How do statins work pharmacology?

Statins act by competitively inhibiting HMG-CoA reductase, the rate-limiting enzyme of the mevalonate pathway. Because statins are similar in structure to HMG-CoA on a molecular level, they will fit into the enzyme’s active site and compete with the native substrate (HMG-CoA).

How does Simvastatin reduce cholesterol?

Statins slow down LDL-cholesterol production by blocking an enzyme called HMG-CoA-Reductase – the medical name for statins is HMG-CoA Reductase inhibitors. Enzymes are proteins in the body which speed up normal processes.

What is the work of simvastatin tablets?

Simvastatin belongs to a group of medicines called statins. It’s used to lower cholesterol if you’ve been diagnosed with high blood cholesterol. It’s also taken to prevent heart disease, including heart attacks and strokes.

Is simvastatin an antagonist or agonist?

Our study provides a chemical rationale for simvastatin as CR3 antagonist and novel ways of understanding how antagonists may modulate the ligand binding kinetics of targeted proteins.

How do statins work biochemistry?

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.

How do statins affect cholesterol synthesis?

In vitro statins act indeed as competitive inhibitors of HMG-CoA reductase (HMGCR), the rate-limiting enzyme of cholesterol synthesis. When statins are bound to HMGCR, they block the access of the natural substrate HMG-CoA to the catalytic site and thereby interfere with cholesterol synthesis (4).

Does rosuvastatin remove plaque from arteries?

By snaking a small ultrasound probe into the coronary arteries, the researchers showed that Crestor reduced the volume of plaque in the arteries by 6.8\%.

Do statins make you pee more?

The study also found that statins were linked to fewer sleep disturbances, but an increase in reports of needing to urinate at night and urinate more frequently, while there were too few reports of cognitive problems to draw any conclusions.

What is the difference between rosuvastatin and simvastatin?

Aside from being better at lowering so-called “bad” cholesterol levels in the bloodstream, another advantage to rosuvastatin is that it has far fewer negative interactions with other medications than simvastatin, or most other statins, for that matter.

What happens if you give simvastatin together with an inhibitor of this enzyme?

Key Messages. Simvastatin and to a lesser extent atorvastatin are metabolised by the hepatic isoenzyme CYP3A4. CYP3A4 inhibitors may increase the plasma concentration of these statins, increasing the risk of adverse reactions such myopathy and/or rhabdomyolysis.

How is simvastatin absorbed?

Simvastatin is well absorbed (about 60–80\%) after oral administration, but it undergoes extensive first-pass metabolism by the hepatic CYP3A4 system [10]. The bioavailability of active HMG-CoA reductase inhibitors following simvastatin tablets is <5\% of the oral dose.