Zolmitriptan - oral


Concise Prescribing Info
Indications/Uses
Acute migraine attacks.
Dosage/Direction for Use
Adult : PO Initial: 2.5 mg, 2nd dose may be taken at least 2 hr after the 1st dose if symptoms recur w/in 24 hr. Max: 10 mg/24 hr. Nasal 1 spray (5 mg) into 1 nostril as soon as possible after onset of symptoms. 2nd dose may be used at least 2 hr after the 1st dose if symptoms recur w/in 24 hr. Max: 10 mg/day.
Dosage Details
Nasal
Acute migraine attacks
Adult: 5 mg (1 spray) into 1 nostril as soon as possible after onset of symptoms, repeated at least 2 hr after the 1st dose if symptoms recur w/in 24 hr. Max: 10 mg/day. Safety of treating >4 headaches in a 30 day period is not established.

Oral
Acute migraine attacks
Adult: Initially, 2.5 mg. A 2nd dose may be taken at least 2 hr after the 1st dose if symptoms recur within 24 hr. Max dose: 10 mg in 24 hr. Safety of treating > three headaches in a 30-day period has not been established.
Special Patient Group
Concurrent use with cimetidine, quinolone antibacterials: Max dose: 5 mg in 24 hr.
Hepatic Impairment
Nasal:
Avoid use.
Oral:
Dose reduction may be needed with BP monitoring. Moderate to severe: Max dose: 5 mg/24 hr
Administration
May be taken with or without food.
Contraindications
Patients at risk of coronary artery disease (post-menopausal women, men >40 yr, hypertension, hypercholesterolemia, smoking, obesity, DM, family history of coronary artery disease) unless evaluated. Wolff-Parkinson-White syndrome; arrhythmias associated with accessory cardiac conduction pathways; previous cerebrovascular accident; uncontrolled or severe hypertension; ischaemic heart disease, history of MI, coronary vasospasm, transient ischaemic attack. Basilar or hemiplegic migraine.
Special Precautions
Use only if there is a clear diagnosis of migraine; exclude other potentially serious neurological conditions. Monitor BP closely. May impair ability to drive or operate machinery. Pregnancy and lactation. Child. Moderate to severe hepatic impairment. Prior CV evaluation for patients with risk factors of coronary heart disease; admin of first dose under close supervision and ECG if satisfactory CV assessment in these patients. Periodic CV evaluation for patients with risk factors of coronary arteries on zolmitriptan. Avoid oral disintegrating formulation for patients with phenylketouria. Long term use may cause accumulation of zolmitriptan in melanin rich tissue (e.g. eye).
Adverse Reactions
Dizziness, asthenia, dry mouth, hyperesthesia, paresthesia, drowsiness, nausea, pain or sensations of tingling, heaviness, pressure or tightness in any part of the body including throat/chest; cerebrovascular events; transient increases in blood pressure; hypotension, ischaemic colitis, GI infarction, hypersensitivity reactions, coronary vasospasm.
Potentially Fatal: Cardiac arrhythmias, MI, subarachnoid haemorrhage.
Drug Interactions
Increased risk of serotonin syndrome with SSRI, selective serotonin- and norepinephrine-reuptake inhibitors (SNRI). Increased zolmitriptan concentrations with cimetidine, quinolone antibacterials and drugs that inhibit the cytochrome P450 isoenzyme CYP1A2.
Potentially Fatal: Increased risk of fatal serotonin syndrome with sibutramine. Increased risk of serotonin syndrome with MAOI and reversible inhibitors of monoamine oxidase type-A (RIMA); do not use zolmitriptan during and for 2 wk after the use of MAOI and RIMAs Do not use within 24 hr of treatment with another 5-HT1 agonist. Increased risk of additive vasoconstriction with ergot alkaloids; zolmitriptan should not be taken within 24 hr of any ergotamine or ergot-type medication.
Action
Description: Zolmitriptan is a selective agonist for serotonin (5HT1 receptors). It relieves migraine by selective constriction of intracranial blood vessels, neuropeptide release inhibition and decreased transmission in the trigeminal pain pathway.
Onset: 1 hr (oral); 15 min (intranasal).
Pharmacokinetics:
Absorption: Absolute bioavailability: 40% (oral and intranasal). Peak plasma concentration: 1.5-3 hr (oral); 3 hr (intranasal).
Distribution: Protein binding: 25%.
Metabolism: Undergo hepatic metabolism mainly by the cytochrome P450 isoenzyme CYP1A2 to more active metabolite, N-desmethyl metabolite and inactive metabolites. N-desmethyl metabolite is further metabolised by monoamine oxidase type A.
Excretion: Excreted via urine as metabolites (over 60%) and unchanged drug (30%). Elimination half life: 2.5-3 hr; prolonged in liver disease.
Storage
Store at 20-25°C (68-77°F).
Disclaimer: This information is independently developed by MIMS based on Zolmitriptan from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
  • Zomig Rapimelt
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