Livazo pills 4mg, 28pcs

$116.0

Active ingredient:	Pitavastatin
Dosage form:	Pills

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Categories: Atherosclerosis, Medication, Metabolism

Description
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Composition

Active ingredient: pitavastatin calcium, which corresponds to the content of pitavastatin 4 mg, Excipients: lactose monohydrate, hyprolose low-substituted, hypromellose, magnesium aluminometasilicate, magnesium stearate. Composition of the film shell: White opadray, including hypromellose, titanium dioxide, triethyl acetate, colloidal silicon dioxide.

Pharmacological action

Pitavastatin competitively inhibits HMG-CoA reductase, limiting the rate of action of the enzyme in cholesterol biosynthesis, and inhibits the synthesis of cholesterol (Ch) in the liver. As a result, the expression of LDL receptors in the liver increases, contributing to the capture of circulating LDL in the blood, reducing total cholesterol and LDL cholesterol (LDL-C) in the blood. Its persistent inhibition of hepatic cholesterol synthesis reduces the secretion of LDL into the blood, reducing the level of triglycerides in the blood plasma. Livazo reduces elevated levels of LDL-C, total cholesterol, and triglycerides, and increases HDL cholesterol (HDL-C). The drug reduces the level of apolipoproteins (Apo-B) and leads to a variable increase in Apo-A1. pharmacokineticsabsorption Pitavastatin is rapidly absorbed in the upper gastrointestinal tract, Cmax in blood plasma is reached within 1 h after oral use. Absorption is independent of food intake. The drug in unchanged form passes through enterohepatic circulation and is well absorbed in the small intestine. The absolute bioavailability of pitavastatin is 51%. The cmax of pitavastatin in blood plasma decreased by 43% with a high-fat meal, but the AUC remained unchanged. Distribution Pitavastatin binds more than 99% to plasma proteins, mainly albumin and α1-acid glucoprotein, with an average Vd of about 133 L. Pitavastatin is actively transported to hepatocytes, the site of action and metabolism, by many hepatic carriers, including OATP1B1 and OATP1B3. Plasma AUC varies with an approximately 4-fold range between the highest and lowest values. Studies on SLCO1B1 (the gene that encodes OATP1B1) suggest that polymorphism of this gene may explain the large fluctuation in AUC. Pitavastatin is not a substrate for P-glucoprotein. Metabolizmitavastatin unchanged is the majority of the drug in the blood plasma. The main metabolite is inactive lactone, which is formed via the ether-type pitavastatin glucuronide conjugate UDP by glucuronosyltransferase (UGT1A3 and 2B7). In vitro studies using 13 isoforms of human cytochrome P450 (CYP) show that the metabolism of pitavastatin by CYP is minimal; CYP2C9 (and to a lesser extent CYP2C8) is responsible for the metabolism of pitavastatin to minor metabolites. Excretion Pitavastatin in unchanged form is rapidly excreted from the liver into the bile, but undergoes enterohepatic recirculation, which determines the duration of its action. Less than 5% of pitavastatin is excreted in the urine. T1 / 2 from blood plasma ranges from 5.7 h (1 dose) to 8.9 h (steady state), the geometric mean of oral clearance is 43.4 l / h after a single dose.

Indications

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 (e. g. exercise, weight loss) are insufficient.

Contraindications

Severe hepatic insufficiency (more than 9 points on the Child-Pugh scale) or Child-Pugh class C, liver diseases and active phase, including a persistent increase in the activity of hepatic transaminases in blood serum (more than 3 times compared to the ULN);myopathy;concomitant use of cyclosporine;pregnancy, breast-feeding, lack of adequate methods of contraception in women of childbearing age;age up to 18 years (efficacy and safety have not been established);hypersensitivity to pitavastatin, auxiliary components of the drug and other HMG-CoA reductase inhibitors (statins).

Side effects

Frequency is defined as: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10,000 to <1/1000), very rare (Common: headache, constipation, diarrhea, indigestion, nausea, myalgia, joint pain. Infrequently: anemia, anorexia, insomnia, dizziness, bluntness of taste, drowsiness, ringing in the ears, abdominal pain, dry mouth, vomiting, increased transaminases (AST, ALT), itching of the skin, rash, muscle spasms, pollakiuria, asthenia, malaise, weakness, peripheral edema. Rare: decreased visual acuity, burning mouth syndrome, acute pancreatitis, cholestatic jaundice, impaired liver function, liver disorders, myopathy, rhabdomyolysis, urticaria, erythema. The following side effects have been reported with some statins: sleep disorders, including nightmares, memory loss, sexual dysfunction, depression, and isolated cases of interstitial lung disease, especially with long-term therapy.

Cyclosporine interaction: concomitant use of a single dose of cyclosporine with Livazo at steady state resulted in a 4.6-fold increase in pitavastatin AUC. Livazo is contraindicated in patients receiving cyclosporine treatment. Erythromycin: concomitant use with Livazo resulted in a 2.8-fold increase in pitavastatin AUC. It is recommended to suspend the use of Livazo for the duration of treatment with erythromycin or other macrolide antibiotics. Gemfibrozil and other fibrates: the use of fibrates is sometimes associated with the development of myopathy. Concomitant use of fibrates with statins increases the risk of developing myopathy and rhabdomyolysis. According to pharmacokinetic studies, concomitant use of pitavastatin with gemfibrozil resulted in a 1.4-fold increase in the AUC of pitavastatin and a 1.2-fold increase in the AUC of fenofibrate. In this regard, Livazo should be taken with caution at the same time as fibrates. Niacin: niacin monotherapy has been associated with the development of myopathy and rhabdomyolysis. Caution should be exercised when prescribing Livazo concomitantly with niacin. Fusidic acid: Serious muscle problems, such as rhabdomyolysis, have been reported due to interactions between fusidic acid and statins. It is recommended to suspend the use of Livazo for the duration of treatment with fusidic acid. Rifampicin: concomitant use of Livazo resulted in a 1.3-fold increase in pitavastatin AUC due to reduced hepatic absorption (AUC decreased by 20%). Protease inhibitors: concomitant use of Livazo may result in minor changes in the AUC of pitavastatin. Atazanavir is an inhibitor of OATP1B1 and liver glucuronyltransferases UGT1A3 and UGT2B7 (responsible for the metabolism of pitavastatin). Concomitant use of atazanavir and Livazo resulted in a 1.3-fold increase in the AUC of pitavastatin, but did not affect the concentration of atazanavir (a 1.1-fold increase in AUC). Ezetimibe and its metabolite glucuronide inhibit the absorption of cholesterol from food and bile. Concomitant use with pitavastatin does not affect the plasma concentration of ezetimibe or its metabolite glucuronide, and ezetimibe does not affect the plasma concentration of pitavastatin. CYP3A4 inhibitors: Drug interaction studies with itraconazole and grapefruit juice, known CYP3A4 inhibitors, did not have a clinically significant effect on pitavastatin plasma concentrations. Digoxin, a known P-gp substrate, does not interact with Livazo. No significant changes in pitavastatin or digoxin concentrations were observed with concomitant use. Warfarin: at steady state, the pharmacokinetic and pharmacodynamic properties (INR and prothrombin time) of warfarin in healthy volunteers were independent of the concomitant use of Livazo at a dose of 4 mg / day. However, as with other statins, prothrombin time or INR should be monitored in patients taking warfarin when Livazo is included in the treatment regimen.

How to take, course of use and dosage

Inside, tablets should be swallowed whole. It is preferable to take the tablet at the same time every day, preferably in the evening, in accordance with the circadian rhythm of lipid metabolism. Patients should follow a hypocholesterolemic diet before and during treatment. The initial dose of the drug is 1 mg/daykiki 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 selected individually according to LDL-C concentrations, the purpose of treatment, and the patient’s response to treatment. Most patients require a dose of 2 mg. The maximum daily dosage is 1 mg. Patients with mild to moderate hepatic impairment: a maximum daily dosage of 2 mg is recommended. Patients with impaired renal function: in patients with mild renal impairment (it is desirable to objectively assess this degree with a reflection of creatinine clearance or glomerular filtration rate), Livazo should be used with caution. Data on the use of the maximum daily dose of the drug 4 mg in patients with impaired renal function of any severity are limited, so the maximum daily dose of 4 mg should be prescribed only with careful monitoring of renal function after a gradual increase in the dose. It is not recommended that patients with severe renal impairment receive a maximum daily dose of 4 mg; it is recommended to consider limiting the maximum daily dose to 2 mg in severe renal insufficiency. Elderly patients: no dose adjustment is required.

Overdose

Overdose may increase the symptoms of adverse reactions.There is no specific antidote. Symptomatic treatment and supportive measures should be taken as needed. Liver function indicators and creatine kinase levels should be monitored. Hemodialysis is ineffective.

Special instructions

The effect on muscle along with other HMG-CoA reductase inhibitors (statins) causes the development of myalgia, myopathy, and less often rhabdomyolysis. Patients should be warned to seek immediate medical attention if they experience any symptoms in their muscles. If patients develop muscle pain or muscle weakness, especially if they are accompanied by malaise or fever, creatine kinase levels should be determined. Creatine kinase should not be measured after exercise or if there are any other possible causes of increased creatine kinase, which may be confusing when interpreting the results. After detecting an increased concentration of creatine kinase (more than 5 times compared to ULN), a control analysis is required for 5-7 days and, if necessary, stop taking the drug. Prior to treatment, Levazo should be used with caution in patients with predisposing risk factors for rhabdomyolysis. In the following cases, measurement of creatine kinase levels is required to establish standard baseline data:— kidney failure— – reduced thyroid function; – personal or family history of inherited muscle disorders;- previous case of muscle toxicity from 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 rhabdomyolysis. During treatment, if severe muscle symptoms occur, therapy should be discontinued, even if the creatine kinase level is less than 5 times the ULN. If symptoms stop and creatine kinase levels return to normal, then you can resume taking Livazo at a dose of 1 mg/day per week and with careful monitoring. Effects on the liver Levazo should be used with caution in patients with a history of liver disease or in patients who abuse alcohol. Before starting treatment with Livazo and periodically during the entire course of therapy, it is necessary to monitor liver function indicators. Treatment should be discontinued in patients with a persistent increase in plasma transaminases (ALT and AST) by more than 3 times compared to ULN. Effects on the kidneys: Ivazo should be used with caution in patients with moderate or severe renal insufficiency. Increasing the dose should only be performed with careful monitoring of renal function after gradual titration of the dose. Patients with severe renal insufficiency are not recommended to use a dose of 4 mg. Interstitial lung disease Interstitial lung diseases have been reported during the use of certain statins, especially during long-term therapy. Severe symptoms may include shortness of breath, an unproductive cough, and poor overall health (fatigue, weight loss, and fever). If a patient is suspected of developing interstitial lung disease, statin therapy should be discontinued. Influence on the ability to drive motor vehicles and manage mechanismmi Net of data on the impact on the ability to drive a vehicle and manage moving mechanisms.