- Molecular NameLevobunolol
- SynonymLevobunolol HCl; Levobunololum [INN-Latin]
- Weight291.391
- Drugbank_IDDB01210
- ACS_NO47141-42-4
- Show 3D model
- LogP (experiment)2.4
- LogP (predicted, AB/LogP v2.0)2.4
- pka9.4
- LogD (pH=7, predicted)-0.06
- Solubility (experiment)0.25 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-0.38
- LogSw (predicted, AB/LogsW2.0)3.0
- Sw (mg/ml) (predicted, ACD/Labs)0.53
- No.of HBond Donors2
- No.of HBond Acceptors4
- No.of Rotatable Bonds6
- TPSA58.56
- StatusFDA approved
- AdministrationN/A
- PharmacologyA non-selective beta blocker. It is used topically to manage glaucoma.
- Absorption_value100.0
- Absorption (description)Some systemic absorption occurs following topical application, but after oral administration levobunolol is rapidly and almost completely absorbed from the gastro-intestinal tract.
- Caco_2N/A
- Bioavailability75.0
- Protein bindingN/A
- Volume of distribution (VD)5.5 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmIt is extensively metabolised in the liver and the principal metabolite is dihydrolevobunolol, which possesses β-blocking activity, approx. 65% of that of the parent drug. Other metabolites include bunolol glucuronide, bunolol sulfate and dihydrobunolol glucuronide. Levobunolol and its metabolites are subsequently glucuronidated.
- Half life(levobunolol) 6.1 h; (metabolite, dihydrolevobunolol) between 5.7 and 7.1 h.
- ExcretionMetabolites and some of the unchanged drug are excreted in urine (78%) and in faeces (3%), in 4 days. The metabolism of levobunolol following ophthalmic application has not been clearly determined. Peak levels of the drug and metabolite are reached within 1 h and the duration of action is 12 to 14 h. Distribution has not been determined.
- Urinary ExcretionN/A
- Clerance0.66 L/h/kg
- ToxicityRespiratory and cardiac reactions have been reported, rarely resulting in death caused by bronchospasm or associated with cardiac failure. No data available on human overdose.
- LD50 (rat)LD50=700 mg/kg
- LD50 (mouse)LD50=700