- Molecular NameDiazoxide
- SynonymNA
- Weight230.675
- Drugbank_IDDB01119
- ACS_NO364-98-7
- Show 3D model
- LogP (experiment)1.2
- LogP (predicted, AB/LogP v2.0)1.06
- pka8.7
- LogD (pH=7, predicted)0.98
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-2.74
- LogSw (predicted, AB/LogsW2.0)0.85
- Sw (mg/ml) (predicted, ACD/Labs)0.42
- No.of HBond Donors1
- No.of HBond Acceptors4
- No.of Rotatable Bonds0
- TPSA66.91
- StatusFDA approved
- AdministrationN/A
- PharmacologyA potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential.
- Absorption_value90.0
- Absorption (description)Readily absorbed after oral administration.
- Caco_2N/A
- Bioavailability90.0
- Protein binding94.0
- Volume of distribution (VD)0.2 to 0.3 L/kg
- Blood/Plasma Partitioning ratio (D_blood)Plasma : whole blood ratio, about 1.7.
- MetabollsmMetabolised by oxidation to the 3-hydroxymethyl derivative which is conjugated with sulfate or further metabolised to the 3-carboxy derivative.
- Half life20~70 h; appears to be lower in children.
- ExcretionAbout 90% of a dose is excreted in the urine in 5 to 6 days, of which 6 to 50% is unchanged drug; the 3-hydroxymethyl and 3-carboxy metabolites each account for about 20 to 30% of the excreted material; the amount of unchanged drug excreted in the urine appears to be reduced in hypertensive patients; about 2% of a dose is eliminated in the faeces.
- Urinary ExcretionN/A
- Clerance0.1 ml/min/kg.
- ToxicityToxic effects may be associated with plasma concentrations greater than 100 mg/L.
- LD50 (rat)980 mg/kg
- LD50 (mouse)444 mg/kg