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Zolmitriptan

    DEA Class; Rx

    Common Brand Names; Zomig, Zomig Rapimelt, Zomig-ZMT

    • Serotonin 5-HT-Receptor Agonists; 
    • Antimigraine Agents

    Serotonin agonist for migraine treatment
    Available in oral and nasal spray formulas
    Similar to sumatriptan, but unlike sumatriptan, zolmitriptan can penetrate the CNS to act centrally within the trigeminovascular system

    Indicated for acute treatment of migraine with or without aura

    Hypersensitivity

    History of myocardial infarction

    Ischemic or vasospastic artery disease, including Prinzmetal variant angina or other significant underlying cardiovascular disease

    Uncontrolled HTN

    Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders

    Peripheral vascular disease

    Ischemic bowel disease

    Not indicated for basilar or hemiplegic migraine

    Do not use concurrently with or within 2 wk of using MAO Inhibitors

    Recent use (ie, within 24 hr) of another 5-HT1 agonist, ergotamine-containing medication, or ergot-type medication (such as dihydroergotamine or methysergide)

    History of stroke

    Transient ischemic attack, or history of hemiplegic or basilar migraine

    • Dizziness (6-10%)
    • Neck/throat/jaw pain (4-10%)
    • Parasthesia (5-9%)
    • Nausea (4-9%)
    • Weakness (3-9%)
    • Somnolence (5-8%)
    • Warm/cold sensation (5-7%)
    • Xerostomia (3-5%)
    • Chest pain (2-4%)
    • Diaphoresis (3%)
    • Pain (2-3%)
    • Dyspepsia (1-3%)
    • Dysphagia (2%)
    • Myasthenia (2%)
    • Palpation (2%)
    • Vertigo (2%)
    • Hypoesthesia (1-2%)
    • Myalgia (1-2%)

    Little added benefit with 5 mg PO dose compared with 2.5 mg

    Coronary artery vasospasm, myocardial infarction, transient ischemia, ventricular tachycardia/fibrillation, cardiac arrest, and death reported with use

    In patients who experience symptoms or signs suggestive of a vasospastic reaction following the use of any 5-HT1 agonist, rule out a vasospastic reaction before receiving additional doses

    Overuse of acute migraine drugs (eg, ergotamine, triptans, opioids, or combination of these drugs for ≥10 days/month) may lead to exacerbation of headache (medication overuse headache)

    As with other 5-HT1 agonists, sensations of tightness, pain, pressure, and heaviness in the precordium, throat, neck, and jaw commonly occur that are not cardiac in origin

    Cerebral hemorrhage, subarachnoid hemorrhage, and stroke have occurred with 5-HT1 agonists, including some fatalities

    Before treating headaches in patients not previously diagnosed as migraineurs, and in migraineurs who present with symptoms atypical for migraine, exclude other potentially serious neurological conditions; drug is contraindicated in patients with a history of stroke or transient ischemic attack

    May cause noncoronary vasospastic reactions (eg, peripheral vascular ischemia, GI vascular ischemia and infarction, splenic infarction, and Raynaud’s syndrome

    Significant elevation in blood pressure, including hypertensive crisis reported in patients with and without history of hypertension; monitor blood pressure in patients receiving therapy

    Potentially life-threatening serotonin syndrome may occur, particularly during combined use with SSRIs (eg, fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) or SNRIs (eg, venlafaxine, duloxetine); discontinue therapy if serotonin syndrome suspected

    Partial vision loss and blindness (transient and permanent) reported with 5-HT1 agonists

    Use caution in elderly patients, who are more likely to have underlying cardiovascular disease and hepatic or renal impairment; cardiovascular evaluation recommended in patients with other cardiovascular risk factors prior to initiation of therapy

    Therapy is indicated for acute treatment of migraine headache; not for migraine prophylaxis

    There are no adequate data on the developmental risk associated with the use in pregnant women

    There are no data on presence of drug or metabolites in human milk, effects on the breastfed infant, or on milk production

    Adults

    5 mg per single dose or 10 mg per 24 hours PO or intranasally. The safety of treating an average of more than 3 headaches with the tablets or 4 headaches with the nasal spray in a 30-day period has not been established.

    Geriatric

    5 mg per single dose or 10 mg per 24 hours PO or intranasally. The safety of treating an average of more than 3 headaches with the tablets or 4 headaches with the nasal spray in a 30-day period has not been established.

    Adolescents

    5 mg per single dose or 10 mg per 24 hours intranasally. The safety of treating an average of more than 4 headaches in a 30-day period has not been established. Safety and efficacy of oral dosage forms have not been established.

    Children

    >= 12 years: 5 mg per single dose or 10 mg per 24 hours intranasally. The safety of treating an average of more than 4 headaches in a 30-day period has not been established. Safety and efficacy of oral dosage forms have not been established.
    < 12 years: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    Zolmitriptan 

    tablet

    • 2.5mg (scored)
    • 5mg

    oral disintegrating tablet

    • 2.5mg
    • 5mg

    intranasal spray

    • 2.5mg/single-use device
    • 5mg/single-use device