Gene/Protein Disease Symptom Drug Enzyme Compound
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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

The 5-HT(1B/1D/1F) agonist eletriptan, at an oral dose of 80 mg, has been shown to be more efficacious than sumatriptan 100 mg and placebo in the treatment of migraine attacks with or without aura. Another commonly prescribed oral treatment for migraine attacks is Cafergot (1 mg ergotamine tartrate with 100 mg caffeine per tablet). The efficacy, tolerability and safety of 40- and 80-mg doses of eletriptan and 2 tablets of Cafergot were compared in a double-blind, randomised, placebo-controlled, parallel-group trial involving 733 migraine patients. Patients recorded symptoms at baseline (before treatment) and 1, 2, 4 and 24 h after dosing. Headache intensity was assessed on a 4-point scale (3 = severe pain, 2 = moderate pain, 1 = mild pain, 0 = no pain). Significantly more eletriptan-treated patients (80 mg, 68%; 40 mg, 54%) than Cafergot-treated patients (33%; p < 0.001) reported headache response (improvement from moderate-to-severe to mild or no pain) at 2 h. Substantially more eletriptan recipients reported no pain (80 mg, 38%; 40 mg, 28%; Cafergot, 10%; placebo, 5%; p < 0.001). Eletriptan headache response rates at 1 h were significantly higher (80 mg, 39%; 40 mg, 29%; Cafergot, 13%; placebo, 13%; p < 0.002 for each comparison). Both doses of eletriptan were significantly more effective than Cafergot in reducing nausea (p < 0.0001), photophobia (80 mg, p < 0.0001; 40 mg, p < 0.002), phonophobia (80 mg, p < 0.0001; 40 mg, p < 0.003) and functional impairment (p < or = 0.001) at 2 h. Adverse events were generally mild or moderate and transient. This randomised trial shows that oral eletriptan is more efficacious in the acute treatment of migraine than oral Cafergot and is well tolerated.
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PMID:Efficacy, tolerability and safety of oral eletriptan and ergotamine plus caffeine (Cafergot) in the acute treatment of migraine: a multicentre, randomised, double-blind, placebo-controlled comparison. 1184 98

The efficacy, safety and tolerability of the 5-HT1B/D receptor agonist eletriptan (40 mg and 80 mg) in acute treatment of migraine was evaluated in a multinational, randomized, double-blind, parallel-group, placebo-controlled, three-attack study treating 1153 patients. In the initial attack, significantly more eletriptan patients reported headache relief and complete pain relief at 2 h vs. placebo (40 mg 62% and 32%, 80 mg 65% and 34%, placebo 19% and 3%; P < 0.0001). Headache relief occurred faster after eletriptan, with more patients at both doses reporting relief 30 min (P < 0.01) and 1 h (P < 0.0001) after treatment than after placebo. There was a significantly lower recurrence rate with eletriptan 80 mg compared with placebo (P < 0.01). Adverse events for all treatments were generally mild or moderate and self-limiting. Eletriptan 40 mg and eletriptan 80 mg both appear to be effective and well-tolerated acute migraine treatments.
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PMID:Efficacy, safety and tolerability of oral eletriptan in the acute treatment of migraine: results of a phase III, multicentre, placebo-controlled study across three attacks. 1199 10

This prospective multicentre, double-blind, randomized, parallel-group, placebo-controlled trial evaluated the efficacy and safety of a single dose of eletriptan 20 mg, 40 mg and 80 mg in Japanese migraineurs. A total of 402 adult Japanese migraineurs were diagnosed using International Headache Society (IHS) criteria. At 2 h after a single dose, the headache response rates of eletriptan 20 mg, 40 mg, 80 mg and placebo were 64%, 67%, 76% and 51%, respectively, with all doses significantly superior to placebo (P<0.05). Eletriptan had a statistically significant dose response for headache relief and pain-free response at 2 h post-dose (P=0.0011 and P=0.0291, respectively). Most all-causality adverse events were mild and there were no deaths or discontinuations. Saliva samples were used to assess serum eletriptan levels 2 h post-dose. Pharmacokinetic evaluations showed no clinically significant differences between Japanese and Western subjects. Eletriptan was shown to be efficacious, safe, and well tolerated in Japanese migraineurs.
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PMID:Efficacy and safety of eletriptan 20 mg, 40 mg and 80 mg in Japanese migraineurs. 1213 40

Eletriptan is a member of the triptan family of selective serotonin receptor agonists. These act against migraine by inducing vasoconstriction of the meningeal arteries. In pharmacological tests, eletriptan has shown high affinity for the 5-HT(1B/1D) receptors, which have been implicated in the etiology of migraine headache attacks. Pharmacokinetic evaluations have concluded that eletriptan offers greater bioavailability than sumatriptan, the effective predecessor to eletriptan. A rapid onset of action has also been characteristic of eletriptan in clinical trials, which have likewise demonstrated eletriptan's superiority to sumatriptan in granting relief of headache pain and other symptoms associated with migraine to a greater number of migraine patients. The drug has generally been well tolerated with only mild to moderate adverse events reported. These characteristics make eletriptan an attractive alternative to sumatriptan in the treatment of migraine. (c) 2001 Prous Science. All rights reserved.
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PMID:Migraine headache treatment with eletriptan, a second-generation serotonin receptor agonist. 1278 88

To determine the tolerability and efficacy of eletriptan in patients who had discontinued oral sumatriptan due to lack of efficacy or intolerable adverse events (AEs) during previous clinical treatment (not a controlled trial). Eletriptan is a potent, selective 5-HT1B/1D receptor agonist with beneficial pharmacokinetic properties compared with sumatriptan. In a double-blind, parallel group, placebo-controlled multicentre study, patients with and without aura (n = 446) were randomized to 40 mg eletriptan (E40, n = 188), 80 mg eletriptan (E80, n = 171) or placebo (n = 87) for treatment of up to three migraine attacks. Two-hour headache response, based on first-dose, first-attack data, was 59% for eletriptan 40 mg, 70% for eletriptan 80 mg, and 30% for placebo (P < 0.0001 for both doses of eletriptan vs. PBO; P < 0.05 for E80 vs. E40). Onset of action was rapid, with 1-h headache response rates significantly superior for E40 and E80 vs. placebo (40%, 48%, 15%; P < 0.0005). Both E40 and E80 were significantly superior to placebo, based on first-dose, first-attack data, for 2-h pain-free response (35%, 42%, and 7%; P < 0.0001). Both E40 and E80 demonstrated significant consistency of response, with headache relief rates at 2 h on at least two of three attacks in 66% and 72% vs. 15% on placebo (P < 0.001). AEs were mild to moderate in severity and dose related. The most commonly reported AEs included nausea, vomiting, asthenia, and chest symptoms. E40 and E80 produce an effective response in patients who had previously discontinued treatment with sumatriptan due to lack of efficacy or side-effects.
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PMID:Eletriptan for the treatment of migraine in patients with previous poor response or tolerance to oral sumatriptan. 1280 26

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

This was a randomized, double-blind study designed to evaluate the comparative efficacy and tolerability of the 40-mg dose of eletriptan and the 2.5-mg dose of naratriptan. Patients (n = 548) meeting International Headache Society (IHS) criteria for migraine were randomized to treat a single migraine attack with either eletriptan 40 mg, naratriptan 2.5 mg, or placebo. Headache response rates at 2 h and 4 h, respectively, were 56% and 80% for eletriptan, 42% and 67% for naratriptan (P < 0.01 for both time-points vs. eletriptan), and 31% and 44% for placebo (P < 0.0001 vs. both active drugs at both time-points). Eletriptan also showed a significantly greater pain-free response at 2 h (35% vs. 18%; P < 0.001) as well as lower use of rescue medication (15% vs. 27%; P < 0.01) and higher sustained headache response at 24 h (38%) compared with naratriptan (27%; P < 0.05) and placebo (19%; P < 0.01). Both eletriptan and naratriptan were well tolerated. The results confirm previous meta-analyses that have suggested the superiority of eletriptan vs. naratriptan in the acute treatment of migraine.
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PMID:Comparative efficacy of eletriptan vs. naratriptan in the acute treatment of migraine. 1461 28

Meta-analysis provides valuable information regarding relative efficacies of triptans, but head-to-head comparator studies remain the gold standard. Three similar head-to-head trials comparing eletriptan 40 mg (E40) with sumatriptan 100 mg (S100) provide a rare opportunity and sufficient power, for robust comparisons of efficacy. Data were combined from three double-blind, placebo-controlled, first-dose, first-attack acute migraine treatment studies comparing E40 (n=1132), S100 (n=1129), and placebo (n=645). The primary outcome was headache response at 2 h. Secondary outcomes included headache response at 1 h, pain-free and functional responses, and sustained headache and pain-free responses. Odds ratios were calculated for summary estimates of probability of response. There were higher headache response rates with eletriptan versus sumatriptan at 2 h (67% vs. 57%; P<0.0001) and 1 h (34% vs. 26%; P<0.0001). Eletriptan also had higher 2 h pain-free (35% vs. 25%; P<0.0001) and functional responses (67% vs. 58%; P<0.0001). Sustained headache (42%) and pain-free (22%) response rates were higher for eletriptan versus sumatriptan (34%, P<0.0001; 15%, P<0.0001). The probability of response for eletriptan versus sumatriptan ranged from 36% higher (relief of nausea) to 64% higher (sustained pain-free rate). Combined analysis demonstrates that E40 has superior efficacy versus S100 across all clinically relevant outcomes.
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PMID:The 40-mg dose of eletriptan: comparative efficacy and tolerability versus sumatriptan 100 mg. 1474 74

Migraine is a highly prevalent, chronic and disabling illness in which the gap between practice guideline recommendations and actual clinical practice remains wide. Eletriptan, similar to other triptans, is a potent 5-HT(1B/1D) receptor agonist with a high selectivity for cranial versus coronary artery constriction and favorable pharmacokinetic profile. An extensive program of double-blind, placebo-controlled, head-to-head comparator trials has demonstrated the superior efficacy of eletriptan compared with the combination of ergotamine and caffeine, and selected oral triptans for the acute treatment of migraine. Eletriptans tolerability profile makes it a good choice as a first-line treatment of migraine. An early treatment study suggests that treatment of mild headache is associated with unusually high sustained pain-free rates and a tolerability profile that is equivalent to placebo.
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PMID:Eletriptan in migraine. 1585 73


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