Pitavastatin

Pitavastatin (usually as a calcium salt) is a novel member of the medication class of statins.^[1] Like the other statins, it is an inhibitor of HMG-CoA reductase, the enzyme that catalyses the first step of cholesterol synthesis. It has been available in Japan since 2003, and is being marketed under licence in South Korea and in India.^[2] It is likely that pitavastatin will be approved for use in hypercholesterolaemia (elevated levels of cholesterol in the blood) and for the prevention of cardiovascular disease outside South and Southeast Asia as well.^[3]

Additional recommended knowledge

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Uses

Like the other statins, pitavastatin is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease.

Side-effects

Common statin-related side-effects (headaches, stomach upset, abnormal liver function tests and muscle cramps) were similar to other statins.^[3]

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). Pitavastatin appears to be a substrate of CYP2C9, and not CYP3A4 (which is a common source of interactions in other statins).^[3]

History

Pitavastatin (previously known as itavastatin, itabavastin, nisvastatin, NK-104 or NKS-104) was discovered in Japan by Nissan Chemical Industries, Ltd. and developed further by Kowa Pharmaceuticals, Tokyo.^[3]

References

1. ^ Kajinami K, Takekoshi N, Saito Y. Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor. Cardiovasc Drug Rev 2003;21:199-215. PMID 12931254.
2. ^ Zydus Cadila launches pitavastatin in India
3. ^ ^{a b c d} Mukhtar RY, Reid J, Reckless JP. Pitavastatin. Int J Clin Pract 2005;59:239-52. PMID 15854203.