| 词条 | Pravastatin |
| 释义 |
| Verifiedfields = changed | verifiedrevid = 464213376 | IUPAC_name = (3R,5R)-3,5-dihydroxy-7-((1R,2S,6S,8R,8aR)-6-hydroxy-2-methyl-8[(2S)-2-methylbutanoyl]oxy1,2,6,7,8,8a-hexahydronaphthalen-1-yl)-heptanoic acid | image = Pravastatin.svg | width = 181 | tradename = Pravachol, Selektine, other | Drugs.com = {{drugs.com|monograph|pravastatin-sodium}} | MedlinePlus = a692025 | pregnancy_AU = D | pregnancy_US = X | legal_AU = S4 | legal_CA = Rx-only | legal_UK = POM | legal_US = Rx-only | legal_status = | routes_of_administration = By mouth | bioavailability = 18%[1] | protein_bound = 50%[1] | metabolism = Liver (minimal)[1] | elimination_half-life = 1-3 hours[1] | IUPHAR_ligand = 2953 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 81093-37-0 | ATC_prefix = C10 | ATC_suffix = AA03 | ATC_supplemental = | PubChem = 54687 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00175 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 49398 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = KXO2KT9N0G | ChEBI_Ref = {{ebicite|changed|EBI}} | ChEBI = 63618 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 1144 | C=23 | H=36 | O=7 | molecular_weight = 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 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 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 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = TUZYXOIXSAXUGO-PZAWKZKUSA-N }}Pravastatin, sold under the brand name Pravachol among others, is a statin medication, used preventing cardiovascular disease in those at high risk and treating abnormal lipids.[5] It should be used together with diet changes, exercise, and weight loss.[5] It is taken by mouth.[2] Common side effects include joint pain, diarrhea, nausea, headaches, and muscle pains.[2] Serious side effects may include rhabdomyolysis, liver problems, and diabetes.[2] Use during pregnancy may harm the baby.[2] Like all statins, pravastatin works by inhibiting HMG-CoA reductase, an enzyme found in liver that plays a role in producing cholesterol.[2] Pravastatin was patented in 1980 and approved for medical use in 1989.[3] It is available as a generic medication.[2] In the United States the wholesale cost per dose is less than 0.20 USD as of 2018.[4] In the United Kingdom it costs the NHS about a pound per dose.[5] In 2016 it was the 27th most prescribed medication in the United States with more than 24 million prescriptions.[6] Medical usesPravastatin is primarily used for the treatment of dyslipidemia and the prevention of cardiovascular disease.[7] It is recommended to be used only after other measures, such as diet, exercise, and weight reduction, have not improved cholesterol levels.[7] 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 40 mg daily (a common starting dose) and those receiving usual care.[8] Adverse effects and contraindicationsPravastatin has undergone over 112,000 patient-years of double-blind, randomized trials using the 40-mg, once-daily dose and placebos. These trials indicate pravastatin is well tolerated and displays few noncardiovascular abnormalities in patients.[9] However, side effects may occur. A doctor should be consulted if symptoms such as heartburn or headache are severe and do not go away. These uncommon side effects should be promptly reported to the prescribing doctor or an emergency medical service:[7]
These symptoms should be reported to the prescribing doctor if they persist or increase in severity:
Drug interactionsMedications that should not be taken with pravastatin include, but are not limited to:[7][10]
Pravastatin is cleared by the kidneys, giving it a distinct advantage over other statins when a potential for drug interactions using the hepatic pathway exists. Mechanism of actionPravastatin 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, thus LDL uptake increases, removing it from the bloodstream.[12] 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. HistoryInitially known as CS-514, pravastatin is a derivative of ML236B (compactin), which was identified in a fungus called Penicillium citrinum in the 1970s by researchers of the Sankyo Pharma Inc.[13] It is 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.[14] 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.[14] References1. ^1 2 3 {{cite journal | vauthors = Neuvonen PJ, Backman JT, Niemi M | title = Pharmacokinetic comparison of the potential over-the-counter statins simvastatin, lovastatin, fluvastatin and pravastatin | journal = Clinical Pharmacokinetics | volume = 47 | issue = 7 | pages = 463–74 | date = 2008 | pmid = 18563955 | doi = 10.2165/00003088-200847070-00003 }} 2. ^1 2 3 4 5 6 7 {{cite web |title=Pravastatin Sodium Monograph for Professionals |url=https://www.drugs.com/monograph/pravastatin-sodium.html |website=Drugs.com |publisher=AHFS |accessdate=23 December 2018 |language=en}} 3. ^{{cite book|last1=Fischer|first1=Janos|last2=Ganellin|first2=C. Robin|title=Analogue-based Drug Discovery|date=2006|publisher=John Wiley & Sons|isbn=9783527607495|page=472|url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA472|language=en}} 4. ^{{cite web |title=NADAC as of 2018-12-19 |url=https://data.medicaid.gov/Drug-Pricing-and-Payment/NADAC-as-of-2018-12-19/g7bs-ahj4 |website=Centers for Medicare and Medicaid Services |accessdate=22 December 2018 |language=en}} 5. ^{{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|page=202|edition=76}} 6. ^{{cite web |title=The Top 300 of 2019 |url=https://clincalc.com/DrugStats/Top300Drugs.aspx |website=clincalc.com |accessdate=22 December 2018}} 7. ^1 2 3 {{cite web|title=Pravachol|url=https://www.drugs.com/monograph/pravachol.html|work=The American Society of Health-System Pharmacists|access-date=3 April 2011}} 8. ^{{cite journal | author = ALLHAT Officers and Coordinators for the ALLHAT Collaborative Research Group. The Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial | title = 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) | journal = JAMA | volume = 288 | issue = 23 | pages = 2998–3007 | date = December 2002 | pmid = 12479764 | doi = 10.1001/jama.288.23.2998 }} 9. ^{{cite journal | vauthors = Pfeffer MA, Keech A, Sacks FM, Cobbe SM, Tonkin A, Byington RP, Davis BR, Friedman CP, Braunwald E | title = Safety and tolerability of pravastatin in long-term clinical trials: prospective Pravastatin Pooling (PPP) Project | journal = Circulation | volume = 105 | issue = 20 | pages = 2341–6 | date = May 2002 | pmid = 12021218 | doi = | url = }} 10. ^1 {{cite web|last=Williams|first=Eni | name-list-format = vanc |title=Pravachol Side Effects Center|url=http://www.rxlist.com/pravachol-side-effects-drug-center.htm|publisher=RxList|access-date=1 December 2012}} 11. ^{{cite web|title=Pravastatin|url=http://toxnet.nlm.nih.gov/cgi-bin/sis/search/f?./temp/~MNhuQa:1|work=LactMed|publisher=U.S. National Library of Medicine|access-date=1 December 2012}} 12. ^{{cite journal | vauthors = Vaughan CJ, Gotto AM | title = Update on statins: 2003 | journal = Circulation | volume = 110 | issue = 7 | pages = 886–92 | date = August 2004 | pmid = 15313959 | doi = 10.1161/01.CIR.0000139312.10076.BA }} 13. ^{{cite journal | vauthors = Tobert JA | title = Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors | journal = Nature Reviews. Drug Discovery | volume = 2 | issue = 7 | pages = 517–26 | date = July 2003 | pmid = 12815379 | doi = 10.1038/nrd1112 }} 14. ^1 {{cite web |url=http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/2006/ucm108644.htm |title=FDA Approves First Generic Pravastatin |access-date=2008-01-20 |work=}} External links
9 : Statins|Bristol-Myers Squibb|Daiichi Sankyo|Diols|Carboxylic acids|Carboxylate esters|Naphthalenes|Beta hydroxy acids|RTT |
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