|Trade names||Zomig, others|
|Main uses||Migraines, cluster headaches|
|Side effects||Tingling, nausea, dry mouth, dizziness, medication overuse headaches|
|By mouth, nasal spray|
|Typical dose||2.5 to 5 mg|
|Bioavailability||40% (by mouth)|
|Metabolism||Liver (CYP1A2-mediated, to active metabolite)|
|Elimination half-life||3 hours|
|Excretion||Kidney (65%) and fecal (35%)|
|Chemical and physical data|
|Molar mass||287.363 g·mol−1|
|3D model (JSmol)|
Zolmitriptan, sold under the brand name Zomig among others, is a medication used to treat migraine attacks and cluster headaches. It may also be used to prevent menstrual migraines. It is used as a tablet by mouth or as a nose spray.
Common side effects include tingling, nausea, dry mouth, and dizziness. Other side effects may include medication overuse headaches. Serious side effects may include coronary vasospasm, stroke, high blood pressure, anaphylaxis, and serotonin syndrome. It is unclear if use during pregnancy or breastfeeding is safe. It is a triptan that works as a selective serotonin receptor agonist of the 1B and 1D subtypes.
Zolmitriptan was patented in 1990 and approved for medical use in 1997. It is avaliable as a generic medication. In the United Kingdom 6 doses costs the NHS about £12 as of 2020. This amount in the United States costs about 30 USD as of 2021.
People who get migraines from aspartame should not use the disintegrating tablet (Zomig ZMT), which contains aspartame.
A 2014 Cochrane review found that zolmitriptan 5 mg nasal spray was more effective than the 5 mg tablet by mouth.
- Acute treatment of cluster headaches—Level A recommendation from the American Academy of Neurology
- Acute treatment of menstrual migraine
Zolmitriptan is available as a swallowable tablet, an oral disintegrating tablet, and a nasal spray, in doses of 2.5 and 5 mg.
Zolmitriptan is contraindicated in people with cerebrovascular or cardiovascular disease because 5-HT 1B receptors are present in coronary arteries. Such conditions include, but are not limited to, coronary artery disease, stroke, and peripheral vascular disease.
As for cardiovascular side effects, zolmitriptan can increase systolic blood pressure in the elderly and increase diastolic blood pressure in both the elderly and young people. Additionally, there is the side effect of a dose-related increase in sedation. There is a risk of headaches caused by medication withdrawal or medication overuse.
Zolmitriptan has a weak affinity for 5-HT 1A receptors; these receptors have implications in the development of serotonin syndrome.
Mechanism of action
Zolmitriptan is a selective 5-hydroxytryptamine 1B/1D receptor agonist with a weak affinity for the 5-HT 1A receptor subtypes. Its action on 5-HT 1B/1D receptors causes vasoconstriction in intracranial blood vessels; as well it can inhibit the release of pro-inflammatory neuropeptides from trigeminal perivascular nerve endings. It crosses the blood-brain-barrier as evidenced by the presence of radioactive [3H]-zolmitriptan labels within the cells of the trigeminal nucleus caudalis and nucleus tractus solitaries.
Zolmitriptan has a rapid onset of action and has been detected in the brain as early as within 5 minutes of intranasal administration. On average, zolmitriptan has an oral bioavailability of 40%, a mean volume of distribution of 8.3 L/kg after oral administration, and 2.4L/kg after intravenous administration.
Zolmitriptan is metabolized into three major metabolites by the human hepatic cytochrome P450 enzymes—primarily CYP1A2. Two-thirds of the parent compound breaks down into the active metabolite N-desmethyl-zolmitriptan (183C91), while the remaining one-third separates into the other two inactive metabolites: zolmitriptan N-oxide and an indole acetic acid derivative. It has an elimination half-life of about three hours before it undergoes renal elimination; its clearance is greater than the glomerular filtration rate suggesting that there is some renal tubular secretion of the compound.
Society and culture
Zolmitriptan is marketed by AstraZeneca with the brand names Zomig, Zomigon (Argentina, Canada & Greece), AscoTop (Germany) and Zomigoro (France).
In 2008, Zomig generated nearly $154 million in sales.
AstraZeneca's U.S. patent on the tablets expired on November 14, 2012, and its pediatric exclusivity extension expired on May 14, 2013. The patent in certain European countries has already expired too, and generic drug maker Actavis released a generic version in those countries, starting in March 2012.
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ДМТ (диметилтриптамин) и его производные, за исключением производных, включенных в качестве самостоятельных позиций в перечень
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