What Is Micronized Fenofibrate?
The main ingredient of this product is fenofibrate, and its chemical name is 2- [4- (4-chlorobenzoyl) phenoxy] -2-methyl-propionic acid methyl ethyl ester.
Its structural formula is:
- Fenofibrate micropowder granules, the indication is for the treatment of hypercholesterolemia (abnormal increase in blood cholesterol level and / or hypertriglyceridemia (triglyceride or fat level) Abnormal increase)). Especially when dietary cholesterol continues to rise, or when there are other concurrent risk factors. Diet control should be continued during the medication. Currently, there are no long-term clinically controlled studies demonstrating the effectiveness of fenofibrate in primary and secondary prevention of atherosclerotic complications.
- Drug Name
- Fenofibrate fine particles
- Drug type
- prescription
- Use classification
- Lipid-lowering drugs
Fenofibrate powder composition
- The main ingredient of this product is fenofibrate, and its chemical name is 2- [4- (4-chlorobenzoyl) phenoxy] -2-methyl-propionic acid methyl ethyl ester.
Its structural formula is:
Molecular formula: C20H21ClO4
Molecular weight: 360.84
Fenofibrate fine powder
- This product is white or off-white particles.
Indications of fenofibrate fine particles
- It is used to treat hypercholesterolemia (abnormal increase in blood cholesterol level and / or hypertriglyceridemia (abnormal increase in blood triglyceride or fat level) in blood) in adults with unsatisfactory diet control therapy. Especially when dietary cholesterol continues to rise, or when there are other concurrent risk factors.
Diet control should be continued during the medication.
Currently, there are no long-term clinically controlled studies demonstrating the effectiveness of fenofibrate in primary and secondary prevention of atherosclerotic complications.
Fenofibrate powder specifications
- (1) 67mg, (2) 200mg.
Fenofibrate powder usage and dosage
- Prior to treatment with fenofibrate micropowder granules, patients should have an appropriate lipid-lowering diet and should also adhere to a lipid-lowering diet during treatment. Fenofibrate powder should be taken with food to optimize the bioavailability of the drug.
The starting dose for adult patients with primary hypercholesterolemia and mixed hyperlipidemia is 200 mg / day.
For the treatment of adult patients with hypertriglyceridemia, the initial dose of fenofibrate micronized granules is 67 ~ 200mg / day. The dose should be individualized according to the patient's response to the administration, blood lipids should be measured at intervals of 4 to 8 weeks, and if necessary, the dose should be adjusted. The maximum dose is 200 mg / day.
The starting dose of fenofibrate micronized granules for patients with renal insufficiency is 67 mg / day, and the dose can only be increased after evaluating the effects of renal function and blood lipid levels at this dose. For elderly patients, the initial dose should also be 67 mg / day.
Serum lipid levels should be measured regularly, and if the blood lipids significantly decrease below the target range, consideration should be given to reducing the dose of fenofibrate micronized particles.
Fenofibrate fine powder particles adverse reactions
- -When combined with other fibrates, there have been reports of muscular dysfunction (diffuse pain, tenderness, muscle weakness) and rare severe rhabdomyolysis. Most of these adverse reactions were reversible after discontinuation. If you feel muscle pain, painful muscle sensitivity, muscle weakness, contact your doctor immediately because sometimes muscle problems are severe.
-Others are rare and moderate adverse reactions have also been reported:
Gastric or intestinal digestive disorders such as indigestion;
Elevated transaminase;
Occasional allergic skin reactions such as rash, pruritus, urticaria, or photosensitivity have been reported. In some cases, even if the drug is stopped for several months, erythema, pimples, and flowers may appear after skin exposure to sunlight or artificial ultraviolet light Macular rash and eczema.
There are currently no long-term comparative studies to comprehensively assess adverse reactions, especially the risk of developing gallstones.
Fenofibrate fine powder particles taboo
- This drug is prohibited in the following cases:
-Disable allergy to fenofibrate;
-People with liver dysfunction;
-People with renal insufficiency;
-It is known that fenofibrate or similar structural drugs, especially ketoprofen, will cause phototoxicity or photosensitivity during the treatment process;
-Combination with other fibrates;
-Children disabled.
The drug is generally not recommended for use in combination with HMG-CoA reductase inhibitors and should not be used during lactation.
Precautions for fenofibrate fine particles
- WARNINGS It has been reported that fibrates can cause muscle-related adverse reactions, including less frequent rhabdomyolysis. This situation often occurs with low plasma albumin.
Muscle-related symptoms in any patient should be considered, including diffuse muscle pain, muscle tenderness, and a substantial increase in muscle-derived CPK (more than five times the normal concentration). In this case, medication should be stopped immediately.
In addition, the risk of muscle side effects is increased when combined with HMG-CoA reductase inhibitors or other fibrates.
Precautions for use
-If blood lipids have not improved effectively after taking it for several months (3-6 months), supplementary treatment or other methods should be considered.
Taking this product can not be used as an alternative therapy for diet control, continued diet control is still necessary, and regular blood tests are required.
-Transaminase elevation may occur in some patients, usually transiently. As far as is known, these seem to indicate:
Fully check the transaminase concentration every 3 months during the first 12 months of treatment;
When ASAT and ALAT rise to more than three times the normal value, treatment should be stopped.
-When combined with oral anticoagulants, the thrombin concentration should be closely monitored, expressed as INR.
Fenofibate powder for pregnant and lactating women
- pregnancy
-Animal test results show no teratogenic effect.
-So far, teratogenicity and embryo toxicity have not appeared clinically. However, the use of fenofibrate during pregnancy is not enough to rule out any danger, so pregnant women should generally be disabled.
Fibrates are not used in pregnant women, except when dietary control cannot effectively reduce high triglycerides (> 10g / L) and increase the risk of acute pancreatitis in the mother.
There is no information on fenofibrate access to breast milk during lactation, but it is prohibited during lactation.
Fenofibrate powder for children
- Children disabled.
Fenofibrate fine powder granules for the elderly
- It is recommended to use a normal adult dose, which can be reduced if there is renal impairment.
Fenofibrate micropowder drug interactions
- Prohibited in combination with
+ Other fibrates: Increasing the incidence of adverse reactions such as rhabdomyolysis and antagonism between the two molecules.
Drugs not recommended for combined use
+ HMG-CoA reductase inhibitor: Increases the incidence of muscle adverse reactions such as rhabdomyolysis.
Cautiously combined drugs
+ Oral anticoagulants: When combined with oral anticoagulants, they increase the risk of bleeding (due to their replacement reaction in plasma).
Inspect and monitor INR more frequently. The dose of oral anticoagulant was adjusted during treatment with fenofibrate and after 8 days of discontinuation.
Fenofibrate powder overdose
- Symptomatic treatment.
Pharmacology and toxicology of fenofibrate powder
- Pharmacological effects Fenofibrate can reduce serum cholesterol by 20-25% and reduce triglycerides by 40-50%.
-Cholesterol reduction is achieved by lowering low-density atherogenic components (VLDL and LDL), and by reducing the total cholesterol / HDL cholesterol ratio (which is elevated in atherosclerotic hyperlipidemia) The distribution of cholesterol in plasma.
-The relationship between high cholesterol and atherosclerosis, and the relationship between atherosclerosis and the risk of coronary artery disease has been confirmed. Low levels of HDL increase the risk of coronary artery disease. Elevated triglycerides are associated with an increased risk of cardiovascular disease. In addition, triglycerides may also be involved in the atherosclerotic process and thrombosis.
-Long-term effective treatment (significantly reduce cholesterol), can make the extravascular cholesterol deposition (nodular xanthomas) significantly subsided, or even completely eliminated.
-The effect of fenofibrate uric acid in patients with hyperlipidemia can reduce uric acid in plasma by 25%.
-Fenofibrate treatment increases apoA1 and decreases apoB, thereby improving the apoA1 / apoB ratio, which is considered to be a risk indicator of atherosclerosis.
-Animal studies and human clinical studies have shown that fenofibrate has an anti-platelet agglutination effect, which is achieved by reducing the agglutination response caused by ADP, arachidonic acid and epinephrine.
-Fenofibrate activates PPAR (peroxidase proliferator-activated receptor alpha), activates lipolytic enzymes, and reduces apolipoprotein CIII synthesis, resulting in a significant increase in plasma fat degradation and triglyceride clearance.
In toxicology studies, tumors and / or hepatocellular carcinoma of the liver of mice and rats were found at doses exceeding 45 mg / kg, and rat pancreatic acinar cell tumors and adenocarcinomas were also found at this dose. 60 mg / Stromal cell tumors were found in testes of kg rats. The results of carcinogenicity studies show that the incidence of tumors in rodents treated with fenofibrate increased significantly in three organs: liver (tumor and hepatocellular carcinoma), pancreas (acinoma and adenocarcinoma), and testis (interstitial Cell tumor).
The results of toxicity studies in rats and mice show that excessive catalase stimulation can cause toxic reactions. This change occurs only in small rodents, and has not yet occurred in other animal specimens. And there is no correlation with human treatment.
The following experimental results confirm that fenofibrate has no potential mutagenic effects: Ames test, mouse lymphoma test, chromosomal aberration test, and irregular DNA synthesis experiment.
Reproductive studies have shown that fenofibrate is not teratogenic, but when toxic doses are used in pregnant women, it can cause some embryo toxicity in rats and rabbits. When the dosage of rats is more than 75mg / kg / day, it will delay the delivery and reduce the survival rate after birth. This product should not be used during pregnancy. If you become pregnant while using this product, stop using it immediately and consult your doctor.
Pharmacokinetics of fenofibrate powder particles
- Fenofibrate was not found in the plasma, and the main metabolite was fenofibrate. The maximum plasma concentration is usually reached within 5 hours after administration.
Continuous treatment of the same patient has stable blood concentration levels.
Fenofibrate is tightly bound to plasma albumin and can replace vitamin K anticoagulants from the protein-binding site to enhance anticoagulant effects.
The elimination half-life of fenofibrate in the blood is about 20 hours.
The drug is mainly excreted from the urine and almost all products are eliminated from the body within 6 days.
Fenofibrate is excreted mainly in the form of fenofibrate acid and its glucuronide derivatives.
Single- and multi-dose pharmacokinetic studies have shown that fenofibrate has no accumulation effect.
Hemodialysis cannot remove fenofibrate.
Fenofibrate powder storage
- Store in a light-proof, cool and dry place.
Fenofibrate powder packaging
- Composite film packaging, 10 bags / box.
Expiration date of fenofibrate powder
- Tentatively set for two years.