- Molecular NameBrinzolamide
- SynonymNA
- Weight383.514
- Drugbank_IDDB01194
- ACS_NO138890-62-7
- Show 2D model
- LogP (experiment)-0.222
- LogP (predicted, AB/LogP v2.0)-0.14
- pkaN/A
- LogD (pH=7, predicted)-0.43
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-1.58
- LogSw (predicted, AB/LogsW2.0)1.15
- Sw (mg/ml) (predicted, ACD/Labs)6.45
- No.of HBond Donors3
- No.of HBond Acceptors8
- No.of Rotatable Bonds7
- TPSA163.8
- StatusFDA approved
- AdministrationOphthalmic
- PharmacologyA carbonic anhydrase inhibitor used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- BioavailabilityN/A
- Protein binding60.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmWhile definitive sites of metabolism have not been firmly established, there are several metabolites worthy of note. N-Desethylbrinzolamide is an active metabolite of the parent compound, and thus exhibits carbonic anhydrase inhibitory activity (largely carbonic anhydrase-I, when in the presence of Brinzolamide) and also accumulates in the erythrocytes. However, Brinzolamide's other known metabolites (N-Desmethoxypropylbrinzolamide and O-Desmethylbrinzolamide) either have no activity or their activity is currently unknown.
- Half life111 days
- ExcretionRenal (60%). Brinzolamide is excreted primarily unchanged (60%) in the urine, although the renal clearance rate has not been definitively determined. N-Desethylbrinzolamide is also found in the urine along with lower concentrations of the inactive metabolites, N-Desmethoxypropylbrinzolamide and O-Desmethylbrinzolamide; exact levels have not been definitively determined.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityN/A
- LD50 (rat)N/A
- LD50 (mouse)N/A