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)

Rizatriptan is a highly potent, selective serotonin 5-HT(1B/1D)-receptor agonist. Current theories on the mechanism of migraine suggest the central role of vasodilation of intracranial, extracerebral blood vessels and activation of perivascular trigeminal sensory nerves. There abundantly exist 5-HT(1B) receptors in meningeal blood vessels and 5-HT(1D) receptors in the trigeminal ganglia. The therapeutic activity of rizatriptan in migraine can most likely be attributed to agonist effects at 5-HT(1B/1D) receptors on these target sites. Two types of the 10 mg formulation, a tablet (Maxalt) tablet) and an orally disintegrating tablet (Maxalt)RPD tablet), are available. The latter may have a clinical relevance for patients who administer it without liquid. Pharmacokinetic study demonstrated the approximate T(max) of 1.0 or 1.1 h in tablets and 1.3 h in RPD tablets, resulting in early onset for headache relief and also pain free. Bioavailability was estimated to be about 45%. The efficacy and good tolerability and underlying profiles of pharmacokinetics of rizatriptan are almost similar between Japanese and other races, and a reduction in headache response up to 2 h can be attained in a large majority of patients. Several reports have described the favorable clinical profile of rizatriptan in comparison to other triptans. Rizatriptan is thus effective and provides migraine sufferers with an appropriate quality of life.
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PMID:[Rizatriptan (Maxalt), a new entity of triptan for migraine: pharmacology and therapeutic relevance]. 1505 46

Rizatriptan represents a major advance in the treatment of migraine attack: inhibition of peripheral trigeminal nerve and constriction of intracranial extracerebral blood vessels have been proposed as its main antimigraine mechanisms of action. Although many studies may suggest that rizatriptan causes highly selective vasoconstriction within intracranial extracerebral vessels (i.e., meningeal arteries), no literature data are available to date on possible cerebral hemodynamic changes in humans after treatment with rizatriptan. The aim of this study was to evaluate the effect of rizatriptan on cerebral blood flow velocity performing transcranial Doppler during spontaneous attacks of migraine without aura. Fourteen patients suffering from migraine without aura were monitored to evaluate mean flow velocity changes on both middle cerebral arteries during migraine attack 30 min before and 120 min after oral administration of rizatriptan 10mg. Monitoring was repeated for 30 min during the pain-free period. All patients turned out to be drug responders and no significant mean flow velocity changes were observed between the pain-free period and pre-treatment phase; besides no significant difference in mean flow velocity value have been detected between the periods after the drug administration during the attack versus both pre-treatment period and pain-free phase. These findings indicate that the antimigraine action of rizatriptan is not associated with clear intracranial cerebral hemodynamic changes and may support its cerebrovascular safety.
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PMID:Rizatriptan does not change cerebral blood flow velocity during migraine attacks. 1581 94

Rizatriptan (MAXALT MK-0462) is a new 5-HT(1B/1D) receptor agonist for the acute treatment of migraine. The marketed 10 mg and 5 mg oral doses are rapidly and consistently effective in relieving headache pain with associated migraine symptoms, and in enabling patients to return to their normal activities of daily living. Rizatriptan 10 mg is more effective than rizatriptan 5 mg. Compared to oral sumatriptan, the established agent in this class, rizatriptan has a shorter Tmax and greater bioavailability. In comparative clinical trials, the probability of having pain relief sooner was higher for rizatriptan 10 mg than for sumatriptan 100 mg or 50 mg. Over the 2 h after dosing, rizatriptan 10 mg was also superior to sumatriptan 100 mg and 50 mg on a range of other outcome measures. Both doses of rizatriptan are well-tolerated. The most common side-effects are dizziness, drowsiness, and asthenia/fatigue, which are short-lasting and of mild or moderate severity. In summary, rizatriptan is an effective and well-tolerated acute treatment for migraine, which may offer some advantages over oral sumatriptan.
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PMID:Rizatriptan: a new 5-HT1B/1D receptor agonist for the treatment of migraine. 1599 22

Rizatriptan (Maxalt; Maxalt-MLT; Maxalt-Melt) is an oral serotonin 5-HT(1B/1D) receptor agonist (triptan) used in the acute treatment of migraine with or without aura in adults. Rizatriptan 5 mg and 10 mg are effective in relieving the symptoms of migraine and the 10 mg dose provided faster pain relief than sumatriptan 50 mg, naratriptan 2.5 mg, ergotamine/caffeine 2 mg/200 mg and possibly zolmitriptan 2.5 mg, while displaying similar tolerability. Two cost-utility analyses performed from a societal perspective indicated that rizatriptan 10 mg was dominant over ergotamine/caffeine 2 mg/200 mg, sumatriptan 50 mg or 100 mg, naratriptan 2.5 mg, zolmitriptan 2.5 mg and analgesic-based usual care in the acute treatment of migraine. In one analysis also performed from the perspective of a healthcare payer, rizatriptan was still dominant over naratriptan, sumatriptan and zolmitriptan. Rizatriptan was cost effective compared with usual care with an incremental cost per quality-adjusted life-year (QALY) gained of 31,845 Can dollars (2002 values) and an incremental cost per additional attack aborted of 49.82 Can dollars. A modelled cost-effectiveness analysis conducted from a healthcare payer's perspective indicated that almotriptan 12.5 mg was more cost effective than rizatriptan 10 mg as a result of better tolerability. The incremental cost per additional successfully treated patient (defined as being sustained pain free without adverse events) with almotriptan was 6.94 US dollars (1999 values). In other nonmodelled cost-effectiveness analyses, rizatriptan 10 mg, eletriptan 40 mg and almotriptan 12.5 mg most consistently displayed the greatest cost effectiveness in different analyses using different clinical endpoints. A modelled analysis of the costs of migraine-related productivity losses in US corporations indicated that the use of rizatriptan rather than usual care to treat migraines could result in annual cost offsets of approximately 84-118 US dollars (2000 values) per employee in lost productivity avoided. An intervention study in Spanish postal service workers demonstrated that replacement of usual care with rizatriptan reduced the mean per-patient cost of lost productivity per migraine attack from 34.47 euros (2001/2002 values) before the intervention to 13.94 euros and 4.59 euros for the first and second post-intervention migraine attacks. In conclusion, rizatriptan is one of the more clinically effective and therefore cost-effective oral triptans available for the acute treatment of migraine. The available data from cost-utility analyses suggest that rizatriptan is more cost effective than ergotamine/caffeine, simple analgesics, naratriptan, zolmitriptan and sumatriptan. The economic value of rizatriptan depends on the payer's perspective, as the greatest savings can be expected to be achieved in terms of reduced migraine-related loss of work productivity compared with less effective treatments. For healthcare payers, the high acquisition cost appears to be at least partly offset by reduced migraine-related healthcare resource use when compared with usual care. The comparative cost effectiveness of the newer triptans requires further elucidation from comprehensive direct comparisons.
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PMID:Rizatriptan: a pharmacoeconomic review of its use in the acute treatment of migraine. 1633 21

According to an epidemiological study in Japan, there are as many as 22 million patients with tension headache and 8.4 million with migraine. Furthermore, patients suffering from both types of headache concurrently are estimated to account for more than 50% of headache patients. We studied the efficacy of drug therapy for migraine accompanied by tension headache-like symptoms, focusing principally on neck stiffness. We evaluated the efficacy of rizatriptan by comparison of findings before and after therapy in 34 migraine patients, consisting of 16 without neck stiffness (migraine without neck factor: WONF) and 18 with it (migraine with neck factor: WNF), who received treatment at our neurology/internal medicine department from 1 March 2004 to 31 May 2005. In the study, all the patients were asked to keep a record of their migraine status. The severity of migraine was classified by physicians according to the International Headache Society diagnostic criteria, based on which drug efficacy was evaluated. We selected rizatriptan for migraine treatment in our study based on Dr. Ferrari's report. In the efficacy study of rizatriptan, in the group of 34 migraine patients, the pain relief rate (79.4%) and pain-free rate (41.2%) at two hours after treatment were as high as those reported in the meta-analysis performed by Ferrari et al., indicating high efficacy of rizatriptan. In the efficacy comparison between the WONF and WNF groups, the painfree rates were 56.3% and 27.8%, and cumulative pain relief rates were 100% and 61.1%, respectively, with better results in the WONF group. A test result was also significantly better (p=0.0076) in the WONF group. Rizatriptan was proved effective in treating migraine patients accompanied by tension headache-like symptoms. Comparison of efficacy rates between patient groups with and without tension headache-like symptoms showed that the pain relief rate in the group without neck stiffness was higher.
J Headache Pain 2005 Dec
PMID:Clinical efficacy of rizatriptan for patients with migraine: efficacy of drug therapy for migraine accompanied by tension headache-like symptoms, focusing on neck stiffness. 1638 40

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

We report the case of a male liver transplant recipient who developed de novo migraine while on tacrolimus therapy. Considering the inadequate control of pain using nonsteroidal antiinflammatory drugs, rizatriptan benzoate (10 mg orally) was administered (double administration). After both administrations a clinically transient ischemic attack (TIA) occurred. Rizatriptan was discontinued, the patient recovered without sequelae from both episodes of TIA. Remission of migraine occurred after discontinuation of tacrolimus and substitution with cyclosporine. We suggest that the association of rizatriptan and tacrolimus could potentially lead to an excessive risk of cerebral vasospasm and should be used with caution. A change in immunosuppressive therapy (from tacrolimus to cyclosporine or sirolimus) may improve migraine and should be the first choice. Further prospective comparative randomized trials are needed to establish the best therapeutic option in this particular subset of patients.
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PMID:Transient ischemic attack after rizatriptan administration in a liver transplant recipient: a case report. 1711 20

These are the first prospective studies to use criteria for menstrual migraine proposed in the 2004 revision of the International Classification of Headache Disorders (ICHD-II) to examine the efficacy of rizatriptan for treatment of a menstrual attack. Two identical protocols (MM1 and MM2) were randomized, parallel, placebo-controlled, double-blind studies. Adult women with ICHD-II menstrual migraine were assigned to either rizatriptan 10-mg tablet or placebo in a 2 : 1 ratio. Patients treated a single menstrual migraine attack of moderate or severe pain intensity. The primary end-point was 2-h pain relief and the secondary end-point was 24-h sustained pain relief. A total of 707 patients (MM1 357, MM2 350) treated a menstrual migraine attack. The percentage of patients reporting 2-h pain relief was significantly greater for rizatriptan than for placebo (MM1 70% vs. 53%, MM2 73% vs. 50%), as was the percentage of patients reporting 24-h sustained pain relief (MM1 46% vs. 33%; MM2 46% vs. 33%). Rizatriptan 10 mg was effective for the treatment of ICHD-II menstrual migraine, as measured by 2-h pain relief and 24-h sustained pain relief.
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PMID:Rizatriptan for the acute treatment of ICHD-II proposed menstrual migraine: two prospective, randomized, placebo-controlled, double-blind studies. 1744 79

The objective of this study was to compare the efficacy of rizatriptan and ibuprofen in migraine. The study was a randomised placebo-controlled trial in a tertiary care teaching hospital. Migraine patients with <8 attacks/months were included. One hundred and fifty-five migraine patients were randomised to rizatriptan 10 mg (53), ibuprofen 400 mg (52) and placebo (50). Efficacy was assessed by headache relief, and headache freedom at 2 h and 24 h. Two-hour headache relief, was noted in 73% in rizatriptan, 53.8% in ibuprofen and 8% in placebo groups. Headache freedom was achieved in 37.7% in rizatriptan, 30.8% in ibuprofen and 2% in placebo groups. Rizatriptan was superior to ibuprofen and placebo in relieving headache at 2 h but not at 24 h. Side effects were noted in 9 patients in rizatriptan, 8 in ibuprofen and 3 in placebo, all of which were nonsignificant. Rizatriptan and ibuprofen are superior to placebo. Rizatriptan is superior to ibuprofen in relieving headache, associated symptoms and functional disability.
J Headache Pain 2007 Jun
PMID:Rizatriptan vs. ibuprofen in migraine: a randomised placebo-controlled trial. 1756 41

Migraine is a common, disabling disorder associated with considerable personal and societal burden. Current guidelines recommend triptans for the acute treatment of migraine unlikely to respond to less effective therapies. Rizatriptan is a second-generation triptan available in tablet or orally disintegrating tablet (wafer) formulations that offers several advantages over other members of its class. Rizatriptan is rapidly absorbed from the gastrointestinal tract and achieves maximum plasma concentrations more quickly than other triptans, providing rapid pain relief. Clinical trials have shown that rizatriptan is at least as effective or superior to other oral migraine-specific agents in the acute treatment of migraine, and has more consistent long-term efficacy across multiple migraine attacks. Rizatriptan has a favorable tolerability profile, and patients have reported greater satisfaction and a preference for rizatriptan over other migraine-specific agents. Improvements in quality of life reported with rizatriptan are consistent with its favorable efficacy and tolerability profiles. Notably, multi-attribute decision models that combine clinical data with patient- and physician-reported treatment preferences have identified rizatriptan as one of three triptans closest to a hypothetical "ideal". The efficacy and tolerability of rizatriptan for the acute treatment of migraine have thus been well established.
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PMID:Rizatriptan in the treatment of migraine. 1941 72


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