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Almotriptan

Pronunciation

(al moh TRIP tan)

Index Terms

  • Almotriptan Malate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral, as maleate:

Axert: 6.25 mg

Axert: 12.5 mg [contains fd&c blue #2 (indigotine)]

Generic: 6.25 mg, 12.5 mg

Brand Names: U.S.

  • Axert

Pharmacologic Category

  • Antimigraine Agent
  • Serotonin 5-HT1B, 1D Receptor Agonist

Pharmacology

Selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in cranial arteries; causes vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine

Absorption

Well absorbed

Distribution

Vd: ~180 to 200 L

Metabolism

Via MAO type A oxidative deamination (~27% of dose) and CYP3A4 and 2D6 (~12% of dose) to inactive metabolites

Excretion

Urine (~75%; ~40% of total dose as unchanged drug); feces (~13% of total dose as unchanged drug and metabolites)

Time to Peak

Plasma: 1 to 3 hours

Half-Life Elimination

Mean: 3 to 5 hours (Baldwin 2004; McEnroe 2005)

Protein Binding

∼35%

Special Populations: Renal Function Impairment

Clearance is decreased approximately 65% in those with CrCl 10 to 30 mL/minute and decreased approximately 40% in those with CrCl 31 to 71 mL/minute. Cmax increased approximately 80%.

Special Populations: Hepatic Function Impairment

The maximum decrease expected in almotriptan clearance due to hepatic function impairment would be 60%.

Special Populations: Elderly

A longer terminal half-life (3.7 vs 3.2 h) and a 25% higher AUC has been observed in elderly patients.

Use: Labeled Indications

Acute treatment of migraine with or without aura in adults (with a history of migraine) and adolescents (with a history of migraine lasting ≥4 hours when left untreated)

Contraindications

Hypersensitivity to almotriptan or any component of the formulation; hemiplegic or basilar migraine; known or suspected ischemic heart disease (eg, angina pectoris, MI, documented silent ischemia, coronary artery vasospasm, Prinzmetal's variant angina); cerebrovascular syndromes (eg, stroke, transient ischemic attacks); peripheral vascular disease (eg, ischemic bowel disease); uncontrolled hypertension; use within 24 hours of another 5-HT1 agonist; use within 24 hours of ergotamine derivatives and/or ergotamine-containing medications (eg, dihydroergotamine, ergotamine)

Dosing: Adult

Migraine: Oral: Initial: 6.25-12.5 mg in a single dose; if the headache returns, repeat the dose after 2 hours; no more than 2 doses (maximum daily dose: 25 mg)

Note: The safety of treating more than 4 migraines/month has not been established.

Dosage adjustment with concomitant use of an enzyme inhibitor:

Patients receiving a potent CYP3A4 inhibitor: Initial: 6.25 mg in a single dose; maximum daily dose: 12.5 mg

Patients with renal impairment and concomitant use of a potent CYP3A4 inhibitor: Avoid use

Patients with hepatic impairment and concomitant use of a potent CYP3A4 inhibitor: Avoid use

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Migraine: Oral: Children ≥12 years: Refer to adult dosing.

Dosing: Renal Impairment

Severe renal impairment (CrCl ≤30 mL/minute): Initial: 6.25 mg in a single dose; maximum daily dose: 12.5 mg

Dosing: Hepatic Impairment

Initial: 6.25 mg in a single dose; maximum daily dose: 12.5 mg

Administration

Administer without regard to meals.

Dietary Considerations

May be taken without regard to meals.

Storage

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

Analgesics (Opioid): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Antiemetics (5HT3 Antagonists): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Antipsychotic Agents: Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Almotriptan. Management: Limit initial almotriptan adult dose to 6.25 mg and maximum adult dose to 12.5 mg/24-hrs when used with a strong CYP3A4 inhibitor. Avoid concurrent use in patients with impaired hepatic or renal function. Consider therapy modification

Dapoxetine: May enhance the adverse/toxic effect of Serotonin Modulators. Avoid combination

Droxidopa: Serotonin 5-HT1D Receptor Agonists may enhance the hypertensive effect of Droxidopa. Monitor therapy

Ergot Derivatives: Serotonin 5-HT1D Receptor Agonists may enhance the vasoconstricting effect of Ergot Derivatives. Ergot Derivatives may enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists. Exceptions: Nicergoline. Avoid combination

MAO Inhibitors: May decrease the metabolism of Serotonin 5-HT1D Receptor Agonists. Management: If MAO inhibitor therapy is required, naratriptan, eletriptan or frovatriptan may be a suitable 5-HT1D agonist to employ. Avoid combination

Metaxalone: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Methylene Blue: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Avoid combination

Metoclopramide: Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome. Monitor therapy

Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Exceptions: Nicergoline; Tedizolid. Monitor therapy

SUMAtriptan: Serotonin 5-HT1D Receptor Agonists may enhance the adverse/toxic effect of SUMAtriptan. Avoid combination

TraMADol: Serotonin Modulators may enhance the adverse/toxic effect of TraMADol. The risk of seizures may be increased. TraMADol may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Adverse Reactions

1% to 10%:

Central nervous system: Drowsiness (≤5%), dizziness (≤4%), headache (≤2%)

Gastrointestinal: Nausea (1% to 3%), vomiting (≤2%), xerostomia (1%)

Neuromuscular & skeletal: Paresthesia (≤1%)

<1% (Limited to important or life-threatening): Anaphylactic shock, anaphylaxis, angina pectoris, angioedema, colitis, coronary artery vasospasm, hemiplegia, hypersensitivity reaction, hypertension, ischemic heart disease, mastalgia, myocardial infarction, neuropathy, seizure, skin rash, syncope, tachycardia, ventricular fibrillation, ventricular tachycardia

Warnings/Precautions

Concerns related to adverse effects:

• Cardiac events: Coronary artery vasospasm, transient ischemia, myocardial infarction, ventricular tachycardia/fibrillation, cardiac arrest, and death have been reported with 5-HT1 agonist administration. Patients who experience sensations of chest pain/pressure/tightness or symptoms suggestive of angina following dosing should be evaluated for coronary artery disease or Prinzmetal's angina before receiving additional doses; if dosing is resumed and similar symptoms recur, monitor with ECG.

• Cerebrovascular events: Cerebral/subarachnoid hemorrhage and stroke have been reported with 5-HT1 agonist administration.

• Elevated blood pressure: Significant elevation in blood pressure, including hypertensive crisis, has been reported on rare occasions following 5-HT1 agonist administration in patients with and without a history of hypertension.

• Headaches: Acute migraine agents (eg, triptans, opioids, ergotamine, or a combination of the agents) used for 10 or more days per month may lead to worsening of headaches (medication overuse headache); withdrawal treatment may be necessary in the setting of overuse.

• Ocular effects: Transient and permanent blindness and partial vision loss have been reported (rare) with 5-HT1 agonist administration.

• Sulfonamide allergy: Almotriptan contains a sulfonyl group which is structurally different from a sulfonamide. Cross-reactivity in patients with sulfonamide allergy has not been evaluated; however, the manufacturer recommends that caution be exercised in this patient population.

• Vasospasm-related events: Peripheral vascular ischemia and colonic ischemia have been reported with 5-HT1 agonist administration.

Disease-related concerns:

• Coronary artery disease: Almotriptan should not be given to patients with documented ischemic or vasospastic CAD. Patients with risk factors for CAD (eg, hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, menopause, male >40 years of age) should undergo adequate cardiac evaluation prior to administration; if the cardiac evaluation is “satisfactory,” first dose should be given in the healthcare provider's office (consider ECG monitoring). All patients should undergo periodic evaluation of cardiovascular status during treatment.

• Hepatic impairment: Use with caution in patients with hepatic impairment. Drug clearance may be reduced leading to increased plasma concentrations; dosage reduction is recommended.

• Renal impairment: Use with caution in patients with moderate-to-severe renal failure. Drug clearance may be reduced leading to increased plasma concentrations; dosage reduction is recommended for severe renal impairment.

Concurrent drug therapy issues:

• Serotonin syndrome: Symptoms of agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, and tachycardia may occur with concomitant proserotonergic drugs (ie, SSRIs/SNRIs or triptans) or agents which reduce almotriptan's metabolism. Concurrent use of serotonin precursors (eg, tryptophan) is not recommended. If concomitant administration with SSRIs is warranted, monitor closely, especially at initiation and with dose increases.

Other warnings/precautions:

• Appropriate use: Only indicated for treatment of acute migraine; it is not indicated for migraine prophylaxis, or for the treatment of cluster headaches, hemiplegic migraine, or basilar migraine. If a patient does not respond to the first dose, the diagnosis of acute migraine should be reconsidered.

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were observed in animal reproduction studies. Information related to almotriptan use in pregnancy is limited (Källén, 2011; Nezvalová-Henriksen, 2010; Nezvalová-Henriksen, 2012). Until additional information is available, other agents are preferred for the initial treatment of migraine in pregnancy (Da Silva, 2012; MacGregor, 2012; Williams, 2012).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience fatigue, dizziness, or dry mouth. Have patient report immediately to prescriber severe headache, constipation, diarrhea, severe nausea, severe vomiting, severe abdominal pain, bloody diarrhea, burning or numbness feeling, weight loss, leg cramps, leg pain, sensation of cold, burning or aching pain in feet or toes, shortness of breath, vision changes, blindness, abnormal heartbeat, signs of serotonin syndrome (dizziness, severe headache, agitation, hallucinations, tachycardia, abnormal heartbeat, flushing, tremors, sweating a lot, change in balance, severe nausea, or severe diarrhea), signs of a heart attack (angina; pain in arms, back, neck, jaw, or abdomen; shortness of breath; cold sweats; severe dizziness; passing out; or severe nausea or vomiting), or signs of severe cerebrovascular disease (change in strength on one side is greater than the other, difficulty speaking or thinking, change in balance, or vision changes) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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