Medication Description: Lovastatin (Lovastatin)
LOVASTATIN (Lovastatin) *.
Lovastatin is a cholesterol-lowering substance isolated from the strain Aspergillus terreus. [1S- (1 a (R *), H a, 7 b, 8 b (2S *, 4S *), 8 ab] 1, 2, 3, 7, 8, 8 a - Hexahydro-3, 7dimethyl-8 [2- (tetrahydro) -4-hydroxy-6-oxo-2H-pyran-2-yl] -1-naphthalenyl 2-methylbutanoate.
White crystalline powder; insoluble in water, slightly soluble in alcohol.
Synonyms: Mevacor (Name of the drug company "MERCK & CO., INC.", Rahway, NJ, USA), Mefacor, Mevacor.
The action of lovastatin is associated with inhibition of cholesterol biosynthesis. When it enters the body, lovastatin, which does not have hypocholesterolemic activity, is metabolized to form free b-hydroxy acid, which is a competitive inhibitor of the enzyme 3-hydroxy3-methylglutaryl coenzyme A (HMG-CoA) reductase, which catalyzes the initial and intermediate stages of cholesterol biosynthesis (mevalonate formation) . Lovastatin can therefore be considered a “prodrug”.
Under the influence of lovastatin, the total cholesterol in the blood plasma, the concentration of LDL and VLDL are reduced; there is also a moderate increase in HDL concentration and a decrease in plasma triglycerides. The preparation does not have a pronounced effect on platelet aggregation and the thromboxane-prostacyclin system.
Lovastatin is prescribed to patients with primary hypercholesterolemia, accompanied by a high content of LDL in the absence of a therapeutic effect from diet therapy, as well as patients with a combination of hypercholesterolemia and triglyceridemia.
Adults are prescribed, usually starting with a dose of 0.04 g (40 mg), 1 time per day during dinner (cholesterol synthesis occurs mainly at night). In milder forms of hypercholesterolemia, smaller doses may be sufficient (20 mg per day). The patient must comply with the appropriate diet. The effect develops after about 2 weeks (maximum effect after 4-6 weeks). With insufficient effectiveness of the drug, the dose is increased (at intervals of at least 4 weeks) to 80 mg in 1 or 2 doses - during breakfast and dinner. By reducing the total cholesterol level in the blood plasma below 140 mg / 100 ml (3.6 mol / L), the dose of lovastatin must be reduced. In case of insufficient kidney function, no more than 20 mg per day is prescribed.
The drug is usually well tolerated. Possible changes in liver function with an increase in serum transaminase levels, muscle aches, myopathies, dyspepsia, headache, skin rash.
Contraindicated in pregnancy and lactation, acute liver disease, persistent increase in plasma levels of transaminases. Children do not prescribe the drug.
The drug enhances the effect of coumarin anticoagulants.
Form release: tablets of 0.1 g (yellowish-peach color), 0.2 g (blue) and 0.4 g (green).
Storage: List B. In a cool, dark place at room temperature (no higher than + 30 'C).