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Almotriptan (Monograph)

Brand name: Axert
Drug class: Selective Serotonin Agonists
- Antimigraine Agents
- Selective Vascular Serotonin Type 1-Like Receptor Agonists
- 5-HT1 Agonists
VA class: CN105
Chemical name: Hydroxybutanedioate-1-[[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine
Molecular formula: C17H25N3O2S•C4H6O5
CAS number: 181183-52-8

Medically reviewed by Drugs.com on Jul 26, 2023. Written by ASHP.

Introduction

Selective serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptor agonist (“triptan”).

Uses for Almotriptan

Vascular Headaches

Acute treatment of migraine attacks with or without aura in adults.

Acute management of migraine headache pain in adolescents 12–17 years of age who have migraine attacks with or without aura that usually last ≥4 hours without treatment. Efficacy in reducing migraine-associated symptoms (nausea, photophobia, phonophobia) in adolescents not established.

Not recommended for management of hemiplegic or basilar migraine or for prophylaxis of migraine.

Safety and efficacy not established for management of cluster headaches.

Almotriptan Dosage and Administration

Administration

Oral Administration

Administer orally without regard to meals.

Dosage

Available as almotriptan malate; dosage is expressed in terms of almotriptan.

Dosage adjustment recommended when used concomitantly with potent CYP3A4 inhibitors. (See Drugs Affecting Hepatic Microsomal Enzymes under Interactions.)

Pediatric Patients

Vascular Headaches
Migraine
Oral

Adolescents 12–17 years of age: 6.25 or 12.5 mg as a single dose; individualize dosage selection, since individual response may vary. In clinical study, 12.5-mg dose provided no additional pain relief compared with 6.25-mg dose.

If headache recurs, dose may be repeated after 2 hours.

Following failure to respond to first dose, reconsider diagnosis of migraine prior to administration of a second dose.

Adults

Vascular Headaches
Migraine
Oral

6.25 or 12.5 mg as a single dose; individualize dosage selection, weighing the possible benefit (greater effectiveness) and risks (increased adverse effects) of the 12.5-mg dose. In clinical studies, doses >12.5 mg did not lead to substantially greater response.

If headache recurs, dose may be repeated after 2 hours.

Following failure to respond to first dose, reconsider diagnosis of migraine prior to administration of a second dose.

Prescribing Limits

Pediatric Patients

Vascular Headaches
Migraine
Oral

Adolescents 12–17 years of age: Maximum 12.5 mg as a single dose; do not exceed 2 doses (maximum total dosage of 25 mg) in any 24-hour period.

Safety of treating an average of >4 headaches per 30-day period has not been established.

Adults

Vascular Headaches
Migraine
Oral

Maximum 12.5 mg as a single dose; do not exceed 2 doses (maximum total dosage of 25 mg) in any 24-hour period.

Safety of treating an average of >4 headaches per 30-day period has not been established.

Special Populations

Hepatic Impairment

Initial dose of 6.25 mg; maximum dosage of 12.5 mg over a 24-hour period.

Renal Impairment

Initial dose of 6.25 mg; maximum dosage of 12.5 mg over a 24-hour period.

Geriatric Patients

Cautious dosage selection recommended; generally start at low end of dosing range due to greater frequency of decreased hepatic, renal, or cardiac function and of concomitant illnesses or other drug therapy in geriatric population.

In geriatric patients with normal renal function for their age, dosage is the same as that recommended for younger adults.

Cautions for Almotriptan

Contraindications

Warnings/Precautions

Careful Diagnosis of Migraine

Use only in patients in whom a clear diagnosis of migraine has been established.

If first migraine attack treated with almotriptan fails to respond to the drug, reconsider diagnosis before administering almotriptan to treat subsequent attacks.

Exclude other potentially serious neurologic disorders before administering almotriptan to patients not previously diagnosed with migraine or to those with atypical symptoms.

Cardiac Effects

Possible myocardial ischemia and/or infarction and coronary vasospasm, even in patients without a history of CAD. Contraindicated in patients with ischemic or vasospastic heart disease.

Possible fatal or life-threatening cardiac rhythm disturbances (e.g., ventricular tachycardia or fibrillation). Discontinue if such disturbances occur.

Tightness, pain, pressure, and heaviness in the precordium, throat, neck, and jaw occur frequently but usually are noncardiac in origin. Manufacturer states that patients with symptoms suggestive of angina after receiving almotriptan should be evaluated for the presence of CAD or predisposition to Prinzmetal variant angina before receiving additional doses; if administration is resumed and such signs or symptoms recur, ECG evaluation recommended.

Patients at Risk for CAD

Perform cardiovascular evaluation prior to initiating therapy in patients with multiple cardiovascular risk factors (e.g., postmenopausal women; men >40 years of age; patients with risk factors such as hypertension, hypercholesterolemia, smoking, obesity, diabetes, family history of CAD) who have not previously received 5-HT1 receptor agonist therapy.

If evaluation provides evidence of CAD or coronary vasospasm, do not administer the drug.

If results of evaluation are satisfactory, consider administering the initial dose in a medically supervised setting followed immediately by an ECG.

Periodic cardiovascular evaluation recommended in patients with risk factors for CAD if receiving intermittent long-term therapy.

Cerebrovascular Events

Possible cerebral or subarachnoid hemorrhage and stroke, sometimes fatal. (See Careful Diagnosis of Migraine under Cautions.) Discontinue therapy if a cerebrovascular event occurs.

Risk of certain cerebrovascular events (e.g., stroke, hemorrhage, TIA) may be increased in patients with migraine.

Other Vasospastic Effects

Possible noncoronary vasospastic reactions (e.g., peripheral vascular ischemia, GI ischemia and infarction with abdominal pain and bloody diarrhea, splenic infarction, Raynaud’s syndrome); transient or permanent blindness and partial vision loss reported very rarely in patients receiving 5-HT1 receptor agonists.

If signs or symptoms suggestive of vasospasm occur following administration, evaluate patient to rule out vasospastic reaction before administering additional doses.

Hypertensive Effects

Substantial increases in BP, including hypertensive crisis with acute impairment of organ systems, reported rarely with 5-HT1 receptor agonists in patients with or without history of hypertension.

Increases in mean pulmonary arterial pressure observed following administration of a 5-HT1 receptor agonist to patients undergoing cardiac catheterization.

Serotonin Syndrome

Potentially life-threatening serotonin syndrome reported in patients receiving 5-HT1 receptor agonists, particularly in those receiving SSRIs or SNRIs concomitantly. (See Specific Drugs under Interactions.) Also may occur in patients receiving MAO inhibitors or tricyclic antidepressants concomitantly.

Symptoms may include mental status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile BP, hyperthermia), neuromuscular aberrations (e.g., hyperreflexia, incoordination), and/or GI symptoms (e.g., nausea, vomiting, diarrhea).

If manifestations of serotonin syndrome occur, discontinue almotriptan and any concurrently administered serotonergic agents and initiate supportive and symptomatic treatment.

Medication Overuse Headache

Overuse of drugs indicated for management of acute migraine attacks (e.g., use of 5-HT1 receptor agonists, ergotamine, opiates, or certain analgesic combinations on a regular basis for ≥10 days per month) may result in migraine-like daily headaches or a marked increase in frequency of migraine attacks.

Detoxification, including withdrawal of overused drugs; treatment of withdrawal symptoms (e.g., transient worsening of headaches); and consideration of prophylactic migraine therapy may be necessary.

Sensitivity Reactions

Hypersensitivity

Hypersensitivity reactions (e.g., anaphylaxis) reported.

Sulfonamide Hypersensitivity

Potential for cross-sensitivity between almotriptan, which contains a sulfonyl group, and sulfonamides not systematically evaluated. Use almotriptan with caution in patients with known hypersensitivity to sulfonamides.

Ocular Effects

Possible accumulation of almotriptan in melanin-rich tissues (e.g., eye) over time, resulting in potential toxicity in these tissues with extended use.

Specific Populations

Pregnancy

Category C.

Lactation

Distributed into milk in rats; not known whether distributed into milk in humans. Caution advised if almotriptan is used.

Pediatric Use

Safety and efficacy not established in children <12 years of age.

Safety and tolerability in adolescents 12–17 years of age similar to that in adults. Serious adverse events reported in limited number of pediatric patients receiving 5-HT1 receptor agonists.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger adults. (See Geriatric Patients under Dosage and Administration.)

Hepatic Impairment

Use with caution; dosage adjustment recommended. (See Hepatic Impairment under Dosage and Administration and see Drugs Affecting Hepatic Microsomal Enzymes under Interactions.)

Renal Impairment

Use with caution; dosage adjustment recommended. (See Renal Impairment under Dosage and Administration and see Drugs Affecting Hepatic Microsomal Enzymes under Interactions.)

Common Adverse Effects

Adults: Nausea, paresthesia, dry mouth.

Adolescents: Dizziness, somnolence, headache, paresthesia, nausea, vomiting.

Drug Interactions

Metabolized principally by MAO-A, CYP3A4, and CYP2D6.

Drugs Affecting Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction (decreased almotriptan metabolism) with concomitant use of CYP3A4 inhibitors.

When used concomitantly with a potent CYP3A4 inhibitor, recommended initial almotriptan dose is 6.25 mg; do not exceed 12.5 mg within a 24-hour period.

Avoid concomitant use of almotriptan and potent CYP3A4 inhibitors in patients with renal or hepatic impairment.

Specific Drugs

Drug

Interaction

Comments

Alcohol

Pharmacokinetic or pharmacologic interaction unlikely

Antidepressants, SSRIs (e.g., citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline) and SNRIs (e.g., duloxetine, venlafaxine)

Potentially life-threatening serotonin syndrome

Potential increase in plasma almotriptan concentrations with concurrent fluoxetine administration

Observe carefully if used concomitantly, particularly during treatment initiation, dosage increases, or when another serotonergic agent is initiated

No dosage adjustment required if fluoxetine is used concomitantly

Ergot alkaloids (e.g., ergotamine, dihydroergotamine, methysergide [no longer commercially available in the US])

Additive vasospastic effects

Use within 24 hours contraindicated

5-HT1 receptor agonists

Additive vasospastic effects

Use within 24 hours contraindicated

Itraconazole

Potential decrease in almotriptan metabolism

Recommended initial almotriptan dose is 6.25 mg; do not exceed 12.5 mg within a 24-hour period

Avoid concomitant use in patients with renal or hepatic impairment

Ketoconazole

Decrease in almotriptan metabolism with increased systemic exposure

Recommended initial almotriptan dose is 6.25 mg; do not exceed 12.5 mg within a 24-hour period

Avoid concomitant use in patients with renal or hepatic impairment

MAO inhibitors

Potential decrease in almotriptan metabolism

No dosage adjustment required

Propranolol

Pharmacokinetic interaction unlikely

Ritonavir

Potential decrease in almotriptan metabolism

Recommended initial almotriptan dose is 6.25 mg; do not exceed 12.5 mg within a 24-hour period

Avoid concomitant use in patients with renal or hepatic impairment

Verapamil

Potential increase in plasma almotriptan concentrations

No dosage adjustment required

Almotriptan Pharmacokinetics

Absorption

Bioavailability

Well absorbed from GI tract. Absolute bioavailability is approximately 70%.

Peak plasma concentrations attained within 1–3 hours after oral administration.

Rate and extent of absorption in adolescents 12–17 years of age is similar to that in adults.

Food

Food does not affect pharmacokinetics.

Distribution

Extent

Appears to be widely distributed throughout the body.

Distributed into milk in rats; not known whether distributed into milk in humans.

Plasma Protein Binding

Approximately 35%.

Elimination

Metabolism

Metabolized to inactive metabolites principally via MAO-mediated oxidative deamination, CYP3A4, and CYP2D6, with minor contribution of flavin monooxygenase.

Elimination Route

Excreted in urine (75%) and feces (13%), with 40% of dose recovered in urine as unchanged drug.

Half-life

3–4 hours.

Special Populations

Pharmacokinetics not evaluated in patients with hepatic impairment. Based on mechanism of almotriptan clearance, maximum decrease in clearance of 60% would be expected.

In patients with moderate or severe renal impairment, clearance is reduced by approximately 40 or 65%, respectively; peak plasma concentrations increased by approximately 80% in these patients.

In healthy geriatric patients, clearance is decreased, resulting in increases in half-life and AUC compared with younger adults; not considered clinically important.

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).

Actions

Advice to Patients

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Almotriptan Malate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

6.25 mg (of almotriptan)

Axert

Janssen

12.5 mg (of almotriptan)

Axert

Janssen

AHFS DI Essentials™. © Copyright 2024, Selected Revisions August 5, 2013. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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