Properties
- Form
- tableti saghech i
- Dosage mg
- 20
- Pack
- 100
What is it?
Composition Active substance: 1 retard tablet contains 20 mg Nifedipine Excipients: microcrystalline cellulose, corn starch, lactose monohydrate, polysorbate 80, magnesium stearate, hypromellose, macrogol 6000, talc, titanium dioxide, iron oxides. Description Pink, round, biconvex tablets, approximately 8mm in diameter. Pharmacological properties Nifedipine belongs to the group of dihydropyridine type calcium antagonists. These substances inhibit calcium influx into the cell membrane. On smooth muscle cells, especially coronary and peripheral resistance vessels, nifedipine acts as a calcium antagonist. This leads to vasodilation. In therapeutic doses, nifedipine does not directly affect the myocardium. At the beginning of treatment with calcium antagonists, a reflex increase in heart rate and cardiac output is observed. However, this increase is not so pronounced as to compensate for vasodilation. With prolonged treatment with nifedipine, the initially increased heart rate returns to baseline levels. A pronounced decrease in blood pressure is particularly observed in patients with hypertension after taking nifedipine. See blog: How to use Nifedipine - a blood pressure medication for proper heart function Pharmacokinetics After oral administration on an empty stomach, nifedipine is rapidly and almost completely absorbed. Nifedipine undergoes hepatic first-pass metabolism. As a result, the systemic bioavailability of orally administered nifedipine is 50-70%. Peak plasma concentration is reached approximately 15 minutes after administration of a solution containing nifedipine, and 30-85 minutes after administration of an immediate-release drug. 95-98% of nifedipine is bound to plasma proteins. The mean volume of distribution Vss was 0.77 – 1.12 L/kg. Nifedipine is almost completely metabolized in the liver, mainly by oxidation. These metabolites have no pharmacodynamic activity. Both unchanged substance and metabolite (M-1) are excreted by the kidneys in negligible amounts (dose < 0.1%). Polar metabolites, M-2 and M-3, are excreted in urine in an amount of approximately 50% of the administered dose. The main part is excreted within 24 hours, and the remaining metabolites are excreted via feces. The elimination half-life is 1.7-3.4 hours. No cases of substance accumulation have been observed during prolonged therapy with normal doses. In case of impaired liver function, the elimination half-life significantly increases and total clearance decreases. In this case, dose reduction is necessary. Preclinical safety data: In vivo and in vitro mutagenicity tests were negative without exception. Therefore, a mutagenic effect in humans can be excluded. Long-term studies in rats did not reveal any tumorogenic potential of nifedipine. Experimental studies in 3 species (rats, mice, and rabbits) revealed teratogenic effects of the drug (cleft palate, cardiovascular and digital anomalies). In monkeys during treatment, a small placenta and underdevelopment of chorionic villi were observed. Hypoxia and acidosis were also observed in this animal species. Bioavailability: In 1995, bioavailability studies conducted in 36 probands in a steady state revealed the following results: Tested product Comparable product Maximum plasma concentration (Cmax12h) 1 7.1 ng/mL ± 5.47 16.9 ng/mL ± 5.45 Maximum plasma concentration (Cmax 12-24h) 19.6 ng/mL ± 5.68 24.8 ng/mL ± 9.29 Peak between fluctuations (PTF 0–12h) 124 % ± 20.1 132 % ± 41 Peak between fluctuations (PTF 12-24h) 141 % ± 25.0 181 % ± 44.9 Area under the concentration-time curve (AUC): 0-24h 240 (ng/mL×h) ± 77.2 249 (ng/mL×h) ± 90.1 (These data represent average values and deviation). The concentration-dose diagram shows the formation of the average plasma level of the drug compared to the concentration of the comparable preparation. Indications Chronic stable angina (angina of effort); - Vasospastic angina (Prinzmetal's angina, variant angina); - Essential hypertension Dosage and administration Unless otherwise prescribed by a doctor, the following dosage guidelines are given for adults: - Chronic stable angina (angina of effort): 1 retard tablet 2 times a day (equivalent to 20 mg nifedipine per day); - Vasospastic angina (Prinzmetal's angina, variant angina): 1 retard tablet 2 times a day (equivalent to 20 mg nifedipine per day). If necessary, the daily dose can be gradually increased from 2 x 20 mg (equivalent to 2 retard tablets 2 times a day) to 2 x 40 mg (equivalent to 4 retard tablets 2 times a day); - Essential hypertension: 1 retard tablet 2 times a day (equivalent to 20 mg nifedipine per day). If necessary, the daily dose can be gradually increased from 2 x 20 mg (equivalent to 2 retard tablets 2 times a day) to 2 x 40 mg (equivalent to 4 retard tablets 2 times a day). Nife-Denk 20 retard should be swallowed whole with sufficient water after meals. Nife-Denk 20 retard is taken in the morning and evening at the same time. Side effects Unless otherwise prescribed by a doctor, the following dosage guidelines are given for adults: - Chronic stable angina (angina of effort): 1 retard tablet 2 times a day (equivalent to 20 mg nifedipine per day); - Vasospastic angina (Prinzmetal's angina, variant angina): 1 retard tablet 2 times a day (equivalent to 20 mg nifedipine per day). If necessary, the daily dose can be gradually increased from 2 x 20 mg (equivalent to 2 retard tablets 2 times a day) to 2 x 40 mg (equivalent to 4 retard tablets 2 times a day); - Essential hypertension: 1 retard tablet 2 times a day (equivalent to 20 mg nifedipine per day). If necessary, the daily dose can be gradually increased from 2 x 20 mg (equivalent to 2 retard tablets 2 times a day) to 2 x 40 mg (equivalent to 4 retard tablets 2 times a day). Nife-Denk 20 retard should be swallowed whole with sufficient water after meals. Nife-Denk 20 retard is taken in the morning and evening at the same time. Contraindications Nife-Denk 20 retard is contraindicated in the following cases: - Hypersensitivity to nifedipine; - Unstable angina; - Cardiocirculatory shock; - Severe narrowing of the blood vessels leading from the heart to the aorta (high-grade aortic stenosis); - Pregnancy and lactation; - Combination therapy with rifampicin (active substance for tuberculosis treatment, see Interactions with other medicines) - Acute myocardial infarction (within the first 4 weeks). Special attention should be paid in the following cases when taking Nife-Denk 20 retard (consult your doctor). Pronounced low blood pressure (severe hypotension, systolic pressure is 90 mmHg); - Decompensated heart failure. - In dialysis patients with high blood pressure (malignant hypertension), a sharp drop in blood pressure is expected due to vasodilation resulting from reduced circulating blood volume (hypovolemia). Safety precautions: In case of liver dysfunction, nifedipine excretion may be delayed. Therefore, your doctor should strictly monitor the course of treatment and reduce the dose if necessary. If your doctor has diagnosed a disorder of blood circulation in the brain (cardiovascular disease), treatment should be continued with reduced doses. Pregnancy and lactation The use of Nife-Denk 20 retard is not recommended at any stage of pregnancy, as studies on the active substance nifedipine have revealed cases of fetal distress (malformations). There is insufficient data in humans. If a woman becomes pregnant during Nife-Denk 10 treatment, the treatment should be changed under medical supervision. Nifedipine passes into breast milk. No experiments on the effects on the fetus have been conducted, therefore, if nifedipine treatment is necessary during lactation, breastfeeding should be discontinued. Special precautions The use of Nife-Denk 20 retard is not recommended at any stage of pregnancy, as studies on the active substance nifedipine have revealed cases of fetal distress (malformations). There is insufficient data in humans. If a woman becomes pregnant during Nife-Denk 10 treatment, the treatment should be changed under medical supervision. Nifedipine passes into breast milk. No experiments on the effects on the fetus have been conducted, therefore, if nifedipine treatment is necessary during lactation, breastfeeding should be discontinued. Overdose The use of Nife-Denk 20 retard is not recommended at any stage of pregnancy, as studies on the active substance nifedipine have revealed cases of fetal distress (malformations). There is insufficient data in humans. If a woman becomes pregnant during Nife-Denk 10 treatment, the treatment should be changed under medical supervision. Nifedipine passes into breast milk. No experiments on the effects on the fetus have been conducted, therefore, if nifedipine treatment is necessary during lactation, breastfeeding should be discontinued. Interactions with other medicines If you are taking or have recently taken any medicines, including medicines obtained without a prescription, please inform your doctor or pharmacist. Please note that this information also applies to medicines taken in the recent past. Simultaneous use of Nife-Denk 20 retard with other preparations may lead to the following reactions: Medications that lower blood pressure and tricyclic antidepressants (medication for depression) enhance the hypotensive effect of Nife-Denk 20 retard. The effect of Nife-Denk 20 retard on blood pressure and heart rate is enhanced when used in combination with nitrates (medications for coronary arteries). Diltiazem (a drug used to treat coronary arteries and high blood pressure) reduces the breakdown of nifedipine. In this case, your doctor should frequently monitor the course of treatment and reduce the dose if necessary. When beta-blockers are used concurrently, frequent patient monitoring is necessary, as a sharp drop in blood pressure and the development of heart failure may occasionally occur. Cimetidine (medication for stomach and duodenal ulcers): enhances the effect of Nife-Denk 20 retard due to an increase in its blood levels. Rifampicin (medication for tuberculosis) enhances the degradation of nifedipine. Simultaneous use of rifampicin and Nife-Denk 20 retard is not possible, as nifedipine does not reach active levels in the blood. Antiarrhythmics (medications for treating heart rhythm disorders): Some drugs in the calcium antagonist group increase the negative inotropic effect (weakening of heart function) of antiarrhythmics (such as amiodarone and quinidine). There is no data on nifedipine in this case. In individual cases, nifedipine reduces plasma levels of quinidine; when nifedipine treatment is discontinued, quinidine plasma concentration increases sharply. Therefore, in case of concomitant therapy, monitoring of quinidine plasma levels is recommended. Digoxin (used to treat heart failure) and theophylline (medication used for respiratory system diseases): Concomitant administration of Nife-Denk 20 retard may lead to an increase in the levels of these drugs in the blood, and therefore periodic monitoring of their blood levels is recommended. Nifedipine reduces the excretion of vincristine, which may lead to an increase in vincristine side effects. A reduction in vincristine dose should be considered. Cephalosporins (antibiotics used to treat bacterial infections, e.g., Cefixime): increase the plasma levels of cephalosporins. Please note that this information also applies to recently used preparations. Which foods and drinks should be avoided? Grapefruit juice: Do not take Nife-Denk 20 retard with grapefruit juice, as it inhibits the breakdown of nifedipine and thus enhances the effect of Nife-Denk 20 retard. Storage conditions and expiry dates The preparation should be stored in a dry place, at a temperature below 25°C. Protect from light, heat, and moisture. Keep out of reach of children. Shelf life is 3 years. The preparation should not be used after the expiry date indicated on the packaging. Dispensing from pharmacy: By prescription
