Sumatriptan


Generic Medicine Info
Indications and Dosage
Nasal
Acute migraine attacks
Adult: For cases with or without aura: As spray: Initially, 10 mg or 20 mg as a single spray into one nostril at 1st sign of migraine headache. If the 1st dose was partially effective but headache recurs, may repeat dose after at least 1 or 2 hours. Max: 30 mg/24 hours or 40 mg/24 hours. As powder in cap: Initially, 22 mg, given as 11 mg insufflated into each nostril via a product-specific breath-activated delivery device at 1st sign of migraine headache. If the 1st dose was partially effective but headache recurs, may repeat dose after at least 2 hours. Max: 44 mg/24 hours. If there is no response to the initial dose, a 2nd dose must not be used for the same attack. Dosage recommendations may vary among individual products or between countries (refer to product-specific guidelines).
Child: 12-17 years As spray: Initially, 10 mg as a single spray into one nostril at 1st sign of migraine headache. If the 1st dose was partially effective but headache recurs, may repeat dose after at least 2 hours. Max: 20 mg/24 hours. If there is no response to the initial dose, a 2nd dose must not be used for the same attack. Dosage recommendations may vary among individual products or between countries (refer to product-specific guidelines).

Oral
Acute migraine attacks
Adult: For cases with or without aura: Initially, 50-100 mg taken as soon as signs of migraine headache appear. If the 1st dose was partially effective but headache recurs, may repeat dose after at least 2 hours. Max: 100 mg/dose; 200 mg/24 hours. Alternatively, up to Max of 300 mg may be taken in 24 hours. If there is no response to the initial dose, a 2nd dose must not be taken for the same attack. Dosage recommendations may vary among individual products or between countries (refer to product-specific guidelines).

Subcutaneous
Acute migraine attacks
Adult: For cases with or without aura: Initially, 6 mg as a single dose injected at 1st sign of migraine headache. If the 1st dose was partially effective but headache recurs, may repeat dose after at least 1 hour. Alternatively, if starting dose was intolerable due to side effects, lower single doses of 1-5 mg may be used. Max: 6 mg/dose; 12 mg/24 hours. If there is no response to the initial dose, a 2nd dose must not be used for the same attack. Dosage recommendations may vary among individual products or between countries (refer to product-specific guidelines).

Subcutaneous
Acute attack of cluster headache
Adult: Initially, 6 mg as a single dose at 1st signs of headache. If the 1st dose was effective but headache recurs, may repeat dose after at least 1 hour. Max: 6 mg/dose; 12 mg/24 hours. If there is no response to the initial dose, a 2nd dose must not be used for the same attack. Dosage recommendations may vary among individual products or between countries (refer to product-specific guidelines).
Hepatic Impairment
Oral:
Mild to moderate: Max single dose: 50 mg. Severe: Contraindicated.

Subcutaneous/Nasal:
Severe: Contraindicated.
Administration
May be taken with or without food.
Contraindications
Ischaemic heart disease, signs or symptoms of ischaemic coronary artery disease (CAD) or ischaemic heart disease (e.g. angina pectoris of any type, silent myocardial ischaemia, previous MI), coronary artery vasospasm including Prinzmetal’s angina, history of cerebrovascular syndromes (e.g. CVA, TIA), peripheral vascular disease (e.g. ischaemic bowel disease), moderate and severe hypertension, uncontrolled hypertension, Wolff-Parkinson-White syndrome or arrhythmias associated with cardiac accessory conduction pathway disorders; history of hemiplegic or basilar migraine, ophthalmoplegic migraine. Severe hepatic impairment. Concurrent use of sumatriptan with or within 24 hours of taking ergotamine, ergotamine derivatives and other 5-HT1 agonists. Concomitant use with or within 2 weeks of discontinuing MAO type A inhibitors.
Special Precautions
Patient with CV risk factors (e.g. diabetes, strong family history of CAD, controlled hypertension, hypercholesterolaemia, postmenopausal women, males >40 years, obesity, smoking); history of seizure disorder or conditions that lower seizure threshold; previous hypersensitivity to sulfonamides or multiple allergens. Not indicated for prophylaxis of migraine or cluster headache. SC inj: Not for IV administration. Mild to moderate hepatic and renal impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Sensation of heaviness, pressure, pain and tightness in the chest, throat, jaw or neck; peripheral vascular ischaemia, colonic ischaemia (with abdominal pain and bloody diarrhoea), splenic infarction, Raynaud’s syndrome; exacerbation of headache or medication overuse headache (frequent/prolonged use). Rarely, hypertensive crisis, seizures.
Gastrointestinal disorders: Nausea, vomiting; dysgeusia (intranasal).
General disorders and administration site conditions: Injection site reactions (e.g. pain, burning, stinging, swelling, erythema, bruising, bleeding); pain, heat or cold sensation, pressure or tightness; malaise, fatigue.
Investigations: Transient increase in blood pressure.
Musculoskeletal and connective tissue disorders: Myalgia.
Nervous system disorders: Dizziness, drowsiness, paraesthesia, hypoaesthesia.
Respiratory, thoracic and mediastinal disorders: Dyspnoea; epistaxis, nasal mucosa or throat discomfort, irritation or burning sensation (intranasal).
Vascular disorders: Flushing.
Potentially Fatal: Serious cardiac events (e.g. coronary artery vasospasm, acute MI, transient ischaemia, ventricular tachycardia and fibrillation, cardiac arrest), cerebrovascular events (e.g. cerebral or subarachnoid haemorrhage, stroke), serotonin syndrome, hypersensitivity reactions (e.g. angioedema, anaphylaxis).
IM/IV/Nasal/Parenteral/PO/SC: C
Patient Counseling Information
This drug may cause drowsiness, if affected, do not drive or operate machinery.
Monitoring Parameters
Perform CV evaluation prior to initiation of therapy in patients with multiple CV risk factors. For patients with some CV risk factors who have negative CV evaluation, obtain ECG during 1st dose administration in a medically supervised setting. Monitor headache severity, mental alertness, blood pressure; sign and symptoms of serotonin syndrome (e.g. mental status changes, autonomic instability, neuromuscular changes, gastrointestinal symptoms), angina and sensations of chest pain, tightness or pressure.
Drug Interactions
Potentially Fatal: Increased risk of coronary vasospasm with ergotamine, ergotamine derivatives (including dihydroergotamine or methysergide), and other 5-HT1 agonists (e.g. zolmitriptan). Increased risk of serotonin syndrome with MAOIs, SSRIs, TCAs and serotonin norepinephrine reuptake inhibitors (SNRIs).
Food Interaction
Increased incidence of adverse events with St. John’s wort.
Action
Description: Sumatriptan is an agonist of serotonin or 5-hydroxytryptamine 1 (5-HT1) receptor subtype. It relieves migraine by selectively acting at 5-HT1B and 5-HT1D receptors in intracranial blood vessels and sensory nerves of trigeminal system, thereby causing vasoconstriction and inhibition of neurogenic inflammation.
Onset: Oral: Approx 30 minutes; Intranasal: Approx 15-30 minutes; SC: Approx 10-15 minutes.
Pharmacokinetics:
Absorption: Rapidly but incompletely absorbed from the gastrointestinal tract (oral). Bioavailability: Approx 14-15% (oral); 19% (intranasal powder); approx 16% or 58-87% (intranasal spray [varies on brand formulation]); 97% ± 16% (SC). Time to peak plasma concentration: Approx 2-2.5 hours (oral); approx 45 minutes (intranasal powder); median 10 minutes or approx 1.5 hours (intranasal spray [varies on brand formulation]); 12 (range: 4-25) minutes (SC).
Distribution: Crosses the placenta and enters breast milk (small amounts). Volume of distribution (central): 50 L (SC). Volume of distribution (apparent): 2.7 L/kg (oral, intranasal). Plasma protein binding: 14-21%.
Metabolism: Metabolised in the liver into inactive indole acetic acid metabolite; further converted via ester glucuronide conjugation. May be metabolised primarily by monoamine oxidase type A isoenzyme. Undergoes extensive first-pass metabolism.
Excretion: Oral: Via urine (Approx 60%; predominantly as indole acetic acid metabolite, 3% as unchanged drug); faeces (approx 40%). Intranasal: Via urine (42% as indole acetic acid metabolite; 3% as unchanged drug). SC: Via urine (38% as indole acetic acid metabolite; 22% as unchanged drug). Elimination half-life: Approx 2 hours (range: 1-4 hours).
Chemical Structure

Chemical Structure Image
Sumatriptan

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5358, Sumatriptan. https://pubchem.ncbi.nlm.nih.gov/compound/Sumatriptan. Accessed June 25, 2021.

Storage
Conventional/fast-disintegrating tab: Store below 30°C. Nasal spray: Store between 15-30°C. Do not refrigerate or freeze. Protect from light. Nasal powder in cap: Store between 20-25°C. Do not refrigerate or freeze. Vial/prefilled syringe for inj: Store between 2-30°C. Protect from light.
ATC Classification
N02CC01 - sumatriptan ; Belongs to the class of selective serotonin (5HT1) agonists preparations. Used to relieve migraine.
References
Anon. Sumatriptan. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/06/2021.

Buckingham R (ed). Sumatriptan. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/06/2021.

Imigran 20 mg Nasal Spray (Glaxo Wellcome UK Ltd trading as Glaxo SmithKline UK). MHRA. https://products.mhra.gov.uk. Accessed 07/06/2021.

Imigran FDT (GlaxoSmithKline Pharmaceuticals Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/06/2021.

Imigran Injection; Imigran Subject (Glaxo Wellcome UK Ltd. trading as Glaxo SmithKline UK). MHRA. https://products.mhra.gov.uk. Accessed 07/06/2021.

Imigran Tablets 100 mg (Glaxo Wellcome UK Ltd. trading as Glaxo SmithKline UK). MHRA. https://products.mhra.gov.uk. Accessed 07/06/2021.

Imitrex Injection (GlaxoSmithKline LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 21/06/2021.

Joint Formulary Committee. Sumatriptan. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/06/2021.

Onzetra Xsail Capsule (Currax Pharmaceuticals LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 13/06/2021.

Sumatriptan Succinate Tablet (NuCare Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/06/2021.

Tosymra Spray (Promius Pharma, LLC.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 21/06/2021.

Disclaimer: This information is independently developed by MIMS based on Sumatriptan 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 © 2021 MIMS. All rights reserved. Powered by MIMS.com
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