Peringatan Keamanan

The acute oral toxicity (LD50) was 2,227 mg/kg in rats and 700-1,631 mg/kg in mice.L46028

No overdoses of rizatriptan were reported in clinical trials. Some adult patients who received 40 mg of rizatriptan either a single dose or as two doses with a two-hour interdose interval had dizziness and somnolence. Syncope, dizziness, bradycardia including third degree AV block, vomiting, and/or incontinence were experienced by two adults who received a total cumulative doses of 80 mg (given within four hours) in a clinical pharmacology study. Some adolescent patients (aged 12 to 17 years old) receiving two 10-mg doses of orally disintegrating tablets of rizatriptan experienced abdominal discomfort, fatigue, and dyspnea.L46018

Based on the pharmacological properties of rizatriptan, hypertension and myocardial ischemia are possible after overdosage. Gastrointestinal decontamination, (i.e., gastric lavage followed by activated charcoal) should be considered in patients suspected of an overdose with rizatriptan. Clinical and electrocardiographic monitoring should be continued for at least 12 hours, even if clinical symptoms are not observed. The effects of hemo- or peritoneal dialysis on serum concentrations of rizatriptan are unknown.L46018

Rizatriptan

DB00953

small molecule approved

Deskripsi

Rizatriptan is a second-generation triptan A258918 and a selective 5-HT1B and 5-HT1D receptor agonist.L46018 Used in the treatment of migraines, rizatriptan was first approved in the US in 1998.L46018 Rizatriptan is available in oral tablets, orally disintegrating tablets (wafers), and oral film formulations.

Struktur Molekul 2D

Berat 269.3449
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma half-life of rizatriptan in males and females ranges from two to three hours.[L46018]
Volume Distribusi The mean volume of distribution is approximately 140 L in male subjects and 110 L in female subjects.[L46018]
Klirens (Clearance) An early study involving healthy subject reported plasma clearance of 1042 mL/min in males and 821 mL/min in females; however, this difference in clearance rates is not thought to be clinically relevant.[A258918, A258923]

Absorpsi

Rizatriptan is readily absorbed (approximately 90%) following oral administration;A1460 however, the mean oral absolute bioavailability of the rizatriptan tablet is about 45%, owing to extensive first-pass metabolism. The Tmax is approximately one to 1.5 hours. The presence of a migraine headache did not appear to affect the absorption or pharmacokinetics of rizatriptan. Food has no significant effect on the bioavailability of rizatriptan but delays the time to reach peak concentration by an hour. In clinical trials, rizatriptan was administered without regard to food.L46018 The bioavailability and Cmax of rizatriptan were similar following the administration of rizatriptan tablets and rizatriptan orally disintegrating tablets. Still, the absorption rate is somewhat slower with orally disintegrating tablets, with Tmax delayed by up to 0.7 hours. The AUC of rizatriptan is approximately 30% higher in females than males. No accumulation occurred on multiple dosing.L46018

Metabolisme

Rizatriptan primarily undergoes oxidative deamination mediated by monoamine oxidase-A (MAO-A) to form triazolomethyl-indole-3-acetic acid, which is not pharmacologically active. N-monodesmethyl-rizatriptan is a minor metabolite with a pharmacological activity comparable to the parent compound's. Plasma concentrations of N-monodesmethyl-rizatriptan are approximately 14% of those of the parent compound, which is eliminated at a similar rate. Other pharmacologically inactive minor metabolites include the N-oxide, the 6-hydroxy compound, and the sulfate conjugate of the 6-hydroxy metabolite.A1460, A258963, L46018

Rute Eliminasi

Following oral administration of a single 10 mg of 14C-rizatriptan, the total radioactivity of the administered dose recovered over 120 hours in urine and feces was 82% and 12%, respectively. Following oral administration of 14C-rizatriptan, rizatriptan accounted for about 17% of circulating plasma radioactivity. Approximately 14% of an oral dose is excreted in urine as unchanged rizatriptan, while 51% is excreted as indole acetic acid metabolite, indicating substantial first-pass metabolism.L46018

Farmakogenomik

1 Varian
GNB3 (rs5443)

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

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food has no significant effect on the bioavailability of rizatriptan but delays the time to reach peak concentration by an hour.

Interaksi Obat

1220 Data
Valsartan Rizatriptan may decrease the antihypertensive activities of Valsartan.
Ramipril Rizatriptan may decrease the antihypertensive activities of Ramipril.
Esmolol Rizatriptan may decrease the antihypertensive activities of Esmolol.
Betaxolol Rizatriptan may decrease the antihypertensive activities of Betaxolol.
Remikiren Rizatriptan may decrease the antihypertensive activities of Remikiren.
Guanadrel Rizatriptan may decrease the antihypertensive activities of Guanadrel.
Olmesartan Rizatriptan may decrease the antihypertensive activities of Olmesartan.
Atenolol Rizatriptan may decrease the antihypertensive activities of Atenolol.
Diltiazem Rizatriptan may decrease the antihypertensive activities of Diltiazem.
Minoxidil Rizatriptan may decrease the antihypertensive activities of Minoxidil.
Treprostinil Rizatriptan may decrease the antihypertensive activities of Treprostinil.
Amlodipine Rizatriptan may decrease the antihypertensive activities of Amlodipine.
Nimodipine Rizatriptan may decrease the antihypertensive activities of Nimodipine.
Prazosin Rizatriptan may decrease the antihypertensive activities of Prazosin.
Trandolapril Rizatriptan may decrease the antihypertensive activities of Trandolapril.
Lercanidipine Rizatriptan may decrease the antihypertensive activities of Lercanidipine.
Benazepril Rizatriptan may decrease the antihypertensive activities of Benazepril.
Bosentan Rizatriptan may decrease the antihypertensive activities of Bosentan.
Enalapril Rizatriptan may decrease the antihypertensive activities of Enalapril.
Doxazosin Rizatriptan may decrease the antihypertensive activities of Doxazosin.
Candoxatril Rizatriptan may decrease the antihypertensive activities of Candoxatril.
Losartan Rizatriptan may decrease the antihypertensive activities of Losartan.
Moexipril Rizatriptan may decrease the antihypertensive activities of Moexipril.
Nitroglycerin Rizatriptan may decrease the antihypertensive activities of Nitroglycerin.
Cryptenamine Rizatriptan may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil Rizatriptan may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Rizatriptan may decrease the antihypertensive activities of Eprosartan.
Quinapril Rizatriptan may decrease the antihypertensive activities of Quinapril.
Telmisartan Rizatriptan may decrease the antihypertensive activities of Telmisartan.
Felodipine Rizatriptan may decrease the antihypertensive activities of Felodipine.
Irbesartan Rizatriptan may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Rizatriptan may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Rizatriptan may decrease the antihypertensive activities of Deserpidine.
Pentolinium Rizatriptan may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Rizatriptan may decrease the antihypertensive activities of Trimethaphan.
Carvedilol Rizatriptan may decrease the antihypertensive activities of Carvedilol.
Bretylium Rizatriptan may decrease the antihypertensive activities of Bretylium.
Terazosin Rizatriptan may decrease the antihypertensive activities of Terazosin.
Acebutolol Rizatriptan may decrease the antihypertensive activities of Acebutolol.
Captopril Rizatriptan may decrease the antihypertensive activities of Captopril.
Bepridil Rizatriptan may decrease the antihypertensive activities of Bepridil.
Bevantolol Rizatriptan may decrease the antihypertensive activities of Bevantolol.
Practolol Rizatriptan may decrease the antihypertensive activities of Practolol.
Cilazapril Rizatriptan may decrease the antihypertensive activities of Cilazapril.
Saprisartan Rizatriptan may decrease the antihypertensive activities of Saprisartan.
Spirapril Rizatriptan may decrease the antihypertensive activities of Spirapril.
Mibefradil Rizatriptan may decrease the antihypertensive activities of Mibefradil.
Dexpropranolol Rizatriptan may decrease the antihypertensive activities of Dexpropranolol.
Debrisoquine Rizatriptan may decrease the antihypertensive activities of Debrisoquine.
Celiprolol Rizatriptan may decrease the antihypertensive activities of Celiprolol.
Nebivolol Rizatriptan may decrease the antihypertensive activities of Nebivolol.
Sitaxentan Rizatriptan may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Rizatriptan may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Rizatriptan may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Rizatriptan may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Rizatriptan may decrease the antihypertensive activities of Pinacidil.
Bupranolol Rizatriptan may decrease the antihypertensive activities of Bupranolol.
Temocapril Rizatriptan may decrease the antihypertensive activities of Temocapril.
Riociguat Rizatriptan may decrease the antihypertensive activities of Riociguat.
Indenolol Rizatriptan may decrease the antihypertensive activities of Indenolol.
Aliskiren Rizatriptan may decrease the antihypertensive activities of Aliskiren.
Trimazosin Rizatriptan may decrease the antihypertensive activities of Trimazosin.
Lacidipine Rizatriptan may decrease the antihypertensive activities of Lacidipine.
Manidipine Rizatriptan may decrease the antihypertensive activities of Manidipine.
Niguldipine Rizatriptan may decrease the antihypertensive activities of Niguldipine.
Rauwolfia serpentina root Rizatriptan may decrease the antihypertensive activities of Rauwolfia serpentina root.
Selexipag Rizatriptan may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Rizatriptan may decrease the antihypertensive activities of Angiotensin 1-7.
Talinolol Rizatriptan may decrease the antihypertensive activities of Talinolol.
Imidapril Rizatriptan may decrease the antihypertensive activities of Imidapril.
BQ-123 Rizatriptan may decrease the antihypertensive activities of BQ-123.
Landiolol Rizatriptan may decrease the antihypertensive activities of Landiolol.
Dihydralazine Rizatriptan may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Rizatriptan may decrease the antihypertensive activities of Zofenopril.
Guanoxan Rizatriptan may decrease the antihypertensive activities of Guanoxan.
Delapril Rizatriptan may decrease the antihypertensive activities of Delapril.
Vincamine Rizatriptan may decrease the antihypertensive activities of Vincamine.
Linsidomine Rizatriptan may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Rizatriptan may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Rizatriptan may decrease the antihypertensive activities of Tolonidine.
Endralazine Rizatriptan may decrease the antihypertensive activities of Endralazine.
Esatenolol Rizatriptan may decrease the antihypertensive activities of Esatenolol.
Cadralazine Rizatriptan may decrease the antihypertensive activities of Cadralazine.
Cloranolol Rizatriptan may decrease the antihypertensive activities of Cloranolol.
Bietaserpine Rizatriptan may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Rizatriptan may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Rizatriptan may decrease the antihypertensive activities of Methoserpidine.
Epanolol Rizatriptan may decrease the antihypertensive activities of Epanolol.
Guanoclor Rizatriptan may decrease the antihypertensive activities of Guanoclor.
Candesartan Rizatriptan may decrease the antihypertensive activities of Candesartan.
Dexniguldipine Rizatriptan may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone Rizatriptan may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Rizatriptan may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Rizatriptan may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Rizatriptan may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Rizatriptan may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Rizatriptan may decrease the antihypertensive activities of Quinaprilat.
Levamlodipine Rizatriptan may decrease the antihypertensive activities of Levamlodipine.
Azilsartan medoxomil Rizatriptan may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Rizatriptan may decrease the antihypertensive activities of Diazoxide.

Target Protein

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

Referensi & Sumber

Synthesis reference: Montserrat Armengol Asparo, Pere Dalmases Barjoan, "Process for preparing a rizatriptan." U.S. Patent US20050148778, issued July 07, 2005.
Artikel (PubMed)
  • PMID: 12093318
    Wellington K, Plosker GL: Rizatriptan: an update of its use in the management of migraine. Drugs. 2002;62(10):1539-74.
  • PMID: 11152011
    Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87.
  • PMID: 19412472
    Lainez MJ: Rizatriptan in the treatment of migraine. Neuropsychiatr Dis Treat. 2006 Sep;2(3):247-59. doi: 10.2147/nedt.2006.2.3.247.
  • PMID: 10233200
    Lee Y, Conroy JA, Stepanavage ME, Mendel CM, Somers G, McLoughlin DA, Olah TV, De Smet M, Keymeulen B, Rogers JD: Pharmacokinetics and tolerability of oral rizatriptan in healthy male and female volunteers. Br J Clin Pharmacol. 1999 Apr;47(4):373-8. doi: 10.1046/j.1365-2125.1999.00917.x.
  • PMID: 32119394
    Nicolas S, Nicolas D: Triptans. .
  • PMID: 10611145
    Vyas KP, Halpin RA, Geer LA, Ellis JD, Liu L, Cheng H, Chavez-Eng C, Matuszewski BK, Varga SL, Guiblin AR, Rogers JD: Disposition and pharmacokinetics of the antimigraine drug, rizatriptan, in humans. Drug Metab Dispos. 2000 Jan;28(1):89-95.
  • PMID: 11487512
    Williamson DJ, Hill RG, Shepheard SL, Hargreaves RJ: The anti-migraine 5-HT(1B/1D) agonist rizatriptan inhibits neurogenic dural vasodilation in anaesthetized guinea-pigs. Br J Pharmacol. 2001 Aug;133(7):1029-34.
  • PMID: 27013238
    Deen M, Christensen CE, Hougaard A, Hansen HD, Knudsen GM, Ashina M: Serotonergic mechanisms in the migraine brain - a systematic review. Cephalalgia. 2017 Mar;37(3):251-264. doi: 10.1177/0333102416640501. Epub 2016 Jul 11.

Contoh Produk & Brand

Produk: 222 • International brands: 2
Produk
  • Accel-rizatriptan ODT
    Tablet, orally disintegrating • 5 mg • Oral • Canada • Generic • Approved
  • Accel-rizatriptan ODT
    Tablet, orally disintegrating • 10 mg • Oral • Canada • Generic • Approved
  • Act Rizatriptan
    Tablet • 10 mg • Oral • Canada • Approved
  • Act Rizatriptan
    Tablet • 5 mg • Oral • Canada • Approved
  • Act Rizatriptan ODT
    Tablet, orally disintegrating • 5 mg • Oral • Canada • Approved
  • Act Rizatriptan ODT
    Tablet, orally disintegrating • 10 mg • Oral • Canada • Approved
  • Ag-rizatriptan ODT
    Tablet, orally disintegrating • 5 mg • Oral • Canada • Generic • Approved
  • Ag-rizatriptan ODT
    Tablet, orally disintegrating • 10 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 222 produk.
International Brands
  • Maxalt MLT
  • RizaFilm

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