- Molecular NameLabetalol
- SynonymLabetalol HCL; Labetalol hydrochloride; Labetalolum [INN-Latin]; Labetolol
- Weight328.412
- Drugbank_IDDB00598
- ACS_NO36894-69-6
- Show 2D model
- LogP (experiment)3.09
- LogP (predicted, AB/LogP v2.0)2.39
- pka7.4 (phenol), 8.7 (-NH2).
- LogD (pH=7, predicted)0.66
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-1.8
- LogSw (predicted, AB/LogsW2.0)0.82
- Sw (mg/ml) (predicted, ACD/Labs)0.54
- No.of HBond Donors5
- No.of HBond Acceptors5
- No.of Rotatable Bonds8
- TPSA95.58
- StatusFDA approved
- AdministrationOral, IV
- PharmacologyA mixed alpha/beta Adrenergic antagonist, which is used to treat high blood pressure.
- Absorption_value95.0
- Absorption (description)Labetalol is well absorbed after oral administration
- Caco_2-5.03
- Bioavailability25.0
- Protein binding50.0
- Volume of distribution (VD)3 to 10 (mean 7) L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmUndergoes extensive first-pass metabolism. The major metabolites are glucuronides of labetalol.
- Half life3~6 h
- ExcretionUp to about 60% of a dose is excreted in the urine in 24 h as conjugates, one of which has been identified as the O-phenylglucuronide. about 5% of a dose is excreted as unchanged drug.
- Urinary ExcretionN/A
- Clerance25 ml/min/kg
- ToxicityN/A
- LD50 (rat)LD50=66 mg/kg (IV)
- LD50 (mouse)N/A