Bi-layered [1] tablet refers to tablet which contain subunits. In bi-layer [2] tablets, one layer tablet provides immediate release and the other layer acts as sustained release. Sumatriptan is a new class of anti-migraine [3] drugs that selectively activate 5-HT1B/1D receptors and are called triptans. Our objective is to formulate and evaluate the bi-layer tablets of sumatriptan succinate of d...

Sumatriptan succinate is an agonist for a vascular 5-hydroxytryptamine (5-HT)1 receptor subtype (probably a member of the 5-HT1D family). It does not have significant affinity for the remaining 5-HT receptors. It does not have affinity for alpha1, alpha2 or beta-adrenergic, dopamine1, dopamine2, muscarinic or benzodiazepine receptors. The objective of the study was to evaluate the in vitro tran...

Triptans are commonly used anti-migraine drugs and show agonist action mainly at serotonin 5-HT(1B/1D/1F) receptors. It is not known whether frequent or long-term treatment with these drugs would alter 5-HT receptor function. We investigated the effects of protracted (14-18 days) sumatriptan and zolmitriptan treatment in rats on 5-HT(1) receptor mRNA expression and function in tissues related t...

The effects of naratriptan, rizatriptan, and sumatriptan on arteriovenous oxygen saturation difference and carotid hemodynamics were compared in the anesthetized pig. Oxygen and carbon dioxide partial pressures in systemic arterial and jugular venous blood as well as hemoglobin oxygen saturation were determined by conventional blood gas analysis. Vehicle (n = 19) or naratriptan, rizatriptan, or...

OBJECTIVE To study the efficacy and practicality of treating headache in professional footballers with intranasal sumatriptan. METHODS An open label drug trial was performed in elite Australian footballers using intranasal sumatriptan (20 mg) treatment for acute headache. The main outcome measures were treatment response at 30 minutes, two hours, and 24 hours using two criteria: (a) initial s...

A number of drugs, including triptans, promote migraine chronification in susceptible individuals. In rats, a period of triptan administration over 7 days can produce "latent sensitization" (14 days after discontinuation of drug) demonstrated as enhanced sensitivity to presumed migraine triggers such as environmental stress and lowered threshold for electrically induced cortical spreading depre...

The Clinical Profile of Sumatriptan: Cluster Headache

We investigated whether headache-free patients with migraine report a lower health state compared with healthy controls, and whether health state is differently affected during the postattack period after using sumatriptan versus habitual nonvasoactive medication. Mood, health state, and personality questionnaires were administered once during an interictal period and twice within 30 hours afte...

❚ Evidence summary The prevalence of migraine headache is 6% among men and 15% to 17% among women. However, no standardized approach exists for the treatment of acute migraine headache. Systematic reviews of randomized controlled trials (RCTs) summarized that oral sumatriptan (Imitrex), Medications collectively referred to as “triptans” (eg, sumatriptan, naratriptan, etc) have been shown to be ...

Sumatriptan delivered in an electric patch form applied to the skin was approved by the Federal Drug Administration (FDA) in 2013 for the acute treatment of migraine. About 25 years ago, sumatriptan was the first drug in the medication class of triptans to be approved for the treatment of migraine. Sumatriptan already comes in a tablet, injectable form, nasal spray, and in at least 14 countries...