Felodipine extended-release tablets

1 Pharmacology This product is a dihydropyridine calcium channel blocker, which reversibly competes with nitrendipine and (or) other calcium channel blockers for dihydropyridine binding sites, can block voltage-dependent Ca2 currents in vascular smooth muscle and cultured rabbit atrial cells, and block K-induced rat portal vein contracture. In vitro studies have shown that felodipine selectively inhibits vascular smooth muscle and acts on the myocardium; negative inotropic effects can be detected in vitro, but this effect has not been observed in whole animals. Felodipine can reduce peripheral vascular resistance and lead to lower blood pressure. This pharmacological effect is dose-related and is accompanied by a reflex increase in heart rate. The antihypertensive effect of felodipine is dose-dependent and positively correlated with blood drug concentration. There may be a reflex increase in heart rate during the first week of medication, but this effect decreases over time. Long-term administration may increase heart rate by 5 to 10 beats/minute, and beta-blockers can counteract this effect. Felodipine does not affect the P-R interval of the electrocardiogram when used alone or in combination with beta-blockers. Clinical studies and electrophysiological studies have shown that felodipine alone or in combination with beta-blockers has no significant effect on cardiac conduction (P-R, P-Q and H-V intervals). Antihypertensive treatment with felodipine is associated with a significant recovery of pre-existing left ventricular hypertrophy. In clinical trials of hypertensive patients without left ventricular dysfunction, no clear negative inotropic effect was found. In clinical trials of hypertensive patients, felodipine was found to increase plasma norepinephrine levels. Felodipine can reduce the reabsorption of filtered sodium by the renal tubules and produce natriuretic and diuretic effects. This eliminates the sodium and water retention effects common with other vasodilators. Felodipine does not affect daily potassium excretion. Felodipine reduces renal vascular resistance. The normal glomerular filtration rate remains unchanged. In patients with impaired renal function, their glomerular filtration rate will increase. Felodipine does not affect the excretion of urinary albumin. For patients receiving cyclosporine after renal transplantation, felodipine can lower blood pressure, improve renal blood flow and glomerular filtration rate. Felodipine can also improve early graft function. Mild diuresis, increased natriuresis and increased potassium in the first week of medication can be seen, and short-term and long-term treatment does not affect electrolytes. Felodipine exerts anti-anginal and anti-ischemic effects by improving myocardial oxygen supply. Felodipine reduces coronary vascular resistance by dilating epicardial arteries and arterioles, increasing coronary blood flow and myocardial oxygen supply. Felodipine can effectively relieve coronary spasm. The decrease in peripheral blood pressure caused by felodipine reduces the afterload of the left ventricle and the demand for myocardial oxygen. For stable exertional angina, felodipine can improve exercise tolerance and reduce the onset of angina. Felodipine can reduce the occurrence of symptomatic and painless myocardial ischemia in patients with vasospastic angina. Felodipine can be used alone or in combination with beta-receptor blockers to treat stable angina. Regardless of the patient's age and race, felodipine is effective and well tolerated, even in patients with congestive heart failure, asthma and other obstructive lung diseases, renal impairment, diabetes, gout, hyperlipidemia, Raynaud's disease or renal transplantation. 2 Toxicological carcinogenicity experiment: In a two-year carcinogenicity experiment, male rats were given felodipine at 7.7, 23.1 or 69.3 mg/kg, and the incidence of benign interstitial cell tumors (Leydig cell tumors) increased with increasing doses, but this phenomenon was not found in a similar study in which mice were given 138.6 mg/kg per day (28 times the maximum recommended human dose). At the dose used in the previous two-year study on rats, felodipine reduced rat testosterone levels and increased serum luteinizing hormone accordingly. The formation of Leydig cell tumors may be a secondary effect of these hormones, but it has not been found in humans. In the same rat study, the incidence of focal squamous cell hyperplasia in the esophageal grooves was found to increase with dose in male and female rats in all dose groups compared with the control group. No other drug-related esophageal or gastrointestinal pathological changes were found in rats. In mice, no carcinogenic effects were found after 80 weeks in male mice and 99 weeks in female mice after administration of felodipine at 138.6 mg/kg per day (28 times the maximum recommended human dose). Mutagenicity: Felodipine did not show any mutagenic activity in the in vitro Ames microbial mutagenicity test and the mouse lymphoma forward mutation test. No clastogenic effects were found in the in vivo mouse micronucleus test or in vitro human lymphocyte chromosome aberration test at an oral dose of 2500 mg/kg (506 times the maximum recommended human dose). Reproductive toxicity: No significant effects of felodipine on reproductive capacity were found in reproductive studies in male and female rats at 3.8, 9.6 or 26.9 mg/kg per day. Teratological effects studies in pregnant rabbits with felodipine at 0.46, 1.2, 2.3, and 4.6 mg/kg per day (0.4-4 times the maximum recommended human dose) showed that digital abnormalities, including a reduction in the size and extent of ossification of the terminal phalanges, were found in fetal rabbits. The frequency and severity of these changes were dose-related and occurred even at the lowest dose. Similar fetal abnormalities were not found in rats. In teratological studies in rhesus monkeys, no reduction in the size of the terminal phalanges was found, but about 40% of fetuses had terminal phalanges. Studies in rats given felodipine at 9.6 mg/kg per day (4 times the maximum recommended human dose) found prolonged labor and increased frequency of embryonic and neonatal mortality. In experiments in pregnant rabbits given felodipine at greater than or equal to 1.2 mg/kg per day (equivalent to the maximum recommended human dose), it was found that the mammary glands of rabbits were significantly enlarged, exceeding the mammary gland enlargement of normal pregnant rabbits. Toxicity experiment: Male and female mice were given oral administration of 240 mg/kg and 264 mg/kg of felodipine respectively, and male and female rats were given oral administration of 2390 mg/kg and 2250 mg/kg of felodipine respectively, all of which caused death.

The main ingredient of this product is felodipine.

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

Suitable for hypertension and angina pectoris.

Oral administration, dosage should be individualized. The medication should be taken in the morning, swallowed 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. 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.

Like other vasodilators, felodipine extended-release tablets may cause facial flushing, palpitations, dizziness, and fatigue in some patients. Most reactions are dose-related and often occur when starting or increasing the dose. This adverse reaction is often ecological and gradually disappears over time. Like other dihydropyridine calcium antagonists, this drug may cause dose-related (due to pre-telangiectasia) ankle edema. There are also reports that patients with gingivitis or periodontitis may experience mild gingival swelling after taking the drug, but this can be avoided or reversed through dental care. Skin reactions such as rash and itching have also been reported. 1 Common (>=1%): Nervous system: headache; Skin: flushing; Vascular: peripheral edema; 2 Rare (>=1, <1%): Cardiovascular system: tachycardia, palpitations; Nervous system: dizziness, paresthesia; Digestive system: nausea, abdominal pain; Skin: rash, itching; General condition: fatigue. 3 Rare (<1, >= 1/10000): Cardiovascular system: syncope; Digestive system: vomiting; Musculoskeletal: arthralgia, myalgia; Psychiatric: impotence/sexual dysfunction; Skin: urticaria. 4 Very rare (<1/10000) Digestive system: gingival hyperplasia, gingivitis; Liver: increased hepatic enzymes; Skin: photosensitivity reaction, leukocytoclastic vasculitis; Urinary system: frequent urination; General: allergic reactions such as angioedema, fever.

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

Precautions for children: Not clear yet. Precautions for pregnancy and lactation: Contraindicated for pregnant women 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.

1. The simultaneous use of certain drugs that interfere with the cytochrome P4503A4 enzyme system may affect the blood concentration of dihydropyridine calcium antagonists such as felodipine. Hepatic enzyme inhibitors (such as cimetidine, erythromycin, itraconazole, ketoconazole and certain cypermethrin compounds present in grapefruit juice) may cause an increase in the blood concentration of felodipine. Hepatic enzyme inducers (such as phenytoin, carbamazepine, rifampicin, barbiturates) may cause a decrease in the blood concentration of felodipine. 2. Felodipine does not affect the blood concentration of cyclosporine. 3. Although felodipine has a high degree of plasma protein binding, it does not affect the binding degree of other highly plasma protein-bound drugs (such as warfarin). 4. The combination of this product with digoxin did not show significant changes in the pharmacokinetic behavior of digoxin in patients with heart failure. 5. Other drugs such as indomethacin or spironolactone have no obvious interactions with this product.

Store at room temperature.

5mg

36 months.

Shanxi Kangbao Biological Product Co., Ltd.

• Founded in:

  1995-05-18

• Address:

  No. 151, Beihuan West Street, Luzhou District, Changzhi City, Shanxi Province

• Tax NO.:

  91140000602311789X

• Registered Funds:

  69.2 million yuan

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