Livazo
Livazo: 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. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Livazo
ATX code: C10AA08
Active ingredient: pitavastatin (Pitavastatin)
Producer: Pierre Fabre Medicament Production (France)
Description and photo updated: 2019-29-07
Prices in pharmacies: from 427 rubles.
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Livazo is a lipid-lowering drug, an inhibitor of HMG-CoA reductase (hydroxymethylglutaryl-coenzyme A-reductase).
Release form and composition
The drug is available in the form of film-coated tablets: round, biconvex, white shell and core; engraved on each side: on one side - "KC", on the other side for tablets with a dosage of 1 mg - "1", a dosage of 2 mg - "2", a dosage of 4 mg - "4" (in blisters: tablets with a dosage of 1 mg - 7, 14 or 15 pcs., in a cardboard box 1 or 2 blisters; tablets with a dosage of 2 mg - 7, 10, 14, 15 or 20 pcs., in a cardboard box 1, 2, 3 or 5 blisters; tablets dosage of 4 mg - 7, 10, 14 or 15 pcs., 1, 2 or 3 blisters in a cardboard box. Each box also contains instructions for using Livazo).
1 tablet contains:
- active substance: Pitavastatin calcium - 1.045; 2.09 or 4.18 mg, which is equivalent to 1, 2 or 4 mg of pitavastatin, respectively;
- auxiliary components: lactose monohydrate, hypromellose, low-substituted hyprolose, magnesium stearate, magnesium aluminometasilicate;
- film shell: Opadrai white - triethyl acetate, hypromellose, colloidal silicon dioxide, titanium dioxide.
Pharmacological properties
Pharmacodynamics
Livazo is a hypolipidemic drug, the active ingredient of which is pitavastatin.
Pitavastatin is a competitive inhibitor of the HMG-CoA reductase enzyme, which catalyzes the initial stage of cholesterol synthesis and promotes the conversion of HMG-CoA into mevalonic acid. As a result of inhibition of the initial stage of cholesterol formation, the use of pitavastatin is not accompanied by the accumulation of potentially toxic sterols in the body. HMG-CoA is easily biotransformed to acetyl-CoA, which is involved in various synthesis processes.
The use of Livazo is effective both for the purpose of lowering the plasma concentration of total cholesterol (OXC), low density lipoprotein cholesterol (LDL), very low density lipoprotein cholesterol (VLDL), apolipoprotein B (Apo-B) and triglycerides, and for increasing the concentration level high density lipoprotein cholesterol (HDL) and apolipoprotein A1 (Apo-A1).
Therapeutic doses of pitavastatin significantly reduce the concentration of total cholesterol, LDL cholesterol, cholesterol not associated with high density lipoproteins (non-HDL), Apo-B, triglycerides, and increase the concentration of HDL cholesterol and Aro-A1 in the treatment of primary hypercholesterolemia or combined dyslipidemia. There is a decrease in the ratio of total cholesterol or HDL cholesterol and Apo-B or Apo-A1. Taking a dose of Livazo 2 mg lowers the level of LDL cholesterol by 38-39%, and at a dose of 4 mg - by 44-45%.
In patients over the age of 65, the use of pitavastatin at a dose of 1, 2 or 4 mg for the treatment of primary hypercholesterolemia or combined dyslipidemia provides a decrease in LDL cholesterol levels by 31, 39 and 44.3%, respectively. The target level set by the European Atherosclerosis Society (EAS) is reached in 90% of cases.
In the treatment of primary hypercholesterolemia or mixed dyslipidemia in patients with two or more cardiovascular risk factors, or mixed dyslipidemia in combination with type 2 diabetes mellitus, LDL cholesterol levels are reduced by 44% and 41%, respectively, the targets set by the EAS are achieved in 80% cases.
With long-term use of Livazo, the maintenance of the target value established by the EAS is ensured by a constant stable decrease in LDL cholesterol levels by 30.5% and a consistent increase in the concentration of HDL cholesterol. A large increase in HDL cholesterol is observed in patients with lower baseline values of this indicator.
Against the background of the use of pitavastatin at a dose of 4 mg in patients who underwent percutaneous coronary intervention under the control of intravascular ultrasound for acute coronary syndrome, after 8-12 months of treatment, a decrease in the volume of coronary plaques by about 17% and reversible development of vascular wall remodeling (from 113 to 105.4 mm 3).
There is no assessment of the beneficial effects in terms of morbidity or mortality.
It was found that the appointment of Livazo in a daily dose of 1 or 2 mg to patients with hyperlipidemia and concomitant impaired glucose tolerance as an adjunct to recommendations for lifestyle changes helps to slow the development of newly diagnosed diabetes mellitus. The risk ratio after ~ 33.5 months of therapy is 0.82.
Pharmacokinetics
After taking Livazo inside, Pitavastatin is rapidly absorbed in the upper gastrointestinal tract. In unchanged form, pitavastatin undergoes intestinal-hepatic recirculation and is well absorbed from the jejunum and ileum. The maximum concentration (C max) in blood plasma is reached after 1 hour. With the simultaneous intake of fatty foods, C max decreases by 43%, while the AUC (area under the concentration-time curve) remains unchanged. Absolute bioavailability - 51%.
Plasma protein binding (mainly albumin and alpha-1 acid glycoprotein) - more than 99%. Average V d (volume of distribution) - 133 liters. With the help of organic transport proteins OATP1B1 and OATP1B3, it actively penetrates into hepatocytes. AUC can vary from a minimum value to a maximum within a fourfold increase. Pitavastatin is not a substrate for P-glycoprotein.
As a result of biotransformation from the ester-type pitavastatin glucuronide conjugate with the participation of uridine-5-diphosphate glucuronyltransferases (UGT1A3 and UGT2B7), the main metabolite is formed - an inactive lactone. Cytochrome P 450 has a minimal effect on the metabolism of pitavastatin. CYP2C9 and CYP2C8 isoenzymes are involved in the metabolism of pitavastatin to minor metabolites. In plasma, pitavastatin is found mainly unchanged.
Pitavastatin is rapidly excreted from the liver with bile in unchanged form, undergoing intestinal-hepatic recirculation, which provides it with a long-term effect.
Less than 5% of the dose is excreted through the kidneys.
After a single dose, T 1/2 (half-life) from plasma is 5.7 hours (in an equilibrium state - 8.9 hours), the average clearance is 43.4 l / h.
A slight change in pharmacokinetic parameters in elderly patients (over 65 years of age) or of different sex does not have a clinically significant effect on the efficacy or safety of the drug.
Race does not affect the pharmacokinetics of pitavastatin.
With mild liver dysfunction (class A according to the Child-Pugh classification), the AUC increases by 1.6 times. With moderate hepatic dysfunction (class B according to Child-Pugh classification), the AUC is 3.9 times higher than in healthy patients. The use of pitavastatin in patients with severe liver dysfunction is contraindicated.
With moderate renal failure, the AUC indicator increases 1.8 times, in patients on hemodialysis - 1.7 times.
Indications for use
- primary hypercholesterolemia, including heterozygous familial hypercholesterolemia (Fredrickson type IIa hyperlipidemia);
- mixed hypercholesterolemia (type IIb hyperlipidemia according to the Fredrickson classification);
- hypertriglyceridemia (type IV hyperlipidemia according to the Fredrickson classification) - as an adjunct to the diet in cases where the non-drug methods of therapy, including diet, exercise, weight loss, do not have a sufficient effect.
Contraindications
Absolute:
- severe stage of liver failure - class C according to the Child - Pugh classification or more than 9 points on the Child - Pugh scale;
- active phase of liver disease, including a steady increase of more than 3 times, compared with the upper limit of normal (UHN), liver transaminase activity in blood serum;
- lactose intolerance, glucose-galactose malabsorption syndrome, lactase deficiency;
- myopathy;
- concomitant therapy with cyclosporine;
- lack of reliable methods of contraception for women of reproductive age;
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to statins or drug components.
Livazo should be taken with caution if the patient has such risk factors for the development of myopathy or rhabdomyolysis as renal failure, hypothyroidism, hereditary muscle diseases in a personal or family history, an indication in the history of muscle toxicity with the previous use of fibrates or other inhibitors of HMG-CoA reductase, alcohol abuse, history of liver disease, age over 70 years.
Livazo, instructions for use: method and dosage
Livazo tablets are taken orally, swallowing whole, preferably in the evening at the same time.
Before and during treatment, patients should follow a cholesterol-lowering diet.
Recommended dosage: initial dose - 1 mg once a day. In the absence of a sufficient therapeutic effect after 28 days of using Livazo, the daily dose should be increased to 2 mg, in most cases this dose provides the optimal effect. The maintenance dose is selected individually according to the patient's response to treatment, LDL cholesterol concentrations and the goal of treatment. The maximum daily dose of Livazo should not exceed 4 mg.
The maximum daily dose for severe renal failure and mild to moderate liver dysfunction is 2 mg.
The use of a dose of Livazo 4 mg in patients with impaired renal function of any severity is allowed only in cases of urgent need by a gradual increase in the dose, if careful monitoring of renal function is ensured.
Elderly patients do not need dose adjustment.
Side effects
Unwanted disorders that occur when taking Livazo (classified as follows: very often - ≥ 1/10, often - ≥ 1/100 and <1/10, infrequently - ≥ 1/1000 and <1/100, rarely - ≥ 1/10 000 and <1/1000, very rarely - <1/10 000, including isolated cases):
- on the part of the hematopoietic organs: infrequently - anemia;
- from the nervous system: often - headache; infrequently - drowsiness, dizziness, impaired taste;
- mental disorder: often - insomnia;
- from the side of metabolism: infrequently - anorexia;
- from the digestive system: often - dyspepsia, nausea, constipation, diarrhea; infrequently - dryness of the oral mucosa, vomiting, abdominal pain; rarely - cholestatic jaundice, glossodynia, acute pancreatitis;
- from the musculoskeletal system: often - arthralgia, myalgia; infrequently - muscle spasms;
- from the senses: infrequently - ringing in the ears; rarely - decreased visual acuity;
- from the urinary system: infrequently - pollakiuria;
- dermatological reactions: infrequently - itching, skin rash; rarely - erythema, urticaria;
- laboratory indicators: infrequently - increased activity of alanine aminotransferase (ALT) and aspartate aminotransferase (AST), creatine phosphokinase (CPK);
- others: infrequently - increased fatigue, asthenia, malaise, peripheral edema.
In addition, during the post-marketing use of Livazo, the following undesirable phenomena were recorded:
- from the hepatobiliary system: rarely - abnormal liver function, liver disease;
- from the musculoskeletal system: rarely - myopathy, rhabdomyolysis (including with acute renal failure and death);
- from the nervous system: infrequently - hypesthesia;
- from the digestive system: rarely - abdominal discomfort.
It should be borne in mind that against the background of the use of other statins, side effects such as sleep disturbance (including nightmares), depression, diabetes mellitus, interstitial lung disease, increased glycosylated hemoglobin, and sexual dysfunction have occurred.
Overdose
Overdose symptoms have not been established.
Treatment: the appointment of symptomatic therapy. It is necessary to carefully monitor liver function and CPK activity. Hemodialysis is ineffective.
special instructions
When prescribing Livazo to establish a control baseline value, the CPK activity should be determined in patients with predisposing factors for the development of rhabdomyolysis. It is impossible to start treatment with the drug if the CPK values exceed the VGN by 5 times.
Due to the effect of statins on muscle tissue, while using pitavastatin, there is a risk of developing myalgia, myopathy and rhabdomyolysis. Therefore, when prescribing Livazo, it is necessary to warn the patient about the need to see a doctor if muscle pain occurs, muscle soreness on palpation or weakness, convulsions. For any symptoms of the muscular system, the activity of CPK should be determined, especially if they are accompanied by fever or malaise. If the CPK activity is 5 times higher than the VGN, the treatment is stopped and a control analysis is performed 5-7 days later. The question of stopping the pill intake can be considered in case of severe muscle symptoms, even if the CPK activity does not exceed the VGN by 5 times. After resolution of symptoms and return of CPK activity to normal, treatment in a daily dose of 1 mg can be resumed.
Functional liver function tests should be performed before and periodically during treatment. With a persistent increase in the activity of ALT and AST, exceeding 3 times the VGN, Livazo's treatment should be discontinued.
In patients predisposed to the development of hyperglycemia (fasting glucose concentration 5.6–6.9 mmol / l, increased thyroglobulin concentration, body mass index over 30 kg / m 2, arterial hypertension), Livazo should be accompanied by clinical and biochemical control.
Clinical signs of interstitial lung disease include shortness of breath, unproductive cough, fatigue, fever, and weight loss. If the general health condition worsens against the background of their appearance, therapy should be discontinued.
Influence on the ability to drive vehicles and complex mechanisms
In connection with the possible appearance of dizziness and drowsiness during the period of taking Livazo, patients are advised to be careful when driving vehicles or complex mechanisms.
Application during pregnancy and lactation
The use of Livazo is contraindicated during pregnancy and breastfeeding.
Conception should not be allowed while taking the drug, so women of childbearing age need to use reliable methods of contraception. In case of conception, immediate discontinuation of the pill is required.
You can plan a pregnancy only one month after the cancellation of Livazo.
Pediatric use
The efficacy and safety of using the drug in children have not been established, therefore, the appointment of Livazo is contraindicated in patients under 18 years of age.
With impaired renal function
Caution should be exercised when using Livazo in patients with renal insufficiency. The maximum daily dose for patients in this category is 2 mg.
For violations of liver function
The use of Livazo is contraindicated in severe hepatic insufficiency (class C according to the Child-Pugh classification), active liver disease, a sustained increase in the activity of liver transaminases in the blood serum (more than 3 times compared with VGN).
Patients with a history of liver disease should be used with caution. For this category of patients, the daily dose of Livazo 2 mg should not be exceeded.
Use in the elderly
Livazo should be taken with caution in elderly patients; dose adjustment is not required.
Drug interactions
- cyclosporine: a single dose of cyclosporine causes an increase in the AUC of pitavastatin by 4.6 times, therefore, their combined use is contraindicated;
- erythromycin: in the case of prescribing antibiotics of the macrolide group, including erythromycin, it is necessary to temporarily stop treatment with pitavastatin, since against the background of a combination of drugs, the AUC of pitavastatin increases by 2.8 times;
- fibrates, including gemfibrozil: the combination of statins with fibrates increases the risk of myopathy and rhabdomyolysis, therefore, caution should be exercised;
- nicotinic acid (in a daily dose of more than 1 g): take nicotinic acid in lipid-lowering doses with caution, due to the fact that with monotherapy it can cause the development of myopathy and rhabdomyolysis;
- fusidic acid: it should be borne in mind that the interaction of fusidic acid and statins contributes to the occurrence of severe muscle disorders, including rhabdomyolysis. In this regard, if it is necessary to prescribe fusidic acid, Livazo should be temporarily discontinued;
- rifampicin: increases the AUC of pitavastatin by 1.3 times;
- HIV protease inhibitors (human immunodeficiency virus): against the background of their combined intake with pitavastatin, there is a slight change in the latter's AUC;
- ezetimibe: does not affect the concentration of pitavastatin, in turn, pitavastatin does not affect the concentration of ezetimibe or its glucuronide metabolite in plasma;
- grapefruit juice, itraconazole: no effect of these and other inhibitors of the CYP3A4 isoenzyme on the plasma concentrations of pitavastatin was found;
- digoxin: the combination of pitavastatin with digoxin does not lead to significant changes in plasma concentrations of each drug;
- warfarin: concomitant therapy with warfarin is recommended to be accompanied by monitoring of prothrombin time and INR (international normalized ratio).
Analogs
Livazo's analogs are: Cleivas, Crestor, Rosart, Rovix, Rosucard, Roxera, Romazik, Rosvator, Rosulip, Rosuvastatin, Fastrong, Sandoz, Mertenil, Atorvasterol, Atormak, Allesta, Astin, Vabadin, Vasta, Vasoklinor, Zosta, Litorva, Lipodemin, Simvakor, Pravapres, Limistin, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C in a dark place.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Livazo
Reviews about Livazo are positive. Experts call it a drug of a new, innovative generation of statins. It is noted that the target effect from the use of the drug is achieved by taking smaller doses than other statins. Also, the drug received positive reviews in relation to its use in patients over the age of 65 years. Of the shortcomings, some patients mention the cost of Livazo, since it takes a long time to take it.
The price of Livazo in pharmacies
The price of Livazo for a package containing 28 tablets in a dose of 1 mg can be 427-589 rubles, 2 mg - 694-826 rubles, 4 mg - 904-1028 rubles.
Livazo: prices in online pharmacies
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Drug name Price Pharmacy |
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Livazo 1 mg film-coated tablets 28 pcs. 427 r Buy |
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Livazo tablets p.p. 1mg 28 pcs. 632 RUB Buy |
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Livazo 2 mg film-coated tablets 28 pcs. 694 RUB Buy |
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Livazo tablets p.p. 2mg 28 pcs. RUB 879 Buy |
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Livazo 4 mg film-coated tablets 28 pcs. RUB 899 Buy |
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Livazo tablets p.p. 4mg 28 pcs. 1098 RUB Buy |
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!
