Ball-and-stick model of the almotriptan molecule
Clinical data
Trade names Axert
AHFS/ Monograph
MedlinePlus a603028
  • US: C (Risk not ruled out)
Routes of
ATC code N02CC05 (WHO)
Legal status
Legal status
Pharmacokinetic data
Bioavailability 70%
Protein binding 35%
Metabolism Hepatic
Biological half-life 3–4 hours
CAS Number 154323-57-6 N
PubChem (CID) 123606
DrugBank DB00918 YesY
ChemSpider 110198 YesY
KEGG D02824 YesY
ChEBI CHEBI:520985 YesY
Chemical and physical data
Formula C17H25N3O2S
Molar mass 335.465 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Almotriptan (trade name Axert and others) is a triptan drug discovered and developed by Almirall for the treatment of heavy migraine headache.

Medical uses

Almotriptan is prescribed to treat the acute headache phase of migraine attacks with or without aura.[1] Almotriptan is the only oral triptan approved in the USA for the treatment of migraine in adolescent from 12 to 17 years of age.


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. Almotriptan has similar efficacy as a standard dose of sumatriptan, another triptan drug, and fewer adverse effects.[2]


As with other triptans, 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. Other contraindications are previous cerebrovascular accident (CVA) or transient ischaemic attack (TIA), peripheral vascular disease, severe hepatic impairment, concomitant administration of ergotamine, ergotamine derivatives (including methysergide) and other 5-HT1B/D agonists.

Side effects

Almotriptan has proved to have an adverse effects profile similar to placebo when used following the Summary of Product Characteristics instructions (see references).


Mechanism of action

Like all triptans, 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 (brain) blood vessels and thus affects the redistribution of 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 standard dose of almotriptan has no clinically significant effect on blood pressure or heart rate in both young and elderly healthy volunteers. Larger doses seem to slightly increase blood pressure but not beyond clinical relevance.[2]


Almotriptan has linear pharmacokinetics up to the 16-fold standard dose. Its biological half-life is 3 hours, and its bioavailability 70%. 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 the enzymes 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. People with moderate-to-severe renal dysfunction are recommended to use only half the dose.[3]


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.[2]

Society and culture

Brand names

Brand names include 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).


  1. "Almotriptan Facts and Comparisons". Retrieved 7 October 2012.
  2. 1 2 3 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.
  3. 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.

External links

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