Altrip

Approved Indications:

• Acute Treatment of Migraine With or Without Aura in Adults and Adolescents (≥12 years):
  Almotriptan is indicated for the acute management of migraine attacks with or without aura. It is most effective when taken at the earliest onset of headache symptoms.

Clinically Accepted Off-label Use:

• Menstrual Migraine:
  Almotriptan may be used as acute symptomatic relief for menstrual-related migraines under clinical supervision.

Note: Almotriptan is not indicated for prophylactic (preventive) treatment of migraine or for use in hemiplegic, basilar, or ophthalmoplegic migraine types.

Adults (18–65 years):

• Initial dose: 6.25 mg or 12.5 mg orally at the first sign of migraine.
• Repeat dose (if needed): A second dose may be taken after at least 2 hours if the migraine recurs.
• Maximum daily dose: 25 mg in 24 hours.

Adolescents (12–17 years):

• Starting dose: 6.25 mg orally.
• Max daily dose: 25 mg (as two doses of 12.5 mg or one 12.5 mg and one 6.25 mg).

Pediatrics (<12 years):

• Not recommended due to lack of established safety and efficacy.

Elderly (>65 years):

• Use with caution due to increased risk of cardiovascular events; start at lowest effective dose.

Renal Impairment:

• Mild to moderate: No adjustment needed.
• Severe (CrCl <30 mL/min): Maximum single dose 6.25 mg; do not repeat within 24 hours.

Hepatic Impairment:

• Mild to moderate: Start with 6.25 mg cautiously.
• Severe: Contraindicated.

Route of Administration:

• Oral (tablets), with or without food.

Treatment Duration:

• For acute attacks only; not for daily or preventive use.

Almotriptan is a selective serotonin (5-HT1B/1D) receptor agonist. It works by binding to 5-HT1B receptors on cranial blood vessels, causing vasoconstriction, and to 5-HT1D receptors on nerve terminals of the trigeminal system, inhibiting the release of pro-inflammatory neuropeptides such as CGRP and substance P. These effects reduce inflammation, vascular dilation, and pain transmission, leading to relief from migraine headache and associated symptoms.

• Absorption: Rapid and complete oral absorption.
• Bioavailability: ~70%.
• Tmax (peak concentration): 1.5 to 4 hours post-dose.
• Distribution:
• Volume of distribution: ~180 L.
• Plasma protein binding: 35–40%.
• Metabolism:
• Primarily metabolized by MAO-A, with contributions from CYP3A4 and CYP2D6.
• Forms inactive metabolites.
• Elimination:
• Half-life: ~3 to 4 hours.
• Excretion: ~75% via urine (as unchanged drug and metabolites), 13% via feces.

Pregnancy:

• FDA Category (prior system): Not assigned.
• Human data are insufficient; animal studies show no teratogenicity but did observe fetal effects at high doses.
• Use only if the potential benefit outweighs the potential risk.

Lactation:

• Almotriptan is excreted in small amounts into breast milk.
• It is advised to avoid breastfeeding for at least 12 hours after taking a dose to minimize infant exposure.

Caution:

• Use in pregnant or breastfeeding women only when clearly necessary.

• Primary Class: Antimigraine Agent
• Subclass: Selective Serotonin Receptor Agonist (Triptan class)
• Generation: Second-generation triptan

• Hypersensitivity to almotriptan or any tablet excipients
• History of coronary artery disease (CAD), angina, myocardial infarction, or coronary vasospasm
• History of stroke, transient ischemic attack (TIA), or other cerebrovascular conditions
• Peripheral vascular disease
• Uncontrolled hypertension
• Severe hepatic impairment
• Concurrent use of other triptans or ergotamines within 24 hours
• Use within 2 weeks of monoamine oxidase-A (MAO-A) inhibitor therapy

• Cardiovascular Risk:
  Serious adverse events such as myocardial infarction and arrhythmias have occurred. Not recommended in patients with cardiovascular risk factors without prior cardiac evaluation.
• Cerebrovascular Risk:
  May cause stroke or TIA in susceptible individuals.
• Serotonin Syndrome:
  Risk increases with SSRIs, SNRIs, MAOIs, or other serotonergic drugs. Monitor for symptoms like agitation, hyperreflexia, and confusion.
• Medication Overuse Headache (MOH):
  Frequent use may lead to worsening headache frequency. Use only as needed and avoid exceeding recommended dose limits.
• Renal or Hepatic Impairment:
  Adjust dose or avoid in severe impairment.
• Hypersensitivity Reactions:
  Rare cases of anaphylaxis and angioedema have been reported.

Common Side Effects:

• Nervous System: Dizziness, drowsiness, headache recurrence, paresthesia
• Gastrointestinal: Nausea, dry mouth
• General: Fatigue, feelings of heaviness or tightness (chest, throat)

Less Common or Serious Side Effects:

• Cardiovascular: Palpitations, mild transient hypertension, chest pain
• Psychiatric: Anxiety, restlessness
• Dermatologic: Rash, pruritus

Rare but Serious Side Effects:

• Myocardial infarction, stroke, serotonin syndrome, hypersensitivity reactions (including anaphylaxis)

Onset & Severity:

• Most side effects are mild-to-moderate and occur within 4 hours of dosing; serious effects are rare but may be life-threatening.

Drug–Drug Interactions:

• Other Triptans or Ergot Derivatives: Contraindicated within 24 hours due to additive vasoconstrictive effects.
• MAO-A Inhibitors: Contraindicated; increases risk of serious side effects.
• SSRIs/SNRIs/TCAs: Risk of serotonin syndrome; monitor for CNS symptoms.
• CYP3A4 Inhibitors (e.g., ketoconazole, erythromycin): May increase almotriptan plasma levels—use cautiously.
• Beta-blockers & CNS depressants: May enhance sedative effects.

Drug–Alcohol Interaction:

• Alcohol may enhance CNS depression (e.g., drowsiness, dizziness); avoid concurrent use.

Enzyme Involvement:

• MAO-A, CYP3A4, CYP2D6

• Updated Use in Adolescents:
  Almotriptan is now accepted for use in patients aged ≥12 years in several regulatory regions, based on tolerability and efficacy data.
• Label Revisions:
  Current labeling emphasizes cardiovascular risk screening and serotonin syndrome monitoring.
• Migraine Management Guidelines (AHS & NICE):
  Almotriptan remains one of the recommended agents for acute migraine management, particularly for its favorable side effect profile among triptans.

• Temperature: Store at 15°C to 25°C (59°F to 77°F)
• Humidity: Store in a dry place
• Light Protection: Keep in original blister pack to protect from light
• Handling:
• Do not refrigerate or freeze
• Keep out of reach of children
• Do not use expired or physically damaged tablets