Lovastatin
Lovastatin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Lovastatin
ATX code: C10AA02
Active ingredient: lovastatin (lovastatin)
Manufacturer: Replekpharm AD (Republic of Macedonia), Lekpharm (Republic of Belarus), MAKIZ-PHARMA (Russia), Kievmedpreparat (Ukraine)
Description and photo update: 2018-25-10
Lovastatin is a drug with hypocholesterolemic, hypolipidemic action.
Release form and composition
Lovastatin dosage form - tablets: flat-cylindrical round, white with a yellowish tinge, with a chamfer (in a cardboard box 1–3 blisters of 10, 15 or 20 tablets each).
Composition of 1 tablet:
- active substance: lovastatin - 20 or 40 mg (in terms of 100% dry matter);
- auxiliary components: colloidal silicon dioxide, magnesium stearate, corn starch, butylhydroxyanisole, microcrystalline cellulose, milk sugar.
Pharmacological properties
Pharmacodynamics
Lovastatin is an inhibitor of endogenous cholesterol synthesis in the liver. A substance in the body in the form of inactive lactone is directly hydrolyzed to the corresponding therapeutically active form, which acts as a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase). It is an enzyme that catalyzes the conversion of HMG-CoA to mevalonate, which is the initial step in cholesterol biosynthesis.
The main effects of lovastatin:
- a decrease in total blood cholesterol and cholesterol in the composition of LDL and VLDL (low density lipoproteins and very low density lipoproteins);
- weakening the decrease in the content of apolipoprotein B, the concentration of triglycerides in the blood plasma and a moderate increase in the concentration of HDL (high density lipoprotein);
- stabilization of plaques, improvement of endothelial function, anti-thrombogenic and anti-inflammatory effects (contribute to the anti-atherosclerotic effect).
The pronounced therapeutic effect of lovastatin is manifested within 14 days, and the maximum - after 1-1.5 months of systematic administration. During the same period after discontinuation of therapy, the effect persists. With prolonged use (up to 5 years), the effectiveness of lovastatin does not decrease.
Pharmacokinetics
Lovastatin is absorbed in the gastrointestinal tract (gastrointestinal tract) slowly and not completely - about 30% of the dose. When taken on an empty stomach, absorption is reduced by 1/3 in comparison with the use with food.
Tmax (time to reach the maximum concentration) ranges from 2 to 4 hours, Cmax (maximum concentration) is 7.8 and 11.9 ng / ml (for lovastatin and beta-hydroxy acid), then the plasma concentration decreases rapidly. After 24 hours, it is 10% of the maximum. Communication with blood plasma proteins - 95%. With a single dose at night, the clearance of lovastatin and its active metabolites is achieved after 48–72 hours.
Penetrates the blood-brain and placental barrier.
During the first passage through the liver, Lovastatin undergoes intensive metabolism, is oxidized to beta-hydroxy acid, its 6-hydroxy derivative and other metabolites, some of them exhibit pharmacological activity (blocking HMG-CoA reductase). The isoenzymes CYP3A4, CYP3A7 and CYP3A5 are involved in the metabolism of lovastatin.
T 1/2 (half-life) is 3 hours. 83% of the dose is excreted through the intestines, 10% - by the kidneys.
Indications for use
- elevated serum levels of total cholesterol, LDL cholesterol and triglycerides in the blood serum in patients with primary hypercholesterolemia (according to Fredrickson types IIa and IIb), including familial mixed hyperlipidemia, polygenic hypercholesterolemia and heterozygous hypercholesterolemia: Lovastatin is prescribed to reduce their effectiveness in dietary therapy other non-drug activities;
- coronary atherosclerosis in patients with ischemic heart disease (ischemic heart disease): therapy is carried out to slow down its progression.
Contraindications
Absolute:
- liver disease in the active phase or a persistent increase in the activity of hepatic transaminases of unknown origin;
- lactose intolerance, glucose-galactose malabsorption or lactase deficiency;
- pregnancy and lactation;
- age up to 18 years;
- individual intolerance to any component of the drug.
Relative (Lovastatin is prescribed under medical supervision):
- a history of liver disease;
- chronic alcoholism;
- concomitant immunosuppressive therapy;
- organ transplant;
- CRF (chronic renal failure);
- combination therapy with gemfibrozil, fenofibrate and other fibrates, nicotinic acid (from 1000 mg per day), cyclosporine, nefazodone, macrolides (erythromycin, clarithromycin), HIV protease inhibitors (ritonavir), antifungal agents from the azole group (ketoconazole);
- urgent surgical procedures, including dental procedures.
Instructions for the use of Lovastatin: method and dosage
Lovastatin is taken orally, preferably with meals.
Before prescribing therapy, as well as during the use of the drug, the patient should follow a standard cholesterol-lowering diet.
Hyperlipidemia
The recommended daily dose of Lovastatin is 10–80 mg once a day.
In patients with moderate hypercholesterolemia, the initial dose is usually 20 mg once a day in the evening, with a pronounced course of the disease (plasma total cholesterol in the blood - from 7.8 mmol / l) - 40 mg. To achieve target cholesterol levels, the dose can be increased to 80 mg (maximum) in one or more doses (morning and evening).
You need to change the dose at intervals of at least 4 weeks. If the level of concentration of total cholesterol in blood plasma has decreased to 140 mg / 100 ml or LDL-cholesterol to 75 mg / 100 ml, the dose of Lovastatin can be reduced. When combined with cyclosporine, fibrates or nicotinic acid (from 1000 mg per day), the dose of the drug should not exceed 20 mg per day. For patients with severe renal insufficiency with creatinine clearance less than 30 ml / min, the drug is prescribed under medical supervision (maximum dose - 20 mg per day).
Coronary atherosclerosis
Lovastatin is prescribed at 20-80 mg per day in 1-2 doses. The duration of therapy is determined by the doctor individually.
Side effects
As a rule, Lovastatin is well tolerated by patients.
Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01%, including isolated messages - very rare):
- musculoskeletal system: often - muscle cramps, myalgia; rarely - myopathy, dermatomyositis, myositis; very rarely - rhabdomyolysis (when used in combination with cyclosporine, gemfibrozil or nicotinic acid);
- nervous system: often - headache, dizziness; very rarely - sleep disorders, including insomnia, peripheral neuropathy, paresthesias, general weakness, mental disorders (including anxiety);
- digestive system: often - heartburn, nausea, abdominal pain, constipation / diarrhea, dyspeptic disorders, flatulence; very rarely - hepatitis, xerostomia, taste perversion, cholestatic jaundice, biliary cholestasis, gastralgia, hepatitis, liver dysfunction, pancreatitis in acute course;
- sense organs: very rarely - atrophy of the optic nerve, fog before the eyes, cataracts, clouding of the lens;
- hematopoietic organs: leukopenia, hemolytic anemia, thrombocytopenia;
- allergic reactions: very rarely - hypersensitivity syndrome (urticaria, angioedema, anaphylaxis, arthralgia, lupus-like syndrome, erythema multiforme, including Stevens-Johnson syndrome), toxic skin rash, epidermal necrolysis (Lyell's syndrome), pruritus;
- laboratory parameters: a moderate increase in the activity of ALT (alanine aminotransferase) and AST (asparagine aminotransferase); rarely - an increase in the activity of CPK (creatine phosphokinase); very rarely - an increase in alkaline bilirubin and phosphatase;
- other reactions: very rarely - decreased potency, acute renal failure, pain in the chest, palpitations, alopecia.
Overdose
There are no specific symptoms of an overdose of Lovastatin.
Therapy: drug withdrawal, general measures aimed at maintaining and monitoring vital functions, liver function and CPK activity, preventing further absorption of the drug (taking laxatives / activated charcoal, gastric lavage).
There is no specific antidote, hemodialysis is not effective.
special instructions
Control of the enzyme level should be carried out before the start of therapy and at regular intervals during the course of treatment (for 12 months, then at least once every 6 months).
Lovastatin should be discontinued in cases where there is an increase in the activity of ACT and / or ALT in serum 3 times relative to VGN (upper limit of normal). Also, therapy is discontinued with a persistent increase in CPK activity (this should be taken into account when conducting differential diagnosis of chest pain).
Taking Lovastatin can lead to the appearance of myopathy, which in turn can cause the development of rhabdomyolysis and renal failure. The risk of this pathology is higher against the background of combined use with one or more of the following drugs: nefazodone, cyclosporine, fibrates (gemfibrozil, fenofibrate), macrolides (erythromycin, clarithromycin), antifungal azoles (ketoconazole, itraconazole) and protease inhibitors HIV (ritonavir). The likelihood of developing myopathy also increases with severe renal failure.
If any unexplained muscle soreness develops, you should inform your doctor, especially if it is accompanied by fever or malaise.
In patients with rare homozygous familial hypercholesterolemia, Lovastatin is less effective, which may be due to the absence of functioning LDL receptors in this group of patients. There is also an assumption that their activity of hepatic transaminases increases faster.
Lovastatin is not indicated in cases where the main pathology is hypertriglyceridemia (i.e., according to Fredrickson, hyperlipidemia of I, IV and V types), since the drug has only a moderate effect in reducing triglyceride levels.
Application during pregnancy and lactation
According to the instructions, Lovastatin is not prescribed to women during pregnancy / lactation.
Women of reproductive age should use reliable contraception while taking the drug.
Pediatric use
For patients under 18 years of age, therapy is contraindicated.
With impaired renal function
With chronic renal failure, Lovastatin is prescribed with caution.
For violations of liver function
- liver disease in the active phase or a persistent increase in the activity of hepatic transaminases of unknown origin: therapy is contraindicated;
- history of liver disease: Lovastatin is prescribed with caution.
Drug interactions
- colestipol, cholestyramine: decreased bioavailability (you can take lovastatin 2–4 hours after taking these drugs, while the development of an additive effect is noted);
- warfarin: an increase in its effect on blood coagulation parameters, which can increase the risk of bleeding (until stable indicators are achieved, prothrombin time control is required);
- nicotinic acid (at a dose of 1000 mg per day), cyclosporine, macrolide antibiotics (erythromycin, clarithromycin), azole agents with antifungal action (ketoconazole, itraconazole), HIV protease inhibitors (ritonavir), nefazodone: increased plasma concentration of lovastatin in the blood what can cause the development of myopathy with rhabdomyolysis and renal failure;
- derivatives of fibric acid (fibrates): development of myopathies (the mechanism is unclear);
- grapefruit juice (from 1000 ml per day): an increase in Cmax and AUC (area under the concentration-time curve) of lovastatin and the development of myopathies.
Analogs
Lovastatin analogs are: Holetar, Medostatin, Cardiostatin, etc.
Terms and conditions of storage
Store in a place protected from moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Lovastatin
According to reviews, Lovastatin is a safe and effective drug used in complex treatment, and for the prevention of atherosclerosis and its complications. It is usually well tolerated even with a long course. Side effects (flatulence, diarrhea / constipation, abdominal pain, insomnia, muscle pain) are rarely reported.
The price of Lovastatin in pharmacies
The price of Lovastatin is unknown, since it is not available in pharmacies. Approximate price for analogs: Cardiostatin (30 tablets of 20 mg) - 121-280 rubles, Holetar (20 tablets of 20 mg) - 258-342 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
