81131-70-6 Usage
Chemical Properties
White Crystalline Powder
Originator
Apo-Pravastatin ,Apotex Inc., Canada
Uses
Different sources of media describe the Uses of 81131-70-6 differently. You can refer to the following data:
1. A competitive inhibitor of HMG-CoA reductase. Bioactive metabolite of Mevastatin
2. Pravastatin sodium is the salt of pravastatin, a ring-opened member of the statin family. Pravastatin is produced biosynthetically from compactin (mevastatin) by a number of microorganisms, notably Absidia, Cunninghamella, Syncephalastrum, Nocardia or Streptomyces. Typically, statins like compactin, lovastatin and simvastatin possess a β-hydroxy lactone ring which is a pro-drug for the readily ring-opened dihydroxyacid generally regarded as the active HMG-CoAreductase inhibitor. Importantly, the free carboxylic acid enables pravastatin to be freely water soluble within biological pH ranges.
3. An HMGCR inhibitor which blocks cholesterol synthesis
Definition
ChEBI: An organic sodium salt that is the sodium salt of pravastatin. A reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA), it is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but
has the advantage of fewer side effects compared with lovastatin and simvastatin.
Brand name
Pravachol
(Bristol-Myers Squibb).
Therapeutic Function
Antihyperlipidemic
General Description
A water-soluble, competitive 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor that potently blocks in vivo cholesterol synthesis (Ki = ~1 nM). Offers cardioprotection. Also acts as an immunomodulator and an inhibitor of ras p21 isoprenylation.
Biological Activity
Water-soluble, competitive inhibitor of 3-hydroxy-3-methyl coenzyme A (HMG-CoA) reductase. Potently blocks cholesterol synthesis in vivo (K i ~ 1 nM) and displays cardioprotective properties.
Biochem/physiol Actions
Primary TargetAMG-CoA reductase
Clinical Use
HMG CoA reductase inhibitor:
Hypercholesterolaemia
Drug interactions
Potentially hazardous interactions with other drugs
Antibacterials: increased risk of myopathy with
daptomycin, fusidic acid (avoid) and telithromycin;
concentration increased by clarithromycin and
erythromycin.
Antivirals: increased risk of myopathy with
atazanavir and boceprevir; concentration possibly
increased by darunavir; concentration reduced by
efavirenz.
Ciclosporin: increased risk of myopathy.
Colchicine: possible increased risk of myopathy.
Lipid lowering agents: increased risk of myopathy
with fibrates, gemfibrozil (avoid) and nicotinic acid.
Metabolism
Pravastatin undergoes extensive hepatic metabolism to a
relatively inactive metabolite. About 70% of an oral dose
of pravastatin is excreted in the faeces, as unabsorbed
drug and via the bile.
references
[1] bolego c, poli a, cignarella a, catapano al, paoletti r. novel statins: pharmacological and clinical results. cardiovasc drugs ther. 2002 may;16(3):251-7.[2] keidar s, aviram m, maor i, oiknine j, brook jg. pravastatin inhibits cellular cholesterol synthesis and increases low density lipoprotein receptor activity in macrophages: in vitro and in vivo studies. br j clin pharmacol. 1994 dec;38(6):513-9.[3] menter dg, ramsauer vp, harirforoosh s, chakraborty k, yang p, hsi l, newman ra, krishnan k. differential effects of pravastatin and simvastatin on the growth of tumor cells from different organ sites. plos one. 2011;6(12):e28813.
Check Digit Verification of cas no
The CAS Registry Mumber 81131-70-6 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 8,1,1,3 and 1 respectively; the second part has 2 digits, 7 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 81131-70:
(7*8)+(6*1)+(5*1)+(4*3)+(3*1)+(2*7)+(1*0)=96
96 % 10 = 6
So 81131-70-6 is a valid CAS Registry Number.
InChI:InChI=1/C23H36O7.Na/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);/q;+1/p-1/t13?,14-,16+,17+,18+,19-,20-,22?;/m0./s1
81131-70-6Relevant articles and documents
CRYSTALLINE FORM OF PRAVASTATINE AND PROCESS FOR THE PREPARATION THEREOF
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Page/Page column 8-9, (2012/07/13)
The present invention relates to a novel form of pravastatin, notably pravastatin sodium, and a method for the preparation of a novel form of pravastatin.
PURIFICATION OF PRAVASTATIN
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Page/Page column 9, (2009/07/03)
The present invention provides a method for the purification of pravastatin or a pharmacologically acceptable salt thereof by treating an aqueous solution comprising pravastatin with a nitrogen-containing base having a pKa value of 12 or higher. Furthermore, the present invention provides a composition comprising pravastatin sodium and 6-epi-pravastatin the quantity of which is 0.2% or less by weight of the composition and 3-α-isopravastatin the quantity of which is 0.2% or less by weight of the composition.
PROCESS FOR THE PREPARATION OF 1,2,6,7,8,8A-HEXAHYDRO-BETA,DELTA,6-TRIHYDROXY-2-METHYL-8-[(2S)-2-METHYL-1-OXOBUTOXY]-, (BETA R,DELTA R,1S,2S,6S,8S,8AR)-1-NAPHTHALENEHEPTANOIC ACID, SODIUM SALT.
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Page/Page column 8, (2008/06/13)
A process for the preparation of substantially pure 1,2,6,7,8,8a-hexahydro-beta,delta,6-trihydroxy-2-methyl-8-[(2S)-2-methyl-1-oxobutoxy]-, (beta R,delta R,1S,2S,6S,8S,8aR)- 1-Naphthaleneheptanoic acid, sodium salt is disclosed.
