Fenofibrate Capsules (Ⅱ)

[Pharmacology and Toxicology] This product is a clofibric acid derivative lipid regulating drug. It reduces blood low-density lipoprotein, cholesterol and triglycerides by inhibiting the production of very low-density lipoprotein and triglycerides and increasing their catabolism at the same time; it also increases the production of apolipoprotein A1 and A11, thereby increasing high-density lipoprotein. This product also has the effect of reducing blood uric acid in normal people and patients with hyperuricemia. Animal experiments have shown that fenofibrate is teratogenic and carcinogenic. [Pharmacokinetics] After oral administration, this product is well absorbed by the gastrointestinal tract, and taking it with food can increase the absorption of fenofibrate. The blood concentration reaches its peak about 4 to 7 hours after oral administration. The absorption half-life and elimination half-life after a single oral dose are 4.9 hours and 26.6 hours, respectively, and the apparent distribution volume is 0.9L/kg; the half-life b after continuous treatment is 21.7 hours. The plasma protein binding rate is about 99%, and no accumulation is found after multiple doses. After absorption, it is mostly distributed in the liver, kidneys, and intestines, followed by the lungs, heart, and adrenal glands, with a small amount in the testicles, spleen, and skin. It is metabolized in the liver and kidney tissues, undergoing carboxyl reduction and glucuronidation, with glucuronidation products accounting for the majority of metabolites. After radioactive labeling, about 60% of the metabolites are excreted through the kidneys, and 25% of the metabolites are excreted through the stool. The elimination half-life of this product is 20 hours, so it can be administered once a day. Studies have shown that the clearance rate of this product is significantly reduced in patients with severe renal insufficiency, and long-term use can cause accumulation.

The main ingredient of this product is fenofibrate. Its chemical name is isopropyl 2-methyl-2-[4(4-chlorobenzoyl)phenoxy]propionate.

This product is a capsule, and the contents are white or off-white crystalline powder.

This product is used to treat hyperlipidemia in adults who have not responded well to dietary control therapy. Its effect on lowering triglycerides and mixed hyperlipidemia is more obvious than that of cholesterol. However, this product cannot completely replace dietary control therapy and can only be used as an auxiliary treatment based on dietary control.

The usual dosage for adults is 0.1g capsules 3 times a day, and the maintenance dosage is 0.1g each time, 1-2 times a day. To reduce stomach discomfort, it can be taken with food; the dosage should be reduced for patients with renal insufficiency and the elderly; the drug should be discontinued after 2 months of treatment if there is no effect.

The incidence rate is about 2% to 15%. Gastrointestinal reactions include abdominal discomfort, diarrhea, and constipation, which are the most common (about 5%); rash (2%); adverse reactions of the nervous system include fatigue, headache, loss of libido, impotence, dizziness, and insomnia (about 3% to 4%); this product is a derivative of clofibric acid, which may cause myositis, myopathy, and rhabdomyolysis syndrome, leading to increased blood creatine phosphokinase; rhabdomyolysis occurs, mainly manifested as myalgia combined with increased blood creatine phosphokinase, myoglobinuria, and can lead to renal failure, but it is rare; in patients with nephrotic syndrome and other renal damage that lead to decreased blood albumin or patients with hyperthyroidism, the risk of myopathy increases. (about 1%); there is a tendency to increase gallstones, which can cause gallbladder disease and even require surgery; mild to moderate hematological changes may occur in the early stages of treatment, such as decreased hemoglobin, hematocrit, and leukocytes. Occasionally, blood aminotransferases increase, including alanine and aspartate aminotransferases.

It is contraindicated for patients who are allergic to fenofibrate, patients with a history of gallbladder disease or cholelithiasis, as this product can increase the excretion of cholesterol into bile, thus causing gallstones. It is contraindicated for patients with severe renal insufficiency, hepatic insufficiency, primary biliary cirrhosis, or persistent abnormal liver function of unknown cause.

Precautions for children: Children are prohibited from using it. Precautions for pregnancy and lactation: Pregnancy - Animal test results show no teratogenic effects. - So far, clinical teratogenicity and embryotoxicity have not been found. However, the follow-up of fenofibrate use during pregnancy is not sufficient to exclude any danger, so it should be prohibited for pregnant women in general. - Fibrates are not used in pregnant women, except when dietary control cannot effectively reduce high triglycerides (10g/L) and increases the risk of acute pancreatitis in the mother. There is currently no data that fenofibrate can enter breast milk during lactation. However, it is prohibited during lactation. Precautions for the elderly: It is recommended to use the normal adult dose, and the dose can be reduced if there is renal impairment.

This product should be used with caution with HMG-CoA reductase inhibitors, such as pravastatin, fluvastatin, simvastatin, etc., which can cause myalgia, rhabdomyolysis, increased blood creatine phosphokinase and other myopathy, and the drug should be discontinued in severe cases. This product should be used in combination with bile acid binding resins, such as cholestyramine, at least 1 hour before or 4 to 6 hours after taking these drugs before taking fenofibrate. Because bile acid binding drugs can also be combined with other drugs taken at the same time, thereby affecting the absorption of other drugs. This product has the effect of enhancing the efficacy of coumarin anticoagulants. Simultaneous use can prolong the prothrombin time. Therefore, the dose of oral anticoagulants should be reduced when used in combination, and the dosage should be adjusted according to the test results later. This product is mainly excreted by the kidneys. When used in combination with immunosuppressants, such as cyclosporine or other nephrotoxic drugs, there may be a risk of worsening renal function, and the dose should be reduced or discontinued. When this product is used in combination with other drugs with high protein binding rates, their free forms can increase and their efficacy can be enhanced, such as tolbutamide and other sulfonylurea hypoglycemic drugs, phenytoin, furosemide, etc. If the above drugs are taken during lipid-lowering treatment, the dosage of hypoglycemic drugs and other drugs should be adjusted.

Keep in a light-proof and airtight container.

0.2g

24 months

Xi`an Han Feng Pharmaceutical Co., Ltd.

• Founded in:

  2003-03-11

• Address:

  No. 15, Wenji Road, Lantian County Industrial Park

• Tax NO.:

  91610122742829723D

• Registered Funds:

  25 million yuan

• Email:

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