Felodipine sustained-release tablets (Ⅱ)

This product is a dihydropyridine calcium channel antagonist (calcium channel blocker), which acts by reversibly competing for dihydropyridine binding sites, blocking the voltage-dependent Ca2 current of vascular smooth muscle and cultured rabbit atrial cells, and blocking K-induced rat portal vein contracture.

Chemical name: 2,6-dimethyl-4-(2,3-dichlorophenyl)-1,4-dihydro-3,5-pyridinedicarboxylic acid ethyl ester.

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

Hypertension, angina pectoris.

Oral administration, dosage should be individualized. The medication should be taken in the morning with water, and the tablets should not be broken, crushed or chewed. 1 Treatment of hypertension: It is recommended to take 5 mg once a day as the starting treatment dose, and the commonly used maintenance dose is 5 or 10 mg once a day. The dose can be reduced or increased according to the patient's response, or other antihypertensive drugs can be added. The dose adjustment interval is generally not less than 2 weeks. For some patients, such as elderly patients and patients with impaired liver function, 2.5 mg once a day may be sufficient. Doses exceeding 10 mg once a day are usually not required. 2 Treatment of angina pectoris: It is recommended to take 5 mg once a day as the starting treatment dose, and the commonly used maintenance dose is 5 or 10 mg once a day. <b

The most common adverse reaction of this product is mild to moderate ankle edema, which is caused by peripheral vasodilation and is dose-related. Experience from clinical trials shows that 2% of patients discontinued treatment due to ankle edema. Facial flushing, palpitations, dizziness and fatigue may occur when starting treatment or increasing the dose. These reactions are often short-lived. Occasionally, there are case reports of mental confusion and sleep disorders, but the connection with felodipine has not been clearly established. It has also been reported that patients with gingivitis or periodontitis may experience gingival swelling after taking the drug, but this can be avoided or reversed through dental care.

Patients with decompensated heart failure, acute myocardial infarction, unstable angina pectoris, and those who are allergic to felodipine or any of the ingredients in this product.

Precautions for children: Not clear yet. Precautions for pregnancy and lactation: There is a lack of research data on the use of drugs in pregnant women, but according to the results of animal tests, this product should be contraindicated for pregnant women. It is not recommended for lactating women to take this product, and lactating women who take the drug should stop breastfeeding. Precautions for the elderly: The blood concentration of this product increases with age, so the recommended initial dose for elderly patients (over 65 years old) is 2.5 mg per day, and the dose is adjusted according to individual response.

Felodipine is a substrate of CYP3A4. Any substance that can inhibit or induce CYP3A4 can significantly affect the concentration of felodipine. Cytochrome P450 inducers: P450 inducers such as carbamazepine, phenytoin, phenobarbital and rifampicin can increase the metabolism of felodipine. When used in combination with carbamazepine, phenytoin and phenobarbital, the AUC of felodipine decreased by 93% and the Cmax decreased by 82%. Co-use with CYP3A4 inducers should be avoided. Cytochrome P450 inhibitors: Imidazole antifungal drugs (itraconazole, ketoconazole), macrolide antibiotics (erythromycin) and HIV protease inhibitors are potential inhibitors of CYP3A4. When used in combination with itraconazole, the Cmax of felodipine increased by 8 times and the AUC increased by 6 times. When used in combination with erythromycin, the Cmax and AUC of felodipine increased by nearly 2.5 times. Co-use with CYP3A4 inhibitors should be avoided. Grapefruit juice: Grapefruit juice can inhibit CYP3A4. When used with grapefruit juice, the Cmax and AUC of felodipine both increase by nearly 2 times. Avoid using it with grapefruit juice. Cyclosporine: When used with cyclosporine, the plasma concentration of felodipine increases by 150%, and the AUC increases by 60%. Felodipine has little effect on the pharmacokinetics of cyclosporine. Cimetidine: When used with cimetidine, the Cmax and AUC of felodipine both increase by nearly 55%.

Store below 25℃. Valid for 36 months.

5mg

24 months

Hefei Lifeon Pharmaceutical Co., Ltd.

• Founded in:

  2002-07-16

• Address:

  Cube Factory, No. 669, Changjiang West Road, Hefei, Anhui Province

• Tax NO.:

  91340100740870052B

• Registered Funds:

  191.2605 million yuan

• Website:

  Log in to view

• Email:

  Log in to view