Pitavastatin

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Pitavastatin
Clinical data
Trade namesLivalo, Livazo, others
AHFS/Drugs.comMonograph
MedlinePlusa610018
License data
Pregnancy
category
  • AU: D
Routes of
administration		By mouth (tablets)
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • CA: ℞-only
  • UK: POM (Prescription only)
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability60%
Protein binding96%
MetabolismLiver (CYP2C9, minimally)
Elimination half-life11 hours
ExcretionFaeces
Identifiers
  • (3R,5S,6E)-7-[2-Cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid
JSmol)
  • O=C(O)C[C@H](O)C[C@H](O)/C=C/c1c(c3ccccc3nc1C2CC2)c4ccc(F)cc4
  • InChI=1S/C25H24FNO4/c26-17-9-7-15(8-10-17)24-20-3-1-2-4-22(20)27-25(16-5-6-16)21(24)12-11-18(28)13-19(29)14-23(30)31/h1-4,7-12,16,18-19,28-29H,5-6,13-14H2,(H,30,31)/b12-11+/t18-,19-/m1/s1 checkY
  • Key:VGYFMXBACGZSIL-MCBHFWOFSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Pitavastatin (usually as a calcium salt) is a member of the blood cholesterol lowering medication class of statins.[1]

Like other statins, it is an inhibitor of HMG-CoA reductase, the enzyme that catalyses the first step of cholesterol synthesis.

It was patented in 1987 and approved for medical use in 2003.[2] It is available in Japan, South Korea and in India.[3] In the US, it received FDA approval in 2009.[4] Kowa Pharmaceuticals, a subsidiary of Kowa Company, is the owner of the American patent to pitavastatin.

Medical uses

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

A 2009 study of the 104-week LIVES trial found pitavastatin increased

LDL cholesterol 31.3%.[5] HDL improved in patients who switched from other statins and rose over time. In the 70-month CIRCLE observational study, pitavastatin increased HDL more than atorvastatin.[6]

It has neutral or possibly beneficial effects on glucose control. As a consequence, pitavastatin is likely to be appropriate for patients with

diabetes mellitus.[citation needed
]

Side effects

Common statin-related side effects (headaches, stomach upset, abnormal

liver function tests and muscle cramps) were similar to other statins.[7] Pitavastatin is a lipophillic statin.[8][9] Reports indicate that this statin may lead to fewer muscle side effects than other statins.[10] 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).[11][12]

As opposed to other statins, there is evidence that pitavastatin improves insulin resistance in humans, with insulin resistance assessed by the homeostatic model assessment (HOMA-IR) method.[13]

Hyperuricemia or increased levels of serum uric acid have been reported with pitavastatin.[14]

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,[15] 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.[11]

History

Pitavastatin (previously known as itavastatin, itabavastin, nisvastatin, NK-104 or NKS-104) was discovered in

Nissan Chemical Industries and developed further by Kowa Pharmaceuticals, Tokyo.[11]
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. Zypitamag (pitavastatin magnesium), a pharmaceutical alternative to Livalo, was approved for use in the United States by the FDA in 2017.

Names

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.

References

  1. PMID 12931254
    .
  2. ISBN 9783527607495
    .
  3. ^ "Zydus Cadila launches pitavastatin in India". Archived from the original on 26 September 2017. Retrieved 28 May 2006.
  4. PMID 20651638
    .
  5. PMID 19907105
    .
  6. PMID 23819752
    .
  7. S2CID 195680129
    .
  8. S2CID 237494271
    .
  9. PMID 34095267
    .
  10. ^ "Alternative Cholesterol-Lowering Drug for Patients Who Can't Tolerate Statins". ScienceDaily. 11 May 2013.
  11. ^
    S2CID 221814440
    .
  12. S2CID 20956339
    .
  13. PMID 26084792
    .
  14. S2CID 30650248
    .
  15. ^ "Livalo". Drugs.com..

External links

Retrieved from "https://en.wikipedia.org/w/index.php?title=Pitavastatin&oldid=1215135245"