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Sumatriptan
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Sumatriptan

Sumatriptan (Imitrex®, Imigran®) is a triptan drug originally developed by Glaxo for the treatment of migraine headaches. Several dosage forms for sumatriptan have been approved, including tablets, solution for injection, and nasal inhalers. Sumatriptan was the first triptan available (in 1993), and is available only by prescription in the United States.


sumatriptan
4-methylaminosulfonyl-N,N-dimethyltryptamine
Chemical formula C14H21N3O2S
Molecular weight 295.40
Bioavailability 15% (oral)/ 96 % (s.c)
Metabolism MAO
Elimination half life 2.5 hours
Excretion 60% urine
40% feces
Pregnancy category C
Delivery tablet, subcutaneous injection, nasal spray, suppository
Indicated for:
Contraindications:
Side effects:
Severe:

Atypical sensations:

Cardiovascular: Ear, nose, and throat: Gastrointestinal: Muscular: Neurological: Respiratory: Skin: Miscellaneous:

Table of contents
1 Mode of action
2 Pharmacokinetics
3 References

Mode of action

Sumatriptan is a 5-HT (5-HT1D) agonist. The spesific receptor subtype it activates is present in the cranial and basilar arteries. Activation of these receptors causes a vasoconstriction of dilated arteries.

Pharmacokinetics

Sumatriptan is administered in several forms; tablets, subcutaneous injection, suppositories and nasal spray. Oral administration (as succinate) suffers from poor bioavailability, partly due to presystemic metabolism. A new rapid-release tablet formulation has the same bioavailability, but the maximum concentration is achieved on average 10-15 minutes earlier. As injection, sumatriptan is more fast acting (10-15 mins), but the effect lasts for a shorter time. Sumatriptan is metabolised primarily by Monoamine oxidase A into a indole acetic acid analogue, part of which is further conjugated with glucoronic acid. These metabolites are further excreted into the urine and bile.

References


Triptans
{Almotriptan} {Eletriptan} {Frovatriptan} {Naratriptan} {Sumatriptan} {Rizatriptan} {Zolmitriptan}
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