Anti-hyperlipidemia ( Statins )

 

Anti-hyperlipidemia ( Statins ) 

The mechanism of action of statins is arranged in the following steps:

1- Statins inhibit HMG CoA reductase, which leads to a decrease in intracellular cholesterol concentration.

2- When the concentration of cholesterol is reduced inside the cells, this leads to the manufacture of more Low Density Lipoprotein (LDL) receptors.

3- When cells make too many LDL receptors, this helps cells to uptake LDL from the blood, which leads to a decrease in the concentration of LDL in the blood.

4- Reducing the concentration of cholesterol intercellular cells leads to reducing the secretion of very low density lipoprotein (LDL).

Drugs: 

  1. Atorvastatin 
  2. Fluvastatin 
  3. Lovastatin 
  4. Pitavastatin 
  5. Pravastatin
  6.  Rosuvastatin 
  7. Simvastatin

Pharmacological action: 

1- Statins reduce both triglycerides and low density lipoprotein-C.

2- Statins increase the concentration of High Density Lipoprotein.

3- Statins improve coronary endothelial function.

4- Anti-inflammatory activity. 

5- Statins inhibit platelet thrombus formation.

6- plaque stabilization

The use of statins: 

Statins are used as the first line for patients who suffer from hyperlipidemia with a risk of atherosclerotic cardiovascular disease, or for patients who suffer from hypercholesterolemia (meaning that the cells lack the Low Density Lipoprotein receptors).

Side effect: 

1- elevated liver enzymes 

2- myopathy 

3- rhabdomyolysis 

Drug interactions: 

1- warfarin ( Reason: Statins inhibit platelet thrombus formation, so using statins with warfarin increases the risk of bleeding ) 

2- erythromycin ( The reason: erythromycin causes cytochrome P450 3A4 to inhibit statins, which leads to an increased risk of rhabdomyolysis )

Contraindications: 

1- liver dysfunction 

2- muscle disorder 

3- pregnancy and lactation

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