Nifedipine: immediate reduction in blood pressure. Nifedipine tablets are a potent remedy for normalizing systolic blood pressure

Compound:

active substance: nifedipine; 1 tablet contains nifedipine 10 mg or 20 mg;
Excipients: lactose monohydrate, potato starch, microcrystalline cellulose, povidone, sodium lauryl sulfate, magnesium stearate, hypromelose (hydroxypropyl methylcellulose), polysorbate 80, titanium dioxide (E 171), polyethylene glycol 6000, talc, quinoline yellow (E 104).

Dosage form

Film-coated tablets.

Pharmacotherapeutic group

Selective calcium antagonists with a predominant effect on blood vessels. Dihydropyridine derivatives. ATS code C08C A05.

Clinical characteristics

Indications

Arterial hypertension; coronary heart disease: chronic stable angina, vasospastic angina (Prinzmetal's angina).

Contraindications

• Hypersensitivity to the active substance or to any of the components of the drug;

• hypersensitivity to other dihydropyridines;

• cardiogenic shock;

• severe aortic stenosis;

• porphyria;

• condition during myocardial infarction or for a month after it;

• secondary prevention of myocardial infarction;

• combination with rifampicin (due to the inability to achieve effective plasma levels of nifedipine due to enzyme induction);

• unstable angina;

• inflammatory bowel disease or Crohn's disease.

Directions for use and doses

The dose of the drug and the duration of the course of treatment are determined by the doctor individually, taking into account the severity of the disease and the patient’s response to treatment.

Depending on the clinical picture, in each individual case the main dose should be administered gradually. In patients with impaired liver function, it may be necessary to carefully monitor its condition, and in severe cases, to reduce the dose.

If higher doses of the drug are needed, they should be increased gradually until maximum dose– 60 mg/day.

At simultaneous use When taking Nifedipine with CYP3A4 inhibitors or CYP3A4 inducers, it may be necessary to adjust the dose of nifedipine or discontinue nifedipine.

Due to the pronounced anti-ischemic and antihypertensive effect of the drug, it should be discontinued gradually, especially when high doses are used.

The tablets should be swallowed with a glass of water a small amount liquids. The drug is used regardless of food intake.

Adverse reactions

Adverse reactions are reported through organ systems.

From the side of the heart vascular system: increased heart rate; tachycardia; at the beginning of therapy in patients with angina pectoris, an increase in the frequency, duration of attacks or an increase in the severity of symptoms is possible; cases of asymptomatic myocardial ischemia, exacerbation of existing myocardial ischemia, cardiac conduction disorders, abdominal pain (angina pectoris).

From the blood and lymphatic system: changes in blood counts, thrombocytopenia, anemia, leukopenia, aplastic anemia; agranulocytosis.

From the nervous system: headache, dizziness, increased fatigue, weakness; paresthesia, increased excitability, sleep disturbance (insomnia, drowsiness, restless sleep), imbalance, depression; trembling, loss of coordination of movements, feeling of danger, dysesthesia, migraine, loss of consciousness.

On the part of the visual organs: temporary blindness at the maximum concentration of nifedipine in the blood serum, temporary retinal ischemia, excessive lacrimation (lacrimation); decreased visual acuity, eye pain.

From the organs of hearing and inner ear: ringing in the ears.

From the respiratory tract, chest and mediastinum: dyspnea; nose bleed; upper respiratory tract infections, cough and nasal congestion; angioedema.

From the outside gastrointestinal tract: constipation; diarrhea, nausea, abdominal pain, dry mouth oral cavity, flatulence; vomiting, gum hypertrophy, belching; black stool, heartburn, taste disturbance, dysphagia, intestinal obstruction, intestinal ulcer, gastroesophageal sphincter insufficiency.

From the kidneys and urinary tract: polyuria, nocturia; hematuria, dysuria.

From the skin and subcutaneous tissues: rash, itching, redness, erythema of the cheeks (redness of the face); hives, excessive sweating, chills, purpura; in cases of long-term use of nifedipine, gum hyperplasia is possible, which completely disappears after discontinuation of the drug; toxicodermal necrolysis, Stevens-Johnson syndrome, exfoliative dermatitis, erythema multiforme, photosensitivity, alopecia.

From the outside immune system: allergic reactions, angioedema; itching, urticaria, rash; anaphylactic/anaphylactoid reactions.

From the musculoskeletal system and connective tissue: back pain, myalgia, joint swelling; gout, arthralgia, arthritis with the presence of positive antinuclear antibodies; muscle cramps.

Metabolism and digestion: hyperglycemia (especially in patients with diabetes), weight gain, bezoar.

From the vascular system: swelling of the feet, ankles or legs, vasodilation; arterial hypotension, symptomatic hypotension, orthostatic hypotension.

From the liver and biliary tract: cholestasis; toxic-allergic hepatitis, jaundice, transient increase in the activity of liver enzymes.

From the outside reproductive system and mammary glands: gynecomastia, the process is reversible, symptoms disappear after stopping nifedipine; erectile disfunction.

General disorders: poor health, fever, nonspecific pain.

Mental disorders: depression, paranoid syndrome, anxiety, decreased libido.

Overdose

Symptoms: headache, facial flushing, prolonged systemic hypotension, absence of pulse in the peripheral arteries. 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, impaired consciousness up to coma, are observed.

Treatment. Measures to provide emergency care primarily should 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 would be 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, which threatens life, 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 by a high degree of binding to plasma proteins and a relatively small volume of distribution, hemodialysis is not effective, but plasmapheresis is recommended.

Use during pregnancy and lactation

Nifedipine is contraindicated for use during pregnancy before the 20th week.

The use of nifedipine during pregnancy after the 20th week requires a careful individual analysis of the risk of benefit and should only be considered if all other treatment options are impossible or have been ineffective.

It is necessary to carefully monitor blood pressure when prescribing nifedipine with magnesium sulfate intravenously, since there is a possibility of a sharp decrease in blood pressure, which can be dangerous for the woman and the fetus.

Nifedipine passes into breast milk. Since there is no data on the effects of nifedipine on infants, breastfeeding should be discontinued before using nifedipine.

Children

The drug is not used for children (under 18 years of age).

Special Security Measures

Prescribe the drug with caution in case of very low blood pressure (severe arterial hypotension with systolic blood pressure values ​​below
90 mmHg Art.), as well as severe weakness cardiac activity (decompensated heart failure).

With severe arterial hypotension (systolic pressure below 90 mm Hg), severe cerebrovascular accidents, severe heart failure, severe aortic stenosis, diabetes mellitus, liver and kidney dysfunction, Nifedipine can only be used under conditions of constant clinical observation, avoiding prescribing high doses of the drug.

In elderly patients (over 60 years of age), the drug is dosed with great caution.

Features of application

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

When treating 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 leads to an increase in the concentration of the latter in the blood plasma and increased hypotensive effect drug. The use of nifedipine may lead to falsely elevated results when spectrophotometrically determining the concentration of vanillyl-mandelic acid in urine (however, this effect is not observed when using the high-performance liquid chromatography method).

Caution must be exercised when using the drug in patients with existing severe narrowing of the gastrointestinal tract due to possible occurrence obstructive symptoms. Very rarely, bezoars can occur and may require surgery.

In isolated cases, obstructive symptoms have been described in the absence of a history of gastrointestinal disorders.

Do not use in patients with an ileal pouch (ileostomy after proctocolectomy).

The use of the drug may lead to false positive results when X-ray examination using barium contrast agent (for example, filling defects are interpreted as a polyp).

Patients with impaired liver function require careful monitoring, and in severe cases, dose reduction.

Nifedipine is metabolized through the cytochrome P450 3A4 system, therefore drugs that inhibit or induce this enzyme system may alter the first pass or clearance of nifedipine.

Drugs that are weak or moderate inhibitors of the cytochrome P450 3A4 system and can lead to increased plasma concentrations of nifedipine include, for example:

• macrolide antibiotics (eg erythromycin);

• anti-HIV protease inhibitors (eg ritonavir);

• azole antimycotics (eg ketoconazole);

• antidepressants nefazodone and fluoxetine;

• quinupristin/dalfopristin;

• valproic acid;

• cimetidine

When using nifedipine simultaneously with these drugs, it is necessary to monitor blood pressure and, if necessary, consider reducing the dose of nifedipine.

Separate in vitro experiments have found a relationship between the use of calcium antagonists, in particular nifedipine, and reversible biochemical changes in sperm that impair the latter's ability to fertilize. If attempts at in vitro fertilization are unsuccessful, in the absence of other explanations, calcium antagonists, such as nifedipine, can be considered as a possible cause of this phenomenon.

The drug should not be used if there is a possibility of a relationship between previous use of nifedipine and ischemic pain. In patients with angina, attacks may occur more frequently and their duration and intensity may increase, especially at the beginning of treatment.

Medicines containing the active substance nifedipine are not used in patients with acute attack angina pectoris.

The use of nifedipine in patients with diabetes mellitus may require treatment adjustment.

The ability to influence the reaction rate when driving a vehicle or working with other mechanisms

Interaction with other drugs and other types of interactions

With the simultaneous use of antihypertensive drugs, beta-blockers, diuretics, nitroglycerin and extended-release isosorbide, the possibility of a synergistic effect of nifedipine must be taken into account.

Digoxin

Nifedipine may increase plasma concentrations of digoxin. Digoxin plasma concentrations should be monitored and the dose adjusted when initiating treatment with nifedipine, increasing the dose and discontinuing treatment with nifedipine.

Magnesium sulfate

Nifedipine may enhance the toxic effects of magnesium sulfate, leading to neuromuscular blockade. The simultaneous use of nifedipine and magnesium sulfate is dangerous and may threaten the patient's life, therefore the use of these drugs together is not recommended.

Cimetidine

The simultaneous use of nifedipine and cimetidine may lead to an increase in the concentration of nifedipine in the blood plasma and an increase in the hypotensive effect of nifedipine. Cimetidine inhibits the activity of the cytochrome isoenzyme CYP3A4. In patients already taking cimetidine, nifedipine should be used with caution and gradual increase doses.

Quinupristin, dalfopristin may increase plasma levels of nifedipine.

Phenytoin, carbamazepine

The use of nifedipine may lead to an increase in the concentration of carbamazepine and phenytoin in the blood plasma. Patients who are already taking nifedipine and phenytoin or carbamazepine at the same time must be under constant medical supervision. If signs of toxicity or increased plasma concentrations of carbamazepine and phenytoin occur, the dose of these drugs should be reduced.

Nifedipine may cause a decrease in quinidine serum concentrations, while quinidine may sensitize the patient to the effects of nifedipine. If a patient already taking quinidine is started on nifedipine, attention should be paid to the side effects of nifedipine. Serum quinidine levels should be monitored before starting treatment and if treatment with nifedipine is discontinued; the dose of quinidine should also be adjusted.

Theophylline

With the simultaneous use of nifedipine and theophylline, the concentration of the latter in the blood plasma may increase, decrease or remain unchanged. It is recommended to monitor the concentration of theophylline in the blood plasma and, if necessary, adjust its dose.

Rifampicin

The simultaneous use of rifampicin and nifedipine may be accompanied by a decrease in the concentration of nifedipine in the blood plasma and, as a consequence, a decrease in its therapeutic effect. In case of attacks of angina pectoris or high blood pressure while using nifedipine and rifampicin, the dose of nifedipine should be increased.

Diltiazem reduces the dissolution of nifedipine, which may require a dose reduction.

Vincristine

With simultaneous administration of vincristine, a decrease in the excretion of vincristine is observed.

Cephalosporin

With the simultaneous use of nifedipine and cephalosporin, the level of cephalosporin in plasma increases.

Itraconazole, erythromycin, clarithromycin

The simultaneous use of nifedipine and itraconazole (as well as with other azole antifungals, erythromycin and clarithromycin, which slow down the action of the cytochrome isoenzyme CYP3A4) may lead to an increase in the concentration of nifedipine in the blood plasma and an increase in its effect. If side effects of nifedipine occur, it is necessary to reduce its dose (if possible) or discontinue the use of antifungal agents.

Cyclosporine, ritonavir, or saquinavir

The serum concentration of nifedipine and its effect may also be enhanced by concomitant use of nifedipine, cyclosporine, ritonavir or saquinavir (these drugs slow down the action of the cytochrome isoenzyme CYP3A4). If side effects of nifedipine occur, it is necessary to reduce its dose.

Tacrolimus

In liver transplant patients receiving tacrolimus and nifedipine concomitantly, an increase in tacrolimus serum concentrations was observed (tacrolimus is metabolized by cytochrome CYP3A4). The significance and clinical implications of this interaction have not been studied.

Fentanyl

In patients taking nifedipine, fentanyl may cause arterial hypotension. By at least 36 hours before the event elective surgery When using fentanyl anesthesia, it is necessary to discontinue the use of nifedipine.

Anticoagulants like coumarin

In patients taking anticoagulants such as coumarin, an increase in prothrombin time was observed after administration of nifedipine. The significance of this interaction has not been fully explored.

Methacholine

Nifedipine may alter the bronchial response to methacholine. Treatment with nifedipine should be discontinued until a nonspecific bronchoprovocation test with methacholine is performed (if possible).

Experience with the use of the calcium antagonist nimodipine indicates that the following interactions cannot be excluded for nifedipine: carbamazepine, phenobarbital - decrease in plasma levels of nifedipine; with simultaneous administration of macrolides (in particular erythromycin), fluoxetine, nefazodone, valproic acid - an increase in plasma levels of nifedipine.

Anti-HIV protease inhibitors

Clinical studies examining the potential for interaction between nifedipine and certain HIV protease inhibitors (eg ritonavir) have not been conducted. Drugs in this class are known to inhibit the cytochrome P450 3A4 system. In addition, these drugs inhibit the in vitro cytochrome P450 3A4-mediated metabolism of nifedipine. When used simultaneously with nifedipine, a significant increase in its plasma concentration cannot be ruled out due to a decrease in first-pass metabolism and decreased excretion from the body.

Azole antimycotics

Research on the interaction between nifedipine and certain antifungal drugs azole group (eg ketoconazole) has not yet been carried out. Drugs of this class inhibit the cytochrome P450 3A4 system. When administered orally simultaneously with nifedipine, a significant increase in its systemic bioavailability cannot be ruled out due to a decrease in first-pass metabolism.

Antihypertensive drugs

Concomitant use of nifedipine and other antihypertensive drugs listed below may lead to increased antihypertensive effect:

• diuretics;

• β-blockers (can also cause a heart attack in in some cases);

• ACE inhibitors;

• angiotensin receptor antagonists;

• other calcium antagonists;

• α-blockers;

• PDE5 inhibitors;

• α-methyldopa.

Grapefruit juice

Grapefruit juice may increase the serum concentration of nifedipine and increase its hypotensive effect and the incidence of vasodilator side effects.

Other types of interaction

The use of nifedipine may lead to falsely elevated results when spectrophotometrically determining the concentration of vanillyl-mandelic acid in urine (however, this effect is not observed when using the high-performance liquid chromatography method).

Pharmacological properties

Pharmacodynamics. 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 the coronary vessels. At the beginning of treatment with nifedipine, transient reflex tachycardia and an increase in cardiac output that do 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 – about 50%. The maximum concentration in blood plasma is achieved 1-3 hours after administration. Half-life –
2-5 hours. It is excreted mainly in the urine in the form of inactive metabolites. Time of onset of clinical effect: 20 min – with orally, 5 min – with sublingual. The duration of the clinical effect is 4-6 hours.

Pharmaceutical characteristics

Basic physicochemical characteristics: round, film-coated tablets yellow color, the upper and lower surfaces of which are convex. At the fracture, when viewed under a magnifying glass, a core is visible, surrounded by one continuous layer.

Best before date

Storage conditions

Store in original packaging at a temperature not exceeding 25 °C. Keep out of the reach of children.

Name:

Nifedipine

Pharmacological
action:

Selective blocker of "slow" calcium channels, a 1,4-dihydropyridine derivative.
It has a vasodilating, antianginal and antihypertensive effect. Reduces the flow of calcium ions into cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses suppresses the release of calcium ions from intracellular stores.
Reduces the number of functioning channels without affecting the time of their activation, inactivation and recovery.

Uncouples the processes of excitation and contraction in the myocardium, mediated by tropomyosin and troponin, and in vascular smooth muscle, mediated by calmodulin. In therapeutic doses, it normalizes the transmembrane current of calcium ions, which is disturbed in a number of pathological conditions, primarily in arterial hypertension.
Does not affect the tone of the veins. Increases coronary blood flow, improves blood supply to ischemic areas of the myocardium without developing the phenomenon of “stealing”, it activates the functioning of collaterals. By dilating the peripheral arteries, it reduces the overall peripheral vascular resistance, myocardial tone, afterload, myocardial oxygen demand and increases the duration of diastolic relaxation of the left ventricle.
Virtually no effect on the sinoatrial and atrioventricular nodes and does not have antiarrhythmic activity. Increases renal blood flow, causes moderate natriuresis.
The negative chrono-, dromo- and inotropic effects are overlapped by reflex activation of the sympathoadrenal system and an increase in heart rate in response to peripheral vasodilation.
The onset of the effect is 20 minutes, the duration of the effect is 12-24 hours.

Pharmacokinetics

Absorption is high (more than 92-98%). Bioavailability - 40-60%. Eating increases bioavailability. Has a “first pass” effect through the liver. Retard forms provide gradual release active substance into the systemic circulation. TCmax 1.6-4.2 h, Cmax - 47-76 ng/ml. Communication with plasma proteins - 90%.
Penetrates the BBB and placental barrier and is excreted from breast milk.

Completely metabolized in the liver. The metabolism of the drug involves isoenzymes CYP3A4, CYP3A5 and CYP3A7.
T1/2 - 3.8-16.9 hours. In patients with liver failure, total clearance decreases and T1/2 increases. It is excreted in the form of inactive metabolites, mainly by the kidneys (80%) and bile (20%).

There is no cumulative effect. Chronic renal failure, hemodialysis and peritoneal dialysis do not affect pharmacokinetics.
With long-term use (2-3 months), tolerance to the action of the drug develops.
Plasmapheresis may enhance elimination.

Indications for
application:

Chronic stable angina (angina pectoris);
- vasospastic angina (Prinzmetal's angina);
- arterial hypertension (in monotherapy or in combination with other antihypertensive drugs);
- Raynaud's disease and syndrome.

Mode of application:

Inside. The tablets should be swallowed whole, without chewing, during or after meals, with a small amount of water.
The recommended dose of the drug is 20 mg 2 times a day.
If the effect is not sufficiently pronounced, it is possible to increase the dose of the drug to 40 mg 2 times a day.
Maximum daily dose is 80 mg.

If liver function is impaired, the daily dose should not exceed 40 mg.
In elderly patients or patients receiving combination (antianginal or antihypertensive) therapy, lower doses are usually prescribed.
If liver function is impaired, in patients with severe cerebrovascular accidents, the dose should be reduced.
The duration of treatment is determined in each case individually.

Side effects:

The frequency of these side effects is indicated in accordance with the WHO classification: very often - more than 10%; often - more than 1% and less than 10%; infrequently - more than 0.1% and less than 1%; rarely - more than 0.01% and less than 0.1%; very rarely - less than 0.01%, including isolated cases.
From the cardiovascular system: often - peripheral edema (feet, ankles, legs), symptoms of vasodilation (redness of the facial skin, feeling of heat); infrequently - tachycardia, rapid heartbeat, marked decrease in blood pressure, fainting; in some cases - chest pain (angina) up to
development of myocardial infarction, development or worsening of chronic heart failure, arrhythmia.

From the nervous system: very often - headache; often - dizziness, drowsiness; uncommon - asthenia, sleep disturbance (including insomnia), nervousness, increased fatigue, dysesthesia, tremor, mood lability.
From the digestive system: often - nausea; uncommon - gastrointestinal and abdominal pain (pain in the stomach and intestines), diarrhea, constipation, dry oral mucosa, increased appetite; rarely - gum hyperplasia (bleeding, pain, swelling).
With long-term use: infrequently - liver dysfunction (intrahepatic cholestasis, increased activity of "liver" transaminases), rarely - jaundice; in some cases - insufficiency of the cardiac sphincter.

From the respiratory system: infrequently - shortness of breath, rarely - pulmonary edema (difficulty breathing, cough, wheezing).
From the musculoskeletal system: rarely - arthralgia, joint swelling, myalgia, muscle cramps.
From the hematopoietic organs: rarely - anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura; very rarely - asymptomatic agranulocytosis.
From the urinary system: infrequently - increased daily diuresis, deterioration of renal function (in patients with renal failure).

Allergic reactions: often - erythema; rarely - itching, urticaria, exanthema, photosensitivity, autoimmune hepatitis; infrequently - angioedema; in some cases - toxic epidermal necrolysis.
Others: rarely - visual impairment (including transient loss of vision against the background of the maximum concentration of nifedipine in the blood plasma), eye pain, hyperglycemia, gynecomastia (in elderly patients; completely disappearing after discontinuation of the drug), galactorrhea, erectile dysfunction, enlargement body weight, chills, nosebleeds, nasal congestion.

Contraindications:

Arterial hypotension (systolic blood pressure below 90 mm Hg);
- cardiogenic shock;
- collapse;
- severe aortic or subaortic stenosis;
- acute heart failure;
- chronic heart failure in the stage of decompensation;
- unstable angina;
- acute period of myocardial infarction (during the first 4 weeks);
- hypertrophic obstructive cardiomyopathy;
- sick sinus syndrome;
- AV blockade II-III degree;
- pregnancy (up to 20 weeks);
- lactation period;
- age under 18 years (the effectiveness and safety of use have not been studied);
- hypersensitivity to nifedipine or other components of the drug.
The drug contains lactose and is therefore contraindicated for use in patients with rare hereditary diseases of lactose intolerance, lactase deficiency, and glucose-galactose malabsorption.

Carefully: mitral stenosis, severe bradycardia or tachycardia, chronic heart failure, severe cerebrovascular accidents, myocardial infarction with left ventricular failure, gastrointestinal obstruction (for sustained-release forms), liver failure, chronic renal failure (especially patients on hemodialysis - high risk excessive and unpredictable decrease in blood pressure), simultaneous administration beta-blockers and cardiac glycosides, pregnancy (after 20 weeks), old age.

During the treatment period you must abstain from drinking alcohol.
Despite the absence of withdrawal syndrome with slow calcium channel blockers, a gradual dose reduction is recommended before stopping treatment.
The simultaneous administration of beta-blockers must be carried out under conditions of careful medical supervision, since this may cause an excessive decrease in blood pressure, and in some cases, aggravation of heart failure. During treatment positive results are possible when performing the direct Coombs reaction and laboratory tests for antinuclear antibodies.

It is important regularity of treatment regardless of health, since the patient may not feel symptoms of hypertension.
The diagnostic criteria for prescribing the drug for vasospastic angina are: classic, clinical picture, accompanied by characteristic changes electrocardiograms (ST segment elevation); occurrence of ergometrine-induced angina or spasm coronary arteries; identification of coronary spasm during angiography or identification of an angiospastic component, without confirmation (for example, with a different voltage threshold or with unstable angina, when electrocardiogram data indicate transient angiospasm).

For patients with severe hypertrophic cardiomyopathy there is a risk of increasing the frequency, severity and duration of angina attacks after taking nifedipine; V in this case discontinuation of the drug is necessary.
In patients on hemodialysis with high blood pressure, irreversible renal failure, and a decrease in circulating blood volume, the drug should be used with caution, since a sharp drop in blood pressure may occur.

For patients with impaired liver function Close monitoring is established and, if necessary, the dose of the drug is reduced and/or other dosage forms of nifedipine are used.
It should be borne in mind that angina pectoris may occur at the beginning of treatment, especially after recent abrupt withdrawal of beta-blockers (the latter are recommended to be withdrawn gradually).
If during therapy the patient requires surgical intervention under general anesthesia, it is necessary to inform the surgeon-anesthesiologist about the nature of the therapy being performed.
When spectrophotometrically assessed Nifedipine may lead to incorrect detection of increased levels of vanillyl-mandelic acid in the urine; it does not affect studies using high-performance liquid chromatography.

During in vitro fertilization In some cases, blockers of "slow" calcium channels caused changes in the head of the sperm, which could lead to impaired sperm function. In cases in which repeated in vitro fertilization did not occur for an unclear reason, calcium channel blockers, including nifedipine, were considered possible reason failures.
Impact on the ability to drive vehicles and operate machinery
During treatment, care must be taken when managing vehicles and engaging in other potentially hazardous activities that require increased concentration attention and speed of psychomotor reactions.

Interaction
other medicinal
by other means:

The severity of the decrease in blood pressure increases with simultaneous use of nifedipine with other antihypertensive drugs, nitrates, cimetidine, ranitidine (to a lesser extent), inhalational anesthetics,
diuretics and tricyclic antidepressants.
Under the influence of nifedipine significantly the concentration of quinidine in the blood plasma decreases. Increases the concentration of digoxin in the blood plasma, and therefore should be monitored clinical effect and the level of digoxin in blood plasma.
Rifampicin is a powerful inducer of the CYP3A4 isoenzyme. When used together with rifampicin, the bioavailability of nifedipine is significantly reduced and, accordingly, its effectiveness is reduced.

Use of nifedipine together Contraindicated with rifampicin. In combination with citrates, tachycardia and the antihypertensive effect of nifedipine are enhanced.
Calcium supplements may reduce the effect of calcium channel blockers V. When used together with nifedipine, the anticoagulant activity of coumarin derivatives increases.
It can displace drugs characterized by a high degree of binding from their binding to proteins (incl. indirect anticoagulants- coumarin and indandione derivatives, anticonvulsants, quinine, salicylates, sulfinpyrazone), as a result of which their concentrations in the blood plasma may increase.
Suppresses the metabolism of prazosin and other alpha-blockers c, as a result of which the antihypertensive effect may be enhanced.

Procainamide, quinidine and other drugs that cause QT prolongation enhance the negative inotropic effect and may increase the risk of significant QT prolongation.
Concomitant use with magnesium sulfate in pregnant women may cause blockade of neuromuscular synapses.

Inhibitors of the cytochrome P450 3A system such as macrolides (eg, erythromycin), fluoxetine, nefazodone, protease inhibitors (eg, amprenavir, indinavir, nelfinavir, ritonavir or saquinavir), antifungals (ketoconazole, itraconazole or fluconazole) lead to increased plasma concentrations of nifedipine.
Taking into account the experience with the use of the “slow” calcium channel blocker nimodipine, the following interactions with nifedipine cannot be excluded: carbamazepine, phenobarbital - a decrease in the concentration of nifedipine in the blood plasma; quinupristin, dalfopristin, valproic acid - increase the concentration of nifedipine in the blood plasma.

Caution should be exercised when nifedipine is administered concomitantly with disopyramide and flecainide. due to possible strengthening inotropic effect.
Nifedipine inhibits the elimination of vincristine from the body and may cause increased side effects; if necessary, reduce the dose of vincristine.
Grapefruit juice suppresses the metabolism of nifedipine in the body, and therefore their simultaneous use is contraindicated.

Pregnancy:

Controlled No studies have been conducted on the use of Nifedipine in pregnant women..
Animal tests have shown the presence of embryotoxicity, placentotoxicity, fetotoxicity and teratogenicity when taking nifedipine during and after the period of organogenesis.
Based on the available clinical data, it is not possible to judge the specific perinatal risk.
At the same time, there are evidence of an increased likelihood of perinatal asphyxia, caesarean section, premature birth and delays intrauterine development fetus It is unclear whether these cases are a consequence of the underlying disease (arterial hypertension), the treatment being administered, or a specific effect of the drug Nifedipine.
The available information is insufficient to exclude the possibility of side effects that pose a danger to the fetus and newborn.

That's why the use of Nifedipine after the 20th week of pregnancy requires careful individual assessment balance of risk and benefit for the patient, fetus and/or newborn and can only be considered in cases where other methods of therapy are contraindicated or ineffective.

Should Carry out careful monitoring of blood pressure in pregnant women when using the drug Nifedipine simultaneously with intravenous administration of magnesium sulfate due to the possibility of an excessive decrease in blood pressure, which poses a danger to both the mother and the fetus and/or newborn.
Nifedipine is contraindicated during lactation as it is excreted in breast milk. If Nifedipine therapy is absolutely necessary, it is recommended to stop breastfeeding.

Overdose:

Symptoms: headache, facial skin flushing, prolonged pronounced decrease in blood pressure, suppression of sinus node function, bradycardia, bradyarrhythmia. In severe poisoning - loss of consciousness, coma, metabolic acidosis, hypoxia, cardiogenic shock with pulmonary edema.
Treatment: in case of severe poisoning (collapse, depression of the sinus node), gastric lavage is performed and activated charcoal is prescribed.
Calcium is the antidote: slow intravenous administration of 10% calcium chloride or calcium gluconate at a dose of 0.2 ml/kg (but not more than 10 ml) over 5 minutes is indicated; if ineffective, repeated administration is possible under the control of the content of calcium ions in the blood serum; if symptoms resume, it is possible switch to a constant infusion at a rate of 0.2 ml/kg/h, but not more than 10 ml/h.

With a pronounced decrease in blood pressure - intravenous administration of dopamine or dobutamine.
For conduction disorders - atropine, isoprenaline or an artificial pacemaker.
With the development of heart failure - intravenous administration of strophanthin.
Catecholamines should be used only when there is a threat to life (due to their reduced effectiveness, a high dosage is required, which increases the risk of developing arrhythmia). It is recommended to monitor the concentration of glucose in the blood (insulin release may decrease) and electrolytes (potassium ions, calcium ions).
Hemodialysis is ineffective.

Release form:

Pills, coated, 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 bottles 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 syringes of 2 ml in a package of 5 pieces.

Storage conditions:

At a temperature not higher than 25°C. Keep out of the reach of children.
Shelf life - 3 years.

1 tablet of Nifedipine extended release contains:
- active substance: nifedipine - 20 mg;
- Excipients: microcrystalline cellulose - 51 mg, corn starch - 58.25 mg, lactose monohydrate - 36.2 mg, polysorbate 80 - 2 mg, magnesium stearate - 150 mcg, hypromellose - 2.4 mg.

Nifedipine has been used since the 1970s to treat hypertension and cardiovascular diseases. These tablets belong to the group. To this day, nifedipine remains one of the most “popular” drugs in cardiology, that is, doctors prescribe it very often. Nifedipine became an even more popular drug after tablets of this drug were introduced in the 2000s, which acted for 24 hours. They can be taken once a day, and not 2-4 times a day, as before.

There are nifedipine tablets that act quickly, as well as “extended” dosage forms. Long-acting nifedipine begins to act later, but it reduces blood pressure smoothly and for a long time, i.e. for 12-24 hours.

Since 1998, articles began to appear in medical journals that fast-acting nifedipine increases overall mortality in patients, as well as the incidence of heart attacks and strokes. This means that for long-term treatment hypertension and coronary disease only nifedipine extended-release tablets are suitable for heart disease. The most popular of them are OSMO-Adalat and Corinfar UNO, which we will discuss in detail below in the article. Fast-acting nifedipine is only suitable for. Unfortunately, few patients and doctors know about this. Hundreds of thousands of people continue to be treated with it regularly. Patients - if you want to live longer, then use nifedipine extended-release tablets, not “fast”.

Nifedipine - instructions

This article consists of instructions for nifedipine, which is supplemented by information from domestic and foreign medical journals. Official instructions on the use of nifedipine tablets for blood pressure and for the treatment of heart problems is written in detail, but not very clear. We have tried to present the information conveniently so that you can quickly find answers to the questions that interest you.

The instructions for the drug nifedipine, as well as any other materials on the Internet or in print, are intended for specialists. Patients - do not use this information for self-medication. Side effects of self-medication with nifedipine can cause harm to your health, including death. Take this drug only as directed by your doctor. The instructions for nifedipine contain an extensive list of this medicine. Doctors know in practice that these side effects are observed quite often.

Separately, it is worth noting that it is almost impossible to independently select the dosage of nifedipine. It will be either too low or too high. In both cases, there will be no benefit from taking pills, only harm. Therefore, treatment with this drug should only be carried out under the supervision of an experienced, qualified doctor.

Indications for use

The main indications for the use of nifedipine are hypertension (arterial hypertension), as well as angina pectoris in patients who suffer from chronic coronary heart disease. Nifedipine belongs to the group of calcium antagonists, dihydropyridine derivatives. In accordance with all international recommendations, drugs in this group are included in the list of drugs for hypertension of the first choice, i.e., the main ones.

Read about the treatment of diseases associated with hypertension:

Additional indications for prescribing nifedipine:

• elderly age of the patient;
• atherosclerosis of the peripheral arteries (in the legs) and/or the carotid artery;
• pregnancy.

Contraindications

Contraindications to the use of nifedipine are:

• hypotension (excessively low blood pressure);
• cardiogenic shock;
• hypersensitivity to the drug.

It is not recommended to prescribe this medicine for unstable course of coronary heart disease, after a myocardial infarction.

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Side effects

Nifedipine does not have a negative effect on cholesterol levels and uric acid in blood. The most common side effects of this drug are:

• swelling of the legs;
• headache;
• skin redness;
• dizziness
• palpitations (tachycardia).

Back in 1982, the results of a large-scale study of the side effects of nifedipine were published, in which more than 3 thousand patients took part. Of these patients, 2147 had severe angina that was refractory to treatment with beta blockers and nitrates at usual doses. Therefore, the range of nifedipine dosages that were used turned out to be wide - from 10 to 240 mg per day. The patients were prescribed nifedipine tablets, which act quickly but do not last long, since long-acting forms of this drug had not yet been invented.

It turned out that nifedipine had side effects in almost 40% of patients:

• dizziness - 12.1%;
• swelling in the legs - 7.7%;
• feeling of heat - 7.4%;
• complaints from the gastrointestinal tract - 7.5%;
• increased angina pectoris - 1.2%.

To improve tolerability and eliminate undesirable effects, it is advisable to combine nifedipine with or. Read the note “” for more details. If swelling occurs as a result of taking nifedipine, they most often quickly disappear when treatment is stopped.

Nifedipine and other calcium antagonists

Nifedipine belongs to the group of drugs derived from dihydropyridine. Two other subgroups of calcium antagonists are benzothiazepines () and phenylalkylamines (). Medicines from the dihydropyridine group have the following advantages:

• greater ability to relax blood vessels;
• there is no effect on the function of the sinus node of the heart and atrioventricular conduction;
• decreased ability to inhibit the contractility of the left ventricle of the heart.

These differences largely determine the features practical application dihydropyridine calcium antagonists in general and nifedipine in particular.

What are the dosage forms of this drug?

The effectiveness and safety of nifedipine largely depends on the dosage form in which the patient takes it. Rapid-acting nifedipine tablets and capsules have been used since the 1970s. In the late 1990s, long-acting dosage forms appeared. Nifedipine, which sharply lowers blood pressure and is quickly eliminated from the body, is less effective and less well tolerated than one that acts gradually over 12-24 hours.

The effect of nifedipine depends on how much its concentration in the blood fluctuates, how quickly it rises and falls. Regular nifedipine tablets are distinguished by the fact that they sharply reduce blood pressure. In response to this, a reflex release of adrenaline and other “stimulating” hormones occurs. These hormones can cause tachycardia (palpitations), headache, feeling hot, and redness of the skin. Since nifedipine short acting is quickly eliminated from the body, a “ricochet” phenomenon may occur. This means that sometimes your blood pressure rises even higher than it was before taking the pill.

What other disadvantages do “fast” dosage forms of nifedipine have:

• they need to be taken several times during the day, which is inconvenient for patients, and therefore patients often refuse treatment;
• the effect of the drugs is not stable throughout the day and changes due to meals;
• These pills act very differently on different people, depending on genetic characteristics, age and the preservation of kidney function;
• Under the influence of these drugs, blood pressure fluctuates, like on a roller coaster, which is why atherosclerosis quickly develops in the blood vessels.

Currently, “fast” nifedipine is recommended for use only for the relief of hypertensive crises. It is not intended for long-term treatment because it does not improve and even worsens long term forecast for patients. For constant admission For hypertension and cardiovascular diseases, nifedipine in a long-acting dosage form is suitable.

Extended form and its advantages

Long-acting dosage forms of nifedipine ensure slow release of the active substance into the blood. Peak levels of nifedipine in the blood are much lower than with the quick-release tablet. Blood pressure decreases for a period of 12-24 hours and much more gradually. Therefore, there is no reflex release of “stimulating” hormones into the blood. Accordingly, tachycardia (palpitations) and other side effects of nifedipine are observed several times less frequently and are less pronounced. Long-acting forms of nifedipine are not effective for relief hypertensive crisis. But they are less likely to have negative side effects and, most importantly, improve the long-term prognosis for patients.

Characteristics of “extended” dosage forms of nifedipine

The original drug nifedipine was developed by the German company Bayer AG and was called Adalat. It is no longer available in the form of quick-release capsules. The following are currently represented on the pharmaceutical market:

• Adalat-SL - valid for 12-16 hours, prescribed for use 2 times a day;
• OSMO-Adalat - maintains a stable concentration of nifedipine in the blood for more than 24 hours, prescribed once a day.

OSMO-Adalat is a dosage form of nifedipine with significantly prolonged action. It is called GITS or GITS - gastrointerstitial (gastrointestinal) therapeutic system. It has the most beneficial effect due to its ability to maintain a uniform concentration of nifedipine in the blood.

Long-acting nifedipine tablets last 12-24 hours and are prescribed 1-2 times a day. Their pharmacokinetics are independent of food intake. Osmo-Adalat and Corinfar Uno are the most popular nifedipine preparations, because with a single dose they provide a more or less stable concentration of the drug in the blood for a whole day. Thanks to this, the effectiveness of treatment increases, damage to target organs (heart, kidneys, eyes and others) decreases and the frequency of complications of hypertension decreases. In addition, patients are more willing to be treated with blood pressure pills, which can only be taken once a day.

Attention! Nifedipine extended-release tablets require special handling. They cannot be crushed, dissolved or absorbed in the mouth. These medications must be swallowed immediately with water. Do not split the tablet to reduce the dosage unless the instructions say that you can do this.

Analogues and synonyms of nifedipine

Nifedipine (adalat, cordafen, cordaflex, corinfar, cordipine, nicardia, nifebene, procardia, farmadipine, phenigidine, etc.) is available in tablets and capsules of 10 and 20 mg, farmadipine - in drops. Prolonged forms - adalat-SL, corinfar Uno, corinfar-retard, cordipin-retard, nifebene-retard, nifedipine SS and others - are available in slow-release tablets of 20, 30, 40, 60 and 90 mg. As you can see, there are almost two dozen synonyms of nifedipine. Many pharmaceutical companies produce fast-acting and extended-release analogues of nifedipine because this drug is in great demand.

Short-acting nifedipine is no longer recommended for the long-term treatment of hypertension and cardiovascular disease. It is recommended to be taken only for emergency care during hypertensive crises. However, in the CIS countries it still accounts for more than half of sales. The cheap, fast-acting drug is most often available in tablets called nifedipine. For example, nifedipine-Darnitsa.

Nifedipine with a gastrointestinal therapeutic system (GITS or GITS) is available under the name OSMO-Adalat in capsules with a special membrane, through an opening in which the drug is gradually released over 24 hours. In this regard, it can be prescribed once a day, like Corinfar Uno .

Nifedipine for blood pressure

3 subgroups of drugs from the class of calcium antagonists are used as blood pressure tablets:

• phenylalkyalamines();
• benzothiazepines ();
• dihydropyridines, which include nifedipine.

Dihydropyridine calcium antagonists (isradipine, and the most popular among them, nifedipine) are most often prescribed for blood pressure. Because they are characterized by a minimal effect on the conduction function of the heart and the function of the sinus node. These medications also relax blood vessels well.

In 1995, articles began to appear in American medical journals stating that nifedipine in the treatment of hypertension does not improve, but even worsens, the prognosis for patients, i.e., it increases the likelihood of a heart attack or stroke. Later studies showed that this only applies to fast-acting nifedipine tablets. A - are useful for lowering blood pressure, improve prognosis and are well tolerated by patients. Nifedipine retard, which lasts 12-16 hours, has confirmed its effectiveness, and even better is nifedipine in the form of GITS (GITS), one tablet of which lowers blood pressure for as long as 24 hours, and it is enough to take it once a day.

In 2000, the results of a large study, INSIGHT, were published, which compared the effectiveness of 24-hour nifedipine with diuretics for the treatment of hypertension. More than 6,300 patients took part in this study. Half of them took nifedipine, and the other half took . It turned out that nifedipine in the form of GITS (GITS) and diuretics approximately equally reduce blood pressure, overall and cardiovascular mortality. At the same time, among patients treated with nifedipine, new cases of diabetes mellitus, gout and atherosclerosis of the blood vessels of the legs were less common.

Nifedipine and its “relatives” (dihydropyridine calcium antagonists) play a particularly important role in the treatment of hypertension in patients with diabetes and metabolic syndrome (prediabetes). Because these medications do not impair metabolism, i.e. they do not affect blood sugar, cholesterol and triglyceride levels. Nifedipine 24-hour GITS is the drug of choice for blood pressure control in patients with diabetes, metabolic syndrome and high cardiovascular risk.

Nifedipine 24-hour action in the treatment of hypertension not only lowers blood pressure, but also significantly protects internal organs. The organoprotective effect of nifedipine is manifested in the following:

• decreased remodeling of the left ventricle of the heart;
• optimization of tissue blood supply;
• beneficial effect on kidney function;
• improvement functional state retina of the eyes.

In the treatment of hypertension, nifedipine combines well with almost all groups of blood pressure medications that are currently used:

Isolated systolic hypertension in the elderly

Among older people, at least 40-50% suffer from high blood pressure. Isolated systolic hypertension is especially common in older patients. High blood pressure shortens life expectancy, often causes heart attack, stroke or the development of chronic renal failure. An effective drug for the treatment of hypertension in elderly patients should not only lower blood pressure, but also protect target organs from damage. Nifedipine (only in extended-release dosage form!) is one of suitable drugs in this case.

In 2008, specialists from medical institute Penza State University published an article based on a study of the effectiveness of treating hypertension with long-acting nifedipine in 48 elderly patients. Of these 48 patients:

• 20 people suffered from isolated systolic hypertension;
• 28 had increased both “upper” and “lower” blood pressure.

The results of blood pressure reduction were assessed by measuring it with a tonometer at a doctor's appointment. In addition, each patient underwent daily monitoring blood pressure at the beginning and after 24 weeks of treatment. The study authors also found out whether “extended” nifedipine has the properties to protect target organs from damage. To do this, participants underwent echocardiography (of the heart) and were tested for microalbuminuria - protein excretion in the urine - an important indicator for assessing kidney function.

Dynamics of decrease in “upper” and “lower” blood pressure in elderly patients during treatment with nifedipine 24-hour tablets

Note to the table. All values ​​were obtained from the results of daily blood pressure monitoring. The authors of the study found that as a result of the “white coat effect” at a doctor’s appointment, systolic pressure is increased by an average of 13-15 mm Hg. Art.

Study participants noted that their blood pressure began to steadily decrease already in the 2nd week of treatment, and this effect intensified in subsequent weeks and months. The table shows that in patients with isolated systolic hypertension, nifedipine lowers the “upper” pressure significantly, and the “lower” pressure much less. This suggests that nifedipine is the drug of choice for the treatment of isolated systolic hypertension in the elderly because there is no excessive decrease in diastolic pressure.

Normally healthy person At night during sleep, blood pressure decreases. The daily dynamics of blood pressure fluctuations can be tracked based on the results of 24-hour monitoring using a special device. If it turns out that a patient's blood pressure does not decrease at night, and even more so if it increases, then this is called an “abnormal blood pressure profile” and means that the risk of heart attack or stroke is significantly increased. In the study whose results we discuss, 80% of patients with isolated systolic hypertension initially had an abnormal blood pressure profile. In the group of patients with systolic-diastolic hypertension, this was 65%. It turned out that treatment with 24-hour nifedipine improved the 24-hour blood pressure profile in many patients.

Microalbuminuria - protein excretion in the urine - at the beginning of the study was determined in 11 of 26 patients with systolic-diastolic hypertension and in all 20 (100%) patients with isolated systolic hypertension. Taking nifedipine extended-release tablets for 24 weeks led to the fact that in the first group the number of patients with microalbuminuria decreased from 11 to 9, and in the second - from 20 to 8. Thus, it was confirmed that nifedipine protects the kidneys.

Left ventricular hypertrophy is a way for the heart to adapt to increased load, which arises due to arterial hypertension. If studies show that a patient has a change in the shape (remodeling) of the heart, then this significantly worsens his prognosis. Because the likelihood of a heart attack increases. A study on the treatment of hypertension in elderly patients tested how nifedipine treatment affected the degree of left ventricular hypertrophy of the heart. Based on the results of echocardiography, it was found that taking nifedipine for 24 hours reduced the thickness of the heart walls, improved systolic and diastolic function of the left ventricle and reduced total peripheral vascular resistance. Thus, hypertrophy of the left ventricle of the heart regressed in many patients.

Since nifedipine had a positive effect on heart and kidney function, it can be argued that it not only lowers blood pressure, but also protects target organs from damage in elderly patients. In the group of patients with isolated systolic hypertension, all 20 people (100%) completed the study. In the group of patients who had increased both “upper” and “lower” blood pressure, 2 people dropped out due to side effects of nifedipine. They experienced a rush of blood to the skin of the face and swelling.

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Nifedipine is widely used to treat coronary heart disease. It clearly reduces pain in the heart area, reduces the frequency of angina attacks in patients and reduces the need for nitroglycerin. All this was proven in clinical studies back in the early 1980s. When taking nifedipine in an extended-release dosage form, exercise tolerance increases. This drug is as effective as beta blockers and nitrates for heart problems.

In accordance with international recommendations, they are the main group of drugs prescribed for coronary heart disease. In a doctor’s practice, the question often arises: which drug is best to add to them? Which additional medicine will provide a more pronounced antianginal effect - nitrates or nifedipine?

In recommendations American Association cardiologists in the treatment of stable angina pectoris found the effectiveness of nitrates and dihydropyridine calcium antagonists to be equal. However, it is advised to give preference to extended-release nifedipine because it remains effective for 24 hours. Another advantage of dihydropyridine calcium antagonists compared to nitrates: patients are much less likely to develop addiction to them

IN practical work dihydropyridine calcium antagonists, including nifedipine, become the drugs of choice if beta blockers are contraindicated. Such situations include:

• sick sinus syndrome;
• atrioventricular block;
• bronchial asthma.

Also, dihydropyridines can sometimes be prescribed in cases where the use of verapamil and diltiazem, non-dihydropyridine calcium antagonists, is contraindicated. This occurs if the patient has sick sinus syndrome or severe atrioventricular block.

In 2004, the results of the large-scale ACTION study were published, which involved 7665 patients with coronary heart disease or myocardial infarction. The purpose of this study was to determine the effect of adding 24-hour nifedipine in the form of GITS (see “”) to a conventional treatment regimen. Patients were treated before the start of the study and continued to be treated with statins and aspirin. They were divided into two groups. Those included in the first group were added to treatment with nifedipine, and patients in the second group were given a placebo for control.

Doctors observed all study participants for 5 years. It turned out that nifedipine in the form of GITS did not improve or worsen overall and cardiovascular mortality rates, as well as the incidence of new cases of myocardial infarction. But it reduced the number of new cases of heart failure by 29%, strokes by 22%, and the need for coronary artery bypass surgery by 14%. Among patients in whom coronary heart disease was combined with hypertension, the results were even better, approximately 1.5 times. There were no more side effects from taking it than from placebo. The authors of the study explained the effectiveness of nifedipine by the fact that it additionally lowered blood pressure in patients and also inhibited the development of atherosclerosis.

Kidney protection for hypertension and diabetes

If a patient has kidney damage due to diabetes or other reasons, then the target blood pressure level for him will be 130/80 mmHg. Art., and not 140/90, as for people with healthy kidneys. If proteinuria (protein excretion in the urine) is more than 1 g per day, then the target blood pressure level is even lower - 125/75 mm Hg. Art. To protect the kidneys during hypertension, you need to ensure strict control of blood pressure, stop smoking and try to normalize blood cholesterol levels.

It's obvious that regular intake Blood pressure pills can significantly slow down the development of kidney failure. With intensive treatment, the likelihood increases that the patient’s own kidneys will last the rest of his life, and he will not have to experience the “delights” of dialysis or a kidney transplant. Studies have shown that all major classes of hypertension medications reduce kidney damage. But which drugs do this better than others?

Calcium antagonists relax and dilate the blood vessels that feed the kidneys. Under the influence of nifedipine, renal blood flow, glomerular filtration levels and filtration fraction increase. Calcium antagonists slow down the development of nephrosclerosis. Long-acting nifedipine (not short-acting!) reduces microalbuminuria. This medicine preserves kidney function in patients with diabetes mellitus and diabetic nephropathy. Nifedipine protects the kidneys both directly and by lowering blood pressure.

Nifedipine and other calcium antagonists are especially often used to inhibit the development of renal failure if the patient has hypertension and diabetes. Because in such cases it is contraindicated to prescribe diuretics or beta blockers. But which drugs protect the kidneys better - calcium antagonists, or? This issue has not yet been fully clarified and requires additional research.

In 2000, the results of a large study were published that showed that nifedipine prevents kidney failure more effectively than diuretics. We also mention that this medicine to some extent increases the sensitivity of tissues to insulin. Thus, the course of hypertension in diabetes mellitus improves.

Slowing the progression of atherosclerosis

Back in the 1990s, studies using short-acting nifedipine showed that the drug had a beneficial effect on metabolism and to some extent slowed the development of atherosclerosis. An indicator that characterizes the risk of cardiovascular complications is the thickness of the intima-media complex (IMT) carotid arteries. It is measured using ultrasound. The greater this thickness, the higher the patient's risk of heart attack or stroke. Studies have reliably shown that taking nifedipine slows down the increase in IMT. Moreover, this effect of the drug does not depend on its action in lowering blood pressure.

Another important risk factor is calcium deposits in atherosclerotic plaques on the walls of the arteries. Calcium makes them hard and similar to limescale on water pipes. The process of calcium accumulation in atherosclerotic plaques is called calcification. It turned out that nifedipine, although slightly, slows down the calcification of the coronary (feeding the heart) arteries.

It is currently believed that nifedipine slows the development of atherosclerosis better than other calcium antagonists. At the same time, one should not hope to completely inhibit atherosclerosis with nifedipine alone. We recommend getting tested for risk factors for atherosclerosis, which are listed in the article “”. It also indicates what measures effectively help protect blood vessels from atherosclerosis.

Nifedipine during pregnancy

With long-term therapy with nifedipine, started in early dates pregnancy, cases of intrauterine fetal death and anomalies of skeletal development in newborns have been described. It is believed that nifedipine and other dihydropyridine calcium antagonists (with the exception of) are unsafe in the first trimester of pregnancy, therefore they are not recommended for use in women of childbearing age. At the same time, some studies have shown that nifedipine can effectively control arterial hypertension in women in late dates pregnancy (not earlier than 18-21 weeks), without adversely affecting the development of the fetus.

Nifedipine, taken sublingually and orally, has been particularly useful in the treatment of hypertensive crises in pregnant women. There are isolated reports in the literature about the safety of using dihydropyridine calcium antagonists in late pregnancy. However, there are few of them, and therefore it is still in pharmacological reference books Nifedipine is not recommended for use during pregnancy. Doctors prescribe it only in severe cases, when they believe that the benefits of taking the pills will be greater than the risks.

Do not take nifedipine without permission during pregnancy! Consult a doctor!

In 2008, specialists from the Medical Institute of the State University of the Ukrainian city of Sumy published the results of their a little research the effectiveness and safety of nifedipine in the treatment of chronic hypertension, preeclampsia and gestational hypertension during pregnancy. Under their supervision were 50 pregnant women with hypertension, who were divided into three groups:

• Group 1 included 20 pregnant women with gestational hypertension (which began during pregnancy);
• group 2 - 20 pregnant women with preeclampsia;
• in the 3rd group - 10 pregnant women with chronic hypertension, which they had even before pregnancy.

Comprehensive examination of pregnant women was repeated regularly to assess changes. It included a general clinical examination, assessment of the fetal condition in the given functional methods(determining the biophysical profile of the fetus), Doppler study. Determination of the biophysical profile of the fetus was carried out by transabdominal scanning using an ultrasonic portable scanner “Aloka SSD - 1800 (Toshiba, Japan) with a sensor from 3.5 to 10 MHz. The assessment of the biophysical profile of the fetus was carried out on the basis of an assessment of fetometry data, antenatal cardiotocography, the results of a study of tone, respiratory and motor activity fetus, ultrasound placentometry, determination of amniotic fluid volume. The condition of newborns was assessed based on general clinical examination, genetic examination, ultrasound examination.

Nifedipine has been used for gestational hypertension and preeclampsia, as well as for chronic hypertension in pregnant women as an effective fast-acting remedy and for long-term therapy during pregnancy 12-38 weeks. The indication for prescribing short-acting nifedipine tablets was an increase in blood pressure to a level of 150\100 mm Hg. and higher. The drug was prescribed orally in single doses of 5 and 10 mg and sublingually 10 and 20 mg. Daily doses ranged from 30 to 120 mg. The dose of the drug for each patient was selected individually.

Studies have noted a rapid and significant decrease in blood pressure (systolic by the 30th minute, diastolic by the 20th minute when taken orally), which persisted for 2-4 hours. An even faster effect was observed when the medicine was applied sublingually. The severity of the effect on lowering blood pressure was almost the same in pregnant women who did not receive any prior treatment and in those patients who received methyldopa therapy before prescribing nifedipine. Carrying out daily monitoring of blood pressure, it was revealed that the drug has powerful action. However, in pregnant women with chronic hypertension, after dose selection, the effect remained the same over a 24-hour period. Their blood pressure did not exceed 120/90 mmHg.

A similar picture was observed in the group of women with gestational hypertension. In women with preeclamisia, blood pressure was less stable during the day; the effect of taking nifedipine was especially pronounced in the evening and at night. In some cases, nifedipine therapy was supplemented with the administration of clonidine (clonidine). Five pregnant women were admitted to the hospital during a hypertensive crisis. To relieve the latter, nifedipine 10 mg sublingually was used. Positive result was achieved by taking the drug twice every 30 minutes.

Side effects of nifedipine during pregnancy

In pregnant women receiving nifedipine, side effects were noted from:

• fetal heartbeat (unstable heart rate - in 14.0%, tachycardia - in 8.0%);
• breathing movements fetus (increase in the number of episodes of respiratory movements - in 14.0%, disturbance in the form of fetal respiratory movements - gasps-type movements - in 10.0%);
• motor activity of the fetus (increased motor activity - in 6.0%);
• fetal tone (decreased in 6.0%).

Intrauterine growth retardation was observed quite often - in 60.0%, polyhydramnios - in 20.0% of pregnant women, oligohydramnios - in another 20.0%.

When studying the structure of the placenta, in 10.0% of pregnant women there was a decrease in the intervillous space. In pregnant women receiving blood pressure pills, placental hypertrophy (12.0%) was observed less frequently than hypoplastic changes (30.0%). During the study, a delay in its maturation of 18.0% was revealed. Destructive changes in the placenta were observed rarely - 2.0%. Placental abruption was diagnosed in 2 (4.0%) pregnant women.

In 7 women (14.0%) with signs of intrauterine infection of the fetus, changes in the structure of the placenta were accompanied by a disturbance in the pattern of the fetal heartbeat (tachycardia, unstable heart rate), in 4 (8.0%) women - changes in the motor activity of the fetus, in 9 (18 .0%) - impaired respiratory activity and in 3 (6.0%) - decreased fetal tone. When assessing the biophysical profile of the fetus, it was noted that in pregnant women receiving nifedipine therapy, it was 4.6+0.3 points. Signs of a compensated form of fetoplacental insufficiency (4 points) were determined in 80.0% of pregnant women in the main group, and a subcompensated form (3 points) - in 20.0%.

All newborns had an Apgar score of 8-10 points at birth, although the maximum score was 10 points. An examination of newborns by a geneticist and an ultrasound study showed that taking nifedipine by women during pregnancy did not lead to the appearance of fetal malformations. Thus, nifedipine, according to data clinical trials, is not only effective, but also a fairly safe drug for the treatment of pregnant women.

Nifedipine: instructions for use and reviews

Extensive The medicine belongs to the group of drugs that block calcium channels and have pronounced antihypertensive properties.

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

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

The drug Nifedipine has the following indications for use:

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

Extended-release 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 blood vessels and increase their contraction, and the medicine blocks their flow.

It ensures expansion of the lumen of the coronary and peripheral branches of the arterial network, while reducing the resistance of the vascular walls and reducing the load on the heart. The drug is well absorbed into digestive tract, thereby its effect begins in the first ten minutes after consumption, which is especially important during a hypertensive crisis.

Composition and forms of the medicinal product

The international nonproprietary name of the drug Nifedipine (INN) is Nifedipine.

Nifedipine is available in various dosage forms:

1. film-coated tablets. They contain 10 mg of nifedipine, and 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 the bottles is 50 ml. One milliliter in 1 ml contains 0.0001 g of nifedipine;
4. solution for intracoronary administration is available in syringes of 2 ml, in 1 ml - 0.0001 g of nifedipine.

Use of the drug and dose

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

Tablets Nifedipine 10 mg

Rules for using Nifedipine:

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

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

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

The use of medicine requires compliance with certain rules:

1. the drug is used only under the supervision of a doctor. Take medication with caution if you have diabetes, severe forms cerebrovascular accidents, kidney and liver problems, hypovolemia;
2. During treatment with Nifedipine, you should completely abstain from alcohol. At the beginning of treatment, it is not recommended to drive;
3. it is necessary to consider which medications the drug can be combined with and which it should not be combined with. Nifedipine with tricyclic antidepressants, diuretics, nitrates, and blood pressure-lowering agents enhances the hypotensive effect. Combination use of the drug with beta-blockers may contribute to the development of heart failure. Combined 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 taken three times, those that are eliminated within 12 hours are taken twice a day, long-acting ones are taken once. It is advisable to administer the drug intravenously only in a hospital.

The drug intake depends on its half-life.

Contraindications

For collapse, cardiogenic shock, tachycardia, aortic stenosis, acute stage of infarction, severe heart failure, sensitivity to medication components. This medicine is not prescribed to children and patients under 18 years of age.

The drug may cause side effects:

1. from the digestive organs: diarrhea, heartburn, nausea, liver dysfunction. With long-term use of the drug with the prescription of high doses, the manifestation of dyspeptic symptoms and the development of intrahepatic cholestasis are possible;
2. from the hematopoietic organs: thrombocytopenia, leukopenia;
3. from the heart and blood vessels: redness skin, feeling of heat, the appearance of edema, a sharp decrease in pressure, tachycardia, angina, bradycardia;
4. from the outside genitourinary organs : increased secretion urine, kidney dysfunction;
5. from the central nervous system: headaches, sleep disturbances, visual disturbances, tremor of limbs;
6. from the outside endocrine system: gynecomastia;
7. from the skin: rash.

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

When the drug is injected intravenously, a burning sensation may occur at the injection site. When the drug is administered intracoronarily, the pressure may drop in the first minutes 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. Swelling that occurs while taking the medication quickly disappears after its discontinuation.

In case of 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, and the functions of the sinus node are significantly inhibited. If these symptoms are detected, the patient's stomach is washed and activated charcoal is prescribed.

Analogs

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

Drug analogues:

• Adalat;
• Cordiline;
• Calcigard retard;
• Cordafen.

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

A quick-acting medicine is not prescribed for 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 and consult your doctor about possible side effects.

Video on the topic

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

Nifedipine is a drug whose main therapeutic effect is aimed at treating hypertension. When taken, the coronary and peripheral arteries dilate, peripheral vascular resistance decreases, and the flow of calcium into vascular smooth muscle cells slows down. Nifedipine has also found use in the treatment of CHF, ischemia, angina and bradycardia.

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