A review of the 5-HT1B/1D agonist rizatriptan: update on recent research and implications for the future

Mannix, Lisa K.

doi:10.1517/14656566.9.6.1001

Cited by 12 publications

(12 citation statements)

References 56 publications

(71 reference statements)

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“…However, with the only exception of a head-to-head randomized trial versus sumatriptan [10], frovatriptan efficacy had never been tested in comparative trials with other triptans. For this reason a study was setup to compare efficacy and safety of frovatriptan versus rizatriptan, the triptan known to provide consistent relief of migraine attacks and usually preferred over other treatments because of its speed of relief [11, 12]. …”

Section: Introductionmentioning

confidence: 99%

A double-blind, randomized, multicenter, Italian study of frovatriptan versus rizatriptan for the acute treatment of migraine

et al. 2010

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The objective of this study was to assess patient satisfaction with acute treatment of migraine with frovatriptan or rizatriptan by preference questionnaire. 148 subjects with a history of migraine with or without aura (IHS 2004 criteria), with at least one migraine attack per month in the preceding 6 months, were enrolled and randomized to frovatriptan 2.5 mg or rizatriptan 10 mg treating 1–3 attacks. The study had a multicenter, randomized, double-blind, cross-over design, with treatment periods lasting <3 months. At the end of the study, patients assigned preference to one of the treatments using a questionnaire with a score from 0 to 5 (primary endpoint). Secondary endpoints were pain-free and pain relief episodes at 2 h, and recurrent and sustained pain-free episodes within 48 h. 104 of the 125 patients (83%, intention-to-treat population) expressed a preference for a triptan. The average preference score was not significantly different between frovatriptan (2.9 ± 1.3) and rizatriptan (3.2 ± 1.1). The rates of pain-free (33% frovatriptan vs. 39% rizatriptan) and pain relief (55 vs. 62%) episodes at 2 h were not significantly different between the two treatments. The rate of recurrent episodes was significantly (p < 0.001) lower under frovatriptan (21 vs. 43% rizatriptan). No significant differences were observed in sustained pain-free episodes (26% frovatriptan vs. 22% rizatriptan). The number of patients with adverse events was not significantly different between rizatriptan (34) and frovatriptan (25, p = NS). The results suggest that frovatriptan has a similar efficacy to rizatriptan, but a more prolonged duration of action.Electronic supplementary materialThe online version of this article (doi:10.1007/s10194-010-0243-y) contains supplementary material, which is available to authorized users.

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Section: Introductionmentioning

confidence: 99%

A double-blind, randomized, multicenter, Italian study of frovatriptan versus rizatriptan for the acute treatment of migraine

et al. 2010

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“…Therefore, Krymchantowski and Bigal conclude that recent evidence that has been gathered on combination therapies utilizing rizatriptan plus NSAID and even gastrokinetic drugs, such as trimebutine, point to a future of more effective combined therapy for migraine [34]. Targeting other associated mechanisms, such as inflammation and gastric stasis, that occur during the migraine attack, by combining triptans with anti-inflammatory and/or prokinetic agents may possibly enhance the clinical outcomes [35]. …”

Section: Discussionmentioning

confidence: 99%

Combined analgesics in (headache) pain therapy: shotgun approach or precise multi-target therapeutics?

et al. 2011

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BackgroundPain in general and headache in particular are characterized by a change in activity in brain areas involved in pain processing. The therapeutic challenge is to identify drugs with molecular targets that restore the healthy state, resulting in meaningful pain relief or even freedom from pain. Different aspects of pain perception, i.e. sensory and affective components, also explain why there is not just one single target structure for therapeutic approaches to pain. A network of brain areas ("pain matrix") are involved in pain perception and pain control. This diversification of the pain system explains why a wide range of molecularly different substances can be used in the treatment of different pain states and why in recent years more and more studies have described a superior efficacy of a precise multi-target combination therapy compared to therapy with monotherapeutics.DiscussionIn this article, we discuss the available literature on the effects of several fixed-dose combinations in the treatment of headaches and discuss the evidence in support of the role of combination therapy in the pharmacotherapy of pain, particularly of headaches. The scientific rationale behind multi-target combinations is the therapeutic benefit that could not be achieved by the individual constituents and that the single substances of the combinations act together additively or even multiplicatively and cooperate to achieve a completeness of the desired therapeutic effect.As an example the fixesd-dose combination of acetylsalicylic acid (ASA), paracetamol (acetaminophen) and caffeine is reviewed in detail. The major advantage of using such a fixed combination is that the active ingredients act on different but distinct molecular targets and thus are able to act on more signalling cascades involved in pain than most single analgesics without adding more side effects to the therapy.SummaryMultitarget therapeutics like combined analgesics broaden the array of therapeutic options, enable the completeness of the therapeutic effect, and allow doctors (and, in self-medication with OTC medications, the patients themselves) to customize treatment to the patient's specific needs. There is substantial clinical evidence that such a multi-component therapy is more effective than mono-component therapies.

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“…Rizatriptan is also a selective serotonin 5-HT 1 (1B/1D) agonist 15,16. It is rapidly absorbed, eliminated with a plasma half-life of approximately 2–3 hours, and is reported to induce rapid pain relief 15–17.…”

Section: Introductionmentioning

confidence: 99%

“…While both frovatriptan and rizatriptan have independently proven efficacy and tolerability for the treatment of acute migraine,11,16 only two head-to-head trials have actually compared the efficacy of these two triptans 19,20. Both studies were performed on Italian migraineurs (one of which was in females with migraine that was menstrually related), and both demonstrated similar antimigraine efficacy of the two triptans in terms of pain-free and pain-relief rates.…”

Section: Introductionmentioning

confidence: 99%

Efficacy and pharmacokinetic activity of frovatriptan compared to rizatriptan in patients with moderate-to-severe migraine

Savi¹,

Mogavero²,

Egan³

2014

DDDT

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BackgroundMigraine is a painful neurological disorder that affects over 10% of the general population. Frovatriptan and rizatriptan are antimigraine agents belonging to the triptan class. Although previous studies have independently compared the efficacy of these agents, contemporaneous data examining both pharmacokinetic (PK) properties and efficacy in parallel have not previously been available.Materials and methodsIn this single-center double-blind study, 18 subjects (ten female) were treated for a single migraine attack with frovatriptan 2.5 mg or rizatriptan 10 mg. Plasma concentrations were measured predose and at 2, 4, 6, 12, 24, 48, and 72 hours after drug administration. The primary end point of this study was to evaluate the association between PK parameters and efficacy measures and recurrence rate. Secondary end points were pain-free and pain-relief episodes at 2 and 4 hours, recurrent episodes within 48 hours, and cumulative hazard of recurrence within 72 hours.ResultsAt baseline, approximately 17% of patients had mild migraine, while 83% had moderate–severe migraine. Although the time to maximum concentration was similar for both drugs (2.7 versus 2.3 hours), the terminal half-life for frovatriptan was longer than rizatriptan (29.3 versus 3.2 hours, P<0.0001). The proportion of patients who were pain-free at 4 hours without rescue medication was higher in the frovatriptan-treated group, (38.9 versus 5.6%, P=0.045). The cumulative hazard of recurrence over 72 h was reduced by frovatriptan compared to rizatriptan-treated patients (log-rank test, P=0.04). Pain-free and pain-relief episodes for the study period were positively correlated with the concentration:maximum concentration (Cmax) ratio for frovatriptan (r=0.52, P=0.028), but not rizatriptan. Recurrence rate was negatively correlated with the concentration:Cmax ratio for both frovatriptan (r=−0.96, P=0.0024) and rizatriptan (r=−0.98, P=0.0004). Fewer adverse events were observed for frovatriptan compared to rizatriptan (one versus eight, P=0.021).ConclusionThis pilot study indicates that a similar extent of initial pain relief is afforded by both triptans in migraine treatment. The longer duration of action of frovatriptan parallels and correlates with its PK profile.

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A review of the 5-HT1B/1D agonist rizatriptan: update on recent research and implications for the future

Abstract: In the context of these newly available data, the potential for expansion of the role of rizatriptan in the clinic is evaluated.

Cited by 12 publications

References 56 publications

A double-blind, randomized, multicenter, Italian study of frovatriptan versus rizatriptan for the acute treatment of migraine

A double-blind, randomized, multicenter, Italian study of frovatriptan versus rizatriptan for the acute treatment of migraine

Combined analgesics in (headache) pain therapy: shotgun approach or precise multi-target therapeutics?

Efficacy and pharmacokinetic activity of frovatriptan compared to rizatriptan in patients with moderate-to-severe migraine

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