Almotriptan

Pronunciation

(al moh TRIP tan)

U.S. Brand Names

Axert™

Synonyms

Almotriptan Malate

Generic Available

Canadian Brand Names

Axert™

Use

Acute treatment of migraine with or without aura

Pregnancy Risk Factor

Pregnancy Implications

There are no adequate and well-controlled studies in pregnant women. Use in pregnancy should be limited to situations where benefit outweighs risk to fetus. In some (but not all) animal studies, administration was associated with embryolethality, fetal malformations and decreased pup weight.

Lactation

Excretion in breast milk unknown/use caution

Contraindications

Hypersensitivity to almotriptan or any component of the formulation; use as prophylactic therapy for migraine; hemiplegic or basilar migraine; cluster headache; known or suspected ischemic heart disease (angina pectoris, MI, documented silent ischemia, coronary artery vasospasm, Prinzmetal's variant angina); peripheral vascular syndromes (including ischemic bowel disease); uncontrolled hypertension; use within 24 hours of another 5-HT1 agonist; use within 24 hours of ergotamine derivative; concurrent administration or within 2 weeks of discontinuing an MAO inhibitor (specifically MAO type A inhibitors)

Warnings/Precautions

Almotriptan is indicated only in patients

18 years of age with a clear diagnosis of migraine headache. If a patient does not respond to the first dose, the diagnosis of migraine should be reconsidered. Do not give to patients with risk factors for CAD until a cardiovascular evaluation has been performed; if evaluation is satisfactory, the healthcare provider should administer the first dose and cardiovascular status should be periodically evaluated. Cardiac events (coronary artery vasospasm, transient ischemia, myocardial infarction, ventricular tachycardia/fibrillation, cardiac arrest, and death), cerebral/subarachnoid hemorrhage, stroke, peripheral vascular ischemia and colonic ischemia have been reported with 5-HT1 agonist administration. Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension. Use with caution in liver or renal dysfunction. Safety and efficacy in pediatric patients have not been established.

Adverse Reactions

1% to 10%:

Central nervous system: Headache (>1%), dizziness (>1%), somnolence (>1%)

Gastrointestinal: Nausea (1% to 2%), xerostomia (1%)

Neuromuscular & skeletal: Paresthesia (1%)

<1%: Abdominal cramps, abdominal pain, abnormal coordination, anxiety, arthralgia, arthritis, back pain, bronchitis, chest pain, chills, colitis, conjunctivitis, coronary artery vasospasm, creatine phosphokinase increased, depressive symptoms, dermatitis, diaphoresis, diarrhea, diplopia, dream changes, dry eyes, dysmenorrhea, dyspepsia, dyspnea, ear pain, epistaxis, erythema, esophageal reflux, euphoria, eye irritation, eye pain, fatigue, fever, gastritis, gastroenteritis, GGTP increased, hyperacusis, hypercholesterolemia, hypesthesia, hyperglycemia, hyper-reflexia, hypertension, hypertonia, hyperventilation, impaired concentration, insomnia, laryngismus, laryngitis, muscular weakness, myalgia, myocardial ischemia, MI, myopathy, neck pain, nervousness, neuropathy, nightmares, nystagmus, otitis media, palpitation, parosmia, pharyngitis, photosensitivity reaction, pruritus, rash, restlessness, rhinitis, rigid neck, salivation increased, scotoma, shakiness, sinusitis, sneezing, stimulation, syncope, tachycardia, taste alterations, thirst, tinnitus, tremor, vasodilation, ventricular fibrillation, ventricular tachycardia, vertigo, vomiting, weakness

Overdosage/Toxicology

Hypertension or more serious cardiovascular symptoms may occur. Clinical and electrocardiographic monitoring needed for at least 20 hours even if patient asymptomatic. Treatment is symptom-directed and supportive.

Drug Interactions

Substrate (minor) of CYP2D6, 3A4

Ergot-containing drugs: Prolong vasospastic reactions; do not use almotriptan or ergot-containing drugs within 24 hours of each other.

Ketoconazole: Increases almotriptan serum concentration. Monitor for increased almotriptan response.

MAO inhibitors (moclobemide [MAO type A inhibitor]): Almotriptan clearance decreased by 27%; Cmax increased by 6%. Avoid concurrent administration of MAO inhibitors or within 2 weeks of discontinuing an MAO inhibitor, specifically MAO type A inhibitors.

Selegiline: Selegiline is a selective MAO type B inhibitor; while not specifically contraindicated, combination has not been studied.

Verapamil: Increased almotriptan serum concentration by 24%. Dose adjustment not necessary.

SSRIs: Concurrent use may lead to symptoms of hyper-reflexia, weakness, and lack of coordination; monitor.

Stability

Store at 15°C to 30°C (59°F to 86°F).

Mechanism of Action

Selective agonist for serotonin (5-HT1B, 5-HT1D, 5-HT1F receptors) in cranial arteries; causes vasoconstriction and reduce sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine

Pharmacodynamics/Kinetics

Absorption: Well absorbed

Distribution: Vd: 180-200 L

Protein binding: ~35%

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

Bioavailability: 70%

Half-life elimination: 3-4 hours

Time to peak: 1-3 hours

Excretion: Urine (40% as unchanged drug); feces (13% unchanged and metabolized)

Dosage

Oral: Adults: Migraine: 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 in 24-hour period

Note: If the first dose is ineffective, diagnosis needs to be re-evaluated. Safety of treating more than 4 migraines/month has not been established.

Dosage adjustment in renal impairment: Initial: 6.25 mg in a single dose; maximum daily dose: 12.5 mg

Dosage adjustment in hepatic impairment: Initial: 6.25 mg in a single dose; maximum daily dose: 12.5 mg

Dietary Considerations

May be taken without regard to meals

Patient Education

Inform prescriber of all prescriptions (including oral contraceptives), OTC medications, or herbal products you are taking, and any allergies you have. This drug is to be used to reduce your migraine, not to prevent or reduce the number of attacks. Follow exact instructions for use. Do not use more than two doses in 24 hours and do not take within 24 hours of any other migraine medication without consulting prescriber. May cause dizziness, fatigue, or drowsiness (use caution when driving or engaging in tasks requiring alertness until response to drug is known). Report immediately any chest pain, palpitations, or throbbing; feelings of tightness or pressure in jaw or throat; acute headache or dizziness; muscle cramping, pain, or tremors; skin rash; hallucinations, anxiety, panic; or other adverse reactions. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Anesthesia and Critical Care Concerns/Other Considerations

Almotriptan should not be used in patients with a history of vasospastic disease, Prinzmetal's angina, or any critical vascular disease.

Cardiovascular Considerations

Coronary vasospasm has been associated with 5-HT1B/1D agonists. These agents are contraindicated in patients with documented ischemic of vasospastic coronary artery disease. Patients with risk factors for CAD may receive these agents, provided a cardiovascular evaluation yields satisfactory evidence that the patient is free of cardiovascular disease. In patients with risk factors for CAD, administration of the initial dose in a medically staffed/equipped facility (ie, physician's office) is recommended. In addition, ECG monitoring after the initial dose should be considered. Patients who acquire risk factors for CAD, or long-term users of agents from this class of medications, should undergo periodic cardiovascular evaluation.

Dental Health: Effects on Dental Treatment

Key adverse effect(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Dosage Forms

Tablet, as malate: 6.25 mg, 12.5 mg

International Brand Names

Almogran® (AT, BE, DE, DK, ES, FI, FR, GB, IE, IS, IT, NO, PR, SE); Almotrex® (IT); Axert™ (CA)

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