Nifedipine instructions for use, contraindications, side effects, reviews. Nifedipine: immediate reduction in blood pressure


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 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.

Composition

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, Nifeheksal, 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 parameters

Name: NIFEDIPINE
ATX code: C08CA05 -

Hypertensive crisis, the sudden onset of pain behind the sternum, require urgent intervention. Nifedipine - instructions for the use of which stipulates the effective action of the drug as an ambulance, helps to lower blood pressure, relieve an attack. What is the principle of the drug, in what cases does it help to cope with the disease, are there any contraindications for use - more on this in the instructions for use.

What is Nifedipine

The drug Nifedipine (Nifedipine) refers to antihypertensive drugs of vascular, cardiac therapy. It is a member of the calcium channel blockers group. The instruction describes the features of the action of the drug, which:

  • relaxes the smooth muscles of blood vessels;
  • dilates arteries;
  • reduces the heart's need for oxygen;
  • increases blood flow;
  • reduces the heart rate.

The advantage of Nifedipine, as stipulated by the instructions for use, is that the remedy:

  • used for chronic diseases and as an emergency;
  • has antihypertensive property - lowers blood pressure;
  • at the same time it has an antianginal effect - it reduces pain behind the sternum;
  • quickly restores cells affected by ischemia.

pharmachologic effect

According to the instructions, the use of Nifedipine blocks the activity of slow calcium channels of the cell membrane. From this action, the flow of calcium ions into the muscles, arteries of the heart, and peripheral vessels decreases. Processes occur at the cellular level. As a result:

  • activation of blood circulation in the heart;
  • increase in the lumen of the coronary, arterial vessels;
  • increased blood flow in the kidneys;
  • decrease in pressure;
  • decrease in vascular resistance to blood flow in the periphery.

The medicine does not accumulate in the body. After using Nifedipine inside:

  • the active substance is absorbed from the gastrointestinal mucosa;
  • enters the bloodstream, binds to plasma proteins, stays in the body for a long time;
  • the composition is metabolized in the liver, forming decay products;
  • the remains are excreted from the body with urine - half the dose during the day;
  • bioavailability increases after a meal.

Composition

Instructions for use specifies the composition of the drug. The main active ingredient is nifedipine. Auxiliary components:

  • potato starch;
  • milk sugar;
  • povidone 25;
  • microcrystalline cellulose;
  • magnesium stearate;
  • sodium lauryl sulfate;
  • twin 80;
  • hypromelosis;
  • titanium dioxide E171;
  • talc;
  • macrogol 6000;
  • quinoline yellow E 104.

Release form

Instructions for use Nifedipine stipulates that the drug is available in several forms. Each has its own use and action. Doctors prescribe:

  • Dragee - balls with a pleasant taste. They can be swallowed, but for a quick effect, it is better to dissolve under the tongue. Used as an ambulance to relieve symptoms.
  • Solution for intravenous administration - used in the clinical conditions of cardiology departments, with intensive care.
  • Syringes with composition for intracoronary administration.
  • Gel for the treatment of hemorrhoids.

A special conversation about Nifedipine tablets. According to the instructions, two types are used:

  • Short action. The medicine is used to urgently reduce high blood pressure, eliminate retrosternal pain for patients in whom seizures are rare.
  • Long acting nifedipine. The drug is prescribed for daily intake in order to maintain a stable condition of a patient with arterial hypertension, coronary heart disease. It is easy to choose an individual course of compensatory therapy - tablets are available with a variety of dosages.

Indications for use

According to the instructions for use, Nifedipine is used to treat high blood pressure. When it is used, a hypertensive crisis is quickly stopped. Nifedipine may be recommended for:

  • angina pectoris;
  • spasm of the coronary arteries;
  • Raynaud's syndrome;
  • congestive cardiopulmonary insufficiency;
  • arterial hypertension of any degree;
  • hypertrophic cardiomyopathy.

Excellent reviews have the drug Nifedipine from cardiologists, therapists. In accordance with the instructions, its use is effective in diagnosing:

  • pulmonary hypertension;
  • disorders of cerebral circulation;
  • hypertensive crisis;
  • blockage of blood vessels;
  • heart failure;
  • stagnation of blood;
  • ischemic heart disease;
  • atherosclerosis of peripheral arteries;
  • bronchospasms.

Instructions for use Nifedipine

The guide to the drug specifies the composition, indications for use, contraindications and side effects. Instruction Nifedipine warns:

  • the maximum dosage should not exceed 30 mg per day;
  • it is permissible for women during pregnancy to take the medicine from the 16th week under the supervision of a doctor so as not to harm the fetus;
  • the duration of treatment, the dosage is prescribed by the doctor;
  • Nifedipine during breastfeeding requires a transition to artificial nutrition for the duration of treatment.

Side effects

With an increase in the dosage of Nifedipine, according to the instructions for use, side effects may occur. Changes affect the whole body. Observed from the system:

  • cardiovascular - tachycardia, low blood pressure, palpitations, chest pain, fainting, angina attacks;
  • central nervous - dizziness, drowsiness, fatigue, headache, swallowing problems, depression.

The drug Nifedipine at high dosages can cause allergic reactions, itching, dermatitis, anaphylactic shock, Quincke's edema. There are side effects from other body systems:

  • respiratory - the development of shortness of breath, cough, bronchospasm;
  • digestive - nausea, increased appetite, diarrhea, constipation, dry mouth, abnormal liver function;
  • urinary - deterioration of kidney function;
  • musculoskeletal system - hand tremor, joint swelling, myalgia;
  • hematopoietic organs - thrombocytopenia, leukopenia, anemia.

Contraindications

Instructions for use warns of the presence of contraindications. A doctor should prescribe a medication to eliminate the risk of complications. Since the drug greatly reduces pressure, care must be taken. It is forbidden to use Nifedipine in case of:

  • acute myocardial infarction;
  • severe form of heart failure;
  • unstable angina;
  • arterial hypotension;
  • cardiogenic shock;
  • narrowing of the mitral valve;
  • tachycardia;
  • bradycardia.

Although the drug is available, it is inexpensive, according to the instructions, it is contraindicated to carry out drug treatment when:

  • pregnancy;
  • lactation;
  • hypersensitivity to components;
  • allergic reactions;
  • cardiac arrhythmias;
  • hepatic, renal failure;
  • obstruction of the gastrointestinal tract;
  • disorders of cerebral circulation;
  • elderly, children's age - up to 18 years.

Interaction

When prescribing the drug, the doctor should study the instructions for use in order to know the interaction of Nifedipine with other drugs. This is important for the health of the patient. When used simultaneously with:

  • Rifampicin - efficiency decreases;
  • Fluoxetine - more side effects;
  • nitrates - tachycardia increases;
  • ethanol - pressure reduction is activated;
  • beta-blockers - heart failure develops.

special instructions

The instruction stipulates special points that are important during the use of Nifedipine. These include the treatment of the elderly, when a lower dose is required, careful monitoring of kidney function. Factors to consider:

  • it is necessary to give up alcohol for the period of treatment;
  • it is necessary to limit work that requires speed of reaction, concentration of attention;
  • exclude the use of vehicles.

Important points when using Nifedipine - the need:

  • gradual withdrawal of the drug;
  • regular treatment, even if the condition improves, if a prolonged-release medication is prescribed;
  • reducing the dose of the drug in patients with liver dysfunction and cerebrovascular accident;
  • informing the anesthesiologist in case of need for a surgical operation under general anesthesia.

Nifedipine tablets are necessary for hypertensive patients and are a common remedy for pressure , eliminating pain, reducing ischemia.

The drug is produced in several versions:

  • adalat - solution for intravenous administration;
  • short acting tabletsremove the crisis (cordaflex, nifedipine, cordafen, cordipin, fenigidin);
  • long-acting drug that is drunklong-term (cordaflex rd, corinfar, nifecar chl, calciguard retard, osmo-adalat).

Listed medicines for pressure combines the active substance, the mechanism of action on the body and the pharmacological effect. Differ from downgrading AD drugs by the duration of the result obtained, the speed of the onset of the effect from the moment of taking / administering the medication. Given the differences, each form has its own indications, which the doctor must know about.

How does nifedipine affect the body?

Learn more about Nifedipine instructions for use, at what pressureand how to take, what side effects and contraindications. However, it is not necessary to understand medical terminology. The active substance is classified as a Ca-channel blocker. This means that the channels in the cell wall through which calcium enters are blocked.

Many calcium channels in the muscles, including the heart. Penetrating into the cell, calcium provokes excitation, causing a contraction of muscle tissue.

Under conditions of blocking calcium channels, much of it will not enter the cell, which means that the lumen in the vessels will expand, because their walls of their circular muscle fibers will not actively contract under the influence of calcium.

Due to the expansion of the cardiac arteries, blood flow to the myocardium improves, and the increased lumen of distant arteries provides a decrease pressure . The vascular walls relax, the lumen of the veins and arteries increases, the frequency of myocardial contractions succeeds reduce.

Dilated blood vessels, through which blood circulates to the heart and brain, provide blood flow to the main organs, the supply of glucose and oxygen. Against the background of such favorable conditions, cells affected by ischemia and pathologies are poorly restored.

When is Nifedipine prescribed?

pressure medication prescribed for various pathologies, each time selecting the appropriate form of medication:

  • as a prophylaxis of angina pectoris in patients with ischemic disease;
  • in order to reduce vasospasm in patients with Prinzmetal's angina;
  • for downhill pain in the chest if nitroglycerin is not possible take ;
  • to control blood pressure in hypertensive patients in the long term;
  • to quickly to stop a hypertensive crisis;
  • with Raynaud's syndrome to relieve spasms of distant blood vessels.

An intravenous liquid form of the drug is administered in a hospital if the patient is in serious condition. Short acting tablets fast reduce blood pressure, used in case of an acute attack of angina pectoris and hypertension.

For long-term treatment of hypertension, indicators pressure normalized with prolonged-release tablets.

Dosage of the drug


If the patient has read the instructions and knows what dosagereduces pressure, with hypertension, act according to the principle: “what I want, then drink ' is dangerous. The doctor can prescribe pills, they act individually for each patient.

The standard daily dosage is 30-80 g. If short-acting tablets are taken, then the daily dose is divided into 3-4 doses, and if long-acting tablets are prescribed, they are taken 1-2 times a day. In case of severe hypertension and variant angina pectoris, the daily dosage can be increased to 120 mg for some time, but as prescribed by the doctor and when the drug is well tolerated. The maximum daily dose is 120 mg.

When you need to remove the pressure surge, put a 10-20 mg tablet under the tongue, which will work for 15 minutes. Do the same for chest pain. In the hospital, an attack of angina pectoris or a crisis is stopped by intravenous administration of Nifedipine in a volume of 5 mg / h, the daily rate is 30 mg.

An overdose of the drug is manifested by facial swelling, headache, prolonged pressure drop, bradycardia, bradyarrhythmia and the absence of a pulse in distant arteries. In case of severe intoxication, loss of consciousness and collapse are possible.

To provide first aid, you need to do a gastric lavage, then prescribe activated charcoal at the rate of 1 tablet per 10 kg of body weight. Nifedipine's drug antidote is calcium; calcium chloride or calcium gluconate in a 10% solution is administered to help the patient.

Adverse reactions

Like other pressure pills, Nifedipine causes side reactions in the body:

  • from the gastrointestinal tract: diarrhea, nausea, heartburn and liver failure. If you take the drug for a long time in high doses, this will affect the liver in the form of cholestasis or an increase in transaminases;
  • from the side of the cardiovascular system: swelling of the skin and extremities, a strong drop in pressure, a feeling of warmth, asystole, tachycardia, bradycardia, angina pectoris;
  • from the side of the central and peripheral nervous system: headaches, with prolonged use, muscle pain, sleep problems, tremors and visual disturbances;
  • from the genitourinary system: increased diuresis, against the background of long-term use - failure of the kidneys;
  • on the part of hematopoiesis: leukopenia and thrombocytopenia;
  • from the endocrine system - a manifestation of gynecomastia.

As an allergy to the components of Nifedipine, a rash on the skin, burning at the injection site is possible. With intravenous administration, an increase in the frequency of myocardial contractions and the development of hypotension are possible.

Contraindications

Nifedipine is not prescribed for hypotension, collapse, severe aortic stenosis, cardiogenic shock, severe heart failure, acute myocardial infarction, tachycardia, minors.

Pregnant and lactating Nifedipine is not recommended, although in gynecological practice there are cases when the drug was necessary in case of ineffectiveness of the drugs. In such cases, the doctor weighs the risks, and may prescribe the drug in late pregnancy in order to stop the hypertensive crisis and normalize the condition of the expectant mother.

In pregnant women, Nifedipine reduces the tone of the uterus, but clinical studies on this issue have not been conducted. It is strictly forbidden for pregnant women to drink the medicine on their own, the decision should be made by the doctor.

A similar appointment with caution applies to patients with diabetes mellitus, malignant arterial hypertension, serious circulatory disorders in the brain, malfunctions of the kidneys and liver.

The effectiveness of Nifedipine

Since the development of the drug, there have been enough international studies on the effectiveness, according to the results, reports are presented on the benefits, safety and feasibility of prescribing Nifedipine. In 2000, the results of the INSIGHT study were presented, according to which the drug is safe, effectively helps with hypertension, is well tolerated compared to diuretics, and helps reduce the risk of heart attack and stroke in hypertensive patients.

The results of the Action study confirmed the safety of long-acting nifedipine, its ability to reduce the need for coronary artery bypass grafting and coronary angiography. In combination with other drugs, Nifedipine improves the prognosis in hypertensive patients and patients with angina pectoris, including the state after myocardial infarction.

In the recommendations of the European Society of Cardiology there are notes on the positive effect of long-acting nifedipine on the health of patients with stable angina, both in monotherapy and in combination with nitrates and beta-blockers.

Short-term tablets are recommended as a means of emergency care for a hypertensive crisis, if taken for a long time, this is fraught with complications.

Drug Interactions


Before prescribing pills for pressure, the doctor will assess the patient's condition, refer him for diagnosis, select the dosage and regimen of therapy. You need to tell your doctor if you are taking medications, as Nifedipine does not work well with all of them.

The combined use of Nifedipine with diuretics, nitrates, tricyclic antidepressants leads to an accumulation of the effect and an increase in the pressure-reducing effect.

In combination with beta-blockers, the hypotensive effect increases, heart failure develops. Cimetidine together with Nifedipine increases the concentration of the latter in the blood plasma. If you take Rifampicin against the background of Nifedipine, then the metabolism of the latter will accelerate, the effectiveness of its action on the body will decrease.

It is important to consider that long-term treatment of patients with high blood pressure or coronary artery disease is carried out with long-acting drugs. It is valid for 12-24 hours. As for short-term tablets, they should be used as an ambulance for a hypertensive crisis, when you need to effectively and quickly reduce blood pressure.

According to research and practice, if you use short-acting Nifedipine for a long time, this is fraught with a stroke or heart attack.

The doctor selects the dosage of tablets individually in each individual case. Self-treatment, relying on the instructions for the drug - is not worth it, this can lead to dangerous consequences.

Selective calcium channel blocker class II, dihydropyridine derivative
Drug: NIFEDIPINE

The active substance of the drug: nifedipine
ATX encoding: C08CA05
CFG: Calcium Channel Blocker
Registration number: P No. 015233/01
Date of registration: 12.05.08
The owner of the reg. Award: BALKANPHARMA-DUPNITZA AD (Bulgaria)

Nifedipine release form, drug packaging and composition.

Dragee of the correct form, yellow; at the break - 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) - packs of cardboard.

DESCRIPTION OF THE ACTIVE SUBSTANCE.
All the information provided is provided only for familiarization with the drug, you should consult a doctor about the possibility of using it.

Pharmacological action Nifedipine

Selective calcium channel blocker class II, dihydropyridine derivative. It inhibits the entry of calcium into cardiomyocytes and vascular smooth muscle cells. It has antianginal and hypotensive effect. Reduces the tone of vascular smooth muscle. It dilates the coronary and peripheral arteries, reduces peripheral vascular resistance, 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 of the drug.

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. T1 / 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 for use:

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

Dosage and method of application of the drug.

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 doses: when taken orally - 120 mg / day, with intravenous administration - 30 mg / day.

Side effects of Nifedipine:

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: an 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: with intravenous administration, burning 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.

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

Special instructions for the use of Nifedipine.

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 a 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.

Interaction of Nifedipine with other drugs.

With simultaneous use 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.

Extensive. The drug belongs to the group of drugs that block calcium channels, which have pronounced antihypertensive properties.

But the medicine not only reduces pressure, it has an anti-ischemic effect. What is the medicine Nifedipine, what are these tablets prescribed for and in what dosages, this article will tell.

Nifedipine not only reduces, but also protects the myocardium from lack of oxygen, as well as overloads that occur with high peripheral vascular resistance. The drug reduces the stretching of the heart muscle, enhancing its metabolic processes.

The drug Nifedipine indications for use has the following:

  • hypertension syndrome;
  • chronic heart failure;
  • angiospathic circulatory disorders of the brain;
  • ischemia;
  • bradycardia and angina pectoris;
  • spasm of the vessels of the inner ear and retina.

Long-acting nifedipine in combination with bronchodilators is prescribed as maintenance therapy for bronchial asthma and Raynaud's disease.

Efficacy in hypertension

The hypotensive effect of Nifedepine is expressed in slowing down the movement of calcium through the membrane of the smooth muscle cells of the arteries.

Calcium ions spasm the vessels and increase their contraction, and the drug blocks their flow.

It provides an expansion of the lumen of the coronary and peripheral branches of the arterial network, while there is a decrease in the resistance of the walls of blood vessels and a decrease in the load on the heart. The drug is well absorbed into the digestive tract, thus its action begins in the first ten minutes after consumption, which is especially important in hypertensive crisis.

Composition and forms of the drug

The international non-proprietary name of the drug Nifedipine (INN) is Nifedipine.

Nifedipine is available in various dosage forms:

  1. coated tablets. They contain 10 mg of nifedipine and the long-acting tablets contain 20 mg. Excipients: corn starch - 58.25 mg, polysorbate - 2 mg, lactose monohydrate - 36.2 mg, hypromellose - 2.4 mg, microcrystalline cellulose - 51 mg, magnesium stearate - 150 mcg. The film shell contains: talc, hypromellose - 4.2 mg, macrogol - 1.4 mg, titanium dioxide - 1 mg, red oxide - 200 mcg;
  2. capsules of 5 mg and 10 mg;
  3. solution for infusion. The volume of vials is 50 ml. One milliliter in 1 ml contains 0.0001 g of nifedipine;
  4. solution for intracoronary administration is available in 2 ml syringes, in 1 ml - 0.0001 g of nifedipine.

The use of the drug and dose

The recommended dose of the drug is 20 mg twice a day. If the desired effect has not been achieved, it is increased to 40 mg twice a day. The maximum rate is 80 mg. For liver problems, it should not exceed 40 mg.

Tablets Nifedipine 10 mg

Rules for the use of Nifedipine:

  • the tablet is taken half an hour before breakfast at the same time;
  • the medicine is washed down only with clean water;
  • Do not chew or divide long-acting tablets.

You cannot stop taking Nifedipine on your own, if you want to reduce the dose of the drug, the doctor should adjust the treatment regimen.

From pressure Nifedipine can be taken regardless of the meal. It will enter the blood more slowly, but its effectiveness will not decrease.

The use of the drug requires compliance with certain rules:

  1. the drug is used only under the supervision of a doctor. Carefully take the medicine for diabetic disease, severe forms of cerebral circulation disorders, problems with the kidneys and liver, hypovolemia;
  2. during treatment with Nifedipine, alcohol should be completely abandoned. At the beginning of treatment, it is not recommended to drive;
  3. it is necessary to consider with which drugs the drug can be combined, and with which it is not worth it. Nifedipine with tricyclic antidepressants, diuretics, nitrates, pressure-reducing agents enhances the hypotensive effect. The combined use of the drug with beta-blockers can contribute to the development of heart failure. Joint use with cimetidine increases the concentration of the drug in the blood. Rifampicin accelerates the metabolism of nifedipine, which reduces its effectiveness.

Short-acting tablets are drunk three times, those that are excreted in 12 hours are consumed twice a day, prolonged-acting tablets are taken once. It is advisable to administer the drug intravenously only in a hospital.

The intake of the drug depends on its half-life.

Contraindications

With collapse, cardiogenic shock, tachycardia, aortic stenosis, acute stage of infarction, severe heart failure, sensitivity to the components of the drug. Children and patients under 18 years of age are not prescribed this medicine.

The drug may cause side effects:

  1. from the digestive organs: diarrhea, heartburn, nausea, disruption of the liver. With prolonged use of the drug with the appointment of high doses, the manifestation of dyspeptic symptoms, the development of intrahepatic cholestasis are possible;
  2. from the hematopoietic organs: thrombocytopenia, leukopenia;
  3. from the side of the heart and blood vessels: redness of the skin, a feeling of heat, the appearance of edema, a sharp decrease in pressure, tachycardia, angina pectoris, bradycardia;
  4. from the urinary tract: increased urine output, impaired kidney function;
  5. from the side of the central nervous system: headaches, sleep disturbances, visual disturbances, tremor of the extremities;
  6. from the endocrine system: gynecomastia;
  7. from the side of the skin: rash.

If the dose exceeded 120 mg of the drug, a 10% solution of calcium gluconate or calcium chloride is administered intravenously.

With an intravenous infusion of the drug, a burning sensation may appear at the injection site. With intracoronary administration of the drug in the first minutes, pressure may drop and the heart rate may increase.

To improve the tolerability of the drug and eliminate its side effects, it is necessary to take Nifedipine in combination with beta-blockers. Edema that occurs against the background of taking the medication quickly disappears after its withdrawal.

With an overdose, headaches appear, blood pressure drops sharply, the face swells, bradycardia occurs, and the pulse in the peripheral arteries disappears.

In severe cases, collapse develops, the patient loses consciousness, the functions of the sinus node are significantly inhibited. If these symptoms are detected, the patient is washed with a stomach and activated charcoal is prescribed.

Analogues

The appearance on the pharmaceutical market of analogues of Nifedipine is associated with its popularity.

Medicine analogues:

  • Adalat;
  • Cordylin;
  • Calciguard retard;
  • Kordafen.

Most of the analogues are not inferior to Nifedepine in terms of effectiveness. The doctor will determine which drug the patient needs: short-acting or extended-acting.

A fast-acting drug is not prescribed for the long-term treatment of arterial hypertension and heart disease, it will be very useful in a hypertensive crisis.

Before choosing a medicine, you should carefully study the instructions, consult a doctor about possible side effects.

Related videos

The video will tell you what Nifedipine tablets are for, at what pressure to take and when they are contraindicated:

Nifedipine is a drug whose main therapeutic effect is aimed at the treatment of hypertension. When it is taken, the coronary and peripheral arteries expand, the resistance of peripheral vessels decreases, and calcium entry into the smooth muscle cells of the vessels slows down. Nifedipine also found application in the treatment of CHF, ischemia, angina pectoris and bradycardia.

The drug does not affect myocardial conduction and heart rate. Side effects include the appearance of a rash on the skin, tachycardia, impaired kidney function. Rapid-acting tablets are prescribed to relieve a hypertensive crisis, and prolonged Nifedipine is used for long-term therapy. You can get more information about Nifedipine pressure pills in the RLS - Register of Medicines of Russia.

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