Peringatan Keamanan

Toxicity information regarding zolmitriptan is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as cardiovascular symptoms due to excessive vasoconstriction and activation of serotonergic receptors. Patients receiving a single 50 mg oral dose of zolmitriptan often experienced sedation. Symptomatic and supportive measures are recommended.L12978

Zolmitriptan

DB00315

small molecule approved investigational

Deskripsi

Zolmitriptan is a member of the triptan class of 5-hydroxytryptamine(5-HT)1B/1D/(1F) receptor agonists used to treat acute migraine.A462, L12978 Sumatriptan was the first triptan to be developed, but had poor oral bioavailability and lipophilicity. This led to the development of second-generation triptans, including almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, and zolmitriptan.A193791 Triptans can be administered alone or in combination with an NSAID like naproxen, and represent the current "gold standard" for acute migraine treatment.A193797

Zolmitriptan was first approved by the FDA for sale by Zeneca Pharmaceuticals under the trade name Zomig® on November 25, 1997. It is currently available in both tablet and nasal spray forms.L12978

Struktur Molekul 2D

Berat 287.3568
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Zolmitriptan has a mean elimination half-life of approximately three hours following oral or nasal administration. Its active N-desmethyl metabolite has a slightly longer (approximately 3.5 hours) half-life.[L12978, A198759]
Volume Distribusi Zolmitriptan has a volume of distribution between 7 and 8.4 L/kg.[L12978]
Klirens (Clearance) Zolmitriptan has a clearance of 31.5 mL/min/kg for oral tablets and 25.9 mL/min/kg for nasal administration; one-sixth of the clearance is renal.[L12978]

Absorpsi

Zolmitriptan tablets have a mean absolute oral bioavailability of approximately 40%, with food having no effect on the rate or extent of absorption.A462,A198747,L12978 The dosing kinetics are linear over a range of 2.5 to 50 mg with 75% of the eventual Cmax being attained within 1 hour of dosing. The median Tmax for the tablet form is 1.5 hours, while for the orally disintegrating tablet form, it is 3 hours.A198747, L12978 The AUC across studies was in the range of 84.4-173.8 ng/mL*h while the Cmax was between 16 and 25.2 ng/mL.A198747, A198759 Zolmitriptan administered as a nasal spray is detected in the plasma within 2-5 minutes, compared to 10-15 minutes for the tablet form; the faster kinetics likely reflect fast absorption across the nasal mucosa.A198756 The bioavailability compared to the tablet is 102%, and plasma zolmitriptan concentration is maintained for 4-6 hours after intranasal delivery.A198756, L12978 The active N-desmethyl metabolite of zolmitriptan has a mean plasma concentration that is roughly two-thirds of zolmitriptan, regardless of dosage route or concentration.A198747, L12978

Metabolisme

Zolmitriptan is metabolized in the liver, and studies using cytochrome P450 inhibitors like cimetidine suggest that it is likely metabolized by CYP1A2, as well as by monoamine oxidase (MAO).L12978, A37743, A15027 Zolmitriptan metabolism results in three major metabolites: an active N-desmethyl metabolite (183C91) as well as inactive N-oxide (1652W92) and indole acetic acid (2161W92) metabolites.L12978, A198759, A198747

Rute Eliminasi

Zolmitriptan is primarily excreted in urine (approximately 65%) and feces (approximately 30%). Within urine, the most common form is the indole acetic acid metabolite (31%), followed by the N-oxide (7%), and N-desmethyl (4%) metabolites; the majority of zolmitriptan recovered in feces remains unchanged.L12978, A198759

Farmakogenomik

1 Varian
GNB3 (rs5443)

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

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food does not significantly impact the oral bioavalibility of zolmitriptan.

Interaksi Obat

1304 Data
Leflunomide The serum concentration of Zolmitriptan can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Zolmitriptan can be decreased when it is combined with Teriflunomide.
Valsartan Zolmitriptan may decrease the antihypertensive activities of Valsartan.
Ramipril Zolmitriptan may decrease the antihypertensive activities of Ramipril.
Esmolol Zolmitriptan may decrease the antihypertensive activities of Esmolol.
Remikiren Zolmitriptan may decrease the antihypertensive activities of Remikiren.
Torasemide Zolmitriptan may decrease the antihypertensive activities of Torasemide.
Guanadrel Zolmitriptan may decrease the antihypertensive activities of Guanadrel.
Metoprolol Zolmitriptan may decrease the antihypertensive activities of Metoprolol.
Isradipine Zolmitriptan may decrease the antihypertensive activities of Isradipine.
Olmesartan Zolmitriptan may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Zolmitriptan may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Zolmitriptan may decrease the antihypertensive activities of Nitroprusside.
Atenolol Zolmitriptan may decrease the antihypertensive activities of Atenolol.
Diltiazem Zolmitriptan may decrease the antihypertensive activities of Diltiazem.
Minoxidil Zolmitriptan may decrease the antihypertensive activities of Minoxidil.
Timolol Zolmitriptan may decrease the antihypertensive activities of Timolol.
Treprostinil Zolmitriptan may decrease the antihypertensive activities of Treprostinil.
Amlodipine Zolmitriptan may decrease the antihypertensive activities of Amlodipine.
Nimodipine Zolmitriptan may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Zolmitriptan may decrease the antihypertensive activities of Nisoldipine.
Bendroflumethiazide Zolmitriptan may decrease the antihypertensive activities of Bendroflumethiazide.
Prazosin Zolmitriptan may decrease the antihypertensive activities of Prazosin.
Fosinopril Zolmitriptan may decrease the antihypertensive activities of Fosinopril.
Trandolapril Zolmitriptan may decrease the antihypertensive activities of Trandolapril.
Metolazone Zolmitriptan may decrease the antihypertensive activities of Metolazone.
Lercanidipine Zolmitriptan may decrease the antihypertensive activities of Lercanidipine.
Benazepril Zolmitriptan may decrease the antihypertensive activities of Benazepril.
Bosentan Zolmitriptan may decrease the antihypertensive activities of Bosentan.
Enalapril Zolmitriptan may decrease the antihypertensive activities of Enalapril.
Doxazosin Zolmitriptan may decrease the antihypertensive activities of Doxazosin.
Labetalol Zolmitriptan may decrease the antihypertensive activities of Labetalol.
Cyclothiazide Zolmitriptan may decrease the antihypertensive activities of Cyclothiazide.
Bisoprolol Zolmitriptan may decrease the antihypertensive activities of Bisoprolol.
Candoxatril Zolmitriptan may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Zolmitriptan may decrease the antihypertensive activities of Mecamylamine.
Losartan Zolmitriptan may decrease the antihypertensive activities of Losartan.
Moexipril Zolmitriptan may decrease the antihypertensive activities of Moexipril.
Eplerenone Zolmitriptan may decrease the antihypertensive activities of Eplerenone.
Lisinopril Zolmitriptan may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Zolmitriptan may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Zolmitriptan may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Zolmitriptan may decrease the antihypertensive activities of Cryptenamine.
Perindopril Zolmitriptan may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Zolmitriptan may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Zolmitriptan may decrease the antihypertensive activities of Fenoldopam.
Indapamide Zolmitriptan may decrease the antihypertensive activities of Indapamide.
Tadalafil Zolmitriptan may decrease the antihypertensive activities of Tadalafil.
Eprosartan Zolmitriptan may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Zolmitriptan may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Zolmitriptan may decrease the antihypertensive activities of Quinapril.
Telmisartan Zolmitriptan may decrease the antihypertensive activities of Telmisartan.
Methyldopa Zolmitriptan may decrease the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Zolmitriptan may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Zolmitriptan may decrease the antihypertensive activities of Trichlormethiazide.
Felodipine Zolmitriptan may decrease the antihypertensive activities of Felodipine.
Irbesartan Zolmitriptan may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Zolmitriptan may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Zolmitriptan may decrease the antihypertensive activities of Deserpidine.
Pentolinium Zolmitriptan may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Zolmitriptan may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Zolmitriptan may decrease the antihypertensive activities of Diazoxide.
Bretylium Zolmitriptan may decrease the antihypertensive activities of Bretylium.
Terazosin Zolmitriptan may decrease the antihypertensive activities of Terazosin.
Guanethidine Zolmitriptan may decrease the antihypertensive activities of Guanethidine.
Acebutolol Zolmitriptan may decrease the antihypertensive activities of Acebutolol.
Captopril Zolmitriptan may decrease the antihypertensive activities of Captopril.
Nadolol Zolmitriptan may decrease the antihypertensive activities of Nadolol.
Epoprostenol Zolmitriptan may decrease the antihypertensive activities of Epoprostenol.
Bepridil Zolmitriptan may decrease the antihypertensive activities of Bepridil.
Hydralazine Zolmitriptan may decrease the antihypertensive activities of Hydralazine.
Bevantolol Zolmitriptan may decrease the antihypertensive activities of Bevantolol.
Practolol Zolmitriptan may decrease the antihypertensive activities of Practolol.
Polythiazide Zolmitriptan may decrease the antihypertensive activities of Polythiazide.
Cilazapril Zolmitriptan may decrease the antihypertensive activities of Cilazapril.
Saprisartan Zolmitriptan may decrease the antihypertensive activities of Saprisartan.
Spirapril Zolmitriptan may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Zolmitriptan may decrease the antihypertensive activities of Dexpropranolol.
Tienilic acid Zolmitriptan may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Zolmitriptan may decrease the antihypertensive activities of Debrisoquine.
Celiprolol Zolmitriptan may decrease the antihypertensive activities of Celiprolol.
Nebivolol Zolmitriptan may decrease the antihypertensive activities of Nebivolol.
Sitaxentan Zolmitriptan may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Zolmitriptan may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Zolmitriptan may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Zolmitriptan may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Zolmitriptan may decrease the antihypertensive activities of Pinacidil.
Bupranolol Zolmitriptan may decrease the antihypertensive activities of Bupranolol.
Temocapril Zolmitriptan may decrease the antihypertensive activities of Temocapril.
Riociguat Zolmitriptan may decrease the antihypertensive activities of Riociguat.
Macitentan Zolmitriptan may decrease the antihypertensive activities of Macitentan.
Indenolol Zolmitriptan may decrease the antihypertensive activities of Indenolol.
Aliskiren Zolmitriptan may decrease the antihypertensive activities of Aliskiren.
Trimazosin Zolmitriptan may decrease the antihypertensive activities of Trimazosin.
Nicorandil Zolmitriptan may decrease the antihypertensive activities of Nicorandil.
Efonidipine Zolmitriptan may decrease the antihypertensive activities of Efonidipine.
Lacidipine Zolmitriptan may decrease the antihypertensive activities of Lacidipine.
Manidipine Zolmitriptan may decrease the antihypertensive activities of Manidipine.
Niguldipine Zolmitriptan may decrease the antihypertensive activities of Niguldipine.
Rauwolfia serpentina root Zolmitriptan may decrease the antihypertensive activities of Rauwolfia serpentina root.

Target Protein

5-hydroxytryptamine receptor 1B HTR1B
5-hydroxytryptamine receptor 1D HTR1D
5-hydroxytryptamine receptor 1F HTR1F
5-hydroxytryptamine receptor 1E HTR1E
5-hydroxytryptamine receptor 7 HTR7
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 2B HTR2B

Referensi & Sumber

Synthesis reference: Islam Aminul, Bhar Chandan, Katam Sahadev, "Process for preparing optically pure zolmitriptan." U.S. Patent US20050245585, issued November 03, 2005.
Artikel (PubMed)
  • PMID: 9399012
    Martin GR: Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine. Cephalalgia. 1997 Oct;17 Suppl 18:4-14.
  • PMID: 29352859
    Rubio-Beltran E, Labastida-Ramirez A, Villalon CM, MaassenVanDenBrink A: Is selective 5-HT1F receptor agonism an entity apart from that of the triptans in antimigraine therapy? Pharmacol Ther. 2018 Jun;186:88-97. doi: 10.1016/j.pharmthera.2018.01.005. Epub 2018 Jan 17.
  • PMID: 28179394
    Goadsby PJ, Holland PR, Martins-Oliveira M, Hoffmann J, Schankin C, Akerman S: Pathophysiology of Migraine: A Disorder of Sensory Processing. Physiol Rev. 2017 Apr;97(2):553-622. doi: 10.1152/physrev.00034.2015.
  • PMID: 25877672
    Becker WJ: Acute Migraine Treatment in Adults. Headache. 2015 Jun;55(6):778-93. doi: 10.1111/head.12550. Epub 2015 Apr 15.
  • PMID: 1646289
    Feniuk W, Humphrey PP, Perren MJ, Connor HE, Whalley ET: Rationale for the use of 5-HT1-like agonists in the treatment of migraine. J Neurol. 1991;238 Suppl 1:S57-61. doi: 10.1007/bf01642908.
  • PMID: 32192818
    Qubty W, Patniyot I: Migraine Pathophysiology. Pediatr Neurol. 2020 Feb 4. pii: S0887-8994(20)30048-5. doi: 10.1016/j.pediatrneurol.2019.12.014.
  • PMID: -
    Supronsinchai W, Hoffmans J, Akermann S, Goadsby PJ: KCl-induced repetitive cortical spreading depression inhibits trigeminal neuronal firing mediated by 5-HT1B/1D and opioid receptor J Headache Pain. 2013 Feb 21;14(Suppl 1):P69.
  • PMID: 9453271
    Longmore J, Shaw D, Smith D, Hopkins R, McAllister G, Pickard JD, Sirinathsinghji DJ, Butler AJ, Hill RG: Differential distribution of 5HT1D- and 5HT1B-immunoreactivity within the human trigemino-cerebrovascular system: implications for the discovery of new antimigraine drugs. Cephalalgia. 1997 Dec;17(8):833-42. doi: 10.1046/j.1468-2982.1997.1708833.x.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 146 • International brands: 8
Produk
  • Ag-zolmitriptan ODT
    Tablet, orally disintegrating • 2.5 mg • Oral • Canada • Generic • Approved
  • Apo-zolmitriptan
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Apo-zolmitriptan Rapid
    Tablet, orally disintegrating • 2.5 mg • Oral • Canada • Generic • Approved
  • Auro-zolmitriptan
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Bio-zolmitriptan
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Ccp-zolmitriptan
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Dom-zolmitriptan
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Dom-zolmitriptan ODT
    Tablet, orally disintegrating • 2.5 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 146 produk.
International Brands
  • AscoTop — AstraZeneca
  • Nomi — Square
  • Zipton
  • Zolmiles — Actavis
  • Zolmit — Beximco
  • Zomigon — AstraZeneca
  • Zomigoro — AstraZeneca
  • Zomitan — Incepta

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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