Nifedipine original drug. Nifedipine tablets - indications for use. Respiratory system disorders

Medicine Nifedipine effectively eliminates pain in the background of unstable angina pectoris, lowers blood pressure to normal levels, reduces ischemia in the coronary vessels.
It is taken as tablets orally. It is quickly absorbed into the bloodstream and has a selective effect on calcium channels, which conditionally belong to the second selective class. Due to the effect of inhibition of calcium metabolism, the process of entry of these ions into the cellular structures of the myocardium slows down. Also, the vascular bed of large arteries gets rid of excess calcium. The tension tone decreases, the vascular wall relaxes and the lumen of the artery and vein increases. According to the instructions, the use of nifedipine allows you to reduce the heart rate.
Against the background of the expansion of the coronary and cerebral great vessels, there is an increase in the flow of blood enriched with glucose and oxygen to the tissues of the heart and brain. These processes create fertile ground for the rapid recovery of cells affected by ischemia. Oxygen saturation increases, anginal manifestations are reduced.

Indications for use

Apply Nifedipine(fenigidin) as an antianginal agent for coronary artery disease with angina attacks, to reduce blood pressure in various types of hypertension, including renal hypertension. There are indications that nifedipine (and verapamil) in nephrogenic hypertension slows the progression of renal failure.
It is also used in the complex therapy of chronic heart failure. It was previously believed that nifedipine and other calcium ion antagonists are not indicated in heart failure due to a negative inotropic effect. Recently, it has been established that all these drugs, due to their peripheral vasodilator action, improve the function of the heart and contribute to a decrease in its size in chronic heart failure. There is also a decrease in pressure in the pulmonary artery. However, the possibility of a negative inotropic effect of nifedipine should not be excluded, and caution should be exercised in severe heart failure. Recently, there have been reports of the inappropriate use of nifedipine in hypertension, due to an increased risk of myocardial infarction, as well as the possibility of an increased risk of death in patients with coronary heart disease with long-term use of idenfat.
This concerns mainly the use of "regular" nifedipine (short-acting), but not its prolonged dosage forms and long-acting dihydropyridines (for example, amlodipine). This question, however, remains debatable.
There is evidence of a positive effect of nifedipine on cerebral hemodynamics, its effectiveness in Raynaud's disease. In patients with bronchial asthma, no significant bronchodilatory effect was noted, but the drug can be used in combination with other bronchodilators (sympathomimetics) for maintenance therapy.

Mode of application

accept Nifedipine inside (regardless of the time of eating) 0.01-0.03 g (10-30 mg) 3-4 times a day (up to 120 mg per day). The duration of treatment is 1-2 months. and more.
For the relief (removal) of a hypertensive crisis (a rapid and sharp rise in blood pressure), and sometimes with angina attacks, the drug is used sublingually. A tablet (10 mg) is placed under the tongue. Nifedipine tablets, placed under the tongue without chewing, dissolve within a few minutes. To speed up the effect, the tablet is chewed and held, without swallowing, under the tongue. With this method of administration, patients should be in the supine position for 30-60 minutes. If necessary, after 20-30 minutes, repeat the drug; sometimes increase the dose to 20-30 mg. After stopping the attacks, they switch to taking the drug inside.
Retard tablets are recommended for long-term therapy. Assign 20 mg 1-2 times a day; less often 40 mg 2 times a day. Retard tablets are taken after meals, without chewing, with a small amount of liquid.
For the relief (removal) of a hypertensive crisis (a rapid and sharp rise in blood pressure), the drug is recommended to be administered at a dose of 0.005 g for 4-8 hours (0.0104-0.0208 mg / min). This corresponds to 6.3-12.5 ml of infusion solution per hour. The maximum dose of the drug - 15-30 mg per day - can be used for no more than 3 days.

Side effects

Nifedipine usually well tolerated. However, reddening of the face and skin of the upper body, headache are relatively common, probably associated with a decrease in the tone of the cerebral (cerebral) vessels (mainly capacitive) and their stretching due to an increase in blood flow through arteriovenous anastomoses (connections of the artery and vein). In these cases, the dose is reduced or the drug is taken after meals.
Palpitations, nausea, dizziness, swelling of the lower extremities, hypotension (lowering blood pressure), and drowsiness are also possible.

Contraindications

Severe forms of heart failure, unstable angina, acute myocardial infarction, sick sinus syndrome (heart disease accompanied by rhythm disturbance), severe arterial hypotension (low blood pressure).

Nifedipine is contraindicated in pregnancy and lactation.
Caution is needed when prescribing the drug to drivers of transport and other professions that require a quick mental and physical reaction.

Interaction with other drugs

With the simultaneous use Nifedipine with antihypertensive drugs, diuretics, phenothiazine derivatives, the antihypertensive effect of nifedipine is enhanced.
With simultaneous use with anticholinergics, memory and attention impairments are possible in elderly patients.
With simultaneous use with beta-blockers, the development of severe arterial hypotension is possible; in some cases - the development of heart failure.
With simultaneous use with nitrates, the antianginal effect of nifedipine is enhanced.
With simultaneous use with calcium preparations, the effectiveness of nifedipine decreases due to the antagonistic interaction caused by an increase in the concentration of calcium ions in the extracellular fluid.
Cases of the development of muscle weakness have been described with simultaneous use with magnesium salts.
With simultaneous use with digoxin, it is possible to slow down the excretion of digoxin from the body and, consequently, increase its concentration in blood plasma.
With simultaneous use with diltiazem, the antihypertensive effect is enhanced.
With simultaneous use with theophylline, changes in the concentration of theophylline in the blood plasma are possible.
Rifampicin induces the activity of liver enzymes, accelerating the metabolism of nifedipine, which leads to a decrease in its effectiveness.
With simultaneous use 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, itraconazole.
With simultaneous use with fluoxetine, the side effects of nifedipine may increase.
In some cases, with simultaneous use with quinidine, a decrease in the concentration of quinidine in the blood plasma is possible, and when nifedipine is canceled, a significant increase in the concentration of quinidine is possible, which is accompanied by a prolongation of the QT interval on the ECG.
Plasma concentrations of nifedipine may moderately increase.
Cimetidine and, to a lesser extent, ranitidine, increase the plasma concentration of nifedipine and thus enhance its antihypertensive effect.
Ethanol can enhance the effect of nifedipine (excessive arterial hypotension), which causes dizziness and other undesirable reactions.

Pregnancy

Adequate and strictly controlled safety studies Nifedipine not performed during pregnancy. The use of nifedipine during pregnancy is not recommended.
Since nifedipine is excreted in breast milk, its use during lactation should be avoided or breastfeeding should be discontinued during treatment.
In experimental studies, embryotoxic, fetotoxic and teratogenic effects of nifedipine were revealed.

Overdose

Symptoms of drug overdose Nifedipine: sharp bradycardia, bradyarrhythmia, arterial hypotension, in severe cases - collapse, slow conduction. When taking a large number of retard tablets, signs of intoxication appear no earlier than after 3-4 hours and can additionally be expressed in loss of consciousness up to coma, cardiogenic shock, convulsions, hyperglycemia, metabolic acidosis, hypoxia.
Treatment: gastric lavage, activated charcoal, the introduction of norepinephrine, calcium chloride or calcium gluconate in atropine solution (in/in). Hemodialysis is ineffective.

Storage conditions

List B. In a dark place.

Release form

Coated tablets containing 0.01 g (10 mg) of the drug. Long-acting tablets nifedipine retard 0.02 g (20 mg). Solution for infusion (1 ml contains 0.0001 g of nifedipine) in 50 ml vials, complete with a Perfusor (or Injectomat) syringe and a Perfusor (or Injectomat) polyethylene tube. Solution for intracoronary administration (1 ml contains 0.0001 g of nifedipine) in 2 ml syringes in a pack of 5 pieces.

Compound

2,6-Dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester.
Yellow crystalline powder. Practically insoluble in water, hardly soluble in alcohol.
Nifedipine (fenigidin) is the main representative of calcium ion antagonists - derivatives of 1,4-dihydropyridine.

Synonyms

Adalat, Cordafen, Cordipin, Corinfar, Nifangin, Nifecard, Nificard, Adarat, Calcigard, Nifacard, Nifelat, Procardia, Fenigidin, Cordaflex, Nifesan, Apo-Nifed, Depin E, Dignoconstant, Nifadil, Nifebene, Nifehexal, Nifedipat, Novo-Nifidin , Pidilat, Ronian, Sanfidipin, Fenamon, Ecodipin.

Additionally

Nifedipine is also part of the Calbet preparation.
Nifedipine corresponds to the domestic drug - fenigidin (Рhenyhydinum; Рhenigidin, Рhenihidin).

Main settings

Name:	NIFEDIPINE
ATX code:	C08CA05 -

A cardiological agent that is used to lower blood pressure. Not applicable in pediatrics. Drugs based on nifedipine from various manufacturers are available in pharmacies. It is prescribed, as a rule, for long-term use. The daily dosage and frequency of administration are selected only by the doctor individually for each patient. It can also be used in emergency cases for the relief of a hypertensive crisis.

Dosage form

Nifedipine is available on the pharmaceutical market in the form of tablets for oral administration. Externally, the tablets are round, coated yellow. 1 tablet contains 10 or 20 mg of the active ingredient - nifedipine. The drug belongs to calcium channel blockers. Produced in a carton box with blisters No. 5, which contain 50 tablets.

Description and composition

Nifedipine is a drug for the prevention and treatment of diseases of the heart and blood vessels. Taking pills allows you to block calcium channels, expand peripheral vessels, and nourish the heart muscle with the necessary amount of oxygen. The instructions for the drug say that taking Nifedipine leads to a decrease in muscle tone of smooth muscles, thereby normalizing blood pressure.

The drug Nifedipine is often used in the practice of cardiologists and neurologists for the complex treatment of diseases such as hypertension, heart failure. Its reception can reduce the risk of hypertensive crisis, myocardial infarction and other serious conditions. Reviews about the drug are not bad enough. Many patients note not only a good therapeutic effect after taking, but also the affordable cost of the drug.

The basis of the drug is nifedipine, and auxiliary components are also present in its composition.

Pharmacological group

Nifedipine tablets are an antihypertensive drug from the group of calcium channel blockers. It is used in the complex therapy of pathologies affecting the cardiovascular system, in diseases accompanied by an increased level of blood pressure. The active ingredient of the drug refers to derivatives of 1,4-dihydropyridine. The action of the drug allows you to reduce the flow of calcium ions into the tissues of the heart muscle, coronary arteries and peripheral arterial vessels. Taking the drug has the ability to reduce the concentration of ions inside the cells than cause the expansion of arterial and coronary vessels, reducing high blood pressure. Nidedipine, which is the basis of the drug, enhances blood flow, provides myocardial cells with a sufficient amount of glucose, oxygen and other nutrients.

After oral administration of tablets, they act quickly enough, their components penetrate into the blood stream, after which they are evenly distributed in the body. The effect after taking the medicine will be noticeable after 20-30 minutes and will last throughout the day. The drug is metabolized in the liver, excreted by the kidneys. Nifedipine can be used in combination with other drugs to treat diseases affecting the cardiovascular system. The drug can be taken only as directed by a doctor who can select the required dose of the drug, give useful recommendations for the treatment of the underlying disease affecting the heart and blood vessels.

Indications for use

Nifedipine tablets are intended for the treatment and prevention of diseases of the cardiovascular system in adults.

For adults

Among the main indications for the appointment of Nifedipine tablets include:

Arterial hypertension.
Hypertensive crisis and its prevention.
Heart failure.
Cardiac ischemia.
Angina pectoris.

Tablets are often used in combination with bronchodilators for the maintenance treatment of asthma in adults. Nifedipine can also be used for other conditions that disrupt the functioning of the heart and blood vessels, but in any case, only a doctor can prescribe the drug, select its dose.

For kids

Nifedipine in the form of tablets is not used in pediatric practice. The drug can be taken by persons over 18 years of age.

During the period of bearing a child, as well as during lactation, the drug is contraindicated. Its use can harm the fetus and the pregnancy itself. An exception to the appointment of the drug may be arterial hypertension in pregnant women, when taking other drugs does not bring the desired effects.

Contraindications

Nifedipine has a number of contraindications for use, which you need to familiarize yourself with before taking the drug:

Composition intolerance.
Acute myocardial infarction.
Hypotension.
Tachycardia.
Children under 18.
Pregnancy, breastfeeding.

With great care, you need to take the drug to people with impaired liver, kidney function, with peptic ulcer. The medicine is not prescribed for those who are on hemodialysis. Before prescribing the drug, the doctor must make sure that there are no contraindications to prescribing the drug.

Applications and doses

The instructions for the drug provide standard doses of the drug for adults. But the drug is intended for medical use, so the doctor can prescribe the dose of the drug specifically for each patient, taking into account all the characteristics of his body.

For adults

Nifedipine tablets are intended for internal use. In the process of taking the tablet, you need to swallow it whole, without chewing, drink plenty of water. The initial dose of the drug is 5-10 mg per day.

If the patient's history includes pathologies of the liver, kidneys, or the patient's age is over 65 years, the dose should be minimal, not exceeding 5 mg daily.

For kids

In the instructions for use of the dose of the drug for children are not available.

For pregnant women and during lactation

The drug can not be administered during pregnancy or lactation.

Side effects

When studying the instructions for using the drug, it is important to pay attention to possible side effects after taking the medicine. They are rare, but still in some cases, patients complain of the following symptoms:

Gynecomastia.
Allergic reactions.
Increase in daily diuresis.
Headache.
Hyperemia of the skin.
Ventricular tachycardia.
Chair disorder.
Arrhythmia.

The appearance of any of the above symptoms is a reason for discontinuation of the drug or correction of its daily dose.

Interaction with other drugs

Nifedipine tablets can be taken together with diuretics, antidepressants and other antihypertensive drugs, but before combining drugs with other pharmaceuticals, you should consult a specialist.

When taking Rifampicin, metabolic processes are accelerated, which can lead to a decrease in the effectiveness of Nifedipine. The drug is not compatible with alcohol, such an interaction increases the risk of side effects.

special instructions

Before using the drug - read the instructions.
Tablets can only be prescribed by a doctor.
Doses of medication are always determined by the attending physician.
The drug should not be combined with alcohol.
It is forbidden to abruptly stop taking the pills. This should be done gradually, reducing the dose.
You can combine the drug with other drugs on the recommendation of a doctor.
The drug is not intended for self-administration.

Overdose

headache;
hypotension;
pain and cramps in the abdomen;
nausea, urge to.

The appearance of such symptoms requires the use of sorbent preparations, gastric lavage. If the patient's condition does not improve, seek medical attention. In a hospital setting, the patient will receive the necessary help.

Storage conditions

The shelf life of the drug is 3 years from the date of its release. Tablets should be kept in a dark place, away from direct sunlight and children. The optimum storage temperature is not higher than +25°C.

Analogues

The drug has several analogues in composition and therapeutic effect. The choice of any similar drug should be left to the attending physician:

Retard.
Nifecard.

Analogues of the drug are produced by different manufacturers, domestic or foreign pharmaceutical companies, have different prices, but the same mechanism of action.

The price of the drug

The cost of the drug is an average of 34 rubles. Prices range from 26 to 49 rubles.

Calcium channel blockers, which include Nifedipine tablets, have been actively used in the treatment of hypertension and ischemic stroke since the 70s of the last century.

Recently, the drug has also been used in gynecology - both to normalize pressure and to reduce uterine hypertonicity during pregnancy in order to exclude premature birth. But in this case, the dosage is carefully selected, since its excess can harm the embryo.

Only the attending physician can prescribe Nifedipine for pressure - the drug is potent, has many side effects, and must be taken according to the scheme.

About the composition and principle of action

Nifedipine is a drug from the group of drugs for vascular and cardio therapy. The main active ingredient is a derivative of dihydropyridine. It is able to quickly relax the muscles of the vascular system, expand the arteries, increasing blood flow, which helps to reduce heart rate and pressure.

Due to this action, the drug can be used as an ambulance. The therapeutic effect occurs within 15-20 minutes after taking the drug. More than 90% of the active substance is absorbed through the villi of the intestinal tract, which reduces the load on the stomach, kidneys and liver, gallbladder.

Like other drugs in tablet form, Nifedipine also contains excipients. Before prescribing a remedy, the attending physician must make sure that the patient does not have intolerance to substances such as:

Most of the listed substances, with the exception of those from which the shell is made, are able to enhance the action of the main one, which ensures a high therapeutic effect.

With a long-term course of taking the drug, a prolonged form of the drug is prescribed, and for the relief of acute attacks of angina pectoris and hypertension, short-acting forms that do not have a shell.

In the reviews of medical specialists, there are often descriptions of the effective use of Nifedipine to relieve acute chest pain in patients with nitroglycerin intolerance.

How to take Nifedipine - instructions

Self-administration of Nifedipine is unacceptable, as is its administration without the supervision of a medical specialist who has thoroughly familiarized himself with the patient's condition and analyzes of his biological materials, ECG results. The instructions for use of Nifedipine indicate that the age of the patient is of great importance when choosing the dosage and duration of the course of treatment.

The maximum daily dose of the main active substance should not exceed 40 mg. Taking the drug cannot be accompanied by simply drinking water - the pill is taken with food, and it is better to choose liquid, light meals.

You can not drink natural juices or carbonated drinks, as they may contain aggressive substances that will dissolve the tablet shell before it enters the intestines.

Based on the results of the therapeutic action, the attending physician adjusts the single and daily intake, increasing or decreasing the dosage until the desired effect is achieved. In serious cases, the daily dose can reach 80 mg.

The duration of admission is determined individually. Abrupt withdrawal of the drug is not practiced, as this can cause the manifestation of undesirable side effects - increased heart rate, jumps in blood pressure, malfunctions of the intestines and blood-forming organs. Cancellation of the drug should occur gradually, with a decrease in single and daily doses, frequency of administration.

Nifedipine during pregnancy - indications and features of treatment

Many future mothers sincerely do not understand why Nifedipine is prescribed during pregnancy?

Sudden drops in blood pressure
Increased tone of the uterus,
Pathology of the heart and blood vessels.

For each period of bearing a baby, there are rules for taking this potent drug. It is important to understand that Nifedipine should not be taken during pregnancy on the advice of a person who does not have a medical education and is unfamiliar with the results of the patient's examination. Only a gynecologist who has been observing the patient for a long time has the right to give such appointments.

In the first trimester, Nifedipine is categorically contraindicated! It can have a negative impact on the formation of organs and the neural tube of the fetus, which will result in serious pathologies and congenital diseases. During this period, the drug can be prescribed only if, without it, the expectant mother risks dying.

In the second and third trimester, indications for the use of Nifedipine may be:

Instructions for the use of Nifedipine during pregnancy are developed individually by a gynecologist, with the obligatory participation of a general practitioner, in exceptional cases, a cardiologist. In no case should you violate the recommendations, skip a dose or exceed, reduce the dosage on your own.

Taking Nifedipine by pregnant women should be accompanied by medical supervision, that is, the patient should be in the hospital. This is necessary in order to track any changes in the condition of the expectant mother and adjust the dosage of the drug in a timely manner.

Contraindications and side effects

Not only indications for the use of Nifedipine, but also contraindications are strictly monitored. The drug should not be taken by children and adolescents. To solve vascular and cardiological problems in such cases, less active and aggressive substances are used.

In addition, contraindications to taking Nifedipine are such health problems as:

Against the background of taking Nifedipine, side effects often develop, which must be reported to the doctor who prescribed the drug.

Any manifestations of allergic reactions, lethargy and drowsiness, headaches and disorientation, swelling, hot flashes, nausea and malfunctioning of the intestines, exacerbation of joint diseases should alert.

The course of treatment should be accompanied by regular collection of the patient's biological materials - blood from a finger and a vein, urine. The attending physician monitors the content of glucose in the blood, the work of the liver and kidneys, the intensity of urination, the concentration of the main elements of the blood.

The instructions for use of Nifedipine tablets indicate at what pressure it can be used. Do not take the drug to those patients whose second blood pressure indicator often drops below 90.

The drug can provoke its further and sharp decrease, which can be life-threatening. In case of an overdose of Nifedipine, seek medical attention immediately.

If Nifedipine is prescribed as part of a course of treatment or against the background of other therapy, it is necessary to compare its interaction with the drugs already taken.

Nifedipine should not be taken with substances of similar action - diuretics and phenothiazines. Beta-blockers against the background of the action of the drug can provoke heart failure.

Foods and medicines containing calcium in the composition reduce the therapeutic efficacy of Nifedipine. With its course intake, it is necessary to exclude dairy products, nuts, fish, herbs and some types of fruits and berries from the diet.

It is categorically impossible to combine the intake of Nifedipine with alcohol. It greatly enhances the effect of the main substance of the drug, which can lead to death and other dangerous irreversible consequences - paralysis, disability.

Cost and analogues

If the attending physician prescribes such a potent drug, then pharmacists do not recommend replacing it with analogues.

The price of Nifedipine is quite acceptable, the drug is available to all social categories. The cost of a package with 50 tablets ranges from 30 to 50 rubles, depending on the region of sales and the pricing policy of the pharmacy chain. Inpatient treatment using this tool is free.

It is possible to replace Nifedipine only if it is not available in the clinic where the patient is treated or in the pharmacy. The list of drugs with a similar effect includes such drugs as:

Nifedipine (nifedipine)

Composition and form of release of the drug

10 pieces. - cellular contour packings (1) - packs of cardboard.
50 pcs. - cellular contour packings (1) - packs of cardboard.

pharmachologic effect

Selective class II, dihydropyridine derivative. It inhibits the entry of calcium into cardiomyocytes and vascular smooth muscle cells. It has antianginal and hypotensive effects. Reduces the tone of vascular smooth muscle. Expands the coronary and peripheral arteries, reduces OPSS, blood pressure and slightly - myocardial contractility, reduces afterload and myocardial oxygen demand. Improves coronary blood flow. Virtually no antiarrhythmic activity. Does not inhibit myocardial conduction.

Pharmacokinetics

When taken orally, it is rapidly 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. T 1/2 - about 2 hours. It is excreted mainly by the kidneys in the form of metabolites and in trace amounts unchanged; 20% is excreted through the intestines as metabolites.

Indications

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

Contraindications

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

Dosage

Individual. For oral administration, the initial dose is 10 mg 3-4 times / day. If necessary, the dose is gradually increased to 20 mg 3-4 times / day. In special cases (variant angina pectoris, severe arterial hypertension) for a short time, the dose can be increased to 30 mg 3-4 times / day. For the relief of a hypertensive crisis, as well as an attack of angina pectoris, 10-20 mg (rarely 30 mg) can be used sublingually.

In / in for the relief of an attack of angina pectoris or a hypertensive crisis - 5 mg for 4-8 hours.

Intracoronary for the relief of acute spasms of the coronary arteries, a bolus of 100-200 mcg is administered. With stenosis of large coronary vessels, the initial dose is 50-100 mcg.

Maximum daily doses: when taken orally - 120 mg, with a / in the introduction - 30 mg.

Side effects

From the side of the cardiovascular system: hyperemia of the skin, a feeling of warmth, tachycardia, arterial hypotension, peripheral edema; rarely - bradycardia, ventricular tachycardia, asystole, increased angina attacks.

From the digestive system: nausea, heartburn, diarrhea; rarely - deterioration of liver function; in isolated cases - gingival hyperplasia. With prolonged use in high doses, dyspeptic symptoms, increased activity of hepatic transaminases, intrahepatic cholestasis are possible.

From the side of the central nervous system and peripheral nervous system: headache. With prolonged use in high doses, paresthesia, muscle pain, tremor, mild visual disturbances, and sleep disturbances are possible.

From the hematopoietic system: in isolated cases - leukopenia, thrombocytopenia.

From the urinary system: increase in daily diuresis. With prolonged use in high doses, impaired renal function is possible.

From the endocrine system: in isolated cases - gynecomastia.

Allergic reactions: skin rash.

Local reactions: when administered intravenously, a burning sensation at the injection site is possible.

Within 1 min after intracoronary administration, a negative inotropic effect of nifedipine, an increase in heart rate, and arterial hypotension are possible; these symptoms gradually disappear after 5-15 minutes.

drug interaction

With simultaneous use with diuretics, phenothiazine derivatives, the antihypertensive effect of nifedipine is enhanced.

With simultaneous use with anticholinergics, memory and attention impairments are possible in elderly patients.

With simultaneous use with possible development of severe arterial hypotension; in some cases - the development of heart failure.

With simultaneous use with nitrates, the antianginal effect of nifedipine is enhanced.

With simultaneous use with calcium preparations, the effectiveness of nifedipine decreases due to the antagonistic interaction caused by an increase in the concentration of calcium ions in the extracellular fluid.

Cases of the development of muscle weakness have been described with simultaneous use with magnesium salts.

With simultaneous use with it is possible to slow down the excretion of digoxin from the body and, consequently, increase its concentration in the blood plasma.

With simultaneous use with diltiazem, the antihypertensive effect is enhanced.

With simultaneous use with possible changes in the concentration of theophylline in the blood plasma.

Rifampicin induces the activity of liver enzymes, accelerating the metabolism of nifedipine, which leads to a decrease in its effectiveness.

With simultaneous use 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, itraconazole.

With simultaneous use with fluoxetine, the side effects of nifedipine may increase.

In some cases, with simultaneous use with quinidine, a decrease in the concentration of quinidine in the blood plasma is possible, and when nifedipine is canceled, a significant increase in the concentration of quinidine is possible, which is accompanied by a prolongation of the QT interval on the ECG.

Cimetidine and, to a lesser extent, ranitidine, increase the plasma concentration of nifedipine and thus enhance its antihypertensive effect.

Ethanol can enhance the effect of nifedipine (excessive arterial hypotension), which causes dizziness and other undesirable reactions.

special instructions

Nifedipine should only be used in a clinical setting under the strict supervision of a physician in acute myocardial infarction, severe cerebrovascular accident, diabetes mellitus, impaired liver and kidney function, in malignant arterial hypertension and hypovolemia, as well as in patients on hemodialysis. In patients with impaired liver and / or kidney function, high doses of nifedipine should be avoided. Elderly patients are more likely to have reduced cerebral blood flow due to severe peripheral vasodilation.

When taken orally, nifedipine can be chewed to accelerate the effect.

If pain behind the sternum appears during treatment, nifedipine should be discontinued. Cancel nifedipine should be gradual, because with a sudden discontinuation of the reception (especially after long-term treatment), the development of a withdrawal syndrome is possible.

With intracoronary administration in the presence of stenosis of two vessels, nifedipine should not be injected 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 an excessive decrease in blood pressure.

Influence on the ability to drive vehicles and control mechanisms

At the beginning of treatment, driving vehicles and other potentially hazardous activities that require quick psychomotor reactions should be avoided. In the course of further treatment, the degree of restriction is determined depending on the individual tolerability of nifedipine.

Pregnancy and lactation

Adequate and well-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 breastfeeding should be discontinued during treatment.

V experimental studies embryotoxic, fetotoxic and teratogenic effects of nifedipine were revealed.

For impaired renal function

In case of impaired renal function, Nifedipine should be used only in a clinic under the strict supervision of a physician. In patients with impaired renal function, high doses of nifedipine should be avoided.

For impaired liver function

In case of impaired liver function, Nifedipine should be used only in a clinic under the strict supervision of a physician. In patients with impaired liver function, high doses of nifedipine should be avoided.

Use in the elderly

Elderly patients are more likely to have reduced cerebral blood flow due to severe peripheral vasodilation.

Nifedipine: instructions for use and reviews

Nifedipine is a calcium channel blocker.

Release form and composition

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

Active substance: nifedipine, in 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, refers to derivatives of 1,4-dihydropyridine. The drug has antianginal, hypotensive and vasodilating effects. It reduces the current of calcium ions into the smooth muscle cells of peripheral and coronary arteries, as well as into cardiomyocytes. In high doses, nifedipine inhibits the release of calcium ions from the depot inside the 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 heart muscle, mediated by troponin and tropomyosin. In therapeutic doses, the drug normalizes the transport of calcium ions across the membrane, which is disturbed in certain pathological conditions, such as arterial hypertension.

Nifedipine does not affect the tone of the veins. 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. Almost no effect on the atrioventricular and sinoatrial nodes and has no antiarrhythmic effect. Increases blood flow in the kidneys, causes a moderate excretion of sodium in the urine.

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

Pharmacokinetics

Nifedipine is quickly and almost completely (92-98%) absorbed in the digestive tract. The bioavailability of the drug after oral administration is from 40 to 60% (reception along with food increases this figure). Nifedipine undergoes a first pass effect through the liver. In 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 in 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 as inactive metabolites by the kidneys and another 20% in the bile. The half-life is from 2 to 4 hours. With insufficiency of liver function, the total clearance decreases, the half-life is prolonged.

Nifedipine does not accumulate in the body. Chronic renal insufficiency, 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 accelerate elimination.

Indications for use

Angina at rest and exertion (including variant) in 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 mm Hg;
Idiopathic hypertrophic subaortic stenosis;
Tachycardia;
Period 4 weeks after acute myocardial infarction;
Age up to 18 years;
Hypersensitivity to the drug or other derivatives of dihydropyridine.

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 disorders of cerebral circulation;
Severe violations of kidney / liver function;
Chronic heart failure;
Malignant arterial hypertension.

Caution requires the use of the drug by patients on hemodialysis.

Instructions for use of Nifedipine: method and dosage

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

Doses are set individually depending on the severity of the course 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.

The maximum allowable daily dose is 40 mg of nifedipine (4 tablets).

Dose reduction is required for the elderly, patients with impaired liver function, severe disorders of cerebral circulation, as well as patients receiving combination therapy (antihypertensive or antianginal).

Side effects

Cardiovascular system: feeling of heat, flushing of the face, 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 prolonged use in high doses - tremor, paresthesia of the extremities;
Gastrointestinal tract, liver: dyspeptic disorders; with long-term treatment - abnormal liver function (increased activity of hepatic transaminases, intrahepatic cholestasis);
Musculoskeletal system: myalgia, arthritis;
Urinary system: an increase in daily diuresis, in patients with renal insufficiency - a deterioration in kidney function;
Organs of hematopoiesis: thrombocytopenia, leukopenia, thrombocytopenic purpura, anemia;
Allergic reactions: exanthema, urticaria, pruritus, autoimmune hepatitis;
Others: gum hyperplasia, hyperglycemia, changes in visual perception, flushing of the skin of the face, in the elderly - gynecomastia (completely disappearing after discontinuation of the drug).

Overdose

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

As first aid, gastric lavage and activated charcoal are recommended. The ongoing symptomatic therapy is aimed at stabilizing the work of the cardiovascular system. Nifedipine's antidote is calcium. Requires slow intravenous administration of calcium gluconate or 10% calcium chloride at a dose of 0.2 ml / kg (total no more than 10 ml) for 5 minutes. If the effect is not achieved, it is possible to conduct a repeated infusion under the control of serum calcium concentration. The 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.

With a serious decrease in blood pressure, the patient is administered dopamine or dobutamine intravenously. If cardiac conduction is impaired, the administration of isoprenaline, atropine, or the establishment of a pacemaker (artificial pacemaker) is indicated. Developing heart failure should be compensated by intravenous administration of strophanthin. Catecholamines are allowed to be used only in case of circulatory failure, life-threatening. It is desirable to control the level of electrolytes (calcium, potassium) and blood glucose.

Carrying out hemodialysis is ineffective.

special instructions

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

During treatment with Nifedipine, it is necessary to refrain from drinking alcohol, driving vehicles and performing potentially hazardous types of work that require quick psychophysical reactions and increased concentration.

Influence on the ability to drive vehicles and complex mechanisms

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

Use during pregnancy and lactation

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

Application in childhood

Nifedipine should not be used in children and adolescents under 18 years of age, as the safety and efficacy of the drug in this age group has not been established.

For impaired renal function

Nifedipine should be used with caution in patients with severe renal impairment.

For impaired liver function

Nifedipine should be used with caution in patients with severe hepatic impairment.

Use in the elderly

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

drug interaction

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