No

Serotonin 5-HT_1D Receptor Agonist

Acute treatment of migraine with or without auras

C

Use in patients with ischemic heart disease or Prinzmetal angina, patients with signs or symptoms of ischemic heart disease, uncontrolled hypertension; use in patients with symptomatic Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders

Use with ergotamine derivatives (within 24 hours of); use within 24 hours of another 5-HT₁ agonist; concurrent administration or within 2 weeks of discontinuing an MAOI; hypersensitivity to any component; management of hemiplegic or basilar migraine

Zolmitriptan is indicated only in patient populations with a clear diagnosis of migraine. Cardiac events (coronary artery vasospasm, transient ischemia, myocardial infarction, ventricular tachycardia/fibrillation, cardiac arrest, and death) have been reported with 5-HT₁ agonist administration. Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension. Vasospasm-related reactions have been reported other than coronary artery vasospasm. Peripheral vascular ischemia and colonic ischemia with abdominal pain and bloody diarrhea have occurred. Use with caution in patients with hepatic impairment.

>10%:

Central nervous system: Dizziness

Endocrine & metabolic: Hot flashes

Neuromuscular & skeletal: Paresthesia

1% to 10%:

Cardiovascular: Tightness in chest

Central nervous system: Drowsiness, headache

Dermatologic: Burning sensation

Gastrointestinal: Abdominal discomfort, mouth discomfort

Neuromuscular & skeletal: Myalgia, numbness, weakness, neck pain, jaw discomfort

Miscellaneous: Diaphoresis

<1%: Rashes, polydipsia, dehydration, dysmenorrhea, dysuria, renal calculus, dyspnea, thirst, hiccups

Increased toxicity: Ergot-containing drugs, MAOIs, cimetidine, oral contraceptives, SSRIs

Selective agonist for serotonin (5-HT_1B and 5-HT_1D receptors) in cranial arteries to cause vasoconstriction and reduce sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine

Onset of action: Within 30 minutes to 1 hour

Distribution: V_d: 7 L/kg

Protein binding: 25%

Metabolism: Converted to an active N-desmethyl metabolite which is 2-6 times more potent than zolmitriptan

Half-life: 2.8-3.7 hours

Bioavailability, absolute: 49%

Time to peak serum concentrations: 2-3.5 hours

Elimination: Urine (~60% to 65% of the total dose) and feces (30% to 40%)

Adults:

Dosage adjustment in hepatic impairment: Administer with caution in patients with liver disease, generally using doses <2.5 mg. Patients with moderate-to-severe hepatic impairment may have decreased clearance of zolmitriptan, and significant elevation in blood pressure was observed in some patients.

Dizziness is common, may cause drowsiness

Contraindicated with other serotonin agonists (SSRIs) and MAOIs

No information available to require special precautions

No effects or complications reported

This drug is to be used to reduce your migraine, not to prevent or reduce number of attacks. If first dose brings relief, second dose may be taken anytime after 2 hours if migraine returns. If you have no relief with first dose, do not take a second dose without consulting prescriber. Do not exceed 10 mg in 24 hours. You may experience some dizziness or drowsiness; use caution when driving or engaging in tasks requiring alertness until response to drug is known. Frequent mouth care and sucking on lozenges may relieve dry mouth. Report immediately any chest pain, heart throbbing or tightness in throat; swelling of eyelids, face, or lips; skin rash or hives; easy bruising; blood in urine, stool, or vomitus; pain or itching with urination; or pain, warmth, or numbness in extremities. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Tablet: 2.5 mg, 5 mg