Generic
Almotriptan
2 brands available in the market
At a glance
Almotriptan is a selective serotonin receptor agonist used for the acute treatment of migraine attacks. It constricts blood vessels in the brain and relieves migraine headaches.
Description
Almotriptan is a selective and potent serotonin (5-HT1B/1D) receptor agonist. It binds to specific serotonin receptors on meningeal arteries, inhibiting the release of vasoactive peptides and causing arterial constriction. Migraine headaches result from dilation of cerebral blood vessels and release of vasoactive and pro-inflammatory peptides from sensory nerve endings. Almotriptan constricts these blood vessels and prevents the release of chemical messengers, thereby relieving migraine headaches. It has limited effect on arteries supplying blood to the brain and little effect on cardiac and pulmonary vessels.
Indications
Acute headache phase of migraine attacks with or without aura; treatment of migraine in adolescents aged 12-17 years.
Therapeutic class
5-HT Agonist
Pharmacological class
Selective Serotonin Receptor Agonist (5-HT1B/1D)
Pharmacology
Almotriptan is a selective and potent serotonin (5-HT1B/1D) receptor agonist. It binds to specific serotonin receptors on meningeal arteries, inhibiting the release of vasoactive peptides and causing arterial constriction. It has limited effect on arteries supplying blood to the brain and little effect on cardiac and pulmonary vessels.
Mechanism of action
Almotriptan binds to serotonin (5-HT1B/1D) receptors, constricting meningeal arteries and inhibiting the release of vasoactive peptides, thereby relieving migraine headaches.
Dosage
Adults: 6.25-12.5 mg (12.5 mg is more effective) as a single dose at onset of migraine; may repeat after 2 hours if needed; maximum 25 mg/day.
Adolescents (12-17 years): 6.25-12.5 mg as a single dose at onset of migraine; may repeat after 2 hours if needed; maximum 25 mg/day.
Hepatic impairment: Starting dose 6.25 mg; maximum 12.5 mg/24 hours.
Severe renal impairment: Starting dose 6.25 mg; maximum 12.5 mg/24 hours.
Administration
Take as soon as possible at the onset of migraine. May be taken with or without food. Swallow tablet whole; do not crush. Take at a fixed time each day.
Missed dose
If the headache is relieved after the initial dose but returns, the dose may be repeated after 2 hours. Do not exceed 25 mg in 24 hours.
Side effects
Common side effects: Dizziness, dry mouth, flushing (warmth in face, ears, neck, and trunk), jaw pain, nausea, neck pain, sleepiness, throat pain, weakness, paresthesia (tingling or pricking sensation).
Serious (rare): Myocardial infarction, severe allergic reactions, serotonin syndrome (when used with SSRIs or SNRIs).
Precautions & warnings
- Cardiac risk: Ischemic heart disease, coronary artery vasospasm, angina pectoris, silent ischemia, Prinzmetal's angina – contraindicated.
- Hypertension: Uncontrolled hypertension – contraindicated; monitor blood pressure regularly.
- Driving: May cause drowsiness and dizziness; do not drive or operate machinery.
- Mood changes: May cause mood changes or depression; regular monitoring required.
- Pregnancy & breastfeeding: Consult your doctor.
- Sulfonamide allergy: Caution in patients with history.
Contraindications
- Ischemic heart disease or coronary artery vasospasm
- Uncontrolled hypertension
- Severe hepatic or renal impairment
- Prophylaxis of migraine, hemiplegic or basilar migraine
- Cluster headache
- Hypersensitivity to almotriptan or any component
- Previous cerebrovascular accident (CVA) or transient ischemic attack (TIA)
- Peripheral vascular disease
Drug interactions
- Other 5-HT1 agonists: Do not use within 24 hours
- Ergotamine derivatives: Do not use within 24 hours (prolonged vasospastic reactions)
- SSRIs/SNRIs: Risk of life-threatening serotonin syndrome
- MAO inhibitors: Do not use within 2 weeks of discontinuing
Food interactions
Information on alcohol consumption is not available; consult your doctor.
Use in pregnancy
Pregnancy Category: C. Animal studies have shown harmful effects on the fetus; human studies are limited. Use only if clearly needed with medical advice.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
It is not known whether almotriptan is excreted in human milk; use with caution.
Pediatric use
Under 12 years: Safety and efficacy have not been established.
12-17 years: Adult dose applies (approved in the USA).
Geriatric use
No dose adjustment needed for elderly patients, but caution is required due to reduced liver and kidney function.
Renal / hepatic impairment
Renal impairment: Severe renal impairment: starting dose 6.25 mg; maximum 12.5 mg/24 hours.
Hepatic impairment: Hepatic impairment: starting dose 6.25 mg; maximum 12.5 mg/24 hours.
Overdose effects
Overdose symptoms: excessive increase in blood pressure, dizziness, nausea, vomiting. Treatment: symptomatic and supportive measures.
Storage conditions
Store below 30°C in a cool and dry place, protected from light. Do not freeze. Keep out of reach of children.
Chemical structure
C₁₇H₂₅N₃O₂S (Molecular weight: 335.46 g/mol)