- Molecular NameDebrisoquine
- SynonymDebrisochinum; Debrisoquin hemisulfate; Debrisoquin sulfate; Debrisoquina [inn-spanish]; Debrisoquine; Debrisoquine sulfate; Debrisoquinum [inn-latin]; Isocaramidine; Isocaramidine sulfate
- Weight175.235
- Drugbank_IDDB04840
- ACS_NO1131-64-2
- Show 3D model
- LogP (experiment)0.8
- LogP (predicted, AB/LogP v2.0)0.78
- pka11.9
- LogD (pH=7, predicted)-2.32
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)0.68
- LogSw (predicted, AB/LogsW2.0)0.51
- Sw (mg/ml) (predicted, ACD/Labs)25.14
- No.of HBond Donors3
- No.of HBond Acceptors3
- No.of Rotatable Bonds1
- TPSA53.11
- StatusFDA approved
- AdministrationN/A
- PharmacologyA derivative of guanidine.
- Absorption_valueN/A
- Absorption (description)Rapidly absorbed after oral administration.
- Caco_2N/A
- BioavailabilityN/A
- Protein binding25.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)Plasma:whole blood ratio, 0.45.
- MetabollsmThe main metabolic reaction is 4-hydroxylation; aromatic hydroxylation at positions 5, 6, 7, and 8 also occurs and acidic ring-opened metabolites are also formed. There is no evidence of glucuronic acid conjugation in man. The extent of 4-hydroxylation of debrisoquine is genetically determined.
- Half lifedebrisoquine about 16~30 h, 4-hydroxydebrisoquine about 10 h.
- ExcretionAbout 75% of a dose is excreted in the urine in 24 h. Excretion of unchanged drug ranges from 8 to 80% of a dose. About 90% of the population are extensive metabolisers of debrisoquine and, in these subjects, about 10 to 40% of a dose is excreted as 4-hydroxydebrisoquine; the remaining 10% are poor metabolisers and excrete less than 2% as the 4-hydroxy metabolite. Acidic ring-opened metabolites account for up to 15% of a dose and the 5-, 6-, 7-, and 8-hydroxy metabolites for about 7%. About 12% of a dose is eliminated in the faeces.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityN/A
- LD50 (rat)N/A
- LD50 (mouse)N/A