- Molecular NameDesipramine
- SynonymDemethylimipramine; Desimipramine; Desimpramine; Desipramin; Desipramine Hcl; Desmethylimipramine; Dezipramine; Dimethylimipramine; DMI; Methylaminopropyliminodibenzyl; Monodemethylimipramine; Norimipramine; Norpramine
- Weight266.388
- Drugbank_IDDB01151
- ACS_NO50-47-5
- Show 3D model
- LogP (experiment)4.9
- LogP (predicted, AB/LogP v2.0)4.27
- pkaN/A
- LogD (pH=7, predicted)1.38
- Solubility (experiment)0.0583 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-1.32
- LogSw (predicted, AB/LogsW2.0)0.04
- Sw (mg/ml) (predicted, ACD/Labs)0.05
- No.of HBond Donors1
- No.of HBond Acceptors2
- No.of Rotatable Bonds4
- TPSA15.27
- StatusFDA approved
- AdministrationN/A
- PharmacologyA tricyclic antidepressant (TCA) that inhibits the reuptake of norepinephrine and serotonin and to a lesser extent dopamine.
- Absorption_value98.0
- Absorption (description)Well absorbed after oral administration.
- Caco_2-4.67
- Bioavailability82.5
- Protein binding82.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmMetabolised by aromatic hydroxylation and possibly hydroxylamine formation; N-demethylation to form didesmethylimipramine may occur to a minor extent. 2-Hydroxydesipramine, the major metabolite, is active.
- Half life10~35 h
- ExcretionLess than 5% of a dose is excreted in urine in 24 h as unchanged drug; the urinary excretion of unchanged drug is pH-dependent and is increased in acidic urine; the hydroxylated metabolites are excreted mainly as glucuronide conjugates. The extent of 2-hydroxylation is genetically determined. Desipramine is the major active metabolite of imipramine and lofepramine.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityPlasma concentrations greater than 0.4 mg/L may produce toxic effects. Fatalities are comparatively rare, but may occur with plasma concentrations greater than 10 mg/L.
- LD50 (rat)N/A
- LD50 (mouse)N/A