Escolar Documentos
Profissional Documentos
Cultura Documentos
Length: 260 AA
MW: 29kDa
Inhibitor action
Target: Active site Zinc
Mechanism of Action: Inhibitor binds to active site, blocking
interactions of water bound to zinc and inhibiting enzymatic activity
Target: Carbonic Anhydrase II
Acetazolamide Dorzolamide
For treatment of: For treatment of:
Open angle glaucoma Open angle glaucoma
Drug induced edema Ocular hypertension
Centrencephalic
epilepsies
Edema due to
conjuctive heart failure
Metabolic alkalaemia
Periodic paralysis
Acetazolamide
Dorzolamide
Acetazolamide - Dorzolamide
Acidic Pka: 6.93 - Acidic pKa: 8.1
Basic pKa: -3.3 - Basic pKa: 7.14
LogS: -2.36 Sw: .002 M - LogS: -2.7 Sw: .004 M
Solubility: .980mg/mL @ 30oC - Solubility: .699mg/mL
Protein Binding
Acetazolamide
Protein Binding: 98%
Dorzolamide
Protein Binding: 33%
Target binding
Acetazolamide Dorzolamide
Kd (dissociation 20 nM 0.37 nM
constant)
Acetazolamide Dorzolamide
LogP -0.26 -1
Acetazolamide Dorzolamide
Hydrophilic Hydrophilic
Acetazolamide Dorzolamide
Oral bioavailability: >90% Bioavailability: little to no
systemic absorption
Food co-ingestion: neither
delays the rate of
absorption nor reduces
extent of absorption
Acetazolamide:
Salicylates increase the effect of the
inhibitor
Any other CAH2 inhibitor concurrent use
will result in toxicity
Dorzolamide
Any other CAH2 inhibitor because of
adverse effects
Future