Description of the medicine: Lovastatin (Lovastatin)
LOVASTATIN (Lovastatin) *.
Lovastatin is a hypocholesterolemic substance isolated from Aspergillus terreus strain. [1S- (1 a (R *), 3 a, 7 b, 8 b (2S *, 4S *), 8 ab] 1, 2, 3, 7, 8, 8 a-Hexahydro-3, 7 dimethyl-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 effect of lovastatin is associated with inhibition of cholesterol biosynthesis. When ingested, 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 (NMG-CoA) reductase, which catalyzes the initial and intermediate stages of cholesterol biosynthesis (formation of mevalonate) . Lovastatin may therefore be considered a “prodrug”.
Under the influence of lovastatin, the content of 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 drug 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 LDL content in the absence of a therapeutic effect from diet therapy, as well as to patients with a combination of hypercholesterolemia and triglyceridemia.
For adults, the drug is 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 (20 mg per day) may be sufficient. The patient must follow an appropriate diet. The effect develops after about 2 weeks (the maximum effect is after 4 to 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. With a decrease in total plasma cholesterol below 140 mg / 100 ml (3.6 mol / L), the dose of lovastatin must be reduced. With insufficient renal function, not more than 20 mg per day is prescribed.
The drug is usually well tolerated. Possible changes in liver function with an increase in serum transaminases, muscle pain, myopathy, dyspepsia, headache, skin rash.
It is contraindicated during pregnancy and lactation, acute liver diseases, persistent increase in plasma transaminases. Children are not prescribed the drug.
The drug enhances the effect of coumarin anticoagulants.
Release form: tablets on 0,1 g (yellowish-peach color), 0,2 g (blue color) and 0,4 g (green color).
Storage: List B. In a cool, dark place at room temperature (no higher than + 30 ° C).