Atorvastatin Calcium Tablets

Atorvastatin is a selective, competitive inhibitor of HMG-CoA reductase, a rate-limiting enzyme that converts 3-hydroxy-3-methyl-glutaryl-CoA to mevalonic acid, a precursor of sterols including cholesterol. Triglycerides and cholesterol are combined in the liver to form very low-density lipoprotein cholesterol (VLDL-C) and released into the plasma for further transport to peripheral tissues. Low-density lipoprotein cholesterol (LDL-C) is formed from very low-density lipoprotein cholesterol (VLDL) and is mainly metabolized by receptors for high-affinity low-density lipoprotein cholesterol (LDL-C). Atorvastatin reduces plasma cholesterol and serum lipoprotein concentrations by inhibiting HMG-CoA reductase and cholesterol biosynthesis in the liver, and by increasing LDL receptors on the surface of liver cells to enhance LDL uptake and metabolism. Atorvastatin reduces LDL cholesterol production and the number of LDL cholesterol particles. Atorvastatin leads to a significant and sustained increase in LDL-C receptor activity, which in turn leads to beneficial changes in the mass of circulating LDL-C particles. Atorvastatin is effective in lowering LDL-C levels in patients with homozygous familial hypercholesterolemia, a group of patients for whom lipid-lowering drugs are generally ineffective.

The main ingredient of this product is atorvastatin calcium, and its chemical name is: EP,-(R', R')]-2-(4-fluorophenyl)-B·6-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(anilino)yl]-1-hydrogen-pyrrole-1-heptanoic acid calcium trihydrate.

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

Patients with primary hypercholesterolemia, including familial hypercholesterolemia (heterozygous type) or mixed hyperlipidemia (equivalent to type IIa and IIb of Fredrickson classification), can use this product to treat elevated total cholesterol (TC), elevated low-density lipoprotein cholesterol (LDL-C), elevated apolipoprotein B (ApoB) and elevated triglycerides (TG) if dietary therapy and other non-drug treatments are unsatisfactory. In patients with homozygous familial hypercholesterolemia, atorvastatin calcium can be used in combination with other lipid-lowering therapies or alone (when no other treatment is available) to reduce total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C).

1. Before starting treatment with this product, patients should follow a standard low-cholesterol diet and maintain a reasonable diet throughout the treatment period. The dose should be adjusted individually according to the baseline level of low-density lipoprotein cholesterol, the treatment goal and the patient's treatment effect. 2. The commonly used starting dose is 10 mg, once a day. The dose adjustment time is 4 weeks or longer. The maximum dose of this product is 80 mg, once a day. The daily dose of atorvastatin can be taken once at any time of the day and is not affected by meals. 3. For patients with confirmed coronary heart disease or other patients with increased risk of ischemic events, the treatment goal is low-density lipoprotein cholesterol <3mmol/L or 115mg/dL and total cholesterol <5mmol/L or 190mg/dL (Excerpt from "Prevention and Treatment of Coronary Heart Disease in Clinical Practice: The Second Joint Recommendation for the Prevention of Coronary Artery Disease in Europe" in the Journal of Atherosclerosis, Issue 140, 1998, pp. 199-270). 4. Treatment of primary hypercholesterolemia and mixed hyperlipidemia Most patients can control their blood lipid levels by taking atorvastatin 10 mg once a day. Significant therapeutic effects can be seen within 2 weeks of treatment, and the maximum therapeutic effect can be seen within 4 weeks of treatment. Long-term treatment can maintain the therapeutic effect. 5. The initial dose for patients with heterozygous familial hypercholesterolemia is 10 mg per day. The principle of individualized dosage should be followed and the dose should be gradually adjusted to 40 mg per day every 4 weeks. If satisfactory therapeutic effects are still not achieved, the dose can be adjusted to the maximum dose of 80 mg per day or 40 mg per day of this product can be used in combination with bile acid crab mixture. 6. Treatment of homozygous familial hypercholesterolemia In a charitable drug study involving 64 patients, 46 of them had corresponding LDL receptor information. The average low-density lipoprotein cholesterol of these 46 patients decreased by 21%. The dose of this product can be increased to 80 mg per day. For patients with homozygous familial hypercholesterolemia, the recommended dose of this product is 10-80 mg per day. Atorvastatin should be used as an adjunct to other lipid-lowering treatments (such as LDL plasma dialysis). Or when these treatment conditions are unavailable, this product can be used alone. 7. Dosage for patients with renal insufficiency Renal disease will not affect the plasma concentration of this product, nor its lipid-lowering effect. Therefore, there is no need to adjust the dose.

1. The most common adverse reactions of this product are constipation, flatulence, dyspepsia and abdominal pain, which usually ease after continued medication. 2. Less than 2% of patients in clinical trials discontinued treatment due to adverse reactions related to this product. 3. As usual, the estimated incidence of adverse events is ranked as follows: common (1/100, 1/10); uncommon (1/1000, 1/100); rare (1/10000, 1/1000); very rare (1/10000). 4. Based on the data of clinical studies and extensive post-marketing experience, the adverse events of this product are as follows. 5. Gastrointestinal abnormalities Common: constipation, flatulence, dyspepsia, nausea, diarrhea. Uncommon: anorexia, vomiting. 6. Blood and lymphatic system abnormalities Uncommon: thrombocytopenia. 7. Immune system abnormalities Common: allergic reactions. Endocrine disorders Uncommon: alopecia, hyperglycemia, hypoglycemia, pancreatitis. 8. Mental common: insomnia. Uncommon: amnesia. 9. Nervous system abnormalities Common: headache, dizziness, paresthesia, dysesthesia. Uncommon: peripheral neuropathy. 10. Hepatobiliary abnormalities Rare: hepatitis, cholestatic jaundice. 11. Skin/limbs Common: rash, pruritus. Uncommon: urticaria. Very rare: angioedema, bullous rash (including erythema multiforme, Stevens-Johnson syndrome and toxic epidermolysis). 12. Ear-labyrinth abnormalities Uncommon: tinnitus. 13. Musculoskeletal abnormalities Common: myalgia, arthralgia. Uncommon: myopathy. Rare: myositis, rhabdomyolysis. 14. Reproductive system abnormalities Uncommon: impotence. 15. General abnormalities: Common: asthenia, chest pain, back pain, peripheral edema. Uncommon: malaise, weight gain. 16. Studies As with other HMG-CoA reductase inhibitors, patients taking this product have been reported to have elevated transaminases. However, these changes are usually mild, transient, and do not require interruption of treatment. The incidence of clinically significant increases in serum aminotransferases (3 times the upper limit of normal) was 0.8% in patients treated with this product. These changes in all patients were dose-related and reversible. Similar to HMG-CoA reductase inhibitors in other clinical trials, 2.5% of patients taking this product had increases in serum creatine phosphokinase (CPK) greater than 3 times the upper limit of normal. 0.4% of patients taking this product had increases in CPK greater than 10 times the upper limit of normal (see [Precautions]).

This product is contraindicated for those who are allergic to any of the ingredients contained in this product. This product is contraindicated for patients with active liver disease, patients with serum transaminase that continues to rise more than 3 times the upper limit of normal and the cause is unknown, patients with myopathy, pregnant women, lactating women, and any women of childbearing age who have not taken appropriate contraceptive measures.

Precautions for children: The use of this product in children should be determined by a specialist. The therapeutic experience of this product in children is limited to a small number of patients (4 to 17 years old) with severe lipid disorders such as homozygous familial hypercholesterolemia. The recommended starting dose of this product in this patient population is 10 mg/day. Depending on the patient's response and tolerance, the dose can be increased to 80 mg per day. There is no safety data on the growth and development of this population. Precautions for pregnancy and lactation: Atorvastatin calcium tablets are contraindicated for pregnant and lactating women. Women of childbearing age should take appropriate contraceptive measures. The safety of atorvastatin for pregnant and lactating women has not been confirmed. Animal experiments have confirmed that HMG-CoA reductase inhibitors may affect the growth and development of embryos and infants. When taking atorvastatin at a dose exceeding 20 mg/kg/day (equivalent to the clinical human dose), the offspring of rats are delayed in development and the survival rate after birth is reduced. The concentrations of atorvastatin and its active metabolites in rat plasma are the same as those in their milk. It is not clear whether the drug and its active metabolites are secreted in human milk. Note for the elderly: When the recommended dose of atorvastatin is used in elderly people over 70 years old, its efficacy and safety are no different from those in the general population.

1. When statins are used in combination with cyclosporine, fibric acid derivatives, macrolide antibiotics (including erythromycin), conazole antifungal drugs or niacin, the risk of myopathy increases. In extremely rare cases, rhabdomyolysis may occur, accompanied by myoglobulinuria and subsequent renal insufficiency. Therefore, the risk-benefit ratio of use should be carefully weighed (see [Precautions]). 2. Cytochrome P4503A4 inhibitor Atorvastatin is metabolized by cytochrome P4503A4. When this product is used in combination with cytochrome P4503A4 inhibitors (macrolide antibiotics such as cyclosporine, erythromycin and clarithromycin, conazole antifungal drugs such as itraconazole and HIV protease inhibitors), drug interactions may occur, and combined use leads to increased plasma concentrations of atorvastatin. Therefore, special attention should be paid when atorvastatin is used in combination with the above drugs (see [Precautions]). P-glycoprotein inhibitors: Atorvastatin and atorvastatin metabolites are P-glycoprotein substrates. P-glycoprotein inhibitors (such as cyclosporine) can increase the bioavailability of atorvastatin. Erythromycin, clarithromycin: The plasma concentration of atorvastatin increased when atorvastatin 10 mg once daily was combined with erythromycin (500 mg, 4 times a day) or clarithromycin (500 mg, 2 times a day), the inhibitors of cytochrome P4503A4. Clarithromycin increased the maximum plasma concentration (Cmax) and area under the concentration-time curve (AUC) of atorvastatin by 56% and 80%, respectively. Itraconazole: The combined use of atorvastatin 40 mg and itraconazole 200 mg/day can lead to a 3-fold increase in the AUC of the former. Protease inhibitors: When protease inhibitors are used in combination with atorvastatin, the plasma concentration of atorvastatin is increased. Grapefruit juice: Contains one or more ingredients that inhibit cytochrome P4503A4, which can increase the plasma concentration of drugs metabolized by this enzyme. Intake of 240 ml of grapefruit juice increased the AUC of atorvastatin by 37% and decreased the AUC of the active para-hydroxy metabolite by 20.4%. However, intake of large amounts of grapefruit juice (more than 1.2 liters per day for 5 consecutive days) increased the AUC of atorvastatin and active (atorvastatin and metabolites) HMG-CoA reductase inhibitor by 2.5 times and 1.3 times, respectively. Therefore, it is recommended that patients taking atorvastatin should not simultaneously ingest large amounts of grapefruit juice. 3. Cytochrome P450 3A4 inducers The effect of cytochrome P450 3A4 inducers (rifampicin, phenytoin) on this product is unknown. The possible interaction between this product and other substrates of this isoenzyme is unknown, but attention should be paid to drugs with narrow therapeutic indications such as class III antiarrhythmic drugs (amiodarone). 4. Other combined therapies Gemfibrozil/fibric acid derivatives: Fibric acid derivatives may increase the risk of atorvastatin-induced myopathy. According to the results of in vitro studies, gemfibrozil inhibits the glucuronide metabolic pathway of atorvastatin, which may lead to increased plasma concentrations of atorvastatin (see [Precautions]). Digoxin: When 10 mg of this product is co-administered with multiple doses of digoxin, the steady-state plasma concentration of digoxin is not affected. When 80 mg of this product is co-administered once daily with digoxin, the digoxin concentration increases by about 20%. This is due to the inhibition of the cell membrane transport protein P-glycoprotein. Patients taking digoxin should be appropriately monitored. Oral contraceptives: When this product is used in combination with oral contraceptives, the plasma concentrations of norethindrone and ethinyl estradiol increase. When choosing oral contraceptives, you should pay attention to their increased concentrations. Colestipol (cholestyramine): When colestipol is used in combination with this product, the plasma concentrations of atorvastatin and its active metabolites decrease by about 25%, but the lipid-lowering effect of the two drugs combined is greater than that of a single drug. Antacids: When this product is used in combination with an oral antacid suspension containing magnesium hydroxide and aluminum hydroxide, the plasma concentration of atorvastatin and its active metabolites decreases by about 35%; however, its effect on lowering low-density lipoprotein cholesterol is not affected. Warfarin: When this product is used in combination with warfarin, the prothrombin time decreases slightly in the first few days and returns to normal after 15 days. Even so, patients taking warfarin should be closely monitored when this product is added. Amitpyrine: No effect on the clearance of amitpyrine was found when multiple doses of this product were used in combination with amitpyrine. Cimetidine: Studies on the interaction between this product and cimetidine did not find an interaction between the two. Amlodipine: The pharmacokinetics of atorvastatin at steady-state concentrations were not changed when atorvastatin 80 mg and amlodipine 10 mg were used in combination. Others: In clinical trials of this product used in combination with antihypertensive or hypoglycemic drugs, no clinically significant drug interactions were found. 5. Effects on driving and operating abilities: There are currently no adverse event reports indicating that taking this drug will have any effects on the patient's driving ability and ability to operate dangerous machinery.

Keep away from light and store in sealed container.

10mg (calculated as C33H35FN2O5)

36 months.

Beijing Jialin Pharmaceutical Co., Ltd.

• Founded in:

  1977-08-05

• Address:

  No. 2 Jiuxianqiao Road, Dashanzi, Dongzhimenwai, Chaoyang District, Beijing

• Tax NO.:

  911101051016610948

• Registered Funds:

  30.5 million yuan

• Website:

  Log in to view

• Email:

  Log in to view