- Molecular NameCarteolol
- SynonymCarteolol HCl; Carteolol Hydrochloride; Carteololum [INN-Latin]
- Weight292.379
- Drugbank_IDDB00521
- ACS_NO51781-06-7
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- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)1.66
- pkaN/A
- LogD (pH=7, predicted)-0.81
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)0.53
- LogSw (predicted, AB/LogsW2.0)5.47
- Sw (mg/ml) (predicted, ACD/Labs)8.96
- No.of HBond Donors3
- No.of HBond Acceptors5
- No.of Rotatable Bonds6
- TPSA70.59
- StatusFDA approved
- AdministrationN/A
- PharmacologyA non-selective beta blocker used to treat glaucoma.
- Absorption_value95.0
- Absorption (description)Carteolol is well absorbed after oral administration with peak plasma concentrations being reached within 1 to 3 h.
- Caco_2N/A
- Bioavailability88.0
- Protein binding15.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmCarteolol undergoes minimal hepatic metabolism to form the active metabolite, 8-hydroxycarteolol and glucuronic acid conjugates of carteolol and 8-hydroxycarteolol.
- Half life6 h (carteolol) and about 8 to 12 h (8-hydroxycarteolol).
- ExcretionThe major route of elimination is renal with 50 to 70% being excreted unchanged in urine.
- Urinary ExcretionN/A
- Clerance10 ml/min/kg.
- ToxicityThe following ocular adverse reactions have been reported in clinical trials with Carteolol: transient eye irritation, burning, tearing, conjunctival hyperemia and edema occurred in about 1 of 4 patients. Ocular symptoms including blurred and cloudy vision, photophobia, decreased night vision, and ptosis and ocular signs including blepharoconjunctivitis, abnormal corneal staining, and corneal sensitivity occurred occasionally. As nonselective adrenergic blocking agent, Carteolol may cause bradycardia and decreased blood pressure.
- LD50 (rat)N/A
- LD50 (mouse)LD50=810