Peringatan Keamanan

Symptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation.L6793,L6796,L6799,L6805,L6808,L6811 Overdoses may be fatal and patients should be monitored for 3-5 half lives or while symptoms persist.L6793,L6796,L6799,L6805,L6808,L6811

Sumatriptan

DB00669

small molecule approved investigational

Deskripsi

Sumatriptan is a serotonin receptor agonist commonly used to treat migraines and sometimes cluster headaches.L6793,L6796,L6799,L6805,L6808,L6811 Sumatriptan is the first of the triptans and was made available in Europe in 1991 to treat migraines.A179761 Sumatriptan was granted FDA approval on 28 December 1992.L6805

Struktur Molekul 2D

Berat 295.4
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Subcutaneous sumatriptan has a half life of 1.9h (95% CI of 1.7-2.0h).[A179737] Oral sumatriptan has a half life of 1.7h (95% CI of 1.4-1.9h).[A179737] Rectal sumatriptan has a half life of 1.8h (95% CI of 1.6-2.2h).[A179737] Intrsnasal sumatriptan has a half life of 1.8h (95% CI of 1.7-2.0h).[A179737]
Volume Distribusi Sumatriptan has a volume of distribution of 50±8L for a 6mg subcutaneous dose[L6799], or 2.7L/kg.[L6811]
Klirens (Clearance) Subcutaneous sumatriptan has a clearance of 0.22L/min (95% CI of 0.19-0.25L/min).[A179737] Oral sumatriptan has a clearance of 0.17L/min (95% CI of 0.14-0.21L/min).[A179737] Rectal sumatriptan has a clearance of 0.17L/min (95% CI of 0.14-0.21L/min).[A179737] Intrsnasal sumatriptan has a clearance of 0.21L/min (95% CI of 0.18-0.25L/min).[A179737] Total plasma clearance of sumatriptan is approximately 1200mL/min.[L6796]

Absorpsi

A 6mg subcutaneous injection of sumatriptan reaches a Cmax of 69.5ng/mL (95% CI of 62.8-76.9ng/mL) with a Tmax of 0.17h (95% CI of 0.08-0.33h), an AUC of 9.0h\*ng/mL (95% CI of 7.5-10.9h\*ng/mL), and a bioavailability of 100%.A179737 A 25mg oral dose of sumatriptan reaches a Cmax of 16.5ng/mL (95% CI of 13.5-20.1ng/mL) with a Tmax of 1.50h (95% CI of 0.50-2.00h), an AUC of 8.7h\*ng/mL (95% CI of 6.1-12.5h\*ng/mL), and a bioavailability of 14.3% (95% CI of 11.4-17.9%).A179737 A 20mg intranasal dose of sumatriptan reaches a Cmax of 12.9ng/mL (95% CI of 10.5-15.9ng/mL) with a Tmax of 1.50h (95% CI of 0.25-3.00h), an AUC of 7.4h\*ng/mL (95% CI of 5.0-10.8h\*ng/mL), and a bioavailability of 15.8% (95% CI of 12.6-19.8%).A179737 A 25mg rectal dose of sumatriptan reaches a Cmax of 22.9ng/mL (95% CI of 18.4-28.6ng/mL) with a Tmax of 1.00h (95% CI of 0.75-3.00h), an AUC of 14.6h\*ng/mL (95% CI of 11.3-18.8h\*ng/mL), and a bioavailability of 19.2% (95% CI of 15.3-24.1%).A179737

Metabolisme

Sumatriptan is predominantly metabolized by monoamine oxidase AL6799,L6811,L6805,L6811,L6793,L6808. The main metabolites are the inactive indole acetic acid and indole acetic acid glucuronide.L6799,L6811,L6805,L6811,L6793,L6808

Rute Eliminasi

22±4% is excreted in the urine as unchanged sumatriptan and 38±7% in urine as indole acetic acidL6799,L6805 approximately 40% is excreted in the fecesL6811,L6793.

Farmakogenomik

1 Varian
GNB3 (rs5443)

Patients with this genotype have an increased likelihood of responding to sumatriptan when treating (condition: cluster headache).

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Alcohol increased the risk of GI bleeding, ulcer, and perforation when taken with sumatriptan.
  • 2. Take with or without food.

Interaksi Obat

1769 Data
Ramipril Sumatriptan may decrease the antihypertensive activities of Ramipril.
Esmolol Sumatriptan may decrease the antihypertensive activities of Esmolol.
Betaxolol Sumatriptan may decrease the antihypertensive activities of Betaxolol.
Remikiren Sumatriptan may decrease the antihypertensive activities of Remikiren.
Guanadrel Sumatriptan may decrease the antihypertensive activities of Guanadrel.
Olmesartan Sumatriptan may decrease the antihypertensive activities of Olmesartan.
Atenolol Sumatriptan may decrease the antihypertensive activities of Atenolol.
Minoxidil Sumatriptan may decrease the antihypertensive activities of Minoxidil.
Treprostinil Sumatriptan may decrease the antihypertensive activities of Treprostinil.
Trandolapril Sumatriptan may decrease the antihypertensive activities of Trandolapril.
Lercanidipine Sumatriptan may decrease the antihypertensive activities of Lercanidipine.
Benazepril Sumatriptan may decrease the antihypertensive activities of Benazepril.
Bosentan Sumatriptan may decrease the antihypertensive activities of Bosentan.
Candoxatril Sumatriptan may decrease the antihypertensive activities of Candoxatril.
Moexipril Sumatriptan may decrease the antihypertensive activities of Moexipril.
Nitroglycerin Sumatriptan may decrease the antihypertensive activities of Nitroglycerin.
Cryptenamine Sumatriptan may decrease the antihypertensive activities of Cryptenamine.
Eprosartan Sumatriptan may decrease the antihypertensive activities of Eprosartan.
Quinapril Sumatriptan may decrease the antihypertensive activities of Quinapril.
Irbesartan Sumatriptan may decrease the antihypertensive activities of Irbesartan.
Deserpidine Sumatriptan may decrease the antihypertensive activities of Deserpidine.
Bretylium Sumatriptan may decrease the antihypertensive activities of Bretylium.
Bevantolol Sumatriptan may decrease the antihypertensive activities of Bevantolol.
Practolol Sumatriptan may decrease the antihypertensive activities of Practolol.
Saprisartan Sumatriptan may decrease the antihypertensive activities of Saprisartan.
Spirapril Sumatriptan may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Sumatriptan may decrease the antihypertensive activities of Dexpropranolol.
Nebivolol Sumatriptan may decrease the antihypertensive activities of Nebivolol.
Sitaxentan Sumatriptan may decrease the antihypertensive activities of Sitaxentan.
Diethylnorspermine Sumatriptan may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Sumatriptan may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Sumatriptan may decrease the antihypertensive activities of Pinacidil.
Bupranolol Sumatriptan may decrease the antihypertensive activities of Bupranolol.
Temocapril Sumatriptan may decrease the antihypertensive activities of Temocapril.
Riociguat Sumatriptan may decrease the antihypertensive activities of Riociguat.
Indenolol Sumatriptan may decrease the antihypertensive activities of Indenolol.
Aliskiren Sumatriptan may decrease the antihypertensive activities of Aliskiren.
Trimazosin Sumatriptan may decrease the antihypertensive activities of Trimazosin.
Lacidipine Sumatriptan may decrease the antihypertensive activities of Lacidipine.
Manidipine Sumatriptan may decrease the antihypertensive activities of Manidipine.
Rauwolfia serpentina root Sumatriptan may decrease the antihypertensive activities of Rauwolfia serpentina root.
Angiotensin 1-7 Sumatriptan may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Sumatriptan may decrease the antihypertensive activities of Imidapril.
BQ-123 Sumatriptan may decrease the antihypertensive activities of BQ-123.
Landiolol Sumatriptan may decrease the antihypertensive activities of Landiolol.
Dihydralazine Sumatriptan may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Sumatriptan may decrease the antihypertensive activities of Zofenopril.
Guanoxan Sumatriptan may decrease the antihypertensive activities of Guanoxan.
Delapril Sumatriptan may decrease the antihypertensive activities of Delapril.
Vincamine Sumatriptan may decrease the antihypertensive activities of Vincamine.
Linsidomine Sumatriptan may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Sumatriptan may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Sumatriptan may decrease the antihypertensive activities of Tolonidine.
Endralazine Sumatriptan may decrease the antihypertensive activities of Endralazine.
Esatenolol Sumatriptan may decrease the antihypertensive activities of Esatenolol.
Cadralazine Sumatriptan may decrease the antihypertensive activities of Cadralazine.
Cloranolol Sumatriptan may decrease the antihypertensive activities of Cloranolol.
Bietaserpine Sumatriptan may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Sumatriptan may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Sumatriptan may decrease the antihypertensive activities of Methoserpidine.
Epanolol Sumatriptan may decrease the antihypertensive activities of Epanolol.
Guanoclor Sumatriptan may decrease the antihypertensive activities of Guanoclor.
Tocopherylquinone Sumatriptan may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Sumatriptan may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Sumatriptan may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Sumatriptan may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Sumatriptan may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Sumatriptan may decrease the antihypertensive activities of Quinaprilat.
Diltiazem Sumatriptan may decrease the antihypertensive activities of Diltiazem.
Amlodipine Sumatriptan may decrease the antihypertensive activities of Amlodipine.
Nimodipine Sumatriptan may decrease the antihypertensive activities of Nimodipine.
Prazosin Sumatriptan may decrease the antihypertensive activities of Prazosin.
Enalapril Sumatriptan may decrease the antihypertensive activities of Enalapril.
Doxazosin Sumatriptan may decrease the antihypertensive activities of Doxazosin.
Losartan Sumatriptan may decrease the antihypertensive activities of Losartan.
Candesartan cilexetil Sumatriptan may decrease the antihypertensive activities of Candesartan cilexetil.
Felodipine Sumatriptan may decrease the antihypertensive activities of Felodipine.
Nitrendipine Sumatriptan may decrease the antihypertensive activities of Nitrendipine.
Carvedilol Sumatriptan may decrease the antihypertensive activities of Carvedilol.
Terazosin Sumatriptan may decrease the antihypertensive activities of Terazosin.
Acebutolol Sumatriptan may decrease the antihypertensive activities of Acebutolol.
Captopril Sumatriptan may decrease the antihypertensive activities of Captopril.
Bepridil Sumatriptan may decrease the antihypertensive activities of Bepridil.
Cilazapril Sumatriptan may decrease the antihypertensive activities of Cilazapril.
Mibefradil Sumatriptan may decrease the antihypertensive activities of Mibefradil.
Debrisoquine Sumatriptan may decrease the antihypertensive activities of Debrisoquine.
Celiprolol Sumatriptan may decrease the antihypertensive activities of Celiprolol.
Ambrisentan Sumatriptan may decrease the antihypertensive activities of Ambrisentan.
Niguldipine Sumatriptan may decrease the antihypertensive activities of Niguldipine.
Selexipag Sumatriptan may decrease the antihypertensive activities of Selexipag.
Talinolol Sumatriptan may decrease the antihypertensive activities of Talinolol.
Dexniguldipine Sumatriptan may decrease the antihypertensive activities of Dexniguldipine.
Levamlodipine Sumatriptan may decrease the antihypertensive activities of Levamlodipine.
Azilsartan medoxomil Sumatriptan may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Sumatriptan may decrease the antihypertensive activities of Diazoxide.
Buprenorphine Sumatriptan may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Sumatriptan.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Sumatriptan.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Sumatriptan.
Hydrocodone Sumatriptan may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.

Target Protein

5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 1D HTR1D
5-hydroxytryptamine receptor 1B HTR1B
5-hydroxytryptamine receptor 1F HTR1F

Referensi & Sumber

Synthesis reference: Rajeev Mathur, T. Kumar, Sunilendu Roy, Rajiv Malik, "Taste masked sumatriptan tablets and processes for their preparation." U.S. Patent US20060233875, issued October 19, 2006.
Artikel (PubMed)
  • PMID: 18723285
    Nikai T, Basbaum AI, Ahn AH: Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008 Oct 31;139(3):533-40. doi: 10.1016/j.pain.2008.06.002. Epub 2008 Aug 23.
  • PMID: 1320526
    Ferrari MD, Saxena PR: Clinical effects and mechanism of action of sumatriptan in migraine. Clin Neurol Neurosurg. 1992;94 Suppl:S73-7.
  • PMID: 9795022
    Duquesnoy C, Mamet JP, Sumner D, Fuseau E: Comparative clinical pharmacokinetics of single doses of sumatriptan following subcutaneous, oral, rectal and intranasal administration. Eur J Pharm Sci. 1998 Apr;6(2):99-104.
  • PMID: 18471110
    Humphrey PP: The discovery and development of the triptans, a major therapeutic breakthrough. Headache. 2008 May;48(5):685-7. doi: 10.1111/j.1526-4610.2008.01097.x.

Contoh Produk & Brand

Produk: 362 • International brands: 21
Produk
  • Act Sumatriptan
    Tablet • 25 mg • Oral • Canada • Approved
  • Act Sumatriptan
    Tablet • 50 mg • Oral • Canada • Approved
  • Act Sumatriptan
    Tablet • 100 mg • Oral • Canada • Approved
  • Ag-sumatriptan
    Tablet • 25 mg • Oral • Canada • Generic • Approved
  • Ag-sumatriptan
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Ag-sumatriptan
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Alsuma
    Injection, solution • 6 mg/0.5mL • Subcutaneous • US • Approved
  • Alsuma
    Injection, solution • 6 mg/0.5mL • Subcutaneous • US • Approved
Menampilkan 8 dari 362 produk.
International Brands
  • Adracon — Inti
  • Altaxa — Alapis Pharma
  • Apigrane — Advanced Pharmaceutical
  • Boots Pharmacy Migraine Relief — Boots
  • Cinie — Zentiva
  • Frimig — Orion
  • Illument — Pliva
  • Imigen — Mylan
  • Imigran — GlaxoSmithKline
  • Imigran mite — GlaxoSmithKline

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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