Pravastatin sodium

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

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.

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).

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.