Maropitant Prevent Vomiting

Product Name: Maropitant
CAS number: 147116-67-4
Molecular formula: C32H40N2O
Molecular weight: 468.67
Appearance: off white to yellow granules or powder
Density: 1.11 ± 0.1 g/cm3
Boiling point: 572.6 ± 50.0 ° C
Acidity coefficient: 9.99 ± 0.70
Solubility: DMSO: 33.33 mg/mL (71.12 mM; ultrasound required)
H2O:<0.1 mg/mL (insoluble)
Storage: Store in a dark, dry, sealed, and cool place

Maropitant is a neurokinin (NK1) receptor antagonist that can block the binding of substance P to receptors in the central nervous system and has antiemetic effects. Substance P is a type of neurotransmitter associated with vomiting. Blocking the binding between substance P and its receptors can effectively inhibit central nervous system vomiting, peripheral nervous system vomiting, and vomiting caused by chemical factors.
Indications: Used for the prevention and treatment of vomiting caused by chemotherapy drugs in dogs and cats, as well as vomiting other than motion sickness.
Preparation specification: Calculated based on Malopitant.
Maropitant citrate tablets: 16mg/tablet, 24mg/tablet, 60mg/tablet, 160mg/tablet.
Malapitant Citrate Injection: 20ml: 0.2g.

Pharmacokinetics: The bioavailability of Malopitant is not affected by feeding, with a single oral dose of 2mg/kg and a bioavailability of 23.7%. The binding rate to plasma proteins is higher than 99%. The peak plasma concentration (Cmax) is about 81ng/ml, the peak time (Tmax) is about 1.9 hours, and the half-life (t1/2) is 4.03 hours. There are significant differences in pharmacokinetics among individual animals, with the highest variable (CV) of the drug time curve (AUC) being 70%. In clinical trials, it has been shown that the medication begins to exert its effects one hour after taking and can last for 24 hours.
Metabolism: Malopitant is mainly metabolized through the liver, and the hepatic enzymes that metabolize Malopitant in dogs are CYP2D15 and CYP3A12. The clearance rate of Maropitant and its metabolites through the kidneys is less than 1%.