Peringatan Keamanan

Symptoms of overdose include cardiac arrest, bradycardia, hypotension, electromechanical dissociation and loss of consciousness.

Esmolol

DB00187

small molecule approved withdrawn

Deskripsi

Esmolol, commonly marketed under the trade name Brevibloc, is a cardioselective beta-1 receptor blocker. It has a rapid onset but short duration of action without causing significant intrinsic sympathomimetic or membrane stabilizing activities at recommended therapeutic doses. It works by blocking beta-adrenergic receptors in the heart, which leads to decreased force and rate of heart contractions. Esmolol prevents the action of two naturally occurring substances: epinephrine and norepinephrine.

The FDA withdrew its approval for the use of all parenteral dosage form drug products containing esmolol hydrochloride that supply 250 milligrams/milliliter of concentrated esmolol per 10-milliliter ampule. Other esmolol formulations are still available for use.L43942

Struktur Molekul 2D

Berat 295.374
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Rapid distribution half-life of about 2 minutes and an elimination half-life of about 9 minutes. The acid metabolite has an elimination half-life of about 3.7 hours.
Volume Distribusi -
Klirens (Clearance) * 20 L/kg/hr [Men]

Absorpsi

Rapidly absorbed, steady-state blood levels for dosages from 50-300 µg/kg/min (0.05-0.3 mg/kg/mm) are obtained within five minutes.

Metabolisme

Esmolol undergoes rapid hydrolysis of ester linkage which is catalyzed by esterases found in the cytosol of red blood cells (RBCs). The plasma cholinersterases or RBC membrane acetylcholinesterases are not involved in this metabolic reaction. Metabolism of the drug occurs mainly in RBCs to form a free acid metabolite (with 1/1500 the activity of esmolol) and methanol.

Rute Eliminasi

Consistent with the high rate of blood-based metabolism of esmolol hydrochloride, less than 2% of the drug is excreted unchanged in the urine. The acid metabolite has an elimination half-life of about 3.7 hours and is excreted in the urine with a clearance approximately equivalent to the glomerular filtration rate. Excretion of the acid metabolite is significantly decreased in patients with renal disease, with the elimination half-life increased to about ten-fold that of normals, and plasma levels considerably elevated.

Interaksi Obat

1396 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Esmolol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Esmolol is combined with Levodopa.
Risperidone Esmolol may increase the hypotensive activities of Risperidone.
Ceritinib Esmolol may increase the bradycardic activities of Ceritinib.
Ivabradine Esmolol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Esmolol.
Alfuzosin Alfuzosin may increase the hypotensive activities of Esmolol.
Amifostine Esmolol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Esmolol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Esmolol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Esmolol.
Obinutuzumab Esmolol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Esmolol.
Rituximab Esmolol may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Esmolol.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Esmolol.
Doxapram Doxapram may decrease the antihypertensive activities of Esmolol.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Esmolol.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Esmolol.
Naratriptan Naratriptan may decrease the antihypertensive activities of Esmolol.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Esmolol.
Dopamine Dopamine may decrease the antihypertensive activities of Esmolol.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Esmolol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Esmolol.
Finasteride Finasteride may decrease the antihypertensive activities of Esmolol.
Yohimbine Yohimbine may decrease the antihypertensive activities of Esmolol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Esmolol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Esmolol.
Amineptine Amineptine may decrease the antihypertensive activities of Esmolol.
Flibanserin Flibanserin may decrease the antihypertensive activities of Esmolol.
Naluzotan Naluzotan may decrease the antihypertensive activities of Esmolol.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Esmolol.
Cinitapride Cinitapride may decrease the antihypertensive activities of Esmolol.
Tyramine Tyramine may decrease the antihypertensive activities of Esmolol.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Esmolol.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Esmolol.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Esmolol.
Tianeptine Tianeptine may decrease the antihypertensive activities of Esmolol.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Esmolol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Esmolol.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Esmolol.
Piclozotan Piclozotan may decrease the antihypertensive activities of Esmolol.
Siponimod Siponimod may decrease the antihypertensive activities of Esmolol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Esmolol.
Tramazoline Tramazoline may decrease the antihypertensive activities of Esmolol.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Esmolol.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Esmolol.
Quinupramine Quinupramine may decrease the antihypertensive activities of Esmolol.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Esmolol.
Fenozolone Fenozolone may decrease the antihypertensive activities of Esmolol.
Melitracen Melitracen may decrease the antihypertensive activities of Esmolol.
Lofepramine Lofepramine may decrease the antihypertensive activities of Esmolol.
Xenon Xenon may decrease the antihypertensive activities of Esmolol.
Iprindole Iprindole may decrease the antihypertensive activities of Esmolol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Esmolol.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Esmolol.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Esmolol.
Mefenorex Mefenorex may decrease the antihypertensive activities of Esmolol.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Esmolol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Esmolol.
Solriamfetol Solriamfetol may decrease the antihypertensive activities of Esmolol.
Sufentanil Sufentanil may decrease the antihypertensive activities of Esmolol.
Remifentanil Remifentanil may decrease the antihypertensive activities of Esmolol.
Halothane Halothane may decrease the antihypertensive activities of Esmolol.
Opipramol Opipramol may decrease the antihypertensive activities of Esmolol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Esmolol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Esmolol.
Cannabidiol The metabolism of Esmolol can be decreased when combined with Cannabidiol.
Amiodarone The therapeutic efficacy of Esmolol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Esmolol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Esmolol.
Disopyramide Disopyramide may increase the bradycardic activities of Esmolol.
Dronedarone Dronedarone may increase the bradycardic activities of Esmolol.
Fingolimod Esmolol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Esmolol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Esmolol.
Methacholine Esmolol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Esmolol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Esmolol.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Esmolol.
Regorafenib Regorafenib may increase the bradycardic activities of Esmolol.
Reserpine Reserpine may increase the hypotensive activities of Esmolol.
Deserpidine Deserpidine may increase the hypotensive activities of Esmolol.
Guanethidine Guanethidine may increase the hypotensive activities of Esmolol.
Rivastigmine Esmolol may increase the bradycardic activities of Rivastigmine.
Mirabegron The serum concentration of Esmolol can be increased when it is combined with Mirabegron.
Nicorandil Nicorandil may increase the hypotensive activities of Esmolol.
Molsidomine Molsidomine may increase the hypotensive activities of Esmolol.
Insulin human Esmolol may increase the hypoglycemic activities of Insulin human.
Insulin lispro Esmolol may increase the hypoglycemic activities of Insulin lispro.
Insulin glargine Esmolol may increase the hypoglycemic activities of Insulin glargine.
Insulin pork Esmolol may increase the hypoglycemic activities of Insulin pork.
Insulin aspart Esmolol may increase the hypoglycemic activities of Insulin aspart.
Insulin detemir Esmolol may increase the hypoglycemic activities of Insulin detemir.
Insulin glulisine Esmolol may increase the hypoglycemic activities of Insulin glulisine.
NN344 Esmolol may increase the hypoglycemic activities of NN344.
Insulin beef Esmolol may increase the hypoglycemic activities of Insulin beef.
Insulin degludec Esmolol may increase the hypoglycemic activities of Insulin degludec.
Insulin peglispro Esmolol may increase the hypoglycemic activities of Insulin peglispro.
Insulin tregopil Esmolol may increase the hypoglycemic activities of Insulin tregopil.

Target Protein

Beta-1 adrenergic receptor ADRB1

Referensi & Sumber

Contoh Produk & Brand

Produk: 55 • International brands: 0
Produk
  • Brevibloc
    Injection, solution, concentrate • 250 mg/1mL • Intravenous • US • Approved
  • Brevibloc
    Injection • 20 mg/1mL • Intravenous • US • Approved
  • Brevibloc
    Injection • 10 mg/1mL • Intravenous • US • Approved
  • Brevibloc
    Injection • 20 mg/1mL • Intravenous • US • Approved
  • Brevibloc
    Injection • 10 mg/1mL • Intravenous • US • Approved
  • Brevibloc
    Injection • 20 mg/1mL • Intravenous • US • Approved
  • Brevibloc
    Injection • 10 mg/1mL • Intravenous • US • Approved
  • Brevibloc
    Injection • 10 mg/1mL • Intravenous • US • Approved
Menampilkan 8 dari 55 produk.

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