Zolmitriptan

A to Z Drug Facts

 Action Selective agonist for the vascular serotonin (5–HT) receptor subtype, causing vasoconstriction of cranial arteries and inhibition of pro-inflammatory neuropeptide release.

 Indications Short-term treatment of migraine attacks with/without aura.

 Contraindications Ischemic heart disease or in patients with Prinzmetal’s angina; symptoms consistent with possible ischemic heart disease; uncontrolled hypertension; symptomatic Wolff-Parkinson-White syndrome; use within 24 hr of treatment with another 5–HT agonist or an ergotamine-containing or ergot-like medication; concurrent administration of, or within 2 wks of discontinuation of, a MAO inhibitor, management of hemiplegic or basilar migraines.

 Route/Dosage

ADULTS: PO Initial recommended dose is 2.5 mg or lower (eg, ½ tablet) with fluids; maximum recommended single dose is 5 mg. If headache returns, the dose may be repeated after 2 hr, not to exceed 10 mg within a 24–hr period. The effectiveness of a second dose, if the initial dose is ineffective, has not been determined.

 Interactions

Ergot-containing or ergot-type drugs (eg, methysergide)

May cause additive prolonged vasospastic reactions. Avoid use within 24 hrs of each other.

5–HT₁ agonists (eg, sumatriptan): Avoid use within 24 hrs of each other.

MAO Inhibitors (eg, phenelzine): Do not use zolmitriptan concurrently or within 2 wks of discontinuation of a MAO inhibitor.

Cimetidine: Zolmitriptan levels and half-life may be increased.

Selective Serotonin Reuptake Inhibitors (eg, fluoxetine): Combined use may cause weakness, hyper-reflexia, and incoordination.

 Lab Test Interferences None well documented.

 Adverse Reactions

CARDIOVASCULAR: Palpitations. CNS: Paresthesia; dizziness; somnolence; vertigo; hyperesthesia; paresthesia. GI: Dry mouth; dyspepsia; dysphagia; nausea. OTHER: Asthenia; pain; chest or neck pain; tightness or heaviness; warm sensations; cold sensations; myalgia; myasthenia; sweating.

 Precautions

Pregnancy: Category C. Lactation: Undetermined. Children: Safety and efficacy not established. Elderly: Safety and efficacy in patients > 65 yr not established. Cardiac events/vasoconstriction: Serious coronary events, though extremely rare, can occur after administration of 5–HT₁ agonists. Administer first dose in health care provider’s office to patients at possible risk of unrecognized coronary disease. If symptoms consistent with angina occur, conduct ECG evaluation for ischemic changes. May cause coronary vasospasm in patients with history of CAD. Hepatic Function Impairment: Use with caution; use doses < 2.5 mg.

 Administration/Storage

• Administer prescribed dose at onset of migraine symptoms.
• If first dose is ineffective, do not administer a second dose unless prescribed by health care provider.
• Store at room temperature protected from light and moisture.

 Assessment/Interventions

• Obtain patient history, including drug history, and any known allergies.
• Note recent use of ergot-containing or ergot-type drugs, and current or recent use a MAO inhibitor.
• Assess pain location, intensity, duration, and associated symptoms of migraine attack.
• Administer first dose in health care provider’s office, or other adequately staffed medical facility, to patients with potential for coronary artery disease (CAD) including: Postmenopausal women; men > 40 yr; patients with risk factors for CAD (hypertension, hypercholesterolemia, obesity, diabetes, smokers, family history). If angina occurs, monitor ECG for ischemic changes.
• Provide quite, calm environment. Decrease stimuli, noise, and light.
• Monitor for side effects.

 Patient/Family Education

• Provide patient information pamphlet.
• Explain that drug is to be used during migraine and does not prevent or reduce the number of attacks. Emphasize that drug is used only to treat actual migraine attack.
• Advise patient that drug is to be taken as soon as symptoms of migraine appear. A second dose may be taken if symptoms return, but no sooner than 2 hrs following the first dose. For a given attack, if there is no response to the first tablet, do not take a second tablet without first consulting with a health care provider. Do not take > 10 mg in any 24–hr period.
• Advise patient that if pain, tightness, or pressure in chest or throat occurs when using zolmitriptan, to notify health care provider prior to using drug again. If chest pain is severe or does not go away, tell patient to notify health care provider immediately.
• Instruct patient to notify health care provider immediately if shortness of breath, wheeziness, heart throbbing, swelling of eyelids, face or lips, or a skin rash, skin lumps, or hives occur.
• Advise patient to notify health care provider if experiencing feelings of tingling, heat, heaviness, or pressure after treatment.
• Advise patient to notify health care provider immediately if they have symptoms they do not understand.
• Advise patient that drug may cause drowsiness or dizziness and to use caution while driving or performing other activities requiring mental alertness.
• Instruct patient to notify health care provider if pregnant, plan on becoming pregnant, or are breastfeeding.

Books@Ovid
Copyright © 2003 Facts and Comparisons
David S. Tatro
A to Z Drug Facts