Instructions for use of NIFECARD® XL (NIFECARD® XL)

Release form and composition

The drug is available in the form of modified-release, film-coated tablets: biconvex, round, light brownish-yellow to light brownish-orange in color, with a yellow core visible on the break, the inscription corresponding to the dosage is embossed on one side, for 30 mg - “NDP 30”, for 60 mg – “NDP 60” (10 pieces in blisters, in a cardboard pack of 2, 3 or 6 blisters and instructions for use of Nifecard CL).

Composition per 1 modified-release film-coated tablet:

• active ingredient: nifedipine – 30 mg or 60 mg;
• auxiliary components of the tablet core: sodium lauryl sulfate, magnesium hydrosilicate, povidone, hydroxypropyl methylcellulose (for 30 mg tablets), hydroxypropyl methylcellulose 2906 and hydroxypropyl methylcellulose 2208 (for 60 mg tablets), magnesium stearate, Ludipress (crospovidone, povidone and lactose monohydrate);
• film shell: macrogol, hypromellose phthalate, magnesium hydrosilicate, triethyl citrate, titanium dioxide, hydroxypropylcellulose, hydroxypropylmethylcellulose 2910, yellow iron oxide dye.

Nifecard

Active substance:

Nifedipine*

Pharmgroup:

Calcium channel blockers

Pharmacological properties

Pharmacodynamics

Nifedipine is a selective blocker of slow calcium channels, and according to its chemical structure it belongs to 1,4-dihydropyridine derivatives. It has antihypertensive and antianginal effects. The drug reduces the flow of extracellular calcium into smooth muscle cells of peripheral and coronary arteries, as well as cardiomyocytes; in large doses inhibits the release of Ca2+ from intracellular stores. Nifecard CL reduces the total number of functioning calcium channels, but does not affect the time of their activation, restoration and inactivation.

Nifecard CL uncouples the processes of contraction and excitation in the cardiac muscle (mediated by troponin and tropomyosin) and in the smooth muscles of blood vessels (mediated by calmodulin). In therapeutic doses, the drug normalizes the flow of calcium ions through cell membranes, which is disrupted due to certain pathological conditions (mainly due to arterial hypertension). Nifedipine has no effect on venous tone; it improves blood supply to ischemic lesions of the heart muscle without the development of vertebral-subclavian steal syndrome (VSS), enhances blood circulation through the blood vessels of the myocardium, and activates the functioning of reserve blood pathways.

The drug reduces the force of heart contractions, improves myocardial function and reduces its need for oxygen. Due to the expansion of peripheral arteries, blood pressure (blood pressure) decreases, total peripheral resistance decreases and the afterload on the heart decreases. Nifecard CL has almost no effect on the atrioventricular and sinoatrial nodes; increases blood flow in the renal arteries and veins; moderately increases sodium excretion in urine.

The drug has an antiatherogenic effect (especially with long-term therapy), inhibits platelet aggregation; has a positive effect on cerebral blood supply; reduces pressure in the pulmonary artery.

Pharmacokinetics

Due to the delayed release of the active substance Nifecard CL, its plasma concentration increases gradually and reaches a plateau approximately 6 hours after oral administration. After which it is maintained at this level for 24 hours (with minor fluctuations).

As a result of taking the drug orally, nifedipine is quickly and almost completely absorbed in the gastrointestinal tract (absorbed from 92 to 98%). The binding to plasma proteins is about 90%. Metabolism occurs in the liver, active metabolites have not been established. The half-life is approximately 2 hours. The main part of the drug is excreted by the kidneys (80%) and a small amount (about 20%) is excreted in the bile (the drug is excreted in the form of inactive metabolites). No cumulative effect was found.

Nifedipine crosses the placental and blood-brain barriers and is also secreted into breast milk.

In patients with chronic renal failure, as well as in persons on peritoneal dialysis or hemodialysis, changes in pharmacokinetics have not been recorded.

In case of impaired liver function, the clearance of nifedipine is reduced, therefore, in case of severe impairment of hepatic function, a change in the dose of Nifecard CL may be required.

In elderly patients, with intravenous administration of nifedipine, a decrease in its clearance by 33% was observed (compared to healthy younger volunteers).

Long-term drug therapy can lead to addiction.

Instructions:

Clinical and pharmacological group

01.015 (Calcium channel blocker)

Release form, composition and packaging

Controlled-release, light brownish-yellow to light brownish-orange, film-coated tablets, round, biconvex, with "NDP 30" embossed on one side.

Excipients: povidone, sodium lauryl sulfate, hypromellose (hydroxypropyl methylcellulose), ludipress (a mixture of lactose monohydrate, povidone, crospovidone), talc (magnesium hydrosilicate), magnesium stearate.

Shell composition: hypromellose phthalate (hydroxypropyl methylcellulose phthalate), triethyl citrate, hypromellose (hydroxypropyl methylcellulose), hyprolose (hydroxypropylcellulose), macrogol (polyethylene glycol), talc (magnesium hydrosilicate), titanium dioxide, iron oxide yellow dye.

10 pieces. - blisters (2) - cardboard packs. 10 pcs. - blisters (3) - cardboard packs.

Light brownish-yellow to light brownish-orange, controlled-release, film-coated tablets, round, biconvex, with "NDP 60" embossed on one side.

Excipients: povidone, sodium lauryl sulfate, hypromellose (hydroxypropyl methylcellulose), ludipress (a mixture of lactose monohydrate, povidone, crospovidone), talc (magnesium hydrosilicate), magnesium stearate.

Shell composition: hypromellose phthalate (hydroxypropyl methylcellulose phthalate), triethyl citrate, hypromellose (hydroxypropyl methylcellulose), hyprolose (hydroxypropylcellulose), macrogol (polyethylene glycol), talc (magnesium hydrosilicate), titanium dioxide, iron oxide yellow dye.

10 pieces. - blisters (3) - cardboard packs.

pharmachologic effect

Selective blocker of slow calcium channels, 1,4-dihydropyridine derivative. Has antianginal and hypotensive effects. Reduces the flow of extracellular calcium into cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses inhibits the release of calcium ions from intracellular stores. Reduces the number of functioning channels without affecting the time of their activation, inactivation and recovery.

It uncouples the processes of excitation and contraction in the myocardium, mediated by tropomyosin and troponin, and in vascular smooth muscles, mediated by calmodulin. In therapeutic doses, it normalizes the transmembrane current of calcium ions, which is disturbed in a number of pathological conditions, primarily in arterial hypertension. Does not affect the tone of the veins. Strengthens coronary blood flow, improves blood supply to ischemic areas of the myocardium without developing the “steal” phenomenon, and activates the functioning of collaterals.

Improves myocardial function, reduces the force of heart contractions and myocardial oxygen demand. By expanding peripheral arteries, it lowers blood pressure and reduces peripheral vascular resistance and afterload on the heart. Almost no effect on the sinoatrial and AV nodes. Increases renal blood flow, causes moderate natriuresis.

Inhibits platelet aggregation and has antiatherogenic properties (especially with long-term use). Reduces pressure in the pulmonary artery and has a positive effect on the blood supply to the blood vessels of the brain.

Pharmacokinetics

Suction and distribution

After oral administration, nifedipine is almost completely absorbed (92-98%).

Due to the delayed release of the active substance, a gradual, controlled increase in plasma concentrations of nifedipine is ensured. Plasma concentrations of nifedipine reach a plateau after approximately 6 hours and are maintained with minor fluctuations for 24 hours.

Binding to blood plasma proteins is 90%.

Penetrates through the BBB and placental barrier, excreted in breast milk.

There is no cumulative effect.

Metabolism

Metabolized in the liver. No active metabolites were identified.

Removal

T1/2 of nifedipine is approximately 2 hours. It is excreted mainly in the form of inactive metabolites in the urine (80%) and bile (20%).

Pharmacokinetics in special clinical situations

Chronic renal failure, hemodialysis and peritoneal dialysis do not affect the pharmacokinetics of nifedipine.

The clearance of nifedipine is reduced in patients with impaired liver function.

Dosage

The initial dose of the drug is 30 mg 1 time / day. If necessary, the dose is gradually increased at intervals of 7-14 days.

The average daily dose of the drug is 30 mg or 60 mg. The maximum daily dose is 90 mg.

The tablets should be taken whole, without breaking or chewing.

Overdose

An overdose of Nifecard CL causes peripheral vasodilation with severe and possibly prolonged systemic arterial hypotension (headache, flushing of the facial skin, prolonged pronounced decrease in blood pressure, depression of the sinus node, bradycardia and/or tachycardia, bradyarrhythmia); in severe cases - loss of consciousness, coma.

Treatment: administration of activated carbon, gastric lavage, restoration of stable hemodynamic parameters, careful monitoring of the activity of the heart, lungs and excretory system. Due to the high degree of binding to plasma proteins, hemodialysis is not effective. Calcium preparations are antidotes. The clearance of nifedipine is reduced in patients with impaired liver function.

Drug interactions

With simultaneous use of nifedipine with other antihypertensive drugs, beta-blockers, nitrates, cimetidine (to a lesser extent ranitidine), inhalational anesthetics, diuretics and tricyclic antidepressants, an increase in antihypertensive effect is observed.

With the simultaneous use of nifedipine and quinidine, the concentration of the latter in the blood plasma decreases; after discontinuation of nifedipine, a sharp increase in the concentration of quinidine may occur.

With the simultaneous use of nifedipine with digoxin or theophylline, the concentrations of the latter in the blood plasma increase, and therefore the clinical effect and the content of digoxin and theophylline in the blood plasma should be monitored.

Inducers of microsomal liver enzymes (including rifampicin), when used simultaneously with nifedipine, reduce the concentration of nifedipine.

With simultaneous use of nifedipine with nitrates, tachycardia increases.

The antihypertensive effect of nifedipine is reduced by sympathomimetics, NSAIDs, estrogens, and calcium supplements.

Nifedipine can displace drugs characterized by a high degree of binding from protein binding (including indirect anticoagulants derived from coumarin and indanedione, anticonvulsants, NSAIDs, quinine, salicylates, sulfinpyrazone), as a result of which their concentration in the blood plasma may increase while simultaneously use with nifedipine.

Nifedipine inhibits the elimination of vincristine from the body and may cause increased side effects of vincristine; if necessary, the dose of vincristine is reduced.

Nifedipine may enhance the toxic effects of lithium preparations (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

With the simultaneous administration of cephalosporins (for example, cefixime) and nifedipine, the bioavailability of cephalosporin increases by 70%.

Grapefruit juice suppresses the metabolism of nifedipine in the body, and therefore their simultaneous use is contraindicated.

Use during pregnancy and lactation

The use of Nifecard CL in the second and third trimesters of pregnancy is indicated only if the expected benefit to the mother outweighs the potential risk to the fetus.

Nifedipine is excreted in breast milk, therefore, when prescribing Nifecard CL during lactation, breastfeeding must be stopped.

Side effects

From the cardiovascular system: manifestations of excessive vasodilation (asymptomatic decrease in blood pressure, a feeling of flushing of the facial skin, flushing of the facial skin, a feeling of heat), tachycardia, palpitations, arrhythmia, peripheral edema, chest pain; rarely - excessive decrease in blood pressure, fainting, syncope; In some patients, especially at the beginning of treatment, angina attacks may occur, which requires discontinuation of the drug. Isolated cases of myocardial infarction have been described.

From the side of the central nervous system: headache, dizziness, increased fatigue, weakness, drowsiness; with long-term use in high doses - paresthesia of the limbs, depression, anxiety, extrapyramidal (parkinsonian) disorders (ataxia, mask-like face, shuffling gait, stiffness in the movements of the arms and legs, tremor of the hands and fingers, difficulty swallowing).

On the part of the organ of vision: very rarely - visual impairment (including transient blindness at the maximum concentration of nifedipine in the blood plasma).

From the digestive system: dry mouth, loss of appetite, dyspepsia (nausea, diarrhea or constipation); rarely - gum hyperplasia (bleeding, pain, swelling); with long-term use - liver dysfunction (intrahepatic cholestasis, increased activity of liver transaminases).

From the hematopoietic organs: anemia, asymptomatic agranulocytosis, thrombocytopenia, thrombocytopenic purpura, leukopenia.

From the musculoskeletal system: arthritis; rarely - arthralgia, swelling of the joints, myalgia, convulsions of the upper and lower extremities.

From the urinary system: increased daily diuresis, deterioration of renal function (in patients with renal failure).

From the respiratory system: rarely - difficulty breathing, cough; very rarely - pulmonary edema, bronchospasm.

From the endocrine system: very rarely - gynecomastia (in elderly patients, completely disappearing after discontinuation of the drug), hyperglycemia, galactorrhea, weight gain.

Allergic reactions: rarely - skin itching, exanthema, exfoliative dermatitis, photodermatitis; very rarely - autoimmune hepatitis.

Storage conditions and periods

The drug should be stored out of the reach of children at a temperature not exceeding 25°C. Shelf life: 3 years. Do not use after the expiration date stated on the packaging.

Indications

- arterial hypertension;

— IHD: stable angina pectoris, angiospastic angina (Prinzmetal angina).

Contraindications

- severe stenosis of the aortic valve;

— severe arterial hypotension (systolic blood pressure below 90 mm Hg);

— chronic heart failure in the stage of decompensation;

— cardiogenic shock (risk of myocardial infarction);

- acute period of myocardial infarction (during the first 4 weeks);

— I trimester of pregnancy;

- lactation period;

- hypersensitivity to nifedipine, components of the drug and other 1,4-dihydropyridine derivatives.

The drug should be prescribed with caution in cases of severe stenosis of the aortic orifice or mitral valve, hypertrophic obstructive cardiomyopathy, severe tachycardia, SSSS, malignant arterial hypertension, myocardial infarction with left ventricular failure, unstable angina, simultaneous administration of beta-blockers or cardiac glycosides, simultaneous use of rifampicin, severe cerebrovascular accidents, liver and/or kidney dysfunction, during hemodialysis (risk of arterial hypotension), patients under 18 years of age (efficacy and safety have not been established).

special instructions

Nifecard® CL should be discontinued gradually.

It should be borne in mind that at the beginning of treatment with Nifecard HL, angina pectoris may occur, especially after the recent abrupt withdrawal of beta-blockers (the latter should be withdrawn gradually).

The simultaneous administration of beta-blockers must be carried out under conditions of careful medical supervision, as this may cause an excessive decrease in blood pressure, and in some cases, aggravation of symptoms of heart failure.

In case of severe heart failure, the drug is dosed with great caution.

The diagnostic criteria for prescribing the drug for vasospastic angina are: the classic clinical picture, accompanied by an increase in the ST segment, the occurrence of ergonovine-induced angina or coronary artery spasm, the detection of coronary spasm during angiography or the identification of an angiospastic component without confirmation (for example, with a different voltage threshold or with unstable angina, when ECG data indicate transient vasospasm).

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

Nifecard® CL should be used with caution in patients on hemodialysis with high blood pressure and irreversible renal failure with a reduced total blood volume, because A sharp drop in blood pressure may occur.

When prescribing Nifecard CL to patients with impaired liver function, it is necessary to establish careful medical supervision and, if necessary, reduce the dose of the drug and/or use other dosage forms of nifedipine.

If during treatment with Nifecard CL the patient requires surgery under general anesthesia, it is necessary to inform the anesthesiologist about the nature of the therapy being performed.

During treatment, positive results are possible with direct Coombs test and laboratory tests for antinuclear antibodies.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, care must be taken when engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Use for renal impairment

The drug should be prescribed with caution in case of impaired renal function or during hemodialysis (risk of arterial hypotension).

Use for liver dysfunction

The drug should be prescribed with caution in case of liver dysfunction.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Contraindications

Absolute:

• unstable angina;
• severe arterial hypotension (with systolic blood pressure less than 90 mmHg);
• cardiogenic shock (due to the risk of myocardial infarction);
• CHF (chronic heart failure) in the stage of decompensation;
• myocardial infarction in the acute stage (during the first 4 weeks after the attack);
• severe aortic valve stenosis (with hemodynamic disturbances);
• lactase deficiency, hereditary lactose intolerance, glucose-galactose malabsorption syndrome (due to lactose in the tablets);
• children and adolescents up to 18 years of age;
• pregnancy period (up to the 20th week);
• lactation period;
• co-administration with rifampicin;
• hypersensitivity to the main or auxiliary components of the drug, as well as other drugs from the group of 1,4-dihydropyridine derivatives.

Relative (Nifecard XL tablets are used with caution):

• severe tachycardia;
• myocardial infarction with left ventricular failure;
• mitral valve or aortic stenosis;
• malignant arterial hypertension;
• cerebrovascular diseases;
• hypertrophic obstructive cardiomyopathy;
• SSS (sick sinus syndrome);
• diabetes;
• impaired renal and/or liver function;
• intestinal obstruction;
• hemodialysis (due to the risk of developing arterial hypotension);
• co-administration with cardiac glycosides, beta-blockers, inhibitors or inducers of the CYP3A4 isoenzyme.

Nifecard HL, instructions for use: method and dosage

Nifecard HL tablets are taken orally without chewing. They should not be divided or crushed, nor should they be washed down with grapefruit juice. The dosage regimen for the drug is individual, but it is advisable to take it at the same time of the day.

The recommended dose is 1 tablet (Nifecard CL 30 mg or 60 mg) once a day. The initial dose is 30 mg per day, then it is gradually increased to 60 mg per day (the interval between dose increases should be from 7 to 14 days). The maximum dose of nifedipine is 90 mg per day.

In elderly patients, the elimination of nifedipine may be slower, so they should be prescribed lower maintenance doses.

In case of impaired renal function, no adjustment of the daily dose is required, and in patients with impaired liver function and severe cerebrovascular diseases, a reduction in the initial and maintenance doses of Nifecard CL may be required.

It is recommended to gradually discontinue Nifecard CL with a gradual dose reduction.

Side effects

• digestive system: often – constipation; uncommon – loss of appetite, abdominal pain, dyspeptic disorders (diarrhea, nausea), dry oral mucosa; rarely – pain, bleeding and swelling of the gums; with unknown frequency - insufficiency of the gastroesophageal sphincter, vomiting, erosive and ulcerative lesions of the intestinal mucosa, swallowing disorder, with long-term treatment - formation of lumps from the remains of undigested food in the stomach, impaired liver function (jaundice, increased activity of liver enzymes, intrahepatic cholestasis );
• metabolism and nutrition: with unknown frequency – increase in blood sugar;
• respiratory system: uncommon – cough, difficulty breathing, nosebleeds, sinusitis, nasal congestion, upper respiratory tract infections; with unknown frequency - bronchospasm, shortness of breath, pulmonary edema;
• cardiovascular system: often - flushing of the facial skin, asymptomatic decrease in blood pressure, feeling of heat, flushing of the facial skin, peripheral edema; infrequently - palpitations, excessive decrease in blood pressure (especially in patients on hemodialysis who have a reduced circulating blood volume and malignant hypertension), fainting or fainting, tachycardia; very rarely - attacks of angina (especially at the beginning of treatment), requiring discontinuation of Nifecard CL; isolated cases - myocardial infarction; with unknown frequency - worsening of heart failure, chest pain;
• nervous system: often – headache; infrequently – migraine, tremor, dizziness, increased fatigue; rarely - perversion of susceptibility in the extremities; with unknown frequency - with long-term therapy in large doses - anxiety, increased excitability, depression, sleep disorders (including insomnia and nightmares), extrapyramidal disorders [tremor of the fingers and hands, drowsiness, shuffling gait, decreased sensitivity to real stimuli, ataxia, difficulty swallowing, mask-like (amimic) face, stiffness of leg and arm movements], decreased libido;
• sense organs: infrequently – taste disturbance, transient visual impairment, ringing in the ears; with unknown frequency – pain in the eye area;
• musculoskeletal system: infrequently - swelling of the joints, gout, cramps of the lower and upper extremities, back pain; with unknown frequency – pain in muscles or joints, arthritis;
• lymphatic system and blood: with unknown frequency - decreased platelet and leukocyte counts, agranulocytosis, anemia;
• immune system: uncommon – angioedema/allergic edema, allergic reactions; rarely - skin rash, urticaria, itching; with unknown frequency - photodermatitis, thrombocytopenic purpura, exfoliative dermatitis, autoimmune hepatitis, toxic epidermal necrolysis, anaphylactoid/anaphylactic reactions;
• genitourinary system: infrequently - impotence, decrease or increase in daily diuresis; rarely - enlargement of the mammary glands in men, completely disappearing after discontinuation of Nifecard CL (mainly in elderly patients); with unknown frequency - deterioration of renal function, lactorrhea;
• skin and subcutaneous fat: uncommon – hyperhidrosis, hemorrhagic rash, pathological hair loss;
• other reactions: often – weakness, asthenia; Uncommon: chills, fever, nonspecific pain, weight gain, facial swelling and periorbital edema.

Side effects when using the medication

Adverse reactions after consuming Nifecard are associated with activation of the sympathetic nervous system and a generalized decrease in blood pressure.

The main side effects of the drug:

• tachycardia (rapid heartbeat);
• feeling of heat, redness of the face and neck;
• supraventricular arrhythmias (most often atrial fibrillation);
• swelling of the ankles, legs and back of the hand;
• hypotension (low blood pressure), manifested by headache, dizziness, weakness;
• dyspeptic manifestations: diarrhea, anorexia, nausea, vomiting and dry mouth;
• depression, fatigue, insomnia.

Often, after stopping the drug, withdrawal syndrome develops with a sharp increase in blood pressure and chest pain. In this case, it is recommended to gradually reduce the dose or switch to low-dose substitutes.

Overdose

Signs of an overdose of nifedipine include hypoxia, hyperglycemia, peripheral vasodilation with a pronounced and sometimes prolonged decrease in blood pressure (manifested by tachycardia and/or bradycardia, headache, bradyarrhythmia, flushing of the facial skin and depression of the sinus node), cardiogenic shock (accompanied by pulmonary edema), metabolic acidosis. In case of severe intoxication, the patient may experience loss of consciousness, in particularly difficult cases, to a coma.

Treatment is standard: taking activated carbon orally and gastric lavage. In addition, it is necessary to carefully monitor the activity of the lungs, heart and kidneys, as well as take measures aimed at restoring stable hemodynamic parameters.

In case of an overdose of long-acting medications, the first step is to ensure the most complete removal of drug residues from the body. To do this, it is necessary, if possible, to flush the small intestine to prevent further absorption of nifedipine. Blockers of slow calcium channels can reduce the tone of the intestinal muscles up to complete atony, which should be taken into account when prescribing laxatives.

Hemodialysis is not effective for removing nifedipine. It is advisable to perform plasmapheresis (since the drug has a high degree of binding to plasma proteins and a relatively small volume of distribution). In order to stop bradyarrhythmia, beta-sympathomimetics and/or atropine are used, and if a bradyarrhythmia occurs that threatens the patient’s life, a temporary pacemaker must be installed.

A persistent, pronounced decrease in blood pressure caused by arterial vasodilation and cardiogenic shock is treated with calcium (1–2 g of calcium gluconate intravenously), dobutamine (up to 15 mcg/kg body weight per minute), dopamine (up to 25 mcg/kg body weight per minute ), adrenaline or norepinephrine. Calcium preparations are an antidote to nifedipine.

Infusion therapy should be carried out with caution, monitoring hemodynamic parameters (to avoid possible volume overload of the heart).

Pharmacokinetics of the drug

The tablets are intended for oral administration. After taking the tablet, it enters the stomach, where it dissolves under the action of gastric juice. The main components penetrate into the bloodstream, from where they travel to organs and tissues. The release process of components is slow. The maximum concentration is observed 6 hours after administration.

The effect of one tablet lasts for a day. High binding to plasma proteins. Metabolites are formed in the liver. The drug is excreted through the kidneys with urine within 24 hours.

The components of the drug Nifecard XL penetrate the placental barrier and into breast milk.

With prolonged use of the medicine, addiction may develop. There is no cumulative effect.

special instructions

Treatment with Nifecard HL is discontinued gradually. It must be taken into account that at the beginning of therapy, the patient may develop an attack of angina, especially in the case of recent withdrawal of beta-blockers (they also cannot be discontinued abruptly).

The combined use of nifedipine and beta-blockers should only be carried out under close medical supervision, since the combination of these drugs can cause an excessive decrease in blood pressure, and sometimes aggravate the course of heart failure.

In patients with severe heart failure, dosing of the drug is carried out with great caution. With severe stenosis of the coronary arteries, at the beginning of treatment with Nifecard HL or with an increase in the dose of the drug, the frequency and severity of anginal pain may increase, sometimes even leading to myocardial infarction (rarely).

Diagnostic criteria for the use of nifedipine in patients with vasospastic angina:

• coronary artery spasm or ergonovine-induced angina;
• classic clinical picture with an increase in the ST segment on the ECG (electrocardiogram);
• coronary spasm detected by angiography;
• vasospasm without confirmation (for example, in the case of unstable angina or at different voltage thresholds, when ECG data indicate transient vasospasm).

In persons with severe hypertrophic obstructive cardiomyopathy, the risk of increased severity, duration and frequency of angina attacks after taking Nifecard CL increases, and therefore in this case the drug should be discontinued.

In patients with diabetes mellitus, additional monitoring of blood glucose levels may be required during treatment with Nifecard HL.

For patients on hemodialysis with high blood pressure, reduced circulating blood volume and irreversible impairment of renal function, the drug is prescribed with caution, as a sharp drop in blood pressure is possible.

In case of liver dysfunction, the patient is monitored and, if necessary, the dose is reduced and/or nifedipine is used in other dosage forms.

In patients with severe stenosis of any part of the gastrointestinal tract, intestinal obstruction may develop. Very rarely, bezoars (stomach stones) may appear, which can sometimes only be removed through surgery. Signs of intestinal obstruction in isolated cases may also occur in patients who do not have any pathologies of the gastrointestinal tract. The likelihood of bezoars is greater in patients with reduced intestinal motility, diverticulitis, vertical gastroplasty, intestinal tumors, inflammatory bowel diseases, gastric bypass surgery, after colostomy and partial resection of the small intestine, as well as in patients who simultaneously take anticholinergics, opiates, laxatives (laxatives), H2-blockers, muscle relaxants or non-steroidal anti-inflammatory drugs.

In isolated reports, information appeared about tablets sticking to the intestinal walls, which led to the formation of ulcers with further hospitalization of patients and surgical intervention. The possibility of false-positive symptoms of a polyp (the so-called filling defect) should be taken into account during a barium X-ray examination of the intestine.

Before performing surgical operations under general anesthesia, it is necessary to warn the anesthesiologist about taking Nifecard CL.

Slow calcium channel blockers, including nifedipine, can inhibit platelet aggregation in vitro, but there is very little evidence of a statistically significant increase in bleeding time and a decrease in platelet aggregation.

In patients receiving Nifecard CL, there may be an increase in the titer of antinuclear antibodies, as well as a positive result when performing a direct Coombs test.

Impact on the ability to drive vehicles and complex mechanisms

During treatment with Nifecard HL, care must be taken when driving a car or other transport, as well as performing work that requires high concentration and quick reaction.

Indications for use

The entire group of CCB drugs is used primarily in cardiological or neurological practice due to its effect on the vascular system. Dihydropyridine derivatives have a greater effect on the vessels of the brain, and less on the coronary arteries.

Instructions for use of Nifecard highlight the main indications:

• 
  hypertension (persistent increase in blood pressure above 140/90 mmHg);

• stable form of angina pectoris;
• vasospastic (variant) Prinzmetal angina;
• Raynaud's syndrome;
• vegetative-vascular dystonia, which occurs in the hypertensive variant;
• prevention of ischemic strokes in patients with hypertension;
• diffuse spasm of the esophagus.

At what pressure should I take it and in what dose?

Selection of treatment for arterial hypertension is carried out by titration (continuous adjustment of the drug dose) depending on the patient’s sensitivity and target parameters.

Approximate start of Nifecard therapy for the treatment of hypertension:

• 1st degree (systolic 140-160 mmHg / diastolic 90-100 mmHg) – 30 mg (1 tablet) 1 time per day;
• 2nd degree (160-180/100-110 mmHg) – 30 mg 1 time per day, if ineffective – 2 times per day;
• 3rd degree (more than 180/110 mmHg) – 60 mg 1 time per day, if ineffective – 60+30 mg 1 time per day. Alternative management – ​​60 mg Nifecard + a drug from the group of beta blockers.

Nifecard belongs to the group of modern retard drugs, the use of which involves monotherapy (1 drug) 1-2 times a day.

When to take 30 mg?

The dosage of the drug 30 mg is considered the starting therapy for the treatment of patients with:

• 
  stable angina pectoris;

• mild arterial hypertension of the 1st degree (without complications from target organs);
• Prinzmetal's angina;
• vegetative-vascular dystonia;
• Raynaud's syndrome;
• liver pathology, including alcohol consumption (the ability to eliminate the drug decreases, which leads to increased concentration and prolonged circulation in the blood);
• patients over 65 years of age;
• diabetes mellitus (medium and high doses contribute to an increase in hyperglycemia).

In addition, simultaneous use with other drugs slows down the administration of the drug. The use of Nifecard 30 is recommended when taking Azithromycin, Cimetidine, Fluoxetine, Diltiazem, Ketoconazole, and medications for the treatment of HIV infection.

In what cases should I use a dose of 60 mg?

Treatment with medium and high doses of Nifedipine is recommended for:

• arterial hypertension 2 and 3 degrees;
• if beta blockers and ACE inhibitors (angiotensin-converting enzyme) are ineffective or have contraindications;
• when taken simultaneously with Valproic acid, Phenobarbital, Rifampicin (drugs that accelerate the elimination of Nifecard from the body).

Treatment of angina pectoris with high doses of nifedipine, according to studies, increases the risk of complications and death.

The dose of the drug is selected under the supervision of a physician, monitoring the patient’s condition and the results of paraclinical studies.

Use during pregnancy and lactation

Blockers of slow calcium channels can cause reversible biochemical changes in the head of sperm, which can lead to disruption of their functions. In men who have repeatedly had problems conceiving during IVF (in vitro fertilization), the use of nifedipine may be one of the possible reasons, if no other explanation is found.

Nifecard CL is contraindicated in women before the 20th week of pregnancy, as nifedipine has been shown to be feto/embryotoxic and teratogenic in animal studies. After the 20th week of pregnancy, the use of the drug is possible only in a hospital setting (for timely monitoring of the pregnant woman’s blood pressure and regular ultrasound examination of the viability and development of the embryo) and in cases where the benefit to the mother clearly outweighs the possible risk to the fetus. If abnormalities occur, Nifecard XL should be discontinued.

If the use of Nifecard CL during lactation is necessary, breastfeeding should be discontinued.

Overdose of a drug

If you use Nifecard for blood pressure without following your doctor’s recommendations, a reaction to an overdose of components may occur, which manifests itself in the following symptoms:

• dilation of blood vessels;
• a strong decrease in blood pressure;
• headaches;
• facial redness;
• sinus node dysfunction;
• sinus rhythm disturbance;
• increased heart rate;
• bradyarrhythmias.

In severe cases of intoxication caused by an overdose of the drug, fainting or coma may occur.

At the first signs of an overdose, it is necessary to help the patient flush the stomach. To do this, he should be given an adsorbent or induce vomiting. In case of an overdose, blood flow, the functioning of the heart and other organs are often disrupted. it is necessary to direct measures to stabilize the condition. Further treatment is prescribed and carried out by the attending physician in a hospital setting or on an outpatient basis, depending on the patient’s condition. Hemodialysis is ineffective.

Drug interactions

The main isoenzyme involved in the metabolism of nifedipine is CYP3A4. Medicines that induce or inhibit this isoenzyme can alter the clearance and first-pass metabolism of Nifecard CL.

When using nifedipine together with inducers of the CYP3A4 isoenzyme, the following changes are possible:

• rifampicin: there is a significant decrease in the bioavailability of nifedipine, which does not allow achieving effective plasma concentrations of the drug;
• phenytoin: bioavailability decreases and the effectiveness of Nifecard CL decreases (its dose may need to be increased);
• phenobarbital and carbamazepine: a decrease in the plasma concentration of nifedipine is possible.

When using Nifecard CL simultaneously with inhibitors of the CYP3A4 isoenzyme, the following interactions are possible:

• macrolide antibiotics (erythromycin, etc.): can increase the plasma concentration of nifedipine;
• HIV protease inhibitors (ritonavir, indinavir, saquinavir, amprenavir, nelfinavir, etc.): it is possible to increase the concentration of nifedipine in plasma;
• imidazole derivatives (fluconazole, itraconazole, ketoconazole): reliable interaction studies have not been conducted, but there is a possibility of increased plasma concentrations of nifedipine;
• fluoxetine, nefazodone, dalfopristin/quinupristin: the possibility of increased plasma concentrations of nifedipine cannot be excluded;
• valproic acid: a decrease in the concentration of nifedipine in the blood plasma is possible;
• cimetidine: the plasma concentration of nifedipine increases and its antihypertensive effect increases;
• grapefruit juice: the first-pass metabolism of nifedipine decreases and its plasma concentration increases, which increases the bioavailability of the drug and increases the risk of unstable angina and heart attack (the use of grapefruit juice during treatment is not recommended).

Possible drug interactions of Nifecard CL with other drugs:

• cisapride, cyclosporine: when used together, they can increase the plasma concentration of nifedipine;
• diltiazem: the clearance of nifedipine decreases and its plasma concentration increases.
• antihypertensive drugs (beta-blockers, diuretics, angiotensin II receptor antagonists, alpha-blockers, alpha-methyldopa, angiotensin-converting enzyme inhibitors, phosphodiesterase-5 inhibitors, other slow calcium channel blockers): the antihypertensive effect of these drugs may be enhanced;
• digoxin: nifedipine increases the serum concentration of digoxin (the dose of the latter may need to be changed);
• quinidine: its plasma concentration decreases, at the same time the concentration of nifedipine in plasma may increase (it is recommended to monitor blood pressure and, if necessary, adjust the doses of both drugs);
• vincristine: the elimination of vincristine slows down and its dose may need to be reduced;
• tacrolimus: the metabolism of tacrolimus may be slowed (reducing its dose is required);
• Magnesium sulfate: a pronounced decrease in blood pressure is possible;
• phenytoin: the toxic effect of phenytoin increases due to a slowdown in its metabolism;
• cephalosporins: the concentration of cephalosporins in plasma increases;
• theophylline: plasma concentration of theophylline increases;
• nitrates: when used simultaneously with nitrates, a synergistic effect is observed;
• fentanyl: severe arterial hypotension may develop (it is advisable to discontinue Nifecard CL at least 36 hours before anesthesia);
• indirect anticoagulants: there are rare reports of an increase in prothrombin time.

Acetylsalicylic acid, ranitidine, benazepril, rosiglitazone, doxazosin, omeprazole, triamterene/hydrochlorothiazide, candesartan, irbesartan, orlistat, debrisoquin and pantoprazole do not have any effect on the pharmacokinetics of Nifecard CL.

In patients receiving nifedipine, false-positive results are possible with the spectrophotometric method for determining vanillylmandelic acid in urine, so it is recommended to measure using another method.

Compatibility with other drugs

For high blood pressure, Nifecard is often prescribed in combination with other drugs. The combined treatment regimen is drawn up by the attending physician, taking into account drug compatibility.

Undesirable combinations of Nifecard with medications:

• antihypertensive drugs, diuretic tablets, nitrate-containing medications, beta blockers, tricyclics, Cimetidine, Ranitidine enhance the hypotensive effect;
• Quinidine reduces the content of tablet components in the blood;
• Digoxin. Theophylline increases the maximum content of Nifecard components in the blood;
• liver enzyme inducers reduce the total content of Nifedipine;
• nitrates increase the risk of increased heart rate;
• sympathomimetic drugs, calcium-containing drugs, estrogens reduce the effectiveness of Nifecard.

Nifecard XL may affect the pharmacological properties of other drugs. Nifedipine increases blood concentrations:

• antithrombotic agents;
• anticonvulsants;
• Indandione derivatives;
• Coumarin derivatives;
• Quinine;
• Sulfinpyrazone;
• salicylates.

Nifedipine delays the removal of Vincristine components from the body, which leads to increased adverse reactions.

When using Nifecard simultaneously with lithium-containing drugs, the risk of lithium poisoning increases, which is characterized by: attacks of vomiting, loose stools, impaired coordination of movements, involuntary trembling of the limbs, ringing in the ears.

Drinking grapefruit juice or the fruit itself can lead to a decrease in the metabolism of Nifedipine, so it should be excluded from the diet throughout the entire period of use.

You should consult your doctor about the compatibility of Nifecard with other drugs.

Reviews of Nifecard HL

According to reviews, Nifecard HL is a high-quality and effective drug for reducing high blood pressure. The tablets are convenient to take and are available in pharmacies. The drug helps from the first dose, and the effect of treatment is quite long-lasting.

The disadvantages of Nifecard HL, according to patients, include existing contraindications and possible side effects. Some users did not like the specific taste and smell, as well as the rather large size of the tablets, but despite this, most reviews are positive. Start of form