ZOLMITRIPTAN
(zol-mi-trip′tan)
Zomig, Zomig ZMT, Zomig Nasal Spray
Classifications: SEROTONIN 5-HT1 RECEPTOR AGONIST; ERGOT ALKALOID
Therapeutic: ANTIMIGRAINE
Prototype: Sumatriptan
Pregnancy Category: C
AVAILABILITY
Tablet; orally disintegrating tablet; nasal spray
ACTION & THERAPEUTIC EFFECT
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. 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.
CAUTIOUS USE
Men older than 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; adults older than 65 y; pregnancy (category C), lactation; children younger than 18 y.
ROUTE AND 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
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Nursing Implications ZOLMITRIPTAN(zol-mi-trip′tan) |
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ADMINISTRATION
Oral
- Give any time after symptoms of migraine appear. Give 2.5 mg or less 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 older than 40 y, persons with known CAD risk factors) or coronary artery vasospasms.
- Periodic cardiovascular evaluation is recommended with longterm use.
- Report to prescriber 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.
- Do not remove orally disintegrating tablet from blister until just prior to dosing.
- Concurrent oral contraceptive use may increase incidence of adverse effects.
- Contact prescriber 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 prescriber visit.
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