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Pharmacology: Pharmacodynamics: Pitavastatin inhibits 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase by competition with its substrate so that it inhibits hepatic cholesterol synthesis. The total plasma cholesterol decreases when the expression of low-density lipoprotein (LDL) receptors followed by the uptake of LDL from blood to liver is accelerated. Additionally, the levels of very low density decrease from the sustained inhibition of cholesterol synthesis in the liver.
Pharmacokinetics: Tmax, oral: 1 hour.
Bioavailability: 51%.
Effect of food: decreases Cmax by 43% but has no significant effect on AUC.
Distribution: Vd: 148 L.
Protein binding: albumin and alpha 1-acid glycoprotein: 99%.
Metabolism: Liver: extensive glucuronide conjugation by UGT1A3 and UGT2B7 and minimally by CYP2C9 and CYP2C8.
Lactone (major metabolite): inactive.
Excretion: Bile: extensive, fecal: 79%, renal: 15%.
Elimination half life: 11 to 12 hours.
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