Tablets from high cholesterol

In the complex therapy of hypercholesterolemia, medications are used that help to lower the level of cholesterol and lipoprotein in the blood-various lipid-lowering drugs or, as they are often called, tablets from high cholesterol. This review reviews drugs that are usually prescribed by doctors.

Indications for the use of tablets from high cholesterol

The main indications for the use of tablets from high cholesterol - the level of its content in the blood above 5.5-6 mmol per liter against the background of existing diseases of the cardiovascular system, including atherosclerosis, arterial hypertension, coronary artery disease and myocardial infarction.

In addition, the drugs in this group are designed to reduce the excess levels of cholesterol in adiposity of adipose tissue (obesity), liver and pancreas pathologies, diabetes and chronic renal failure, with various types of hyperlipoproteinemia and hypertriglyceridemia.

Names of tablets from high cholesterol, most often prescribed to patients with the above diseases, are as follows:

• Atorvastatin (Atoris, Liprimar, Torvacard), Lovastatin (Lovasterol, Mevakor, Mefakor), Simvastatin (Aktalipid, Zokor, Zorstat), Rosuvastin (Crestor) - statins;
• Gemfibrozil (Gevilon, Gipolyssan, Lipolipid, Clopidogrel), Fenofibrate (Benprofibrate, Lipidil, Lipofen, Nolipax, Protolipan) are lipid modifiers of the fibrate group (fibrates);
• Nicotinomide (Niacinamide, Nikamid, Nicofort, Nicovite) nicotinic acid (vitamin PP) and its derivatives;
• Cholestipol (Cholestide) drugs that bind bile acids;
• Fenbutol (Laurelkol, Lesterol, Sinestan, etc.) derivatives of butylphenols;
• Ezetimib (Ezetrol) is a selective inhibitor of cholesterol absorption.

Pharmacodynamics of tablets from high cholesterol

Different groups of lipid-lowering drugs have a different mechanism of action. Pharmacodynamics of tablets from high cholesterol, belonging to the group of statins, is based on the inactivation of the enzyme, which regulates one of the first stages of the biosynthesis of cholesterol in the liver and intestines. First, due to a decrease in the activity of this enzyme, the production of cholesterol in the body is reduced. Secondly, on the membranes of liver cells, the number of receptors of protein-fatty compounds with a high content of low-density lipoprotein (LDL) cholesterol, which bind cholesterol and ensure its transportation with blood flow to the tissues of the body, increases.

In the pharmacodynamics of gemfibrozil and other fibrates, the main task of facilitating lipid metabolism and the cleavage of fats (triglycerides) and LDL is to make fenofibric acid compounds (belonging to the class of amphipathic carboxylic acids). These substances activate LPL (lipoprotein lipase) - an enzyme that regulates the fat content in the blood. And already LPL affects intracellular alpha receptors (PPAR-α), which modulate carbohydrate-lipid metabolism and differentiation of adipose tissue.

Nicotinic acid serves as a non-protein enzyme involved in the oxidation-reduction processes of the body, including the breakdown of carbohydrates and fats for energy. An increase in the content of nicotinic acid leads to the activation of lipoprotein lipase and, as a result, to an increase in the utilization of lipids and a decrease in the content of triglycerides and lipoproteins in the blood plasma.

The pharmacological action of the bile acid-binding cholestipol provides insoluble in the gastrointestinal tract of high-molecular-weight anion-exchange resins of the microheterogeneous structure, which prevent re-absorption of bile and cholesterol in the intestine. This leads to the removal of cholesterol from the body through the intestine and a decrease in its content in the blood.

The derivatives of butylphenols (Fenbutol, etc.) not only inhibit the production of cholesterol, but also reduce its absorption during digestion. And the pharmacodynamics of drugs that selectively inhibit the absorption of cholesterol from the intestine (Ezetimibe) is due to the blocking of a specific protein that is responsible for transporting cholesterol to the liver cells.

Pharmacokinetics of tablets from high cholesterol

Active substances of tablets from high cholesterol Atorvastatin, Lovastatin and other statins after oral intake are absorbed into the digestive tract and enter the bloodstream to reach the highest concentration in the plasma after 90-120 minutes. When binding statins to plasma proteins by almost 96%, the level of their systemic bioavailability does not exceed 30%, which is explained by the formation of active metabolites in the liver at the first stage of transformation of the active component of the drugs. In the liver, the statins are oxidized, after which the secondary metabolites are excreted through the intestine (approximately within 24 hours).

The pharmacokinetics of gemfibrozil and all lipid modifiers differ from statins in that the hepatic metabolism of the active substance proceeds more rapidly, after 2 hours the kidneys remove half the dose taken from the body (the rest is excreted with the bile in the intestine).

Due to the slow absorption in the GIT, tablets from high cholesterol Fenbutol act gradually, which provides the drugs of this group prolonged (about half a year after stopping the regular intake) therapeutic effect in the form of antioxidant and antisclerotic action - reducing oxidation of blood lipids and settling them on the walls of blood vessels in the form of atherosclerotic plaques.

For the pharmacokinetics of the absorbing cholesterol of Ezetimibe, an active compound with phenols of glucuronic acid formed in the small intestine and liver during self-cleaning of the body from foreign and harmful substances is characteristic. The pharmacologically active ezetimibe-glucuronide conjugate binds to plasma proteins and is released from the blood through the kidneys and intestines for about 10 days.

Dosing and Administration

The only way to use tablets from high cholesterol is oral. It should be recalled that the individual doses of any lipid-lowering drug are determined only by the attending physician - on the basis of a blood test for cholesterol level.

The standard daily dose of statins is 0.01 g (taken once a day, at the same time), followed by an increase to a maximum of 0.08 g as prescribed by the doctor.

Usual single dose Gemfibrozil 0.3 g (twice a day, half an hour before meals); Fenofibrate is also taken twice a day for 0.1 g (during meals, in the morning and in the evening).

The optimal single dose of nicotinic acid is 20-50 mg (2-3 times during the day); simultaneous reception of methionine will provide protection of the liver from fat accumulation.

Cholestipol (1 g tablets) is recommended to take 5 tablets a day, after 1-2 months the daily dose is doubled. Fenbutol is prescribed one tablet (0.25 g) twice a day, during meals. Recommended daily dose of tablets from high cholesterol Ezetimib 10 mg (single dose).

Overdosage of the listed drugs, as noted in the instructions to the drugs, can occur if the dosage prescribed by the doctor is exceeded, but there is no information on such cases.

[6], [7], [8], [9]

Contraindications for use

Tablets from high cholesterol, in addition to individual hypersensitivity to the active substances of drugs, have the following contraindications for use:

• statins: pronounced or existing history of liver, kidney, disease of the musculoskeletal system;
• fibrates: problems with biliary tracts, autoimmune biliary cirrhosis;
• nicotinic acid and its derivatives: acute form of stomach ulcers and duodenal ulcers, kidney stones, hepatitis;
• drugs that bind bile acids: impaired absorption of fats in the intestine (steatorrhea), children's age;
• derivatives of butylphenols: liver and / or kidney disease, age up to 14 years;
• selective inhibitors of cholesterol absorption: hepatic insufficiency of any etiology, age to 18 years.

The use of tablets from high cholesterol during pregnancy is included in the list of contraindications for hypolipidemic drugs of all pharmacological subgroups, including nicotinic acid.

[1], [2], [3], [4], [5]

Side effects

Tablets from high cholesterol from the group of statins can have such side effects as: headaches and dizziness, dry mouth, heartburn, nausea, diarrhea, abdominal pain; disorders in the work of the liver (increase in the concentration of hepatic enzymes of transmnaz), pancreas and heart (tachycardia); diabetes mellitus, insomnia, cramps and muscle pain; reduction of visual acuity (up to the development of cataracts), impotence, cognitive impairment.

The use of gemfyrozil can accompany nausea, stomach discomfort and diarrhea; skin reactions (dermatitis); pain - head, muscle, joint, stomach; dysfunction of the liver and gallbladder; anemia, leukopenia, anemia, as well as a decrease in the number of cellular elements (hypoplasia) of the bone marrow. Another drug of this group, Fenofibrate, is associated with the listed side effects of the threat of developing cholelithiasis.

When used to reduce cholesterol drugs nicotinic acid, it is possible to drop blood pressure, the appearance of excess uric acid in the blood, increase intracellular enzymes of the liver and its fatty degeneration. Receiving tablets Cholestipol can cause nausea and vomiting, constipation or diarrhea, hives and skin inflammation. In case of prolonged treatment with this drug, a shortage of vitamins (A, D, E, K) in the body is possible.

Problems with digestion and cardiac arrhythmia are side effects of Fenbutol, and the drug Ezitimibe can cause headache, nausea, pain in the muscles and abdominal cavity, diarrhea and flatulence, and allergic skin rashes.

Interactions with other drugs

Identified by manufacturers of tablets Atorvastatin, Lovastatin, Simvastatin interactions with other drugs consist in increasing their concentrations in blood plasma with simultaneous use of antibiotics and fungicides. The combination of statins with hormonal contraceptives increases the concentration of the latter in plasma, and with indirect anticoagulants - reduces the time of blood clotting.

Absolute incompatibility of gemfibrozil with lovastatin: may develop kidney failure in acute form and muscular dystrophy. And in patients who use hormonal drugs to protect themselves from pregnancy, a serious violation of lipid metabolism is possible. Fenofibrate enhances the effect of anticoagulants coumarinic series and derivatives of phenylidandione, as well as drugs containing salicylates, and tablets from diabetes.

Cholestipol, binding bile acids in the intestine, disrupts the normal absorption of other oral medications, to avoid which all other medications must be taken 1-2 hours earlier.

All of the above tablets from high cholesterol have the same storage conditions: dry, protected from bright light and inaccessible to children, the usual room temperature (not more than + 25-28 ° C).

The expiration date is also standard: two years from the date of issue indicated on the package.

Also see the article Treatment of High Cholesterol: The Most Common Methods