- Molecular NameGranisetron
- SynonymAPF530; Granisetron base; Granisetron HCl; Granisetron hydrochloride; Granisetronum [INN-Latin]
- Weight312.417
- Drugbank_IDDB00889
- ACS_NO109889-09-0
- Show 2D model
- LogP (experiment)2.795
- LogP (predicted, AB/LogP v2.0)3.01
- pkaN/A
- LogD (pH=7, predicted)0.69
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-0.42
- LogSw (predicted, AB/LogsW2.0)0.38
- Sw (mg/ml) (predicted, ACD/Labs)0.3
- No.of HBond Donors1
- No.of HBond Acceptors5
- No.of Rotatable Bonds2
- TPSA50.16
- StatusFDA approved
- AdministrationN/A
- PharmacologyA serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
- Absorption_value100.0
- Absorption (description)Granisetron is rapidly and completely absorbed after oral administration
- Caco_2N/A
- Bioavailability60.0
- Protein binding65.0
- Volume of distribution (VD)3 L/kg
- Blood/Plasma Partitioning ratio (D_blood)Distributed freely between plasma and red blood cells.
- MetabollsmMetabolised in the liver by 7-hydroxylation, N-demethylation, aromatic ring oxidation and conjugation. Its active metabolite is 7-hydroxygranisetron.
- Half life5.3 h
- Excretion< 20% of a dose is recovered in urine unchanged and the rest is excreted in urine and faeces as its metabolites.
- Urinary Excretion16
- Clerance11 ml/min/kg
- ToxicityDuring clinical trials, one patient received over 10 times the recommended dose (total of 38.5 mg) and complained of a headache only. Acute overdose: somnolence and myalgia.
- LD50 (rat)N/A
- LD50 (mouse)N/A