Product Overview
[Drug Name]
Generic Name: Atorvastatin Calcium Tablets
Trade Name: YouLiPing Atorvastatin Calcium Tablets 20mg*7 Tablets
Pinyin Full Code: YouLiPing ATuoFaTaTingGaiPian 20mg*7 Tablets
[Main Ingredients]
Atorvastatin Calcium
[Properties]
This product is a white film-coated tablet that appears white after the film coating is removed.
[Indications/Main Functions]
For the treatment of hypercholesterolemia and combined hyperlipidemia; prevention and treatment of coronary heart disease and stroke
[Specifications]
20mg*7 tablets
[Dosage and Administration]
This product can be swallowed orally orally. It can also be dissolved in an appropriate amount of boiled water and allowed to disperse evenly before oral administration. The usual starting dose is 10mg once daily. The dose adjustment interval should be 4 weeks or longer.
The maximum dose is 80mg once daily. Atorvastatin can be taken at any time of day, regardless of meals. Adverse [Reactions]
1. General: malaise, fever;
2. Digestive System: abdominal discomfort, fever, flatulence, hepatitis, cholestasis;
3. Musculoskeletal System: myalgia, muscle fatigue, neck pain, joint swelling;
4. Nutritional and Metabolic System: elevated transaminases, abnormal liver function tests, elevated alkaline phosphatase, elevated creatine phosphokinase, hyperglycemia;
5. Nervous System: nightmares;
6. Respiratory System: epistaxis;
7. Skin and Appendages: urticaria;
8. Special Senses: blurred vision, tinnitus;
9. Urogenital System: positive for leukocytes in urine.
[Contraindications]
1. Active liver disease, including persistently elevated liver transaminases with unexplained causes.
2. Known hypersensitivity to any of the ingredients in this product.
3. Pregnancy. This product is contraindicated in pregnant women or women of childbearing potential who may become pregnant. This product may cause fetal harm when taken by pregnant women. Serum cholesterol and triglyceride levels are elevated during normal pregnancy.
4. Cholesterol or cholesterol-lowering agents are essential for fetal development. Atherosclerosis is a chronic disease process; therefore, discontinuing lipid-lowering medication during pregnancy in patients with primary hypercholesterolemia has minimal effect on the long-term outcome of atherosclerotic disease. Adequately controlled studies of atorvastatin use in pregnant women are lacking; however, there have been occasional reports of congenital anomalies in fetuses exposed to statins in utero. Rat and rabbit reproduction studies have not observed evidence of teratogenicity with atorvastatin. Lipitor should be prescribed to women of childbearing potential only if they are extremely unlikely to conceive and have been informed of the potential risks. If a patient becomes pregnant while taking this medication, discontinue the drug immediately and consider the potential hazard to the fetus (see [Use in Pregnant and Lactating Women]).
5. Lactating Women: It is unknown whether atorvastatin is excreted in human breast milk; however, other drugs in this class are excreted in breast milk in small amounts. Because statins may have potentially serious adverse reactions in nursing newborns, women taking this drug should not breastfeed.
[Drug Interactions]
During statin therapy, coadministration of the following drugs may increase the risk of myopathy: fibrates, lipid-modifying doses of niacin, cyclosporine, or strong CYP3A4 inhibitors (such as clarithromycin, HIV protease inhibitors, and itraconazole) (see [Precautions], "Skeletal Muscle" and [Pharmacology and Toxicology]). 1. Strong CYP3A4 Inhibitors: Lipitor is metabolized by cytochrome P450 3A4. Coadministration of Lipitor with strong CYP3A4 inhibitors may increase atorvastatin plasma concentrations. The extent of the drug interaction and the potential for potentiation depend on the degree to which the drug affects CYP3A4. 2. Clarithromycin: Coadministration of 80 mg of Lipitor with clarithromycin (500 mg twice daily) significantly increased the atorvastatin AUC compared to Lipitor alone (see [Pharmacology and Toxicology]). Therefore, caution should be exercised when Lipitor is used at a dose of 20 mg in patients taking clarithromycin (see "Skeletal Muscle" and "Dosage and Administration" in the "Precautions" section). 3. Coadministration with protease inhibitors: Compared with Lipitor alone, the AUC of atorvastatin was significantly increased when Lipitor 40 mg was coadministered with ritonavir + saquinavir (400 mg twice daily) or when Lipitor 20 mg was coadministered with lopinavir + ritonavir (400 mg + 100 mg twice daily) (see "Pharmacology and Toxicology"). Therefore, caution should be exercised when Lipitor is used at a dose of 20 mg in patients taking HIV protease inhibitors (see "Skeletal Muscle" and "Dosage and Administration" in the "Precautions" section). 4. Itraconazole: The AUC of atorvastatin is significantly increased when Lipitor 40 mg is co-administered with itraconazole 200 mg (see [Pharmacology and Toxicology]). Therefore, caution should be exercised when Lipitor 20 mg is used in patients taking itraconazole (see "Skeletal Muscle" and [Dosage and Administration] in the [Precautions] section). 5. Grapefruit juice: Contains one or more components that inhibit cytochrome P450 3A4 and can increase atorvastatin plasma concentrations, especially when large amounts of grapefruit juice are consumed (more than 1 serving per day). .2 liters). 6. Cyclosporine: Atorvastatin and its metabolites are substrates of the OATP1B1 transporter. OATP1B1 inhibitors (such as cyclosporine) can increase the bioavailability of atorvastatin. Compared with atorvastatin alone, the combined use of Lipitor 10 mg and cyclosporine 5.2 mg/kg/day significantly increased the AUC of atorvastatin (see [Pharmacology and Toxicology]). If Lipitor and cyclosporine must be used together, the dose of Lipitor should not exceed 10 mg (see [Pharmacology and Toxicology]). [Precautions], "Skeletal Muscle"). 7. Rifampicin and Other Cytochrome P450 3A4 Inducers: Coadministration of Lipitor with cytochrome P450 3A4 inducers (e.g., efavirenz, rifampicin) can result in varying degrees of reduction in atorvastatin plasma concentrations. Due to rifampicin's dual interaction mechanism, delayed administration of Lipitor after rifampicin is associated with a significant decrease in atorvastatin plasma concentrations. Therefore, coadministration of Lipitor and rifampicin is recommended. 8. Digoxin: When multiple doses of Lipitor are used, When Lipitor is coadministered with digoxin, steady-state plasma concentrations of digoxin increase by approximately 20%. Patients taking digoxin should be appropriately monitored. 9. Oral Contraceptives: When coadministered with oral contraceptives, Lipitor increases the area under the concentration-time curve (AUC) of norethindrone and ethinyl estradiol (see [Pharmacology and Toxicology]) by approximately 30% and 20%, respectively. Women taking this product should consider this increase in AUC when choosing an oral contraceptive. 10. Warfarin: Lipitor has no clinically significant effect on prothrombin time in patients receiving long-term warfarin therapy.
[Precautions]
1. Skeletal Muscle: Rare cases of acute renal failure secondary to myoglobinuria due to rhabdomyolysis have been reported with atorvastatin and other statins. A history of renal impairment may be a risk factor for rhabdomyolysis, and such patients require close monitoring for drug effects on skeletal muscle. Like other statins, atorvastatin can occasionally cause myopathy (defined as muscle pain or weakness accompanied by creatine phosphokinase (CPK) levels exceeding 10 times the upper limit of normal). Concomitant use of high-dose atorvastatin with certain medications, such as cyclosporine or strong CYP3A4 inhibitors (such as clarithromycin, itraconazole, and HIV protease inhibitors), may increase the risk of myopathy or rhabdomyolysis. Myopathy should be considered in any patient with diffuse muscle pain, tenderness, or weakness, and/or significant creatine phosphokinase elevations. Patients should be advised to immediately report unexplained muscle pain, tenderness, or weakness, especially if accompanied by malaise or fever. If a significant elevation in creatine phosphokinase levels occurs or myopathy is confirmed/suspected, atorvastatin therapy should be interrupted. The risk of myopathy is increased during treatment with these medications if cyclosporine A, fibrates, erythromycin, clarithromycin, ritonavir plus saquinavir or lopinavir plus ritonavir, niacin, or imidazole antifungals are used concurrently. Physicians considering the combined use of atorvastatin with fibrates, erythromycin, clarithromycin, ritonavir plus saquinavir or lopinavir plus ritonavir, immunosuppressants, imidazole antifungals, or lipid-lowering doses of niacin should carefully weigh the potential benefits and risks and monitor patients carefully for any signs and symptoms of muscle pain, tenderness, or weakness, particularly during the initial months of treatment and during dose increases of any medication. When atorvastatin is used concomitantly with the aforementioned drugs (see [Drug Interactions]), consideration should be given to reducing the initial and maintenance doses of atorvastatin. In this setting, regular creatine phosphokinase testing should be considered, but such monitoring cannot guarantee the prevention of severe myopathy. 2. Liver Function Abnormalities: Like other lipid-lowering therapies, statins can cause abnormalities in liver biochemical parameters. Clinical trial results showed that 0.7% of patients treated with Lipitor experienced persistent elevations in serum transaminases (two or more episodes exceeding three times the upper limit of normal). The incidence of transaminase abnormalities was 0.2%, 0.2%, 0.6%, and 2.3% in patients receiving doses of 10, 20, 40, and 80 mg, respectively. The following findings were observed in patients taking Lipitor in clinical trials: One patient developed jaundice; elevations in liver function tests (LFTs) in the other patients were not associated with jaundice or other clinical signs or symptoms. After dose reduction, drug interruption, or discontinuation, transaminase levels returned to or near pre-treatment levels without sequelae. Of the 30 patients with persistently elevated liver function test values, 18 continued treatment with a reduced Lipitor dose. Liver function tests should be performed before treatment, 12 weeks after the start of treatment, and 12 weeks after a dose increase, and periodically thereafter (e.g., every six months). Liver enzyme abnormalities typically occur within the first three months of Lipitor treatment, and patients with elevated transaminases should be monitored until normalization occurs. If ALT or AST persistently rises by more than three times the upper limit of normal, a dose reduction or discontinuation of Lipitor is recommended. Lipitor should be used with caution in patients who consume alcohol excessively and/or have a history of liver disease. It is contraindicated in patients with active liver disease or persistently elevated transaminases. 3. Endocrine Function: Statins interfere with cholesterol synthesis and theoretically could inhibit adrenal and/or gonadal steroid synthesis. Clinical studies have shown that Lipitor does not reduce basal plasma cortisol concentrations or impair adrenal reserve. There are insufficient case studies on the effects of statins on male fertility, and their effects on the pituitary-gonadal axis in premenopausal women are currently unknown. Statins should be used with caution when combined with drugs that reduce endogenous steroid hormone levels or activity, such as ketoconazole, spironolactone, and cimetidine. Central nervous system toxicity has been reported in a female dog given atorvastatin at 120 mg/kg/day for 3 months, resulting in cerebral hemorrhage. Another female dog, treated with atorvastatin at an increased dose of 280 mg/kg/day for 11 weeks, was sacrificed in a moribund state and also exhibited cerebral hemorrhage and optic nerve vacuolation. A dose of 120 mg/kg body weight, calculated at the maximum human daily dose of 80 mg, results in systemic exposure approximately 16 times the human plasma area under the curve (AUC, 0-24 hours). In a 2-year study, one tonic seizure was observed in two male dogs (one receiving 10 mg/kg/day and the other 120 mg/kg/day). No central nervous system damage was observed in mice and rats following chronic administration for two years at doses up to 400 mg/kg/day and 100 mg/kg/day. Based on the recommended maximum human dose of 80 mg daily, these doses represent 6-11 times (mice) and 8-16 times (rats) the area under the curve (AUC) in humans (0-24). Central nervous system vascular damage, characterized by perivascular hemorrhage, edema, and mononuclear cell infiltration into the perivascular space, has been observed in dogs following administration of other statins. In clinically normal dogs, another drug of the same chemical structure produced dose-dependent optic nerve degeneration (Wallerian degeneration of the retinal-geniculate fibers) at plasma levels approximately 30 times higher than the recommended maximum human dose. The SPARCL (Stroke Prevention with Intensive Cholesterol Lowering) study enrolled 4,731 patients without coronary artery disease who had a stroke or transient ischemic attack within the previous six months and received either Lipitor 80 mg or placebo. A post-hoc analysis of the study showed a higher incidence of hemorrhagic stroke in the Lipitor 80 mg group compared with the placebo group (55 patients [2.3%] vs. 33 patients [1.4%]; HR = 1.68; 95% CI: 1.09-2.59; p = 0.0168). The incidence of fatal hemorrhagic stroke was similar in the atorvastatin and placebo groups (17 and 18 patients, respectively). The incidence of nonfatal hemorrhagic stroke was higher in the atorvastatin group (38 patients, 1.6%) compared with the placebo group (16 patients, 0.7%). The higher incidence of hemorrhagic stroke in the atorvastatin group was associated with certain baseline characteristics of the patients at study entry (including hemorrhagic stroke and lacunar stroke).
[Pediatric Use]
This drug should only be used in children by specialists. Pediatric experience with this drug is limited to a small number of patients (aged 4 to 17 years) with severe lipid disorders, such as homozygous familial hypercholesterolemia.
[Elderly Use]
Use with caution.
[Overdose]
No specific treatment is available for overdose with this drug. In the event of an overdose, patients should receive symptomatic and supportive measures as needed. Because atorvastatin is extensively bound to plasma proteins, hemodialysis does not significantly increase its clearance.
[Pharmacology and Toxicology]
Carcinogenic, teratogenic, and reproductive harm.
