Mewakor

Mevakor is a lipid-lowering medication from the category of statins. Slows down the activity of HMG-CoA reductase.

Indications of the mevacore

It is used for therapy in such cases:

• hypercholesterolemia of a primary nature (hypolipoproteinemia, IIa, and IIb form), against which a high LDL level is noted (if dietotherapy in people with an increased likelihood of developing coronary atherosclerosis did not have the desired effect);
• hypercholesterolemia, as well as hypertriglyceridemia of a combined nature;
• atherosclerosis.

[1], [2], [3],

Release form

The release takes place in tablets, 14 pieces inside the blister plate. In the packet there are 2 such plates.

[4]

Pharmacodynamics

The statin ring of the lactone type is similar in structure to the part of the HMG-CoA reductase enzyme. Using the scheme of competitive antagonism, the statin molecule is synthesized with the site of the end of coenzyme A, to which the enzyme is attached. The second part of this molecule slows the process of transformation of hydroxymethylglutarate into a mevalonate element, which is an intermediate component of the binding of the cholesterol molecule.

The slowing down of the activity of the action of HMG-CoA reductase causes a series of successive reaction manifestations, which result in a decrease in the intracellular level of cholesterol, and in addition a compensatory increase in the activity of the action of LDL-ends, according to which the cholesterol catabolism of LDL is accelerated.

The hypolipidemic effect of statins develops due to a decrease in the values of total Xc due to the elements of Xc-LDL. The decrease in LDL-C depends on the size of the portion and has non-linear, and exponential parameters.

Statins have no effect on hepatic as well as lipoprotein lipase, and in addition do not have a significant effect on catabolism and binding of free fatty acids. Because of this, their effect on the indices of TG is secondary and mediated by the main effects of decreasing the values of Xc-LDL. The moderate decrease in TG values during statin therapy is most likely due to the expression of the endonous type (apoE) endings located on the surface of hepatocytes that are participants in the catabolism of the disease and contain about 30% TG.

The results of controlled tests showed that lovastatin increases the HDL-C values up to 10%.

In addition to hypolipidemic effects, statins have a positive effect in the case of endothelial dysfunction (preclinical symptom of an early stage of atherosclerosis), and in addition to the walls of the vessels and the state of atheroma. Together with this, they improve the rheological characteristics of the blood and have an antiproliferative and antioxidant effect.

[5], [6], [7], [8]

Pharmacokinetics

Inside the gastrointestinal tract, the drug after absorption is not absorbed completely (approximately 30% of the dose) and slowly. The use of the drug on an empty stomach reduces the absorption by approximately 30%. The level of bioavailability of drugs that are trapped inside the circulatory system is limited due to active extraction during the 1 st hepatic pass, followed by withdrawal of the substance along with bile. Peak values of the active element and its metabolic products within the blood plasma are noted after 2-4 hours after the use of a single dose.

The metabolic products within the blood plasma increase linearly in accordance with the increase in the portion of the drug to 120 mg.

The synthesis of Mevacor, as well as its active decay products with the blood plasma protein, is more than 95%. The drug passes through GEB and the placenta, and also cumulates inside the liver, in which it undergoes a hydrolysis process, during which active, as well as inactive, metabolic products are formed. Among the main active decay products are 6-hydroxy; and in addition 6-hydroxymethyl- and 6-hydroxymethylene derivatives of b-hydroxy acid.

At daily disposable reception of a medicine persistent plasma parameters of its active, and besides it inactive substances-inhibitors are noted after lapse of 2-3 days of treatment. These values are approximately 1.5 times higher than the metabolic products of drugs with a single dose.

Approximately 10% of the substance is excreted in the urine, and about 83% - with feces. With feces, the part of the drug that is excreted with bile is excreted, as well as its non-absorbed part. The half-life of lovastatin is 3 hours.

In people with kidney failure in the severe stage (CC level is within the range of 10-30 ml / minute), the indices of active, as well as inactive, metabolism of drugs inside the blood plasma after consuming a single dose of the drug are approximately twice as high as those within the blood plasma in healthy of people.

[9], [10], [11], [12], [13], [14]

Dosing and administration

The medicine is taken orally. The size of the initial portion is 10-20 mg, with a single use for the day - in the evening, along with the food. If required, the dose may be increased, but this is allowed only once per 1 month.

The maximum allowed daily dose is 80 mg, which is taken for 1 or 2 applications (along with breakfast and dinner). With a decrease in the plasma parameters of Xc to 140 mg / dl (3.6 mmol / L) or Xc-LDL up to 75 mg / dl (1.94 mmol / l), the dose of lovastatin should be reduced.

When a combination of the drug with immunosuppressors should be taken within a day not more than 20 mg of lovastatin.

[22], [23]

Use of the mevacore during pregnancy

Do not prescribe Mevakor to pregnant women or breastfeeding mothers.

Contraindications

The main contraindications:

• hepatic pathology in acute degree;
• an increase in the activity of the transaminase activity of the liver inside the blood serum (having an unknown nature);
• suspected pregnancy;
• the general severe condition of the patient;
• the presence of intolerance against lovastatin.

[15], [16], [17], [18], [19]

Side effects of the mevacore

The use of medication can cause various side effects:

• disorders of the digestive function: the appearance of heartburn. Occasionally, constipation, nausea, bloating, vomiting and dry mouth, and in addition anorexia, taste disorders and an increase in the transaminase activity of the liver inside the blood. Individual hepatitis, a disorder in the liver, intrahepatic cholestasis, gastralgia and pancreatitis;
• lesions affecting the structure of bones and muscles: myopathy with myalgia, and also myositis or rhabdomyolysis (in the case of combination with gemfibrozil, cyclosporine or niacin), as well as arthralgia and an increase in the level of the extracardiac fraction of CK within the blood plasma;
• disorders of the central nervous system and PNS: the occurrence of headaches, dizziness, seizures with paresthesias, or problems with sleep. Individual disorders of the psyche are noted;
• problems in the hematopoietic system: leuko- or thrombocytopenia, as well as hemolytic form of anemia;
• lesions affecting the visual organs: clouding of the lens, visual fogging, atrophy affecting the optic nerve, as well as cataracts;
• signs of allergy: rashes on the epidermis and itching. TEN, angioedema and urticaria are noted singly;
• others: weakened potency, and in addition, kidney failure in the acute stage (caused by rhabdomyolysis), a strong palpitation and pain in the sternum.

[20], [21]

Interactions with other drugs

Combined use with macrolide antibiotics, immunosuppressors (including ciclosporin), gemfibrozil, and also with niacin increases the likelihood of rhabdomyolysis, which further leads to kidney failure in the acute stage (especially in people with diabetic glomerulosclerosis).

Combination of drugs with derivatives of indandion and coumarin, as well as with anticoagulants causes an increase in bleeding and lengthening the values of PTV.

Taking medication together with oral contraception can interfere with the development of hyperlipidemia caused by the use of hormonal contraception.

It is believed that a decrease in the hypolipidemic effect of lovastatin is observed when combined with thiazide and loop diuretics.

Verapamil with diltiazem, and apart from this, isradipine slows the activity of the isoenzyme CYP3A4, which participates in the metabolism of lovastatin. Because of this, when combined with Mevacore, the plasma index of lovastatin and the likelihood of myopathy may increase.

There is evidence that when combined with itraconazole, hepatotoxicity and rhabdomyolysis in the acute stage may develop.

A single case of the occurrence of hyperkalemia in a severe degree in a patient with diabetes mellitus was described as a result of drug use together with lisinopril.

[24], [25]

Storage conditions

Mevakor should be kept in a dark and dry place, with temperatures not exceeding 25 ° C.

[26], [27], [28]

Shelf life

Mevakor can be used for 3 years from the date of manufacture of the drug.

[29], [30],

Application for children

There is no information on the effectiveness of the use and safety of medicines for children.

[31], [32], [33], [34]

Analogues

Analogues of the medication are preparations Amvastan, Leskol and Choletar with Lipantil.

[35], [36]