Livazo 4 mg 28 pcs. film-coated tablets

An increase in blood cholesterol levels and the initial stage of atherosclerosis are direct indications for starting therapy. The basis of all medications used in the course of treatment are statins. They reduce the amount of cholesterol produced in the body and significantly improve the patient’s well-being.

One of these drugs is Livazo 2 mg. This medicine is also available in active ingredient quantities of 1 mg and 4 mg, and the specific dosage prescribed depends on the severity of the disease and is at the discretion of the attending physician.

Active substance and indications for use

The active ingredient of the drug Livazo is pitavastatin - this component is a lipid-lowering agent designed to reduce the production of its own “bad” cholesterol in the human body. Livazo is a prominent representative of HMG-CoA reductase inhibitors (statins); this group of drugs is prescribed to almost all patients with high cholesterol in the blood.

Indications for use of Livazo:

• primary hypercholesterolemia (increased cholesterol levels in the blood, recorded for the first time, without linking the pathology to concomitant diseases);
• hereditary hypercholesterolemia (to reduce low-density lipoproteins in the blood).

This drug is also prescribed in cases where it is not possible to reduce cholesterol in patients on a diet or performing therapeutic exercises.

Livazo is produced by the manufacturer in three dosages:

• 1 mg – contains 1.045 mg of pitavastatin calcium (corresponding to 1 mg of pitavastatin);
• 2 mg – includes 2.090 mg pitavastatin calcium (corresponding to 2 mg pitavastatin);
• 4 mg – pitavastatin calcium content 4.180 mg (equivalent to 4 mg pitavastatin).

Tablets in all three dosages are film-coated, they are painted white, have a round shape, on one side there is an engraving of KS, and on the other - the volume of the active substance, indicated by the numbers 1,2,3 (respectively 1 mg, 2 mg, 4 mg ).

According to the official instructions for use of Livazo from the manufacturer, the tablets should be taken orally without chewing first and without coordinating the time of administration with food. The drug is taken once a day, it is advisable to take the tablets at the same time to achieve maximum effect

Livazo 4 mg 28 pcs. film-coated tablets

pharmachologic effect

Pitavastatin is a competitive inhibitor of HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase.
an enzyme that catalyzes the initial stage of cholesterol synthesis - the formation of mevalonic acid from HMG-CoA. Since the conversion of HMG-CoA to mevalonic acid is the initial stage of cholesterol synthesis, the use of pitavastatin does not cause the 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. Clinical studies have shown the effectiveness of Livazo in reducing the concentration of total cholesterol (OXC) in the blood plasma and low-density lipoprotein cholesterol (LDL-C). very low density lipoprotein cholesterol (VLDL cholesterol). triglycerides (TG) and apolipoprotein B (Apo-B). as well as increased concentrations of high-density lipoprotein cholesterol (HDL-C) and apolipoprotein A1 (Apo-A1) (see Table 1). Table 1. Dose responses in patients with primary hypercholesterolemia (adjusted mean percent change from baseline)

*uncorrected

In controlled clinical studies involving 1687 patients with primary hypercholesterolemia and combined (mixed) dyslipidemia, including 1239 patients receiving therapeutic doses (average initial LDL cholesterol concentration of about 4.8 mmol/l), pitavastatin significantly reduced the concentration of LDL cholesterol and total cholesterol. non-HDL-C, TG and Apo-B and increased the concentration of HDL-C and Apo-A1. The ratios of TC/HDL cholesterol and Apo-B/Apo-A1 decreased.

The concentration of LDL cholesterol decreased by 18-39% when using Livazo at a dose of 2 mg and by 44-45% when using a dose of 4 mg. Most patients receiving a dose of 2 mg. achieved the LDL cholesterol treatment target according to the recommendations of the European Atherosclerosis Society (EAS) (

Composition and release form Livazo 4 mg 28 pcs. film-coated tablets

Tablets - 1 tablet:

• Active substance: pitavastatin calcium 4.18 mg, which corresponds to the content of pitavastatin 4 mg.
• Excipients: lactose monohydrate, low-substituted hyprolose, hypromellose, magnesium aluminometasilicate, magnesium stearate.
• Film shell composition: Opadry white, including hypromellose, titanium dioxide, triethyl acetate, colloidal silicon dioxide.

14 pcs. - blisters (2) - cardboard packs.

Description of the dosage form

Tablets, film-coated, white, round, biconvex, with a white core in cross section; on one side of the tablet there is an engraving “KC”, on the other there is an engraving “2”.

Directions for use and doses

Inside, tablets must be swallowed whole.

It is preferable to take the tablet at the same time of day, preferably in the evening, in accordance with the circadian rhythm of lipid metabolism. Before starting treatment and during the process, patients should adhere to a cholesterol-lowering diet.

The initial dose of the drug is 1 mg/day once. If necessary, the dose of the drug is increased at intervals of at least 4 weeks to 2 mg/day. The dose should be individualized based on LDL-C concentrations, the goal of treatment, and the patient's response to treatment. Most patients require a dose of 2 mg. The maximum daily dose is 1 mg.

Patients with mild to moderate liver dysfunction: A maximum daily dose of 2 mg is recommended.

Patients with impaired renal function: in case of mild renal impairment (it is advisable to objectively assess this degree by reflecting CC or glomerular filtration rate), Livazo should be used with caution. Data on the use of a maximum daily dose of 4 mg for renal impairment of any severity are limited, therefore, a maximum daily dose of 4 mg should be prescribed only with careful monitoring of renal function after a gradual dose increase. It is not recommended that patients with severe renal impairment be prescribed a maximum daily dose of 4 mg; It is recommended to consider limiting the maximum daily dose to 2 mg in severe renal impairment.

Elderly patients: no dose adjustment is required.

Pharmacokinetics

Suction

Pitavastatin is rapidly absorbed in the upper gastrointestinal tract, Cmax in blood plasma is achieved within 1 hour after taking the drug. Eating does not affect absorption. Cmax of pitavastatin in blood plasma decreases by 43% when taken together with fatty foods, but AUC remains unchanged. The unchanged drug undergoes enterohepatic circulation and is well absorbed from the jejunum and ileum. The absolute bioavailability of pitavastatin is 51%.

Distribution

More than 99% of pitavastatin is bound to plasma proteins, mainly albumin and alpha-1 acid glycoprotein. Average Vd 133 l. Pitavastatin actively penetrates into hepatocytes using the transport proteins OATP1B1 and OATP1B3. AUC varies within a 4-fold increase from minimum to maximum values. Pitavastatin is not a substrate for P-glycoprotein.

Metabolism

Plasma contains mainly unchanged pitavastatin. The main metabolite is an inactive lactone, which is formed from the ether-type pitavastatin glucuronide conjugate with the participation of UDP-glucuronosyltransferases (UGT1A3 and 2B7). Cytochrome P450 has a minimal effect on the metabolism of pitavastatin. The CYP2C9 isoenzyme (and to a lesser extent the CYP2C8 isoenzyme) is involved in the metabolism of pitavastatin to minor metabolites.

Removal

Pitavastatin, unchanged, is rapidly excreted from the liver with bile, but undergoes enterohepatic recirculation, which ensures its long-lasting effect. Less than 5% of pitavastatin is excreted by the kidneys. T1/2 from plasma varies from 5.7 hours (single dose) to 8.9 hours (at steady state), the average clearance is 43.4 l/h after a single oral dose.

Pharmacokinetics of different groups of patients

Elderly patients: In clinical studies of the pharmacokinetics of pitavastatin, it was shown that in elderly patients over 65 years of age, the AUC of pitavastatin was 1.3 times higher. This did not affect efficacy or safety.

Hepatic impairment: in patients with mild hepatic impairment (Child-Pyot class A), the AUC was 1.6 times higher than in healthy volunteers, while in patients with moderate hepatic impairment (Child-Pyot class B) the AUC was 1.6 times higher than in healthy volunteers. AUC was 3.9 times higher. In cases of severe liver dysfunction, the use of pitavastatin is contraindicated.

Renal failure: in patients with moderate renal failure and on hemodialysis, an increase in AUC was observed by 1.8 times and 1.7 times, respectively.

Gender differences: there was a 1.6-fold increase in AUC in women compared to men in a study of healthy volunteers, which did not in any way affect the effectiveness and safety of the drug Livazo.

Race: According to the results of pharmacokinetic analysis of data obtained from healthy volunteers of different races, factors such as gender and age did not affect the pharmacokinetics of pitavastatin.

Indications for use Livazo 4 mg 28 pcs. film-coated tablets

Primary hypercholesterolemia, including heterozygous familial hypercholesterolemia (Fredrickson type IIa hyperlipidemia) or mixed hypercholesterolemia (Fredrickson type IIb hyperlipidemia), hypertriglyceridemia (Fredrickson type IV hyperlipidemia) as an adjunct to diet, when diet and other non-drug treatments ( for example, physical exercise, weight loss) are insufficient.

Contraindications

• Hypersensitivity to pitavastatin, auxiliary components of the drug and other HMG-CoA reductase inhibitors (statins);
• severe liver failure (more than 9 points on the Child-Pugh scale) or class C according to the Child-Pugh classification, liver disease and active phase, including a persistent increase in the activity of “liver” transaminases in the blood serum (more than 3 times compared with the upper limit norms (ULN));
• lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
• myopathy;
• simultaneous use of cyclosporine;
• pregnancy, breastfeeding, lack of adequate methods of contraception in women of childbearing age;
• age under 18 years (efficacy and safety have not been established).

Carefully

If there is a risk of developing myopathy/rhabdomyolysis - renal failure, hypothyroidism, personal or family history of hereditary muscle diseases and previous history of muscle toxicity when using other HMG-CoA reductase inhibitors or fibrates, excessive alcohol consumption, age over 70 years, history of liver disease .

Application of Livazo 4 mg 28 pcs. film-coated tablets during pregnancy and breastfeeding

Pregnancy

The use of Livazo during pregnancy is contraindicated. Women of childbearing age should use reliable methods of contraception when treating Livazo. Because Since cholesterol and other products of cholesterol biosynthesis are necessary for fetal development, the potential risk of inhibition of HMG-CoA reductase outweighs the benefit of treatment with the drug during pregnancy. Animal studies have shown that pitavastatin has reproductive toxicity but no teratogenic potential. If the patient is planning a pregnancy, treatment should be discontinued at least one month before conception. If pregnancy occurs while using Livazo. treatment should be stopped immediately.

Breastfeeding period

The use of Livazo during breastfeeding is contraindicated. Pitavastatin is excreted in the milk of lactating rats. There are no data on the excretion of pitavastatin in breast milk. If it is necessary to use the drug Livazo during lactation, breastfeeding should be stopped.

Use in childhood

The use of the drug in patients under the age of 18 is prohibited (since the effectiveness and safety have not been established).

special instructions

Effect on muscle tissue

As with the use of other HMG-CoA reductase inhibitors (statins). there is a possibility of developing myalgia, myopathy and, in rare cases, rhabdomyolysis. Patients should be warned to report any muscle symptoms. CPK activity should be determined in any patient reporting muscle pain, muscle tenderness or weakness, especially if accompanied by malaise or fever.

CPK activity should not be determined after physical exercise or in the presence of any other possible reasons for the increase in CPK that may distort the result. If CPK activity increases (5 times higher than ULN), a control analysis should be performed within 5-7 days.

Before treatment

Like all statins, Livazo should be prescribed with caution to patients with predisposing factors for the development of rhabdomyolysis. CPK activity should be determined to establish a reference baseline value in the following cases:

• renal failure;
• hypothyroidism;
• personal or family history of hereditary muscle diseases;
• previous history of muscle toxicity during treatment with fibrates or other statins;
• a history of liver disease or alcohol abuse;
• elderly patients (over 70 years of age) with other predisposing risk factors for the development of rhabdomyolysis.

In such cases, clinical monitoring is recommended and the risk of treatment should be considered in relation to the potential benefit. Treatment with Livazo cannot be started if CK levels are 5 times higher than the ULN.

During the flow

The patient should be advised to immediately report muscle pain, weakness or cramps to the doctor. CPK activity should be determined, and treatment should be stopped if CPK activity is elevated (5 times the ULN). Consideration should be given to discontinuing treatment if severe muscle symptoms occur, even if CPK activity does not exceed 5 times the ULN. When symptoms resolve and CPK activity returns to normal, re-prescribing Livazo at a dose of 1 mg may be considered, subject to careful monitoring.

Effects on the liver

Like all statins, Livazo should be prescribed with caution to patients with a history of liver disease or to patients who regularly drink excessive amounts of alcohol. Before starting treatment with Livazo and then periodically during treatment, liver function tests should be performed. Patients with a persistent increase in the activity of “liver” transaminases (ALT and AST), exceeding ULN by 3 times, should stop treatment with Livazo.

Effects on the kidneys

Livazo should be administered with caution to patients with moderate or severe renal impairment. The dose should be increased only with careful monitoring. The 4 mg dose is not recommended for patients with severe renal impairment.

Diabetes

Some data suggests that. that statins, as a class, cause an increase in blood glucose concentrations and, in some patients at high risk of developing diabetes mellitus, can lead to a level of hyperglycemia at which appropriate diabetes treatment is necessary. However, this risk is offset by the reduction in vascular risk with statin treatment and should therefore not be a reason to discontinue statin treatment. Patients at risk of developing hyperglycemia (fasting glucose concentration from 5.6 to 6.9 mmopi/l, BMI>30 kg/m2, elevated TG concentrations, arterial hypertension) should be subjected to clinical and biochemical monitoring in accordance with national recommendations.

Interstitial lung disease

Rare cases of interstitial lung disease have been reported with the use of some drugs, especially with long-term therapy.

Observed clinical signs include shortness of breath, nonproductive cough, and deterioration in general health (fatigue, weight loss, and fever). If interstitial lung disease is suspected, statin therapy should be discontinued.

Impact on the ability to drive vehicles and maintain moving mechanisms

Caution must be exercised when driving vehicles or performing other work that requires increased attention, as undesirable reactions such as dizziness and drowsiness may develop.

Overdose

There is no specific treatment for overdose.

It is necessary to carry out symptomatic therapy, monitor CPK activity and liver function. Hemodialysis is ineffective.

Side effects of Livazo 4 mg 28 pcs. film-coated tablets

In controlled clinical studies, when taking recommended doses, less than 4% of patients treated with Lnvaso. was excluded from the study due to the development of adverse reactions. The most common was myapgia.

Depending on the frequency of occurrence, the following adverse reactions are distinguished in accordance with the WHO classification: very often: ≥10, often: from ≥1/100 to

From the hematopoietic organs: infrequently - anemia.

From the side of metabolism: infrequently - anorexia.

Mental disorders: often - insomnia.

From the nervous system: often - headache; infrequently - dizziness, taste disturbance, drowsiness.

From the senses: infrequently - ringing in the ears; rarely - decreased visual acuity.

From the skin: infrequently - itchy skin, soup; rarely - urticaria, erythema.

From the musculoskeletal system: often - myalgia, arthralgia; infrequently - muscle spasms.

From the urinary system: infrequently - pollakiuria.

From the digestive system: often - constipation, diarrhea, dyspepsia, nausea; infrequently - abdominal pain, dryness of the oral mucosa, vomiting; rarely - glossodynia, acute pancreatitis, cholestatic jaundice.

Laboratory indicators: infrequently - increased activity of liver transaminases AST, ALT, increased activity of creatine phosphokinase (CPK).

In clinical studies, after taking Livazo, an increase in CK activity was observed 3 times higher than the ULN in 49 patients out of 2800 (1.8%). Levels of 10 times or more ULN with associated muscle symptoms were rare and were observed in only one patient out of 2406 patients receiving 4 mg Livazo (0.04%) in the clinical trial program.

Other: infrequently - asthenia, malaise, increased fatigue, peripheral edema.

Post-marketing experience

A 2-year prospective post-marketing follow-up study was conducted on approximately 20,000 patients in Japan. The vast majority of these patients received pitavastatin 1 or 2 mg rather than 4 mg. In 10.4% of patients, adverse reactions were reported in which a causal relationship with pitavastatin cannot be excluded, and 7.4% of patients discontinued treatment due to the development of adverse reactions. The incidence of myalgia was 1.08%. Most adverse reactions were mild. Over a 2-year period, the incidence of adverse reactions was higher in patients with a history of drug allergies (20.4%) or liver or kidney disease (13.5%).

Adverse reactions and their incidence observed in a prospective post-marketing surveillance study, but not in international controlled clinical studies, with the use of the drug and recommended doses are listed below.

From the liver and biliary tract: rarely - impaired liver function.

From the musculoskeletal system: rarely - myopathy, rhabdomyolysis.

In the post-marketing surveillance study, there were two reports of rhabdomyolysis requiring hospitalization (0.01% of patients).

In addition, there are spontaneous reports of musculoskeletal effects, including myalgia and myopathy, in patients treated with Livazo at all recommended doses. There have also been reports of rhabdomyolysis with and without acute renal failure, including fatal rhabdomyolysis.

Spontaneous reports of the following adverse reactions have also been received (frequency based on incidence observed in post-marketing studies).

From the nervous system: infrequently - hypoesthesia.

From the digestive system: rarely - abdominal discomfort.

Adverse events when using other statins:

• sleep disturbances, including nightmares;
• amnesia;
• sexual dysfunction;
• depression;
• interetitial lung disease;
• diabetes mellitus: the incidence depends on the presence or absence of risk factors (fasting blood glucose concentration ≥5 mmol/l, BMI>30 kg/m2, elevated TG concentration, history of arterial hypertension);
• increase in glycosylated hemoglobin.

Drug interactions

Pitavastatin is actively transported into the human hepatocyte by numerous hepatic transporters (including organic anion transport polypeptide (OATP)), which may be involved in some of the following interactions.

Cyclosporine: Co-administration of a single dose of cyclosporine with pitavastatin at steady state results in a 4.6-fold increase in pitavastatin AUC unknown. Livazo is contraindicated in patients receiving treatment with cyclosporine.

Erythromycin: Concomitant administration of erythromycin with pitavastatin results in a 2.8-fold increase in the AUC of pitavastatin. It is recommended to temporarily discontinue taking pitavastatin during treatment with erythromycin or other macrolide antibiotics.

Gemfibrozole and other fibrates have rarely been associated with fibrate monotherapy with the development of myopathy. Concomitant use of fibrates with statins has been associated with an increased incidence of myopathy and rhabdomyolysis. Caution should be exercised when using pitavastatin concomitantly with fibrates. In pharmacokinetic studies, coadministration of pitavastatin with gemfibrozil resulted in a 1.4-fold increase in pitavastatin AUC and a 1.2-fold increase in fenofibrate AUC.

Nicotinic acid (at lipid-lowering doses): interaction studies have not been conducted during treatment with pitavastatin and nicotinic acid at lipid-lowering doses (more than 1 g/day). The use of nicotinic acid in monotherapy has been associated with the development of myopathy and rhabdomyolysis. Therefore, when used simultaneously with nicotinic acid in lipid-lowering doses (more than 1 g/day), Livazo should be prescribed with caution.

Fusidic acid: Severe muscle disorders, such as rhabdomyolysis, have been reported and have been attributed to an interaction between fusidic acid and statins. During treatment with fusidic acid, it is recommended to temporarily stop using Livazo.

Rifampicin: Coadministration with pitavastatin resulted in a 1.3-fold increase in pitavastatin AUC.

Ezetimibe and its glucuronide metabolite inhibits the absorption of dietary and biliary cholesterol. Concomitant use of pitavastatin had no effect on plasma concentrations of pitavastatin.

CYP3A4 inhibitors: Interaction studies with itraconazole and grapefruit juice, known inhibitors of the CYP3A4 isoenzyme, did not reveal a clinically significant interaction on plasma concentrations of pitavastatin.

Digoxin, a known P-glycoprotein (Pgp) substrate, does not interact with pitavastatin. When used together, there were no significant changes in plasma concentrations of pitavastatin or digoxin.

Warfarin: Steady-state pharmacokinetics and pharmacodynamics (INR and prothrombin time (PT)) of warfarin in healthy volunteers were not affected by coadministration of warfarin with pitavastatin 4 mg daily. However, as with other statins, PT and INR should be monitored in patients receiving warfarin when pitavastatin is added to treatment.

How the drug works

The active substance of the drug Livazo pitavastatin slows down the rate of production of HMG-CoA reductase, thereby reducing the amount of cholesterol produced by liver tissue. As a result, receptors that produce low-density lipoproteins in the liver are activated, and the amount of total cholesterol in the blood plasma decreases.

Pitavastatin is well absorbed by intestinal tissues, and its bioavailability is 51%. After taking a tablet in a dosage of 1, 2 or 4 mg, the maximum concentration of the substance in the blood plasma is observed after 60 minutes. The absorption efficiency of Livazo is not associated with food intake. According to medical statistics, when pitavastatin was taken orally and at the same time consumed fatty foods, the concentration of the substance in the blood decreased to 43%.

No ads 1

Livazo tablet p o film 2 mg x28

Livazo film tablet 2 mg x28, ATX code: C10AA08 (Pitavastatin) Active substance: pitavastatin (pitavastatin) Rec.INN registered by WHO

Dosage form

LIVAZO

film-coated tablets, 4 mg: 7, 10, 14, 15, 20, 28, 30, 42 or 45 pcs.reg. No.: LP-002855 dated 02/09/15 - Valid

Release form, composition and packaging

The tablets are white, film-coated, round, biconvex, with a white core on the cross section, on one side of the tablet there is an engraving “KC”, on the other there is an engraving “4”.

1 tab.

pitavastatin calcium 4.18 mg,

 which corresponds to the content of pitavastatin 4 mg

Excipients: lactose monohydrate - 252.34 mg, low-substituted hyprolose - 50.16 mg, hypromellose - 5.32 mg, magnesium aluminometasilicate - 6.4 mg, magnesium stearate - 1.6 mg.

Film shell composition: Opadry white - 9 mg, including hypromellose - 5.952 mg, titanium dioxide - 2.409 mg, triethyl acetate - 0.594 mg, colloidal silicon dioxide - 0.045 mg.

Clinical and pharmacological group: Lipid-lowering drug Pharmaco-therapeutic group: Lipid-lowering drug - HMG-CoA reductase inhibitor,

Indications: primary hypercholesterolemia, including heterozygous familial hypercholesterolemia (hyperlipidemia type IIa according to the Fredrickson classification) or mixed hypercholesterolemia (hyperlipidemia type IIb according to the Fredrickson classification), hypertriglyceridemia (hyperlipidemia type IV according to the Fredrickson classification) as an addition to the diet, when diet and other non-drug Treatment methods (eg, exercise, weight loss) are insufficient. ICD-10 codes,

Dosage regimen

Inside, tablets must be swallowed whole.

It is preferable to take the tablet at the same time of day, preferably in the evening, in accordance with the circadian rhythm of lipid metabolism. Before starting treatment and during the process, patients should adhere to a cholesterol-lowering diet.

The initial dose of the drug is 1 mg/day once. If necessary, the dose of the drug is increased at intervals of at least 4 weeks to 2 mg/day. The dose should be individualized based on LDL-C concentrations, the goal of treatment, and the patient's response to treatment. Most patients require a dose of 2 mg. The maximum daily dose is 1 mg.

Patients with mild to moderate liver dysfunction: A maximum daily dose of 2 mg is recommended.

Patients with impaired renal function: in case of mild renal impairment (it is advisable to objectively assess this degree by reflecting CC or glomerular filtration rate), Livazo should be used with caution. Data on the use of a maximum daily dose of 4 mg for renal impairment of any severity are limited, therefore, a maximum daily dose of 4 mg should be prescribed only with careful monitoring of renal function after a gradual dose increase. It is not recommended that patients with severe renal impairment be prescribed a maximum daily dose of 4 mg; it is recommended to consider limiting the maximum daily dose to 2 mg in severe renal impairment.

Elderly patients: no dose adjustment is required.

Side effect

In controlled clinical studies, when taking recommended doses, less than 4% of patients treated with Lnvaso. was excluded from the study due to the development of adverse reactions. The most common was myapgia.

Depending on the frequency of occurrence, the following adverse reactions are distinguished in accordance with the WHO classification: very often: ≥10, often: from ≥1/100 to <.1/10, infrequently: from ≥1/1000 to <.1/100, rarely : from ≥1/10000 to <.1/10000, very rare: <.1/10000 n frequency unknown (available data do not allow frequency to be determined).

From the hematopoietic organs: infrequently - anemia.

From the side of metabolism: infrequently - anorexia.

Mental disorders: often - insomnia.

From the nervous system: often - headache, infrequently - dizziness, taste disturbance, drowsiness.

From the senses: infrequently - ringing in the ears, rarely - decreased visual acuity.

From the skin: infrequently - itching, soup, rarely - urticaria, erythema.

From the musculoskeletal system: often - myalgia, arthralgia, infrequently - muscle spasms.

From the urinary system: infrequently - pollakiuria.

From the digestive system: often - constipation, diarrhea, dyspepsia, nausea, infrequently - abdominal pain, dry oral mucosa, vomiting, rarely - glossodynia, acute pancreatitis, cholestatic jaundice.

Laboratory indicators: infrequently - increased activity of liver transaminases AST, ALT, increased activity of creatine phosphokinase (CPK).

In clinical studies, after taking Livazo, an increase in CK activity was observed 3 times higher than the ULN in 49 patients out of 2800 (1.8%). Levels of 10 times or more ULN with associated muscle symptoms were rare and were observed in only one patient out of 2406 patients receiving 4 mg Livazo (0.04%) in the clinical trial program.

Other: infrequently - asthenia, malaise, increased fatigue, peripheral edema.

Post-marketing experience

A 2-year prospective post-marketing follow-up study was conducted on approximately 20,000 patients in Japan. The vast majority of these patients received pitavastatin 1 or 2 mg rather than 4 mg. In 10.4% of patients, adverse reactions were reported in which a causal relationship with pitavastatin cannot be excluded, and 7.4% of patients discontinued treatment due to the development of adverse reactions. The incidence of myalgia was 1.08%. Most adverse reactions were mild. Over a 2-year period, the incidence of adverse reactions was higher in patients with a history of drug allergies (20.4%) or liver or kidney disease (13.5%).

Adverse reactions and their incidence observed in a prospective post-marketing surveillance study, but not in international controlled clinical studies, with the use of the drug and recommended doses are listed below.

From the liver and biliary tract: rarely - impaired liver function.

From the musculoskeletal system: rarely - myopathy, rhabdomyolysis.

In the post-marketing surveillance study, there were two reports of rhabdomyolysis requiring hospitalization (0.01% of patients).

In addition, there are spontaneous reports of musculoskeletal effects, including myalgia and myopathy, in patients treated with Livazo at all recommended doses. There have also been reports of rhabdomyolysis with and without acute renal failure, including fatal rhabdomyolysis.

Spontaneous reports of the following adverse reactions have also been received (frequency based on incidence observed in post-marketing studies).

From the nervous system: infrequently - hypoesthesia.

From the digestive system: rarely - abdominal discomfort.

Adverse events when using other statins:

- sleep disturbances, including nightmares,

- amnesia,

- sexual dysfunction,

- depression,

- interetitial lung disease,

— diabetes mellitus: the incidence depends on the presence or absence of risk factors (fasting blood glucose concentration ≥5 mmol/l, BMI>30 kg/m2, elevated TG concentration, history of arterial hypertension),

- increase in glycosylated hemoglobin.

Contraindications for use

- hypersensitivity to pitavastatin, auxiliary components of the drug and other HMG-CoA reductase inhibitors (statins),

- severe liver failure (more than 9 points on the Child-Pugh scale) or class C according to the Child-Pugh classification, liver disease and active phase, including a persistent increase in the activity of “liver” transaminases in the blood serum (more than 3 times compared with the upper normal limit (ULN)),

- lactose intolerance, lactase deficiency or glucose-galactose malabsorption,

- myopathy,

- simultaneous use of cyclosporine,

- pregnancy, breastfeeding, lack of adequate methods of contraception in women of childbearing age,

- age under 18 years (efficacy and safety have not been established).

Carefully

If there is a risk of developing myopathy/rhabdomyolysis - renal failure, hypothyroidism, personal or family history of hereditary muscle diseases and previous history of muscle toxicity when using other HMG-CoA rsductase inhibitors or fibrates, excessive alcohol consumption, age over 70 years, history of liver disease .

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Instructions for use

Therapy with statin drugs requires mandatory adherence to a diet with a reduced amount of plant-based fats in the diet. When using Livazo, preference should be given to plant foods, cereals, grains, vegetables and fruits.

It is necessary to give up table salt and sugar or reduce the amount of their consumption. Prohibited foods are fatty meats and fish, bread, carbonated drinks, baked goods, spicy, over-salted, smoked foods. The dosage of pitavastatin per day required for a particular patient is selected in accordance with the test results.

The patient buys Livazo at the pharmacy exclusively in the dose recommended by the attending doctor. Initially, the patient is prescribed tablets at a dosage of 1 mg, adjusting the recommendation over the next 4 weeks. Practice shows that for most people with elevated blood cholesterol levels, the best option is to take Livazo 2 mg once a day.

Contraindications and side effects

Statins are a group of drugs that have a large number of side effects, which is why their independent use is unacceptable. Patients often complain about the following negative effects of Livazo:

• headache;
• nausea, urge to vomit, disturbances in stool stability (alternating constipation and diarrhea);
• pain in muscles and joints, myalgia;
• drowsiness or, conversely, insomnia;
• slight loss of taste;
• general malaise.

With long-term therapy with statins, some patients experience ringing in the ears, swelling on the body, and allergic-type rashes on the skin. The level of hemoglobin in the blood may decrease and the volume of transaminases may increase.

The rarest side effects of Livazo include impaired liver function, the development of acute pancreatitis, significant deterioration in memory and visual function, and a tendency to depression and psychosis. In isolated cases, patients taking statins have experienced nightmares, decreased libido, and loss of sexual function.

You should not take statin drugs, including Livazo, if you have the following health problems:

Doctor Myasnikov’s opinion on the benefits and harms of statins

• liver diseases occurring in acute form or their chronic forms in the acute stage;
• special sensitivity to the drug group statins and their active ingredients;
• galactose intolerance (including those having a hereditary etiology);
• malabsorption syndrome;
• simultaneous use of drugs from the cephalosporin group;
• myopathy.

Statins are not prescribed to patients under 18 years of age, as well as to women who are pregnant or breastfeeding a newborn child. If Livazo is recommended for use by a woman of childbearing age, she must take oral contraceptives so that an unexpected pregnancy does not occur during statin therapy.

No ads 2

Livazo 2 mg tablet p/o No. 28

Effect on muscle tissue

As with other HMG-CoA reductase inhibitors (statins), there is a possibility of developing myalgia, myopathy and, in rare cases, rhabdomyolysis. Patients should be warned to report any muscle symptoms. CPK activity should be determined in any patient reporting muscle pain, muscle tenderness or weakness, especially if accompanied by malaise or fever.

CPK activity should not be determined after physical exercise or in the presence of any other possible reasons for the increase in CPK that may distort the result. If CPK activity increases (5 times higher than ULN), a control analysis should be performed within 5–7 days.

Very rare cases of immune-mediated necrotizing myopathy (IONM) have been reported during treatment or when discontinuing statins. IONM clinically manifests itself in the form of persistent weakness of the proximal muscles and increased CPK activity in the blood serum, which persist despite the abolition of statins.

Before treatment

Like all statins, Livazo should be prescribed with caution to patients with predisposing factors for the development of rhabdomyolysis. CPK activity should be determined to establish a reference baseline value in the following cases:

- Kidney failure,

- Hypothyroidism,

– Personal or family history of hereditary muscle diseases,

- Previous history of muscle toxicity when treated with fibrates or other statins,

- A history of liver disease or alcohol abuse,

— Patients over 70 years of age with other predisposing risk factors for the development of rhabdomyolysis.

In such cases, clinical monitoring is recommended and the risk of treatment should be considered in relation to the potential benefit. Treatment with Livazo cannot be started if CPK activity is 5 times higher than the ULN.

During treatment

The patient should be advised to immediately report muscle pain, weakness or cramps to the doctor. CPK activity should be determined, and treatment should be stopped if CPK activity is elevated (5 times the ULN). Discontinuation of treatment should be considered if severe muscle symptoms occur, even if CPK activity does not exceed 5 times the ULN. When symptoms resolve and CPK activity returns to normal, re-prescribing Livazo at a dose of 1 mg may be considered, subject to careful monitoring.

Effects on the liver

Like all statins, Livazo should be prescribed with caution to patients with a history of liver disease or to patients who regularly drink excessive amounts of alcohol. Before starting treatment with Livazo and then periodically during treatment, liver function tests should be performed. Patients with a persistent increase in the activity of “liver” transaminases (ALT and AST), exceeding ULN by 3 times, should stop treatment with Livazo.

Effects on the kidneys

Livazo should be administered with caution to patients with moderate or severe renal impairment. The dose should be increased only with careful monitoring. The 4 mg dose is not recommended for patients with severe renal impairment.

Diabetes

Some evidence suggests that statins, as a class, increase blood glucose levels, increasing the risk of developing diabetes mellitus in the future, and in some patients at high risk of developing diabetes mellitus, may lead to a level of hyperglycemia at which formal treatment becomes indicated. diabetes mellitus However, this danger is outweighed by the reduction in vascular risk with statin treatment and should therefore not be a reason to discontinue statin treatment. Patients at risk of developing hyperglycemia (fasting glucose concentration from 5.6 to 6.9 mmol/l, body mass index (BMI) >30 kg/m, increased TG concentration, arterial hypertension) require clinical and biochemical monitoring in accordance with with national recommendations. However, based on the results of both post-marketing observations to assess safety and prospective studies, no confirmed signals were identified regarding the risk of diabetes mellitus with the use of pitavastatin.

Interstitial lung diseases

Rare cases of interstitial lung disease have been reported with the use of some statins, especially with long-term therapy.

Observed clinical signs include shortness of breath, nonproductive cough, and deterioration in general health (fatigue, weight loss, and fever). If interstitial lung disease is suspected, statin therapy should be discontinued.

Impact on the ability to drive vehicles and machinery

Caution must be exercised when driving vehicles or performing other work that requires increased attention, as undesirable reactions such as dizziness and drowsiness may develop.

Possible effects on the body

Speaking about the use of statin drugs, including Livazo, to lower blood cholesterol levels, one cannot fail to mention the effect they have on the human body. It has been established that taking Livazo does not require giving up driving a car or controlling moving mechanisms.

Before prescribing statins, specialists need to make sure that the patient does not have a tendency to rhabdomyolysis. This is a syndrome of extreme myopathy, when muscle tissue cells are destroyed, the level of myoglobin and creatine kinase in the blood rises, as a result of which signs of kidney failure quickly increase.

To avoid this, first monitor the level of creatine kinase in the blood and determine the presence of certain problems:

• dysfunction of the thyroid gland;
• problems with muscle tissue of a personal or hereditary nature;
• taking fibrates or statins resulting in muscle intoxication;
• tendency to alcoholism and diseases of the liver system;
• age over 65–70 years (elderly patients are more prone to rhabdomyolysis).

Livazo is a representative of statins, which reduces the level of “bad” cholesterol in the blood

During treatment with Livazo, if severe muscle symptoms occur, the drug should be discontinued. When creatine kinase levels return to normal, you can resume using Livazo, but under strict medical supervision and at an initial dose of 1 mg per day.

The effect of statins on certain organs and systems:

• liver – if you are prone to alcoholism or have existing disorders in the liver, after prescribing statins, it is necessary to monitor the indicators of the hepatic system (in particular, plasma transaminases);
• kidneys - in the presence of renal failure (moderate and severe) during treatment with Livazo, it is necessary to monitor the functioning of organs. Patients with this disease are not prescribed the drug at a dosage of 4 mg;
• lungs - in the case of long-term therapy with statins, the development of interstitial diseases of the pulmonary system, accompanied by shortness of breath, dry cough, sudden weight loss and fever, was sometimes observed.

If acute signs of liver or kidney failure, as well as interstitial lung diseases, develop, you should immediately consult a doctor and stop taking Livazo. Over time, after the disappearance of pathological symptoms, treatment can be continued, but with a dosage adjustment of statins.

No ads 3

Livazo

Effect on muscle tissue

As with the use of other HMG-CoA reductase inhibitors (statins), when taking the drug there is a possibility of developing myalgia, myopathy and, in rare cases, rhabdomyolysis. Patients should be warned to report any muscle symptoms. CPK activity should be determined in any patient reporting muscle pain, muscle tenderness or weakness, especially if accompanied by malaise or fever. CPK activity should not be determined after physical exercise or in the presence of any other possible reasons for the increase in CPK that may distort the result. If CPK activity increases (5 times higher than ULN), a control analysis should be performed within 5-7 days.

Before treatment

Like all statins, the drug is prescribed with caution to patients with predisposing factors for the development of rhabdomyolysis. CPK activity should be determined to establish a reference baseline value in the following cases:

- renal failure;

- hypothyroidism;

- personal or family history of hereditary muscle diseases;

- previous history of muscle toxicity during treatment with fibrates or other statins;

- a history of liver disease or alcohol abuse;

- elderly patients (over 70 years old) with other predisposing risk factors for the development of rhabdomyolysis.

In such cases, clinical monitoring is recommended and the risk of treatment should be considered in relation to the potential benefit. Treatment with the drug cannot be started if CK levels are 5 times higher than ULN.

During treatment

The patient should be advised to immediately report muscle pain, weakness or cramps to the doctor. CPK activity should be determined, and treatment should be stopped if CPK activity is elevated (5 times the ULN). Consideration should be given to discontinuing treatment if severe muscle symptoms occur, even if CPK activity does not exceed 5 times the ULN. When symptoms resolve and CPK activity returns to normal, re-prescribing the drug at a dose of 1 mg may be considered, subject to careful monitoring.

Effects on the liver

Like all statins, the drug should be prescribed with caution to patients with a history of liver disease or to patients who regularly drink excessive amounts of alcohol. Liver function tests should be performed before starting treatment and then periodically during treatment. Patients with a persistent increase in the activity of “liver” transaminases (ALT and AST), exceeding ULN by 3 times, should stop treatment with the drug.

Effects on the kidneys

Use with caution in patients with moderate or severe renal impairment. The dose should be increased only with careful monitoring. The 4 mg dose is not recommended for patients with severe renal impairment.

Diabetes

Some evidence suggests that statins as a class cause increases in blood glucose concentrations and, in some patients at high risk of developing diabetes mellitus, may lead to levels of hyperglycemia at which appropriate diabetes treatment is necessary. However, this risk is offset by the reduction in vascular risk with statin treatment and should therefore not be a reason to discontinue statin treatment. Patients at risk of developing hyperglycemia (fasting glucose concentration from 5.6 to 6.9 mmol/l, BMI>30 kg/m2, elevated TG concentrations, arterial hypertension) should be subjected to clinical and biochemical monitoring in accordance with national recommendations.

Interstitial lung disease

Rare cases of interstitial lung disease have been reported with the use of some statins, especially with long-term therapy. Observed clinical signs include shortness of breath, nonproductive cough, and deterioration in general health (fatigue, weight loss, and fever). If interstitial lung disease is suspected, statin therapy should be discontinued.

Impact on the ability to drive vehicles and maintain moving mechanisms

Caution must be exercised when driving vehicles or performing other work that requires increased attention, as undesirable reactions such as dizziness and drowsiness may develop.

Cross interaction

During the period of use of pitavastatin, it is necessary to take into account the use of drugs that were previously recommended to the patient to eliminate signs of concomitant diseases. Below is a list of pharmacological groups with which you must be careful when interacting with Livazo:

• Cyclosporine - simultaneous use of statins is prohibited due to a sharp increase in AUC;
• Erythromycin and other macrolide antibiotics give the same reaction as taking statins while taking Cyclosporine, so they cannot be used;
• fibrates – simultaneous therapy with statins leads to the development of myopathy and rhabdomyolysis with severe muscle damage (requires selection of the correct dose and caution);
• Niacin and fusidic acid also lead to the formation of gross disorders of muscle tissue;
• Rifampicin and protease inhibitors - reduce the absorption of pitavastatin by liver tissue;
• Warfarin - when taken simultaneously with Livazo 4 mg, monitoring of prothrombin time is necessary.

Drugs such as Digoxin, inhibitors of CYP3A4, OATP1B1 do not affect the concentration of pitavastatin in the blood, so their use simultaneously with Livazo is allowed by doctors.

Analogues of the drug

If for some reason it is impossible to prescribe pitavastatin to a patient, you can select analogues of Livazo, which are also in the statin group:

• Crestor is a drug belonging to the statin group, based on the active substance rosuvastine (available in dosages of 10, 20 and 40 mg);
• Simvastatin – tablets based on simvastatin, available in the form of 10 and 20 mg dosages;
• Lescol is a drug whose active component is fluvastatin sodium. Sold in the form of capsules containing 21.06 and 42.12 mg of active ingredient;
• Lipobay - tablets consisting of cerivastatin sodium in a dose of 0.2 or 0.4 mg;
• Pravastatin – includes the same name (pravastatin) as the main substance;
• Liprimar is a product containing atorvastatin in dosages of 10, 20, 40 and 80 mg.

Preparations with a similar composition that can replace Livazo

Each of the listed drugs has its own contraindications and side effects, which is why you cannot independently replace Livazo with analogues. Only a specialist can evaluate the medications already taken by the patient, knows the medical history and examination results, and is able to recommend one or another substitute.

Reviews

It should be noted that the majority of patients who were prescribed the drug Livazo, and doctors who work with these tablets, leave only positive reviews. Doctors prescribe pitavastatin due to the quickly onset effect of administration and the good tolerability of Livazo in most patients. Naturally, before prescribing tablets, a complete examination is necessary, and during therapy, monitoring of body functions and blood counts is necessary.

Svetlana, 54 years old: When the doctor prescribed me Livazo 2 mg tablets, I started reading information about them on medical websites. I was afraid of a lot of side effects. But in fact, my body tolerated the pills well, especially since I need to take them once a day. At the same time, I followed a diet that I still maintain today. After 2 months, my blood cholesterol levels dropped and I began to feel much better.

Olga, 48 years old: Livazo tablets were prescribed to me by my doctor after my blood cholesterol rose sharply due to excess weight. At the same time, I was prescribed therapeutic exercise sessions, a diet and walks in the evenings. Now I try to eat healthy food, provide myself with physical activity, and take Livazo 2 mg once a day. The last time I took tests, the doctor said that there were significant improvements.

Vasily, 56 years old: I really like Livazo, it gives results within a month. You feel much better, and the doctor says that tests confirm progress in therapy. One disadvantage of the tablets is their high cost for me. But my sister, who lives in Germany, says that Livazo is a very effective drug; it has been widespread among them for 10–15 years. Therefore, I follow the doctor’s orders; health is still more expensive than pills.