Product Overview
[Drug Name]
Generic Name: Rosuvastatin Calcium Tablets
Trade Name: Dongyang Sunshine Rosuvastatin Calcium Tablets 10mg 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. After removing the coating, it appears white or off-white.
[Indications/Main Functions]
This product is indicated for patients with primary hypercholesterolemia (type IIa, including heterozygous familial hypercholesterolemia) or mixed dyslipidemia (type IIb), 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-C depletion therapy), or when these measures are inadequate.
[Specifications]
10mg x 14 tablets
[Dosage and Administration]
Before treatment begins, patients should be on 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. For oral administration, the usual starting dose is 5 mg once daily. The selection of the starting dose should be based on the patient's individual cholesterol level, expected cardiovascular risk, and potential risk of adverse reactions. For patients requiring more robust low-density lipoprotein cholesterol (LDL-C) lowering, a starting dose of 10 mg once daily can be considered. This dose controls lipid levels in most patients. If necessary, the dose can be adjusted to the next higher dose level after 4 weeks of treatment. The maximum daily dose of this product is 20 mg. This product can be taken at any time of day, with or without food. Patients with Renal Impairment: 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. 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. In these patients, renal function should be evaluated. There is no experience with the use of this product in patients with a Child-Pugh score of 9 or higher. This product is contraindicated in patients with active liver disease. Ethnicity: Increased systemic exposure has been observed in subjects of Asian descent. This factor should be considered when determining the dosage for patients of Asian descent. Dosage 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 the package insert for details.
[Contraindications]
This product is contraindicated in patients with: Hypersensitivity to rosuvastatin or any of its ingredients; Active liver disease, including unexplained persistent elevations in serum transaminases and any elevation of serum transaminases exceeding three times the upper limit of normal (ULN); Severe renal impairment (creatinine clearance <30 ml/min); Myopathy; Patients taking cyclosporine concomitantly; Pregnancy, lactation, and women of childbearing potential who are not using adequate contraception.
[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"). Skeletal Muscle Effects: Skeletal muscle effects, such as myalgia, myopathy, and, rarely, rhabdomyolysis, have been reported in patients receiving all doses of this product, particularly in doses greater than 20 mg. There have been extremely rare reports of rhabdomyolysis with the concomitant use of ezetimibe and HMG-CoA reductase inhibitors. Drug interactions cannot be ruled out, and 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 factors that could potentially cause elevated CK, as this can confound 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. As with other HMG-CoA reductase inhibitors, caution should be exercised when using this drug in patients with predisposing factors to myopathy/rhabdomyolysis. These factors include: renal impairment, hypothyroidism, personal or family history of hereditary muscle disorders, a history of muscle toxicity with other HMG-CoA reductase inhibitors or fibrates, and alcohol abuse. Elevated blood concentrations may occur in patients over 70 years of age. For patients receiving concurrent fibrates, the potential benefits of treatment should be weighed against the potential risks, 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 promptly report unexplained muscle pain, weakness, or cramping, especially if accompanied by malaise and fever. Creatine kinase levels should be measured in these patients. Treatment should be discontinued if creatine kinase levels are significantly elevated (>5×ULN) or if muscle symptoms are severe and cause daylong discomfort (even if creatine kinase is ≤5×ULN). If symptoms resolve and creatine kinase levels return to normal, consider restarting levofloxacin or switching to the lowest dose of another HMG-CoA reductase inhibitor and closely monitoring the patient. Regular monitoring of creatine kinase levels is not necessary for asymptomatic patients. Rare cases 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 despite discontinuation of other medications. Muscle biopsy reveals necrotizing myopathy without significant inflammation; this condition improves with immunosuppressive therapy. In clinical studies, there was no evidence of increased skeletal muscle effects in the small number of patients receiving this medication concurrently with other therapies. However, an increased incidence of myositis and myopathy has been observed 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, concomitant use of this medication with gemfibrozil is not recommended. The benefits of combining this medication with fibrates or niacin to further improve lipid levels should be carefully weighed against the potential risks of this combination. Combination use of rosuvastatin and fusidic acid is not recommended. Rhabdomyolysis (including fatalities) has been reported in patients receiving this combination. (See "Drug Interactions.") This medication should not be used 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, trauma, severe metabolic, endocrine, or electrolyte abnormalities, or uncontrolled epilepsy). Similar to other HMG-CoA reductase inhibitors, this medication should be used with caution in patients with excessive alcohol consumption and/or a history of liver disease. Liver function tests are recommended before and three months after starting treatment. If serum aminotransferases are elevated more than three times the upper limit of normal, this medication should be discontinued or the dose reduced. For hypercholesterolemia secondary to hypothyroidism or nephrotic syndrome, the underlying condition should be treated before initiating rosuvastatin therapy. Ethnic pharmacokinetic studies have shown that Asian subjects have higher drug exposure than Caucasians. Protease inhibitors: Increased systemic exposure of rosuvastatin has been observed in subjects receiving rosuvastatin concomitantly with various protease inhibitors (including ritonavir). The lipid-lowering benefits of rosuvastatin in HIV patients receiving protease inhibitor therapy should be carefully considered, as should the potential for increased rosuvastatin plasma concentrations with concomitant protease inhibitor therapy. Coadministration with protease inhibitors is not recommended unless the dose of rosuvastatin is adjusted. Lactose intolerance: Patients with rare hereditary conditions such as galactose intolerance, lactase deficiency, or glucose-galactose malabsorption should not take rosuvastatin. 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, nonproductive cough, and a decline in overall health status (fatigue, weight loss, and fever). Statin therapy should be discontinued in patients suspected of developing interstitial lung disease. In patients with diabetes, use of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (including this product) has been reported to be associated with elevated glycated hemoglobin A1C (HbA1c) 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 mmol/L, BMI >30 kg/m2, elevated triglycerides, and hypertension). Pediatric Patients: Rosuvastatin is limited to one year for pediatric patients aged 10-17 years who are at the stage of secondary sexual maturity according to Tenner staging, as assessed by linear growth (height, weight, and body mass index). After 52 weeks of study treatment, there were no effects on growth, weight, body mass index, or sexual maturation. Clinical trial experience in children and pediatric patients is limited, and the long-term effects of rosuvastatin treatment (greater than one year) in adolescents are unknown. In 52-week clinical trials, creatine kinase elevations greater than 10×ULN and muscle symptoms associated with exercise or increased physical activity were observed more frequently in children and adolescents treated with rosuvastatin than in adult clinical trials (see "Adverse Reactions"). Effects on Driving and Operating Machinery: Studies to determine the effects of this drug on driving and operating machinery have not been conducted. However, based on its pharmacodynamic properties, this drug is unlikely to affect these abilities. The potential for dizziness during treatment should be considered when driving and operating machinery.
