関: Statins.

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/04/30 23:53:18」(JST)

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Pitavastatin (usually as a calcium salt) is a member of the blood cholesterol lowering medication class of statins,^[1] marketed in the United States under the trade name Livalo. Like 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] In the US, it received FDA approval in 2009.^[4]

Uses

Like the other statins, pitavastatin 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%).^[5] As a consequence, pitavastatin is most likely to be appropriate for patients with metabolic syndrome with high LDL, low HDL and diabetes mellitus.

Side effects

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).^[6] 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).^[3]^[7]

Hyperuricemia or increased levels of serum uric acid have been reported with pitavastatin.^[8]

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). As a result, pitavastatin 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.^[3]

History

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.^[3] 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.

References

^ Kajinami, K; Takekoshi, N; Saito, Y (2003). "Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor". Cardiovascular drug reviews 21 (3): 199–215. PMID 12931254. edit
^ Zydus Cadila launches pitavastatin in India
^ ^a ^b ^c ^d Mukhtar, R. Y. A.; Reid, J.; Reckless, J. P. D. (2005). "Pitavastatin". International Journal of Clinical Practice 59 (2): 239–252. doi:10.1111/j.1742-1241.2005.00461.x. PMID 15854203. edit
^ The Seventh Statin; Pitavastatin
^ http://www.ncbi.nlm.nih.gov/pubmed/19907105
^ ScienceDaily (11 May 2013). "Alternative Cholesterol-Lowering Drug for Patients Who Can't Tolerate Statins". ScienceDaily.
^ Clin Pharmacol Ther. 2008 May;83(5):731-9. Epub 2007 Oct 24. Comparison of effects of pitavastatin and atorvastatin on plasma coenzyme Q10 in heterozygous familial hypercholesterolemia: results from a crossover study. Kawashiri MA, Nohara A, Tada H, Mori M, Tsuchida M, Katsuda S, Inazu A, Kobayashi J, Koizumi J, Mabuchi H, Yamagishi M.
^ Ogata, N.; Fujimori, S.; Oka, Y.; Kaneko, K. (2010). "Effects of Three Strong Statins (Atorvastatin, Pitavastatin, and Rosuvastatin) on Serum Uric Acid Levels in Dyslipidemic Patients". Nucleosides, Nucleotides and Nucleic Acids 29 (4–6): 321. doi:10.1080/15257771003741323. edit

External links

FDA approval history

UpToDate Contents

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English Journal

Pharmacokinetic Properties of Single- and Multiple-Dose Pitavastatin Calcium Tablets in Healthy Chinese Volunteers.

Luo Z1, Zhang Y2, Gu J2, Feng P1, Wang Y1.
Current therapeutic research, clinical and experimental.Curr Ther Res Clin Exp.2015 Mar 3;77:52-7. doi: 10.1016/j.curtheres.2015.02.001. eCollection 2015.
BACKGROUND: Pitavastatin is a newly developed 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor approved for the treatment of hyperlipidemia. Pharmacokinetic properties of pitavastatin have been studied previously.OBJECTIVE: To investigate the pharmacokinetic properties of pitavastatin in he
PMID 26082816

Pitavastatin attenuates monocyte activation in response to orthopedic implant‑derived wear particles by suppressing the NF‑κB signaling pathway.

Zhang Z1, Dai F1, Cheng P1, Luo F1, Hou T1, Zhou Q1, Xie Z1, Deng M2, Xu JZ1.
Molecular medicine reports.Mol Med Rep.2015 Nov;12(5):6932-8. doi: 10.3892/mmr.2015.4306. Epub 2015 Sep 9.
Aseptic loosening secondary to particle‑induced periprosthetic osteolysis is considered to be the primary cause of long‑term implant failure in orthopedic surgery. Implant‑derived wear particles activate and recruit macrophages and osteoclasts, which cause a persistent inflammatory response wi
PMID 26352276

Statin action favours normalisation of the plasma lipidome in the atherogenic mixed dyslipidemia of metabolic syndrome: Potential relevance to statin-associated dysglycemia.

Meikle PJ1, Wong G2, Tan R2, Giral P3, Robillard P3, Orsoni A3, Hounslow N4, Magliano DJ2, Shaw J2, Curran JE5, Blangero J5, Kingwell BA2, Chapman MJ3.
Journal of lipid research.J Lipid Res.2015 Oct 20. pii: jlr.P061143. [Epub ahead of print]
The impact of statin treatment on the abnormal plasma lipidome of mixed dyslipidemic patients with Metabolic syndrome (MetS), a group at increased risk of developing diabetes, was evaluated. Insulin-resistant, hypertriglyceridemic, hypertensive, obese males (n=12) displaying MetS were treated with p
PMID 26486974

Japanese Journal

Statins Induce the Gene Expression of Apolipoprotein A5 in HepG2 Cells

Arishima Hiroaki,Matsunaga Akira,Uehara Yoshinari,Niimura Hideya,Zhang Bo,Ohwaki Kazuo,Hayashida Kazue,Yoshimizu Kayo,Saku Keijiro
福岡大学医学紀要 38(4), 161-169, 2011-12
NAID 110008720006

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竹内利治,太田久宣,長谷部直幸
日本臨床 69 (1010増刊9), 336-340, 2011-11
NAID 40019062274

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リンク元	「ピタバスタチン」
拡張検索	「pitavastatin calcium」

「ピタバスタチン」

Pitavastatin
Systematic (IUPAC) name
	(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid
Clinical data
Trade names	Livalo
AHFS/Drugs.com	monograph
MedlinePlus	a610018
Licence data	US FDA:link
Pregnancy cat.	D (AU) X (US)
Legal status	Prescription Only (S4) (AU) ℞-only (CA) POM (UK) ℞-only (US)
Routes	Oral
Pharmacokinetic data
Bioavailability	60%
Protein binding	96%
Metabolism	minimally CYP2C9
Half-life	11 hours
Excretion	Faeces
Identifiers
CAS number	147511-69-1
ATC code	C10AA08
PubChem	CID 5282452
ChemSpider	4445604
UNII	M5681Q5F9P
ChEBI	CHEBI:32020
ChEMBL	CHEMBL1201753
Chemical data
Formula	C25H24FNO4
Mol. mass	421.461
	SMILES O=C(O)C[C@H](O)C[C@H](O)/C=C/c1c(c3ccccc3nc1C2CC2)c4ccc(F)cc4;
	InChI 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 ; Key:VGYFMXBACGZSIL-MCBHFWOFSA-N ;
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英: pitavastatin
化: ピタバスタチンカルシウム pitavastatin calcium
商: リバロ
関: スタチン

「pitavastatin calcium」

　　[★] ピタバスタチン。ピタバスタチンカルシウム

[Kajinami-1] Kajinami, K; Takekoshi, N; Saito, Y (2003). "Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor". Cardiovascular drug reviews 21 (3): 199–215. PMID 12931254. edit

[Zydus-2] Zydus Cadila launches pitavastatin in India

[Mukhtar-3] Mukhtar, R. Y. A.; Reid, J.; Reckless, J. P. D. (2005). "Pitavastatin". International Journal of Clinical Practice 59 (2): 239–252. doi:10.1111/j.1742-1241.2005.00461.x. PMID 15854203. edit

[Seventh-4] The Seventh Statin; Pitavastatin

[5] ttp://www.ncbi.nlm.nih.gov/pubmed/19907105

[6] ScienceDaily (11 May 2013). "Alternative Cholesterol-Lowering Drug for Patients Who Can't Tolerate Statins". ScienceDaily.

[7] Clin Pharmacol Ther. 2008 May;83(5):731-9. Epub 2007 Oct 24. Comparison of effects of pitavastatin and atorvastatin on plasma coenzyme Q10 in heterozygous familial hypercholesterolemia: results from a crossover study. Kawashiri MA, Nohara A, Tada H, Mori M, Tsuchida M, Katsuda S, Inazu A, Kobayashi J, Koizumi J, Mabuchi H, Yamagishi M.

[8] Ogata, N.; Fujimori, S.; Oka, Y.; Kaneko, K. (2010). "Effects of Three Strong Statins (Atorvastatin, Pitavastatin, and Rosuvastatin) on Serum Uric Acid Levels in Dyslipidemic Patients". Nucleosides, Nucleotides and Nucleic Acids 29 (4–6): 321. doi:10.1080/15257771003741323. edit

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pitavastatin