Pitavastatin - instructions for use, reviews, analogs and formulations (1 mg, 2 mg and 4 mg tablets) of the drug for the treatment of hypercholesterolemia or the reduction of elevated blood cholesterol in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Pitavastatin. There are reviews of visitors to the site - consumers of this medication, as well as opinions of physicians specialists on the use of Pitavastatin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Pitavastatin in the presence of existing structural analogues.Use to treat hypercholesterolemia or reduce elevated blood cholesterol and hyperglyceridemia in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Pitavastatin - a competitive inhibitor of HMG-CoA reductase, an enzyme that catalyzes the initial stage of cholesterol synthesis. The use of Pitavastatin does not cause the accumulation of potentially toxic sterols in the body. Clinical studies have shown the efficacy of Pitavastatin in reducing the concentration of total cholesterol in the blood plasma, low and very low-density lipoproteins, triglycerides and apolipoprotein B, as well as increasing the concentration of high-density lipoproteins and apolipoprotein A1.

Composition

Pitavastatin calcium + excipients.

Pharmacokinetics

Pitavastatin is rapidly absorbed in the upper parts of the gastrointestinal tract, the maximum concentration in the blood plasma is reached within 1 hour after ingestion. Eating does not affect absorption. Absolute bioavailability of Pitavastatin 51%. More than 99% of the substance binds to blood plasma proteins.Pitavastatin in unchanged form is rapidly excreted from the liver with bile, but undergoes intestinal hepatic recirculation, which ensures its long-term effect. Less than 5% of the substance is excreted by the kidneys.

Indications

• primary hypercholesterolemia, including heterozygous familial hypercholesterolemia (the second type A hyperlipidemia according to Fredrickson classification);
• mixed hypercholesterolemia (hyperlipidemia of the second B-type according to Fredrickson classification);
• hypertriglyceridemia (hyperlipidemia of the fourth type according to Fredrickson classification).

Pitavastatin is prescribed as a supplement to the diet, when the diet and other non-medicamentous methods of treatment (for example, physical exercises, weight loss) are insufficient.

Forms of release

Tablets coated with 1 mg, 2 mg and 4 mg.

Instructions for use and dosing regimen

Inside, the tablets must be swallowed whole.

It is preferable to take the pill at the same time of the day, preferably in the evening, in accordance with the circadian rhythm of lipid metabolism. Before the start of treatment and in the process, patients should adhere to the hypocholesterolemic diet.

The initial dose of the drug is 1 mg per day once.If necessary, the dose of the drug is increased at intervals of at least 4 weeks to 2 mg per day. The dose should be selected individually in accordance with the concentrations of low density lipoprotein, the purpose 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 and moderate impairment of liver function are recommended a maximum daily dose of 2 mg.

If the renal function is mild (it is desirable to objectively assess this degree with a reflection of the creatinine clearance or glomerular filtration rate), the drug Livazo (trade name Pitavastatin) should be used with caution. Data on the application of the maximum daily dose of the drug 4 mg for violations of kidney function of any severity are limited, so a maximum daily dose of 4 mg is necessary only with careful monitoring of kidney function after a gradual increase in the dose. It is not recommended for patients with severe renal dysfunction to prescribe a maximum daily dose of 4 mg. It is recommended to consider limiting the maximum daily dose to 2 mg in severe renal failure.

Side effect

Often (from 1 in 100 to 1 out of 10 subjects):

• Myalgia (pain in the muscles);
• arthralgia (joint pain);
• insomnia;
• headache;
• constipation;
• diarrhea;
• dyspepsia (heaviness in the stomach);
• nausea;
• increased activity of creatine phosphokinase (CK).

Infrequently (from 1 in 100 to 1 in 1000):

• anemia (decrease in the concentration of hemoglobin in the blood);
• anorexia (lack of appetite when the body needs an objective diet);
• dizziness;
• a taste disorder;
• drowsiness;
• tinnitus;
• itching;
• rash;
• muscle spasms;
• pollakiuria (increased frequency of urination while maintaining the volume of secretions);
• stomach ache;
• dryness of the oral mucosa;
• vomiting;
• increased activity of hepatic transaminases (ALT, AST);
• asthenia, malaise;
• increased fatigue;
• peripheral edema;
• hypoesthesia (decreased sensitivity, numbness).

Rarely (from 1 in 1000 to 1 in 10,000):

• decreased visual acuity;
• urticaria (an allergic rash);
• erythema (redness);
• glossodynia (pain in the tongue);
• acute pancreatitis (inflammation of the pancreas);
• Cholestatic jaundice (jaundice caused by congestion of bile);
• abnormal liver function;
• myopathy (muscular tissue dystrophy);
• rhabdomyolysis (destruction of muscle cells);
• abdominal discomfort (abdominal discomfort).

Contraindications

• increased sensitivity to Pitavastatin, auxiliary components of the drug and other statins;
• severe hepatic insufficiency (more than 9 on the Child-Pugh scale) or Child-Pugh class C;
• liver diseases in the active phase, including persistent increase in hepatic transaminase activity in blood serum (more than 3 times compared with the upper limit of the norm);
• lactose intolerance;
• deficiency of lactase;
• glucose-galactose malabsorption;
• myopathy;
• simultaneous administration of cyclosporine;
• pregnancy, the period of breastfeeding;
• lack of adequate methods of contraception in women of childbearing age;
• age to 18 years (efficacy and safety not established).

Carefully:

• kidney failure;
• hypothyroidism;
• personal or family history of hereditary muscle diseases;
• previous history of muscle toxicity with other statins or fibrates;
• excessive use of alcohol;
• age over 70 years;
• liver disease in anamnesis.

Application in pregnancy and lactation

The use of Pitavastatin in pregnancy is contraindicated. Women of childbearing age in the treatment of Pitavastatin should use reliable methods of contraception. Since cholesterol and other cholesterol biosynthesis products are necessary for fetal development, the potential risk of HMG-CoA reductase inhibition is greater than the benefit of Pitavastatin treatment during pregnancy. Animal studies have shown that Pitavastatin has reproductive toxicity, but without teratogenic potential. If the patient is planning a pregnancy, discontinue treatment at least 1 month before conception. When a pregnancy occurs during the application of Pitavastatin, treatment should be stopped immediately.

The use of Pitavastatin during breastfeeding is contraindicated. It is excreted in milk of lactating rats. There is no data on the isolation of lactating women with breast milk. If you need to use Pitavastatin during lactation, breastfeeding should be discontinued.

Use in children

Pitavastatin is contraindicated at the age of 18 years (efficacy and safety not established).

Application in elderly patients

Correction of the dose is not required.Caution should be exercised when prescribing to patients older than 70 years with predisposing factors to myopathy.

special instructions

Pitavastatin tablets contain lactose, so they can not be prescribed for lactose intolerance, lactase deficiency, or glucose-galactose malabsorption.

As with the use of other statins, there is a possibility of developing myalgia, myopathy and in rare cases rhabdomyolysis. Patients should be warned about reporting any muscular symptoms.

The activity of creatine phosphokinase (CKF) should be determined in any patient reporting muscle pain, muscle soreness during palpation or weakness, especially if accompanied by malaise or fever. Treatment with Pitavastatin should not begin if the CK values ​​are 5 times higher than normal. It is necessary to determine the activity of CK and stop treatment if the activity of CK is increased (5 times higher than normal).

Impact on the ability to drive vehicles and service moving machinery

Care must be taken when driving a vehicle or doing other work that requires increased attention,since it is possible to develop such undesirable reactions as dizziness and drowsiness.

Drug Interactions

Simultaneous reception of a single dose of cyclosporine with Pitavastatin in the equilibrium state leads to a 4.6-fold increase in the total concentration of Pitavastatin. The effect of the equilibrium state of cyclosporin on the equilibrium state of Pitavastatin is unknown. Pitavastatin is contraindicated in patients receiving cyclosporine.

Simultaneous reception of Erythromycin with Pitavastatin leads to a 2.8-fold increase in the total concentration of Pitavastatin. A temporary discontinuation of taking Pitavastatin during treatment with erythromycin or other antibiotics of the macrolide group is recommended.

In rare cases, monotherapy with fibrates was associated with the development of myopathy. Simultaneous application of fibrates with statins was associated with an increase in the incidence of myopathy and rhabdomyolysis. Caution should be exercised while using Pitavastatin with fibrates.

Investigations of interaction in the treatment of nitavastatin and nicotinic acid in lipid-lowering doses (more than 1 g per day) were not performed.The use of nicotinic acid in monotherapy was associated with the development of myopathy and rhabdomyolysis. Therefore, with simultaneous use with nicotinic acid in lipid-lowering doses (more than 1 g per day), Pitavastatin should be administered with caution.

Severe muscular abnormalities, such as rhabdomyolysis, were attributed to the interaction between fusidic acid and statins. During treatment with fusidic acid, it is recommended to temporarily stop the use of Pitavastatin.

Simultaneous administration of Rifampicin with Pitavastatin resulted in a 1.3-fold increase in the total concentration of Pitavastatin due to a decrease in accumulation in the liver.

Simultaneous administration of HIV protease inhibitors with Pitavastatin resulted in insignificant changes in total Pitavastatin concentrations.

The equilibrium state of the pharmacokinetics and pharmacodynamics of Warfarin in healthy volunteers did not change with the simultaneous use of warfarin with Pitavastatin at a dose of 4 mg daily. However, as with the use of other statins, patients who receive warfarin should be monitored for blood clotting when added to the treatment of Pitavastatin.

Like other statins, Pitavastatin should be used with caution in patients who consume a significant amount of alcohol.

Analogues of the drug Pitavastatin

Structural analogs for the active substance:

• Livazo.

Analogues for the pharmacological group (statins):

• Anistat;
• Atherostat;
• Atokord;
• Atomax;
• Ator;
• Atorvastatin;
• Atorvox;
• Atoris;
• The Vasator;
• Vazilip;
• Zocor;
• Zorstat;
• Cardiostatin;
• The Cross;
• Leskol;
• Lipobay;
• Lipon;
• Lipostat;
• Lipofford;
• Liprimar;
• Liptonorm;
• Lovacor;
• Lovastatin;
• Lovasterol;
• Mevakor;
• Medostatin;
• Mertenil;
• Novostat;
• Ovenkor;
• Pravastatin;
• Rovacor;
• Rosart;
• Rosystark;
• Rosuvastatin;
• Rosewood;
• Rosulip;
• Rozufast;
• Roxer;
• Rustor;
• Simvagexal;
• Simvakol;
• Simvale;
• Simvastatin;
• Simvastol;
• Symvor;
• Simgal;
• Simlo;
• Sinquard;
• Suvardio;
• Tevastor;
• Torvacard;
• Torvalip;
• Torvas;
• Tulip;
• Holvasim;
• Holletar.

Response of a cardiologist

Pitavastatin, as well as other statins, is prescribed to patients with high risk of developing or already available atherosclerosis to prevent heart attacks and strokes.If the increase in cholesterol and low-density lipoprotein is detected for the first time and slightly above the norm, statins can be dispensed with a special diet and increased physical exertion. But, if the indicators significantly exceed the norm, and in the family history there is atherosclerosis and cardiovascular pathology, especially at a young age, statin prescription is mandatory. Despite the abundance of possible side effects, the benefit of using the drug in the presence of real indications is much higher than its possible harm. The main disadvantage of the drug is high cost. Given that it is often taken for years, treatment results in a decent amount.

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