Product Overview
[Drug Name]
Generic Name: Atorvastatin Calcium Tablets
Trade Name: Taiyou Atorvastatin Calcium Tablets (10mg x 7 tablets)
[Main Ingredients]
The main ingredient of this product is atorvastatin calcium.
[Indications/Main Functions]
This product is indicated for the treatment of elevated total cholesterol, LDL cholesterol, apolipoprotein B, and triglycerides in patients with primary hypercholesterolemia, including familial hypercholesterolemia (heterozygous) or mixed hyperlipidemia (equivalent to Fredrickson classification types IIa and IIb), who are unsatisfactory responders to dietary therapy and other non-drug treatments. In patients with homozygous familial hypercholesterolemia, atorvastatin calcium can be used in combination with other lipid-lowering therapies or alone (when other treatment options are unavailable) to lower total cholesterol and LDL cholesterol.
[Specifications]
10mg*7 tablets
[Dosage and Administration]
Patients should follow a standard low-cholesterol diet before starting treatment with this drug and maintain a healthy diet throughout treatment. The dose should be individually adjusted based on baseline LDL cholesterol levels, treatment goals, and the patient's response to treatment. The usual starting dose is 10 mg once daily. Dose adjustments should be made every four weeks or longer. The maximum dose is 80 mg once daily. Atorvastatin can be taken once daily at any time of day, regardless of mealtimes. For the treatment of primary and combined hyperlipidemia: Lipid levels are controlled in most patients with atorvastatin calcium 10 mg once daily. Significant efficacy is seen within two weeks of treatment, with maximum efficacy achieved within four weeks. Efficacy is maintained with long-term treatment. For the treatment of heterozygous familial hypercholesterolemia: Patients should start with an initial dose of 10 mg/day. Dosage should be individualized and titrated to 40 mg/day every four weeks. If satisfactory efficacy is still not achieved, the dose can be adjusted to a maximum of 80 mg/day or 40 mg once daily in combination with a bile acid sequestrant. Treatment of homozygous familial hypercholesterolemia: In a charitable study of 64 patients, 46 of whom had LDL receptor information, the average LDL-C reduction in these 46 patients was 21%. The dose of this drug can be increased to 80 mg/day. For patients with homozygous familial hypercholesterolemia, the recommended dose is 10-80 mg/day. Atorvastatin calcium should be used as an adjunct to other lipid-lowering therapies (such as LDL plasma dialysis). Alternatively, this drug can be used alone when these treatments are unavailable. Dosage for patients with renal impairment: Renal disease does not affect the plasma concentration of this drug or its lipid-lowering effect, so no dose adjustment is required.
[Adverse Reactions]
1. The most common adverse reaction to this product is gastrointestinal discomfort; others include headache, rash, dizziness, blurred vision, and taste disturbance. 2. It may occasionally cause a reversible elevation in serum aminotransferases. Therefore, liver function should be monitored. 3. Rare adverse reactions include impotence and insomnia. 4. Rare adverse reactions include myositis, myalgia, and rhabdomyolysis, manifesting as muscle pain, fatigue, fever, and accompanied by elevated serum creatine phosphokinase and myoglobinuria. Rhabdomyolysis can lead to renal failure, but this is rare. 5. Concomitant use of this product with immunosuppressants, folic acid derivatives, niacin, gemfibrozil, and erythromycin may increase the risk of myopathy. 6. Hepatitis, pancreatitis, and allergic reactions such as angioedema have been reported.
[Contraindications]
1. Hypersensitivity to this product. 2. Active liver disease or persistent elevation of serum aminotransferases for unknown reasons. 3. Pregnant women and peripartum women.
[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 in patients taking clarithromycin when Lipitor doses > 20 mg are used (see "Skeletal Muscle" in the [Precautions] section and [Dosage and Administration]). 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 in patients taking HIV protease inhibitors when Lipitor doses > 20 mg are used (see "Skeletal Muscle" in the [Precautions] section and [Dosage and Administration]). 4. Itraconazole: The AUC of atorvastatin was significantly increased when Lipitor 40 mg was coadministered with itraconazole 200 mg (see [Pharmacology and Toxicology]). Therefore, caution should be exercised in patients taking itraconazole when Lipitor doses >20 mg are used (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 1.2 liters per day). 6. Cyclosporine: Atorvastatin and its metabolites are substrates for 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 coadministration of Lipitor and cyclosporine is necessary, the Lipitor dose should not exceed 10 mg (see "Skeletal Muscle" in the "Precautions" section). 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 decreases in atorvastatin plasma concentrations. Due to the dual interaction mechanism of rifampicin, 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 coadministered with digoxin, steady-state plasma concentrations of digoxin increase by approximately 20%. Patients taking digoxin should be appropriately monitored. 9. Oral Contraceptives: Coadministration of Lipitor with oral contraceptives increases the area under the concentration-time curve (AUC) of quinolones and ethinyl estradiol (see [Pharmacology and Toxicology]) by approximately 30% and 20%, respectively. This increase in AUC should be considered when choosing an oral contraceptive for women taking this product. 10. Warfarin: Lipitor has no clinically significant effect on prothrombin time in patients receiving long-term warfarin therapy.
[Precautions]
1. Liver Effects: Liver function tests should be performed before initiating treatment and regularly reviewed. Patients should have their liver function checked if they develop any symptoms or signs suggestive of liver damage. Patients with elevated transaminase levels should be monitored until they return to normal. If transaminase levels persist exceeding 3 times the normal value, dose reduction or discontinuation of this drug is recommended (see [Adverse Reactions]). This drug should be used with caution in patients who consume excessive alcohol and/or have a history of liver disease. 2. Skeletal Muscle Effects: Like other HMG-CoA reductase inhibitors, atorvastatin may rarely affect skeletal muscle, causing myalgia, myositis, and myopathy, which may progress to life-threatening rhabdomyolysis, manifested by markedly elevated CPK (greater than 10 times the upper limit of normal), myosinemia, and myoglobulinuria, leading to renal failure.
