ALMOTRIPTAN MALATE

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

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

MetabolismAlmotriptan is metabolized by two major and one minor pathways. Monoamine oxidase (MAO)-mediated oxidative deamination (approximately 27% of the dose), and cyt...

14.1 Adults The efficacy of almotriptan tablets (almotriptan malate) was established in three multi-center, randomized, double-blind, placebo-controlled European trials. Patients enrolled in these studies were primarily female (86%) and Caucasian (more than 98%), with a mean age of 41 years (range of 18 to 72). Patients were instructed to treat a moderate to severe migraine headache. Two hours after taking one dose of study medication, patients evaluated their headache pain. If the pain had not decreased in severity to mild or no pain, the patient was allowed to take an escape medication. If t...

Serious cardiac reactions, including myocardial infarction, have occurred following the use of almotriptan (almotriptan malate) tablets. These reactions are extremely rare and most have been reported in patients with risk factors predictive of CAD. Reactions reported in association with triptans have included coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia, and ventricular fibrillation [see Contraindications (4.1) and Warnings and Precauti...

• Ischemic heart disease, coronary artery vasospasm, or other significant underlying cardiovascular disease ( 4.1 )
• Cerebrovascular syndromes (e.g., history of stroke or TIA) ( 4.2 )
• Peripheral vascular disease (including ischemic bowel disease) ( 4.3 )
• Uncontrolled hypertension ( 4.4 )
• Do not use almotriptan tablets within 24 hours of an ergotamine-containing, or ergot-type medication, or...

• Serious adverse cardiac events, including acute myocardial infarction and life-threatening disturbances of cardiac rhythm ( 5.1 )
• It is strongly recommended that almotriptan tablets not be given to patients in whom unrecognized coronary artery disease (CAD) is predicted by the presence of risk factors. In very rare cases, serious cardiovascular events have been reported in association with almotriptan tablet use in the absence of known cardiovascular disease. If almotriptan tablets are consi...

7 DRUG INTERACTIONS

• Do not use almotriptan tablets and ergotamine-containing or ergot-type medications within 24 hours of each other ( 4.5 , 7.1 )
• Do not use almotriptan tablets and other 5-HT 1 agonist (e.g., triptans) within 24 hours of each other ( 4.6 , 7.2 )
• SSRI or SNRI: life-threatening serotonin syndrome reported during combined use with triptans ( 5.5 , 7.3 )
• Ketoconazole: use sin...