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:
- Atorvastatin
- Fluvastatin
- Lovastatin
- Pitavastatin
- Pravastatin
- Rosuvastatin
- 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