Adult: For cases with or without aura: As spray: Initially, 2.5 mg or 5 mg as a single spray into one nostril. If migraine headache continues to persist or recur, may give a 2nd dose at least 2 hours after the initial dose. Doses must be given as soon as possible after the onset of attack. Max: 10 mg/24 hours. Dosage recommendations may vary among countries or individual products (refer to specific product guidelines). Elderly: Initiate at the lower end of the dosing range. Child: Treatment recommendations may vary among countries or individual products (refer to specific product guidelines).
Oral Acute migraine attacks
Adult: For cases with or without aura: As conventional tab: Initially, 1.25-2.5 mg. As orodispersible tab: Initially, 2.5 mg. If migraine headache continues to persist or recur, may give a 2nd dose at least 2 hours after the initial dose. If needed, subsequent attacks may be treated with 5 mg doses. Doses must be given as soon as possible after the onset of attack. Max: 10 mg/24 hours. Dosage recommendations may vary among countries or individual products (refer to specific product guidelines). Elderly: Initiate at the lower end of the dosing range.
Oral:
Moderate to severe: Max: 5 mg in 24 hours. Alternative dosing regimen: Moderate to severe: 1.25 mg. Max: 5 mg daily in severe impairment. Dosage recommendations may vary among countries or individual products (refer to specific product guidelines).
Nasal:
Moderate to severe: Not recommended.
Administration
May be taken with or without food.
Contraindications
Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders, ischaemic coronary artery disease (e.g. angina pectoris, history of MI, silent ischaemia), coronary vasospasm (e.g. Prinzmetal angina), uncontrolled or moderate to severe hypertension, history of CVA or TIA, peripheral vascular disease, ischaemic bowel disease, history of hemiplegic or basilar migraine. Concomitant administration of zolmitriptan with or within 24 hours of taking other 5-HT1 receptor agonists, ergotamine or ergotamine derivatives. Concomitant use with or within 2 weeks of discontinuing MAO-A inhibitors.
Special Precautions
Patient with risk factors for coronary artery disease (e.g. strong family history of coronary artery disease, hypertension, hypercholesterolaemia, diabetes, obesity, menopause, smoker, male >40 years). Not indicated for migraine prophylaxis or the management of hemiplegic, basilar or ophthalmoplegic migraine. Moderate to severe hepatic impairment. Elderly. Pregnancy and lactation. Patients taking cimetidine or CYP1A2 inhibitors.
Adverse Reactions
Significant: MI, coronary vasospasm, angina pectoris, peripheral or gastrointestinal vascular ischaemia and infarction, splenic infarction, Raynaud syndrome; migraine-like daily headaches, increased frequency of migraine attacks (excessive use); heaviness, pressure or tightness over the precordium. Rarely, significant elevation in blood pressure (including hypertensive crisis); partial vision loss, transient or permanent blindness; anaphylaxis or anaphylactoid reactions. Cardiac disorders: Palpitations. Gastrointestinal disorders: Nausea, vomiting, dry mouth, abdominal pain, dysphagia. General disorders and administration site conditions: Asthenia; heaviness, tightness, pain or pressure in throat, neck, limbs, or chest. Musculoskeletal and connective tissue disorders: Myalgia, muscle weakness. Nervous system disorders: Dizziness, headache, somnolence, hyperaesthesia, paraesthesia, abnormalities or disturbances of sensation, warm sensation. Potentially Fatal: Cardiac rhythm disturbances (e.g. ventricular tachycardia or fibrillation), transient ischaemia, cardiac arrest; cerebral or subarachnoid haemorrhage, stroke.
Obtain blood pressure, LFTs; ECG (with 1st dose in patients at risk of having unrecognised coronary artery disease). Assess headache severity. Perform CV evaluation in patients who have multiple CV risk factors before initiation of therapy. Monitor for signs and symptoms of angina and serotonin syndrome.
Overdosage
Symptom: Sedation. Management: Supportive treatment. In severe cases, establish and maintain patent airway, ensure adequate ventilation and oxygenation; monitor CV system.
Drug Interactions
Increased plasma concentration with MAO-A inhibitor (e.g. moclobemide), cimetidine and CYP1A2 inhibitors (e.g. fluvoxamine, ciprofloxacin). Potentially Fatal: May increase the risk of coronary vasospasm with ergotamine, ergotamine derivatives (e.g. dihydroergotamine, methysergide) or other 5-HT1B/1D agonists. Increased risk of serotonin syndrome with SSRIs (e.g. fluoxetine, paroxetine, sertraline), serotonin-norepinephrine reuptake inhibitors or SNRIs (e.g. venlafaxine, duloxetine), TCAs, MAOIs, or agents which reduce zolmitriptan's metabolism.
Food Interaction
Increased risk of adverse effects with St. John's wort.
Action
Description: Mechanism of Action: Zolmitriptan is a selective agonist of serotonin (5-HT1B and 5-HT1D receptors) that are in sensory nerves and cranial arteries of the trigeminal system. This results in the constriction of cranial vessels and inhibition of pro-inflammatory neuropeptide release, leading to relief of migraine. Onset: Within 1 hour (oral); within 15 minutes (intranasal). Pharmacokinetics: Absorption: Well absorbed (oral); rapidly absorbed via the nasopharynx (intranasal). Absolute bioavailability: Approx 40%. Time to peak plasma concentration: 1.5 hours (tab); 3 hours (orodispersible tab; nasal spray). Distribution: Volume of distribution: 7 L/kg (oral); 8.4 L/kg (intranasal). Plasma protein binding: 25%. Metabolism: Metabolised in the liver mainly into indole acetic acid, N-oxide, and N-desmethyl analogues; primary metabolism is mainly by CYP1A2. The active N-desmethyl metabolite undergoes further metabolism by MAO-A. Excretion: Via urine (approx 60-65%; 8% as unchanged drug, 31% as indole acetic acid, 7% as N-oxide, and 4% as N-desmethyl metabolites); faeces (approx 30%, mainly as unchanged drug). Elimination half-life: 2.5-3 hours.
Chemical Structure
Zolmitriptan Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 60857, Zolmitriptan. https://pubchem.ncbi.nlm.nih.gov/compound/Zolmitriptan. Accessed Feb. 22, 2022.
Storage
Store between 20-25°C. Tab: Protect from light and moisture.
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