Simvastatin - instructions for use, doses, side effects, contraindications

Pharmacodynamics:Prodrug. Being inactive lactone, after ingestion, it is hydrolyzed to the β-hydroxyl metabolite, which competitively inhibits HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutarylcoenzyme A into mevalonic acid, the precursor of styrenes, including cholesterol.
It inhibits the synthesis of cholesterol in the liver, which leads to an increase in the density of low-density lipoprotein receptors on hepatocytes.As a result, the capture of low density lipoproteins from the blood plasma increases, which causes a decrease in the concentration of cholesterol and lipoproteins in the blood plasma.

Pharmacokinetics:

After oral ingestion, up to 85% is absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is reached after 4 hours. The connection with plasma proteins is 95%.

Therapeutic effect develops 2 weeks after the beginning of the admission. Metabolism in the liver.

The half-life is 2 hours.

Metabolism in the liver with the participation of enzymes: 3A4 and CYP3A3. Elimination with feces, about 13% - by the kidneys.

Indications:

It is used to treat primary hypercholesterolemia (type IIa and IIb) in patients with an increased risk of developing coronary atherosclerosis, with hypercholesterolemia not controlled by diet and exercise, also for the prevention of stroke and myocardial infarction, in order to reduce the risk of vascularization procedures.

ICD-10

IV.E70-E90.E78.2 Mixed hyperlipidemia

IV.E70-E90.E78.5 Hyperlipidemia, unspecified

VI.G40-G47.G45 Transitory transient cerebral ischemic attacks [attacks] and related syndromes

IX.I20-I25.I22 Repeated myocardial infarction

IX.I20-I25.I25.1 Atherosclerotic Heart Disease

IX.I20-I25.I25.9 Chronic ischemic heart disease, unspecified

IX.I60-I69.I64 Stroke not specified as a hemorrhage or infarction

IV.E70-E90.E78.0 Pure hypercholesterolemia

Contraindications:

Hepatitis in the active phase.

Individual intolerance.

Carefully:Liver failure.

In chronic inflammatory processes in the liver. When the activity of ALT and AST is increased 3 times, it is recommended to cancel the drug.

Pregnancy and lactation:Simvastatin contraindicated in pregnancy. There are several reports of the development of anomalies in newborns whose mothers were taking simvastatin. Women of childbearing age who receive simvastatin, should avoid conception. If in the course of treatment the pregnancy nevertheless has come, simvastatin should be canceled, and a woman should be warned about the possible danger to the fetus.
Data on the isolation of simvastatin with mother's milk are absent. If it is necessary to prescribe simvastatin during breastfeeding, it should be borne in mind that many drugs are excreted in breast milk and there is a threat of development of severe reactions,so breast-feeding during taking the drug is not recommended.
Action category for the fetus by FDA-X.

Dosing and Administration:

Use in children

Inside

5-10 years: 5 mg at night, if necessary, the dose rises after 4 weeks to 20 mg (maximum dose).

10-18 years: 10 mg at night, if necessary, the dose rises after 4 weeks to 40 mg (maximum dose).

Adults

It is taken orally, once a day. The initial dose (in terms of simvastatin) is 10 mg / day. The effect is detected two weeks after the start of treatment. The dose is adjusted depending on the effectiveness of therapy.

The highest daily dose: 80 mg.

The highest single dose: 80 mg.

Side effects:

Central and peripheral nervous system: headache, dizziness, unpleasant dreams, peripheral neuropathy, migraine.

Cardiovascular system: palpitation, orthostatic hypotension, arrhythmia.

The system of hematopoiesis: anemia, thrombocytopenia.

Respiratory system: exacerbation of bronchial asthma.

Muscular system: myopathy.

Digestive system: nausea, dysphagia, stomatitis, hepatitis, rectal bleeding (melena), tenesmus.

Analyzers: noises in the ears, amblyopia, loss of taste sensations.

Genitourinary system: dysuric disorders, impotence.

Allergic reactions.

Overdose:

Cases of overdose are not described.

Treatment is symptomatic, hemodialysis is ineffective.

Interaction:

Grapefruit juice increases the concentration of simvastatin - an increase in side effects (myopathy).

At reception of alcohol during treatment by a preparation activity of transaminases raises.

Antifungal agents, erythromycin, ciclosporin increase the concentration of simvastatin by 40%, digoxin - by 20%. With simultaneous use, a dose adjustment is required.

Special instructions:

Taking the drug is incompatible with alcohol, so people with chronic alcoholism, simvastatin not assigned.

In the treatment of simvastatin in patients with chronic renal failure, the progression of the disease slows down, or proteinuria decreases or ceases.

Instructions

Simvastatin (Simvastatinum)