Rizatriptan in the treatment of migraine

Láinez, Miguel J. A.

doi:10.2147/nedt.2006.2.3.247

Cited by 27 publications

(14 citation statements)

References 74 publications

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“…The triptans and nonsteroidal anti-inflammatory drugs have been found to provide a symptomatic relief in migraine (3). Rizatriptan benzoate is a selective 5-hydroxytriptamine (5-HT) 1B/1D receptor agonist which is used for the acute treatment of migraine in adults with or without aura (4). Although it is a cost effective oral triptan available for the treatment of migraine, it suffers from some drawbacks such as poor oral bioavailability due to an extensive first-pass effect and the bitter taste (5).…”

Section: Introductionmentioning

confidence: 99%

Taste Masked Oral Fast Dissolving Sublingual Strips of Rizatriptan Benzoate for Migraine Therapy

Mali¹,

Dias²,

Ghorpade³

et al. 2017

Marmara Pharmaceutical Journal

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The aim of present investigation was to develop a taste masked fast dissolving sublingual strips of rizatriptan benzoate. The fast dissolving strips (FDS) were prepared by solvent casting method using polyox N-10 and polyethylene glycol 400 (PEG 400) as polymer and plasticizer respectively. The FDS were evaluated for pH, folding endurance, tensile strength, moisture absorption, disintegration time and in vitro dissolution. All formulations were free from bubble and exhibited smooth appearance. The pH of the films was acidic. It was observed that increase in the concentration of polyox N-10 increased the disintegration time but reduced the dissolution rate. The formulation A2 showed all the evaluation parameters within the acceptable range and was considered as optimized formulation. The optimized formulation was subjected to the taste masking and stability study. The results of taste masking study indicated an efficient masking of the bitter taste of drug by the flavouring agents in the film. The formulation A2 was found to be stable for three months with an insignificant change in the drug content and mean dissolution time (MDT). The compatibility study performed using ATR-FTIR and DSC analysis indicated absence of any unusual interaction between drug and excipients used in formulation. Thus, the FDS comprised of polyox N-10 and PEG 400 may be a better alternative to the other available fast dissolving systems for delivery of rizatriptan benzoate.

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Section: Introductionmentioning

confidence: 99%

Taste Masked Oral Fast Dissolving Sublingual Strips of Rizatriptan Benzoate for Migraine Therapy

Mali¹,

Dias²,

Ghorpade³

et al. 2017

Marmara Pharmaceutical Journal

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“…It is available either as a tablet or as a wafer (orally disintegrating tablet [ODT]). 48 The efficacy of rizatriptan has been demonstrated in randomised, double-blind, placebo-controlled trials. In one study, 80 patients with unilateral cranial autonomic symptoms were treated for a single moderate or severe migraine attack with 10 mg rizatriptan (wafer) or placebo.…”

Section: Rizatriptanmentioning

confidence: 99%

Overview of Triptans in the Treatment of Acute Migraine

Cortelli¹,

Allais²,

Benedetto³

2017

European Neurological Review

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T he advent of triptans for effective relief of migraine represented a therapeutic breakthrough. Triptans are serotonin (5-hydroxytryptamine, or 5-HT) agonists with high affinity for 5-HT 1B and 5-HT 1D receptors. There are, at present, seven commonly used triptans: almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, and zolmitriptan. Some controversy still surrounds the mode of action of this class. When first studied, it was thought that triptans provided relief from migraine through cranial vasoconstriction, probably via action at postsynaptic 5-HT 1B receptors on the smooth-muscle cells of blood vessels. More recently, however, triptans have also been demonstrated to block release of vasoactive peptides from the perivascular trigeminal neurons owing to their action at presynaptic 5-HT 1D receptors on the nerve terminal. Triptans may also facilitate descending pain inhibitory systems. However, it is not certain whether or not the activation of vascular 5-HT 1B receptors is essential for relieving migraine. Many drug characteristics need to be taken into account when selecting the best triptan for an individual patient. Clinical characteristics of the migraine attack and the patient's lifestyle and medical history are also important. Despite their biochemical similarity, triptans have distinct pharmacokinetic and pharmacodynamic profiles. Frovatriptan and naratriptan, for example, have a longer half-life and therefore a delayed onset of action and prolonged duration compared with the other triptans, which are fast acting, with a rapid dose-dependent efficacy and higher risk of adverse events and migraine recurrence. Migraine recurrence is affected by the pharmacological and pharmacokinetic properties of the triptan but is unrelated to initial clinical efficacy. Triptans with a longer half-life and largest 5-HT 1B receptor affinity have the lowest rates of headache recurrence.

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“…It is used for treating acute migraine with and without aura and minimising migraine symptoms, including pain, nausea, and photophobia or phonophobia. The half life of rizatriptan is 2-3 hrs and absorption is rapid up to 90%, but absolute bioavailability is low, i.e., 47% because of high first pass effect when taken orally [11,12].…”

Section: Introductionmentioning

confidence: 99%

Formulation of Rizatriptan Benzoate Sublingual Tablets Prepared by Direct Compression With Different Bioadhesive Polymer: In Vitro and Ex Vivo Evaluation

Singh

Jaiswal

Gupta

et al. 2017

Asian J Pharm Clin Res

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Objective: The current investigation deals with formulation and evaluation of fast disintegrating sublingual tablets of rizatriptan benzoate (RTB) to produce its intended therapeutic effect for acute treatment of migraine. When the drug is given by sublingual route, it overcomes the first pass metabolism and quick entry of drug in systemic circulation is obtained. It would result in fast pharmacological response hence faster relief from migraine which is an important criterion in migraine therapy.Methods: In this study, RTB sublingual tablets were prepared using direct compression process using various bioadhesive polymers such as sodium carboxymethyl cellulose, hydroxyl propyl methyl cellulose-K4M, and chitosan at various concentration ranging 0.5-5% w/w along with sodium starch glycolate (SSG) or cross carmellose sodium (CCS) as super disintegrants at different concentration ranging 2-8% w/w.Results: The tablets disintegrated quickly and dissolution tests conclude that RTB was released from the formulation within the compendial limits. The formulations batches (A8 and B8) containing 2% w/w chitosan along with 2% w/w SSG or CCS which disintegrate rapidly and show high dissolution and ex vivo permeation were selected as optimized formulations.Conclusion: The results obtained from the study showed that the bioavailability problem of the drug has been solved as the drug is given by sublingual route and it directly enters into systemic circulation. Furthermore, the formulation overcomes the problems associated with migraine attack as fast disintegrating technology is used.

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Rizatriptan in the treatment of migraine

Cited by 27 publications

References 74 publications

Taste Masked Oral Fast Dissolving Sublingual Strips of Rizatriptan Benzoate for Migraine Therapy

Taste Masked Oral Fast Dissolving Sublingual Strips of Rizatriptan Benzoate for Migraine Therapy

Overview of Triptans in the Treatment of Acute Migraine

Formulation of Rizatriptan Benzoate Sublingual Tablets Prepared by Direct Compression With Different Bioadhesive Polymer: In Vitro and Ex Vivo Evaluation

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