|Trade names||Livalo, Livazo, Zypitamag, others|
|Main uses||Abnormal lipid levels, high risk of heart disease|
|Side effects||Muscle pain, diarrhea|
|By mouth (tablets)|
|Typical dose||1 to 4 mg OD|
|Metabolism||Liver (CYP2C9, minimally)|
|Elimination half-life||11 hours|
|Chemical and physical data|
|Molar mass||421.461 g·mol−1|
|3D model (JSmol)|
Common side effects include muscle pain and diarrhea. Other side effects may include muscle breakdown with kidney problems, liver problems, diabetes, allergic reactions, and memory problems. Use in pregnancy may harm the baby. It is a statin and works by blocking HMG-CoA reductase.
Pitavastatin was patented in 1987 and approved for medical use in 2003. It was approved in the United States in 2009. It is available in a number of countries in Europe. In the United States 3 month of medication costs about 1,000 USD as of 2021.
Like the other statins, pitavastatin is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease.
A 2009 study found pitavastatin increased HDL cholesterol, especially in patients with HDL lower than 40 mg/dL, who had a 25% rise, in addition to reducing LDL cholesterol 31%. HDL improved in patients who switched from other statins and rose over time. In the 70-month CIRCLE observational study, pitavastatin increased HDL similar or more than atorvastatin.
It is taken at a dose of 1 to 4 mg per day.
Common statin-related side effects (headaches, stomach upset, abnormal liver function tests and muscle cramps) were similar to other statins. However, pitavastatin seems to lead to fewer muscle side effects than certain statins that are lipid-soluble, as a result of the fact that pitavastatin is water-soluble (as is pravastatin, for example). One study found that coenzyme Q10 was not reduced as much as with certain other statins (though this is unlikely given the inherent chemistry of the HMG-CoA reductase pathway that all statin drugs inhibit).
Metabolism and interactions
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). The primary metabolism pathway of pitavastatin is glucuronidation. It is minimally metabolized by the CYP450 enzymes CYP2C9 and CYP2C8, but not by 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.
Pitavastatin (previously known as itavastatin, itabavastin, nisvastatin, NK-104 or NKS-104) 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. Pitavastatin has been also approved by the Medicines and Healthcare products Regulatory Agency (MHRA) in UK on 17 August 2010.
The drug is marketed in the United States under the trade names Livalo and Zypitamag, and in the European Union and Russia under the trade name Livazo.
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