|Systematic (IUPAC) name|
|N,N-dimethyl-2- [5-(pyrrolidin-1-ylsulfonylmethyl)- 1H-indol-3-yl]-ethanamine|
|Mol. mass||335.465 g/mol|
|(what is this?)|
Almotriptan (trade names Axert (US, Canada), Almogran (Belgium, Denmark, Finland, France, Germany, Italy, Ireland Portugal, Spain, the United Kingdom, the Netherlands, Sweden, Switzerland, South Korea… ), Almotrex (Italy) and Amignul (Spain)) is a triptan drug discovered and developed by Almirall for the treatment of heavy migraine headache. It is available in 12.5 mg in most countries and also 6.25 mg in US and Canada.
Almotriptan is prescribed to treat the acute headache phase of migraine attacks with or without aura.
Almotriptan is the only oral triptan approved in the USA for the treatment of migraine in adolescent from 12 to 17 years of age.
Mechanism of action
Almotriptan has a high and specific affinity for serotonin 5-HT1B/1D receptors. Binding of the drug to the receptor leads to vasoconstriction of the cranial blood vessels and thus affects the redistribution of cranial blood flow. Almotriptan significantly increases cerebral blood flow and reduces blood flow through extracerebral cranial vessels. Even though it affects cranial blood vessels a single dose of almotriptan (12.5 mg) has no clinically significant effect on blood pressure or heart rate in both young and elderly healthy volunteers. However larger doses seem to slightly increase blood pressure but not beyond clinical relevance.
Almotriptan has a linear pharmacokinetic up to 200 mg dose. Its half life is 3 hours and nearly 70% bioavailability.
Cmax is observed 1.5–4 hours after oral administration and approximately 50% of the drug is excreted unchanged in the urine. Metabolism is mediated through MAO-A and CYP3A4 and CYP2D6 oxidation. Almotriptan clearance is moderately reduced in the elderly but does not require dose adjustment. Sex does not alter the pharmacokinetics of the drug. However, patients with moderate-to-severe renal dysfunction should limit their total daily dose to 12.5 mg. 
As mentioned previously almotriptan is metabolized mainly by MAO-A and to lesser extent by CYP3A4 and CYP2D6. Studies of drugs used as preventive against migraine (propranolol and verapamil), anti-depressants (moclobemide and fluoxetine) yielded results that showed significant altering of the pharmacokinetics of almotriptan though they were deemed not clinically relevant.
The efficacy and tolerability of almotriptan has been studied in numerous randomised, control-led trials totaling more than 4800 adults with either moderate or severe attacks of migraine. Its efficacy is significantly more effective than placebo and alleviates nausea, photophobia and phonophobia linked to migraine attacks. Compared to other triptan drug, 12.5 mg of almotriptan has similar efficacy as 50 mg of sumatriptan and fewer adverse effects.
(see SmPC) Hypersensitivity to the active substance or to any of the excipients.
As with other 5-HT1B/1D receptor agonists, almotriptan should not be used in patients with a history, symptoms or signs of ischaemic heart disease (myocardial infarction, angina pectoris, documented silent ischaemia, Prinzmetal’s angina) or severe hypertension and uncontrolled mild or moderate hypertension.
Patients with a previous cerebrovascular accident (CVA) or transient ischaemic attack (TIA). Peripheral vascular disease.
Concomitant administration with ergotamine, ergotamine derivatives (including methysergide) and other 5-HT1B/1D agonists is contraindicated.
Patients with severe hepatic impairment.
"For rare adverse events, please refer to the manufacturer´s webpage"
||This article includes a list of references, but its sources remain unclear because it has insufficient inline citations. (August 2012)|
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- Triptans (serotonin, 5-HT1B/1D agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials. MD Ferrari et al., (Cephalalgia 2002; 22:633-658)
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- Characteristics of migraine attacks and responses to almotriptan treatment: a comparison of menstrually related and nonmenstrually related migraines. Diamond ML et al., Headache 2008;48:248–258
- R&D page by Almirall Prodesfarma
- Axert Official homepage by Ortho-McNeil
- Axert prescribing information
- "Almotriptan Facts and Comparisons". Drugs.com. Retrieved 7 October 2012.
- Keam, SJ; Goa, KL; Figgitt, DP (2002). "Almotriptan: a review of its use in migraine.". Drugs 62 (2): 387–414. doi:10.2165/00003495-200262020-00010. PMID 11817980.
- McEnroe, JD; Fleishaker, JC (2005). "Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine.". Clinical pharmacokinetics 44 (3): 237–46. doi:10.2165/00003088-200544030-00002. PMID 15762767.