Almotriptan
AXERT
Pronunciation: al-moe-TRIP-tan (AX-ert)
What it is5-HT1B/1D agonist; acute migraine.
Why this oneAmong the best-tolerated triptans, with a low adverse-event rate.
What limits itCoronary vasospasm. Medication-overuse headache above ten days a month.
FDA-approved for
- migraine (2001)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Acute migraine | Adults & adolescents 12-17 yr | 6.25-12.5 mg single dose | 25 mg/day | |
| Acute migraine — hepatic or severe renal impairment | 6.25 mg single dose | 12.5 mg/day |
Renal Severe impairment: start 6.25 mg; max 12.5 mg/day
Hepatic Impairment: start 6.25 mg; max 12.5 mg/day
May repeat after 2 h; max 25 mg/24 h (12.5 mg/24 h in hepatic or severe renal impairment)
Instructions
- May repeat once after 2 hours if headache returns (efficacy of second dose not established); do not exceed 25 mg/day
- Safety of treating more than ~4 migraines per 30 days not established
Available strengths
- tab 6.25, 12.5 mg
Contraindications
- Ischemic or vasospastic coronary artery disease, or other significant cardiovascular disease
- Cerebrovascular syndromes (e.g., stroke or TIA)
- Peripheral vascular disease (including ischemic bowel disease)
- Uncontrolled hypertension
- Use within 24 hours of an ergotamine/ergot-type medication or another 5-HT1 agonist (triptan)
- Hemiplegic or basilar migraine
Cautions
- MAOIs due to risk of serotonin syndrome
- Myocardial ischemia/infarction and coronary vasospasm
- Chest/throat/neck/jaw pain, tightness, pressure
- Cerebrovascular events (some fatal)
- Peripheral and GI vasospastic ischemia
- Medication overuse headache
- Increases in blood pressure
- Caution in patients with sulfonamide hypersensitivity
Adverse reactions
- Adults: nausea, dry mouth, paresthesia, somnolence, headache
- Adolescents: dizziness, somnolence, headache, paresthesia, nausea, vomiting
Pregnancy Pregnancy Category C. Animal developmental toxicity at high doses; use only if potential benefit justifies risk.
Lactation Unknown whether excreted in human milk; use with caution (rat-milk levels up to 7x plasma).
Cost
Generic entry2015
NO BOXED WARNINGS
Principal riskCoronary vasospasm
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityAgent-specific vascular, serotonergic or hepatic risks; acute overdose is usually limited outside ergot or cardiovascular agents.
Serotonicity
This drug is routinely called serotonergic. By Gillman’s human-effect criteria it does not raise serotonin in the synapse.
Triptan receptor agonism is not a mechanistic serotonin-toxicity interaction with SRIs.
Gillman’s four human testsA measurable SERT affinity that fails all four is not clinical serotonicity.
- Retarded orgasm
- Efficacy in OCD and cataplexy
- Clonus and hyperreflexia in single-drug overdose
- Serotonin toxicity when combined with an MAOI
Non-elevating action5-HT1B/1D agonist
Evidence confidenceHigh
Background: what serotonicity is · what is and is not an SRI · what counts as a relevant MAOI.