- Molecular NameRisperidone
- Synonymrisperdone; Risperidona [Spanish]; risperidone; Risperidonum [Latin]
- Weight410.493
- Drugbank_IDDB00734
- ACS_NO106266-06-2
- Show 2D model
- LogP (experiment)3.04
- LogP (predicted, AB/LogP v2.0)2.97
- pka3.11, 8.24
- LogD (pH=7, predicted)1.76
- Solubility (experiment)0.0666 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-3.53
- LogSw (predicted, AB/LogsW2.0)0.1
- Sw (mg/ml) (predicted, ACD/Labs)0.01
- No.of HBond Donors0
- No.of HBond Acceptors6
- No.of Rotatable Bonds4
- TPSA61.94
- StatusFDA approved
- AdministrationOral and extended-release intramuscular injection
- PharmacologyAn atypical antipsychotic used to treat schizophrenia (including adolescent schizophrenia), the mixed and manic states associated with bipolar disorder, and irritability in children with autism.
- Absorption_value97.0
- Absorption (description)Well absorbed. The absolute oral bioavailability of risperidone is 70% (CV=25%). The relative oral bioavailability of risperidone from a tablet is 94% (CV=10%) when compared to a solution.
- Caco_2N/A
- Bioavailability66.0
- Protein binding89.0
- Volume of distribution (VD)1.1 L/kg (extensive metabolisers); 2.1 L/kg (intermediate); 0.7 L/kg (poor)
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmThe main metabolic pathway is through hydroxylation of risperidone to 9-hydroxyrisperidone by the enzyme, CYP 2D6. A minor metabolic pathway is through N-dealkylation. The main metabolite, 9-hydroxyrisperidone, has similar pharmacological activity as risperidone. Consequently, the clinical effect of the drug results from the combined concentrations of risperidone plus 9-hydroxyrisperidone.
- Half life3.2 h
- ExcretionUrinary
- Urinary Excretion3
- Clerance5.4 ml/min/kg
- ToxicitySymptoms of overdose include drowsiness, sedation, tachycardia, hypotension, and extrapyramidal symptoms. LD50=82.1mg/kg (orally in mice).
- LD50 (rat)N/A
- LD50 (mouse)N/A