Trade Names:Axert- Tablets 6.25 mg- Tablets 12.5 mg
Selective agonist for vascular serotonin (5-HT) receptor subtype, causing vasoconstriction of cranial arteries.
Well absorbed. Absolute bioavailability is about 70%. T max is 1 to 3 h. C max is 49.5 to 64 mcg/L.
Approximately 35% is protein bound; Vd is approximately 180 to 200 L.
Metabolized to inactive metabolites by MAO-mediated oxidation (about 27%), CYP-450 (3A4 and 2D6)–mediated oxidation (about 12%), and flavin monooxygenase (minor).
The mean half-life is 3 to 4 h. About 75% is excreted by the kidneys (about 40% as unchanged drug). About 13% is excreted in feces.
Cl is decreased approximately 65% in those with CrCl 10 to 30 mL/min and decreased approximately 40% in those with CrCl 31 to 71 mL/min. C max increased approximately 80%.Hepatic Function Impairment
The max decrease expected in almotriptan Cl due to hepatic function impairment would be 60%.Elderly
A longer terminal half-life (3.7 vs 3.2 h) and a 25% higher AUC has been observed in elderly patients.Children
No differences observed in rate or extent of absorption in adolescents compared with adults.Gender
No gender differences have been observed.Race
No significant differences have been observed between black and white volunteers.
Acute treatment of migraine with or without aura in adults; acute treatment of migraine headache pain in adolescents with a history of migraine attacks, with or without aura, usually lasting 4 h or more (when untreated).
Ischemic heart disease (eg, angina pectoris, history of MI, documented silent ischemia); symptoms or findings consistent with ischemic heart disease, coronary artery vasospasm (including Prinzmetal variant angina), or other significant underlying CV disease; cerebrovascular syndromes, including but not limited to stroke of any type as well as transient ischemic attacks; peripheral vascular disease, including but not limited to ischemic bowel disease; uncontrolled hypertension; use within 24 h of treatment with another 5-HT 1 agonist or ergotamine-containing or ergot-type medication; hemiplegic or basilar migraine; hypersensitivity to any component of the product.
PO 6.25 to 12.5 mg. If headache returns, may repeat dose after 2 h (max, 2 doses per 24 h).Hepatic or Renal Function Impairment/Concomitant Therapy With Potent CYP3A4 InhibitorsAdults
PO 6.25 mg initially (max, 12.5 mg per 24 h).
Store at 59° to 86°F.
May cause prolonged vasospastic reactions; therefore, contraindicated within 24 h of almotriptan administration.MAOIs (eg, moclobemide)
Almotriptan clearance may be decreased.Other 5-HT agonists (eg, sumatriptan)
Use contraindicated within 24 h of each other.Potent CYP3A4 inhibitors (eg, erythromycin, itraconazole, ketoconazole, ritonavir)
Almotriptan plasma levels may be elevated, increasing the risk of adverse reactions.SNRIs (eg, venlafaxine), SSRIs (eg, fluoxetine)
Risk of life-threatening serotonin syndrome may be increased.Verapamil
Almotriptan plasma concentrations may be increased.
None well documented.
Hypertension, palpitations, syncope, tachycardia, vasodilation; acute MI, angina pectoris, coronary artery vasospasm (postmarketing).
Somnolence (5%); dizziness (4%); headache (2%); paresthesia (1%).
Dry mouth (1%).
Nausea (3%); vomiting (2%).
Ensure that patients with potential for coronary artery disease (CAD), including postmenopausal women, men older than 40 yr of age, and patients with risk factors for CAD (eg, diabetes, family history, hypercholesterolemia, hypertension, obesity, smoking), undergo a CV evaluation before initiating therapy. Consider obtaining an ECG during the interval immediately following the first use of almotriptan in patients with CAD risk factors.Migraine evaluation
Assess pain location, intensity, duration, and associated symptoms of migraine attack and response to treatment.
Category C .
Safety and efficacy not established in children younger than 12 years of age.
Use with caution, starting at the low end of the dosing range.
Use with caution in patients with known hypersensitivity to sulfonamides. Cross-sensitivity has not been systematically evaluated.
Cl is reduced; use with caution.
Cl is reduced; use with caution.
Serious coronary events, though rare, can occur after administration of 5-HT 1 agonists. It is strongly recommended that almotriptan not be given to patients in whom unrecognized CAD is predicted by presence of risk factors (eg, hypertension, obesity). For patients with CAD risk factors, administer first dose in health care provider's office or similarly staffed and equipped facility. Consider obtaining an ECG during interval following administration of first dose of medication to patient with potential for CAD. Coronary artery vasospasm, acute MI, life-threatening cardiac rhythm disturbances, and death have been reported.Vasospastic reactions
Vasospastic reactions such as peripheral and GI vascular ischemia with abdominal pain and bloody diarrhea may occur.
Cerebral hemorrhage, subarachnoid hemorrhage, stroke, and other cerebrovascular events have been reported with 5-HT 1 agonists, and some events have resulted in fatalities.
Because almotriptan could accumulate in melanin-rich tissues over time, there is the possibility that it could causes toxicity in these tissues with extended use. Rare reports of transient and permanent blindness and significant partial vision loss have been reported with use of triptans.
Significant elevations in systemic blood pressure have been reported on rare occasions in patients with and without a history of hypertension. Use is contraindicated in patients with uncontrolled hypertension.
Potentially life-threatening serotonin syndrome may occur, particularly during coadministration of SSRIs or SNRIs.
Hypertension, serious CV symptoms.
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