Nifedipine - instructions for use, analogs, reviews and release forms (tablets and pills 10 mg, retard or prolonged 20 mg, capsules 5 mg and 10 mg) of the drug for the treatment of angina and depression in adults, children and pregnancy

In this article, you can read the instructions for using the drug Nifedipine. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Nifedipine in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Nifedipine in the presence of existing structural analogs.Use to treat angina and reduce pressure in adults, children, as well as during pregnancy and lactation.

Nifedipine - selective blocker of "slow" calcium channels, derivative of 1,4-dihydropyridine. Has vasodilating, antianginal and antihypertensive action. Reduces the current of calcium ions in cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses, suppresses the release of calcium ions from the intracellular depot. Reduces the number of functioning channels, without affecting the time of their activation, inactivation and recovery.

Separates the processes of excitation and contraction in the myocardium mediated by tropomyosin and troponin, and in smooth muscles of vessels, mediated by calmodulin. In therapeutic doses normalizes the transmembrane current of calcium ions, disrupted in a number of pathological conditions, especially in hypertension. Does not affect the tone of the veins. Strengthens the coronary blood flow, improves the blood supply of the ischemic zones of the myocardium without the development of the phenomenon of "stealing", activates the functioning of collaterals.Expanding the peripheral arteries, reduces the overall peripheral resistance of the vessels, myocardial tone, postload, the need for myocardium in oxygen and prolongs the duration of diastolic relaxation of the left ventricle. Virtually does not affect the sinoatrial and atrioventricular nodes and does not have antiarrhythmic activity. It enhances kidney blood flow, causes a moderate natriuresis. Negative chrono-, dromo- and inotropic action is blocked by reflex activation of the sympathoadrenal system and an increase in heart rate in response to peripheral vasodilation.

The time of the onset of the effect is 20 minutes, the duration of the effect is 12-24 hours.

Composition

Nifedipine + excipients.

Pharmacokinetics

Absorption is high (more than 92-98%). Bioavailability is 40-60%. Eating increases bioavailability. Has the effect of "first pass" through the liver. Retard forms provide a gradual release of the active substance into the systemic bloodstream. Penetrates through the blood-brain barrier (GEB) and the placental barrier, excreted in breast milk. It is completely metabolized in the liver. It is excreted as inactive metabolites, mainly by the kidneys (80%) and bile (20%).

Indications

• chronic stable angina (stress angina);
• vasospastic angina (Prinzmetal angina);
• Arterial hypertension (in monotherapy or in combination with other antihypertensive agents);
• disease and Reynaud's syndrome.

Forms of release

Dragee 10 mg.

Tablets 10 mg.

Tablets of prolonged action (retard), film-coated 20 mg.

Capsules 5 mg and 10 mg.

Instructions for use and dosage

Dragee or tablets

The dosage regimen is set individually, depending on the degree of severity of the disease and the patient's response to ongoing therapy. It is recommended to take the drug during or after a meal, with a small amount of water.

Initial dose: 1 tablet (tablet) (10 mg) 2-3 times a day. If necessary, the dose of the drug can be increased to 2 tablets or dragees (20 mg) - 1-2 times a day.

The maximum daily dose is 40 mg.

In elderly patients or patients receiving combined (antianginal or antihypertensive) therapy, as well as in violation of liver function, in patients with severe impairment of cerebral circulation, the dose should be reduced.

Retard tablets

Inside. Tablets should be swallowed whole, without chewing, during or after a meal, with a small amount of water.

The recommended dose of the drug is 20 mg twice a day.If the effect is insufficient, it is possible to increase the dose to 40 mg twice a day. The maximum daily dose is 80 mg.

If the liver function is impaired, the daily dose should not exceed 40 mg.

In elderly patients or patients receiving combined (antianginal or antihypertensive) therapy, smaller doses are usually given.

Duration of treatment is determined in each case individually.

Side effect

• peripheral edema (feet, ankles, legs);
• symptoms of vasodilation (redness of the face, sensation of heat);
• tachycardia;
• cardiopalmus;
• marked decrease in blood pressure;
• fainting;
• pain behind the sternum (angina pectoris) until the development of myocardial infarction;
• development or aggravation of the course of chronic heart failure;
• arrhythmias;
• headache;
• dizziness;
• drowsiness;
• asthenia;
• nervousness;
• increased fatigue;
• tremor;
• mood lability;
• nausea;
• pain in the stomach and intestines;
• diarrhea;
• constipation;
• dryness of the oral mucosa;
• increased appetite;
• dyspnea;
• swelling of the lungs (difficulty breathing, coughing, breathy breathing);
• swelling of the joints;
• myalgia;
• muscle cramps;
• anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura, agranulocytosis;
• impairment of renal function (in patients with renal insufficiency);
• itching;
• hives;
• photosensitization;
• angioedema;
• toxic epidermal necrolysis;
• visual impairment (including transient loss of vision against the background of the maximum concentration of nifedipine in blood plasma);
• Pain in the eyes;
• gynecomastia (in elderly patients, completely disappearing after drug withdrawal);
• galactorrhea;
• erectile disfunction;
• increase in body weight;
• chills;
• nose bleed;
• nasal congestion.

Contraindications

• arterial hypotension (systolic blood pressure below 90 mmHg);
• cardiogenic shock;
• collapse;
• pronounced aortic or subaortic stenosis;
• acute heart failure;
• chronic heart failure in the stage of decompensation;
• unstable angina;
• acute period of myocardial infarction (within the first 4 weeks);
• hypertrophic obstructive cardiomyopathy;
• syndrome of weakness of the sinus node;
• AV-blockade of 2-3 degrees;
• pregnancy (up to 20 weeks);
• lactation period;
• age under 18 years (efficacy and safety of use not investigated);
• hypersensitivity to nifedipine or other components of the drug.

Application in pregnancy and lactation

Controlled studies of the use of Nifedipine in pregnant women have not been conducted.

Tests in animals showed the presence of embryotoxicity, placental toxicity, fetotoxicity and teratogenicity when taking nifedipine during and after the organogenesis period.

According to available clinical data, it is impossible to judge the specific perinatal risk. At the same time, there are data on the increase in the probability of perinatal asphyxia, cesarean section, premature birth and intrauterine growth retardation. It is unclear whether these cases are the result of a major illness (hypertension), treatment or a specific effect of Nifedipine. The information available is insufficient to exclude the possibility of side effects, which are dangerous for the fetus and the newborn. Therefore, the use of Nifedipine after the 20th week of pregnancy requires a careful individual assessment of the risk-benefit relationship for the patient,fetus and / or newborn and can be considered only in cases where other methods of therapy are contraindicated or ineffective.

Careful monitoring of blood pressure in pregnant women with Nifedipine should be carried out simultaneously with the intravenous administration of magnesium sulfate due to the possibility of excessive reduction in blood pressure, which is dangerous for both the mother and the fetus and / or the newborn.

Nifedipine is contraindicated in the lactation period, since it is excreted in breast milk. If Nifedipine therapy is absolutely necessary, it is recommended to stop breastfeeding.

Use in children

Contraindicated in children under 18 years.

special instructions

During the treatment it is necessary to refrain from drinking alcohol.

Despite the lack of "slow" calcium channels of the syndrome of "cancellation" in blockers, a gradual decrease in doses is recommended before cessation of treatment.

Simultaneous prescribing of beta-blockers should be carried out under conditions of careful medical supervision, as this can lead to an excessive decrease in blood pressure, and in some cases, an aggravation of the phenomena of heart failure.During treatment, positive results are possible with a direct Coombs reaction and laboratory tests for antinuclear antibodies.

It is important that the regularity of treatment is independent of the state of health, since the patient may not feel the symptoms of hypertension.

Diagnostic criteria for the prescription of the drug for vasospastic angina are: classical, clinical picture, accompanied by characteristic changes in the electrocardiogram (elevation of the ST segment); the occurrence of ergometrine-induced angina or spasm of the coronary arteries; the detection of coronarospasm in angiography or the detection of an angiospastic component without confirmation (for example, with a different voltage threshold or with unstable angina, when the electrocardiogram data indicate a transient angiospasm).

For patients with severe hypertrophic cardiomyopathy, there is a risk of increased frequency, severity and duration of angina attacks after taking nifedipine; in this case, it is necessary to cancel the drug.

In patients who are on hemodialysis, with high blood pressure, irreversible failure of kidney function, with a decrease in the volume of circulating blood, the drug should be used cautiously, as there may be a sharp fall in blood pressure.

Patients with impaired liver function are carefully monitored and, if necessary, reduce the dose of the drug and / or use other dosage forms of nifedipine.

It should be borne in mind that at the beginning of treatment can occur angina, especially after the recent abrupt abolition of beta-blockers (the latter is recommended to cancel gradually).

If during the therapy the patient is required to undergo surgery under general anesthesia, it is necessary to inform the anesthesiologist about the nature of the therapy.

With in vitro fertilization, in some cases, blockers of "slow" calcium channels caused changes in the head part of spermatozoa, which could lead to a disruption of the functions of spermatozoa. In cases in which repeated in vitro fertilization was not carried out for an unclear reason, blockers of "slow" calcium channels,including nifedipine, were considered a possible cause of failure.

Impact on the ability to drive vehicles and manage mechanisms

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Drug Interactions

The severity of lowering blood pressure is enhanced by the simultaneous use of nifedipine with other antihypertensive drugs, nitrates, cimetidine, Ranitidine (to a lesser extent), inhalational anesthetics,

diuretics and tricyclic antidepressants.

Under the influence of nifedipine, the concentration of quinidine in the blood plasma is significantly reduced. Increases the concentration of Digoxin in the blood plasma, and therefore it is necessary to monitor the clinical effect and the content of digoxin in the blood plasma.

Rifampicin is a powerful inducer of isoenzyme СUR3А4. When combined with rifampicin, the bioavailability of nifedipine is significantly reduced and, accordingly, its effectiveness decreases. The use of nifedipine in conjunction with rifampicin is contraindicated.In combination with citrates, tachycardia and antihypertensive effects of nifedipine are enhanced. Calcium preparations can reduce the effect of blockers of "slow" calcium channels. When combined with nifedipine, anticoagulant activity of coumarin derivatives increases.

Drugs that are characterized by a high degree of binding (including indirect anticoagulants - coumarin and indanedione derivatives, anticonvulsant drugs, quinine, salicylates, sulfinpyrazone) can be dislodged from the bond with proteins, so that their concentrations in the blood plasma can increase. Suppresses the metabolism of prazosin and other alpha-adrenoblockers, as a result of which the antihypertensive effect may increase.

Procainamide, quinidine, and other drugs that cause prolongation of the QT interval increase the negative inotropic effect and may increase the risk of a significant prolongation of the QT interval.

Simultaneous use with magnesium sulfate in pregnant women can cause blockade of neuromuscular synapses.

Inhibitors of the cytochrome P450 3A system, such as macrolides (eg, erythromycin), fluoxetine, nefazodone, protease inhibitors (eg, amprenavir, indinavir,nelfinavir, ritonavir or saquinavir), antifungal agents (ketoconazole, Itraconazole or fluconazole) lead to an increase in the concentration of nifedipine in the blood plasma. Taking into account the experience of using the blocker of the "slow" calcium channels of nimodipine, the following interactions with nifedipine can not be excluded: carbamazepine, Phenobarbital - a decrease in the concentration of nifedipine in the blood plasma; quinupristin, dalfopristin, valproic acid - an increase in the concentration of nifedipine in blood plasma.

Caution should be given nifedipine simultaneously with disopyramide and flecainide because of the possible increase in inotropic effect.

Nifedipine inhibits the excretion of vincristine from the body and can cause an increase in its side effects; if necessary, reduce the dose of vincristine.

Grapefruit juice inhibits the metabolism of nifedipine in the body, and therefore contraindicated in their simultaneous reception.

Analogues of the drug Nifedipine

Structural analogs for the active substance:

• Adalate;
• Vero Nifedipine;
• Calzigard retard;
• Kordafen;
• Cordaflex;
• Cordaflex RD;
• Cordipine;
• Cordipine XL;
• Cordipine retard;
• Corinfar;
• Corinfar retard;
• Corinfar OOE;
• Nicardy;
• Nykardija SD retard;
• Nyfadil;
• Nifébyen;
• Nifhexal;
• Nifedex;
• Nifedikap;
• Nifedikor;
• Nifecard;
• Nifecard HL;
• Nifelate;
• Nifelat Q;
• Nifelat R;
• Nifesan;
• Osmo Adalat;
• Sanfidipine;
• Sponify 10;
• Phenigidine.

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