Migraine, moderate to severe, acute treatment:
Note: Do not use within 24 hours of an ergotamine preparation or a different triptan. Limit use to <10 days per month to avoid medication-overuse headache. Administration early in the course of a migraine attack, at the first sign of pain, may improve response to treatment. When attack is complicated by severe nausea or vomiting, a non-oral medication may be more effective (AHS [Ailani 2021]).
Oral: 12.5 mg as a single dose; if symptoms persist or return, may repeat dose after ≥2 hours. Maximum: 12.5 mg/dose; 25 mg per 24 hours (Bartolini 2011; Pascual 2000; manufacturer's labeling).
Dosage adjustment with concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl >30 mL/minute: No dosage adjustment necessary.
CrCl ≤30 mL/minute: 6.25 mg as a single dose; if symptoms persist or return, may repeat dose after ≥2 hours. Maximum: 12.5 mg per 24 hours.
6.25 mg as a single dose; if symptoms persist or return, may repeat dose after ≥2 hours. Maximum: 12.5 mg per 24 hours.
(For additional information see "Almotriptan: Pediatric drug information")
Migraine: Children ≥12 years and Adolescents: Oral: Initial: 6.25 to 12.5 mg in a single dose; if headache returns, may repeat the dose after 2 hours; maximum 2 doses/day; maximum daily dose: 25 mg/day. Note: The safety of treating >4 migraines/month has not been established.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Children ≥12 years and Adolescents: Severe renal impairment (CrCl ≤30 mL/minute): Initial: 6.25 mg in a single dose; maximum daily dose: 12.5 mg/day
Children ≥12 years and Adolescents: Initial: 6.25 mg in a single dose; maximum daily dose: 12.5 mg/day
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral, as maleate:
Generic: 6.25 mg, 12.5 mg
Yes
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral, as maleate:
Generic: 6.25 mg, 12.5 mg
Administer without regard to meals.
Oral: May administer without regard to meals.
Migraine, moderate to severe, acute treatment: 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).
Axert may be confused with Antivert
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
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%, postmarketing, and/or case reports: Abdominal cramps, abdominal discomfort, abdominal pain, abnormal dreams, altered sense of smell, anaphylactic shock, anaphylaxis, angina pectoris, angioedema, anxiety, arthralgia, arthritis, ataxia, back pain, blepharospasm, blurred vision, bronchitis, central nervous system stimulation, chest pain, chills, cold extremities, colitis, confusion, conjunctivitis, coronary artery vasospasm, decreased visual acuity, depression, dermatitis, diaphoresis, diarrhea, diplopia, dry eye syndrome, dysgeusia, dysmenorrhea, dyspepsia, dyspnea, epistaxis, erythema, euphoria, eye irritation, eye pain, fatigue, fever, gastritis, gastroenteritis, gastroesophageal reflux disease, hemiplegia, hyperacusis, hypercholesterolemia, hyperglycemia, hyperhidrosis, hyperreflexia, hypersensitivity reaction, hypertension, hypertonia, hyperventilation, hypoesthesia, increased creatine phosphokinase, increased gamma-glutamyl transferase, increased thirst, insomnia, ischemic heart disease, lack of concentration, laryngismus, laryngitis, limb pain, malaise, mastalgia, myalgia, myasthenia, myocardial infarction, myopathy, neck pain, neck stiffness, nervousness, neuropathy, nightmares, nystagmus, otalgia, otitis media, palpitations, pharyngitis, pruritus, restlessness, rhinitis, scotoma, seizure, shakiness, sialorrhea, sinusitis, skin photosensitivity, skin rash, sneezing, syncope, tachycardia, tinnitus, tremor, vasodilation, ventricular fibrillation, ventricular tachycardia, vertigo, weakness
Hypersensitivity to almotriptan or any component of the formulation; hemiplegic migraine or migraine with brainstem aura; known or suspected ischemic heart disease (eg, angina pectoris, MI, documented silent ischemia, coronary artery vasospasm, Prinzmetal's variant angina) or other significant underlying cardiovascular disease; cerebrovascular syndromes (eg, stroke, transient ischemic attacks); peripheral vascular disease (including 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).
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 migraine with brainstem aura. If a patient does not respond to the first dose, the diagnosis of acute migraine should be reconsidered.
Substrate of CYP2D6 (minor), CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Bromocriptine: May enhance the adverse/toxic effect of Serotonin 5-HT1D Receptor Agonists (Triptans). Management: Consider alternatives to this combination when possible. If combined, monitor for increased bromocriptine and triptan toxicities. Risk D: Consider therapy modification
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Almotriptan. Management: Limit initial almotriptan dose to 6.25 mg and maximum dose to 12.5 mg in any 24-period when used with a strong CYP3A4 inhibitor. Avoid concurrent use in patients with impaired hepatic or renal function. Risk D: Consider therapy modification
Droxidopa: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the hypertensive effect of Droxidopa. Risk C: Monitor therapy
Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the vasoconstricting effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Monoamine Oxidase Inhibitors: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. Monoamine Oxidase Inhibitors may increase the serum concentration of Serotonin 5-HT1D Receptor Agonists (Triptans). Risk X: Avoid combination
Nefazodone: Almotriptan may enhance the serotonergic effect of Nefazodone. This could result in serotonin syndrome. Nefazodone may increase the serum concentration of Almotriptan. Management: Limit the initial almotriptan dose to 6.25 mg when combined with nefazodone, and do not exceed 12.5 mg in any 24-hour period. Avoid concomitant use in patients with impaired hepatic or renal function. Monitor for serotonin syndrome. Risk D: Consider therapy modification
Serotonergic Agents (High Risk): Almotriptan may enhance the serotonergic effect of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
SUMAtriptan: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the adverse/toxic effect of SUMAtriptan. Risk X: Avoid combination
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).
It is not known if almotriptan is excreted in breast milk. The manufacturer recommends that caution be exercised when administering almotriptan to nursing women.
Headache severity, BP, signs/symptoms suggestive of angina; perform a cardiovascular evaluation in triptan-naive patients who have multiple cardiovascular risk factors (eg, increased age, diabetes, hypertension, smoking, obesity, strong family history of coronary artery disease), monitor ECG with first dose in patients with multiple cardiovascular risk factors who have a negative cardiovascular evaluation, and consider periodic cardiovascular evaluation in such patients if they are intermittent long-term users.
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
Note: Reported values are similar between adolescent and adult patients (Baldwin 2004).
Absorption: Well absorbed
Distribution: Vd: ~180 to 200 L
Protein binding: ~35%
Metabolism: Via MAO type A oxidative deamination (~27% of dose) and CYP3A4 and 2D6 (~12% of dose) to inactive metabolites
Bioavailability: ~70%
Half-life elimination: Mean: 3 to 5 hours (Baldwin 2004; McEnroe 2005)
Time to peak, plasma: 1 to 3 hours
Excretion: Urine (~75%; ~40% of total dose as unchanged drug); feces (~13% of total dose as unchanged drug and metabolites)
Altered kidney function: 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%.
Hepatic function impairment: The maximum decrease expected in almotriptan clearance due to hepatic function impairment would be 60%.
Older adult: A longer terminal half-life (3.7 vs 3.2 h) and a 25% higher AUC has been observed in elderly patients.
Tablets (Almotriptan Malate Oral)
6.25 mg (per each): $41.91 - $41.97
12.5 mg (per each): $41.92 - $41.97
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