What is the mechanism of action of HMG-CoA reductase inhibitors?
HMG-CoA reductase inhibitors block the enzyme HMG-CoA reductase that is responsible for synthesizing cholesterol in the liver. Statins competitively inhibit the HMG-CoA reductase enzyme. Statins bind to the active site of the enzyme and change its structure.
What is the mechanism of the cholesterol lowering agents HMG-CoA reductase inhibitors?
Drug, Indications, Mechanism of Action, and Pharmacology Statins inhibit HMG-CoA reductase, thwarting the formation of the rate-limiting mevalonate; consequently, plasma low-density lipoprotein (LDL) clearance is increased, and hepatic very-low-density lipoprotein (VLDL) and LDL production is decreased.
What happens if HMG-CoA reductase is inhibited?
Inhibition of HMG-CoA reductase, a rate-limiting enzyme in hepatic cholesterol synthesis by statins, results in the reduction of intracellular cholesterol content that in turn induces an increase in SREBP-2-mediated hepatic LDL receptor synthesis (Sahebkar and Watts, 2013b) (Chapter 11).
What does HMG-CoA reductase do?
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]).
What is the mechanism of action for statins?
Mechanism of Action Statins work by competitively blocking the active site of the first and key rate-limiting enzyme in the mevalonate pathway, HMG-CoA reductase. Inhibition of this site prevents substrate access, thereby blocking the conversion of HMG-CoA to mevalonic acid.
What lab results should be monitored when someone is taking an HMG-CoA reductase inhibitor?
Monitor lipid profile, liver function tests, creatine kinase (CK), and thyroid function tests in individuals who start statin treatment: Lipid profile: Perform a lipid profile at baseline before initiating statins. The lipid panel should be repeated two months after starting the therapy.
What lab results should be monitored when someone is taking an HMG CoA reductase inhibitor?
How do you reduce HMG-CoA reductase?
The two therapies that have been researched to reduce myalgias in patients taking statin therapy (HMG CoA reductase inhibitors) are coenzyme Q10, or CoQ10, and vitamin D.
Why is HMG-CoA reductase a good drug target?
The inhibition of HMG-CoA reductase effectively lowers the level of cholesterol in humans and most animals by the activation of sterol-regulatory element-binding protein-2 (SREBP-2) which upregulates the HMG-CoA reductase and LDL receptor that lead to the reduction of cholesterol levels [4].
Where is HMG-CoA reductase found in the body?
In humans, the gene for HMG-CoA reductase (NADPH) is located on the long arm of the fifth chromosome (5q13. 3-14). Related enzymes having the same function are also present in other animals, plants and bacteria.