SUMMARY of Pitavastatin calcium
Pitavastatin calcium is an inhibitor of HMG-CoA reductase. It is a synthetic lipid-lowering agent for oral administration.The empirical formula for pitavastatin is C50H46CaF2N2O8 and the molecular weight is 880.98. The CAS NO is 147526-32-7.
Pitavastatin calcium is odorless and occurs as white to pale-yellow powder. It is freely soluble in pyridine, chloroform, dilute hydrochloric acid, and tetrahydrofuran, soluble in ethylene glycol, sparingly soluble in octanol, slightly soluble in methanol, very slightly soluble in water or ethanol, and practically insoluble in acetonitrile or diethyl ether. Pitavastatin is hygroscopic and slightly unstable in light.
Pitavastatin calcium (previously known as itavastatin, itabavastin, nisvastatin) was discovered in Japan by Nissan Chemical Industries and developed further by Kowa Pharmaceuticals, Tokyo. Pitavastatin was approved for use in the United States by the FDA on 08/03/2009 under the trade name Livalo. It has been also approved by the Medicines and Healthcare products Regulatory Agency (MHRA) in UK on 17 August 2010.
Pitavastatin calcium (CAS NO:147526-32-7)is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease. A 2009 study showed that pitavastatin increased HDL cholesterol (24.6%), especially in patients with HDL lower than 40 mg/dl, in addition to greatly reducing LDL cholesterol (31.3%). As a consequence, pitavastatin is most likely to be appropriate for patients with metabolic syndrome with high LDL, low HDL and diabetes mellitus.
Most statins are metabolised in part by one or more hepatic cytochrome P450 enzymes, leading to an increased potential for drug interactions and problems with certain foods (such as grapefruit juice). Pitavastatin calcium appears to be a substrate of CYP2C9, and not CYP3A4 (which is a common source of interactions in other statins). As a result, it is less likely to interact with drugs that are metabolized via CYP3A4, which might be important for elderly patients who need to take multiple medicines.
Common statin-related side-effects (headaches, stomach upset, abnormal liver function tests and muscle cramps) were similar to other statins. However, Pitavastatin calcium seems to lead to fewer muscle side effects than other statins, since coenzyme Q10 is not significantly reduced. Hyperuricemia or increased levels of serum uric acid have been reported with pitavastatin. Pitavastatin calcium interactions have: Muscular Weakness, Malaise, Hepatic Function Abnormal, Constipation, Gamma-glutamyltransferase Increased, Blood Lactate Dehydrogenase Increased, Aspartate Aminotransferase Increased, Alanine Aminotransferase Increased, Vomiting, Pyrexia.
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