Pitavastatin Calcium Dispersible Tablets

Pharmacology Pitavastatin calcium inhibits cholesterol synthesis in the liver by antagonizing HMG-CoA reductase, the rate-limiting enzyme in the cholesterol biosynthesis pathway. It promotes the expression of low-density lipoprotein (LDL) receptors in the liver and the entry of LDL from the blood into the liver, thereby reducing total cholesterol. In addition, it continuously inhibits the biosynthesis of cholesterol in the liver, reduces the secretion of very low-density lipoprotein (VLDL) into the blood, and reduces triglycerides in plasma. 1. Inhibition of HMG-CoA reductase In vitro rat liver microsome tests showed that pitavastatin calcium has an antagonistic effect on HMG-CoA reductase, with an IC50 of 6.8nM. 2. Inhibition of cholesterol synthesis In vitro tests conducted on human liver cancer cell line HepG2 showed that pitavastatin calcium has an inhibitory effect on cholesterol synthesis, and it is concentration-dependent. Oral administration tests in rats showed that pitavastatin calcium can selectively inhibit cholesterol synthesis in the liver. 3. Reduce plasma lipids Oral administration tests in dogs and woodchucks showed that pitavastatin calcium can reduce plasma total cholesterol and serum triglycerides. 4. Inhibit the accumulation of blood lipids and intimal thickening. In vitro experiments with mouse macrophage cell lines showed that pitavastatin calcium can inhibit the accumulation of cholesterol esters. Oral administration of the drug to rabbits in the carotid artery rub model showed that the drug can inhibit the thickening of the vascular intima. 5. Mechanism of action (1) Promote the expression of LDL receptors. In vitro experiments with human liver cancer cell line HepG2 showed that pitavastatin calcium can promote the expression of LDL receptor mRNA in HepG2 cells, increase the binding amount, entry amount and decomposition of ApoB of LDL. Oral administration experiments in woodchucks showed that it has a promoting effect on the expression of LDL receptors, and is dose-dependent. (2) Reduce the secretion of VLDL. Oral administration experiments in woodchucks showed that pitavastatin calcium can significantly reduce the secretion of VLDL-triglycerides.

Pitavastatin calcium. Molecular weight: C50H46CaF2N2O8

Off-white tablets, off-white after removing the coating.

For the treatment of hypercholesterolemia and familial hypercholesterolemia Note: 1. Before using this drug, you should conduct a full examination and use it only after you are diagnosed with hypercholesterolemia or familial hypercholesterolemia. 2. There is a lack of treatment experience for patients with homozygous familial hypercholesterolemia. This drug can only be used as an auxiliary drug for non-drug therapy of low-density lipoprotein after clinically determining that the treatment is ineffective.

Usually, adults take 1-2 mg of pitavastatin calcium once a day, orally after meals. The dosage can be increased or decreased according to age and condition. When the low-density lipoprotein value does not decrease significantly, you can consider increasing the dosage. The maximum daily dosage is 4 mg. Note: 1. The first dose for patients with liver disorders starts with 1 mg/day, and the maximum daily dosage is 2 mg. 2. Since rhabdomyolysis may occur with increasing dosage, when increasing the dosage, pay attention to whether the CK value increases, whether myoglobin appears in the urine, muscle pain or fatigue and other early symptoms of rhabdomyolysis.

197 (22.2%) of the 886 subjects in the clinical trial experienced adverse reactions. A total of 50 subjects (5.6%) experienced subjective and subjective symptoms, mainly abdominal pain, drug rash, fatigue, numbness, itching, etc. Abnormalities related to clinical examination values occurred in 167 subjects (18.8%), mainly increased γ-GTP, increased CK (CPK), increased serum ALT (GPT), and increased serum AST (GOT). 1. Major adverse reactions (1) Rhabdomyolysis (frequency unknown): Rhabdomyolysis is characterized by muscle pain, fatigue, increased CK (CPK), increased myoglobin in blood and urine, etc., and is accompanied by acute renal impairment. Therefore, when these symptoms occur, the drug administration is immediately stopped. (2) Myopathy (frequency unknown): Because it can cause myopathy, the drug administration is stopped when systemic muscle pain, muscle tenderness, and significant CK (CPK) increase occur. (3) Liver function impairment (frequency unknown), jaundice (frequency unknown): Since this drug may cause liver function impairment and jaundice accompanied by a significant increase in AST (GOT) and ALT (GPT), regular liver function tests are required and administration should be stopped immediately if abnormalities are found.

1. Patients with a history of allergy to the ingredients contained in this drug; 2. Patients with severe liver dysfunction or bile duct occlusion (when these patients take this drug, the blood concentration of the drug will increase, the chance of adverse reactions will be relatively high, and the liver disease may be aggravated) 3. Patients taking cyclosporine (when these patients take this drug, the blood concentration of the drug will increase, the chance of adverse reactions will be relatively high. And there may be rhabdomyolysis) 4. Pregnant or preparing to become pregnant or breastfeeding women 5. The following patients are prohibited from using this drug in principle, but it can be used with caution when necessary: Patients with abnormal renal function in clinical examinations taking this drug and phenoxyacetic acid drugs at the same time can only be used when necessary.

Precautions for children: The safety of the drug for children has not been established (no experience of use). Precautions for pregnancy and lactation: 1. Pregnant women or women who are preparing to become pregnant are prohibited from using it. Safety is not yet determined. Perinatal and lactation tests in rats showed that pregnant rats in the dose group of 1 mg/kg or more died before or after delivery. The results of the teratogenic sensitive period test in rabbits showed that pregnant rabbits in the dose group of 0.3 mg/kg or more died. There are reports that when rats are given a large amount of other HMG-CoA reductase inhibitors, fetal rats have skeletal deformities. There are also reports that pregnant women who take other HMG-CoA reductase inhibitors in the first 3 months of pregnancy have congenital malformations in their fetuses. 2. Women who are breastfeeding are prohibited from using it. The drug is secreted in rat milk. Precautions for the elderly: Generally speaking, the physiological functions of the elderly decline, so when adverse reactions occur, you should pay attention to reducing the dosage. Reports show that the elderly are prone to rhabdomyolysis.

Drug interactions may occur if used with other drugs. Please consult your doctor or pharmacist for details.

Keep sealed.

1mg

24 months

Zhejiang Jingxin Pharmaceutical Co., Ltd.

• Founded in:

  1999-02-13

• Address:

  No. 800, Xinchang Avenue East Road, Yulin Street, Xinchang County, Zhejiang Province

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  91330000704503984N

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  861.02914 million yuan

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