Therapeutic Classification: vascular headache suppressants
Pharmacologic Classification: five ht1 agonists
Absorption: Completely absorbed after oral administration, but first-pass metabolism results in 45% bioavailability.
Distribution: Unknown.
Metabolism/Excretion: Primarily metabolized by monoamine oxidase-A (MAO-A); minor conversion to an active compound; 14% excreted unchanged in urine.
Half-Life: 2–3 hr.
Contraindicated in:
- Hypersensitivity;
- Ischemic or vasospastic cardiovascular, cerebrovascular, or peripheral vascular syndromes;
- History of significant cardiovascular disease;
- Uncontrolled hypertension;
- Should not be used within 24 hr of other 5-HT1 agonists or ergot-type compounds (dihydroergotamine);
- Basilar or hemiplegic migraine;
- Concurrent MAO-A inhibitor therapy or within 2 wk of discontinuing MAO-A inhibitor therapy;
- Phenylketonuria (orally disintegrating tablet [ODT] contains aspartame).
Use Cautiously in:
- Severe renal impairment, especially in patients on dialysis;
- Moderate hepatic impairment;
- OB: Safety not established in pregnancy;
- Lactation: Safety not established in breastfeeding;
- Pedi: Safety and effectiveness not established in children <12 yr (oral films) or <6 yr (tablets and ODTs).
Exercise Extreme Caution in:
- Cardiovascular risk factors (hypertension, hypercholesterolemia, cigarette smoking, obesity, diabetes, strong family history, menopausal women or men >40 yr); use only if cardiovascular status has been evaluated and determined to be safe and 1st dose is administered under supervision.
