Almotriptan

— THERAPEUTIC CATEGORIES —
  • Migraine and headache
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Almotriptan Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Almotriptan (as malate) 6.25mg, 12.5mg; tabs.

    Pharmacological Class

    Selective 5-HT1B/1D receptor agonist.

    How Supplied

    Contact supplier

    Manufacturer

    Various generic manufacturers

    Almotriptan Indications

    Indications

    Acute treatment of migraine attacks in adults. Acute treatment of migraine headache pain in adolescents age 12–17yrs with a history of migraine attacks lasting ≥4hrs (when untreated).

    Limitations of Use

    Confirm diagnosis. Not established for adolescents with migraine-associated symptoms or in older males for cluster headaches. Do not use for migraine prophylaxis.

    Almotriptan Dosage and Administration

    Adult

    6.25–12.5mg single dose; may repeat once after 2hrs; max 25mg/24hrs. Hepatic or severe renal impairment (CrCl 10–30mL/min) or concomitant potent CYP3A4 inhibitors (eg, ketoconazole): initially 6.25mg once; max 12.5mg/24hrs. The safety of treating an average of more than 4 migraines over 30 days is not established.

    Children

    Not established.

    Renal Impairment

    The recommended starting dose of almotriptan maleate in patients with severe renal impairment is 6.25mg. Maximum daily dose should not exceed 12.5mg per 24-hour period.

    Hepatic Impairment

    The recommended starting dose of almotriptan maleate in patients with hepatic impairment is 6.25mg. Maximum daily dose should not exceed 12.5mg per 24-hour period.

    Almotriptan Contraindications

    Contraindications

    Ischemic heart disease (eg, angina pectoris, silent ischemia, history of MI). Coronary artery vasospasm (eg, Prinzmetal's variant angina). Other significant cardiovascular disease. Uncontrolled hypertension. Cerebrovascular events (eg, stroke, TIA). Peripheral vascular disease (eg, ischemic bowel disease). Basilar or hemiplegic migraine. Within 24hrs of other 5-HT1 agonists or ergot-type drugs.

    Almotriptan Boxed Warnings

    Not Applicable

    Almotriptan Warnings/Precautions

    Warnings/Precautions

    Reevaluate if angina or ischemia symptoms (eg, ischemic bowel syndrome, Raynaud's syndrome) occur, or if no response after 1st dose. Exclude underlying cardiovascular disease, supervise 1st dose, and consider monitoring ECG in patients with likelihood of unrecognized coronary artery disease (eg, postmenopausal women, men over age 40, hypertension, hypercholesterolemia, obesity, diabetes, smokers, strong family history). Monitor cardiovascular function in long-term intermittent use. Cerebrovascular events (eg, stroke, hemorrhage, TIA), peripheral vascular or colonic ischemia following other 5-HT1 agonists. May exacerbate headache with overuse. Hepatic or renal dysfunction. Sulfonamide hypersensitivity. Elderly. Labor & delivery. Pregnancy (Cat.C). Nursing mothers.

    Warnings/Precautions

    Risk of Myocardial Ischemia and Infarction and Other Adverse Cardiac Events

    • Almotriptan maleate may cause serious adverse cardiac events, including myocardial infarction, and life-threatening disturbances of cardiac rhythm and death. The incidence of these events is extremely low.

    • Almotriptan maleate may cause coronary vasospasm. Evaluate for presence of coronary artery disease (CAD) or a predisposition to Prinzmetal’s variant angina in patients who experience signs or symptoms suggestive of angina following dosing before administering additional doses. Monitor electrocardiographically if dosing is resumed and similar symptoms recur.

    • Do not administer almotriptan maleate to patients with documented ischemic or vasospastic CAD (see Contraindications).

    • Strongly recommended that almotriptan maleate not be given to patients with risk factors for CAD (eg, hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, or male >40 years of age) unless a cardiovascular evaluation shows that the patient is reasonably free of CAD and ischemic myocardial disease or other underlying cardiovascular disease.

    • For patients with risk factors for CAD who have a satisfactory cardiovascular evaluation, it is strongly recommended to administer the first dose of almotriptan maleate in a medically supervised setting and performing an electrocardiogram (ECG) immediately following almotriptan maleate administration. 

    • Consider periodic cardiovascular evaluation in intermittent long-term users of almotriptan maleate and who have or acquire risk factors predictive of CAD. 

    Sensations of Pain, Tightness, Pressure in the Chest and/or Throat, Neck, and Jaw

    • Sensations of tightness, pain, and pressure in the chest, throat, neck, and jaw commonly occur after treatment with almotriptan maleate. 

    • Evaluate for the presence of CAD or a predisposition to Prinzmetal’s variant angina in patients who experience signs or symptoms suggestive of angina following dosing before receiving additional doses. Monitor electrocardiographically if dosing is resumed and similar symptoms recur.

    • 5-HT1 agonists, including almotriptan maleate, are contraindicated in patients with CAD and those with Prinzmetal’s variant angina. 

    Cerebrovascular Events and Fatalities

    • Cerebral hemorrhage, subarachnoid hemorrhage, stroke, and other cerebrovascular events have occurred in patients treated with 5-HT1 agonists, and some have resulted in fatalities. 

    • Patients with migraine may be at increased risk of certain cerebrovascular events (eg, stroke, hemorrhage, TIA). 

    • Before treating headaches in patients not previously diagnosed as migraineurs, and in migraineurs who present with symptoms atypical for migraine, exclude other potentially serious neurological conditions. Almotriptan maleate is contraindicated in patients with a history of stroke or TIA. 

    Other Vasospasm-Related Events, Including Peripheral Vascular Ischemia and Colonic Ischemia

    • Almotriptan maleate may cause non-coronary vasospastic reactions, such as peripheral vascular ischemia, gastrointestinal vascular ischemia and infarction (presenting with abdominal pain and bloody diarrhea), splenic infarction, and Raynaud’s syndrome.

    • Reports of transient and permanent blindness and significant partial vision loss have been reported with the use of 5-HT1 agonists. Visual disorders may be part of a migraine attack.

    Serotonin Syndrome 

    • Serotonin syndrome may occur with almotriptan maleate, particularly during coadministration with selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs). Serotonin syndrome symptoms may include mental status changes, autonomic instability, neuromuscular aberrations, and/or gastrointestinal symptoms. 

    Medication Overuse Headache 

    • Overuse of acute migraine drugs (eg, ergotamine, triptans, opioids, or combination of these drugs for 10 or more days per month) may lead to exacerbation of headache (medication overuse headache). 

    • Medication overuse headache may present as migraine-like daily headaches or as a marked increase in frequency of migraine attacks. 

    • Detoxification of patients, including withdrawal of the overused drugs, and treatment of withdrawal symptoms (which often includes a transient worsening of headache) may be necessary.

    Increase in Blood Pressure 

    • Significant elevation in blood pressure has been reported on rare occasions with almotriptan maleate use, including patients with and without a history of hypertension. 

    • Monitor blood pressure in patients treated with almotriptan maleate. 

    • Almotriptan maleate is contraindicated in patients with uncontrolled hypertension. 

    Hypersensitivity to Sulfonamides

    • Use caution in patients with known hypersensitivity to sulfonamides.

    Impaired Hepatic or Renal Function

    • Use caution in patients with diseases that may alter the absorption, metabolism, or excretion of drugs, such as those with impaired hepatic or renal function.

    Binding to Melanin-Containing Tissues

    • Almotriptan maleate could accumulate in melanin-rich tissues over time that may cause toxicity in these tissues with extended use. There was no systematic monitoring of ophthalmologic function in clinical trials.

    • Prescribers should be aware of the possibility of long-term ophthalmologic effects.

    Pregnancy Considerations

    Pregnancy Category C

    • Only use almotriptan maleate if the potential benefit justifies the potential risk to the fetus.

    Labor and Delivery

    • The effect of almotriptan maleate on labor and delivery is unknown.

    Nursing Mother Considerations

    • It is not known whether almotriptan maleate is excreted in human milk. Exercise caution when administered to a nursing women.

    Pediatric Considerations

    • Safety and efficacy of almotriptan maleate in pediatric patients under the age of 12 years have not been established. 

    Geriatric Considerations

    • Clinical trials of almotriptan maleate did not include sufficient numbers of patients aged 65 and older to determine whether they respond differently from younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. 
    • In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy. 

     

    Renal Impairment Considerations

    The recommended starting dose of almotriptan maleate in patients with severe renal impairment is 6.25mg. Maximum daily dose should not exceed 12.5mg per 24-hour period.

    Hepatic Impairment Considerations

    The recommended starting dose of almotriptan maleate in patients with hepatic impairment is 6.25mg. Maximum daily dose should not exceed 12.5mg per 24-hour period.

    Almotriptan Pharmacokinetics

    Absorption

    The absolute bioavailability of almotriptan is about 70%, with peak plasma levels occurring 1 to 3 hours after administration; food does not affect pharmacokinetics.

    Distribution

    Almotriptan is minimally protein bound (approximately 35%) and the mean apparent volume of distribution is approximately 180 to 200 liters.

    Metabolism

    Almotriptan is metabolized by two major and one minor pathways. Monoamine oxidase (MAO)-mediated oxidative deamination (approximately 27% of the dose), and cytochrome P450-mediated oxidation (approximately 12% of the dose) are the major routes of metabolism, while flavin monooxygenase is the minor route. 

    Elimination

    Almotriptan has a mean half-life of 3 to 4 hours. Almotriptan is eliminated primarily by renal excretion (about 75% of the oral dose), with approximately 40% of an administered dose excreted unchanged in urine. Renal clearance exceeds the glomerular filtration rate by approximately 3-fold, indicating an active mechanism. Approximately 13% of the administered dose is excreted via feces, both unchanged and metabolized.

    Almotriptan Interactions

    Interactions

    Methysergide, other ergotamines, or other 5-HT1 agonists: see Contraindications. Monitor for serotonin syndrome with SSRIs (eg, fluoxetine, fluvoxamine, paroxetine, sertraline, citalopram, escitalopram), SNRIs (eg, venlafaxine, duloxetine). Potentiated by ketoconazole, other potent CYP3A4 inhibitors (avoid if concomitant hepatic or renal impairment).

    Almotriptan Adverse Reactions

    Adverse Reactions

    Nausea, dry mouth, paresthesia, somnolence, dizziness, headache, vomiting, throat/neck/chest pain, pressure or tightness; rare: serious cardiac events, vision loss.

    Almotriptan Clinical Trials

    Clinical Trials

    Adults

    • The efficacy of almotriptan maleate was established in 3 multicenter, randomized, double-blind, placebo-controlled European trials (Study 1, 2, and 3). Patients were randomly assigned to receive either almotriptan 6.25mg, 12.5mg, or placebo to treat moderate to severe migraine headache.

    • Headache pain was evaluated 2 hours after taking one dose of study medication; if the pain had not decreased in severity to mild or no pain, the patient was allowed to take a rescue medication. If the pain had decreased to mild or no pain at 2 hours but subsequently increased in severity between 2 and 24 hours, it was considered a relapse and the patient was instructed to take a second dose of study medication. 

    • In Study 1, 55.4% (P =.002) and 58.5% (P <.001) of patients treated with almotriptan 6.25mg and 12.5mg, respectively, achieved response rates 2 hours following treatment of initial headache vs 33.8% of those treated with placebo. 

    • In Study 2, 57.1% of patients treated with almotriptan 12.5mg achieved response rates 2 hours following treatment of initial headache vs 40% of those treated with placebo (P =.008).

    • In Study 3, 55.6% (P <.001) and 64.9% (P <.001) of patients treated with almotriptan 6.25mg and 12.5mg achieved response rates 2 hours following treatment of initial headache vs 33% of those treated placebo.

    • In all studies, patients with migraine-associated photophobia, phonophobia, nausea, and vomiting at baseline experienced a decreased incidence of these symptoms after receiving almotriptan maleate compared with placebo.

    • Additionally, the estimated probability of patients taking escape medication or a second dose of study medication 2 to 24 hours after the initial dose was lower in the almotriptan arm vs the placebo arm.

    Adolescents Age 12 to 17 Years

    • The efficacy of almotriptan maleate in adolescent patients aged 12 to 17 years was established in a randomized, double-blind, placebo-controlled study. Patients had at least a 1-year history of migraine attacks with or without aura usually lasting 4 hours or more (when untreated). Patients were randomly assigned to receive either almotriptan 6.25mg, 12.5mg, or placebo to treat moderate to severe migraine headache.

    • Headache pain was evaluated 2 hours after taking one dose of study medication; if the pain had not decreased in severity to mild or no pain, the patient was allowed to take a rescue medication. If the pain had decreased to mild or no pain at 2 hours but subsequently increased in severity between 2 and 24 hours, it was considered a relapse and the patient was instructed to take a second dose of study medication. 

    • Results showed that 71.8% (P =.001) and 72.9% (P <.001) of patients treated with almotriptan 6.25mg and 12.5mg, respectively, achieved response rates 2 hours following treatment of initial headache compared with 55.3% of those treated with placebo.

    • The prevalence of the migraine-associated symptoms (nausea, photophobia, and phonophobia) at 2 hours after taking the dose was not significantly different between patients who received almotriptan 6.25mg or 12.5mg and those who received placebo.

    Almotriptan Note

    Notes

    Formerly known under the brand name Axert.

    Almotriptan Patient Counseling

    Patient Counseling

    Risk of Myocardial Ischemia and/or Infarction, Other Adverse Cardiac Events, Other Vasospasm-Related Events, and Cerebrovascular Events 

    • Inform patients that almotriptan maleate may cause serious cardiovascular side effects such as myocardial infarction or stroke. 

    • Be alert for the signs and symptoms of chest pain, shortness of breath, irregular heartbeat, significant rise in blood pressure, weakness, and slurring of speech and should ask for medical advice if any indicative signs or symptoms are observed. Apprise patients of the importance of this follow-up.

    Serotonin Syndrome 

    • Caution patients about the risk of serotonin syndrome with the use of almotriptan maleate or other triptans, particularly during combined use with SSRIs or SNRIs.

    Medication Overuse Headache 

    • Inform patients that use of acute migraine drugs for 10 or more days per month may lead to an exacerbation of headache and encourage patients to record headache frequency and drug use (eg, by keeping a headache diary).

    Pregnancy 

    • Advise patients to notify their healthcare provider if they become pregnant during treatment or intend to become pregnant.

    Nursing Mothers

    • Advise patients to notify their healthcare provider if they are breastfeeding or plan to breastfeed.

    Ability to Operate Machinery or Vehicles

    • Treatment with almotriptan maleate may cause somnolence and dizziness; advise patients not to drive, operate complex machinery, or engage in other hazardous activities until they have gained sufficient experience with almotriptan maleate. 

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