Sumatriptan migraine

Sumatriptan is a 5HT (serotonin) agonist indicated in the treatment of migraine. Sumatriptan causes vasoconstriction and must therefore be used with caution in patients with coronary heart disease, such as angina. Concurrent administration of the agonist, sumatriptan and antagonists, such as fluoxetine, which is a selective serotonin re-uptake inhibitor, leads to increased CNS toxicity. 

Among the indole derivatives which have found use as drugs are indo-methacin, one of the first non-steroidal anti-inflammatory agentsfll], sumatriptan, which is used in the treatment of migraine headaches[12] and pindolol[13], one of the p-adrenergic blockers. 

Imitrex (Sumatriptan) 82 is the first selective 5-HTid agonist developed by Glaxo for the treatment of migraine. The synthesis of Imitrex has been carried out by several different routes all of which involved a Fischer indolization reaction as the key step. Outlined below is one of the synthetic routes. 

Interest in this receptor has been generated by the possibility that its activation accounts for the anti-migraine effects of the non-selective 5-HTib/id agonist, sumatriptan. The exact process(es) that account for this action are unresolved but... 

Sumatriptan succinate is effective for the treatment of acute migraine headaches by acting as... 

NSAIDs are contraindicated after 37 weeks gestation. For refractory migraines, narcotics may be used. Salicylates and indomethacin should be avoided throughout pregnancy if possible. The use of sumatriptan is controversial. Nausea of migraines may be treated with metoclopramide. 

Sumatriptan, zolmitriptan, naratriptan, rizatriptan, almotriptan, fro-vatriptan, and eletriptan are appropriate first-line therapies for patients with moderate to severe migraine or as rescue therapy when nonspecific medications are ineffective. 

Sumatriptan is a 5HT agonist, which is indicated in the treatment of acute migraine attacks. Sumatriptan may cause vasoconstriction as a side-effect and therefore its use is reserved for patients in whom other conventional migraine analgesics have failed. 

Serotonin syndrome (sibutramine) The rare, but serious, constellation of symptoms also has been reported with the concomitant use of selective serotonin reuptake inhibitors and agents for migraine therapy (eg, sumatriptan, dihydroergotamine), certain opioids (eg, dextromethorphan, meperidine, pentazocine, fentanyl), lithium, or tryptophan. Because sibutramine inhibits serotonin reuptake, it should not be administered with other serotonergic agents. 

Not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Safety and efficacy have not been established for cluster headache, which is present in an older, predominantly male population (almotriptan, eletriptan, frovatriptan, sumatriptan tablets and spray, zolmitriptan). 

Sumatriptan (Imitrex) [Antimigraine Agent/Selective 5-HTi Receptor Agonist] Uses Rx acute migraine Action Vascular serotonin receptor agonist Dose Adults. SQ 6 mg SQ as a single dose PRN repeat PRN in 1 h to a max of 12 mg/24 h PO 25 mg, repeat in 2 h, PRN, 100 mg/d max PO dose max 300 mg/d Nasal spray 1 spray into 1 nostril, repeat in 2 h to 40 mg/24 h... 

Sumatriptan was specifically developed as an anti-migraine drug. Injectable sumatriptan has been shown to be more effective than injectable DHE at two hours but the rate of recurrence (30 0%) is higher than with DHE. Efficacy is better and delay to action is shorter with the injectable formulation. Both the nasal spray and the injectable formulation... 

The adverse effects of the different members of the triptan class are quite similar, with the exception of chest oppression which is frequent with sumatriptan. Nausea, vomiting, fatigue, vertigo are frequently reported. Triptans are contraindicated (perhaps excessively) in aura migraine. 

Wilkinson M, Pfaffenrath V, Schoenen J, Diener HC, Steiner TJ. Migraine and cluster headache their management with sumatriptan a critical review of the current clinical experience. Cephalalgia 1995 15 337-57. 

Triptans and dihydroergotamine are drugs of choice for moderate to severe migraine attacks nasal sumatriptan is usually considered the triptan of choice due to its rapid onset there are a number of oral triptans, including frovatriptan, with more favorable biopharmaceuticprofiles and high costs comparisons not available... 

Alternative to sumatriptan for the treatment of migraine headache has not been compared head-to-head with sumatriptan choice should be based on cost and availability... 

Effects of sumatriptan (734 patients) or placebo (370 patients) on symptoms of acute migraine headache 60 minutes after injection of 6 mg subcutaneously. All differences between placebo and sumatriptan were statistically significant. 

Data from Cady RK et al Treatment of acute migraine with subcutaneous sumatriptan. JAMA 1991 265 2831.)... 

Sumatriptan Partial agonist at 5-HT1B/1D receptors Effects not fully understood may reduce release of calcitoningene-related peptide and perivascular edema in cerebral circulation Migraine and cluster headache Oral, nasal, parenteral duration 2 h Toxicity Paresthesias, dizziness, coronary vasoconstriction Interactions Additive with other vasoconstrictors... 

The most recent treatment for migraine is a class of compounds known as the "triptans" - sumatriptan and its progeny. These seem to be about 65% effective and show fewer side effects. 

Buzzi, M. G. and Moskowitz, M. A. The anti-migraine drug sumatriptan (GR 43175), selectively blocks neurogenic plasma extravasation from blood vessels in dura mater, Br. J. Pharmacol. 1990, 99, 202-206. 

Moskowitz, M. A. Neurogenic vs. vascular mechanisms of sumatriptan and ergot alkaloids in migraine, Trends Pharmacol. Sci. 1992, 13, 307-311. 

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