81131-70-6 Usage
Description
Pravastatin sodium is a water-soluble, competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, derived from the statin family. It is a bioactive metabolite of Mevastatin and is produced biosynthetically from compactin (mevastatin) by various microorganisms. As a reversible inhibitor, it potently blocks in vivo cholesterol synthesis and offers cardioprotection while also acting as an immunomodulator and an inhibitor of ras p21 isoprenylation. Pravastatin sodium is one of the lower potency statins but has the advantage of fewer side effects compared to other statins like lovastatin and simvastatin. It is a white crystalline powder and is commercially available under the brand name Pravachol by Bristol-Myers Squibb.
Uses
Used in Pharmaceutical Industry:
Pravastatin sodium is used as a cholesterol-lowering agent for the prevention and treatment of cardiovascular diseases. It works by inhibiting HMG-CoA reductase, an enzyme involved in cholesterol synthesis, thus reducing the levels of low-density lipoprotein (LDL) cholesterol, total cholesterol, and triglycerides in the blood.
Used in Cardiovascular Health:
Pravastatin sodium is used as a cardioprotective agent to reduce the risk of heart attacks, strokes, and other cardiovascular events in patients with high cholesterol levels or a history of cardiovascular disease.
Used in Immunomodulation:
Pravastatin sodium is used as an immunomodulator to modulate the immune system and potentially treat various immune-related disorders.
Used in Ras p21 Isoprenylation Inhibition:
Pravastatin sodium is used as an inhibitor of ras p21 isoprenylation, which is involved in cell growth and proliferation. This property makes it a potential candidate for the treatment of certain types of cancer.
Used in Drug Development:
Pravastatin sodium serves as a starting point for the development of new drugs with improved potency, selectivity, and reduced side effects in the treatment of hypercholesterolemia and related conditions.
Originator
Apo-Pravastatin ,Apotex Inc., Canada
Therapeutic Function
Antihyperlipidemic
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
-
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
-
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.
-
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.
