Mechanism of action
Calcium channel blocker. It inhibits the flow of Calcium ions through the membrane of cardiomyocytes and vascular smooth muscles, which leads to a decrease in calcium accumulation inside the cells. This causes the expansion of the coronary arteries, peripheral blood vessels, which leads to a decrease in the OPSS and, consequently, reducing the load on the heart, increasing the supply of myocardium with oxygen. Reducing the work of the heart, the drug reduces the consumption of oxygen by the myocardium, and also indirectly reduces the need of the myocardium for oxygen by reducing OPS and afterload.
The inhibition of the intake and accumulation of calcium ions in cardiomyocytes prevents the depletion of myocardial energy reserves and provides a protective effect on the heart muscle.
Under the influence of the drug, blood pressure decreases, chest pain associated with myocardial hypoxia disappears or decreases. Due to the vasodilating effect on the coronary arteries, the poststenotic circulation is improved in atherosclerotic obstruction.
The release of Nifedipine from pills cordipin CL is very slow. The effect of the drug lasts 24 hours, so once a day is enough.
After initiation of therapy, the intensity of the hypotensive effect increases and reaches a stable state for 3-4 days, while the effect on chest pain reaches a plateau at 3-4 weeks.
Preferably, at the beginning of therapy, the heart rate and cardiac output may decrease as a result of the activation of the baroreceptors. With long-term therapy with nifedipine, the heart rate and cardiac output return to the values that they had before the start of therapy. In patients with arterial hypertension, a more pronounced decrease in blood pressure is observed.
Suction and distribution
The release of nifedipine from Cordipin CL pills is slow and almost linear, which ensures the effect of the drug during the day. After release, nifedipine is rapidly and almost completely absorbed from the gastrointestinal tract. Simultaneous food intake accelerates absorption.
When equilibrium is reached Cssmax nifedipine in the blood is noted after 5.0 ± 2.7 h.
Binding of nifedipine to plasma proteins - 94-99%.
Metabolism and excretion
Nifedipine is almost completely biotransformed in the body.
T1/2 is 14.9 ± 6 hours. Less than 1% of the dose is excreted in the urine unchanged, 70-80% of the dose is in the form of metabolites.
Pharmacokinetics in special clinical situations
With impaired renal function may increase T1/2.
Indications and usage
- arterial hypertension;
- stable angina (angina pectoris);
- angiospastic stenocardia.
Install individually.
The drug is prescribed in an average dose of 40 mg (1 tab.) 1 time / day, both at the beginning of therapy and with prolonged treatment.If necessary, increase the dose to a maximum of 80 mg (2 tab.) Per day in 1 or 2 doses.
If the patient has forgotten to take the next dose of the drug, the next dose should not double the dose.
In patients with impaired renal function, dose adjustment is usually not required.
Tablets should be taken whole, without breaking, with a glass of water.
Adverse reactions
Cardiovascular: possible headache, redness of the face, swelling of the ankles; rarely - orthostatic hypotension, cardiac arrhythmias, chest pain.
From the side of the central nervous system: rarely - dizziness, fatigue.
Gastrointestinal: rarely - nausea, heartburn, constipation, diarrhea, gingival hyperplasia.
Allergic reactions: rarely - skin rash, hives, itching.
Other: rarely, muscle cramps.
Contraindications
- cardiogenic shock;
- porphyria;
- severe aortic stenosis;
- arterial hypotension;
- collapse;
- severe heart failure in the stage of decompensation;
- acute myocardial infarction;
- pregnancy;
- lactation (breastfeeding);
- children's and teenage age up to 18 years;
- hypersensitivity to nifedipine and other components of the drug;
- Hypersensitivity to dihydropyridines.
Pregnancy and breastfeeding
To date, the safety of use cordipin CL in pregnancy has not been established, and therefore the drug is not recommended to use.
Nifedipine is excreted in breast milk, so if you need to use the drug during lactation should stop breastfeeding.
Special notes
At the beginning of treatment with cordipin CL, especially with simultaneous use of beta-blockers, arterial hypotension is possible, which some patients do not tolerate well. In such cases, patients require careful monitoring.
In patients taking beta-blockers, at the beginning of treatment may develop congestive heart failure.
Observation by a physician, especially at the beginning of treatment, is required for patients with myocardial infarction in patients with hypertrophic cardiomyopathy, unstable angina, diabetes, severe liver disease, and pulmonary hypertension, as well as elderly patients.
During treatment with cordipin CL in patients with acute coronary insufficiency, due to reflex tachycardia, worsening of the course of coronary artery disease (more frequent strokes) is possible.
Reception of cordipin CL should be stopped 36 hours before the planned anesthesia using fentanyl.
Cordipin CL is not recommended for patients with lactase deficiency, galactosemia and impaired glucose / galactose absorption syndrome.
If necessary, an inhalation test with methacholine to determine bronchial hyperreactivity should take into account that the patient is taking cordipin CL.
In the period of treatment should be avoided the use of grapefruit juice and alcohol.
If it is necessary to stop therapy, the dose is reduced gradually, since with a sudden cessation of the use of the drug (especially after long-term treatment), withdrawal syndrome may develop. In patients with arterial hypertension after discontinuation of the drug may increase blood pressure.
The physician should inform the patient about the desired level of blood pressure and pulse rate; if after taking the first dose of cordipin CL there is pain or a feeling of pressure in the chest, then a doctor should be consulted before taking the next dose; If during the reception of cordipin CL, more frequent, severe and prolonged chest pain occurs both at rest and during physical exertion, consultation with a doctor is also required.
Control of laboratory parameters
With the use of nifedipine, changes in alkaline phosphatase, ALT, AST, LDH are possible; there is a positive Coombs reaction without clinical manifestations, although in some cases cholestasis and jaundice were observed.
Against the background of nifedipine, there is a decrease in the number of platelets and an increase in bleeding time, which has no clinical significance.
Use in pediatrics
Safety and efficacy of cordipin CL in children have not been established.
Influence on ability to drive motor transport and control mechanisms
In some patients, especially at the beginning of treatment, the drug may cause dizziness, which is reversible.Therefore, until an individual patient’s response to treatment is established, one should refrain from driving and practicing other potentially dangerous activities.
Overdosage
Symptoms: excessive hypotension; When taking a large number of pills, tachycardia, bradycardia, arrhythmia, nausea, vomiting, weakness, redness of the skin, dizziness, drowsiness, lethargy, color perception disorders, metabolic acidosis, convulsions, loss of consciousness may occur.
Treatment: if the patient is conscious, induce vomiting. Careful observation of the hemodynamic state, symptomatic therapy is necessary.
Drug Interactions
With simultaneous use of cordipin CL with other antihypertensive drugs, beta-blockers, diuretics, Nitroglycerin and isosorbide mononitrate or long-acting dinitrate, a synergistic effect on blood pressure is observed.
With simultaneous use cordipin CL and fentanyl may further decrease blood pressure.
With the simultaneous use of cordipin CL with cimetidine, tricyclic antidepressants, Ranitidine , it is possible to enhance the antihypertensive effect of nifedipine.
Rifampicin induces the activity of liver enzymes, accelerating the metabolism of nifedipine, which leads to a decrease in the effectiveness of the latter.
With simultaneous use with calcium preparations, the therapeutic efficacy of cordipin CL decreases.
Pharmacokinetic interaction
With simultaneous use of cordipin CL and Digoxin , Carbamazepine , phenytoin and theophylline, there is an increase in the concentrations of the latter in the blood plasma.
With simultaneous use of cordipin CL and quinidine, there is a decrease in the concentration of the latter in the blood plasma.
The drug should be stored at a temperature not higher than 25 ° C. Do not use after the expiration date printed on the package.
Pharmacy sales terms
The drug is available on prescription.
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