ZOLMITRIPTAN

ZOLMITRIPTAN
(zol-mi-trip'tan)
Zomig, Zomig ZMT, Zomig Nasal Spray
Classifications: serotonin 5-ht₁ receptor agonist;
Therapeutic: antimigraine; ergot alkaloid
Prototype: Sumatriptan
Pregnancy Category: C

Availability

2.5 mg, 5 mg tablets orally disintegrating tablets; 5 mg nasal spray

Action

Selective serotonin (5-HT_1B/1D) receptor agonist. The agonist effects at 5-HT_1B/1D reverse the vasodilation of cranial blood vessels and inhibit release of pro-inflammatory neuropeptides.

Therapeutic Effect

Vasoconstricts dilated cranial blood vessels and decreased neuropeptide release relieve the pain of a migraine headache.

Uses

Acute migraine headaches with or without aura.

Contraindications

Hypersensitivity to zolmitriptan; ischemic heart disease (angina pectoris, arteriosclerosis, ECG changes, history of MI or Prinzmetal's angina); cardiac arrhythmias, symptomatic Wolff-Parkinson-White syndrome, uncontrolled hypertension; hemiplegia or basilar migraine; concurrent administration of ergotamine or sumatriptan; PKU; adults >65 y; pregnancy (category C); children <18 y.

Cautious Use

Men >40 y; postmenopausal women; patients with other cardiac risk factors, such as diabetes, obesity, cigarette smoking, high cholesterol levels, strong family history of CAD; concurrent administration of MAOIs; GI disease, PVD, ischemic colitis, Raynaud's disease, cerebrovascular disease, stroke, intracranial bleeding; renal failure or renal disease; lactation.

Route & Dosage

Acute Migraine
Adult: PO 2.5–5 mg, may repeat in 2 h if necessary (max: 10 mg/24 h) Nasal Spray One spray into one nostril

Administration

Oral

Give any time after symptoms of migraine appear. Give ≤2.5 mg by breaking a 5 mg tablet in half. If headache returns, may repeat q2h up to 10 mg in 24 h.
Do NOT give zolmitriptan within 24 h of an ergot-containing drug or other 5-HT₁ agonist.
Discard unused tablets that have been removed from the packaging.

Intranasal

Unit-dose spray device delivers a 5 mg dose. Do not exceed the maximum dose of 10 mg in 24 h.
Store at 2°–25° C (36°–77° F) and protect from light.

Adverse Effects (≥1%)

Body as a Whole: Asthenia, fatigue, malaise, pain, pressure sensation, paresthesia, throat pressure, warm/cold sensations, hypesthesia. CNS: Somnolence, dizziness, drowsiness, headache, hypesthesia, decreased mental acuity, euphoria, tremor. CV: Coronary artery vasospasm, transient myocardial ischemia, MI, ventricular tachycardia, ventricular fibrillation, chest pain/tightness/heaviness, palpitations. GI: Dry mouth, nausea, vomiting. Respiratory: Dyspnea. Skin: Flushing. Other: Hot flushes.

Interactions

Drug: Dihydroergotamine, methysergide, other 5-ht₁ agonists may cause prolonged vasospastic reactions; ssris have rarely caused weakness, hyperreflexia, and incoordination; maois should not be used with 5-ht₁ agonists; cimetidine increases half-life of zolmitriptan. Herbal: St. John's wort may increase triptan toxicity.

Pharmacokinetics

Absorption: Rapidly absorbed, 40% bioavailability. Peak: 2–3 h. Distribution: 25% protein bound. Metabolism: In liver to active metabolite. Elimination: Primarily in urine (65%), 30% in feces. Half-Life: 3 h.

Nursing Implications

Assessment & Drug Effects

Monitor for therapeutic effectiveness: Relief or reduction of migraine pain within 1–4 h.
Monitor cardiovascular status carefully following first dose in patients at risk for CAD (e.g., postmenopausal women, men >40 y, persons with known CAD risk factors) or coronary artery vasospasms.
Perform periodic cardiovascular evaluation and ECG with long-term use.
Report to physician immediately chest pain, nausea, or tightness in chest or throat that is severe or does not quickly resolve.

Patient & Family Education

Carefully review patient information insert and guidelines for taking drug.
Do NOT take zolmitriptan during the aura phase, but as early as possible after onset of migraine.
Concurrent oral contraceptive use may increase incidence of adverse effects.
Contact physician immediately if any of the following occur after zolmitriptan use: Symptoms of angina (e.g., severe or persistent pain or tightness in chest or throat, sudden nausea), hypersensitivity (e.g., wheezing, facial swelling, skin rash, hives), fainting, or abdominal pain.
Report any other adverse effects (e.g., tingling, flushing, dizziness) at next physician visit.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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