Trade Names:Zomig- Tablets 2.5 mg- Tablets 5 mg
Trade Names:Zomig- Spray, nasal 5 mg
Trade Names:Zomig ZMT- Tablets, orally disintegrating 2.5 mgZomig Rapimelt (Canada)
Selective agonist for the vascular serotonin (5-HT) receptor subtype, causing vasoconstriction of cranial arteries and inhibition of pro-inflammatory neuropeptide release.
Vd is about 7 L/kg. It is well absorbed after oral administration of both conventional tablets and the orally disintegrating tablets. T max for oral disintegrating tablets is 3 h and for conventional tablets is 1.5 h. Bioavailability is about 40%.
Plasma protein binding is about 25%.
Converted to an active N-desmethyl metabolite such that the metabolite concentrations are about 2/ 3 that of zolmitriptan.
The t ½ is 3 h. About 8% of the dose is recovered in urine as unchanged drug. Mean total plasma Cl is about 31.5 mL/min/kg and 25.9 mL/min/kg for nasal spray. Cl is renal tubular secretion.
Cl was reduced 25% in patients with severe renal function impairment. No change in Cl was found in moderately renally impaired patients.Hepatic Function Impairment
In severely hepatically impaired patients, the C max , T max , and AUC were increased 1.5-, 2-, and 3-fold, respectively. When dosed orally, the effect of hepatic disease on zolmitriptan nasal spray has not been evaluated. Administer with caution in subjects with liver disease, generally using doses less than 2.5 mg.Gender
Mean plasma concentrations were up to 1.5-fold higher in women than men.
Short-term treatment of migraine attacks with/without aura.
Ischemic heart disease or in patients with Prinzmetal angina; symptoms consistent with possible ischemic heart disease; uncontrolled hypertension; symptomatic Wolff-Parkinson-White syndrome; use within 24 h of treatment with another 5-HT agonist or an ergotamine-containing or ergot-like medication; coadministration of, or within 2 wk of discontinuation of, an MAO inhibitor, management of hemiplegic or basilar migraines.
PO Initial recommended dose is up to 2.5 mg (eg, ½ tablet) with fluids; max recommended single dose is 5 mg. If headache returns, the dose may be repeated after 2 h, not to exceed 10 mg within a 24-h period. The effectiveness of a second dose, if the initial dose is ineffective, has not been determined.Adults
Intranasal One dose of 5 mg for acute migraine. If headache returns, dose may be repeated after 2 h (max, 10 mg per 24 h). Response is individual. Doses lower than 5 mg can only be achieved through the use of an oral formulation. Make the choice of dose and route of administration on an individual basis.
Store tablets, orally-disintegrating tablets, and nasal spray at controlled room temperature (68° to 77°F). Protect from light and moisture.
Avoid use within 24 h of each other.Cimetidine
Zolmitriptan levels and t ½ may be increased.Ergot-containing or ergot-type drugs (eg, methysergide)
May cause additive prolonged vasospastic reactions. Avoid use within 24 h of each other.MAO inhibitors (eg, phenelzine)
Do not use zolmitriptan concurrently or within 2 wk of discontinuation of a MAO inhibitor.Selective serotonin reuptake inhibitors (eg, fluoxetine)
Combined use may cause weakness, hyperreflexia, and incoordination.Sibutramine
Serotonin syndrome, including CNS irritability, motor weakness, shivering, myoclonus, and altered consciousness, may occur.
None well documented.
Palpitations; coronary artery vasospasm, transient myocardial ischemia, angina pectoris, MI (postmarketing).
Paresthesia, dizziness, somnolence, vertigo, hyperesthesia (at least 2%); headache (postmarketing).
Nasal cavity discomfort (at least 2%).
Unusual taste (21% intranasal); dry mouth, dyspepsia, dysphagia, nausea (at least 2%); ischemic colitis, GI infarction or necrosis (postmarketing).
Anaphylaxis or anaphylactoid reactions, angioedema (postmarketing).
Asthenia, pain, chest/throat/neck pain, tightness, or heaviness, warm or cold sensations, sweating (at least 2%).
Category C .
Safety and efficacy not established.
Safety and efficacy in patients older than 65 yr of age not established.
Use with caution; use doses less than 2.5 mg.
Serious coronary events, though extremely rare, can occur after administration of 5-HT 1 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 coronary artery disease (CAD).
Cerebral hemorrhage, subarachnoid hemorrhage, stroke, and other cerebrovascular events have been reported with 5-HT 1 agonists.
Elevation in BP, including hypertensive crisis, have been reported.
Orally-disintegrating tablets contain phenylalanine. Do not administer orally disintegrating tablet to patient with phenylketonuria without first discussing with health care provider.
Copyright © 2009 Wolters Kluwer Health.