セリバスタチンナトリウム

関: cerivastatin

WordNet

a silvery soft waxy metallic element of the alkali metal group; occurs abundantly in natural compounds (especially in salt water); burns with a yellow flame and reacts violently in water; occurs in sea water and in the mineral halite (rock salt) (同)Na, atomic number 11
an oral drug (trade name Baycol) to reduce blood cholesterol levels (同)Baycol

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ソジウム,ナトリウム(金属元素;化学記号はNa)

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/03/23 15:19:51」(JST)

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Cerivastatin (brand names: Baycol, Lipobay) is a synthetic member of the class of statins used to lower cholesterol and prevent cardiovascular disease. It was marketed by the pharmaceutical company Bayer A.G. in the late 1990s, competing with Pfizer's highly successful atorvastatin (Lipitor). Cerivastatin was voluntarily withdrawn from the market worldwide in 2001, due to reports of fatal rhabdomyolysis.

During postmarketing surveillance, 52 deaths were reported in patients using cerivastatin, mainly from rhabdomyolysis and its resultant renal failure.^[1] Risks were higher in patients using fibrates, mainly gemfibrozil (Lopid), and in patients using the highest (0.8 mg/day) dose of cerivastatin. Bayer A.G. added a contraindication for the concomitant use of cerivastatin and gemfibrozil to the package 18 months after the drug interaction was found.^[2] The frequency of deadly cases of rhabdomyolysis with cerivastatin was 16 to 80 times higher than with other statins.^[3] Another 385 nonfatal cases of rhabdomyolysis were reported. This put the risk of this (rare) complication at 5-10 times that of the other statins. Cerivastatin also induced myopathy in a dose-dependent manner when administered as monotherapy, but that was revealed only after Bayer was sued and unpublished company documents were opened.^[4]

References

^ Furberg CD, Pitt B. Withdrawal of cerivastatin from the world market. Curr Control Trials Cardiovasc Med 2001;2:205-207. PMID 11806796.
^ Psaty BM, Furberg CD, Ray WA, Weiss NS (2004). "Potential for conflict of interest in the evaluation of suspected adverse drug reactions: use of cerivastatin and risk of rhabdomyolysis". JAMA 292 (21): 2622–31. doi:10.1001/jama.292.21.2622. PMID 15572720.
^ Zeitlinger M, Müller M (2003). "[Clinico-pharmacologic explanation models of cerivastatin associated rhabdomyolysis]". Wien Med Wochenschr (in German) 153 (11–12): 250–4. doi:10.1046/j.1563-258X.2003.03029.x. PMID 12879633.
^ Saito M, Hirata-Koizumi M, Miyake S, Hasegawa R (2005). "[Withdrawal of cerivastatin revealed a flaw of post-marketing surveillance system in the United States]". Kokuritsu Iyakuhin Shokuhin Eisei Kenkyusho Hokoku (in Japanese) (123): 41–5. PMID 16541751.

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1. 腎集合管ナトリウムチャンネルの遺伝的障害：リドル症候群および偽性低アルドステロン
症1型 genetic disorders of the collecting tubule sodium channel liddles syndrome and pseudohypoaldosteronism type 1
2. バーター症候群およびギテルマン症候群 bartter and gitelman syndromes
3. 低ナトリウム血症患者の評価 evaluation of the patient with hyponatremia
4. 低ナトリウム血症患者におけるナトリウム欠乏の評価 estimation of the sodium deficit in patients with hyponatremia
5. 急性腎障害におけるナトリウムおよび尿素の排泄率 fractional excretion of sodium and urea in acute kidney injury

English Journal

Explication of interactions between HMGCR isoform 2 and various statins through In silico modeling and docking.

Karthik MV, Satya Deepak MV, Shukla P.SourceEnzyme Technology Laboratory, Department of Biotechnology, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, India.
Computers in biology and medicine.Comput Biol Med.2011 Dec 15. [Epub ahead of print]
The enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGCR) catalyzes the conversion of HMG-CoA to mevalonate, a four-electron oxidoreduction that is the rate-limiting step in the synthesis of cholesterol and other isoprenoids. This study was designed to understand the mode of interactions of
PMID 22177940

Association of lower total bilirubin level with statin usage: The United States National Health and Nutrition Examination Survey 1999-2008.

Ong KL, Wu BJ, Cheung BM, Barter PJ, Rye KA.SourceLipid Research Group, Heart Research Institute, 7 Eliza Street, Newtown, Sydney, NSW 2042, Australia.
Atherosclerosis.Atherosclerosis.2011 Dec;219(2):728-33. Epub 2011 Jul 23.
OBJECTIVE: A low circulating level of bilirubin is associated with increased cardiovascular risk. As statins can stimulate heme oxygenase-1 (HO-1), which increases bilirubin production, we investigated whether statins in routine use increase total bilirubin levels in subjects at high cardiovascular
PMID 21840000

Japanese Journal

Effect of cerivastatin sodium, a new inhibitor of HMG-CoA reductase, on plasma lipid levels, progression of atherosclerosis, and the lesional composition in the plaques of WHHL rabbits.

SHIOMI M.
Br J Pharmacol 126, 961-968, 1999
NAID 80010935915

Effect of cerivastatin sodium, a new inhibitor of HMG-CoA reductase, on plasma lipid levels, progression of atherosclerosis, and the lesional composition in the plaques of WHHL rabbits

SHIOMI M
Br J Pharmacol 126, 961-968, 1999
NAID 30022968362

No Interethnic Difference in the Pharmacokinetics of Cerivastatin Sodium, a Novel Anti-hyperlipidemic Agent

河野浩一,MUECK W.,AHR G.,松木孝道
臨床薬理 28(1), 335-336, 1997-03-31
NAID 10011506090

「セリバスタチン」

Cerivastatin
Systematic (IUPAC) name
	(3R,5S,6E)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoic acid
Clinical data
Pregnancy; category	AU: D;
Legal status	Withdrawn from market;
Pharmacokinetic data
Half-life	2–3 hours
Identifiers
CAS Registry Number	145599-86-6
ATC code	C10AA06
PubChem	CID 446156
DrugBank	DB00439
ChemSpider	393588
UNII	AM91H2KS67
KEGG	D07661
ChEBI	CHEBI:3558
ChEMBL	CHEMBL1477
Chemical data
Formula	C26H34FNO5
Molecular mass	459.55 g/mol
	SMILES O=C(O)C[C@H](O)C[C@H](O)/C=C/c1c(nc(c(c1c2ccc(F)cc2)COC)C(C)C)C(C)C;
	InChI InChI=1S/C26H34FNO5/c1-15(2)25-21(11-10-19(29)12-20(30)13-23(31)32)24(17-6-8-18(27)9-7-17)22(14-33-5)26(28-25)16(3)4/h6-11,15-16,19-20,29-30H,12-14H2,1-5H3,(H,31,32)/b11-10+/t19-,20-/m1/s1 ; Key:SEERZIQQUAZTOL-ANMDKAQQSA-N ;
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　　[★]

英: cerivastatin、cerivastatin sodium
関: セリバスタチンナトリウム。Baycol

「セリバスタチンナトリウム」

　　[★]

英: cerivastatin sodium
関: セリバスタチン

「cerivastatin」

　　[★]

セリバスタチン

関: cerivastatin sodium

同: Baycol

[1] Furberg CD, Pitt B. Withdrawal of cerivastatin from the world market. Curr Control Trials Cardiovasc Med 2001;2:205-207. PMID 11806796.

[pmid15572720-2] Psaty BM, Furberg CD, Ray WA, Weiss NS (2004). "Potential for conflict of interest in the evaluation of suspected adverse drug reactions: use of cerivastatin and risk of rhabdomyolysis". JAMA 292 (21): 2622–31. doi:10.1001/jama.292.21.2622. PMID 15572720.

[pmid12879633-3] Zeitlinger M, Müller M (2003). "[Clinico-pharmacologic explanation models of cerivastatin associated rhabdomyolysis]". Wien Med Wochenschr (in German) 153 (11–12): 250–4. doi:10.1046/j.1563-258X.2003.03029.x. PMID 12879633.

[pmid16541751-4] Saito M, Hirata-Koizumi M, Miyake S, Hasegawa R (2005). "[Withdrawal of cerivastatin revealed a flaw of post-marketing surveillance system in the United States]". Kokuritsu Iyakuhin Shokuhin Eisei Kenkyusho Hokoku (in Japanese) (123): 41–5. PMID 16541751.

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cerivastatin sodium