Rosuvastatin Calcium Tablets

1. Rosuvastatin is a selective and competitive HMG-CoA reductase inhibitor. HMG-CoA reductase is the rate-limiting enzyme in the conversion of 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, which is a precursor of cholesterol. Animal and cell culture test results show that rosuvastatin is highly absorbed by the liver and is selective, and the liver is the target organ for lowering cholesterol. In vivo and in vitro test results show that rosuvastatin can increase the number of liver LDL receptors on the cell surface, thereby enhancing the uptake and catabolism of LDL, and inhibiting liver VLDL synthesis, thereby reducing the total number of VLDL and LDL particles. 2. For patients with homozygous and heterozygous familial hypercholesterolemia, non-familial hypercholesterolemia, and mixed dyslipidemia, rosuvastatin can reduce total cholesterol, LDL-C, ApoB, and non-HDL-C levels. Rosuvastatin can also reduce TG and increase HDL-C levels. For patients with simple hypertriglyceridemia, rosuvastatin can reduce total cholesterol, LDL-C, VLDL-C, ApoB, non-HDL-C, TG levels, and increase HDL-C levels. The effect of rosuvastatin on cardiovascular morbidity and mortality has not yet been determined.

The main ingredient of this product is rosuvastatin calcium.

This product is a film-coated tablet, which appears white or off-white after removing the coating.

1. This product is suitable for primary hypercholesterolemia (type IIa, including heterozygous familial hypercholesterolemia) or mixed dyslipidemia (type IIb) whose dyslipidemia cannot be properly controlled by diet control and other non-drug treatments (such as exercise therapy, weight loss). 2. This product is also suitable for patients with homozygous familial hypercholesterolemia as an adjuvant treatment for diet control and other lipid-lowering measures (such as LDL removal therapy), or when these methods are not applicable.

Before the start of treatment, patients should be given a standard cholesterol-lowering diet and maintain diet control during treatment. The use of this product should follow the principle of individualization, taking into account the individual cholesterol level of the patient, the expected cardiovascular risk, and the potential risk of adverse reactions. Oral. The common starting dose of this product is 5 mg, once a day. The selection of the starting dose should take into account the individual cholesterol level of the patient, the expected cardiovascular risk, and the potential risk of adverse reactions. For patients who need to more effectively reduce low-density lipoprotein cholesterol (LDL-C), 10 mg once a day can be considered as the starting dose, which can control the blood lipid level of most patients. If necessary, the dose can be adjusted to a higher dose level after 4 weeks of treatment. The maximum daily dose of this product is 20 mg. This product can be administered at any time of the day, either with food or on an empty stomach. 1. Medication for patients with renal insufficiency Patients with mild and moderate renal impairment do not need to adjust the dose. All doses of this product are contraindicated for patients with severe renal impairment. 2. Use in Patients with Impaired Liver Function In subjects with a Child-Pugh score of 7 or less, the systemic exposure of rosuvastatin was not increased. In subjects with Child-Pugh scores of 8 and 9, an increase in systemic exposure was observed. In these patients, an assessment of renal function should be considered. There is no experience with the use of this product in patients with a Child-Pugh score of more than 9. This product is contraindicated in patients with active liver disease. 3. Race Increased systemic exposure has been observed in Asian subjects. This factor should be considered when determining the dosage for patients of Asian descent.

The adverse reactions seen with this product are usually mild and transient. In controlled clinical trials, less than 4% of patients withdrew from the trial due to adverse events. 1. The frequency of adverse events is ranked in the following order: common (1/100, 1, 10): occasional (1/1,000, 1/100); rare (1/10,000, 1/1000); very rare (1/10,000). 1.1 Common: endocrine disorders (diabetes): nervous system abnormalities (headache, dizziness): gastrointestinal abnormalities (constipation, nausea, abdominal pain); skeletal muscle, joint and bone abnormalities (myalgia): systemic abnormalities (weakness). Occasionally: skin and subcutaneous tissue abnormalities (itching, rash and urticaria) 1.2 Rare: immune system abnormalities (allergic reactions, including angioedema): gastrointestinal abnormalities (pancreatitis): skeletal muscle, joint and bone abnormalities (myopathy (including myositis) and rhabdomyolysis). Like other HMG-CoA reductase inhibitors, the incidence of adverse reactions of this product tends to increase with increasing doses. Effects on the kidneys: Proteinuria (test strip method) was observed in patients receiving this product, and most of the protein originated from the renal tubules. Less than 1% of patients had proteinuria from none or trace to or more at certain times during 10mg and 20mg treatment, and this proportion was about 3% in patients receiving 40mg treatment. In 20mg dose treatment, proteinuria was observed to increase from none or trace to a mild increase. In most cases, proteinuria automatically decreased or disappeared after continued treatment. Based on clinical trials and post-marketing data to date, a causal relationship between proteinuria and acute or progressive renal disease cannot be determined. 2. Hematuria has been observed in patients using this product, and data from clinical trials show that its incidence is very low. 2.1 Effects on skeletal muscle: Effects on skeletal muscle have been reported in patients receiving various doses of this product, such as myalgia, myopathy (including myositis), and rare rhabdomyolysis, especially in patients using doses greater than 20mg. 2.2 Dose-related increases in creatine kinase (CK) levels were observed in patients taking this product: most cases were mild, asymptomatic and transient. If CK levels are elevated (5 times; ULN), treatment should be discontinued (see [Precautions]). 2.3 Effects on the liver: As with other HMG-CoA reductase inhibitors, dose-related increases in transaminases were observed in a small number of patients taking this product: most cases were mild, asymptomatic and transient. 3. Post-marketing experience: In addition to the above reactions, the following adverse events have been reported during the post-marketing use of this product: 3.1 Rare: Hepatobiliary system disorders (elevated liver transaminase). 3.2 Very rare: Nervous system disorders (polyneuropathy, memory loss); Hepatobiliary system disorders (jaundice, hepatitis): Musculoskeletal system disorders (arthralgia): Urinary system disorders (hematuria). 3.3 Unknown: Respiratory, thoracic, mediastinal disorders (cough, dyspnea): Gastrointestinal disorders (diarrhea): Skin and subcutaneous tissue disorders (Stevens-Johnson syndrome): General symptoms and medication site conditions (edema); Psychiatric disorders: Depression, sleep disorders (including insomnia and nightmares) 3.4 Pediatric patient population: In a 52-week clinical trial, children and adolescent patients treated with rosuvastatin were found to have an increase in creatine kinase greater than 10 times; ULN, and muscle symptoms observed after exercise or increased physical activity, which were observed more frequently than in clinical trials conducted in adults. In other aspects, the safety of rosuvastatin in children and adolescents is similar to that in adults.

This product is contraindicated for: 1. Patients who are allergic to rosuvastatin or any of the ingredients in this product. 2. Patients with active liver disease, including patients with unexplained persistent elevation of serum aminotransferase and any elevation of serum aminotransferase exceeding 3 times the upper limit of normal (ULN). 3. Patients with severe renal impairment (creatinine clearance 30ml/min). 4. Patients with myopathy. 5. Patients who are taking cyclosporine at the same time. 6. Women who are pregnant, breastfeeding, or who may become pregnant but do not take appropriate contraceptive measures.

Precautions for children: The safety and effectiveness of this product in children have not been established. The experience of pediatric use is limited to a small number of children (age 8 years) with homozygous familial hypercholesterolemia. Therefore, this product is not recommended for pediatric use at present. Precautions for pregnancy and lactation: 1. This product is contraindicated for use in pregnant and lactating women. 2. Women who may become pregnant should take appropriate contraceptive measures. 3. Because cholesterol and other cholesterol biosynthesis products are important for the development of the embryo, the risks from HMG-CoA reductase inhibition outweigh the benefits of treatment for pregnant women. Animal studies provide limited evidence of reproductive toxicity. If a patient becomes pregnant while using this product, treatment should be discontinued immediately. Rosuvastatin can be secreted into human rat milk. There is no information on the secretion of rosuvastatin into human milk. Precautions for the elderly: No dosage adjustment is required.

1. Cyclosporine: When this product is used in combination with cyclosporine, the AUC of rosuvastatin is 7 times higher than the average observed in healthy volunteers (compared with taking the same dose of this product). Co-administration does not affect the plasma concentration of cyclosporine. 2. Vitamin K antagonists: Like other HMG-CoA reductase inhibitors, for patients who are also taking vitamin K antagonists (such as warfarin), starting this product or gradually increasing the dose of this product may lead to an increase in INR. Discontinuation of this product or gradually reducing the dose of this product may lead to a decrease in INR. In this case, appropriate monitoring of INR is necessary. 3. Gemfibrozil and other lipid-lowering products: When this product is used simultaneously with gemfibrozil, the Cmax and AUC of rosuvastatin can be increased by 2 times. Based on the data from special interaction studies, it is expected that this product has no pharmacokinetic interaction with fenofibrate, but pharmacodynamic interactions may occur. The risk of myopathy increases when gemfibrozil, fenofibrate, other fibrates, and lipid-lowering doses of niacin (1 g/day) are used in combination with HMG-CoA reductase inhibitors, which may be due to their ability to cause myopathy when administered alone. 4. Protease inhibitors: Although the mechanism of drug interaction is not clear, the simultaneous use of protease inhibitors may greatly increase the exposure of rosuvastatin. In a pharmacokinetic study, healthy volunteers took 20 mg of this product and a combination product of two protease inhibitors (400 mg lopinavir/100 mg ritonavir) at the same time. The results showed that the steady-state AUC (0-24) and Cmax of rosuvastatin increased by approximately 2 times and 5 times, respectively. Therefore, the simultaneous use of this product is not recommended in HIV patients receiving protease inhibitor treatment (see [Precautions]). 5. Antacids: The simultaneous administration of this product and an antacid suspension containing aluminum magnesium hydroxide can reduce the plasma concentration of rosuvastatin by approximately 50%. This effect can be mitigated if the antacid is given 2 hours after taking this product. The clinical significance of this drug interaction has not been studied. 6. Erythromycin: The co-administration of this product with erythromycin resulted in a 20% decrease in the AUC (0-t) of rosuvastatin and a 30% decrease in Cmax. This interaction may be due to the increased gastrointestinal motility caused by erythromycin. 7. Oral contraceptives, hormone replacement therapy (HRT): The simultaneous use of this product and oral contraceptives increased the AUC of estradiol and norgestrel by 26% and 34%, respectively. These increases in blood concentrations should be considered when selecting the dose of oral contraceptives. There are no pharmacokinetic data on subjects who use this product and HRT at the same time, so similar interactions cannot be ruled out. However, in clinical trials, this combination was widely used and well tolerated by patients. 8. Other drugs: Based on data from dedicated drug interaction studies, it is estimated that this product does not have a clinically relevant interaction with digoxin. 9. Cytochrome P450 enzymes: Data from both in vitro and in vivo studies have shown that rosuvastatin is neither an inhibitor nor an enzyme inducer of cytochrome P450 isoenzymes. In addition, rosuvastatin is a weak substrate for these enzymes. There are no clinically relevant interactions between rosuvastatin and fluconazole (an inhibitor of CYP2C9 and CYP3A4) or ketoconazole (an inhibitor of CYP2A6 and CYP3A4). Co-administration with itraconazole (an inhibitor of CYP3A4) increased the AUC of rosuvastatin by 28%, an increase that is not considered clinically significant. Therefore, drug interactions due to cytochrome P450-mediated metabolism are not expected.

Sealed, store in a dry place.

5mg

36 months

Nanjing Chia Tai-tianqing Pharmaceutical Co., Ltd.

• Founded in:

  2001-08-31

• Address:

  No. 9 Huiou Road, Nanjing Economic and Technological Development Zone

• Tax NO.:

  91320100730586189T

• Registered Funds:

  336.031726 yuan

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