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    Zolmitriptan

    Table of Contents > Drugs > Zolmitriptan     Print

    Pronunciation
    U.S. Brand Names
    Synonyms
    Generic Available
    Canadian Brand Names
    Use
    Pregnancy Risk Factor
    Pregnancy Implications
    Lactation
    Contraindications
    Warnings/Precautions
    Adverse Reactions
    Overdosage/Toxicology
    Drug Interactions
    Ethanol/Nutrition/Herb Interactions
    Stability
    Mechanism of Action
    Pharmacodynamics/Kinetics
    Dosage
    Administration
    Patient Education
    Additional Information
    Anesthesia and Critical Care Concerns/Other Considerations
    Cardiovascular Considerations
    Dental Health: Effects on Dental Treatment
    Dental Health: Vasoconstrictor/Local Anesthetic Precautions
    Mental Health: Effects on Mental Status
    Mental Health: Effects on Psychiatric Treatment
    Dosage Forms
    International Brand Names

    Pronunciation

    (zohl mi TRIP tan)

    U.S. Brand Names

    Zomig®; Zomig-ZMT™

    Synonyms

    311C90

    Generic Available

    No

    Canadian Brand Names

    Zomig®; Zomig® Rapimelt

    Use

    Acute treatment of migraine with or without aura

    Pregnancy Risk Factor

    C

    Pregnancy Implications

    There are no adequate and well-controlled studies using sumatriptan in pregnant women. Use only if potential benefit to the mother outweighs the potential risk to the fetus. In animal studies, administration was associated with embryolethality, fetal abnormalities, and pup mortality.

    Lactation

    Excretion in breast milk unknown/use caution

    Contraindications

    Hypersensitivity to zolmitriptan or any component of the formulation; ischemic heart disease or Prinzmetal's angina; signs or symptoms of ischemic heart disease; uncontrolled hypertension; symptomatic Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders; use with ergotamine derivatives (within 24 hours of); use within 24 hours of another 5-HT1 agonist; concurrent administration or within 2 weeks of discontinuing an MAO inhibitor; management of hemiplegic or basilar migraine

    Warnings/Precautions

    Zolmitriptan is indicated only in patient populations with a clear diagnosis of migraine. Not for prophylactic treatment of migraine headaches. Cardiac events (coronary artery vasospasm, transient ischemia, myocardial infarction, ventricular tachycardia/fibrillation, cardiac arrest, and death) have been reported with 5-HT1 agonist administration. Should not be given to patients who have risk factors for CAD (eg, hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, menopause, male >40 years of age) without adequate cardiac evaluation. Patients with suspected CAD should have cardiovascular evaluation to rule out CAD before considering zolmitriptan's use; if cardiovascular evaluation negative, first dose would be safest if given in the healthcare provider's office. Periodic evaluation of those without cardiovascular disease, but with continued risk factors should be done. Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension. Vasospasm-related reactions have been reported other than coronary artery vasospasm. Peripheral vascular ischemia and colonic ischemia with abdominal pain and bloody diarrhea have occurred. Use with caution in patients with hepatic impairment. Zomig-ZMT™ tablets contain phenylalanine. Safety and efficacy not established in patients <18 years of age.

    Adverse Reactions

    Percentages noted from oral preparations.

    1% to 10%:

    Cardiovascular: Chest pain (2% to 4%), palpitation (up to 2%)

    Central nervous system: Dizziness (6% to 10%), somnolence (5% to 8%), pain (2% to 3%), vertigo (2%)

    Gastrointestinal: Nausea (4% to 9%), xerostomia (3% to 5%), dyspepsia (1% to 3%), dysphagia (2%)

    Neuromuscular & skeletal: Paresthesia (5% to 9%), weakness (3% to 9%), warm/cold sensation (5% to 7%), hypesthesia (1% to 2%), myalgia (1% to 2%), myasthenia (up to 2%)

    Miscellaneous: Neck/throat/jaw pain (4% to 10%), diaphoresis (up to 3%), allergic reaction (up to 1%)

    <1% Agitation, akathisia, alkaline phosphatase increase, amnesia, anorexia, anxiety, apathy, apnea, appetite increased, arrhythmia, arthritis, ataxia, back pain, bradycardia, bronchitis, bronchospasm, bruising, cerebral ischemia, chills, constipation, cyanosis, cystitis, depression, diplopia, dry eyes, dysmenorrhea, dystonia, ear pain, edema, emotional lability, eosinophilia, epistaxis, esophagitis, extrasystole, euphoria, eye pain, facial edema, fever, gastritis, gastroenteritis, hallucinations, hematemesis, hematuria, hiccups, hyperacusis, hyperesthesia, hyperglycemia, hyperkinesias, hypertension, hypertensive crisis, hypertonia, hypotonia, insomnia, irritability, lacrimation, laryngitis, leg cramps, leukopenia, liver function abnormality, malaise, melena, miscarriage, pancreatitis, parosmia, photosensitivity, polyuria, postural hypotension, pruritus, QT prolongation, rash, syncope, tachycardia, tenosynovitis, tetany, thirst, thrombocytopenia, thrombophlebitis, tinnitus, tongue edema, twitching, ulcer, urinary frequency, urinary urgency, urticaria, voice alteration, yawning

    Postmarketing and/or case reports: Anaphylactoid reaction, anaphylaxis, angina pectoris, coronary artery vasospasm, gastrointestinal infarction/necrosis, headache, ischemic colitis, MI, myocardial ischemia, splenic infarction

    Events related to other serotonin 5-HT1D receptor agonists: Cerebral hemorrhage, stroke, subarachnoid hemorrhage, peripheral vascular ischemia, ventricular fibrillation

    Overdosage/Toxicology

    Treatment is symptom-directed and supportive. It is not known if hemodialysis or peritoneal dialysis is effective.

    Drug Interactions

    Substrate of CYP1A2 (minor)

    Cimetidine: Zolmitriptan serum levels increased; avoid concurrent use

    Ergot-containing drugs (dihydroergotamine, methysergide): Concurrent use may lead to vasospastic reactions; separate use by at least 24 hours.

    MAO inhibitors: Increases systemic exposure to zolmitriptan. Avoid concurrent use and use within 2 weeks of discontinuing a MAO inhibitor. Selegiline (selective MAO type B inhibitor) does not affect zolmitriptan levels.

    Oral contraceptives: Zolmitriptan serum levels increased with concurrent use.

    Propranolol: Increased zolmitriptan toxicity

    Selective serotonin reuptake inhibitors (SSRIs): Concurrent use may lead to serotonin syndrome.

    Sibutramine: Concurrent use may lead to serotonin syndrome.

    Ethanol/Nutrition/Herb Interactions

    Ethanol: Limit use (may have additive CNS toxicity).

    Stability

    Store at 20°C to 25°C (68°F to 77°F); protect from light and moisture

    Mechanism of Action

    Selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in cranial arteries to cause vasoconstriction and reduce sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine

    Pharmacodynamics/Kinetics

    Onset of action: 0.5-1 hour

    Absorption: Well absorbed

    Distribution: Vd: 7 L/kg

    Protein binding: 25%

    Metabolism: Converted to an active N-desmethyl metabolite (2-6 times more potent than zolmitriptan)

    Half-life elimination: 2.8-3.7 hours

    Bioavailability: 40%

    Time to peak, serum: Tablet: 1.5 hours; Orally-disintegrating tablet and nasal spray: 3 hours

    Excretion: Urine (~60% to 65% total dose); feces (30% to 40%)

    Dosage

    Oral:

    Children: Safety and efficacy have not been established

    Adults: Migraine:

    Tablet: Initial: 2.5 mg at the onset of migraine headache; may break 2.5 mg tablet in half

    Orally-disintegrating tablet: Initial: 2.5 mg at the onset of migraine headache

    Nasal spray: Initial: 1 spray (5 mg) at the onset of migraine headache

    Note: Use the lowest possible dose to minimize adverse events. If the headache returns, the dose may be repeated after 2 hours; do not exceed 10 mg within a 24-hour period. Controlled trials have not established the effectiveness of a second dose if the initial one was ineffective

    Elderly: No dosage adjustment needed but elderly patients are more likely to have underlying cardiovascular disease and should have careful evaluation of cardiovascular system before prescribing.

    Dosage adjustment in renal impairment: No dosage adjustment recommended. There is a 25% reduction in zolmitriptan's clearance in patients with severe renal impairment (Clcr 5-25 mL/minute)

    Dosage adjustment in hepatic impairment: Administer with caution in patients with liver disease, generally using doses <2.5 mg. Patients with moderate-to-severe hepatic impairment may have decreased clearance of zolmitriptan, and significant elevation in blood pressure was observed in some patients.

    Administration

    Administer as soon as migraine headache starts.

    Tablet: May be broken

    Orally-disintegrating tablet: Must be taken whole; do not break, crush or chew; place on tongue and allow to dissolve; administration with liquid is not required

    Nasal spray: Blow nose gently prior to use. After removing protective cap, instill device into nostril. Block opposite nostril; breathe in gently through nose while pressing plunger of spray device. One dose (5 mg) is equal to 1 spray in 1 nostril.

    Patient Education

    Inform prescriber of all prescriptions (including oral contraceptives), OTC medications, or herbal products you are taking, and any allergies you have. This drug is to be used to reduce your migraine, not to prevent or reduce the number of attacks. Follow exact instructions for use. Remove orally-disintegrating tablet from blister package just before using, place on tongue, and allow to dissolve. Do not crush, break, or chew. Regular tablet may be broken in half for use. Do not remove protective cap from nasal spray until ready to use. Do not take within 24 hours of any other migraine medication without first consulting prescriber. If first dose brings relief, second dose may be taken anytime after 2 hours if migraine returns. If you have no relief with first dose, do not take a second dose without consulting prescriber. Do not exceed 10 mg in 24 hours. May cause dizziness or drowsiness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or dry mouth (frequent mouth care and sucking on lozenges may help). Report immediately any chest pain, heart throbbing, or tightness in throat; swelling of eyelids, face, or lips; skin rash or hives; easy bruising; blood in urine, stool, or vomitus; pain or itching with urination; or pain, warmth, or numbness in extremities. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

    Additional Information

    Not recommended if the patient has risk factors for heart disease (high blood pressure, high cholesterol, obesity, diabetes, smoking, strong family history of heart disease, postmenopausal woman, or a male >40 years of age).

    This agent is intended to relieve migraine, but not to prevent or reduce the number of attacks. Use only to treat an actual migraine attack.

    Anesthesia and Critical Care Concerns/Other Considerations

    Zolmitriptan should not be used in patients with a history of vasospastic disease, Prinzmetal's angina, or any critical vascular disease.

    Cardiovascular Considerations

    Coronary vasospasm has been associated with 5-HT1B/1D agonists. These agents are contraindicated in patients with documented ischemic of vasospastic coronary artery disease. Patients with risk factors for CAD may receive these agents, provided a cardiovascular evaluation yields satisfactory evidence that the patient is free of cardiovascular disease. In patients with risk factors for CAD, administration of the initial dose in a medically staffed/equipped facility (ie, physician's office) is recommended. In addition, ECG monitoring after the initial dose should be considered. Patients who acquire risk factors for CAD, or long-term users of agents from this class of medications, should undergo periodic cardiovascular evaluation.

    Dental Health: Effects on Dental Treatment

    Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).

    Dental Health: Vasoconstrictor/Local Anesthetic Precautions

    No information available to require special precautions

    Mental Health: Effects on Mental Status

    Dizziness is common, may cause drowsiness

    Mental Health: Effects on Psychiatric Treatment

    Contraindicated with other serotonin agonists (SSRIs) and MAO inhibitors

    Dosage Forms

    Solution, nasal spray [single dose] (Zomig®): 5 mg/0.1 mL (0.1 mL)

    Tablet (Zomig®): 2.5 mg, 5 mg

    Tablet, orally-disintegrating (Zomig-ZMT™): 2.5 mg [contains phenylalanine 2.81 mg/tablet; orange flavor]; 5 mg [contains phenylalanine 5.62 mg/tablet; orange flavor]

    International Brand Names

    AscoTop® (DE); Flezol® (ES); Zomig® (AT, AU, BE, BG, BR, CA, CH, DK, ES, FI, FR, GB, HR, HU, IE, IL, IT, MX, NL, NO, PL, PT, RU, SE, SG, SI, TH, TR, YU, ZA); Zomigon® (AR); Zomigoro® (FR); Zomig® Rapimelt (CA); Zomig Rapimelt® (GB, IL)

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