Peringatan Keamanan

Oral, mouse: LD50 = 400 mg/kg. In the presence of life-threatening arrhythmias, underdosing with bretylium probably presents a greater risk to the patient than potential overdosage. However, one case of accidental overdose has been reported in which a rapidly injected intravenous bolus of 30 mg/kg was given instead of an intended 10 mg/kg dose during an episode of ventricular tachycardia. Marked hypertension resulted, followed by protracted refractory hypotension. The patient expired 18 hours later in asystole, complicated by renal failure and aspiration pneumonitis. Bretylium serum levels were 8000 ng/mL.

Bretylium

DB01158

small molecule approved

Deskripsi

Bretylium blocks the release of noradrenaline from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. The primary mode of action for bretylium is thought to be inhibition of voltage-gated K(+) channels. Recent evidence has shown that bretylium may also inhibit the Na,K-ATPase by binding to the extracellular K-site.

Struktur Molekul 2D

Berat 243.163
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half-life in four normal volunteers averaged 7.8±0.6 hours (range 6.9-8.1). During hemodialysis, this patient's arterial and venous bretylium concentrations declined rapidly, resulting in a half-life of 13 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

No metabolites have been identified following administration in man and laboratory animals.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

991 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Bretylium is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Bretylium is combined with Levodopa.
Risperidone Bretylium may increase the hypotensive activities of Risperidone.
Ceritinib Bretylium may increase the bradycardic activities of Ceritinib.
Ivabradine Bretylium may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Bretylium.
Alfuzosin Alfuzosin may increase the hypotensive activities of Bretylium.
Amifostine Bretylium may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Bretylium.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Bretylium.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Bretylium.
Obinutuzumab Bretylium may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Bretylium.
Rituximab Bretylium may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Bretylium.
Cyclosporine Cyclosporine may decrease the antihypertensive activities of Bretylium.
Eletriptan Eletriptan may decrease the antihypertensive activities of Bretylium.
Methysergide Methysergide may decrease the antihypertensive activities of Bretylium.
Cabergoline Cabergoline may decrease the antihypertensive activities of Bretylium.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Bretylium.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Bretylium.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Bretylium.
Buspirone Buspirone may decrease the antihypertensive activities of Bretylium.
Doxapram Doxapram may decrease the antihypertensive activities of Bretylium.
Lisuride Lisuride may decrease the antihypertensive activities of Bretylium.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Bretylium.
Ergotamine Ergotamine may decrease the antihypertensive activities of Bretylium.
Nicergoline Nicergoline may decrease the antihypertensive activities of Bretylium.
Propiomazine Propiomazine may decrease the antihypertensive activities of Bretylium.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Bretylium.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Bretylium.
Almotriptan Almotriptan may decrease the antihypertensive activities of Bretylium.
Naratriptan Naratriptan may decrease the antihypertensive activities of Bretylium.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Bretylium.
Dopamine Dopamine may decrease the antihypertensive activities of Bretylium.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Bretylium.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Bretylium.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Bretylium.
Dutasteride Dutasteride may decrease the antihypertensive activities of Bretylium.
Nefazodone Nefazodone may decrease the antihypertensive activities of Bretylium.
Finasteride Finasteride may decrease the antihypertensive activities of Bretylium.
Yohimbine Yohimbine may decrease the antihypertensive activities of Bretylium.
Periciazine Periciazine may decrease the antihypertensive activities of Bretylium.
Acepromazine Acepromazine may decrease the antihypertensive activities of Bretylium.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Bretylium.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Bretylium.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Bretylium.
Lysergic acid diethylamide Lysergic acid diethylamide may decrease the antihypertensive activities of Bretylium.
Amineptine Amineptine may decrease the antihypertensive activities of Bretylium.
Flibanserin Flibanserin may decrease the antihypertensive activities of Bretylium.
Naluzotan Naluzotan may decrease the antihypertensive activities of Bretylium.
Cariprazine Cariprazine may decrease the antihypertensive activities of Bretylium.
Mianserin Mianserin may decrease the antihypertensive activities of Bretylium.
Pizotifen Pizotifen may decrease the antihypertensive activities of Bretylium.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Bretylium.
Vilazodone Vilazodone may decrease the antihypertensive activities of Bretylium.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Bretylium.
Saralasin Saralasin may decrease the antihypertensive activities of Bretylium.
Cinitapride Cinitapride may decrease the antihypertensive activities of Bretylium.
Tyramine Tyramine may decrease the antihypertensive activities of Bretylium.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Bretylium.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Bretylium.
Cannabidiol Cannabidiol may decrease the antihypertensive activities of Bretylium.
Vortioxetine Vortioxetine may decrease the antihypertensive activities of Bretylium.
Brexpiprazole Brexpiprazole may decrease the antihypertensive activities of Bretylium.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Bretylium.
Tianeptine Tianeptine may decrease the antihypertensive activities of Bretylium.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Bretylium.
Dihydroergocornine Dihydroergocornine may decrease the antihypertensive activities of Bretylium.
Atipamezole Atipamezole may decrease the antihypertensive activities of Bretylium.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Bretylium.
Propiverine Propiverine may decrease the antihypertensive activities of Bretylium.
Piclozotan Piclozotan may decrease the antihypertensive activities of Bretylium.
Siponimod Siponimod may decrease the antihypertensive activities of Bretylium.
Idazoxan Idazoxan may decrease the antihypertensive activities of Bretylium.
Theodrenaline Theodrenaline may decrease the antihypertensive activities of Bretylium.
Opipramol Opipramol may decrease the antihypertensive activities of Bretylium.
Tramazoline Tramazoline may decrease the antihypertensive activities of Bretylium.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Bretylium.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Bretylium.
Quinupramine Quinupramine may decrease the antihypertensive activities of Bretylium.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Bretylium.
Fenozolone Fenozolone may decrease the antihypertensive activities of Bretylium.
Dihydroergocristine Dihydroergocristine may decrease the antihypertensive activities of Bretylium.
Melitracen Melitracen may decrease the antihypertensive activities of Bretylium.
Dihydroergocryptine Dihydroergocryptine may decrease the antihypertensive activities of Bretylium.
Terguride Terguride may decrease the antihypertensive activities of Bretylium.
Lofepramine Lofepramine may decrease the antihypertensive activities of Bretylium.
Xenon Xenon may decrease the antihypertensive activities of Bretylium.
Iprindole Iprindole may decrease the antihypertensive activities of Bretylium.
Buflomedil Buflomedil may decrease the antihypertensive activities of Bretylium.
Metergoline Metergoline may decrease the antihypertensive activities of Bretylium.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Bretylium.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Bretylium.
Mefenorex Mefenorex may decrease the antihypertensive activities of Bretylium.
Deoxyepinephrine Deoxyepinephrine may decrease the antihypertensive activities of Bretylium.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Bretylium.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Bretylium.
Solriamfetol Solriamfetol may decrease the antihypertensive activities of Bretylium.
Dexmedetomidine Dexmedetomidine may decrease the antihypertensive activities of Bretylium.

Target Protein

Sodium/potassium-transporting ATPase subunit alpha-1 ATP1A1
Beta-1 adrenergic receptor ADRB1

Referensi & Sumber

Synthesis reference: Copp, F.C. and Stephenson, D.; US. Patent 3,038,004; June 5, 1962; assigned to Burroughs Wellcome & Co.

Contoh Produk & Brand

Produk: 7 • International brands: 7
Produk
  • Bretylate Inj 50mg/ml
    Liquid • 50 mg / mL • Intramuscular; Intravenous • Canada • Approved
  • Bretylium Tosylate
    Injection • 50 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
  • Bretylium Tosylate
    Injection • 50 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
  • Bretylium Tosylate 0.2% and Dextrose 5% Inj
    Solution • - • Intravenous • Canada • Approved
  • Bretylium Tosylate 0.4% and Dextrose 5% Inj
    Solution • - • Intravenous • Canada • Approved
  • Bretylium Tosylate Inj 50mg/ml
    Solution • 50 mg / mL • Intramuscular; Intravenous • Canada • Approved
  • Bretylium Tosylate Injection USP
    Solution • 50 mg / mL • Intramuscular; Intravenous • Canada • Approved
International Brands
  • Anxyrex — Sanofi-Aventis
  • Bretylol — ICI
  • Bromidem — Nycomed
  • Creosedin — AstraZeneca
  • Darenthin — Burroughs Wellcome
  • Lexotan — Roche
  • Xionil — Novartis

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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