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-HT1B/1D) receptor agonist. The agonist effects at 5-HT1B/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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