Rizatriptan was launched for the first time as Maxalt in Mexico for the
acute treatment of migraine headaches with or without aura in adults. It is the
third in a new generation of triptan migraine drugs to challenge the firstgeneration
product Sumatriptan from Glaxo Wellcome, after Zolmitriptan
(Zeneca) and Naratriptan (Glaxo Wellcome).
It can be synthetically obtained by two related routes having respectively 3 and 4
steps, both starting from 1 -(4-aminobenzyl)-l,2,4-triazole. Rizatriptan is a full 5-HT1D/1B receptor agonist retaining a significant affinity at 5-HT1A sites (pIC50
= 6.4), with a low affinity for nond-HT sites. It shows craniovascufar selectivity
for human isolated middle meningeal over coronary arteries ; its effect on
coronary artery constriction is significantly less than that for Sumatriptan.
Rizatriptan inhibits the release of neuropeptides that cause swelling of cranial
blood vessels. Rizatriptan has a good oral bioavailability (64% and 47% in rats
and dogs respectively). and a rapid onset of action : the headache relief in
human occurs within 30 to 45 minutes of taking 20 mg. It also relieved nausea
and hypersensitivity to noise (phonophobia) and light (photophobia) that are
often symptoms accompanying a migraine attack. Among at least 6 metabolites
identified in humans after a single oral dose (60 mg), the major urinary
metabolite was the corresponding indole-3-acetic acid. Maxalt is available as a
novel oral formulation of rapidly dissolving tablets or wafers that does not require
liquid for ingestion.
화학적 성질
Off-White Solid
용도
Rizatriptan Benzoate is a selective serotonin 5-HTID receptor agonist and used to treat migraine (1,2,3). It is structurally derived from tryptamine.
일반 설명
Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards
