Nifecard XL is presented on the pharmaceutical market as an effective product for angina pectoris. You can use the tool for various forms of the disease. The tablet medicine is made using nifedipine. It is prescribed to facilitate the course of hypertensive crisis. Among the indications for the appointment are a spasm of arteries that feed the heart muscle, some forms of hypertension.
Technical information
The drug demanded for the treatment of hypertension is available in the form of tablets. Modified release provided. Each tablet is coated with a thin film. Color varies from light yellowish to brownish with an orange tint. Instances are made round, convex on both sides. There is an engraving on one of the surfaces. If you cut the tablet across, you can see the yellowish inner contents.
Each tablet contains 30-60 mg of the active ingredient - nifedipine. As additional components used sodium, magnesium compounds, talc, povidone, ludipress, mellose. For the manufacture of the shell, the manufacturer used hypromellose, triethyl citrate, hyprolose, macrogol, coloring components, talc and titanium compounds.
Pharmacology
The drug under consideration for the fight against vasospastic angina and other pathological conditions belongs to the category of calcium channel inhibiting pharmaceutical products. The tool has a selective effect, working only with the so-called slow channels. The main ingredient is the transformation product of 1,4-dihydropyridine. This compound has the ability to reduce pressure; antianginal effect is observed.
Under the influence of the drug, calcium flow outside the cells to the myocytes of the heart muscle becomes less active. The calcium supply to the cells of smooth muscle tissue of the arterial walls at the periphery and nourishing the heart is changing. If the drug is used in a high dose, under its influence the release of calcium ions from the depot inside the cells is reliably inhibited. The number of working channels is reduced, while the activation, recovery and loss of activity are not adjusted.
The drug, which has an antianginal effect, also divides myocardial excitations, contractions; affects the same processes in smooth muscle vascular walls - they are mediated by calmodulin. The use of the drug in a therapeutic dosage allows to achieve a stable transmembrane calcium ion flux, often disturbed due to a pathological reason.
Most often, this is observed with high blood pressure in the arteries. The drug does not correct venous tone, makes blood flow to the heart richer, improves the quality of blood supply to areas affected by ischemia. In this case, the phenomenon of "robbery" is not formed. The drug makes collaterals more active.
Pharmacological Nuances
The pharmacological action of Nifecard XL is that the product improves myocardial functionality, lowers the power of contractions of the heart muscle, and reduces the organ’s oxygen demand. Under its influence, arterial lumens expand on the periphery, pressure drops, and vascular resistance decreases. The drug leads to a decrease in cardiac afterload, almost does not correct the work of the atrioventricular, sinoatrial nodes. The blood flow in the kidneys becomes more powerful, and average natriuresis is observed. Prolonged use is associated with the appearance of tolerance to the main ingredient.
The drug inhibits platelet aggregation. It has inherent general anti-atherogenic qualities, especially pronounced with prolonged use. During treatment with tablets, the pressure in the arteries that feed the lungs decreases. A positive change in blood flow in the vascular cerebral system is observed.
Kinetics
Having a pronounced antianginal effect, the drug is absorbed soon after oral administration. The efficiency of the process is estimated at 92-98%. There is a slow release of the active ingredient. This provides a controlled gradual increase in the concentration of the ingredient in the blood serum. Plasma concentration reaches a plateau level on average six hours after the next dose is ingested, and remains at that level for about a day. During this time, minor fluctuations are possible.
Plasma protein binding is estimated at 90% on average. A pharmaceutical product crosses the barriers of the placenta and protects the brain. A study of breast milk has shown the ability of the active ingredient to be excreted along with the secretion of the mammary glands. No accumulation effect was detected.
Transformation processes are mainly localized in the liver. Effective in vasospastic angina, nifedipine does not produce any reaction products after treatment that would have inherent therapeutic effects. The elimination half-life of this substance is on average estimated at a couple of hours. Elimination is carried out by inactive metabolic products. About 80% is excreted in urine, the remaining volumes are excreted from the gallbladder.
Special cases and kinetics
Studies have been conducted that prove the absence of the effect of blood dialysis on the kinetic features of the pharmaceutical product. No dependence of the parameters on peritoneal dialysis or weakness of the kidneys in the form of a chronicle was revealed. If hepatic functioning is impaired, the clearance of the main active substance is reduced. If the functionality of the organ is severely impaired, it may be necessary to correct the amount of funds prescribed to the patient.
In elderly people, the average clearance is reduced by a third in comparison with a study of young people without serious diseases.
When will it help?
For indications for the use of Nifecard XL, you should refer to the instructions accompanying the product compiled by the manufacturer. It refers to the effectiveness of the drug in hypertension. It is recommended to prescribe a drug with stable angina pectoris. It can be used in various forms of the disease, including Prinzmetal angina.
Indications are vasospastic type, tension disease. You can use the drug with an unstable form of angina pectoris, if nitrates do not give a pronounced effect, treatment with beta-blockers is ineffective. You can use the product for Raynaud’s disease. Indications for the appointment are coronary arterial spasms that occur against the background of diagnosis or therapy, including angioplasty, bypass surgery.
The drug is used if it is necessary to organize differential diagnosis, when the patient is suspected of coronary aortic stenosis of an organic or functional form. The drug is effective for high blood pressure in a small circle of blood flow.
Dosage and rules of administration
The dosage regimen of "Nifecard XL" is determined by the doctor, based on the characteristics of the case, diagnosis, patient condition, tolerance to the body. The product is intended for oral use daily at a stable time. Each instance is swallowed without violating the integrity of the shell. It is forbidden to chew, crush, cut, otherwise grind tablets, as this leads to the loss of a number of important functional qualities. Do not drink the medicine with grapefruit juice.
The standard dose is one tablet per day. The tool is used daily in a copy. First, the patient is prescribed a drug in minimal form, that is, containing 30 mg of the active ingredient. If necessary, increase the dosage. Between changes in servings, a one-week or ten-day pause must be maintained. The daily maximum is 90 mg of the active ingredient.
With renal impairment, the dosage is standard. In case of liver failure, it is necessary to monitor the patient's condition, in order to notice the need for a dose reduction in time. In elderly people, it is possible to slow down elimination, which requires the use of a pharmaceutical product in a reduced volume that supports a person’s condition. In severe cerebrovascular pathologies, it is necessary to use the drug in the lowest possible dose. If there is a need for cancellation, the amount of product entering the body is reduced gradually.
Unwanted effects
Side effects of Nifecard XL include leuko-, thrombocytopenia, agranulocytosis, anemia, allergies, dizziness, hepatitis, dermatitis, and purple. Some had a headache, worried about paresthesia, stiffness of limb mobility, tremors, sleep problems, nightmares, decreased sexual activity. There may be visual malfunctions, ear ringing, swelling, vasodilation symptoms, a violation of the frequency, rhythm of the heartbeat.
Some complained of an increase in the sensation of heart contractions, while others recorded syncope, fainting, pain in the sternum and behind it. Possible nosebleeds, cough, pulmonary edema, bronchial spasm, infection of the airways. There are known cases of worsening stool, appetite. The stomach can hurt. There is a risk of dysphagia, gastric or intestinal erosion, impaired liver function.
It is noted that the hypotensive effect of the drug (as well as other positive effects of its administration) can be accompanied by negative phenomena, including gout, arthritis, convulsions, back pains. It is possible to change the volume of urine output per day, there is a danger of gynecomastia that disappears after the completion of the therapeutic program completely. Cases of hair loss, skin rashes, active sweating, asthenia, and weakness have been recorded. Some were bothered by general pains, chilled, feverish, swollen face, weight gain.
Sometimes you can’t
The contraindications indicated in the instructions for use of Nifecard XL include a severe condition of low blood pressure in the arteries, in which the systole is less than 90 units. You can not prescribe a pharmaceutical product for severe aortic valve stenosis, accompanied by clinically important blood flow disorders. In some cases, unstable angina pectoris becomes a contraindication. The drug is not prescribed if a decompensated weakness of the functioning of the heart muscle is recorded.
Contraindications to the appointment are cardiogenic shock, rifampicin, acute heart attack and the first four weeks after the peak state. You can not use a tablet product if a person suffers from rare genetic diseases, because of which the body does not tolerate lactose, lacks lactase. You can not prescribe a medicine for problems of assimilation of galactose, glucose. It is noted that the use of "Nifecard XL" during pregnancy in the first 20 weeks of gestation is strictly prohibited. The drug is not prescribed for lactating women.
The product is not used for the treatment of minors, since no experiments and trials have been organized to confirm the reliability of such treatment and the safety of using the product for this category of people. It is forbidden to prescribe the product to people whose body is too sensitive to nifedipine and other ingredients of the pharmaceutical product. Do not use if other sensitization products of 1,4-dihydropyridine transformation provoke a sensitization reaction.
Accuracy is the key to safety
It is noted that the agent under consideration, which has a reliable hypotensive effect, should be used very carefully if stenosis of the aortic orifice or mitral valve is detected. Certain risks are associated with cardiomyopathy with obstruction and hypertrophy. Careful monitoring of persons who are diagnosed with CVS, high blood pressure in a malignant form, cerebrovascular pathology is necessary. Strong tachycardia, insufficiency of the left heart ventricle with a heart attack, severe malfunctioning of the kidneys and liver are responsible for careful use. It is necessary to carefully prescribe the drug if the patient needs blood dialysis, since the risk of hypotension increases.
The drug is very carefully prescribed for diabetic disease, intestinal obstruction, patients receiving beta-blockers, drugs that inhibit CYP3A4 or induce this enzyme. Accuracy requires the use of glycosides for the heart. Very carefully and with constant monitoring of the condition, the pharmaceutical product is used to treat pregnant women if the gestation period is more than 20 weeks.
"Interesting" position: features of the reception
A variety of tests were conducted to show how nifedipine helps reliably how to use the product so as not to harm itself. At the same time, it has not yet been possible to organize specific controlled studies involving pregnant women. Scientific works involving animals indicate the feto-, embryotoxic effect of the drug, teratogenic qualities. This explains the impossibility of using the medicinal product before the 20th week of pregnancy.
The use of funds later than this period is allowed if among the diagnoses of the patient there is something that nifedipine helps with, while the benefit to the mother is obvious, and the risks to the fetus are minimal. If the first significantly exceeds the second, you can prescribe the use of the medication, transferring the needy to inpatient treatment. During the treatment course, you will have to constantly check the condition of the maternal and child organisms. Take blood pressure indicators, check the viability of the embryo, its degree of development. If deviations, anomalies are observed, the course is immediately stopped.
Since the product is able to penetrate the secret of the mammary glands, they do not use the drug during the period of feeding the baby. If it is impossible to avoid its use, stop natural feeding.
Reproductive function
Measures were organized to evaluate the effects of nifedipine (the main ingredient of Nifecard Chl tablets) and other drugs that inhibit slow calcium channels. Reversible changes in the biochemistry of sperm heads were found. Such corrections can cause the loss of sperm functionality. If a man has difficulty conceiving a child, the use of the drug should be evaluated as one of the possible provocative factors. The drug is regarded as the cause, if it is not possible to find other explanations for the problem.
The nuances of safe use
If it is necessary to cancel "Nifekard HL", the procedure is carried out slowly, gradually. At the beginning of the therapeutic course, an angina attack is possible. This is especially likely if beta-blockers have recently been abruptly stopped, which normally cease to be taken gradually. If you combine the use of the pharmaceutical product in question and beta-blockers, you need to remember the need to regularly check the health of the body. This combination can cause an excessive decrease in blood pressure in the arteries. In some cases, in the presence of weakness of the heart, it is possible to exacerbate the manifestations of this pathology.
If Nifecard XL is used against a background of severe cardiac weakness, you need to carefully select the dose. Sometimes in people with severe arterial coronary stenosis, at the beginning of the therapeutic course or with a dose increase, pain in the stomach became stronger, more often. Cases of heart attack are known.
In the case of vasospastic angina pectoris, the drug product under consideration is prescribed if the flow pattern is classical, the CT segment on the ECG is higher than normal, coronary arterial spasm is observed, or ergonovin-induced angina pectoris is recorded. Among the diagnostic criteria for the appointment are: coronary spasm during angiography, the growth of the angiospastic element.
Diagnoses and nuances of use
If cardiac myopathy is established, weighted by obstruction, hypertrophy, there is a risk of changes in angina attacks - they appear more often, proceed more heavily, last longer. This is possible after the start of the course of the drug "Nifecard XL". This course requires the withdrawal of the drug.
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Combination treatment
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Phenytoin induces the specified enzyme, reduces the bioavailability of nifedipine. At the same time, the effectiveness of the drug decreases. The combination of these two drugs requires a responsible assessment of the clinical effect and increase the dosage if the need arises to such an extent. If the dose of Nifecard XL is increased, take this into account when phenytoin is canceled.