Atorvastatin Calcium Tablets

Clinical Pharmacology 1. Mechanism of Action Lipitor is a selective, competitive inhibitor of HMG-CoA reductase. The role of HMG-CoA is to convert hydroxymethylglutaryl coenzyme A into mevalonate, a precursor of sterols including cholesterol. Clinical, pathological and epidemiological studies have shown that elevated plasma levels of total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C) and apolipoprotein B (apoB) promote the formation of atherosclerosis in humans and are risk factors for cardiovascular disease, while elevated levels of high-density lipoprotein cholesterol are associated with a reduced risk of cardiovascular disease. In animal models, Lipitor reduces plasma cholesterol and lipoprotein levels by inhibiting the synthesis of HMG-CoA reductase and cholesterol in the liver, and enhances the uptake and catabolism of low-density lipoprotein by increasing the number of LDL receptors on the surface of liver cells; Lipitor also reduces low-density lipoprotein production and the number of low-density lipoprotein particles. Lipitor can reduce LDL cholesterol levels in some patients with homozygous familial hypercholesterolemia (FH), for whom other lipid-lowering drugs are generally ineffective. Lipitor reduces total cholesterol, LDL cholesterol, and apolipoprotein B levels in patients with homozygous and heterozygous FH, non-familial hypercholesterolemia, and mixed dyslipidemia. Lipitor also reduces VLDL cholesterol and triglyceride levels, and can increase HDL cholesterol and apolipoprotein A-1 levels. Lipitor reduces total cholesterol, LDL cholesterol, VLDL cholesterol, apolipoprotein B, triglycerides, and non-HDL cholesterol in patients with isolated hypertriglyceridemia, and increases HDL cholesterol levels. Lipitor reduces intermediate-density lipoprotein cholesterol in patients with dyslipidemia of beta. 2. Pharmacodynamics Lipitor and some of its metabolites are pharmacologically active in humans. The liver is the primary site of action and major site for cholesterol synthesis and LDL clearance. The dose rather than the systemic drug concentration is more related to the reduction of LDL cholesterol. Individualized dose should be determined based on the efficacy of the treatment (see [Dosage and Administration]).

The main ingredient of this product is atorvastatin calcium.

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

1. Hypercholesterolemia 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, elevated low-density lipoprotein cholesterol, elevated apolipoprotein B and elevated triglycerides 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 (such as LDL plasma dialysis) or alone (when no other treatment is available) to lower total cholesterol and low-density lipoprotein cholesterol. 2. Coronary heart disease Coronary heart disease or coronary heart disease-related critical illnesses (such as diabetes, symptomatic atherosclerotic disease, etc.) combined with high

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 based on the baseline level of low-density lipoprotein cholesterol, treatment goals, and the patient's treatment effect. The commonly used starting dose is 10 mg once a day. The dose adjustment interval should be 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. (See the instructions for other details)

The following serious adverse reactions are described in detail elsewhere in this manual: Rhabdomyolysis and myopathy (see [Precautions]) Abnormal liver enzymes (see [Precautions]) Clinical adverse reactions (foreign literature) The subjects' conditions are complicated during the implementation of clinical trials, so the incidence of adverse reactions obtained from clinical studies of two different drugs cannot be directly compared, and may not reflect the incidence of adverse reactions in clinical practice. A total of 16,066 patients (atorvastatin n=8755, placebo n=7311, aged from 10 to 93 years old, 39% female; 91% Caucasian, 3% black, 2% Asian, 4% other races) were included in the placebo-controlled clinical trial of atorvastatin calcium. The median treatment period was 53 weeks. Without considering causality, 9.7% and 9.5% of patients in the atorvastatin calcium group and the placebo group, respectively, discontinued the drug due to adverse reactions. The five most common adverse reactions that led to discontinuation of treatment and occurred at a higher rate in the atorvastatin calcium group than in the placebo group were: myalgia (0.7%), diarrhea (0.5%), nausea (0.4%), increased alanine aminotransferase (ALT) (0.4%), and increased other liver enzymes (04%). Regardless of causality, the most common adverse reactions (≥2%) and with an incidence higher than placebo in placebo-controlled trials of atorvastatin calcium (n=8755) were: nasopharyngitis (8.3%), arthralgia (6.9%), diarrhea (6.8%), pain in the limbs (6.0%), and urinary tract infection (5.7%). Table 1 summarizes the adverse reactions (regardless of causality) with an incidence ≥2% and higher than placebo in 8755 patients treated with atorvastatin calcium in 17 placebo-controlled trials (see the instructions for other details)

1. Active liver disease, which may include unexplained persistent elevation of liver transaminases. 2. Known allergy to any ingredient in this product. 3. Pregnancy. This product is prohibited for pregnant women or women of childbearing age who may become pregnant. Pregnant women may cause harm to the fetus when taking this product. In normal pregnancy, serum cholesterol and triglyceride levels in the body are elevated, and cholesterol or cholesterol derivatives are essential substances for fetal development. Atherosclerosis is a chronic disease process, so the discontinuation of lipid-lowering drug treatment during pregnancy in patients with primary hypercholesterolemia has little effect on the long-term outcome of atherosclerotic disease. There is currently a lack of sufficient controlled studies on pregnant women taking atorvastatin; however, occasional reports have observed that congenital abnormalities of the fetus may occur when exposed to statins in utero. Rat and rabbit reproduction studies have not observed evidence that atorvastatin is teratogenic. For women of childbearing age, only those who are extremely unlikely to become pregnant and have been informed of the potential hazards can be prescribed Lipitor. If a patient becomes pregnant during medication, the drug should be discontinued immediately, and the potential harm of the drug to the fetus should be considered (see [Use of drugs in pregnant and lactating women]). 4. It is not known whether atorvastatin can be secreted from human breast milk during lactation; however, other drugs of this type can be secreted into breast milk in small amounts. Because statins may have potentially serious adverse reactions on breastfed newborns, women taking this product are prohibited from breastfeeding (see [Use of atorvastatin in pregnant and lactating women]).

Precautions for children: This product should only be used in children by specialists. The 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. There is no safety data on the growth and development of this population. Precautions for pregnancy and lactation: Pregnancy classification X1. Pregnant women or women of childbearing age who may become pregnant are prohibited from taking Lipitor. 1.1 Serum cholesterol and triglyceride levels in the body are elevated during normal pregnancy, and cholesterol or cholesterol derivatives are essential substances for fetal development. Atherosclerosis is a chronic disease process, so the discontinuation of lipid-lowering drug treatment during pregnancy in patients with primary hypercholesterolemia has little effect on the long-term outcome of atherosclerotic disease. 1.2 There is currently a lack of adequate controlled studies on the use of Lipitor during pregnancy. There are rare reports of congenital abnormalities caused by intrauterine exposure to statins. A follow-up study of approximately 100 pregnant women exposed to other statins found that the incidence of congenital anomalies, spontaneous abortion, and fetal death/stillbirth did not exceed the expected values for the general population, but this study could only exclude a risk of 3-4 times the baseline incidence of congenital anomalies. At the same time, 89% of the patients started taking the drug before pregnancy but stopped taking it within 3 months after being informed of pregnancy. 1.3 Atorvastatin crosses the placenta of rats and reaches drug levels in the fetal liver that are equivalent to maternal plasma. Atorvastatin did not produce teratogenic effects when dosed up to 300 mg/kg/day in rats and 100 mg/kg/day in rabbits. Based on body surface area (mg/m2), these doses are approximately 30 times (rats) or 20 times (rabbits) the human exposure (see [Contraindications], Pregnancy). 1.4 In one study, rats were dosed with 20, 100, or 225 mg/kg/day from gestation day 7 to lactation day 21 (weaning). The survival of pups at birth, neonatal, weaning, and maturity was reduced when the mothers were dosed with 225 mg/kg/day. The weight of pups on days 4 and 21 was reduced when the mothers were dosed with 100 mg/kg/day; the weight of pups at birth, days 4, 21, and 91 was reduced when the mothers were dosed with 225 mg/kg/day; the development of pups was delayed (Rothel's syndrome occurred at 100 mg/kg/day, while auditory startle response occurred at 225 mg/kg/day; auricular separation and palpebral fissures occurred at 225 mg/kg/day). These doses are equivalent to 6 times (100 mg/kg/day) and 22 times (225 mg/kg/day) the area under the curve of humans taking 80 mg daily. 1.5 Statins may harm the fetus when given to pregnant women. Women of childbearing age should only take this product when the possibility of pregnancy is extremely small and they have been informed of the potential risks of the drug to pregnant women. Once a woman taking this product becomes pregnant, she should stop taking it immediately and be informed of the potential risks to the fetus. There is a lack of known clinical benefits to continuing the drug during pregnancy. 2. It is not clear whether atorvastatin is secreted through human milk in lactating women, but another similar drug can be secreted into breast milk in small amounts. The atorvastatin drug concentrations in the plasma and liver of lactating rat pups are 50% and 40% of the drug concentrations in breast milk, respectively. The drug concentration level in animal milk may not accurately reflect the drug concentration level in human milk, because another similar drug can be secreted through human milk. At the same time, statins may cause serious adverse reactions to newborns receiving breastfeeding, so mothers taking this product should not breastfeed (see [Contraindications]). Elderly precautions: Among the 39,828 patients taking Lipitor in clinical studies, 15,813 (40%) were 65 years old and 2,800 (7%) were 75 years old. There is no difference in overall safety and efficacy between these two populations and younger subjects. Other clinical experience reports also show no difference between the elderly and younger populations. However, it cannot be ruled out that some elderly patients are more sensitive to drugs, and advanced age (ge; 65 years old) is a susceptibility factor for myopathy, so Lipitor should be used with caution in the elderly.

Drugs that may interact with statins include: HIV protease inhibitors (such as lopinavir, darunavir, ritonavir), azole antifungal drugs (such as itraconazole, ketoconazole), macrolide anti-infective drugs (such as erythromycin, clarithromycin, qinlimycin), fibrate lipid-lowering drugs (such as gemfibrozil, bezafibrate), niacin, nefazodone, cyclosporine, amiodarone, diltiazem, fudicinic acid, etc. During statin treatment, the risk of myopathy may be increased when used in combination with the following drugs, such as: fibric acid derivatives, lipid-lowering doses of niacin, cyclosporine, or strong CYP3A4 inhibitors (such as clarithromycin, HIV protease inhibitors and itraconazole) (see skeletal muscle and [pharmacology and toxicology] in the [Precautions] section). (For other details, see the instructions)

Keep tightly closed.

20mg [calculated as atorvastatin (C33H35FN2O5)]

36 months.

Beijing Jialin Pharmaceutical Co., Ltd.

• Founded in:

  1977-08-05

• Address:

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

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  911101051016610948

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  30.5 million yuan

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