Cardiostatin, tablets 20 mg, 30 pcs.

Hypolipidemic agent, disrupts early stages of cholesterol synthesis in the liver (at the stage of levanic acid).

In the body it forms free beta-hydroxy acid, which competitively inhibits Z-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase) and disrupts its conversion into mevalonate, resulting in reduced cholesterol synthesis and increased catabolism.

Reduces the blood content of very low density lipoproteins, low density lipoproteins and triglycerides, moderately increases high density lipoproteins.

Significantly reduces the amount of apoprotein B (part of low-density lipoproteins) and other circulating components of low-density lipoproteins.

The pronounced therapeutic effect is manifested within 2 weeks, and the maximum effect – after 4-6 weeks from the start of treatment.

Pharmacokinetics

In the gastrointestinal tract is absorbed slowly and not completely – about 30% of the taken dose, intake on an empty stomach reduces absorption by 30%.

Maximal concentration (7,8 ng/ml for lovastatin and 11,9 ng/ml for beta-hydroxyacid) in plasma is noted within 2-4 hours, then plasma level decreases rapidly, being 10% of maximal level in 24 hours.

Blood plasma protein binding is 95%. Clearance of lovastatin and its active metabolites in case of a single administration at night is achieved on 2-3 days of therapy and is 1.5 times higher than after single administration.

Passes through the blood-brain barrier and the placental barrier.

It is metabolized intensively during the “first passage” through the liver and is oxidized to beta-hydroxy acid, its 6-oxy derivative and other metabolites, some of which are pharmacologically active (block Z-hydroxy-3-methylglutaryl coenzyme A reductase).

CYP3A4, CYP3A5 and CYP3A7 isoenzymes are involved in metabolism of the drug.

Half-life – 3 hours. Excreted through the intestine – 83%, by the kidneys – 10%.

Indications

Active ingredient

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Overdose

Pregnancy use

It is contraindicated. Breastfeeding should be stopped during treatment.