Livalo 2mg Kowa medicine for hyperlipidemia (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Pitavastatin calcium

Ingredient

Composition information	Content
Pitavastatin calcium	2mg

Uses

indications

Livalo drug used in the following cases:

Patients with primary blood lipid hyperlemen include hyperlested blood cholesterol or mixed blood lipid disorders as a supplementary therapy for the diet to reduce the high level of TC, LDL-C, APO B, TG and to increase HDL-C levels and children from 10 years of age or older with hyperlested family blood cholesterol when responding to other non-medical treatments.

Because there is no experience used in cases of hyperlestolytic hyperlested hypertension, it is advisable to consider using livalo as an additional treatment for non -drug non -drug therapy such as low density lipoprotein (LDL apheris) and only when assessing the treatment with Livalo is indispensable.

Pharmacology

Pharmacological Therapy Group: HMG-COA Reductase inhibitors

ATC code: C10A A08

Mechanism of action

Pitavastatin inhibits HMG-COA Reductase competition, enzymes limit speed in cholesterol biosynthesis and inhibit cholesterol synthesis in the liver. As a result, the expression of low density lipoprotein receptors (LDL) in the liver, promotes the absorption of LDL during blood circulation, reduces the low density lipoprotein cholesterol level (LDL-C) and total cholesterol (TC) in the blood. The inhibition of cholesterol synthesis in the liver is maintained to reduce the secretion of lipoprotein very low density (VLDL) into the blood, reducing the concentration of triglycerides (TG) in plasma.

Pharmacological effect

Livalo reduces the increasing concentration of LDL-C, TC and TG and increases high density lipoprotein cholesterol levels (HDL-C). It reduces apolipoprotein B (APO-B) and creates an increase in variability of APO-A1 (see Table 1). It also reduces high density lipoprotein (Non-HDL-C), high TC/HDL-C and high APO-B/APO-A1.

Dynamic pharmacokinetics

absorption: Pitavastatin is quickly absorbed from the above digestive tract and the peak concentration of plasma is achieved within 1 hour after oral use. The absorption is not affected by food. The drug in the form of unchanged guts and intestinal circulation is well absorbed from the nodes and ileum. Pitavastatin's absolute bioavailability is 51%.

Distribution: Pitavastatin binds more than 99% of protein in human plasma, mainly albumin and alpha 1-acid glycoprotein, and the geometric average distribution volume is about 133 liters. Pitavastatin is actively transported into liver cells as an acting and metabolic position, because many liver transportation includes OATP1B1 and OATP1B3. The area under the curve (AUC) in plasma variables with about 4 times between the highest and lowest value. Studies with SLCO1B1 (OATP1B1 encoding gene) show that the polymorphism of this gene can explain most of the variables of AUC. Pitavastatin is not a substrate for p-glycoprotein.

Biological metabolism: Pitavastatin in constant form is the active ingredient that dominates plasma. The metabolites are mainly inactive lactons, formed through the ester pitavastatin glucuronide combination by UDP glucuronosyltransferase (UGT1A3 and 2B7). In vitro studies, using 13 ISOForm Cytochrom P450 (CYP), shows the metabolism of pitavastatin because CYP is a minimum; CYP2C9 (and less than CYP2C8) is responsible for the metabolism of pitavastatin into small metabolites.

Elimination: Pitavastatin in the form of unchanged removal from the liver through bile, but through the intestinal circulation, contributing to its time. Under 5% Pitavastatin is excreted in urine. Sales time in plasma is about 5.7 hours (single dose) to 8.9 hours (stable state) and average geometric medium geometric clearance is 43.4 liters/hour after single dose.

Effect of food: Pitavastatin's maximum concentration in plasma decreased by 43% when used with a high -fat meal, but AUC did not change.

Special patient groups

Elderly: In a pharmacokinetic study, comparing young and healthy young volunteers (65 years old), Pitavastatin's AUC AUC is 1.3 times higher than the elderly subjects. This does not affect the safety and effectiveness of Livalo in elderly patients in clinical trials.

Sex: In a pharmacokinetic study, comparing healthy men and women, Pitavastatin's AUC increased by 1.6 times in women. This does not affect the safety and effectiveness of Livalo in women in clinical trials.

Race: There is no difference in pitavastatin pharmacokinetics records among healthy Japanese and white volunteers when taking into account age and weight.

Children: Use Pitavastatin calcium (1 or 2mg) oral once a day before breakfast repeated for 52 weeks in 7 Japanese male children with hyperlested blood cholesterol has been done. The plasma concentration of pitavastatin is constant after drinking 1 hour is 22.79 ± 11.34 ng/ml (average value + standard deviation) for 1 mg and 32.17 ± 17.65 ng/ml for 2mg dose.

Kidney failure: For patients with medium kidney disease and those who are being hemoglobin, the increase in AUC value in the order is 1.8 times and 1.7 times. In another pharmacokinetic study, patients with severe renal impairment were not allowed to hemorrhage, a 4mg livalo dose. ACO-INF and CMAX are 36% and 18% higher than healthy volunteers. (See the dose and usage).

Hepatic failure: For patients with mild hepatic impairment (Child-Pugh a), AUC is 1.6 times higher in healthy subjects, while for patients with medium liver impairment (Child-Pugh B), AUC is 3.9 times higher.

Before taking Livalo 2mg Kowa medicine for hyperlipidemia (3 blisters x 10 tablets)

How to use

use orally and should take whole or half tablets 2mg if needed 1mg Pitavastatin calcium. Livalo can be used at any time of the day, or not with food. The desire is that patients should take pills at the same time every day. Statin therapy is usually more effective in the evening of day and night of lipid metabolism. Patients should follow a diet to reduce cholesterol before treatment. It is important that the patient continues to control the diet during treatment.

Dosage

Adults: The starting dose is 2mg of pitavastatin calcium oral 1 time/day. The patient's age and symptoms can be adjusted. When the decrease in the level of LDL-C is incomplete, the dose may increase to 4 mg/day.

Elderly: No need to adjust the dose (see the pharmacological properties and pharmacokinetic properties).

Group of children's patients: The usual dosage for children from 10 years old and older is 1mg of pitavastatin calcium oral 1 time/day. The dose can be adjusted according to the patient's symptoms. When the reduction of LDL-C levels is incomplete, the dose can be increased to 2 mg/day. The safety of pitavastatin calcium in young children has low birth weight, infants, children and children under 10 years of age have not been determined (pitavastatin calcium has not been used in children under 10 years old in Japan and has not been used in children under 6 years old in Europe).

Should only consider using Livalo for children who are considered to be suitable for livalo under the supervision of a fully trained and experienced doctor to treat hyperlested blood cholesterol in children. When using livalo in children, pay attention to the frequency or intensity of exercise and increase the level of creatine kinase (CK), and be careful when using Livalo. (Because the frequency and intensity of exercise tend to tend to be higher in children, muscle disease is more likely to develop in this patient group).

Patients with renal function impairment:

Medium and severe renal failure (glomerular filtration speed in the order is 30 - 59 and 15 - 29 ml/min/1.73 m2) as well as end stage kidney disease being hemorrhage: The starting dose is 1mg, 1 time/day and a maximum dose of 2mg, 1 time/day.

Patients with liver function impairment:

Contraindicated using livalo in patients with active liver disease, may include an increase in the persistent concentration of unexplained liver transaminase (see the contraindications).

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What to do when overdose?

There is no specific treatment in case of overdose. Patients should be treated with symptoms and supportive measures should be conducted when necessary. Need to monitor liver function and ck concentration. Hematopalysts are not probably beneficial.

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Side Effects

In control clinical trials, in the recommended dose, less than 4% of patients treated with Pitavastatin have been stopped due to adverse events. The adverse reaction related to Pitavastatin is reported the most in clinical trials with muscle pain.

Summary of adverse reactions

The adverse and frequency reactions are observed in controlled clinical trials and expanded studies worldwide, in the recommended dose, listed below in groups of organs. The frequency is defined: Very common (≥ 1/10), common (≥ 1/100 to Table 4: The adverse reactions and the frequency are observed in the control clinical tests and expansion studies worldwide, at the recommended dose according to the agency system. 1/10,000) Unknown Nursing - - Anorexia - - - Sleeps - - - Eye - - - vision reduction - - Tai - - - digestive disorders Level - - Mats - - and bone - muscle pain, joint pain muscle spasm - muscle necrosis through immunominals (see warning and prudence especially when used) The ureter - - Tieu Nhi - - - Border - -

- The concentration of ≥ 10 times ULN with muscle symptoms is also rare and only observed in a patient of 2406 patients treated with Pitavastatin 4 mg (0.04%) in the clinical trial program.

In a double, random, control test for 52 weeks, 252 HIV -infected patients with lipid disorders are treated with pitavastatin 4mg, 1 time/day (n = 126) or another statin (n = 126). All patients are taking Retrovirus resistance therapy (except Darunavir) and has RNA HIV-1 less than 200 copies (COPIES)/ml and the number of CD4 larger than 200 cells/µl for at least 3 months before random classification. Pitavastatin's safety records are generally suitable for safety records in clinical studies described above. A patient (0.8%) is treated with pitavastatin with the peak value of creatin phosphokinase exceeding 10 times ULN, has recovered. Four patients (3%) are treated with Pitavastatin with at least one ALT value exceeding 3 times but less than 5 times ULN, there is no case that leads to stop use of the drug. The failure of the study virus has been reported in 4 patients (3%) treated with Pitavastatin, which is defined as the RNA HIV-1 measurement that has exceeded 200 copies/ml also increased more than the original.

Group of children's patients

In clinical studies in Japan, there is no adverse reaction found in any patient (14 subjects). In clinical studies in Europe, adverse reactions found in 20 out of 128 patients (15.6%). The main symptoms are headache, abdominal pain and muscle pain (at the time of approved for use in children).

After -sales experience

A after -2 -year after -sales surveillance study was conducted in nearly 20,000 patients in Japan. The vast majority of 20,000 serious patients have been treated with Pitavastatin 1mg or 2mg, not 4mg. 10.4% of patients have reported adverse events that the causal relationship with Pitavastatin could not be excluded and 7.4% of patients had stopped treatment due to adverse events. The ratio of muscle pain is 1.08%. Most adverse events are mild. The inconvenience rate is higher for more than 2 years in patients with a history of drug allergies (20.4%), either with liver or kidney disease (13.5%). The adverse and frequency reactions are observed in after -time after -sales surveillance research but not in clinical tests that are controlled worldwide, with the recommended dosage listed below.

Liver disorders - bile:

Rare: Abnormal liver function, liver disorders.

There are also voluntary after -sales reports on the effects of skeletal muscle, including muscle pain and muscle diseases in patients received by livalo treatment at all recommended doses. Reports on the pattern, with and without acute renal failure, including the deadly pattern of the pattern, has also received. Voluntary reports on the following events have also received (frequency based on data observed in after -sales studies):

nervous system disorders:

Uncommon: Sensory reduction.

Gastrointestinal disorders:

Rare: abdominal discomfort

The effect of the statin group

The following adverse events have been reported to some statins:

Sleep disorders, including nightmares. There are or without risk factors (blood glucose at ≥ 5.6 mmol/l, body mass index (BMI)> 30 kg/batch, hypertension, history of hypertension).

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

Livalo drug contraindicated in the following cases:

In patients who know how to be hypersensitively to pitavastatin or any excipients of the drug. Use appropriate contraception.

Caution when using

effects on muscle

As with other HMG-Coa Reductase inhibitors (statins), it may be likely to occur in myalia, muscle disease and rare, muscle pattern. The patient should be required to report any muscle symptoms. CK concentration should be measured in any patient reporting muscle pain, muscle pain or muscle pain, especially if accompanied by discomfort or fever.

Do not measure CK after heavy exercise or the presence of any other reasonable cause that causes increased CK can interfere with the results of the results. When the CK concentration increases (> 5 times the upper limit of the normal level (ULN), a confirmation test must be conducted within 5 to 7 days.

There are very rare reports on muscle necrosis through the immunity (IMNM) during or after treatment with some statins. IMNM is clinically characterized by the persistent speculative weakness and persistent serum although it has stopped treatment with statin.

Do not use simultaneously with livalo with fusidic acid formulas used throughout the body or within 7 days after stopping treatment with fusidic acid. In patients, the use of all -body fusidic acid is considered necessary, should stop using statin during treatment with fusidic acid. There have been reports on the pattern (including some deaths) in patients using a combination of fusidic acid and statin (see the interaction with other drugs and other types of interactions). It is necessary to advise patients to find medical advice immediately if they have any symptoms of muscle weakness, muscle pain or muscle pain.

Statin therapy can be reused after 7 days of the last dose of fusidic acid. In the exception, if it is necessary to use prolonged body fusidic acid, for example, to treat severe bacterial infections, the need for simultaneous use of livalo and fusidic acid should only be considered on the basis of each case and under tight medical supervision.

Before treatment

As with other statins, caution should be cautious when prescribing livalo in patients with elements that are prone to muscle elimination. Creatinine kinase concentration should be measured to determine the initial reference level, in the following conditions:

Renal failure. Van.

In these situations, it is recommended to monitor clinical and consider the risk of treatment compared to possible benefits. Do not start treatment with livalo if the value of CK> 5 times ULN.

during treatment

Patients must be encouraged to report muscle pain, muscle weakness or muscle cramps immediately. Creatin kinase concentration should be measured and stop treatment if CK levels increase (> 5 times ULN). Consider stopping treatment if the symptoms of severe muscle even when the concentration of CK

Effects on the liver

Increased serum transaminase (Aspartat Aminotransferase [AST]/Glutamic-oxaloacetic transaminase serum, or alanin aminotransferase [ALT]/Glutamic-Pyruvic Transaminase serum) has been reported to HMG-COA Reductase inhibitors, including Livalo. In most cases, this gain is transient and recovery or improvement when continuing treatment or after a short time of suspension of treatment.

In phase 2 studies, control with placebo, do not observe the alt> 3 times ULN in groups of placebo, Pitavastatin 1 mg, or Pitavastatin 2 mg. One of 202 patients (0.5%) using Pitavastatin 4 mg has Alt> 3 times ULN.

Recommended the liver enzyme test before starting livalo and if signs or symptoms of liver damage occur.

There have been rare after -sales reports of liver failure and death in patients using statins, including pitavastatin. If serious liver damage has clinical symptoms and/or hypoglycemia of blood or jaundice occurs during livalo treatment, suspension of immediate treatment. If the disease is not found, then do not start using livalo.

Like other HMG-CoA Reductase inhibitors, caution should be used when using livalo in patients who drink significant alcohol. Contraindicated using livalo in active liver disease, may include persistent increase in unexplained transaminase (see the contraindications).

diabetes

Some evidence that statin is a group of drugs that increase blood glucose and in some patients, there is a high risk of future diabetes, which can cause a hyperglycemia that the treatment of diabetes officially is appropriate.However, a decrease in the risk of blood vessels due to statin exceeds this risk and therefore this risk should not be a reason to stop treating with statin. Patients at risk of hyperglycemia (glucose at 5.6 - 6.9 mmol/l, body mass index> 30 kg/m2, increased TG, hypertension) should be monitored both in clinical and biochemical according to the nation's instructions. However, there is no sign of confirming the risk of diabetes for pitavastatin in post -sales safety monitoring studies or in time studies (see the pharmacological properties).

Interstitial lung disease

The exception of interstitial lung disease has been reported to some statins, especially when long -term treatment (see the unwanted effect). The characteristics of expression may include shortness of breath, dry cough and body health decline (fatigue, weight loss and fever). If a patient suspects that the patient has developed interstitial lung disease, he should stop treating with statin.

Other effects

Recommendations to suspend livalo during erythromycin treatment, other antibiotics belonging to macrolid group or fusidic acid (see the interaction with other drugs and other types of interactions). Be careful when taking livalo in patients who are taking drugs that cause muscle disease (eg fibrat or niacin, see the interaction with other drugs and other types of interactions).

Lactose -containing tablets. Patients with rare genetic problems in tolerance of galactose, deficiency of lactase or absorbent Glucose-Galactose should not use this drug.

The effect of drugs on driving and operating machinery

There is no model of adverse events showing that patients using Livalo will suffer any decline in driving and operating dangerous machinery but it should be noted that there is a report on dizziness and drowsiness during Livalo treatment.

Use drugs for women during pregnancy and lactation

Pregnant women

contraindicated using livalo during pregnancy (see the contraindications). Pregnant women must have appropriate contraception during livalo treatment. Because cholesterol and other cholesterol biosynthesis are essential for the development of the fetus, the potential risk of HMG-COA Reductase inhibitors is greater than the benefits of treatment during pregnancy. If the patient is planning to become pregnant, it is necessary to stop treating at least a month before conceiving. If the patient is pregnant while using Livalo, it is necessary to stop treatment immediately.

breastfeeding

contraindicated use of livalo during breastfeeding (see the contraindications). Pitavastatin is excreted into the milk of the rat. It is unclear whether Pitavastatin will excrete in breast milk.

fertility

There is no data.

Drug interaction

pitavastatin is actively transported into human liver cells by many liver transportation (including polypeptide transportation of organic anion - OATP), which may be related to some of the following interactions.

ciclosporin: simultaneously use a single dose of ciclosporin with livalo in a stable state, resulting in an increase of 4.6 times in the area under the curve (AUC) of pitavastatin. The effect of ciclosporin is unknown in a stable state on pitavastatin in a stable state. Contraindications for using livalo in patients being treated with ciclosporin (see the contraindications).

erythromycin: Erythromycin increases the meaning of Pitavastatin exposure. In patients using erythromycin, do not exceed the dose of livalo 1mg, 1 time/day.

Protease inhibitors of HIV and HCV: The simultaneous use of statin lipid medications with HIV and hepatitis C (HCV) can increase the risk of muscle damage, the most serious is muscle pattern, kidney damage leading to kidney failure and can cause death. Livalo has no restrictions on dosage when prescribing with protease inhibitors of HIV and the following HCV:

Atazanavir.

Atazanavir + Ritonavir Darunavir + Ritonavir.

Gemfibrozil and other fibrats: The use of solitary fibrat is sometimes related to muscle disease. Simultaneous use of fibrat with statin has been involved in muscle disease and muscle disease. Caution should be used when using livalo simultaneously with fibrat (see the warning and prudent section especially when used). In pharmacokinetics studies, simultaneously used livalo with gemfibrozil has led to an increase in AUC of Pitavastatin 1.4 times and the AUC increase of Fenofibrat 1.2 times.

Niacin: Interactive studies with pitavastatin and niacin have not been conducted. The use of solitary niacin has been related to muscle disease and muscle pattern when used in a single therapy form. Therefore, it is necessary to be cautious when used simultaneously with livalo with niacin.

Fusidic acid: The risk of muscle disease, including muscle pattern may increase when using fusidic acid simultaneously with statins. This interaction mechanism (whether it is pharmacoketic or pharmacokinetic interaction, or both) is not known. There have been reports on Tieu Co Van (including some deaths) in patients using this combination. If the treatment with Fusidic acid is necessary, it is necessary to stop treating with livalo during the fusidic acid treatment (see the warning and caution especially when used).

Rifampicin: Rifampicin significantly increases the exposure of Pitavastatin. In patients taking rifampicin, do not exceed the dose of 2mg, 1 time/day.

warfarin: pharmacokinetics and pharmacological resources in a stable state (International standardized ratio (INR) and prothrombin (PT) time of Warfarin in healthy volunteers are not affected by simultaneous use of 4 mg/day Livalo. However, like other statins, it is necessary to monitor the time of prothrombin or INR in patients taking warfarin when livalo is added to treatment.

Storage

Leave a cool place, avoid light, temperature below 30⁰C.

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