- Molecular NameFluoxetine
- SynonymFluoxetina [INN-Spanish]; Fluoxetina [Spanish]; Fluoxetine Hcl; Fluoxetine Hydrochloride; Fluoxetinum [INN-Latin]
- Weight309.331
- Drugbank_IDDB00472
- ACS_NO54910-89-3
- Show 3D model
- LogP (experiment)4.5
- LogP (predicted, AB/LogP v2.0)4.64
- pka8.7
- LogD (pH=7, predicted)2.18
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-0.88
- LogSw (predicted, AB/LogsW2.0)0.03
- Sw (mg/ml) (predicted, ACD/Labs)0.12
- No.of HBond Donors1
- No.of HBond Acceptors2
- No.of Rotatable Bonds7
- TPSA21.26
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. Fluoxetine is approved for the treatment of major depression (including pediatric depression), obsessive-compulsive disorder (in both adult and pediatric populations), bulimia nervosa, anorexia nervosa, panic disorder and premenstrual dysphoric disorder.
- Absorption_value80.0
- Absorption (description)Fluoxetine is readily absorbed after oral administration (> 80% of dose is absorbed)
- Caco_2N/A
- Bioavailability60.0
- Protein binding94.0
- Volume of distribution (VD)7 L/kg (between 20 and 42 L/kg for both fluoxetine and norfluoxetine).
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmExtensively metabolised in the liver by demethylation. The primary active metabolite is norfluoxetine, which is excreted via the kidneys. Further metabolism can occur by O-dealkylation producing p-trifluoromethylphenol and hippuric acid.
- Half life53 h
- Excretion80% of a drug dose is excreted in urine with less than 10% as the unchanged parent drug and 15% excreted in faeces. Fluoxetine is widely distributed throughout the body and secreted into breast milk.
- Urinary Excretion<2.5
- Clerance9.6 ml/min/kg
- ToxicitySymptoms of overdose include agitation, restlessness, hypomania, and other signs of CNS excitation. Blood concentrations of 1.3 to 6.8 mg/L fluoxetine and 0.9 to 5.0 mg/L norfluoxetine have been associated with fatalities. Serum levels of 1.96 mg/L fluoxetine (0.42 mg/L norfluoxetine) have been associated with seizures.
- LD50 (rat)N/A
- LD50 (mouse)LD50=284mg/kg