Simvastatin, 40 mg 30 pcs

Simvastatin is a hypolipidemic drug synthetically derived from the fermentation product of Aspergillus terreus, is an inactive lactone, it undergoes hydrolysis in the body to form a hydroxy acid derivative. The active metabolite inhibits 3-hydroxy-3-methylglutaryl-CoA reductase (HMG-CoA reductase), the enzyme that catalyzes the initial reaction of mevalonate formation from HMG-CoA. Since the conversion of HMG-CoA to mevalonate represents an early step in cholesterol synthesis, the use of simvastatin does not cause accumulation of potentially toxic sterols in the body. HMG-CoA is easily metabolized to acetyl-CoA, which is involved in many synthesis processes in the body.

It lowers plasma levels of triglycerides (TG), low-density lipoproteins (LDL), very low-density lipoproteins (VLDL) and total cholesterol (in cases of heterozygous familial and non-familial hypercholesterolemia, in mixed hyperlipidemia, when elevated cholesterol is a risk factor).

Enhances high-density lipoprotein (HDL) and decreases the ratio of LDL/HDL and total cholesterol/HDL.

The onset of the effect is 2 weeks after the start of administration, the maximum therapeutic effect is achieved after 4-6 weeks. The effect is maintained during continuation of treatment, when discontinuing therapy cholesterol content gradually returns to baseline levels.

Pharmacokinetics

The absorption of simvastatin is high. After oral administration Cmax in plasma is reached after about 1.3 – 2.4 h and decreases by 90% after 12 h. The binding to plasma proteins is about 95%.

Metabolized in the liver, it has the effect of first passage through the liver (it is hydrolyzed with the formation of the active derivative: beta-hydroxy acid; other active and inactive metabolites have been found as well).

The T1/2 of active metabolites is 1.9 h. It is excreted mainly with the feces (60%) as metabolites. About 10-15% is excreted by the kidneys in the inactive form.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Contraindications

WARNING

. Patients who have undergone rhabdomyolysis during simvastatin therapy with a complicated history (impaired renal function, usually due to diabetes mellitus) require closer monitoring and simvastatin therapy should be temporarily stopped in these patients several days before major surgical procedures and also in the postoperative period; in patients with persistent elevated serum transaminase activity (exceeding 3 times the upper limit of normal) the drug should be discontinued; in severe renal failure (CK < 30 ml/min) the appropriateness of the drug at doses > 10 mg daily should be carefully considered and, if necessary, they should be prescribed with caution; in alcohol abuse before treatment.

Side effects

Overdose

Similarities