Rostat-10 Global Pharma medicine for hypercholesterol and prevent cardiovascular complications (1 blister x 10 tablets)

Dosage form Box of 1 blister x 10 tablets
Specifications Rosuvastatin

Ingredient

Composition information	Content
Rosuvastatin	10mg

Uses

Indications

Hyper cholesterol treatment:

Rostat is indicated for adults, adolescents and children 6 years of age and older suffering from primary blood cholesterol (type IIA including heterozygous family cholesterol) or mixed blood lipid disorders (type IIB) as a supportive therapy for diet when responding to diet and non -rational therapy (such as exercise, weight loss).

Rostat is also indicated for adults, adolescents and children aged 6 and older with hypercholesterol blood cholesterol as a dietary dose of diet and other lipid reduction treatments (such as LDL blood extract) or when these therapies are not suitable.

Prevention of cardiovascular complications:

Prevent cardiovascular complications in patients who are determined to be at high risk for the first cardiovascular complications, as a support dose to adjust other risk factors.

Pharmacokology

Rosuvastatin is a selective and competitive inhibitor on HMG-COA Reductase, which is a catalyst in the conversion of 3-hydroxy-3-methylglutaryl coenzyme A into Mevalonate, a precursor of cholesterol. Rosuvastatin reduces lipid in two ways. It increases the number of LDL receptors on the surface of liver cells, thus increasing the absorption and catabolism of LDL and inhibiting VLDL synthesis in the liver, thus reducing VLDL and LDL components.

Rosuvastatin reduces LDL-cholesterol levels, total cholesterol and triglycerides and increases HDL-cholesterol. The drug also reduces APOB, Non HDL-C, VLDL-TG and increases APOA-1. Rosuvastatin also reduces the ratio of LDL-C/HDL-C, C full/HDL-C, Non HDL-C/HDL and ароb/ароа-1.

Therapy responds to rosuvastatin clearly within 1 week of starting treatment and 90% of the maximum response is achieved within 2 weeks. The maximum response is usually achieved within 4 weeks and maintained later.

pharmacokinetics

absorption:

Rosuvastatin's peak plasma concentration is about 5 hours after drinking. Absolute bioavailability reaches approximately 20%.

Distribution:

Rosuvastatin is widely distributed in the liver where mainly synthesized cholesterol and LDL-C clearance. Rosuvastatin's distribution volume reaches approximately 134L. About 90% of rosuvastatin combined with plasma proteins, mainly albumin.

Metabolism:

Rosuvastatin is less metabolized (about 10%). Metabolic studies on test tubes using human liver cells show that rosuvastatin is a weak substrate for metabolism based on Cytochrom P450. CYP2C9 is a major enzyme involved in metabolism, 2C19, 3A4 and 2D6 have participated but at a lower level. The main metabolites are identified as N-Desmethyl and lactone metabolites. N-Desmethyl metabolites have 50% less activity than rosuvastatin while using lacton is considered to have no clinical activity.

Era:

approximately 90% of the dose of rosuvastatin is excreted in the feces (including the amount of rosuvastatin that has been absorbed and the amount of rosvastatin is not absorbed) and the rest is excreted into the urine.

approximately 5% rosuvastatin is excreted in a constant form in urine. Half life eliminated in plasma approximately 19 hours. Half lifetime elimination does not increase at higher doses. The average plasma clearance reaches approximately 50 liters/hour (the change coefficient is 21.7%). As with other HMG-COA Reductase inhibitors, the absorption of rosovastatin of the liver is related to OATP-C array. This transportation is very important for the liver elimination of rosuvastatin.

linear : Rosuvastatin's system exposure increases proportional to the dose, no change in daily pharmacokinetics parameters.

Special patient groups:

Age and gender: The impact of age and gender on the pharmacokinetics of rosuvastatin is negligible.

Race: Mobile pharmacokinetic studies show that approximately twice AUC and CMAX in Asians (Japan, China, Philippines, Vietnam and South Korea) compared to white people and Asians - India increased approximately 1.3 times AUC and CMAX. A pharmacokinetics analysis by population shows that there is no clinical difference in pharmacokinetics in white and black groups.

kidney failure: In people's research on kidney failure at different degrees, it shows that the kidney disease from mild to medium does not affect rosuvastatin concentration or N-Desmethyl metabolites in plasma. Patients with severe renal impairment (plasma creatinine clearance

liver failure:

In a study in patients with different levels of liver failure, there is no evidence of increasing exposure to rosuvastatin in humans with child-pugs from 7 or less.

Despite this, the two people with the Child-Pugh index are 8 and 9, showing a minimum increase in the system exposure to a person with lower Child-Pugh index. No experience used in patients with Child-Pugh index above 9.

genetic polymorphism: The distribution of HMG-CoA Reductase inhibitors, including rosuvastatin, is related to OatP1B1 and BCRP transport proteins. In patients with genetic polymorphism SLCOIBI (OATP1B1) and/or ABCG2 (BCRP), there is a risk of increased exposure to Rosuvastatin. SLCO1B1 C.521cc and ABCG2 C.421AA is related to higher exposure to Rosuvastatin (AUC) compared to SLCOIBI 6.521TT or ABCG2 C, 421cc. The specific genetic structure is not set in clinical practice, but for patients with these polymorphic types, a lower daily dose of Rostat should be recommended.

Children: Two pharmacokinetic studies with rosuvastatin (used in the form of tablets) in children with hypertension ages 10-17 or 6 to 17 years old (a total of 214 patients) have shown that exposure in children seems to be similar or lower than adults. Rosuvastatin exposure can be predicted by dosage and time for about 2 years.

Before taking Rostat-10 Global Pharma medicine for hypercholesterol and prevent cardiovascular complications (1 blister x 10 tablets)

How to use

Rostat can be used at any time of the day, with or without food.

Dosage

Before the beginning of treatment, the patient must follow the standard diet to reduce cholesterol and continue to maintain this diet during treatment. Dosage for patients for therapeutic purposes and response of each patient, using the current unified instructions.

blood cholesterol treatment

The recommended starting dose is 5 or 10mg, taken 1 time per day on both patients who have not used statins or patients transferred from other HMG inhibitors. The starting dose should be calculated according to the patient's cholesterol levels and the future cardiovascular risk as well as the potential risk to side effects. The dose adjustment can be conducted after 4 weeks, if necessary. The proportion of side effects reported increased at a dose of 40mg compared to the lower dose, the final dose standard to the maximum dose of 40mg should only be considered in patients with severe cholesterol increased with high cardiovascular risk (especially those with family cholesterol increased), those who do not achieve therapeutic goals at a dose of 20mg and those who will have to monitor daily. Need professional monitoring at the start of 40mg.

Prevent cardiovascular complications

In the study reduces the risk of cardiovascular complications, the dose is 20mg.

Children

Use for children should only be conducted by a specialist.

Children and teenagers from 6 to 17 years old (tanner

Hypermath of blood cholesterol:

In children and adolescents with heterozygous family increases using the starting dose of 5mg daily.

In children from 6 to 9 years old with hyperlested hypertension blood cholesterol, the usual dose is 5 - 10mg orally once a day. The safety and effectiveness of the dose greater than 20mg has not been studied in this group of objects. The safety and effectiveness of the dose greater than 20mg has not been studied in this object. Children and adolescents should be placed in the standard diet that reduces the standard cholesterol before starting the dose of rosuvastatin; This diet should be continued during treatment with rosuvastatin.

Hyper cholesterol of homozygous family:

In children from 6 to 17 years old with hyperlested hypertension, the maximum advanced dose is 20mg once a day.

A starting dose of 5 to 10mg once a day depends on the dose, weight and statin used before. Standard up to the maximum dose of 20mg once a day should be conducted according to the response of each patient and tolerance in children according to the recommendations of dosage treatment in children. Children and adolescents should be used to lower the standard cholesterol diet before starting to treat rosuvastatin dose; This diet continues during the treatment process with rosuvastatin.

also limited experience with a dose of more than 20mg in children.

Children under 6 years old:

Safety and effectiveness of children under 6 years old have not been set up. Therefore, Rostat is not recommended for use in children under 6 years old.

used in the elderly

A 5mg starting dose is recommended in patients ≥ 70 years old. There is no need to adjust other age -related dose.

Dosage in patients with renal failure

Unsurting dose adjustment in patients with mild to moderate renal failure. The starting dose is 5mg in medium renal failure patients (creatinine clearance Dosage in patients with liver failure

Do not increase the exposure of rosuvastatin in patients with a child-pugh score from 7 or less. However, increasing the exposure of rosuvastatin has been observed in patients with child-pugh scores from 8 to 9. In these patients, kidney function should be considered. Inexperienced in patients with Child-Pugh scores above 9. Rostat is contraindicated in patients with prematic liver patients.

race

Increased exposure has been seen in Asians. The recommended starting dose for Asian -based patients is 5mg. The 40mg dose is contraindicated in these patients.

genetic polymorphism

Certain genetic polymorphic types are known to lead to increased exposure to rosuvastatin. For patients known to have certain genetic polymorphisms, recommend daily dose lower than usual.

Dosage in patients with muscular trend factors

The recommended starting dose is 5mg in patients with muscle disease trend factors. The 40mg dose is contraindicated in some of these patients.

combined therapy

Rosuvastatin is a substrate of various shipping proteins (for example, OATP1B1 and BCRP). The risk of muscle diseases (including the granted muscle globin) increases when the Rostat is used simultaneously with a drug that may increase the level of rosuvastatin due to interaction with this shipping protein.

Whenever possible, consider changing the drug, and, if necessary, consider temporarily stop Rostat therapy. In case of inevitable use of these drugs with Rostat, carefully consider the benefits and risks of simultaneous therapy and adjust the dose of Rostat.

When using simultaneously rosuvastatin with protease inhibitors of HIV and HCV such as Atazanavir, Atazanavir + Ritonavir or Lopinavir + Ritonavir; Need to limit the dose of rosuvastatin up to 10 mg once a day.

What to do when overdose?

There is no specific treatment for overdose. When an overdose, the patient is treated with symptoms and applies supportive measures when necessary. Should monitor liver function and ck concentration. Blood decomposition may not benefit.

What to do when you forget 1 dose?

Side Effects

The events are not recorded when using rostat is usually light and transient. In controlled clinical studies, less than 4% of patients treated with Rostat withdrew from research due to unexpected events.

The frequency of unwanted events as follows: Common (> 1/100, 1/10,000,

Rare immune system disorders:

Nervous system disorders: Common: headache, dizziness.

Common digestive system disorders: Common: constipation, nausea, abdominal pain; Rare: Pancreatitis.

Skin and subcutaneous disorders: Uncommon: itchy rash and urticaria.

Disorders of musculoskeletal, connective tissue and bone: Common: muscle pain; Rarely: muscle disease, muscle pattern.

General disorders : Common: weakness. Like other HMG-CoA Reductase inhibitors, the frequency of unwanted effects related to drugs tends to depend on the dose.

The impact on the kidneys: proteinuria, detected by the test strip and has the main origin from the renal tubules, which has been recorded in patients treating Rostat. The change in the amount of proteinuria from no or only traces to positive (++) or higher has been noticed in impact on muscle - bone system: The impact on muscle - bone systems such as muscle pain, muscle diseases and some rare cases of muscle pattern have been recorded in patients treated with Rostat at all doses and especially at the doses> 20mg.

Increase the concentration of CK by use is observed in patients using rosuvastatin; Most in mild cases, asymptomatic and transient, if the concentration of CK increases (> 5 x ULN) the treatment should be temporarily suspended.

Acting on the liver: Like other HMG-CoA Reductase inhibitors, increasing transaminase by doses recorded in a few patients using rosuvastatin; Most cases are light, no symptoms and transparency.

Experience in the circulation of drugs:

In addition to the above -mentioned reactions, the events circulating the unwanted ancient seago drugs are also recorded during the circulation of Rostat drugs.

Liver -biliary disorders: very rare: jaundice, hepatitis; Rare: increasing liver enzymes.

Rare musculoskeletal muscle disorders: : joint pain.

nervous system disorders: very rare: multiple nerve disease, cognitive impairment (such as dementia, confusion, ...).

Rare metabolic disorders: Rare: Hyperglycemia, HBA1C.

Warnings

Contraindicated

Rostat is contraindicated in:

Patients with hypersensitivity to any ingredients of the drug. > Patients with renal failure (CLCR The 40mg dose is contraindicated in patients with a prior tendency for muscle disease/muscular globin. Factors include:

average renal failure (Creatinine clearance

Caution when using

influence on the kidneys

proteinuria, detected by the test strip and is the main origin from the renal tubules, which has been recorded in patients treated with high -dose Rostat, especially at 40mg dose, most of this situation occasionally or occasionally occurs. Proteinuria is not a warning sign of acute or progressive kidney disease. It is necessary to evaluate the kidney function during monitoring of patients who have been treated at a dose of 40mg.

Surgery influence

Musculosa effects such as causing muscle and muscle pain and some rare cases have been recorded in patients treated with rosuvastatin at all doses and especially at the doses of> 20mg.

measurement of creatinine kinase (ck)

Consider monitoring Creatine Kinase (CK) in the case:

Before treatment, CK tests should be conducted in the following cases: impaired renal function, hypothyroidism, self -history or family history of genetic muscle disease, a history of muscle disease due to statin or fibrat before, a history of liver disease and/or drinking lots of alcohol, elderly patients (> 70 years old) with risk factors for medication and some patients. In these cases, the benefits/risks should be considered and monitor patients clinically when treated with statin. If the results of CK test> 5 times the upper limit of normal levels, do not start statin treatment.

Do not measure the creatinine Kinase (CK) concentration after exertion or when there is a certain cause that can increase CK because this can falsify the results.

Before treatment:

Like other HMG-CoA Reductase inhibitors, caution should be cautious when using Rostat in patients with factors that can lead to muscle disease (muscle pilot) such as:

Renal failure. Tuong.

Simultaneously used with fibrats. In these patients should consider the risk and benefits of treatment and clinical monitoring. If the CK concentration increases significantly before treatment (> 5 x ULN), it is not advisable to start treatment with Rostat.

During treatment:

Should ask the patient to immediately report muscle pain, muscle weakness or cracking, especially if there is fatigue or fever. CK concentration should be measured in these patients. Rosuvastatin should be stopped if CK concentration increases significantly (> 5 x ULN) or severe muscle symptoms and daily discomfort (even if the concentration of CK

Periodic monitoring of CK concentrations in patients with no symptoms that are not guaranteed to detect muscle disease.

In clinical trials, there is no increase in skeletal effects in a small number of patients using Rostat simultaneously with other drugs. However, the increase in the incidence of muscle and muscle disease has been seen in patients using other HMG-CoA reductase inhibitors simultaneously simultaneously with the derivatives of fibric acid including gemfibrozil, cyclosporin, nicotinic acid, antifungal group Azol, enamel inhibitors and antibiotic macrolid, gemfibrozils that increase the risk of enamel when using fabric HMG-COA Reductase. Therefore, the coordination between Rostat and Gemfibrozil is not recommended. The use of Rostat combination with fibrat or niacin to achieve further change of lipid levels, should carefully consider the benefits and risks that may occur due to these combinations (see "drug interactions" & "adverse effects").

Do not use Rostat for patients with acute serious condition, suspicion caused by muscle disease or may lead to secondary renal failure with muscle panaseline (such as blood infection, hypotension, surgery, injury, electrolyte disorders, endocrine and severe conveys; or uncontrolled convulsions).

influence on the liver

Like other HMG-CoA Reductase inhibitors, be careful when using Rostat in patients with severe alcoholism and/or a history of liver disease.

Do liver enzyme tests before starting statin treatment and in case of clinical indications for testing later. Rostat dose should be discontinued if the serum transaminase concentration is 3 times the upper limit of the normal level.

In patients with secondary cholesterol hyperpactive patients due to thyroid discharge or nephrotic syndrome, these patients must be treated before they start using Rostat.

race

Dynamic studies show that there is an increase in the level of exposure to drugs calculated by concentration and time in Asian patients compared to white people (see "dose/use" & "pharmacokinetics").

Protease inhibitors

Increased exposure to the Rosuvastatin system has been observed in patients using Rosuvastatin simultaneously along with different protease inhibitors in combination with Ritonavir. It is necessary to consider the benefits of lipid lowering due to the use of Rostat in HIV patients who are using protease inhibitors and the risk of increased plasma Rosuvastatin levels when starting and adjusting the dose of Rostat in patients who treated with protease inhibitors. Simultaneous use with protease inhibitors is not recommended unless the dose is adjusted.

Lactose tolerance

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

Patients with interstitial lung disease

There have been rare reports of cases of interstitial lung disease with some statins, especially prolonged therapy. Symptomatic characteristics may include shortness of breath, dry cough and general health impairment (fatigue, weight loss and fever). If the patient is suspected of having progressive pneumonia, Statin therapy should be stopped immediately.

diabetes

Some evidence that statin is a type of blood glucose and in some patients, at high risk of diabetes, can cause high blood sugar levels, so blood sugar control. However, it is not necessary to stop statin therapy for this reason. Patients with risk (thrilling blood sugar is 5.6 to 6.9 mmol/liter, BMI> 30 kg/m2, increased triglycerides, hypertension) should be controlled both clinical and biochemical under international instructions.

In Jupiter study, the frequency of diabetes was reported by 2.8% in the rosuvastatin group and 2.3% in the placebo group, mainly in patients with blood sugar at 5.6 to 6.9 mmol/l.

Children

The assessment of linear development (height), BMI weight (body weight index), and auxiliary characteristics of sexual development in children from 6 to 17 years old using Rosuvastatin are limited in a 2 -year period. After 2 years of research therapy, there is no impact on growth, weight, BMI or sex development.

On a clinical trial in children and young people using rosuvastatin for 52 weeks, CK increased> 10 x ULN and post -exercise or increased physical activity symptoms were observed with more common frequency than observations in clinical trials in adults.

Pregnant and lactating women

Women may be pregnant should use appropriate contraceptive measures.

Because cholesterol and other cholesterol biosynthesis are necessary for fetal development, the potential risk due to HMG-CAA Reductase inhibitors will dominate the benefits of Rostat treatment during pregnancy. Animal studies show that there are evidence of limited toxicity on the reproductive system ("Pre -clinical safety") If the patient is pregnant while treating cholesterol, the drug should be stopped immediately. In mice, rosuvastatin excreted in milk. There is no corresponding data on human excretion (see contraindicated).

The effect of the drug on driving and operating machinery

studies to determine the effect of Rostat on driving and operating the machine has not been performed. However, based on the pharmaceutical properties, Rostat cannot affect these possibilities. When driving or operating machinery, it should be noted that dizziness may occur during treatment.

Use drugs for women during pregnancy and lactation

Rostat contraindicated in pregnant and lactating women.

Drug interaction

cyclosporin:

Simultaneously use Rostat with cyclosporin, the AUC values of rosuvastatin are 7 times higher than that of this value in healthy volunteers (see "" contraindications "). Simultaneous use of Rostat and Cyclosporin does not affect cyclosporin levels in plasma.

Vitamin K antagonists:

Similar to other HMG-CoA Reductase inhibitors, when starting to treat or increase the dose of Rostat in patients treated simultaneously with vitamin K antagonists (such as warfarin) may increase the Inr value. Stopping or reducing the dose of Rostat may reduce the INR. In such cases, the Inr value should be monitored.

Colchicin: Increased risk of muscle damage when using statin simultaneously with colchicin drugs.

gemfibrozil, high -dose niacin and other blood lipid medications:

Simultaneously use Rostat with Gemfibrozil 2 times the value of CMAX and AUC of Rosuvastatin (see "Preventive and cautious attention when used"). Based on data from specialized drug interactive studies, there is no significant pharmacokinetic interaction with Fenofibrat, but the pharmaceutical interaction may occur. Gemfibrozil, Fenofibrat, other fibrats and niacin (nicotinie acid at lipid doses (> = 1 g/day) increase the risk of muscle disease when used simultaneously with HMC-Coa Reductase inhibitors may be possible because these drugs can cause muscle disease when used individually.

antacids: Use Rostat simultaneously with aluminum antacids and Magnesi Hydoxid, which reduces about 50% of rosvastatin concentrations in plasma. When taking antacids 2 hours after using Rostat, the rosomastatin level in plasma will decrease less. The clinical correlation of this interaction is still unclear.

erythromycin:

Simultaneous use of Rostat with erythromycin reduces 20% AUC (0-T) and 30% cmax of rosuvastatin. This interaction may be due to erythromycin increasing intestinal motility.

Oral contraceptives/hormone replacement therapy (HRT):

Simultaneous use of Rostat with contraceptive pill increased by 26% AUC of Ethinyl Extradiol and 34% AUC of Norgestrel. It should be noted that increasing the concentration of these substances in plasma when choosing birth control pills.

There is no pharmacological data on patients who simultaneously use Rostat and HRT and therefore cannot exclude the same possibility. However, this combination has been widely used in women in clinical trials and has been well tolerated.

Other drugs:

Based on data from specialized drug interactions, there is no clinical interaction when used with digoxin.

Ezetimibe: simultaneously use 10mg of Rostat and 10mg Ezetimid, resulting in an increase of 1.2 times AUC Rosuvastatin in humans of hypercholesterol. It is impossible to exclude a pharmacological interaction that causes side effects between Rostat and Ezetimib.

Cytochrom P450: The result from In Vitro and In Vivo tests proves that RosuVastatin is not an inhibitor or cytochrom P450 inhibitor. Moreover, Rosuvastatin is a weak substrate for these isenzymes. Do not record clinical related interactions between rosuvastatin and fluconazole (CYP2C9 and CYP3A4 inhibitors) or ketoconazole (CYP2A6 and CYP3A4 inhibitors). Simultaneous use with otraconazole (CYP3A4 inhibitor) and rosuvastatin increases 28% AUC of rosuvastatin. This increase is not considered clinical significance. Therefore, there is no drug interaction due to metabolism through cytochrom P450.

Protease inhibitors: In a dynamic study, simultaneously used Rostat with a preparation combining 2 protease inhibitors (Lopinavir 400mg/ritonavir 100mg) in healthy volunteers increasing the AUC index (0-24) stable state 2 times and CMAX up to 5 times. Interaction between Rostat and other protease inhibitors has not been verified. It is necessary to consider the benefits of reducing blood lipids in HIV patients taking Lopinavir/Ritonavir with the risk of increasing concentration and time of Rosuvastatin exposure at the beginning of treatment and when increasing the dose of Rostat.

Simultaneous use of statin lipid medications with HIV and hepatitis C (HCV) can increase the risk of muscle damage, the most serious muscle, kidney damage leading to kidney failure and may be fatal.

Storage

Leave in a dry place, avoid light, the temperature does not exceed 30 ° C.

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