In fact, usually, before intervening with drug therapy, an attempt is made to restore cholesterol values through diet and physical activity. If this is not enough, the doctor may deem it necessary to intervene with the administration of lipid-lowering or cholesterol-lowering drugs.
Therefore, after a brief introduction, the main types of drugs used to lower blood cholesterol levels will be briefly described below.
- the objective of restoring the lipid structure to acceptable values fails. In this regard, it is very important to clarify the fact that:
Medicines for high cholesterol should not replace the correction of lifestyle (diet and physical activity), but be associated with it.
In other words, the use of cholesterol-lowering drugs must not lead the patient to believe that, by taking them, he can adopt an unregulated and high-fat diet and / or that he can abandon physical activity.
The values of cholesterol in the blood beyond which it is necessary to adopt a drug therapy vary from patient to patient, in relation to the individual cardiovascular risk. High-risk patients, for example, may need these drugs even if they have cholesterol values total lower than other subjects in whom drug therapy is not necessary.
Before prescribing these drugs, therefore, the doctor will evaluate factors such as the patient's age, HDL good cholesterol values and their relationship with total or LDL cholesterol, smoking habits, blood glucose and blood pressure values, weight body and the presence of underlying cardiovascular disease.
against High CholesterolStatins are a class of drugs widely used for the treatment of high cholesterol. Among the active ingredients belonging to this class of drugs we mention:
- Simvastatin (Zocor®, Alpheus®, Goltor®, Inegy®, Sinvacor®, Sivastin®, Vytorin®, Cholib®);
- L "atorvastatin (Arkast®, Torvast®, Totalip®);
- Lovastatin (Lovinacor®, Restat®, Tavacor®);
- Pravastatin (Pravafenix®, Selectin®, Aplactin®);
- Rosuvastatin (Simestat®, Cholecomb®, Crestor®);
- Fluvastatin (Lescol®).
Statins can be used either alone, on their own, or in combination therapy with fibrate drugs or with ezetimibe.
Mechanism of action
Statins exert their cholesterol-lowering action through the inhibition of the enzyme 3-hydroxy-3-metiglutaryl coenzyme A reductase (HMG-CoA reductase). This enzyme is responsible for the conversion of 3-hydroxy-3-methylglutaryl coenzyme A into mevalonate, a fundamental precursor in the biosynthesis of sterols, including cholesterol.In particular, statins hinder the production of cholesterol in the liver
Additionally, these types of high cholesterol medications are also capable of:
- Promote the increase in the number of LDL receptors on the cell surface, consequently leading to an increase in LDL uptake and catabolism.
- Reduce plasma triglyceride levels.
Side effects
Generally, statins are well tolerated, although like any other drug they can still cause side effects. Among these, we mention the main ones:
- Allergic reactions in sensitive individuals;
- Gastrointestinal disorders;
- Weakness and muscle aches;
- Headache;
- Changes in taste
- Skin disorders.
Fibrate drugs represent another pharmaceutical class widely used to reduce cholesterol and triglycerides in the blood. To tell the truth, this class of drugs is mainly used to reduce triglyceridemia and, to a lesser extent, to reduce hypercholesterolemia.
In any case, among the active ingredients belonging to this class of drugs for high cholesterol, we find:
- Fenofibrate (Fulcro®, Fulcrosupra®, Lipsin®, Pravafenix®);
- The gemfibrozil (Lopid®);
- Bezafibrate (Bezalip®).
Fibrates can be used either alone or in combination with statins (a practice which however raises some doubts regarding the safety of use).
Mechanism of action
The exact "mechanism of action" by which these high cholesterol drugs perform their activity has not yet been fully understood. Despite this, it has been shown that fibrates:
- They significantly reduce VLDL (Very Low Density Lipoproteins,
high triglyceride lipoproteins); - They induce a moderate increase in HDL (High Density Lipoproteins, also known as "good cholesterol", these are lipoproteins with a very low triglyceride content but high in cholesterol);
- They produce variable effects on LDL (Low Density Lipoproteins, lipoproteins with a low triglyceride content but containing higher quantities of cholesterol).
Side effects
Among the side effects that can occur with the intake of fibrates, we remember:
- Allergic reactions in sensitive individuals;
- Headache;
- Gastrointestinal disorders;
- Liver disorders;
- Pancreatitis;
- Blood disorders.
Among the different resins that sequester bile acids still on the market (February 2019) we find cholestyramine (Questran®). It is an anion exchange resin in hydrochloride form which adsorbs bile acids in the intestine forming an insoluble complex which is excreted in the faeces. This leads to a continuous but partial removal of bile acids from the enterohepatic circulation, thus preventing their reabsorption. All this results in a reduction in circulating beta-lipoproteins and LDLs and in a decrease in blood cholesterol levels.
Side effects
Among the side effects that could occur during treatment with cholestyramine, we remember: gastrointestinal disorders (in particular, constipation); headache and other disorders of the nervous system; kidney and urinary tract disorders; muscle and joint pain.
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