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Almotriptan

Medically reviewed by Drugs.com. Last updated on May 26, 2020.

Pronunciation

(al moh TRIP tan)

Index Terms

  • Almotriptan Malate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral, as maleate:

Axert: 6.25 mg [DSC]

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

Generic: 6.25 mg, 12.5 mg

Brand Names: U.S.

  • Axert [DSC]

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 therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

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.

Administration

Administer 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

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. Exceptions: Nefazodone. Consider therapy modification

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

Ergot Derivatives: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the vasoconstricting effect of Ergot Derivatives. Ergot Derivatives may enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists (Triptans). Exceptions: Lisuride; Nicergoline. 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). Exceptions: Rasagiline; Safinamide; Selegiline. 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. 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. Exceptions: Isocarboxazid; Linezolid; Methylene Blue; Moclobemide; Nefazodone; Phenelzine; Tranylcypromine. Monitor therapy

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

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%, 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

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.

Monitoring Parameters

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.

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

What is this drug used for?

• It is used to treat migraine headaches.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Fatigue

• Dry mouth

• Nausea

• Vomiting

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Severe or persistent headache

• Severe dizziness

• Passing out

• Constipation

• Diarrhea

• Severe abdominal pain

• Bloody diarrhea

• Burning or numbness feeling

• Weight loss

• Leg cramps

• Feeling of heaviness or tightness in legs

• Sensation of cold

• Burning or aching pain in feet or toes

• Skin discoloration

• Vision changes

• Blindness

• Abnormal heartbeat

• Serotonin syndrome like dizziness, severe headache, agitation, sensing things that seem real but are not, fast heartbeat, abnormal heartbeat, flushing, tremors, sweating a lot, change in balance, severe nausea, or severe diarrhea

• Heart attack like chest pain; pain in arms, back, neck, jaw, or abdomen; shortness of breath; cold sweats; severe dizziness; passing out; or severe nausea or vomiting

• Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.