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Nifedipine is a selective blocker of slow calcium channels, derived 1.4-dihydropyridine. Has antianginal and hypotensive action. Reduces the flow of calcium ions through the slow calcium channels into cells, is predominantly inside the cardiomyocytes, smooth muscle cells of the coronary and peripheral arteries, thus lowering peripheral vascular resistance and increasing coronary artery, particularly the major supplying vessels, and even intact segments of the walls of the partially stenosed vessels.
In addition, nifedipine reduces the tone of smooth muscles of the coronary arteries, thereby preventing vasospasm, increasing blood flow in poststenotic parts of vessels and increasing oxygen delivery to the myocardium; reduces myocardial oxygen demand by reducing peripheral vascular resistance and at long reception it is able to prevent development of new atherosclerotic lesions in the coronary arteries. Nifedipine reduces the tone of smooth muscles of arterioles, thus reducing the increased peripheral vascular resistance and therefore BP.
In the beginning of treatment with Adalat may occur temporary reflex increase in heart rate and, as a consequence, the magnitude of cardiac output.
However, this increase is not significantly enough to compensate for the vasodilation.
In addition, nifedipine with short-term and long-term use increases the excretion of sodium and water from organizasyonunu effect of nifedipine is particularly pronounced in patients suffering from hypertension.
Contraindications to the drug:
- Cardiogenic shock;
- Unstable angina;
- Acute myocardial infarction;
- Coadministration with rifampicin;
- The age of 18;
- Hypersensitivity to nifedipine or any component of the drug.
The dose of the drug adalat should be individualized based on the severity of the disease and the patient’s response to therapy, and closely monitor blood pressure and heart rate.
Not recommended simultaneous application of the drug adalat and beta-blockers because of risk expressed lower AD, and in some cases worsening of chronic heart failure. If necessary, the simultaneous application of nifedipine with beta-blockers is necessary to monitor the patient.
Drug adalat should not be used in patients whose pain is expected the relationship to be ischemic in nature with the previous therapy with nifedipine.
As with other vasodilators, with the use of the drug adalat can occur very rarely angina, and worsening angina with weights, lengthening and increasing frequency of angina attacks, especially at the beginning of treatment.
In some cases, the registered myocardial infarction, however, it is not possible to establish a causal relationship of the disease with the use of nifedipine as myocardial infarction can occur as a result of the natural course of coronary heart disease.
Patients with impaired liver function when the drug adalat require careful monitoring; in severe cases, necessary to decrease the dose of the drug adalat.
Nifedipine is metabolized via the CYP3A4 isoenzyme. Thus, the drug inhibitors or inducers of CYP3A4 can affect the metabolism when “first pass” through the liver nifedipine and its clearance in a joint application. In the case of combined application of nifedipine and drugs weak or moderate inhibitors of CYP3A4 izofermenta, as listed below, may increase concentration of nifedipine in blood plasma, therefore, careful monitoring of BP and, if necessary, reduce the dose of nifedipine: antibiotics group macrolides (e.g. erythromycin) inhibitors, HIV protease inhibitors (eg, ritonavir), antifungal drugs from the group of azoles (eg, ketoconazole), antidepressants (nefazodone and fluoxetine), quinupristin/dalfopristin. valproic acid, cimetidine.
Adalat drug contains 18% by volume of ethyl alcohol, which corresponds to 45 g of ethanol per day dose of the drug. This must be taken into account in the application in patients with alcoholism or impaired metabolism of ethanol, as well as in the application in pregnant and lactating women, in children, also in patients at high risk (having liver disease or epilepsy).
In a few cases when conducting in vitro fertilization with the use of blockers of slow calcium channels dihydropyridine noted reversible biochemical changes in the head of spermatozoa, resulting in impaired function of sperm. With the unsuccessful attempts of in vitro fertilization and exclusion of other causes of infertility should take into account the likely effects of blocking slow calcium channel blockers dihydropyridine on sperm under condition of their admission.
Nifedipine causes a false increase in the concentration vanillylmandelic acid in the urine in determining the spectrophotometric method and does not affect the result of this reaction using the method of high performance liquid chromatography (HPLC).
The drug adalat in the vial, equipped with light-proof plastic sheath, remains stable in daylight for 1 h, and artificial light for 6 hours.
Effects on ability to drive vehicle mechanisms: the ethanol contained in the composition of the drug adalat, can affect the action of other medicines. applied simultaneously with the drug adalat, and may impair the ability to drive vehicles and to work with sensitive mechanisms.