Sumatriptan, sold commonly under brand names Imitrex and Treximet.
It is in the triptan class of medications.
Sumatriptan is a medication used to treat migraine and cluster headaches.
It is taken orally, intranasally, or by subcutaneous injection.
Its therapeutic effects generally occur within three hours.
Bioavailability
15% by mouth and 96% by subcutaneous injection.
Protein binding 14–21%.
Metabolism MAO
Elimination half-life 2.5 hours
Excretion 60% urine; 40% feces
Its primary effect as a serotonin 5-HT1B/1D receptor agonist.
It is unclear if use during pregnancy or breastfeeding is safe.
Its mechanism of action not entirely established.
It is effective for ending or relieving the intensity of migraine and cluster headaches.
It is most effective when taken early in the process.
Injected sumatriptan is more effective than other formulations.
Oral sumatriptan can be used also in the treatment of post-dural puncture headache.
Side effects such as chest pressure, fatigue, vomiting, tingling, and vertigo.
The most common side effects reported by at least 2% of patients in controlled trials of sumatriptan for migraine are atypical sensations, paresthesias and warm/cold sensations, reported by 5–6%, pain and other pressure sensations, including chest pain, reported by 6–8%, neurological events, vertigo, reported in 1% to 2%, malaise/fatigue occurred in 2–3%. sleep disturbance occurred in 2% in the sumatriptan group.
Serious side effects may include serotonin syndrome, heart attacks, strokes, and seizures.
Overdose of sumatriptan can cause sulfhemoglobinemia.
Serious cardiac events have been reported: coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia, and ventricular fibrillation.
Sumatriptan is molecularly similar to serotonin (5-HT).
Ot is a 5-HT receptor agonist.
Sumatriptan’s primary therapeutic effect is related in its inhibition of the release of Calcitonin gene-related peptide (CGRP).
CGRP is believed to cause sensitization of trigeminal nociceptive neurons, contributing to the pain experienced in migraine.
Sumatriptan also shown decreases the activity of the trigeminal nerve, which presumably accounts for sumatriptan’s efficacy in treating cluster headaches.
The injectable form of the drug has been shown to abort a cluster headache within 30 minutes in 77% of cases.
Sumatriptan is administered in several forms: tablets, subcutaneous injection, and nasal spray.
Oral administration has low bioavailability, in part due to presystemic metabolism.
A rapid-release tablet formulation with the same bioavailability but a high concentration can achieve therapeutic effects on average 10–15 minutes earlier than other oral forumulations.
When injected it is faster-acting, usually within 10 minutes, but the effect lasts for a shorter time.
Sumatriptan is metabolized primarily by monoamine oxidase A.
Its metabolites are excreted in the urine and bile.
Only about 3% of the active drug may be recovered unchanged.
There is no simple, direct relationship between sumatriptan concentration per se in the blood and its anti-migraine effect.