- Molecular NameEsmolol
- SynonymNA
- Weight295.379
- Drugbank_IDDB00187
- ACS_NO84057-94-3
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)2.02
- pka9.5
- LogD (pH=7, predicted)-0.38
- Solubility (experiment)Soluble
- LogS (predicted, ACD/Labs)(ph=7)0.53
- LogSw (predicted, AB/LogsW2.0)12.19
- Sw (mg/ml) (predicted, ACD/Labs)4.97
- No.of HBond Donors2
- No.of HBond Acceptors5
- No.of Rotatable Bonds10
- TPSA67.79
- StatusFDA approved
- AdministrationIV
- PharmacologyA cardioselective beta1 receptor blocker with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- BioavailabilityN/A
- Protein binding55.0
- Volume of distribution (VD)1.0 to 2.4 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmEsmolol is rapidly hydrolysed, in red blood cells, by esterases. An acidic de-esterified metabolite (ASL-8123, with very little beta-blocking activity), methanol and a number of inactive metabolites are produced.
- Half life9 min for esmolol; increases in patients with liver failure, up to 16 min; 3.7 h for the metabolite.
- ExcretionExcretion is primarily via urine primarily as the de-esterified metabolite (71 to 83%) and less than 2% of the drug appearing unchanged and the rest as the inactive metabolites. The remainder of the dose can be recovered in faeces. Only small amounts of the metabolite are removed by dialysis. The metabolite accumulates in patients with renal failure.
- Urinary ExcretionN/A
- Clerance20 L/kg/h; 0.08 L/h/kg or 1.28 ml/min/kg (metabolite).
- ToxicityMassive accidental overdosing has occurred due to dilution errors, which has resulted in cardiac arrest, death and permanent disability. A concentration between 12.5 and 50 mg/kg is associated with fatalities.
- LD50 (rat)N/A
- LD50 (mouse)N/A