| Generic Name |
Felodipine Extended-Release Tablets |
| Strength |
5mg |
| Packing |
3*10 Tablets/box |
| Origin |
China |
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Product name:
Felodipine Extended-Release Tablets
Character:
This product is a film coating, after removing the film coating white or white.
Indications:
Hypertension, stable angina pectoris.
Adverse reactions:
The most common adverse event is mild to moderate ankle edema, which is caused by peripheral vascular dilatation and is dose-dependent. Experience from clinical trials shows that 2% of patients discontinue treatment due to ankle edema. Facial flushing, headache, heart palpitations, dizziness, and fatigue may occur when starting treatment or increasing the dose. These reactions are often short-lived. Occasional cases of conscious confusion and sleep disturbances have been reported, but a link to felodipine has not been clearly established. It has also been reported that in patients with gingivitis or periodontitis, swelling of the gums may be caused by medication, but can be avoided or reversed through dental care.
Hyperglycemia is an adverse reaction to this class of drugs, but only sporadic cases have been reported in felodipine.
Pharmacology and toxicology:
1. Pharmacology
It is a dihydropyridine calcium channel antagonist (calcium channel blocker) that acts by reversely competing dihydropyridine binding sites, blocking voltage-dependent Ca2+ currents in vascular smooth muscle and cultured rabbit atrial cells, and blocking K+ induced portal vein contracture in mice.
In vitro studies showed that the selective inhibitory effect on vascular smooth muscle was stronger than that on myocardium. Negative inotropic effects were detected in vitro, but were not observed in the whole animal.
This product can reduce peripheral vascular resistance and blood pressure, the pharmacological effect is dose-dependent, and accompanied by a reflex heart rate increase. It has been observed in animals and humans to reduce peripheral vascular resistance and cause mild diuretic effect.
The antihypertensive effect of this product was dose-dependent and positively correlated with blood concentration. There may be a reflexive increase in heart rate during the first week of medication, but this effect decreases with time. Long-term administration of the drug may increase the heart rate by 5-10 beats/minute, and beta-blockers can counter this effect. This product does not affect the P-R interval of the electrocardiogram when used alone or in combination with β-blockers. Clinical and electrophysiological studies have shown no significant effect on cardiac conduction (P-R, P-Q, and H-V interphase), either alone or in combination with beta-blockers.
In clinical trials of hypertensive patients without left ventricular dysfunction, no clear negative inotropic effect has been found.
This product can reduce renal vascular resistance without affecting glomerular filtration. Mild diuresis, increased natriuretic and increased potassium were observed at the first week of treatment, and electrolytes were not affected by short - and long-term treatment.
In clinical trials in hypertensive patients, it was found to increase plasma norepinephrine levels.
Anti-angina action: Felodipine works by dilating coronary blood vessels and also improves perfusion and oxygen supply to the heart. The heart's work load is reduced by lowering peripheral arterial resistance (lower afterload), which reduces the oxygen demand of the heart muscle. Felodipine relieves coronary spasms.
In patients with angina pectoris induced by stable exertion, felodipine can improve exercise tolerance and reduce angina pectoris attacks.
At the beginning of treatment, the heart rate is briefly reflexived to increase, and the combination of boivine and beta-blockers can eliminate this effect. The effective time is 2 hours, and the effect is maintained for 24 hours.
Felodipine can be used in combination with beta-blockers or as a monotherapy for angina pectoris.
2. Toxicology
Carcinogenic experiment:
In a 2-year carcinogenic study, male rats were given felodipine 7.7, 23.1, or 69.3 mg/kg daily, respectively, and it was observed that the incidence of benign Leydig cell tumor increased with the increase of dose. However, this phenomenon was not found in a similar study in mice given 138.6 mg/kg/ day (28 times the maximum recommended human dose). At the doses used in the previous two-year study in rats, felodipine reduced levels in rats while correspondingly increasing serum luteinizing hormone. 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 was found to increase with dose in the esophageal grooves of both male and female rats in all dose groups compared to the control group. No other drug-related pathological changes in the esophagus or gastrointestinal tract were found in the rats.
Mice given 138.6 mg/kg/ day of felodipine (28 times the maximum recommended dose for humans) showed no carcinogenic effects after 80 weeks in male mice and 99 weeks in female mice.
Mutagenicity experiment:
Felodipine did not show any mutagenic activity in vitro Ames microbial mutagenicity test or in mouse lymphoma forward mutagenicity test. No teratogenic effect was found 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 test:
No significant effect of felodipine on reproductive ability was observed in male and female rats given 3.8, 9.6 or 26.9 mg/kg/ day.
Studies of deformities in pregnant rabbits administered felodipine at 0.46, 1.2, 2.3, and 4.6 mg/kg/ day (0.4-4 times the maximum recommended human dose) showed that finger (toe) abnormalities were found in fetal rabbits, including reduced ossification size and degree of the distal finger (toe) bone. The frequency and severity of these changes are dose-dependent and occur even at the lowest dose. No similar abnormalities were found in fetal rats.
Teratological studies of rhesus monkeys have not shown a reduction in the size of the terminal finger (toe) bone, but about 40% of fetal monkeys have terminal finger (toe) bone ectopia.
Studies in rats treated with felodipine above 9.6 mg/kg/ day (4 times the maximum recommended dose for humans) found prolonged labor and increased frequency of fetal and neonatal mouse death.
In pregnant rabbits administered with felodipine greater than or equal to 1.2 mg/kg/ day (equivalent to the maximum recommended human dose), the mammary glands of rabbits were found to be significantly enlarged, exceeding that of normal pregnant rabbits.
Toxicity test:
Oral administration of felodipine at 240 mg/kg and 264 mg/kg in male and female mice, and at 2390 mg/kg and 2250 mg/kg in male and female rats, respectively, caused death.
Storage:
Store below 25ºC.
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