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Application of Bioresponsive Polymers in Drug Delivery
Published in Deepa H. Patel, Bioresponsive Polymers, 2020
Manisha Lalan, Deepti Jani, Pratiksha Trivedi, Deepa H. Patel
Smart polymer-based hydrogels increased the residence time, but they may be exploited with other aims also. Rizatriptan benzoate used in the treatment of migraine suffers from extensive hepatic metabolism upon oral administration. Hence, Kempwade and Taranalli explored nasal delivery as an alternate to escape the first-pass metabolism. Thermo-reversible gels comprised of Poloxamer 407 and Carbopol were developed and investigated. Superior permeation and no toxicity of the developed formulation were observed [55].
Balance Disorders in Children
Published in John C Watkinson, Raymond W Clarke, Christopher P Aldren, Doris-Eva Bamiou, Raymond W Clarke, Richard M Irving, Haytham Kubba, Shakeel R Saeed, Paediatrics, The Ear, Skull Base, 2018
Louisa Murdin, Gavin A.J. Morrison
Attacks of vestibular migraine can be treated with domperidone, cinnarizine or cyclizine for nausea, vomiting or dizziness. Serotonin 5-HT1B/1D receptor agonists such as sumatriptan may be useful in management of headaches. Rizatriptan is reported to be more effective than other drugs of this class and other simple analgesics.14 Preventative measures, if necessary, would be those currently recognized – pizotifen or propanolol – and if those fail, a neurologist might prescribe the full range of antimigraine medications available to use in adults.16 Topiramate and flunairizine have randomized double-blind placebo-controlled trials in children that support their use, and there are open label studies in favour of sodium valproate.14
Migraine: diagnosis and treatment
Published in Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby, Headache in Clinical Practice, 2018
Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby
Rizatriptan has rapid oral absorption and high oral bioavailability at 45% for the 10-mg dose. Rizatriptan was significantly better than placebo for headache relief and complete relief at 2 hours. Rizatriptan (5 and 10 mg) has high consistency from attack to attack in formal blinded consistency studies and a wafer (Melt) formulation that many patients, particularly those with nausea as a prominent feature, find convenient, as it dissolves on the tongue and requires no water, although absorption is gastrointestinal, not transbuccal.48 Rizatriptan has a significant interaction with propranolol, which requires that the dose be halved to 5 mg, and its use is contraindicated with MAOIs because of its route of metabolism. Rizatriptan was significantly better than placebo at relieving recurrent headache pain.82
Pharmacological strategies to treat attacks of episodic migraine in adults
Published in Expert Opinion on Pharmacotherapy, 2021
A rough estimate of the time course up to 2 h is the calculation of the ratio TG at 1 h/TG at 2 h for each drug or dose. The mean of this ratio for pain freedom is approximately 0.25. Estimated by this ratio, only 25% of the ‘final effect’ at 2 h is present at 1 h. In theory, this could be caused by delayed absorption caused by gastric stasis during migraine attacks [30], but the absorption of some drugs during migraine is normal [30]. In addition, one can try to correlate the effects of rizatriptan and sumatriptan to the pharmacokinetics during attacks. During migraine attacks, 10 mg rizatriptan has a TG of 9% for pain freedom at 1 h (conc. 18 ng/ml) and 35% at 2 h, but the concentration of the drug decreases to 12 ng/ml (n = 18) [56]. During migraine, 100 mg sumatriptan has a TG at 1 h and 2 h of 6% (conc. 24 ng/ml) and 21% (conc. 31 ng/ml), respectively (n = 49) [57]. For 50 mg sumatriptan, the TG at 1 h and 2 h is 3% (conc. 13 ng/ml) and 16% (conc. 16 ng/ml), respectively (n = 47) [57]. The combined pharmacokinetic-pharmacodynamics for oral rizatriptan and oral sumatriptan during migraine attacks demonstrates a delay of effect onset, which is compatible with the results for the other oral triptans. For subcutaneous sumatriptan (6 mg), the Tmax is 10 min and a maximum effect occurs between 1 h and 2 h (Table 3), a considerable delay for the maximum effect.
Pharmacotherapy for acute migraines in children and adolescents
Published in Expert Opinion on Pharmacotherapy, 2019
P. Barbanti, L. Grazzi, G. Egeo
When the dose is adjusted, rizatriptan is effective and tolerated in migraineurs over ages of 6 years. In a three-way crossover RCT including children and adolescents receiving doses of 5 or 10 mg on the basis of body weight (< or ≥40 kg) during three attacks, rizatriptan was more effective than placebo for headache relief at 2 h and for all secondary efficacy end points (including relief at 1, 3, and 4 h), showing good consistency of response and good tolerability [30]. Positive results were also reported in a very large, parallel-group RCT performed in 191 sites worldwide and which enrolled 1382 ‘hard to treat’ children aged 6–17 years characterized by an unsatisfactory response to NSAIDs or acetaminophen and having an untreated migraine duration of ≥3 h. This study, which used a weight-based rizatriptan dosing (5 mg for <40 kg, 10 mg for ≥40 kg) and filtered out placebo responders using a run-in enrichment design, demonstrated rizatriptan superiority over placebo for 2 h pain freedom in 12–17-year olds (primary hypothesis; p = 0.025) and had comparable incidence of adverse events within 14 days of dose [31].
An update on acute and preventive treatments for migraine in children and adolescents
Published in Expert Review of Neurotherapeutics, 2020
Four studies have looked at the efficacy of rizatriptan in children and adolescents. Two of those studies found that with rizatriptan 5 mg in adolescents found no benefit in comparison to placebo with both having endpoints of pain relief at 2 hours [10,11]. However, the other two studies were double blind, randomized, placebo-controlled trials that found efficacy of rizatriptan versus placebo. [12,13] Both of those studies included children and adolescents 6–17 years of age and used a dose of 5 mg for less than 40 kg and 10 mg for 40 kg and above. In the first study, a three-way crossover design was used where three migraine attacks were treated at home with two of the capsules being rizatriptan and one was placebo. The goal of giving rizatriptan twice was to assess that the treatment was effective in consecutive migraine attacks. The endpoint of this study was to establish that there was pain reduction at 2 hours by at least 2 points on a 5 point scale. Headache relief at 2 h was 74% with first treatment of rizatriptan and 73% with the second treatment of rizatriptan, while placebo was 36%. Age and sex had no effect on the results[12]. In the second study, they found that the children and adolescents 12–17 years of age had 2-h pain freedom at 30.6% compared to 22% for placebo for the endpoint of 2-h pain freedom on a five-point pain scale. In children 6–11 years of age, they found that there was no clinical significance between the rizatriptan (39.4%) and placebo (36.7%)[13]. Side effects from both studies were minimal and included dizziness, dry mouth, burning feeling in the head, flushing of cheeks, fatigue, somnolence, nausea, vomiting, and upper abdominal pain. Side effects were slightly higher with increased dose of rizatriptan in both studies.