Safety profile of the triptans.
The triptans are 5-HT(1B/1D) agonists used as migraine and cluster-specific agents. Seven are in commercial use worldwide; in order of release these are sumatriptan, zolmitriptan, rizatriptan, naratriptan, almotriptan, frovatriptan and eletriptan. Sumatriptan has been in clinical use since 1991, and although postmarketing studies have stimulated much debate of triptan strengths and weaknesses, their overall safety profile appears excellent. The most serious adverse events are cardiovascular, due to coronary artery narrowing as a consequence of coronary artery 5-HT(1B) receptor activity. Triptans are contraindicated in patients with vascular disease. Other events are even more rare, and include the potential for drug-drug interactions, based on metabolic elimination pathways. Serotonin syndrome has been a concern, but one large prospective study failed to document a single case, and reports are sporadic and not clearly causative.
Tepper
Stewart J
SJ
The New England Center for Headache, 778 Long Ridge Rd, Stamford, CT 06902, USA. sjtepper@aol.com
Millson
David
D
D018435:ATP Binding Cassette Transporter, Subfamily B / Q000378:metabolism; D003027:Cluster Headache / Q000188:drug therapy*; D019388:Cytochrome P-450 CYP1A2 / Q000378:metabolism; D019389:Cytochrome P-450 CYP2D6 / Q000378:metabolism; D051544:Cytochrome P-450 CYP3A; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D004347:Drug Interactions; D006801:Humans; D008881:Migraine Disorders / Q000188:drug therapy*; D058825:Serotonin 5-HT1 Receptor Agonists; D017366:Serotonin Receptor Agonists / Q000009:adverse effects* / Q000493:pharmacokinetics / Q000627:therapeutic use*
D018435:ATP Binding Cassette Transporter, Subfamily B; D058825:Serotonin 5-HT1 Receptor Agonists; D017366:Serotonin Receptor Agonists; D003577:Cytochrome P-450 Enzyme System; C104464:CYP3A protein, human; D019388:Cytochrome P-450 CYP1A2; D019389:Cytochrome P-450 CYP2D6; D051544:Cytochrome P-450 CYP3A