Absorption: Well absorbed (70%) following oral administration.
Distribution: Unknown.
Metabolism/Excretion: 60% excreted unchanged in urine; 30% metabolized by the liver.
Half-life: 6 hr (↑ in renal impairment).
Contraindicated in:
- Hypersensitivity
- Ischemic heart disease or Prinzmetal's angina
- Uncontrolled hypertension
- Wolff-Parkinson-White syndrome, or other arrhythmias involving conduction pathways
- Hemiplegic or basilar migraine
- Stroke or transient ischemic attack
- Peripheral vascular disease
- Ischemic bowel disease
- Severe renal impairment (CCr <15 mL/min)
- Severe hepatic impairment
- Should not be used within 24 hr of other 5-HT1 agonists or ergot-type compounds (dihydroergotamine)
- Geri: Age-related ↓ in renal function and ↑ likelihood of CAD greatly ↑ risk of fatal adverse events.
Use Cautiously in:
- Mild to moderate renal or hepatic impairment (dose should not exceed 2.5 mg/24 hr; initial dose should be ↓)
- OB: Lactation: Pedi: Safety not established.
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.
CV: CORONARY ARTERY VASOSPASM, MI, VENTRICULAR FIBRILLATION, VENTRICULAR TACHYCARDIA, myocardial ischemia.
GI: nausea.
Neuro: paresthesia , dizziness, drowsiness, malaise/fatigue.
Misc: pain/pressure sensation in throat/neck.
Therapeutic Classification: vascular headache suppressants
Pharmacologic Classification: five ht1 agonists
(↓ migraine pain)
34 hr during migraine attack.