プラバスタチンナトリウム

関: pravastatin

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 Pravachol) administered to reduce blood cholesterol levels; recommended after nonfatal heart attacks (同)Pravachol

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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）』「2013/07/11 16:17:51」(JST)

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Pravastatin (marketed as Pravachol or Selektine) is a member of the drug class of statins, used in combination with diet, exercise, and weight-loss for lowering cholesterol and preventing cardiovascular disease.

Medical uses[edit]

Pravastatin is primarily used for the treatment of dyslipidemia and the prevention of cardiovascular disease.^[1] It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels.^[1]

The evidence for the use of pravastatin is generally weaker than for other statins. The antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT), failed to demonstrate a difference in all-cause mortality or nonfatal myocardial infarction/fatal coronary heart disease rates between patients receiving pravastatin 40mg daily (a common starting dose) and those receiving usual care.^[2]

Adverse effects and contraindications[edit]

Pravastatin has undergone over 112,000 patient-years of double-blind randomized trials utilizing the 40mg once daily dose and placebos. These trials indicate that pravastatin is well tolerated and displays few non-cardiovascular abnormalities in patients.^[3]

However, side effects may occur. A doctor should be consulted if symptoms such as heartburn or headache are severe and do not go away.

The following is a list of uncommon side effects that should be promptly reported to the prescribing doctor or an emergency medical service:^[1]

muscle pain, tenderness, or weakness
lack of energy
fever
jaundice, yellowing of the skin or eyes
pain in the upper right part of the stomach
nausea
extreme tiredness
unusual bleeding or bruising
dark colored urine
loss of appetite
flu-like symptoms
rash
hives
itching
difficulty breathing or swallowing
swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
hoarseness

The following symptoms should be reported to the prescribing doctor if they persist or increase in severity:

heartburn
headache
memory loss or forgetfulness
confusion

Contraindications, conditions that warrant withholding treatment with pravastatin, include pregnancy, and breast feeding.^[4] Taking pravastatin while pregnant could lead to birth defects. While the amount of pravastatin ingested by an infant from breast feeding is low, patients breastfeeding should not take pravastatin due to potential effects on the infant's lipid metabolism.^[5]

Drug Interactions[edit]

Medications that should not be taken with pravastatin include, but are not limited to:^[1]^[4]

Cimetidine (Tagamet); colchicine (Colcrys);
cyclosporine (Neoral, Sandimmune);
ketoconazole (Nizoral);
Additional cholesterol-lowering medications such as: fenofibrate (Tricor), gemfibrozil (Lopid), cholestyramine (Questran, Questran Light, Cholybar) and niacin (nicotinic acid, Niacor, Niaspan);
Specific HIV protease inhibitors such as: lopinavir and ritonavir (Kaletra), and ritonavir (Norvir) taken with darunavir (Prezista); and spironolactone (Aldactone).
Pravastatin is cleared by the kidney giving it a distinct advantage over other statins when there is potential for drug interactions using the hepatic pathway.

Mechanism of action[edit]

Pravastatin acts as a lipoprotein-lowering drug through two pathways. In the major pathway, pravastatin inhibits the function of hydroxymethylglutaryl-CoA (HMG-CoA) reductase. As a reversible competitive inhibitor, pravastatin sterically hinders the action of HMG-CoA reductase by occupying the active site of the enzyme. Taking place primarily in the liver, this enzyme is responsible for the conversion of HMG-CoA to mevalonate in the rate-limiting step of the biosynthetic pathway for cholesterol. Pravastatin also inhibits the synthesis of very-low-density lipoproteins, which are the precursor to low-density lipoproteins (LDL). These reductions increase the number of cellular LDL receptors and, thus, LDL uptake increases, removing it from the bloodstream.^[6] Overall, the result is a reduction in circulating cholesterol and LDL. A minor reduction in triglycerides and an increase in high-density lipoproteins (HDL) are common.

History[edit]

Initially known as CS-514, it was originally identified in a bacterium called Nocardia autotrophica by researchers of the Sankyo Pharma Inc..^[7] It is presently being marketed outside Japan by the pharmaceutical company Bristol-Myers Squibb. In 2005, Pravachol was the 22nd highest-selling brand-name drug in the United States, with sales totaling $1.3 billion.^[8]

The U.S. Food and Drug Administration approved generic pravastatin for sale in the United States for the first time on April 24, 2006. Generic pravastatin sodium tablets are manufactured by Biocon Ltd, India and TEVA Pharmaceuticals in Kfar Sava, Israel.^[8]

References[edit]

^ ^a ^b ^c ^d "Prevachol". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.
^ No Authors Listed (2002). "Major outcomes in moderately hypercholesterolemic, hypertensive patients randomized to pravastatin vs usual care: The Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT-LLT)". JAMA 288 (23): 2998–3007. doi:10.1001/jama.288.23.2998. PMID 12479764.
^ Pfeffer MA, Keech A, Sacks FM, et al. “Safety and tolerability of pravastatin in long-term clinical trials: prospective Pravastatin Pooling (PPP) Project.” Circulation 2002;105:2341-2346
^ ^a ^b Williams, Eni. "Pravachol Side Effects Center". RxList. Retrieved 1 December 2012.
^ "Pravastatin". LactMed. U.S. National Library of Medicine. Retrieved 1 December 2012.
^ Vaughan, C. J., and A. M. Gotto, Jr. 2004. Update on statins: 2003. Circulation 110: 886–892.
^ Yoshino G, Kazumi T, Kasama T, et al. (1986). "Effect of CS-514, an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase, on lipoprotein and apolipoprotein in plasma of hypercholesterolemic diabetics". Diabetes Res. Clin. Pract. 2 (3): 179–81. doi:10.1016/S0168-8227(86)80020-1. PMID 3091343.
^ ^a ^b "FDA Approves First Generic Pravastatin". Retrieved 2008-01-20.

External links[edit]

Pravachol information from the National Institute of Health
Package insert for Pravachol

UpToDate Contents

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1. 心血管疾患または糖尿病患者におけるコレステロール低下に関する臨床試験 clinical trials of cholesterol lowering in patients with cardiovascular disease or diabetes
2. スタチン：作用、副作用、および投与 statins actions side effects and administration
3. スタチン誘発性ミオパチー statin myopathy
4. スタチンと慢性腎臓病 statins and chronic kidney disease
5. 心臓移植後の脂質異常 lipid abnormalities after cardiac transplantation

English Journal

Redox markers and inflammation are differentially affected by atorvastatin, pravastatin or simvastatin administered before endotoxin-induced acute lung injury.

Melo AC, Valença SS, Gitirana LB, Santos JC, Ribeiro ML, Machado MN, Magalhães CB, Zin WA, Porto LC.SourcePrograma de Pós-graduação em Biologia Humana e Experimental, Instituto de Biologia Roberto Alcântara Gomes, Universidade do Estado do Rio de Janeiro, Brazil.
International immunopharmacology.Int Immunopharmacol.2013 Sep;17(1):57-64. doi: 10.1016/j.intimp.2013.05.016. Epub 2013 Jun 6.
Statins are standard therapy for the treatment of lipid disorders, and the field of redox biology accepts that statins have antioxidant properties. Our aim in this report was to consider the pleiotropic effects of atorvastatin, pravastatin and simvastatin administered prior to endotoxin-induced acut
PMID 23747588

Regulation of multidrug resistance protein 2 (MRP2, ABCC2) expression by statins: Involvement of SREBP-mediated gene regulation.

Kobayashi M, Gouda K, Chisaki I, Asada K, Ogura J, Takahashi N, Konishi T, Koshida Y, Sasaki S, Yamaguchi H, Iseki K.SourceLaboratory of Clinical Pharmaceutics & Therapeutics, Division of Pharmasciences, Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12-jo, Nishi-6-chome, Kita-ku, Sapporo 060-0812, Japan.
International journal of pharmaceutics.Int J Pharm.2013 Aug 16;452(1-2):36-41. doi: 10.1016/j.ijpharm.2013.04.019. Epub 2013 Apr 20.
Multidrug resistance protein 2 (MRP2, ABCC2) is localized to the apical membrane of hepatocytes and played an important role in the biliary excretion of a broad range of endogenous and xenobiotic compounds and drugs, such as pravastatin. However, the effects of statins on MRP2 in the liver and the p
PMID 23612356

Rational for statin use in psoriatic patients.

Mosiewicz J, Pietrzak A, Chodorowska G, Trojnar M, Szepietowski J, Reich K, Rizzo M.SourceChair and Department of Internal Medicine, Medical University of Lublin, Lublin, Poland.
Archives of dermatological research.Arch Dermatol Res.2013 Aug;305(6):467-72. doi: 10.1007/s00403-013-1374-1. Epub 2013 Jun 11.
Psoriasis represents a common skin disease which is clinically manifested by chronic cutaneous lesions. It has been observed that psoriasis is associated with an increased risk of cardiovascular diseases, which is contributed to the inappropriate lipid metabolism. Statins are commonly used in clinic
PMID 23754638

Japanese Journal

Complex Formation with Layered Double Hydroxides for the Remediation of Hygroscopicity

Hayashi Aki,Kubota Mai,Okamura Miki,Nakayama Hirokazu
Chemical and Pharmaceutical Bulletin 63(1), 13-17, 2015
… Each type was added to an aqueous or methanol (MeOH) solution containing a drug (pravastatin or nateglinide). … With pravastatin sodium, the interlayer distance expanded after reaction with LDH-NO3 and LDH-Cl in aqueous solution. …
NAID 130004803753

EMP速崩錠の概要と応用事例 : プラバスタチン錠の品質比較評価 (口腔内崩壊製剤特集号) -- (口腔内崩壊錠の製剤設計)

森田豊
製剤機械技術学会誌 = Journal of pharmaceutical machinery and engineering 21(4), 523-534, 2012
NAID 40019505607

h-CLATを用いた医薬品のアレルゲン性評価

黒瀬光一,宇梶真帆,斎藤嘉朗,打田光宏,土屋敏行
日本毒性学会学術年会 39.1(0), P-209, 2012
… 】試験を試みた医薬品17物質のうちh-CLATのアッセイ要件を満たしたものは11物質（ampicillin sodium，D-penicillamine，ticlopidine hydrochloride，cephalothin sodium，diclofenac sodium，levofloxacin hydrochloride，gefitinib，albendazole，amiodarone hydrochloride，carbamazepine，pravastatin sodium）であり，これらはいずれも陽性判定となった．他の6物質（いずれも脂溶性物質）につい …
NAID 130005008815

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リンク元

「プラバスタチン」

Pravastatin
Systematic (IUPAC) name
	(3R,5R)-3,5-dihydroxy-7-((1R,2S,6S,8R,8aR)-6-hydroxy-2-methyl-8-{[(2S)-2-methylbutanoyl]oxy}-1,2,6,7,8,8a-hexahydronaphthalen-1-yl)-heptanoic acid
Clinical data
Trade names	Pravachol
AHFS/Drugs.com	monograph
MedlinePlus	a692025
Pregnancy cat.	X
Legal status	℞ Prescription only
Routes	oral
Pharmacokinetic data
Bioavailability	17%
Protein binding	50%
Metabolism	renal and hepatic
Half-life	1.5-2 hours
Identifiers
CAS number	81093-37-0
ATC code	C10AA03
PubChem	CID 54687
DrugBank	DB00175
ChemSpider	49398
UNII	KXO2KT9N0G
ChEMBL	CHEMBL1144
Chemical data
Formula	C23H36O7
Mol. mass	424.528 g/mol
	SMILES O=C(O)C[C@H](O)C[C@H](O)CC[C@H]2[C@H](/C=C\C1=C\[C@@H](O)C[C@H](OC(=O)[C@@H](C)CC)[C@@H]12)C;
	InChI InChI=1S/C23H36O7/c1-4-13(2)23(29)30-20-11-17(25)9-15-6-5-14(3)19(22(15)20)8-7-16(24)10-18(26)12-21(27)28/h5-6,9,13-14,16-20,22,24-26H,4,7-8,10-12H2,1-3H3,(H,27,28)/t13-,14-,16+,17+,18+,19-,20-,22-/m0/s1 ; Key:TUZYXOIXSAXUGO-PZAWKZKUSA-N ;
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　　[★]

英: pravastatin
化: プラバスタチンナトリウム pravastatin sodium
商: アルセチン、コレリット、タツプラミン、プラバスタン、プラバチン、プラバピーク、プラバメイト、プラメバン、プロバチン、マイバスタン、メバトルテ、メバリッチ、メバリリン、メバレクト、メバロチン、メバン、リダックM
関: HMG-CoA還元酵素阻害薬; 高脂血症用剤

[AHFS-1] "Prevachol". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.

[2] No Authors Listed (2002). "Major outcomes in moderately hypercholesterolemic, hypertensive patients randomized to pravastatin vs usual care: The Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT-LLT)". JAMA 288 (23): 2998–3007. doi:10.1001/jama.288.23.2998. PMID 12479764.

[3] Pfeffer MA, Keech A, Sacks FM, et al. “Safety and tolerability of pravastatin in long-term clinical trials: prospective Pravastatin Pooling (PPP) Project.” Circulation 2002;105:2341-2346

[RxList-4] Williams, Eni. "Pravachol Side Effects Center". RxList. Retrieved 1 December 2012.

[LactMed-5] "Pravastatin". LactMed. U.S. National Library of Medicine. Retrieved 1 December 2012.

[6] Vaughan, C. J., and A. M. Gotto, Jr. 2004. Update on statins: 2003. Circulation 110: 886–892.

[pmid3091343-7] Yoshino G, Kazumi T, Kasama T, et al. (1986). "Effect of CS-514, an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase, on lipoprotein and apolipoprotein in plasma of hypercholesterolemic diabetics". Diabetes Res. Clin. Pract. 2 (3): 179–81. doi:10.1016/S0168-8227(86)80020-1. PMID 3091343.

[fda_announcement-8] "FDA Approves First Generic Pravastatin". Retrieved 2008-01-20.

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案内

pravastatin sodium