Peringatan Keamanan

Moxisylyte is very well accepted by the patients and it presents very few adverse effects. The side effects are usually related to a profound alpha blockade than to a toxic response.T45

Moxisylyte

DB09205

small molecule approved investigational

Deskripsi

Moxisylyte, denominated as thymoxamine in the UK, is a specific and orally active ?1-adrenergic antagonist.T45 According to the WHO, moxisylyte is approved since 1987T91 and in the same year, it acquired the denomination of orphan product by the FDA.L1172 This drug was developed by the Japanese company Fujirebio and also by the American company Iolab in the late 80s.

Struktur Molekul 2D

Berat 279.38
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of moxisylyte was of 1-2 hours.[L1174]
Volume Distribusi In preclinical trials, the volume of distribution presented for beagle dogs is in the range of 0.83-0.98 L/kg.[L1178]
Klirens (Clearance) In preclinical trials, the plasma clearance was of 7.17 ml min/kg for beagle dogs.[L1178]

Absorpsi

Moxisylyte is rapidly absorbed after oral administration.L1174 Its pharmacokinetic profile is linear in the dose range from 10 to 30 mg for the values of Cmax and AUC.A31647 After intravenous administration, the maximal plasma concentration was of 352.8 ng/ml with an AUC of 152.6 mcg h/L.A31650 In preclinical trials, the bioavailability was always presented in approximately 10%.L1178

Metabolisme

The pharmacokinetic profile of moxisylyte can make this drug to be considered as a prodrug as its biotransformation is very rapid. This drug gets rapidly hydrolyzed by pseudocholinesterase in plasma and tissues to give the major metabolite deacetyl-thymoxamine.A31647, L1178 This first metabolite is later demethylated by the cytochrome P450 monooxygenase system to form deacetyl-demethyl-thymoxamine.L1178 Both of this major metabolites are pharmacologically active. The pharmacokinetic studies with moxisylyte in urine and feces have shown the presence of 8 different metabolites, where two of them are highly polar and resistant to enzymatic hydrolysis. From this metabolites, it has been detected the sulfate and glucuronide conjugates of the major metabolites.A31641,A31647

Rute Eliminasi

The major elimination route of moxisylyte is via the kidneys.L1174 The complete elimination of all the metabolites by urine is of 75% when administered intravenously and 69% when administered orally.A31649 From the elimination profile, The specific ranges of the two major metabolites of moxisylyte in the urine are of 50% and 10% for desacetyl-thymoxamine and N-monodemethyl-desacetyl-thymoxamine respectively.A31648 The fecal elimination corresponded only to the 14% of the administered dose.L1178

Interaksi Obat

1139 Data
Valsartan Moxisylyte may decrease the antihypertensive activities of Valsartan.
Esmolol Moxisylyte may decrease the antihypertensive activities of Esmolol.
Betaxolol Moxisylyte may decrease the antihypertensive activities of Betaxolol.
Remikiren Moxisylyte may decrease the antihypertensive activities of Remikiren.
Guanadrel Moxisylyte may decrease the antihypertensive activities of Guanadrel.
Olmesartan Moxisylyte may decrease the antihypertensive activities of Olmesartan.
Atenolol Moxisylyte may decrease the antihypertensive activities of Atenolol.
Diltiazem Moxisylyte may decrease the antihypertensive activities of Diltiazem.
Minoxidil Moxisylyte may decrease the antihypertensive activities of Minoxidil.
Treprostinil Moxisylyte may decrease the antihypertensive activities of Treprostinil.
Amlodipine Moxisylyte may decrease the antihypertensive activities of Amlodipine.
Nimodipine Moxisylyte may decrease the antihypertensive activities of Nimodipine.
Prazosin Moxisylyte may decrease the antihypertensive activities of Prazosin.
Trandolapril Moxisylyte may decrease the antihypertensive activities of Trandolapril.
Lercanidipine Moxisylyte may decrease the antihypertensive activities of Lercanidipine.
Benazepril Moxisylyte may decrease the antihypertensive activities of Benazepril.
Bosentan Moxisylyte may decrease the antihypertensive activities of Bosentan.
Enalapril Moxisylyte may decrease the antihypertensive activities of Enalapril.
Doxazosin Moxisylyte may decrease the antihypertensive activities of Doxazosin.
Candoxatril Moxisylyte may decrease the antihypertensive activities of Candoxatril.
Nicardipine Moxisylyte may decrease the antihypertensive activities of Nicardipine.
Losartan Moxisylyte may decrease the antihypertensive activities of Losartan.
Moexipril Moxisylyte may decrease the antihypertensive activities of Moexipril.
Nitroglycerin Moxisylyte may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Moxisylyte may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Moxisylyte may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil Moxisylyte may decrease the antihypertensive activities of Candesartan cilexetil.
Alprenolol Moxisylyte may decrease the antihypertensive activities of Alprenolol.
Eprosartan Moxisylyte may decrease the antihypertensive activities of Eprosartan.
Quinapril Moxisylyte may decrease the antihypertensive activities of Quinapril.
Telmisartan Moxisylyte may decrease the antihypertensive activities of Telmisartan.
Felodipine Moxisylyte may decrease the antihypertensive activities of Felodipine.
Irbesartan Moxisylyte may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Moxisylyte may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Moxisylyte may decrease the antihypertensive activities of Deserpidine.
Pentolinium Moxisylyte may decrease the antihypertensive activities of Pentolinium.
Carvedilol Moxisylyte may decrease the antihypertensive activities of Carvedilol.
Bretylium Moxisylyte may decrease the antihypertensive activities of Bretylium.
Terazosin Moxisylyte may decrease the antihypertensive activities of Terazosin.
Acebutolol Moxisylyte may decrease the antihypertensive activities of Acebutolol.
Captopril Moxisylyte may decrease the antihypertensive activities of Captopril.
Bepridil Moxisylyte may decrease the antihypertensive activities of Bepridil.
Bevantolol Moxisylyte may decrease the antihypertensive activities of Bevantolol.
Practolol Moxisylyte may decrease the antihypertensive activities of Practolol.
Cilazapril Moxisylyte may decrease the antihypertensive activities of Cilazapril.
Saprisartan Moxisylyte may decrease the antihypertensive activities of Saprisartan.
Spirapril Moxisylyte may decrease the antihypertensive activities of Spirapril.
Mibefradil Moxisylyte may decrease the antihypertensive activities of Mibefradil.
Oxprenolol Moxisylyte may decrease the antihypertensive activities of Oxprenolol.
Dexpropranolol Moxisylyte may decrease the antihypertensive activities of Dexpropranolol.
Debrisoquine Moxisylyte may decrease the antihypertensive activities of Debrisoquine.
Celiprolol Moxisylyte may decrease the antihypertensive activities of Celiprolol.
Nebivolol Moxisylyte may decrease the antihypertensive activities of Nebivolol.
Sitaxentan Moxisylyte may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Moxisylyte may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Moxisylyte may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Moxisylyte may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Moxisylyte may decrease the antihypertensive activities of Pinacidil.
Bupranolol Moxisylyte may decrease the antihypertensive activities of Bupranolol.
Temocapril Moxisylyte may decrease the antihypertensive activities of Temocapril.
Riociguat Moxisylyte may decrease the antihypertensive activities of Riociguat.
Indenolol Moxisylyte may decrease the antihypertensive activities of Indenolol.
Hexamethonium Moxisylyte may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Moxisylyte may decrease the antihypertensive activities of Aliskiren.
Trimazosin Moxisylyte may decrease the antihypertensive activities of Trimazosin.
Lacidipine Moxisylyte may decrease the antihypertensive activities of Lacidipine.
Manidipine Moxisylyte may decrease the antihypertensive activities of Manidipine.
Niguldipine Moxisylyte may decrease the antihypertensive activities of Niguldipine.
Rauwolfia serpentina root Moxisylyte may decrease the antihypertensive activities of Rauwolfia serpentina root.
Selexipag Moxisylyte may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Moxisylyte may decrease the antihypertensive activities of Angiotensin 1-7.
Talinolol Moxisylyte may decrease the antihypertensive activities of Talinolol.
Imidapril Moxisylyte may decrease the antihypertensive activities of Imidapril.
BQ-123 Moxisylyte may decrease the antihypertensive activities of BQ-123.
Tetrahydropalmatine Moxisylyte may decrease the antihypertensive activities of Tetrahydropalmatine.
Landiolol Moxisylyte may decrease the antihypertensive activities of Landiolol.
Dihydralazine Moxisylyte may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Moxisylyte may decrease the antihypertensive activities of Zofenopril.
Guanoxan Moxisylyte may decrease the antihypertensive activities of Guanoxan.
Delapril Moxisylyte may decrease the antihypertensive activities of Delapril.
Vincamine Moxisylyte may decrease the antihypertensive activities of Vincamine.
Linsidomine Moxisylyte may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Moxisylyte may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Moxisylyte may decrease the antihypertensive activities of Tolonidine.
Endralazine Moxisylyte may decrease the antihypertensive activities of Endralazine.
Esatenolol Moxisylyte may decrease the antihypertensive activities of Esatenolol.
Cadralazine Moxisylyte may decrease the antihypertensive activities of Cadralazine.
Cloranolol Moxisylyte may decrease the antihypertensive activities of Cloranolol.
Bietaserpine Moxisylyte may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Moxisylyte may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Moxisylyte may decrease the antihypertensive activities of Methoserpidine.
Epanolol Moxisylyte may decrease the antihypertensive activities of Epanolol.
Guanoclor Moxisylyte may decrease the antihypertensive activities of Guanoclor.
Candesartan Moxisylyte may decrease the antihypertensive activities of Candesartan.
Dexniguldipine Moxisylyte may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone Moxisylyte may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Moxisylyte may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Moxisylyte may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Moxisylyte may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Moxisylyte may decrease the antihypertensive activities of Perindoprilat.

Target Protein

Alpha-1D adrenergic receptor ADRA1D
Alpha adrenergic receptor ADRA1A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 6108620
    Wand M, Grant WM: Thymoxamine hydrochloride: an alpha-adrenergic blocker. Surv Ophthalmol. 1980 Sep-Oct;25(2):75-84.
  • PMID: 2973182
    Duchene P, Bernouillet C, Bromet-Petit M, Mosser J, Feniou C, Gaudin D, Virelizier H: Metabolism of 14C-thymoxamine in rat and man. Xenobiotica. 1988 Aug;18(8):919-28. doi: 10.3109/00498258809167515.
  • PMID: 24092932
    Samad F, Ruf W: Inflammation, obesity, and thrombosis. Blood. 2013 Nov 14;122(20):3415-22. doi: 10.1182/blood-2013-05-427708. Epub 2013 Oct 3.
  • PMID: 11110501
    Pandit RJ, Taylor R: Mydriasis and glaucoma: exploding the myth. A systematic review. Diabet Med. 2000 Oct;17(10):693-9.
  • PMID: 8866639
    Bressolle F, Costa P, Rouzier-Panis R, Marquer C: Pharmacokinetics of moxisylyte in healthy volunteers after intracavernous injection of increasing doses. Eur J Clin Pharmacol. 1996;49(5):411-5.
  • PMID: 8229699
    Costa P, Bressolle F, Jarroux E, Sarrazin B, Mosser J, Navratil H, Galtier M: Multiple-dose pharmacokinetics of moxisylyte after oral administration to healthy volunteers. J Pharm Sci. 1993 Sep;82(9):968-71.
  • PMID: 1491345
    Costa P, Bressolle F, Bromet-Petit M, Mosser J, Sarrazin B: Pharmacokinetics of moxisylyte in healthy volunteers after intravenous and oral administration. J Pharm Sci. 1992 Dec;81(12):1223-6.
  • PMID: 8103112
    Costa P, Bressolle F, Sarrazin B, Mosser J, Galtier M: Pharmacokinetics of moxisylyte in healthy volunteers after intravenous and intracavernous administration. J Pharm Sci. 1993 Jul;82(7):729-33.
Textbook
  • WHO (1987). WHO drug information (4th ed.). WHO.
  • Ellis G.P. and West G.B. (1986). Progress in Medicinal Chemistry Volume 23. Elsevier.

Contoh Produk & Brand

Produk: 0 • International brands: 1
International Brands
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