Product Overview
[Drug Name]
Generic Name: Rosuvastatin Calcium Tablets
Trade Name: Dongyang Sunshine Rosuvastatin Calcium Tablets 5mg x 14 Tablets
[Main Ingredients]
The active ingredient of this product is rosuvastatin calcium. Chemical Name: Bis-[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt (2:1) Molecular Formula: (C22H27FN3O6S)2Ca Molecular Weight: 1001.13
[Properties]
This product is a white or off-white film-coated tablet that appears white or off-white after removal of the coating.
[Indications/Main Functions]
This product is indicated for the treatment of primary hypercholesterolemia (type Ia, including heterozygous familial hypercholesterolemia) or mixed dyslipidemia (type Ib), whose dyslipidemia is inadequately controlled with diet and other non-drug therapies (e.g., exercise therapy, weight loss). This product is also indicated for patients with homozygous familial hypercholesterolemia as an adjunct to diet and other lipid-lowering measures (e.g., LDL-denier depletion therapy), or when these approaches are inadequate. Usage.
[Specifications]
5mg*14 tablets
[Dosage and Administration]
Before starting treatment, patients should follow a standard cholesterol-lowering diet and maintain this diet during treatment. The use of this product should be individualized, taking into account the patient's individual cholesterol level, expected cardiovascular risk, and potential risk of adverse reactions. Oral administration. The usual starting dose of this product is 5mg once daily. The starting dose should be selected based on the patient's individual cholesterol level, expected cardiovascular risk, and potential risk of adverse reactions. For patients requiring more intensive low-density lipoprotein cholesterol (LDL-C) lowering, a 10mg once daily dose can be considered. This dose controls lipid levels in most patients. If necessary, the dose can be adjusted to a higher dose level after 4 weeks of treatment. The maximum daily dose is 20mg. This product can be taken at any time of day, with or without food. Use in Patients with Renal Insufficiency No dose adjustment is required for patients with mild and moderate renal impairment. All doses of this product are contraindicated in patients with severe renal impairment. In patients with hepatic impairment, systemic exposure to rosuvastatin was not increased in subjects with a Child-Pugh score of 7 or less. Increased systemic exposure was observed in subjects with Child-Pugh scores of 8 and 9. A functional evaluation should be considered in these patients. There is no experience with the use of this product in patients with a Child-Pugh score exceeding 9, and this product is contraindicated in patients with active liver disease. Increased systemic exposure has been observed in subjects of Asian descent. This factor should be considered when determining the dose for patients of Asian descent. Dosing recommendations for patients with myopathy-predisposing factors: The recommended starting dose for patients with myopathy-predisposing factors (see [Precautions]) is 5 mg.
[Adverse Reactions]
See package insert for details.
[Contraindications]
This product is contraindicated in patients with: Hypersensitivity to rosuvastatin or any of its ingredients; patients with active liver disease, including unexplained persistent elevations of serum transaminases and any elevation of serum transaminases greater than 3 times the upper limit of normal (ULN); patients with severe renal impairment (i.e., anhydride clearance <30 mcg/min); patients with myopathy; patients taking cyclosporine concomitantly; and women who are pregnant, breastfeeding, or at risk of pregnancy and are not using adequate contraceptive measures.
[Precautions]
Renal Effects: Proteinuria (as determined by dipstick) has been observed in patients treated with high doses, particularly 40 mg. The majority of the protein is derived from the renal tubules and, in most cases, is transient or intermittent. Proteinuria is not considered a precursor to acute or progressive renal disease (see "Adverse Reactions"). Effects on skeletal muscle: Skeletal muscle effects, such as myalgia, myopathy, and, rarely, rhabdomyolysis, have been reported in patients treated with all doses of this drug, particularly in patients receiving doses greater than 20 mg. Extremely rare cases of rhabdomyolysis have been reported with the concomitant use of ezetimibe and HMG-CoA reductase inhibitors. Drug interactions cannot be ruled out; caution should be exercised when these drugs are used together. Creatine kinase (CK) testing should not be performed after strenuous exercise or in the presence of plausible factors that could cause elevated CK, as this can confound the interpretation of the results. If baseline CK values are significantly elevated (>5×ULN), retesting should be performed within 5–7 days. If repeat testing confirms a baseline CK value >5×ULN, treatment should not be initiated. Before treatment, and with other HMG-CoA reductase inhibitors, As with other inhibitors, this drug should be used with caution in patients with predisposing factors to myopathy/rhabdomyolysis. These factors include: renal impairment, hypothyroidism, personal or family history of hereditary muscle disease, a history of muscle toxicity with other HMG-CoA reductase inhibitors or fibrates, alcohol abuse, and age >70 years. Elevated blood concentrations may occur. For these patients, the potential benefits of treatment should be balanced against the potential risks when using fibrates concurrently, and clinical monitoring is recommended. Treatment should not be initiated if baseline creatine kinase levels are significantly elevated (>5×ULN). During treatment, patients should be instructed to immediately report unexplained muscle pain, weakness, or cramping, especially if accompanied by malaise and fever. Creatine kinase levels should be measured in these patients. If creatine kinase levels are significantly elevated (>5×ULN) or muscle symptoms are severe and cause overall distress, the patient should be monitored. If symptoms resolve and creatine kinase levels return to normal, consider re-administering this product or switching to the lowest dose of another HMG-CoA reductase inhibitor and closely monitoring patients. Regular monitoring of creatine kinase levels is not necessary for asymptomatic patients. Rare reports of immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy, have been reported in association with statin use. IMNM is characterized by proximal muscle weakness and elevated serum creatine kinase, which persists regardless of statin discontinuation. Muscle biopsy reveals necrotizing myopathy without significant inflammation; improvement occurs with immunosuppressive therapy. In clinical studies, there was no evidence of increased drug effects on skeletal muscle in the small number of patients receiving this product concurrently with other therapies. However, it has been found that The incidence of myositis and myopathy is increased in patients receiving other HMG-CoA reductase inhibitors concomitantly with fibric acid derivatives (including gemfibrozil), cyclosporine, niacin, azole antifungals, protease inhibitors, or macrolide antibiotics. Concomitant use of gemfibrozil with some HMG-CoA reductase inhibitors may increase the risk of myopathy. Therefore, coadministration of this drug with gemfibrozil is not recommended. The benefits of combining this drug with fibrates or niacin to further improve lipid levels should be carefully weighed against the potential risks of this combination. Coadministration of rosuvastatin with fusidic acid is not recommended. Rhabdomyolysis (including fatalities) has been reported in patients receiving this combination. (See "Drug Interactions.") In any patient with an acute, severe illness suggestive of myopathy or with a predisposing condition to renal failure secondary to rhabdomyolysis (e.g., sepsis, hypotension, major surgery). This product should not be used in patients with severe metabolic, endocrine, or electrolyte abnormalities, or uncontrolled epilepsy. Similar to other HMG-CoA reductase inhibitors, this product should be used with caution in patients who consume excessive alcohol and/or have a history of liver disease. Liver function tests are recommended before starting treatment and three months after initiation. If serum transaminases are elevated more than three times the upper limit of normal, this product should be discontinued or the dose reduced. For hypercholesterolemia secondary to hypothyroidism or nephrotic syndrome, the underlying disease should be treated before starting this product. Ethnic pharmacokinetic studies have shown that drug exposure is higher in Asian subjects than in Caucasians. Increased systemic exposure of rosuvastatin has been observed in subjects receiving rosuvastatin in combination with different protease inhibitors (combined with linavir). Patients receiving protease inhibitors should be fully considered. The lipid-lowering benefits of this medication in patients with HIV treated with enzyme inhibitors, as well as the potential for increased rosuvastatin plasma concentrations when co-administered with protease inhibitors, are considered. Co-administration with protease inhibitors is not recommended unless the dose of this medication is adjusted. Lactose intolerance: Patients with rare hereditary conditions such as galactose intolerance, lactase deficiency, or glucose-galactose malabsorption should not take this medication. Interstitial lung disease: Rare cases of interstitial lung disease have been reported with some statin therapy, particularly with long-term treatment. Symptoms include dyspnea, a dry cough without productive cough, and a decline in overall health (fatigue, weight loss, and fever). Statins should be discontinued in patients with suspected interstitial lung disease. Diabetes: There have been reports of an association between the use of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (including this medication) and elevated glycated hemoglobin. Rosuvastatin is associated with elevated A1C, HbA1e, and fasting serum glucose levels. Clinical and biochemical monitoring should be performed in accordance with relevant guidelines for at-risk patients (fasting blood glucose: 5.6-6.9 mol/L, BMI >30 kg/m2, elevated triglycerides, and hypertension). For pediatric patients aged 10-17 years and within the period of secondary sexual maturity according to Tenner stage, the duration of rosuvastatin treatment is limited to one year based on linear growth (height, weight, BMI, and body mass index). After 52 weeks of study treatment, there were no effects on growth, weight, BMI, or sexual maturation. Clinical trial experience in children and pediatric patients is limited. The effects of long-term (greater than one year) treatment with rosuvastatin in adolescent patients are unknown. In 52-week clinical trials, pediatric and adolescent patients treated with rosuvastatin experienced elevations of creatine kinase greater than 10×ULN and muscle symptoms following exercise or increased physical activity at a higher frequency than those observed in adult clinical trials (see Adverse Reactions). Studies to determine the effects of rosuvastatin on driving and operating machinery have not been conducted. However, based on its pharmacodynamic properties, rosuvastatin is unlikely to affect these abilities. The potential for dizziness during treatment should be considered when driving or operating machinery.
