What does Nifedipine help with? Instructions for use. Nifedipine is a drug for cardiac and vascular therapy

Nifedipine is a drug active use which began in the 70s of the last century. Its appearance advanced medicine to a new level - for example, the treatment of the most common cardiovascular diseases became more effective.

For for long years Pharmacologists around the world tested and improved the drug, reducing the risk of side effects and increasing the effectiveness of its use. Currently, Nifedipine is one of the priority drugs used in cardiology.

Dosage forms of the drug

Until the 2000s, Nifedipine was actively used in tablets and capsules fast acting. The effect of them occurs within 20 minutes after taking the drug, but lasts for 2-4 hours.

During this time, the drug instantly reduces blood pressure, causing a reflex release of adrenaline and related hormones, which, in turn, immediately reduce the concentration of Nifedipine in the blood and remove it from the body. Simultaneously with the reception medicinal product in patients in in rare cases tachycardia is observed, headache and a feeling of heat, which means that fast-acting Nifedipine can cause an even greater jump in pressure.

The problem of "instant and dangerous effect" was solved by German pharmacologists, who managed to develop a new prolonged form of the drug, the effect of which begins 40-50 minutes after administration and lasts 20-25 hours.

Compared to fast-acting Nifedipine, the prolonged form has a number of advantages. Therefore, let's talk about everything in order.

"Long-lasting" Nifedipine

For long-term treatment of cardiovascular diseases and arterial hypertension Patients are prescribed long-acting Nifedipine. Exactly this dosage form ensures a slow and measured flow of the component into the human blood, promotes a smooth decrease in blood pressure, reduces the risk of atherosclerosis, tachycardia, headaches and periodic “jumps” in the well-being of the patient.

Compared to other cardiac drugs, Nifedipine extended-release has fewer contraindications and side effects, and therefore is applicable to the majority of the population in need of quality treatment.

Useful properties of Nifedipine

The ongoing clinical trials of the drug made it possible to evaluate the significance of its use in the treatment of arterial hypertension, coronary disease heart, angina pectoris. It is noteworthy that Nifedipine has a pronounced antianginal effect, which is characteristic of beta-blockers and nitrates, and does not have an excessive effect on the body. side effects. In other words, Nifedipine is allowed to be used when similar cardiac drugs are contraindicated.

The effectiveness of the prolonged form is not affected by the amount of food consumed, which, of course, has a positive effect on the rating of the medicine.

The most common and effective forms the drug should include Osmo-Adalat and Corinfar, which allow you to maintain the required level of concentration medicinal substances in the blood during the day. The stability of the drug prevents the progression of arterial hypertension, and also promotes the healing of affected target organs (heart, kidneys, liver, etc.).

Despite the presence of the drug's only significant drawback - it is not used to relieve hypertensive crises, Nifedipine long acting can not only improve the patient’s condition, but also provide full recovery his of cardio-vascular system.

A little about the disadvantages of the drug Nifedipine

The use of a long-acting medication is not advisable for emergency reduction blood pressure during a patient's attack.

It is intended only for the systematic maintenance of a stable state circulatory system body. First aid during hypertension will be provided by the “fast form” of Nifedipine. However, it has a number of disadvantages:

  1. Frequent use. To prolong the effect of the drug, patients have to use it several times a day. Irregular use of the medication reduces its effectiveness.
  2. Instability of condition. The patient’s well-being may constantly change, because... Eating causes weakness clinical action Nifedipine.
  3. Unpredictable effect. Like any other medicine, fast-acting Nifedipine affects patients' bodies differently. Genetic characteristics, affected kidneys, or the age of the patient may reduce or even neutralize the effect of the drug.
  4. "Wave" pressure. The specific properties of the drug cause constant fluctuations in blood pressure. From too high to too low and vice versa. Due to this, the body experiences constant swelling and weakening. blood vessels, which, in turn, provokes the formation of atherosclerosis.

The drug is prescribed only for the relief of hypertensive crises.

Nifedipine dosage

Long-acting tablets are prescribed 1-2 times a day. It is worth noting that the tablets cannot be divided to reduce the dose of the component (unless there are appropriate instructions from the doctor), dissolved or dissolved. The drug is taken orally, with plenty of water.

According to the instructions for Nifedipine, the course of administration should not exceed 14 days. Exceptions are made only in individual cases discussed with the doctor.

Nifedipine: indications for use

Nifedipine is prescribed for the following diseases:

  • Angina pectoris;
  • Hypertrophic cardiomyopathy;
  • Broncho-obstructive syndrome;
  • Raynaud's syndrome;
  • Pulmonary hypertension.

If your diagnosis is included in this list, do not rush to the pharmacy. First, you should visit a cardiologist’s office and consult about the advisability of using the medication. Self-medication can lead to dire consequences, because Nifedipine has a number of contraindications.

Contraindications

The drug is not allowed to be used in case of cardiogenic shock, acute period myocardial infarction, namely: in the first eight days, diagnosed arterial hypotension, tachycardia, bradycardia, stenosis mitral valve, sick sinus syndrome.

Nifedipine is also contraindicated in patients with renal/liver insufficiency; at inflammatory diseases intestines and Crohn's disease.

Nifedipine is strictly contraindicated during pregnancy. Exceptions can only be made in individual cases, discussed with a doctor and under his special supervision.

Unfortunately, many pages of the Internet are filled with false information about the need for expectant mothers to take the drug. Under no circumstances should you follow this advice and self-medicate. It is also prohibited to take Nifedipine while breastfeeding.

Side effects

Like any other drug, Nifedipine has different effects on different organisms. In some cases, the body greedily absorbs the medication and does not betray its presence, in some cases, on the contrary, it tries with all its might to report the presence of a foreign substance. And it is in these cases that side effects appear.

The most common reaction for older people after the first dose of Nifedipine is redness of the hands and swelling of the joints of the arms and legs. This effect disappears after 8 hours after taking the medicine.

The cardiovascular system can also “panic” and cause tachycardia, facial flushing, a rapid decrease in blood pressure (even to the point of fainting), and anemia (rarely).

Concerning gastrointestinal tract, then constipation, diarrhea, and nausea may occur.

Taking the drug in rare cases has a specific effect on the nervous system and sensory organs, causing dizziness, weakness in the limbs, headache and hearing impairment.

In addition to the above, Nifedipine can cause tremor for the entire duration of the drug.

It is important to note that these side effects are not a guaranteed result from using the drug, but a warning about possible failure in organism.

Selective blocker calcium channels Class II, dihydropyridine derivative
Drug: NIFEDIPINE

Active substance of the drug: nifedipine
ATX coding: C08CA05
KFG: Calcium channel blocker
Registration number: P No. 015233/01
Registration date: 05/12/08
Owner reg. credential: BALKANPHARMA-DUPNITZA AD (Bulgaria)

Dragee correct form, yellow color; on the fracture there is a yellow core of a fine-grained structure. 1 tablet nifedipine 10 mg
Excipients: lactose, wheat starch, microcrystalline cellulose, talc, gelatin, magnesium stearate, sugar coating.
10 pieces. - blisters (5) - cardboard packs.

DESCRIPTION OF THE ACTIVE SUBSTANCE.
All information provided is provided for information only about the drug; you should consult your doctor about the possibility of use.

Pharmacological action Nifedipine

Selective class II calcium channel blocker, dihydropyridine derivative. Inhibits the flow of calcium into cardiomyocytes and vascular smooth muscle cells. Has antianginal and hypotensive effects. Reduces the tone of vascular smooth muscles. Dilates coronary and peripheral arteries, reduces peripheral vascular resistance, blood pressure and slightly - myocardial contractility, reduces afterload and myocardial oxygen demand. Improves coronary blood flow. It has virtually no antiarrhythmic activity. Does not inhibit myocardial conductivity.

Pharmacokinetics of the drug.

When taken orally, it is quickly absorbed from the gastrointestinal tract. It is metabolized during the “first pass” through the liver. Protein binding is 92-98%. Metabolized in the liver to form inactive metabolites. T1/2 - about 2 hours. Excreted mainly by the kidneys in the form of metabolites and in trace amounts unchanged; 20% is excreted through the intestines in the form of metabolites.

Indications for use:

Prevention of angina attacks (including vasospastic angina), including in some cases- relief of angina attacks; arterial hypertension, hypertensive crises; Raynaud's disease.

Dosage and method of administration of the drug.

Individual. For oral administration, the initial dose is 10 mg 3-4 times a day. If necessary, the dose is gradually increased to 20 mg 3-4 times a day. IN special cases(variant angina, severe arterial hypertension) on a short time the dose can be increased to 30 mg 3-4 times/day. For cupping hypertensive crisis, as well as an attack of angina, 10-20 mg (rarely 30 mg) can be used sublingually.
IV to relieve an attack of angina or hypertensive crisis - 5 mg for 4-8 hours.
Intracoronary for relief of acute spasms coronary arteries administer a bolus of 100-200 mcg. For stenosis of large coronary vessels, the initial dose is 50-100 mcg.
Maximum doses: when taken orally - 120 mg/day, when administered intravenously - 30 mg/day.

Side effects of Nifedipine:

From the cardiovascular system: hyperemia skin, feeling of warmth, tachycardia, arterial hypotension, peripheral edema; rarely - bradycardia, ventricular tachycardia, asystole, increased angina attacks.
From the outside digestive system: nausea, heartburn, diarrhea; rarely - deterioration of liver function; V isolated cases- gum hyperplasia. With long-term use in high doses Dyspeptic symptoms, increased activity of liver transaminases, and intrahepatic cholestasis are possible.
From the central nervous system and peripheral nervous system: headache. With long-term use in high doses, paresthesia, muscle pain, tremors, mild visual disturbances, and sleep disturbances are possible.
From the hematopoietic system: in isolated cases - leukopenia, thrombocytopenia.
From the urinary system: increased daily diuresis. With long-term use in high doses, renal dysfunction is possible.
From the outside endocrine system: in isolated cases - gynecomastia.
Allergic reactions: skin rash.
Local reactions: with intravenous administration, a burning sensation at the injection site is possible.
Within 1 minute after intracoronary administration, the negative inotropic effect of nifedipine, an increase in heart rate, and arterial hypotension may occur; these symptoms gradually disappear after 5-15 minutes.

Contraindications to the drug:

Arterial hypotension (systolic blood pressure below 90 mm Hg), collapse, cardiogenic shock, severe heart failure, severe aortic stenosis; hypersensitivity to nifedipine.

Use during pregnancy and lactation.

Adequate and strictly controlled studies of the safety of nifedipine during pregnancy have not been conducted. The use of nifedipine during pregnancy is not recommended.
Since nifedipine is excreted in breast milk, its use during lactation should be avoided or discontinued. breast-feeding during treatment.
Experimental studies revealed the embryotoxic, fetotoxic and teratogenic effects of nifedipine.

Special instructions for the use of Nifedipine.

Nifedipine should only be used in a clinical setting under the strict supervision of a physician. acute heart attack myocardium, severe disorders cerebral circulation, diabetes mellitus, liver and kidney dysfunction, with malignant arterial hypertension and hypovolemia, as well as in patients on hemodialysis. In patients with impaired liver and/or kidney function, the use of nifedipine in high doses should be avoided. Elderly patients are more likely to have decreased cerebral blood flow due to acute peripheral vasodilation.
When taken orally, nifedipine can be chewed to accelerate the effect.
If chest pain occurs during treatment, nifedipine should be discontinued. Nifedipine should be discontinued gradually, since sudden cessation administration (especially after long-term treatment), withdrawal syndrome may develop.
When administered intracoronarily in the presence of stenosis of two vessels, nifedipine cannot be administered into the third open vessel due to the danger of a pronounced negative inotropic effect.
During the course of treatment, avoid drinking alcohol due to the risk of excessive reduction in blood pressure.
Impact on the ability to drive vehicles and operate machinery
At the beginning of treatment, you should avoid driving vehicles and other potentially dangerous species activities requiring speed of psychomotor reactions. In progress further treatment the degree of restrictions is determined depending on the individual tolerance of nifedipine.

Interaction of Nifedipine with other drugs.

When used simultaneously with antihypertensive drugs, diuretics, phenothiazine derivatives, the antihypertensive effect of nifedipine is enhanced.
When used simultaneously with anticholinergic drugs, memory and attention problems may occur in elderly patients.
When used simultaneously with beta-blockers, severe arterial hypotension may develop; in some cases - the development of heart failure.
When used simultaneously with nitrates, the antianginal effect of nifedipine is enhanced.
When used simultaneously with calcium preparations, the effectiveness of nifedipine decreases due to an antagonistic interaction caused by an increase in the concentration of calcium ions in the extracellular fluid.
Cases of development have been described muscle weakness when used simultaneously with magnesium salts.
When used simultaneously with digoxin, it is possible to slow down the excretion of digoxin from the body and, consequently, increase its concentration in the blood plasma.
When used simultaneously with diltiazem, the antihypertensive effect is enhanced.
When used simultaneously with theophylline, changes in the concentration of theophylline in the blood plasma are possible.
Rifampin induces the activity of liver enzymes, accelerating the metabolism of nifedipine, which leads to a decrease in its effectiveness.
When used simultaneously with phenobarbital, phenytoin, carbamazepine, the concentration of nifedipine in the blood plasma decreases.
There are reports of an increase in the concentration of nifedipine in the blood plasma and an increase in its AUC when used simultaneously with fluconazole and itraconazole.
When used simultaneously with fluoxetine, increased side effect nifedipine.
In some cases, when used simultaneously with quinidine, a decrease in the concentration of quinidine in the blood plasma is possible, and when nifedipine is discontinued, a significant increase in the concentration of quinidine is possible, which is accompanied by a prolongation of the QT interval on the ECG.
The concentration of nifedipine in blood plasma may increase moderately.
Cimetidine and, to a lesser extent, ranitidine, increase the concentration of nifedipine in the blood plasma and, thus, enhance its antihypertensive effect.
Ethanol may enhance the effect of nifedipine (excessive hypotension), which causes dizziness and other undesirable reactions.

The medicine Nifedipine belongs to the drugs used in medical practice for hypertension and other pathologies of the heart and blood vessels. The drug is a calcium antagonist. Getting into the body, active ingredients Nifedipine has an anti-ischemic effect, reduces blood pressure, and increases coronary blood flow. In addition to tablets and solutions for injection, there is Nifedipine ointment and a drug in gel form, which are used to treat varicose veins veins in the rectal area.

Release form and composition of the drug

The main active ingredient of the drug is nifedipine. Among the auxiliary components are milk sugar, potato starch, cellulose, magnesium stearate, talc, hypromelose, other substances. International name- Nifedipine.

The release form of Nifedipine is as follows:

  • pills short acting, coated, containing 10 mg of active ingredient. Mainly used for periodic use to reduce blood pressure and eliminate chest pain;
  • Nifedipine retard tablets contain 20 mg of the active ingredient. This is long-acting Nifedipine. The drug is prescribed for daily use in patients with hypertension. This scheme allows you to maintain pressure on normal level, avoid other complications in patients;
  • infusion solution in ampoules of 50 ml;
  • ampoules for intravascular administration, 2 ml.

Separate medication group Nifedipine gel and the medicine in the form of a cream are used. These drugs are used in complex therapy hemorrhoids, contain 0.2% nifedipine, isosorbitol dinitrate and lidocaine.

Pharmacological effect of tablets and injections

What is the mechanism of action of the drug? Nifedipine retard and other forms of the drug block calcium channel activity cell membranes. Due to this, the intake of calcium ions into the peripheral vessels, arteries of the heart muscle, muscle fibers the whole body. These complex processes at a deep cellular level they allow you to achieve the following effect:

  • improve blood supply to the heart;
  • expand the lumen of arterial and coronary vessels;
  • increase renal blood circulation;
  • activate the process of removing sodium and water from the body;
  • reduce blood pressure, vascular smooth muscle tone.

Once in the body, the drug Nifedipine is quickly absorbed by the digestive system. The active components of the product bind to blood proteins, long time are in the body. The substance is metabolized in the liver and excreted by the kidneys.

Important! The drug can be used only as prescribed by the attending physician. Self-medication often causes Negative consequences, sometimes incompatible with life.

Effect of the ointment

Nifedipine gel emulsion and ointment are used in combination with other medications to treat hemorrhoids. The drug can be used to treat all forms and stages of the disease. Manufacturers of the drug claim that the use of Nifedipine is an excellent alternative surgical intervention with pathology of the vessels of the anus.

Nifedipine gel is used for hemorrhoids

Thanks to active substances means, during the use of the medicine, relaxation of the smooth muscles of blood vessels occurs, local blood pressure, disappears pain syndrome. Additional components help get rid of cracks and microdamages, have an antibacterial, anti-inflammatory effect, eliminate discomfort, itching and burning.

Indications for the use of injections and tablets

Instructions for use include the following indications for the use of Nifedipine:

  • hypertrophic cardiomyopathy;
  • all degrees hypertension;
  • cardiopulmonary failure, accompanied by congestive processes;
  • Raynaud's syndrome;
  • conditions leading to spasm of the coronary arteries;
  • angina pectoris.

The drug Nifedipine is also used by cardiologists for the treatment of cerebrovascular accidents, during the onset of a hypertensive crisis, during the treatment of heart failure, coronary heart disease, for the treatment of bronchospasms, atherosclerosis of peripheral arteries and other conditions.

Indications for use of gel and ointment

The topical form of the drug is used for the following conditions:

  • acute and chronic hemorrhoids;
  • hemorrhoidal fissures;
  • the presence of external and internal cavernous formations;
  • bleeding;
  • prolapse of hemorrhoidal cones;
  • thrombosis;
  • pain syndrome;
  • hyperemia, itching, burning, irritation of the rectal mucosa.

Nifedipine and auxiliary components, included in the medicine, quickly relieve the main manifestations of hemorrhoids, make the patient feel better, and help prevent complications.

Contraindications

The drug Nifedipine can be taken only if the patient has no contraindications to its use. Treatment with Nifedipine is prohibited following states in the patient:

  • hypotension, other diseases accompanied by low blood pressure;
  • offensive;
  • vascular collapse;
  • acute heart failure;
  • recent myocardial infarction (less than 30 days ago);
  • first 4 weeks of pregnancy;
  • the patient's age is under 18 years;
  • breastfeeding period;
  • allergy to any of the components of the product.


When prescribing the drug, the doctor must take into account contraindications

If the contraindications of the drug are not taken into account, taking the medicine may provoke severe consequences for the body.

Important! The drug in the form of a cream and gel has no serious contraindications, except for personal intolerance, and is used among children and pregnant women.

Instructions for use

How to take Nifedipine? Use any medicinal form medications prescribed by your doctor. The dosage and regimen are determined by a specialist based on the patient’s medical history and diagnosis.

Taking pills

At various states The dose of the drug is usually 1 tablet three times a day. It is recommended to take the medicine after meals. Take the tablet with water. If necessary, the dose is increased by the attending physician. This is possible if the drug is well tolerated and there is no side effects. For elderly patients or patients suffering from kidney pathologies, the dose is reduced.

Use of injections

Indications for the use of Nifedipine in injections include severe conditions in patients. Injections are used exclusively in hospital settings during intensive care. Nifedipine is administered to patients intravenously or via a drip.

The solution is available in finished form, dilution of the drug is not required. Before administration to a person, a sensitivity test to the drug component is performed. If there is no reaction, the drug can be used. The dose is determined by the doctor. Typically it ranges from 15 to 30 mg over 24 hours.

Application of ointment

The use of Nifedipine in the form of an ointment or gel can be done at home. Before applying the medication, it is recommended to hygiene procedures, cleanse the intestines. For external hemorrhoids, treat cavernous formations with a small amount of ointment or gel, gently rubbing the product into the skin. At internal view pathologies need to be treated with ointment hemorrhoids located inside.

In some cases, the drug is used to apply compresses. To do this, a small amount of the product is applied to linen or cotton fabric and applied to the affected area. This method is suitable for the treatment of external hemorrhoids.

How long does it take for the drug to work?

Many patients are interested in how long it takes for Nifedipine to start working? The therapeutic effect depends on the dose of the drug taken and individual characteristics body. Tablets begin to act more slowly compared to injections. This is explained by the fact that during injection the active components immediately enter the blood. Typically this time ranges from 40 minutes to an hour. The effect of the medication in the form of a gel or ointment is observed within a few minutes after application.


The drug takes effect within half an hour

special instructions

To prevent side effects and complications, patients should follow special instructions during treatment with Nifedipine. Do not combine the drug with alcoholic beverages. This interaction can cause serious side effects, including death.

Therapy with the drug should be discontinued according to a specific scheme. Despite the fact that the medicine does not have a withdrawal syndrome, treatment should not be abruptly interrupted.

Beta-blockers should be used carefully with Nifedipine. They combine medications only under the strict supervision of a doctor, since this combination often provokes a rapid decrease in blood pressure.

Many patients stop taking the drug after feeling relief. This cannot be done, because hypertension often occurs without visible symptoms.
Among patients with severe renal failure and patients on hemodialysis, Nifedipine is used very carefully, since therapy can lead to sharp fall pressure.

The standard dose of the drug for people with liver pathologies should be selected according to individually. If necessary, the dosage is reduced.

Important! The medicine can affect a person’s memory concentration and attention, so driving vehicles and engaging in other hazardous activities should be done with extreme caution.

Drug interactions

Intensifying therapeutic effect the drug when used simultaneously with drugs such as nitrates, diuretics, tricyclic antidepressants, inhalation antiseptics.

The effectiveness of Nifedipine is reduced when combined with Rifampicin. When used together with nitrates, the patient experiences increased tachycardia. Fluoxetine increases the likelihood of developing side effects of the drug. At long-term use with beta-blockers, the patient may experience heart failure.

Use among pregnant women

In the first weeks after conception, drinking Nifedipine is prohibited. No studies have been conducted on the effect of the drug on the fetus. Papaverine is used to reduce uterine tone. From the 16th week, the medicine is prescribed to women if the condition of the mother requires it and the risk to her health is higher than the risk of Nifedipine exposure to the fetus.


The drug is prescribed to pregnant women with extreme caution.

Use in pediatrics

Among patients under 18 years of age, Nifedipine is contraindicated.

Overdose and side effects

Side effects of Nifedipine are most often associated with disruption of the cardiovascular system. Complications associated with the functioning of the respiratory, digestive and musculoskeletal systems are less common.

From the heart and blood vessels:

  • redness of the dermis of the face;
  • reflex tachycardia;
  • increased heart rate;
  • chest pain;
  • rapid decrease in pressure.

From the side of the central nervous system:

  • migraine;
  • feeling of goosebumps;
  • dizziness;
  • nausea.

From the digestive side:

  • bowel dysfunction;
  • pain in the stomach and intestines;
  • nausea;
  • flatulence.

From the bone and muscular systems may be observed muscle pain, trembling of limbs. From the respiratory side - shortness of breath, bronchospasm.

An overdose of Nifedipine causes such serious complications like bradycardia, sudden jump pressure, bradyarrhythmia. IN severe cases offensive is noted vascular collapse. The most pronounced signs of overdose are a few hours after taking a large dose of the drug. The patient develops coma, cardiogenic shock, hypoxia, convulsions and other manifestations.

Important! If even minor signs of overdose develop, you should call ambulance. With absence necessary treatment death comes.

Other names for Nifedipine

The RLS drug database includes several names of the drug Nifedipine. The Nifedipine group includes the following drugs:

  • Cordafen;
  • Corinfar;
  • Captopril;
  • Nifedipine Pharm;
  • Phenigidine;
  • Nifedipine elevit;
  • Farmadipin;
  • Nikardia and others.

Many modern companies They produce analogues of medications with rapid or prolonged action. Information about these drugs can be found in the table.

Many patients are interested in how to choose an analogue, which medicine to choose, Phenigidine or Capoten, Cardofen, Krinpharm and others. In order to choose the right analogue, you need to understand what short or prolonged action of the drug means. Short-acting medicine is not recommended for the treatment of hypertension and other pathologies of the heart and blood vessels. This option is suitable for during emergency care. The extended-release agent is suitable for use among patients during long-term treatment. Such drugs are taken in courses; they slowly and safely reduce blood pressure.

Price and where to buy

Buy medicine You can go to any pharmacy with a doctor's prescription. Approximate cost the drug costs from 20 to 30 rubles.

Nifedipine: instructions for use and reviews

Nifedipine is a calcium channel blocker.

Release form and composition

Dosage form – yellow pills (10 pieces in blisters, 5 blisters in a cardboard pack).

Active substance: nifedipine, 1 tablet – 10 mg.

Excipients: wheat starch, gelatin, magnesium stearate, lactose, microcrystalline cellulose PH101, talc.

Shell composition: isopropanol, glycerol, carmellose 7MF, acetone, arlacel 186, purified water, ethylcellulose N22, titanium dioxide, povidone K30, sugar, ethanol 96%, macrogol 6000, talc, polysorbate 20, colloidal silicon dioxide, Eurolake Quinoline Yellow 21 ( E104) and Eurolake Sunset Yellow 22 (E110).

Pharmacological properties

Pharmacodynamics

Nifedipine is a selective blocker of slow calcium channels, a 1,4-dihydropyridine derivative. The drug has antianginal, hypotensive and vasodilating effects. It reduces the flow of calcium ions into the smooth muscle cells of peripheral and coronary arteries, as well as into cardiomyocytes. IN large doses Nifedipine suppresses the release of calcium ions from stores inside cells. It reduces the number of functioning calcium channels without affecting the time of their recovery, inactivation and activation.

Nifedipine uncouples the processes of contraction and excitation in the smooth muscles of blood vessels, mediated by calmodulin, and in the cardiac muscle, mediated by troponin and tropomyosin. IN therapeutic doses the drug normalizes the transport of calcium ions through the membrane, which is disrupted under certain conditions pathological conditions, for example, arterial hypertension.

Nifedipine does not affect venous tone. It reduces spasm, dilates peripheral and coronary vessels (mainly arterial), lowers blood pressure and total peripheral vascular resistance, reduces myocardial tone, afterload and oxygen demand of the heart muscle, and prolongs diastolic relaxation of the left ventricle. Under its influence, coronary blood flow increases, blood supply to ischemic areas of the myocardium improves, and the functioning of collaterals is activated. Has almost no effect on the atrioventricular and sinoatrial nodes and has no effect antiarrhythmic effect. Increases blood flow in the kidneys, causes moderate excretion of sodium in the urine.

The clinical effect occurs within 20 minutes and lasts from 4 to 6 hours.

Pharmacokinetics

Nifedipine is quickly and almost completely (92–98%) absorbed into the digestive tract. Bioavailability of the drug after oral administration ranges from 40 to 60% (taking with food increases this figure). Nifedipine undergoes a first-pass effect through the liver. In blood plasma, the maximum concentration of the substance is 65 ng/ml and is observed after 1–3 hours. 90% bound to plasma proteins. Nifedipine crosses the placental and blood-brain barrier and is secreted into breast milk.

Metabolized completely. Metabolism occurs in the liver with the participation of isoenzymes CYP3A5, CYP3A7 and CYP3A4.

About 80% of the dose taken is excreted in the form of inactive metabolites by the kidneys and another 20% in the bile. The half-life is from 2 to 4 hours. With insufficient liver function, the total clearance is reduced and the half-life is prolonged.

Nifedipine does not accumulate in the body. Chronic failure renal function, peritoneal dialysis and hemodialysis do not affect pharmacokinetic parameters. Long-term use(2–3 months or more) leads to the development of tolerance to the drug. Plasmapheresis may speed up clearance.

Indications for use

  • Angina at rest and exertion (including variant) with coronary heart disease;
  • Arterial hypertension (as a single drug or in combination with other antihypertensive drugs).

Contraindications

  • Cardiogenic shock, collapse;
  • Sick sinus syndrome;
  • Decompensated heart failure;
  • Severe aortic/mitral stenosis;
  • Arterial hypotension with systolic blood pressure below 90 mmHg;
  • Idiopathic hypertrophic subaortic stenosis;
  • Tachycardia;
  • Period 4 weeks after acute myocardial infarction;
  • Age up to 18 years;
  • Hypersensitivity to the drug or other dihydropyridine derivatives.

Nifedipine is also contraindicated during pregnancy and lactation.

Due to the risk of complications, the drug should be used with caution in the following cases:

  • Diabetes;
  • Severe cerebrovascular accidents;
  • Severe renal/liver dysfunction;
  • Chronic heart failure;
  • Malignant arterial hypertension.

Caution is required when using the drug in patients on hemodialysis.

Instructions for use of Nifedipine: method and dosage

Nifedipine is taken orally, swallowing the tablets whole with plenty of liquid, during or after meals.

Doses are set individually depending on the severity of the disease and the patient’s response to the drug.

At the beginning of treatment, 1 tablet is prescribed 2-3 times a day; if necessary, the dose is increased to 2 tablets 1-2 times a day.

Maximum permissible daily dose is 40 mg of nifedipine (4 tablets).

A dose reduction is required for elderly people, patients with impaired liver function, severe cerebrovascular accidents, as well as patients receiving combination therapy (hypotensive or antianginal).

Side effects

  • Cardiovascular system: feeling of heat, facial hyperemia, peripheral edema (ankles, feet, legs), tachycardia, syncope, excessive decrease in blood pressure, heart failure; in some cases, especially at the beginning of treatment, the appearance of angina attacks, requiring discontinuation of the drug;
  • Central nervous system: increased fatigue, drowsiness, dizziness, headache; with long-term use in high doses - tremor, paresthesia of the limbs;
  • Gastrointestinal tract, liver: dyspeptic disorders; at long-term treatment– liver dysfunction (increased activity of liver transaminases, intrahepatic cholestasis);
  • Musculoskeletal system: myalgia, arthritis;
  • Urinary system: increased daily diuresis in patients with renal failure– deterioration of kidney function;
  • Hematopoietic organs: thrombocytopenia, leukopenia, thrombocytopenic purpura, anemia;
  • Allergic reactions: exanthema, urticaria, itchy skin, autoimmune hepatitis;
  • Other: gum hyperplasia, hyperglycemia, changes in visual perception, flushing of the face, in older people - gynecomastia (completely disappearing after discontinuation of the drug).

Overdose

In case of an overdose of Nifedipine, a headache appears, arrhythmia and bradycardia develop, the activity of the sinus node is inhibited, blood pressure decreases, and the facial skin becomes red.

As first aid It is recommended to lavage the stomach and take activated carbon. The symptomatic therapy carried out is aimed at stabilizing the functioning of the cardiovascular system. The antidote for Nifedipine is calcium. Slow intravenous administration of calcium gluconate or 10% calcium chloride at a dose of 0.2 ml/kg (total no more than 10 ml) over 5 minutes is required. If the effect is not achieved, repeated infusion may be performed under the control of serum calcium concentration. Resumption of symptoms of poisoning is an indication for continuous infusion at a rate of 0.2 ml/kg/h, but not more than 10 ml/h.

If the blood pressure is severely low, the patient is given dopamine or dobutamine intravenously. If cardiac conduction is impaired, administration of isoprenaline, atropine or installation of an electrical pacemaker (artificial pacemaker) is indicated. Developing heart failure should be compensated intravenous administration strophanthin. Catecholamines are allowed to be used only in cases of life-threatening circulatory failure. It is advisable to monitor the level of electrolytes (calcium, potassium) and glucose in the blood.

Hemodialysis is ineffective.

special instructions

In case of abrupt cessation of treatment, there is a risk of developing withdrawal syndrome, so the dose should be reduced gradually.

During treatment with Nifedipine, you must refrain from drinking alcohol, drinking vehicles and performing potentially hazardous types of work that require rapid psychophysical reactions and increased concentration.

Impact on the ability to drive vehicles and complex mechanisms

During treatment with Nifedipine, you should refrain from performing potentially hazardous work that requires high concentration attention and speed of psychomotor reaction.

Use during pregnancy and lactation

According to the instructions, Nifedipine is contraindicated during pregnancy and breastfeeding.

Use in childhood

Nifedipine should not be used in children and adolescents under 18 years of age, since the safety and effectiveness of the drug in this age group not installed.

For impaired renal function

Nifedipine should be used with caution in patients with pronounced violations renal function.

For liver dysfunction

Nifedipine should be used with caution in patients with severely impaired hepatic function.

Use in old age

For elderly patients, the drug is prescribed in reduced doses.

Drug interactions

  • Other antihypertensive drugs, diuretics, tricyclic antidepressants, ranitidine, cimetidine: increased severity of lowering blood pressure;
  • Nitrates: increased tachycardia and hypotensive effect nifedipine;
  • Beta-blockers: risk of a pronounced decrease in blood pressure, in some cases - worsening heart failure (this combination treatment should be carried out under close medical supervision);
  • Quinidine: decrease in its concentration in blood plasma;
  • Theophylline, digoxin: increase in their concentration in blood plasma;
  • Rifampicin: acceleration of metabolism and, as a result, weakening of the effect of nifedipine.

Analogues

Analogues of Nifedipine are: Cordaflex, Cordipin HL, Cordipin Retard, Nifecard CL.

Terms and conditions of storage

Store at temperatures up to 25 ºC in a place protected from light and moisture, out of reach of children.

Shelf life – 3 years.

Self-medication can be harmful to your health.
You should consult your doctor and read the instructions before use.

Nifedipine: instructions for use

Compound

active ingredient: nifedipine;

1 tablet contains nifedipine - 10 mg or 20 mg;

excipients: milk sugar, potato starch, microcrystalline cellulose, povidone 25, sodium lauryl sulfate, magnesium stearate, hypromelose, Tween 80, titanium dioxide E 171, macrogol 6000, talc, quinoline yellow E 104.

Description

film-coated tablets, yellow in color, with a biconvex surface; On a cross section, two layers are visible.

pharmachologic effect

Selective calcium channel blocker, dihydropyridine derivative. Inhibits the flow of calcium into cardiomyocytes and vascular smooth muscle cells. It has antianginal and antihypertensive effects. Reduces the tone of vascular smooth muscles. Dilates coronary and peripheral arteries, reduces total peripheral vascular resistance, blood pressure and slightly - myocardial contractility, reduces afterload and myocardial oxygen demand. Improves coronary blood flow. Does not inhibit myocardial conductivity. With long-term use, nifedipine can prevent the formation of new atherosclerotic plaques in coronary vessels. At the beginning of treatment with nifedipine, transient reflex tachycardia and an increase in cardiac output, which does not compensate for the vasodilation caused by the drug. Nifedipine enhances the excretion of sodium and water from the body. In case of Raynaud's syndrome, the drug can prevent or reduce vascular spasm of the extremities.

Pharmacokinetics

When taken orally, nifedipine is quickly and almost completely (more than 90%) absorbed from the gastrointestinal tract. Bioavailability is about 50%.

The maximum concentration in blood plasma is achieved 1-3 hours after administration. The half-life is 2-5 hours. It is excreted mainly in the urine in the form of inactive metabolites. Coming time clinical effect: 20 minutes - for oral administration, 5 minutes - for sublingual administration. The duration of the clinical effect is 4-6 hours.

Indications for use

Included combination therapy the drug is used in the treatment of coronary heart disease (stable angina, vasospastic angina) and arterial hypertension.

Contraindications

The drug should not be used if there is a known history of hypersensitivity to nifedipine, cardiogenic shock, high-grade aortic stenosis, unstable angina, acute attack angina pectoris, acute myocardial infarction (during the first 4 weeks). Nifedipine is contraindicated during pregnancy and breastfeeding. Childhood(up to 14 years old).

Pregnancy and lactation

Nifedipine gets into breast milk Therefore, breastfeeding should be discontinued if the use of Nifedipine is necessary during lactation.

Directions for use and doses

Adults and children over 14 years of age take the drug orally. The tablets should be taken after meals, without chewing and with a sufficient amount of liquid (for example, a glass of water).

The dose is set individually, taking into account the severity of the disease and the patient’s response to the drug.

Typically, the following dosage regimens are used for the treatment of adults.

1. Stable and vasospastic angina.

2. Arterial hypertension.

The drug is prescribed in an average daily dose of 10 mg 2-3 times a day.

If it is necessary to use the drug in higher daily doses, they can be gradually increased to 20-40 mg 2 times a day. The maximum daily dose is 80 mg.

The interval between doses of 2 single doses of 20 mg each should be at least 4 hours. When prescribing the drug twice a day, the interval between tablet doses should be about 12 hours (taken in the morning and evening).

Side effect

Cardiovascular system: most often, especially at the beginning of treatment, tachycardia, flushing of the face and other parts of the body, headache, dizziness and decreased blood pressure, swelling of the legs were observed (usually when using prolonged forms of the drug).

Collapse and chest pain (including typical attacks of angina pectoris) rarely occurred. These adverse reactions required immediate discontinuation of the drug.

Organs of the gastrointestinal tract and liver: dyspepsia, discomfort in epigastric region, nausea, diarrhea. Rarely - increased levels of liver transaminases, cholestasis (impaired liver function).

Hematopoietic system: rarely - anemia, leukopenia, thrombocytopenia, very rarely - agranulocytosis.

Urinary system: increased daily diuresis; in patients with renal failure - impaired renal function.

Allergic reactions: skin allergic reactions(rash, itching, erythema), rarely - systemic reactions, exfoliative dermatitis.

Other reactions: when using higher doses, myalgia, paresthesia of the extremities, temporary visual impairment, and increased fatigue were occasionally observed; very rarely, with long-term treatment, hyperglycemia, gum hyperplasia, and gynecomastia (in older men) are possible.

After discontinuation of the drug, adverse reactions in most cases completely disappeared. Isolated cases of myocardial infarction have been described.

Basically, when using high doses of the drug, in some cases muscle pain (myalgia), trembling of the fingers (tremor), as well as transient changes in visual perception, expressed to a slight extent, may occur.

With long-term treatment, some patients experienced changes in the gums (gingival hyperplasia), which completely disappeared after discontinuation of the drug.

In isolated cases, liver dysfunction was observed (intrahepatic cholestasis, increased activity of transaminases in the blood serum), which disappeared after discontinuation of the drug, liver inflammation (hepatitis) of allergic origin.

Overdose

In case of an overdose of the drug, headache, facial flushing, prolonged systemic hypotension, and absence of pulse in the peripheral arteries occur. In severe cases, tachycardia or bradycardia, dysfunction of the sinus node, slowing of atrioventricular conduction, hyperglycemia, metabolic acidosis and hypoxia, collapse with loss of consciousness and cardiogenic shock, which is accompanied by pulmonary edema. Treatment. In case of overdose, call a doctor immediately.

Emergency care measures should primarily be aimed at removing the drug from the body and restoring stable hemodynamics. In patients, it is necessary to constantly monitor the functions of the cardiovascular and respiratory systems, levels of sugar and electrolytes (potassium, calcium) in the blood plasma, daily diuresis and circulating blood volume. It is possible to administer calcium supplements. If calcium administration is not effective enough, it is advisable to use sympathomimetics such as dopamine or norepinephrine to stabilize blood pressure. The doses of these drugs are selected taking into account the achieved therapeutic effect. Bradycardia can be treated with beta-sympathomimetics. When decelerating heart rate life-threatening, the use of an artificial pacemaker is recommended. Additional fluid administration must be approached very carefully, as this increases the risk of heart overload.

Since nifedipine is characterized high degree binding to plasma proteins and a relatively small volume of distribution, hemodialysis is ineffective, but plasmapheresis is recommended.

Interaction with other drugs

If you are taking any other medicines, be sure to tell your doctor about this!

The drug may potentiate the effect of other antihypertensive drugs. When combined with cardiac glycosides, it can increase the concentration of the latter in the blood plasma, and therefore, if necessary, reduce their dose. Caution should be used in combination with organic nitrates (possible decrease in blood pressure and severe reflex tachycardia). When combined with I-adrenergic receptor blockers, the development of arterial hypotension and heart failure is possible. The use of nifedipine in combination with rifampicin is contraindicated, since the latter accelerates the metabolism of nifedipine and weakens it therapeutic effect. There was no incompatibility of the drug with radiocontrast agents.

Features of application

Nifedipine should be used with particular caution in patients undergoing hemodialysis, as well as in patients with malignant hypotension or hypovolemia (decreased blood volume), since dilation of blood vessels can cause a significant decrease in blood pressure in them.

Some in vitro experiments have revealed a relationship between the use of calcium antagonists, in particular nifedipine, and reverse biochemical changes in sperm that impair the latter’s ability to fertilize.

During therapy coronary vasospasm in the post-infarction period, treatment with Nifedipine should begin approximately 3-4 weeks after myocardial infarction and only if the coronary circulation is stabilized.

Grapefruit juice inhibits the metabolism of nifedipine, which causes an increase in the concentration of the latter in the blood plasma and potentiation of the hypotensive effect of the drug. The use of nifedipine may lead to falsely elevated results when spectrophotometrically determining the concentration of vanillin-mideic acid in urine (however, this effect is not observed when using the high-performance liquid chromatography method).

The ability to influence reaction speed when driving or

working with other mechanisms. When using the drug, management is not recommended

vehicles and working with other potentially dangerous mechanisms.



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