Lovastatin
When ATH:
C10AA02
Characteristic.
White non-hygroscopic crystalline powder; insoluble in water, slightly soluble in alcohol.
Pharmacological action.
Hypolipidemic, hypocholesteremic.
Application.
Hypercholesterolemia: Initial high-LDL (Types IIa and IIb) in the absence of effect of diet, Combined with hypertriglyceridemia (гиперлипопротеинемия типа IIb); atherosclerosis.
Contraindications.
Hypersensitivity, renal dysfunction, severe hepatic insufficiency, persistent increase in transaminase levels in blood plasma, pregnancy, lactation, childhood.
Pregnancy and breast-feeding.
Category actions result in FDA - X. (Animal tests or clinical trials revealed a violation of the fetus and / or there is evidence of the risk of adverse effects on the human fetus, obtained in research or practice; risk, associated with the use of drugs in pregnancy, greater than the potential benefits.)
Side effects.
Abnormal liver function, transaminase elevation, dyspepsia, flatulence, nausea, vomiting, heartburn, dry mouth, taste disturbance, anorexia, constipation / diarrhea, hepatitis, headache, muscle aches, myopathies, raʙdomioliz, generalized weakness, chest pain, arthralgia, insomnia, paresthesia, dizziness, mental disorders, convulsions, optic atrophy, cataracts, allergic reactions (skin rash and others.).
Cooperation.
Cholestyramine bile acids and enhance the effect of. Cyclosporin increases the plasma levels of the active metabolites of lovastatin. Fibrates, niocin, itraconazole and other azole antifungals, erythromycin, or cyclosporine increases the risk of myopathy, indirect anticoagulants (kumarinы) -bleeding.
Dosing and Administration.
Inside, while eating; the NCEP is 10-20 mg once during dinner; When atherosclerosis is 20-40 mg. With the lack of effectiveness of the dosage is increased (at intervals of not less than 4 Sun) up to 60-80 mg in 1-2 reception.
Precautions.
Patients, taking immunosuppressants, or with serious renal dysfunction dose should not exceed 20 mg / day. During treatment, patients must be on a standard diet of low cholesterol. It is recommended to closely monitor overall (the appearance of muscle pain or weakness, especially against fever, It requires the removal of lovastatin), periodically check the level of cholesterol in the blood and liver function tests are carried out.
Cautions.
May increase the levels of creatine phosphokinase and transaminase (It should be considered in the differential diagnosis of chest pain).
Cooperation
| Active substance | Description of interaction |
| Azithromycin | FMR. It increases the risk of acute rhabdomyolysis. |
| Warfarin | FMR: synergism. Against the background enhances the effect of lovastatin. |
| Verapamil | FMR: synergism. It increases the risk of myopathy and rhabdomyolysis. |
| Diltiazem | FKV. Increases (3-4 times) mean AUC and Cmax. |
| Indinavir sulfate | FMR: synergism. Конкурирует за изофермент CYP3A4, slows the biotransformation, increases plasma levels and increases the risk of myopathy and rhabdomyolysis; concurrent use is not recommended. |
| Itraconazole | FMR: synergism. In the systemic action inhibits CYP3A4, slows the biotransformation, It increases the plasma levels and an increased risk of myopathy. |
| Ketoconazole | FKV. FMR. In the systemic action inhibits CYP3A4, slows the biotransformation, increases plasma levels and increases the risk of myopathy and rhabdomyolysis. |
| Clarithromycin | FKV. FMR. Inhibits CYP3A4, slow destruction, can increase plasma levels and an increased risk of myopathy. |
| Clotrimazolum | FKV. FMR. In the systemic action inhibits CYP3A4, slows the biotransformation, increases plasma levels and increases the risk of myopathy and rhabdomyolysis. |
| Levothyroxine sodium | FKV. Against the background of lovastatin is changed distribution and elimination. |
| Nelfinavir | FMR. Конкурирует за изофермент CYP3A4, slows the biotransformation, increases plasma levels and increases the risk of myopathy and rhabdomyolysis; concurrent use is not recommended. |
| Oksikonazol | FKV. FMR. In the systemic action inhibits CYP3A4, slows the biotransformation, increases plasma concentration and increases the risk of myopathy and rhabdomyolysis. |
| Ritonavir | FMR. Конкурирует за изофермент CYP3A4, slows the biotransformation, increases plasma levels and increases the risk of myopathy and rhabdomyolysis; concurrent use is not recommended. |
| Saquinavir | FMR. Конкурирует за изофермент CYP3A4, slows the biotransformation, increases plasma levels and increases the risk of myopathy and rhabdomyolysis; concurrent use is not recommended. |
| Fenofibrate | FMR: synergism. Increases (mutually) Chance of rhabdomyolysis and acute renal failure; combined application admissible, if the risk of complications is less than the benefit of future changes in the level of lipids. |
| Fluconazole | FKV. FMR. In the systemic action inhibits CYP3A4, slows the biotransformation, increases plasma levels and increases the risk of myopathy and rhabdomyolysis; concurrent use is not recommended. |
| Cyclosporine | FKV. FMR. It increases the level of active metabolites of lovastatin plasma; the combined appointment increases the risk of myopathy. |
| Erythromycin | FKV. FMR. Inhibits CYP3A4, slows the biotransformation, increases the concentration in the tissues and increase the likelihood of side effects, incl. miopatiй. |
