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Sumatriptan belongs to the class of medications called
as selective serotonin receptor agonists.
Sumatriptan belongs to the class of medications called as
selective serotonin receptor agonists. Sumatriptan is used to treat the
symptoms of migraine headaches (severe, throbbing headaches that sometimes are
accompanied by nausea or sensitivity to sound and light).
Pharmacological
class: Selective serotonin receptor agonist
Sumatriptan, an antimigraine drug, is a selective agonist of
vascular serotonin (5hydroxytryptamine; 5-HT) type 1-like receptors, likely the
5-HT1D and 5-HT1B subtypes. The 5-HT1B and 5-HT1D receptors function as auto
receptors, which inhibit the firing of serotonin neurons and a reduction in the
synthesis and release of serotonin upon activation. After sumatriptan binds to
these receptors, adenylate cyclase activity is inhibited via regulatory G
proteins, increases intracellular calcium, and affects other intracellular
events. This results in vasoconstriction and inhibition of sensory nociceptive
(trigeminal) nerve firing and vasoactive neuropeptide release.
Adult Dose for Migraine:
Oral:
Initial dose: 25
mg, 50 mg, or 100 mg orally, once
Maximum dose: 200
mg per 24 hours
Subcutaneous:
Initial dose: 1
to 6 mg subcutaneously, once
Maximum dose: 12
mg per 24 hours
Intranasal:
Nasal spray:
Initial dose: 5 mg, 10 mg, or 20 mg into one nostril, once
Sumatriptan shows 15% absorption. It shows 14%-21% protein
binding. Sumatriptan is metabolized by monoamine oxidase (MAO), predominantly
the A isoenzyme. Only 3% of the dose is excreted in the urine as unchanged
sumatriptan; 42% of the dose is excreted as the major metabolite, the indole
acetic acid analogue of sumatriptan. The half-life of sumatriptan is 2.5 hours.
Common (affecting between 1
in 10 to 1 in 100):
Uncommon (affecting 1 in 100 to 1 in 1000):
Very rare (affecting less than 1 in 10,000):
Data from 6 randomized, double-blind, placebo-controlled, early-intervention studies of sumatriptan tablets 50 mg and 100 mg were pooled for analysis. These constitute all the studies conducted to date of sumatriptan tablets prospectively given early for mild pain. In this analysis of pooled data from 6 clinical trials, sumatriptan tablets 50 mg and 100 mg administered early in a migraine attack while the pain was mild were well tolerated and significantly more effective than placebo. The 100-mg dose of sumatriptan was significantly more effective than the 50-mg dose.1
The efficacy and tolerability of oral sumatriptan were
assessed in 187 migraineurs enrolled in a randomized, double-blind,
parallel-group, placebo-controlled study. In the clinic, patients received oral
sumatriptan 25 mg, 50 mg, or 100 mg, or placebo, for the treatment of a
migraine attack. The results demonstrate that by 2 hours post dose, 52 to 57%
of patients treated with sumatriptan 25 mg, 50 mg, 100 mg compared with 17% of
patients treated with placebo achieved relief of headache (p < 0.05 for each
sumatriptan group vs placebo). By 4 hours post dose, 65 to 78% of
sumatriptan-treated patients compared with 19% of placebo-treated patients
achieved relief of headache (p < 0.05 for each sumatriptan group vs
placebo). Oral sumatriptan also effectively relieved nausea and photophobia and
improved clinical disability.2
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