Therapeutic Classification: vascular headache suppressants
Pharmacologic Classification: five ht1 agonists
Absorption: 20–30% following oral administration.
Distribution: Well distributed to tissues.
Metabolism/Excretion: Mostly metabolized by the liver via the CYP1A2 isoenzyme; some metabolites eliminated in urine, <10% excreted unchanged.
Half-Life: 26 hr.
Contraindicated in:
- Hypersensitivity;
- Ischemic heart disease or vasospastic angina (e.g., Prinzmetal's angina);
- Wolff-Parkinson-White Syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders;
- History of stroke or transient ischemic attack;
- History of hemiplegic or basilar migraine;
- Uncontrolled hypertension;
- Peripheral vascular disease;
- Ischemic bowel disease;
- Should not be used within 24 hr of other 5-HT1 agonists or ergot-type compounds (dihydroergotamine).
Use Cautiously in:
- OB: Safety not established in pregnancy;
- Lactation: Safety not established in breastfeeding;
- Pedi: Safety and effectiveness not established in children;
- Geri: Older adults may be more susceptible to adverse cardiovascular effects.
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 first dose is administered under supervision.
