- Molecular NameDolasetron
- SynonymNA
- Weight324.38
- Drugbank_IDDB00757
- ACS_NO115956-12-2
- Show 2D model
- LogP (experiment)2.347
- LogP (predicted, AB/LogP v2.0)2.73
- pkaN/A
- LogD (pH=7, predicted)2.64
- Solubility (experiment)Soluble
- LogS (predicted, ACD/Labs)(ph=7)-3.62
- LogSw (predicted, AB/LogsW2.0)0.8
- Sw (mg/ml) (predicted, ACD/Labs)0.07
- No.of HBond Donors1
- No.of HBond Acceptors5
- No.of Rotatable Bonds3
- TPSA62.4
- StatusFDA approved
- AdministrationIntravenous, oral
- PharmacologyA serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.
- Absorption_value85.0
- Absorption (description)Dolasetron is rapidly absorbed
- Caco_2N/A
- Bioavailability75.0
- Protein binding69.0
- Volume of distribution (VD)1.4 L/kg (patients with mild to moderate renal impairment); 1.5 L/kg (moderate to severe renal impairment); 3.65 L/kg (end-stage renal impairment); 1.03 L/kg (healthy individuals). Hydrodolasetron, 5.8 L/kg.
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmSubsequently metabolised to hydrodolasetron (with the most clinically relevant activity) by carbonyl reductase. The metabolite appears rapidly in plasma with peak concentrations appearing within the hour; the parent drug is rarely detected. Food does not affect the abosorption of the drug. Hydrodolasetron undergoes additional hydroxylation (cytochrome P450 isoenzyme, CYP2D6) and N-oxidation (by flavin mono-oxygenase and isoenzyme, CYP3A).
- Half life8.1 h (Hydrodolasetron)
- ExcretionIt is excreted in urine as hydrodolasetron (53% of administered intravenous dose) and other metabolites including hydroxylated glucuronides and N-oxide. Approximately two-thirds of an administered dose is detected in urine and the remainder in faeces.
- Urinary ExcretionN/A
- Clerance55.7 ml/min/kg (patients with mild to moderate renal impairment); 117.5 mL/min/kg (moderate to severe renal impairment); 66.1 mL/min/kg (end-stage renal impairment); 114.9 mL/min/kg (healthy individuals). Apparent clearance, hydrodolasetron, 9.4 to 13.4 mL/min/kg.
- ToxicitySymptoms of acute toxicity include tremors, depression and convulsions. Dolasetron has been associated with electrocardiogram interval changes; magnitude and frequency are dependent on the concentration of the metabolite, hydrodolasetron, in the blood. This can lead to cardiovascular effects including heart block and cardiac arrhythmias.
- LD50 (rat)N/A
- LD50 (mouse)N/A