relpax, Pfizer) is one of a group of anti-migraine medications commonly referred to as 'triptans'. It is a potent serotonin agonist at the 5-HT(1B/1D) receptor and is indicated for the acute treatment of migraine headaches. Eletriptan is administered orally. It is rapidly absorbed and has a bioavailability of 50% compared to 14% for sumatriptan. The relatively high lipophilicity of eletriptan compared to sumatriptan may explain its faster oral absorption and shorter time to onset of action. Results from comparative studies between oral eletriptan and sumatriptan indicate that eletriptan 80 mg was superior to sumatriptan 100 mg in onset of action, headache response rate, pain free response rate and relief of associated migraine symptoms at the 1 or 2 h time intervals. Although there was a modest increase in adverse events with eletriptan 80 mg than with sumatriptan 100 mg, eletriptan received a high patient acceptability rating (84%).
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PMID:Eletriptan. 1177 92

Eletriptan (Relpax) is a new anti-migraine medication commonly referred to as triptans. Eletriptan is considered to reduce neuronal transmission of pain by causing vasoconstriction of dilated cranial vessels and inhibiting the release of neuropeptides from trigeminal nerves via activation of the 5-HT(1B/1D) receptors. Eletriptan showed selectivity, high affinities, and potent agonistic activity to human 5-HT(1B/1D) receptors. It selectively constricted the cranial artery relative to the coronary artery of the anesthetized dog and the isolated human specimen. The affinity to the 5-HT(1B/1D) receptors and the selectivity for the cranial artery over the coronary artery of eletriptan are higher than those of sumatriptan. Eletriptan inhibited the trigeminal nerve mediated inflammation in the rat dura mater with equal potency and efficacy to sumatriptan. Orally taken eletriptan was rapidly absorbed with good bioavailability. In clinical trials, eletriptan improved the headache response rate with rapid onset, and reduced headache recurrence. The functional impairments as well as associated symptoms such as nausea, vomiting, and photophobia were also improved by eletriptan. Eletriptan showed stable efficacy in chronic use against multiple attacks with no increase in adverse events. Eletriptan was well tolerated in patients and most adverse events were mild-to-moderate in nature.
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PMID:[Pharmacological, pharmacokinetic and clinical profile of eletriptan (Relpax), a new triptan for migraine]. 1284 76

The objective of this study was to use the patient-centered efficacy measurements of sustained pain free and sustained pain free with no adverse events to compare the relative cost-effectiveness of 6 oral triptans in the treatment of acute migraine. Adverse event and sustained pain-free rates were obtained from a comprehensive meta-analysis of 53 clinical trials of oral triptans. Efficacy and tolerability were assumed to be independent. Average wholesale prices were in US dollars as of May 10, 2004. The meta-analysis of oral triptans reported that almotriptan 12.5 mg (Axert) exhibited the highest sustained pain-free rate (25.9%), with the lowest rate associated with eletriptan 20 mg (Relpax) (10.6%). In addition, almotriptan 12.5 mg possessed the lowest overall absolute adverse event rate (14.2%), with the highest adverse event rate exhibited by eletriptan 80 mg (53.9%). To attain 100 sustained pain-free patients, almotriptan 12.5 mg and rizatriptan 10 mg (Maxalt) proved to be the most cost-effective triptans, costing $7120 and $7427, respectively; the least cost-effective were naratriptan 2.5 mg (Amerge) ($13,736) and eletriptan 20 mg ($16,104). To attain 100 sustained pain-free with no adverse events patients, almotriptan 12.5 mg was the most cost-effective triptan ($8298) and the least cost-effective were eletriptan 20 mg ($25,521) and eletriptan 80 mg ($29,614). At average wholesale prices as of May 10, 2004, almotriptan 12.5 mg achieved the highest level of cost-effectiveness using either sustained pain free or sustained pain free with no adverse events as endpoints.
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PMID:Using patient-centered endpoints to determine the cost-effectiveness of triptans for acute migraine therapy. 1698 36