- Molecular NameIndoramin
- SynonymNA
- Weight347.462
- Drugbank_IDN/A
- ACS_NO26844-12-2
- Show 3D model
- LogP (experiment)3.6
- LogP (predicted, AB/LogP v2.0)3.82
- pka7.7
- LogD (pH=7, predicted)3.02
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-1.66
- LogSw (predicted, AB/LogsW2.0)0.07
- Sw (mg/ml) (predicted, ACD/Labs)0.15
- No.of HBond Donors2
- No.of HBond Acceptors4
- No.of Rotatable Bonds5
- TPSA48.13
- StatusN/A
- AdministrationN/A
- PharmacologyA piperidine antiadrenergic agent.
- Absorption_valueN/A
- Absorption (description)Readily absorbed after oral administration
- Caco_2N/A
- Bioavailability34.5
- Protein binding80.0
- Volume of distribution (VD)7 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmUndergoes extensive first-pass metabolism to active metabolites.
- Half life5 h, increased in elderly subjects.
- ExcretionAbout 35% of a dose is excreted in the urine in 5 days, mainly as metabolites; less than 10% of a dose is excreted in the urine as unchanged drug; about 47% of a dose is eliminated in the faeces, mainly as metabolites; 6-hydroxyindoramin has been identified as a major metabolite. Other metabolites include acid-labile conjugates of indoramin and 6-hydroxyindoramin.
- Urinary ExcretionN/A
- Clerance20 ml/min/kg
- ToxicityIn a fatality attributed to indoramin overdose, an antemortem plasma concentration of 6.4 mg/L was reported together with an alcohol concentration of 2.25 g/L. [R. Hunter,BMJ,1982, 285, 1011.]
- LD50 (rat)LD50=1800; LD50=500 (intraperitoneal)
- LD50 (mouse)LD50>400 (intraperitoneal); LD50=127~400mg/kg (intraperitoneal)