Are statins HMG-CoA reductase inhibitors?

HMG-CoA reductase inhibitors (statins) are lipid-lowering medications used in the primary and secondary prevention of coronary heart disease. This activity reviews the indications, contraindications, and mechanism of action of statins for the management of coronary heart disease and familial dyslipidemias.

Why do statins inhibit HMG-CoA reductase?

Statins competitively inhibit the HMG-CoA reductase enzyme. Statins bind to the active site of the enzyme and change its structure. As the structure of the enzyme is changed, it cannot bind with the receptor, thus its activity is reduced.

Which statin is the most effective at inhibiting HMG-CoA reductase?

With these structural properties, rosuvastatin has the most efficient effect to reduce the activity of HMG-CoA reductase enzyme by 50% (6, 7). Pravastatin and rosuvastatin are more hydrophilic due to the polar hydroxyl group and methane sulphonamide group, respectively.

What does HMG-CoA reductase do?

Cholesterol Precursors. HMG-CoA reductase is the rate-limiting enzyme of cholesterol biosynthesis. The expression level of this membrane-bound enzyme is controlled by many factors that in turn regulate cholesterol synthesis and cellular cholesterol homeostasis (reviewed in [1]).

Which cholesterol drug is safest?

Simvastatin and pravastatin had the best safety profile, according to this review. Overall, the researchers found a 9 percent increased risk of type 2 diabetes in people taking statins.

What medicines have statins?

Statins that are approved for use in the U.S. include:

• atorvastatin (Lipitor),
• fluvastatin (Lescol, Lescol XL),
• lovastatin (Mevacor, Altoprev),
• pravastatin (Pravachol),
• rosuvastatin (Crestor),
• simvastatin (Zocor), and.
• pitavastatin (Livalo).

How do you reduce HMG-CoA reductase?

HMG coenzyme-A reductase inhibitors Statins inhibit HMG-CoA reductase and reduce cellular cholesterol synthesis [1]. Lower intracellular cholesterol concentrations cause over-expression of the LDL receptor in the plasma membrane of hepatocytes.

Where do Statins bind?

Statins act by competitively binding to the catalytic domain of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase, HMGCR)8,9 and blocking the conversion of HMG-CoA to mevalonate, the rate-limiting step of cholesterol biosynthesis.

Which is better Lipitor or Crestor?

The study concluded that Crestor lowered LDL cholesterol by 8.2% more than Lipitor, and Crestor lowered total cholesterol significantly more than all the other statins studied. Crestor also increased HDL cholesterol (the good kind of cholesterol) more than Lipitor did.

How is HMG-CoA regulated?

Regulation of HMG-CoA reductase occurs at 4 different levels of feedback regulation. The second level of regulation is at the translation of the HMGR mRNA, which is inhibited by Farnesol, a derivative of the mevalonate pathway. The third level of HMGR regulation involves the degradation of intact reductase.

How are statins used to inhibit HMG-CoA reductase?

Statins act by inhibiting 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and thereby reducing cholesterol synthesis. In X-ray crystallographic studies, we have determined the structures of the catalytic portions of the enzyme in complex with statin molecules.

Why is HMG CoA reductase suppressed in mammals?

Normally in mammalian cells this enzyme is competitively suppressed so that its effect is controlled. This enzyme is the target of the widely available cholesterol-lowering drugs known collectively as the statins, which help treat dyslipidemia .

What kind of enzyme are Statins supposed to inhibit?

Statins inhibit an enzyme called HMG-CoA reductase …. so they’re known as HMG-CoA reductase inhibitors ( hydroxymethylglutaryl – coenzyme A reductase). HMG-CoA reductase is an enzyme that is a major player with cholesterol synthesis in the liver.

How do statins lower cholesterol levels in the blood?

Prava statin etc. How do statins lower cholesterol levels in the blood? Statins inhibit an enzyme called HMG-CoA reductase …. so they’re known as HMG-CoA reductase inhibitors ( hydroxymethylglutaryl – coenzyme A reductase). HMG-CoA reductase is an enzyme that is a major player with cholesterol synthesis in the liver.