Lovastatin (lovastatin)


LOVASTATIN (Lovastatin) *.
     Lovastatin is gipoholesterinemicheskim substances selected from the strain A spergillus terreus. [1S- (1 a (R *), Z, a 7 b, b 8 (2S *, 4S *), 8 ab] 1, 2, 3, 7, 8, 8-N-3, 7 dimethyl-8 [2 - (tetrahydro) -4 gidroksi-6- - oxo-2 H piran-2- d] -1-2-naftalenil metilbutanoat.
     The white crystalline powder; Nerastvorim in the water, little is soluble in alcohol.
     Synonyms : Mevakor (name drug companies "MERCK & CO. , INC. , Rahway, N.J., U.S.A.), Mefakor, Mevacor.
     Step lovastatina linked to the inhibition of the biosynthesis of cholesterol. When the body lovastatin, which lacks gipoholesterinemicheskoy activity metabolised education free b-oxyacids, which is a competitive inhibitor of the enzyme 3-gidroksi3- metilglutarila kofermenta-A (NM G SoA) inhibitors, catalysing elementary and intermediate stages of the biosynthesis of cholesterol (education mevalonata) . Lovastatin can thus be seen as "prolekarstvo."
     Influenced lovastatina reduced total cholesterol content in blood plasma concentration LPNP and LPONP; There is also a modest increase LPVP concentration and the reduction in plasma triglycerides. At platelets aggregation and tromboksan- prostatsiklinovuyu system product expressed no influence.
     Assign lovastatin patients with primary NCEP, accompanied by a high-certainty in the absence of therapeutic effect of diet, as well as patients with a combination of NCEP and triglitseridemii.
     Adult drug designate, starting with the usual dose of 0.04 g (40 mg), 1 per day during dinner (synthesis of cholesterol takes place mainly at night). In milder forms may be sufficient NCEP lower dose (20 mg / day). A patient must comply with the diet. The effect develops in about 2 weeks (maximum effect through 4-6 weeks). Insufficient effective drug dose increases (at intervals of no less than 4 weeks) to 80 mg in 1 - or 2 reception at the luncheon and dinner. By reducing total cholesterol levels in plasma potassium below 140 ml (3, 6 mol / L) lovastatina dose should be reduced. With insufficient kidney function appoint not more than 20 mg per day.
     The drug is usually well. Possible changes in liver function improved transaminaz in blood serum, muscle pain, myo, neuralgia, headache, skin rash.
     Contraindicated in pregnancy and breastfeeding, acute liver diseases and resistant raising transaminaz in plasma. Children drug is not appointed.
     Diluted aggravating anti kumarinovyh.
     Product : pills to 0.1 g (yellowish peach color), 0.2 g (blue) and 0.4 g (green).
     Storage : List B. In cool, the dark place at room temperature (not above + 30 'C).

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