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) 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

Patients expect their acute migraine treatment to have a rapid onset of action, achieve complete pain relief that is sustained for 24 h, and to have a good tolerability profile. Almotriptan has a favourable pharmacokinetic profile that translates clinically to a rapid onset of action and consistent absorption regardless of age, sex, food intake and status of the acute migraine attack. In addition, almotriptan is not associated with any clinically relevant drug-drug interactions. Pain-free status at 2 h postdose is achieved by approximately 39% of patients receiving almotriptan in clinical trials. Recurrence of headaches within 24 h is low with almotriptan (<22%). Almotriptan has a sustained pain-free rate of 25-27%, which in a meta-analysis of triptans was superior to sumatriptan 100 mg. Almotriptan therapy is associated with a low incidence of adverse events, including those affecting the central nervous system and chest.
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PMID:Clinical profile and practice experience of almotriptan. 1559 90

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

Seven triptans are now available for the acute treatment of migraine. While all of these agents have been shown to be safe and more or less well tolerated, they differ in ways that are clinically relevant to individual patients. Almotriptan has been investigated in approximately 3,500 patients enrolled in short-term clinical trials and 1,500 patients enrolled in long-term open-label trials. In a meta-analysis of placebo-controlled almotriptan trials (n = 2,294), treatment with almotriptan 12.5 mg results in a 2-hour pain-relief rate of 63.7% and a 2-hour pain-free rate of 36.4%. Almotriptan is associated with a rapid onset of action, with 30-min pain-relief and pain-free rates significantly better than placebo (p < 0.05). Direct comparator studies show the efficacy of almotriptan 12.5 mg to be comparable to that of sumatriptan but almotriptan is associated with superior tolerability. Trials assessing the efficacy of almotriptan over multiple attacks show that this agent is associated with a consistent and persistent response, not differing from the first to the last attack, an important property for a medication used to treat a chronic condition such as migraine. Early intervention with almotriptan enhances the activity of this agent. Treatment of mild pain with almotriptan has resulted in 2-hour pain-free rates of 84 and 77% and a sustained pain-free rate of 67%. Early treatment (within 1 h) of moderate to severe headaches with almotriptan also improves outcomes. In conclusion, clinical trials and post hoc analyses of such trials have shown almotriptan to be effective and well tolerated for the acute treatment of migraine. Its placebo-like tolerability makes it a good choice for early intervention, a strategy associated with better patient outcomes.
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PMID:Efficacy and tolerability of almotriptan in controlled clinical trials. 1592 Mar 35

A novel model-based meta-analysis was used to quantify the dose-response relationship of sumatriptan and eletriptan for the proportion of patients that achieve migraine pain relief up to 4 h after treatment. The proportion of patients that became pain free was also evaluated. This analysis includes some unique features, allowing comparison of sumatriptan and eletriptan doses that have not been directly compared in a head to head study and also permitting comparison between the two drugs at multiple time points up to 4 h after treatment. Because the analysis allows comparison of response to blinded sumatriptan with that to marketed sumatriptan and contains timepoints as early as 0.5 h, it is especially suited to detection of possible effects of encapsulation on sumatriptan's therapeutic effectiveness and thus was employed to assess this also. Data from 19 randomized placebo controlled clinical trials were jointly analysed using a random-effects logistic regression model. The results of this analysis show a significant clinical benefit of eletriptan 40 mg compared to sumatriptan 100 mg at any point in time up to 4 h after treatment. The benefit of eletriptan 40 mg is greatest around 1.5-2 h after treatment with an absolute difference at 2 h of 9.1% (7.4-11.5%) more patients achieving pain relief and 7.3% (5.8-8.6%) more patient achieving pain free when compared to sumatriptan 100 mg. An absolute benefit of more than 5% of patients is maintained from 45 min up to 4 h after treatment for pain relief and from 1.5 h up to 4 h for pain free. Eletriptan 20 mg was superior to sumatriptan 50 mg and similar to sumatriptan 100 mg for pain relief while it was similar to sumatriptan 50 mg for pain free. The benefit of eletriptan 20 mg when compared to sumatriptan 50 mg is greatest around 1.5-2 h after treatment with an absolute difference at 2 h of 5.0% (2.9-8.1%) more patients achieving pain relief. An absolute benefit of more than 3% of patients was maintained from 1 h up to 3 h after treatment. No significant difference was found between eletriptan 20 mg and sumatriptan 50 mg for the fraction of patients that became pain free. No significant effect of encapsulation of sumatriptan was found on the time course of response up to 4 h after treatment when compared to commercial sumatriptan.
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PMID:Therapeutic benefit of eletriptan compared to sumatriptan for the acute relief of migraine pain--results of a model-based meta-analysis that accounts for encapsulation. 1610 54

The aim of this study was to examine efficacy and tolerability of eletriptan in patients switched from barbiturate-containing combinations (Fiorinal), Fioricet. Migraineurs (n = 160) meeting IHS criteria, with unsatisfactory response in the past year to butalbital-containing combinations, treated up to 16 attacks over 3 months with eletriptan 40 mg. Assessments included headache response and pain-free rates and functional impairment at baseline and 2 h postdose, and global ratings of treatment satisfaction at 24 h. At 2 h postdose, average headache response and pain-free rates were 71% (95% CI, 69-74%) and 37% (95% CI, 35-40%), respectively; 68.5% of patients (95% CI, 65-72%) reported functional response. Within-patient analysis found no efficacy diminution over time (no tolerance). Average headache recurrence rate was 20% (95% CI, 18-23%). Eletriptan was well-tolerated; 6 (3.7%) patients discontinued due to adverse events. There were no serious treatment-related adverse events. We conclude that in poor responders to butalbital-caffeine combinations, switching to eletriptan 40 mg was well-tolerated and efficacious.
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PMID:Eletriptan treatment of migraine in patients switching from barbiturate-containing analgesics: results from a multiple-attack study. 1610 55

This double-blind, placebo-controlled study was designed to evaluate the efficacy and tolerability of early treatment of a single migraine attack, when headache pain was mild, with two doses (20 mg and 40 mg) of eletriptan. Patients (N = 613; female 79%; mean age 39 years) meeting International Headache Society criteria for migraine were encouraged, but not required, to utilize early treatment, thus providing an opportunity to assess the relative contribution to efficacy of pain severity and timing of dose. For the total patient sample (mild-to-severe headaches), 2-h pain-free rates were significantly higher than placebo (22%) on both eletriptan 20 mg (35%; P < 0.01) and eletriptan 40 mg (47%; P < 0.0001). For the cohort of patients who treated their headache when the pain intensity was mild, the 2-h pain-free rate on eletriptan 40 mg was 68% compared with 25% on placebo (P < 0.0001). Pain intensity at the time of taking eletriptan appeared to influence outcome more than the timing of the dose relative to headache onset. Eletriptan was well-tolerated, with adverse event rates similar to placebo when mild headaches were treated.
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PMID:Eletriptan in the early treatment of acute migraine: influence of pain intensity and time of dosing. 1610 56

Almotriptan is a 5-HT(1B/1D) receptor agonist, or triptan, indicated for the acute treatment of migraine. It has been shown to be effective and well tolerated for the treatment of acute migraine in approximately 5000 patients enrolled in short-term placebo- and active-controlled trials and long-term open-label trials. A recent meta-analysis reported that almotriptan has the highest sustained pain-free (SPF) rate and lowest adverse-event (AE) rate of all oral triptans. Sustained pain free is a composite endpoint of pain freedom at 2 h, no recurrence of moderate-to-severe headache and no use of rescue medication from 2 to 24 h after dosing. Patient surveys have indicated that migraine sufferers consider complete pain relief, no recurrence, rapid onset and no side-effects to be the most important attributes of their acute treatment. Composite endpoints such as SPF and SPF with no AEs (SNAE) contain the attributes that migraine sufferers express as being the most important elements of an acute migraine therapy, and their use in future clinical trials should aid in the selection of agents that can offer patients the highest likelihood of consistent treatment success.
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PMID:Focus on trial endpoints of clinical relevance and the use of almotriptan for the acute treatment of migraine. 1623 92


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