Long-acting nifedipine preparations in modern cardiology

Release forms

There are two main forms of release of Nifedipine - tablets and gel-emulsion. Most often, patients are prescribed tablets. They contain a high content of active substance. Gel emulsion is an auxiliary preparation.

Tablets weighing 10 g can be packaged in blisters of 10 pieces each. These blisters are packed in cardboard boxes. Also, tablets of 20 or 50 pieces can be placed in plastic jars.

The gel emulsion is stored in a tube weighing 40 g. This medicine in this form of release is used only for the treatment of hemorrhoids.

There is also Nifedipine in the form of a solution for intravenous injection, as well as in the form of boluses that are injected into the coronary vessels.

How it affects the body

The medicine is a calcium antagonist and belongs to the group of slow calcium channel blockers (SCBC). The substance slows down the process of calcium penetration into the muscle cells of the heart, as well as into the cells of vascular muscles. Under the influence of the drug, the myocardium consumes less oxygen. Nifedipine lowers blood pressure and total peripheral vascular resistance, and the ability of the myocardium to contract is also slightly reduced.

Thanks to the medicine, the tone of the smooth muscles located in the vessels slightly decreases, therefore the peripheral and coronary arteries dilate. Due to this, blood flow in the coronary vessels is normalized. Myocardial conductivity is not inhibited. But you need to remember that Nifedipine does not act against arrhythmia and does not normalize heart rhythm.

Composition and effect of the drug

The drug includes the main active ingredient - nifedipine and auxiliary components. Among them are polysorbate, talc, gelatin, wheat starch, lactose monohydrate and others.

Nifedipine belongs to the group of calcium antagonists. The drug has a direct effect on blood vessels, which makes it possible to expand their walls, relieve spasm of smooth muscles, and lower blood pressure. After the active component of the drug enters the blood, the direct transmembrane movement of calcium through the smooth muscles is inhibited, affecting the myometrium (the muscular layer of the uterus). The important thing is that the level of calcium in the blood remains unchanged, that is, there is no deficiency.

Nifedipine during pregnancy is used for false contractions and increased uterine tone. After entering the body, Nifedipine is absorbed by the digestive system and joins plasma proteins. The maximum therapeutic effect occurs when the active substance of the drug is absorbed by 60–98%. On average, the product begins to work in 20–30 minutes, and its duration of action is up to 8 hours. It is important to note that Nifedipine does not affect blood parameters such as lipid levels, glucose and uric acid.

Indications for use

The doctor prescribes Nifedipine for the treatment of many diseases and pathological conditions:

• angina pectoris, including vasospastic;
• hypertension;
• Raynaud's disease;
• hypertension;
• hypertensive crisis.

Nifedipine is necessary for the prevention and relief of angina attacks, as well as for lowering blood pressure.

The doctor may recommend that the patient take the medicine only once a day. This is due to the fact that Nifedipine is active throughout the day.

For hemorrhoids at any stage up to the 4th stage, the doctor can prescribe Nifedipine gel. This gel dilates blood vessels and normalizes blood flow, which means it will help with rectal bleeding.

For what purpose is it used during pregnancy?

Why is the medicine prescribed to pregnant women? Nifedipine has a vasodilating effect on blood vessels. The drug is widely used in cardiological practice to normalize blood pressure and combat other symptoms of cardiovascular pathologies.

Despite the fact that the instructions for use contain contraindications such as pregnancy and lactation, doctors still prescribe the medicine in the second and third trimester among women suffering from pathologies of the heart and blood vessels. In addition, the medication is prescribed for uterine tone. Nifedipine helps reduce the threat of miscarriage, since its active components have a relaxing effect on the entire body, including the reproductive organ.

Only a doctor makes a decision on prescribing Nifedipine during pregnancy

Nifedipine is prescribed to women to lower blood pressure. During the period of bearing a baby, many patients report unstable blood pressure. To prevent complications and control the situation, doctors often use Nifedipine. During such a delicate period, even minor manifestations of cardiac dysfunction cannot be ignored. Often, heart and vascular diseases cause premature birth and even death of mother and child.

Instructions for use

The attending physician prescribes an individual dosage to the patient and selects the drug in a suitable release form.

How to take Nifedipine tablets - instructions:

1. At the beginning of the course of treatment, the doctor may prescribe 1 tablet (10 mg) 3-4 times a day.
2. Then it may be necessary to take 2 tablets (20 mg) 3-4 times a day.
3. In severe cases, the dose is increased to 3 tablets (30 mg) 3-4 times a day. This occurs with severe hypertension, as well as with variant angina.
4. In case of an acute attack of angina, it is recommended to take 1-2 tablets (10-20 mg) under the tongue.

An acute attack can be stopped with Nifedipine injections. Within 4–8 hours, injections of 5 mg of the drug are given.

For severe spasms of the coronary arteries, Nifedipine boluses of 100–200 mcg are used. They are injected directly into the vessels (intracoronary). To treat coronary stenosis, boluses of 50–100 mcg are taken.

You must take the medicine strictly in accordance with the recommendations and prescriptions of your doctor. You should not self-medicate, otherwise you can harm your health.

Features of treatment in different trimesters

During pregnancy, Nifedipine should only be prescribed by a qualified specialist. Self-medication with the drug can provoke the most severe complications, especially in the early stages of pregnancy. Before using the drug, a woman is prescribed all the necessary tests that will help identify contraindications and prevent the negative effect of the drug on the body of the mother and fetus.

I trimester

Most doctors are of the opinion that Nifedipine is completely contraindicated in the first 12 weeks of pregnancy. It is during this period that the formation of the neural tube and the laying of the child’s organs occurs. The slightest failure can provoke severe consequences, fetal malformations. The risk of miscarriage with all the ensuing consequences for the mother is very high.

Important! In the first weeks of pregnancy, Nifedipine is used only in cases of extreme necessity, when there is a serious threat to the life and health of the mother.

II and III trimester

At this stage, the drug is used if there are certain indications for the mother. These include:

• hypertension;
• angina pectoris;
• conditions accompanied by increased uterine tone;
• risk of premature birth;
• late toxicosis.

Typically, the dose of the drug for a pregnant woman is up to 2 tablets throughout the day. Under no circumstances should you exceed the dose prescribed by your doctor. An overdose leads to the development of severe complications and miscarriage.

Side effects

The medicine may cause some side symptoms. To relieve them, your doctor may prescribe additional medications.

Side effects:

• increased heart rate;
• skin redness;
• feeling of warmth or heat on the skin;
• hypotension;
• slight swelling;
• skin rash;
• ventricular tachycardia;
• slow heart rate;
• increased attacks of angina pectoris;
• cardiac arrest, asystole;
• heartburn, nausea, diarrhea;
• swelling of the gums;
• liver dysfunction;
• muscle pain;
• headache;
• sleep disorders;
• tremor of the limbs;
• visual disturbances;
• thrombocytopenia;
• leukopenia;
• renal dysfunction;
• increase in the daily amount of urine excreted;
• sudden enlargement of the breast (gynecomastia).

After an intravenous injection, the patient may feel a burning sensation. After intracoronary administration of the drug, within the first minute the patient’s pulse may sharply increase and blood pressure may drop. These unpleasant sensations disappear after 5–15 minutes.

Contraindications

There are many contraindications that prohibit the use of this drug for some patients:

• collapse;
• severe form of heart failure;
• hypotension, in which systolic (upper) pressure falls below 90 mmHg;
• cardiogenic shock;
• the first 4 weeks after myocardial infarction (acute period);
• aortic stenosis;
• unstable form of angina;
• lactose intolerance, lactase deficiency;
• GGM syndrome - impaired absorption of glucose and galactose;
• increased individual intolerance;
• lactation period;
• pregnancy less than 20 weeks;
• children's age (up to 18 years).

For these diagnoses and conditions, it is necessary to prescribe other medications to the patient. Nifedipine is not suitable for long-term treatment.

Recently, cardiologists conducted a study in which they proved that Nifedipine increases the risk of sudden cardiac arrest, so this medicine must be taken with extreme caution.

Is Nifedipine dangerous during pregnancy?

The question of how negatively Nifedipine affects the fetus is quite controversial. Supporters of one point of view argue that the drug does not pose the slightest danger to the mother and fetus. Proof of this is many years of practice and some medical research. Other sources claim that no research has been conducted on this matter and the effect of the drug on the development of the fetus and the health of the woman during pregnancy can be very negative. Therefore, the use of the medicine during such a delicate period is strictly not recommended.

Information from third sources indicates that studies were nevertheless conducted and their results revealed that Nifedipine has the most negative effect on the fetus. Another point of view is that the medicine is dangerous only in the first stages of pregnancy, but in the second and third trimester the drug does not pose any threat.

It is quite difficult to understand such opposing opinions. Only a specialist can assess the benefits and risks of taking a drug in a particular case. The doctor is obliged to assess the condition of the pregnant woman and child and make a decision individually for each patient.

Carefully

Patients suffering from certain diseases should be extremely attentive to their health. They will have to drink Nifedipine with caution:

• elderly patients;
• hypertrophic obstructive cardiomyopathy;
• severe liver diseases;
• sick sinus syndrome;
• kidney dysfunction;
• mitral valve stenosis;
• chronic heart failure;
• diabetes;
• stenosis of any part of the intestine;
• disturbances in the functioning of cerebral vessels.

Taking the medication in these cases should be strictly under the control and supervision of the attending physician.

Overdose symptoms

You should not take more than 120 mg tablets per day. The maximum dose of intravenous solution is 30 mg.

Signs of overdose:

• a sharp slowdown in heart rate;
• bradyarrhythmia;
• heart rhythm disturbances;
• hypotension;
• collapse;
• cardiogenic shock;
• convulsions;
• loss of consciousness;
• hypoxia;
• acidosis;
• slowing of cardiac conduction;
• hyperglycemia;
• coma.

Symptoms appear 3-4 hours after taking the tablets. In case of overdose, the patient's stomach is washed and activated charcoal is administered. He is then given intravenous injections of atropine with calcium gluconate, calcium chloride and norepinephrine to relieve intoxication. Due to proven ineffectiveness, hemodialysis is not performed.

Interaction with other drugs

Blood pressure drops sharply when Nifedipine is taken simultaneously with other antihypertensive drugs, as well as diuretics, diltiazem, and drugs based on phenothiazine and its derivatives.

Attention and memory may be affected when Nifedipine is used with anticholinergic medications.

This medicine should not be combined with beta-blockers, otherwise severe hypotension and even heart failure may occur.

In combination with magnesium salts, the patient experiences severe muscle weakness.

The effective effect against angina pectoris is enhanced when the drug is combined with nitrates.

Due to the intake of digoxin and theophylline, the amount of these substances in the blood increases.

You should not take Nifedipine together with medications containing calcium. These substances have opposite properties, which reduces their effectiveness. Side effects of the drug are enhanced in combination with fluoxetine and vincristine. Also, the effect of Nifedipine is reduced in combination with rifampicin, so these two drugs are incompatible with each other.

The level of nifedipine in the blood decreases if you take the medicine together with phenytoin, phenobarbital or carbamazepine. Conversely, concentrations increase in combination with itraconazole, cimetidine, fluconazole and ranitidine.

The QT interval on the ECG is prolonged when Nifedipine is taken simultaneously with quinidine. This occurs because the amount of quinidine in the blood decreases sharply, and when it is discontinued, it suddenly increases.

Severe hypotension, dizziness and other unpleasant symptoms occur if the patient drinks Nifedipine and drinks containing ethyl alcohol. This drug should not be combined with grapefruit juice.

Medicines based on nifedipine are universal and suitable for the treatment of hemorrhoidal disease at any stage. Nifedipine for hemorrhoids helps normalize local blood circulation, eliminates pain in the anorectal area, relieves swelling, reduces nodes and lumps in size.

Nifedipine is a selective calcium channel blocker that can significantly reduce the amount of oxygen consumed by blood vessels. It is for these qualities that nifedipine is actively involved in the treatment of chronically high blood pressure. When applied topically, nifedipine dilates the vessels of the peripheral circulatory system, significantly lowers rectal pressure, eliminates spasms and has a vasodilating effect. Ointment and gel for hemorrhoids "Nifedipine" have the following advantages: rapid analgesic effect; stimulation of the process of regeneration of damaged tissues; elimination of swelling and congestion; bactericidal and antiseptic effects; virtually instant absorption into mucous membranes and muscle tissue. Nifedipine ointment accelerates the healing process of anal fissures, eliminates the feeling of burning and itching and allows you to get rid of most unpleasant symptoms literally in a matter of days. Composition of ointments and gels based on nifedipine. An ointment differs from a gel in the presence of an oil and fat base (the gel uses ordinary water as a base). Composition per 100 g ointment: nifedipine 0.3 g; lidocaine 1.5 g; isosorbitol dinitrate 0.4 g. anhydrous lanolin, starch.

Nifedipine effectively relaxes smooth muscles, promotes dilation of peripheral vessels and reduces rectal pressure. Lidocaine is intended to eliminate burning and pain in the anus. Isosorbitol dinitrate has a dilating effect on the peripheral circulatory system. Thanks to the balanced composition, it is also possible to get rid of microbes and the inflammatory process in the active phase. Indications and contraindications Nifedipine hemorrhoid ointment, emulsion and gel have virtually identical therapeutic effects and indications for use. They are usually recommended in the following cases: the occurrence of hemorrhoids and cones; the presence of internal or external hemorrhoids; the appearance of anal fissures; thrombosis and congestion; hemorrhoidal disease in chronic form. Cream and gel are also prescribed for hemorrhoids and anal fissures that occur in a child or during pregnancy. Such pharmaceutical products have no contraindications, with the exception of rare cases of individual intolerance to one of the components included in the composition. Allergic reactions to lidocaine are possible. No cases of overdose have been recorded to date.

Directions for use and doses

. Nifedipine ointment is used after hygiene procedures. Instructions for use (by day): Day 1. Apply about 1 g of the drug to the index finger and lubricate the anus area with light circular movements. Pay special attention to protruding hemorrhoids. II day. Treat the outer part of the anus. Introduce a small amount of gel into the anus. Act slowly and carefully to avoid mechanical damage to the inflamed areas. In the following days, use the gel internally and externally 4 times a day. After the symptoms of the acute stage of the disease disappear, the drug can be used only in the morning and evening. With proper use of the gel, after a few days the pain decreases and anal bleeding stops. The full course lasts 28 days. In the chronic form, Nifedipine can be used only during exacerbation of the disease.

Cost of 1 can of 50g: 400 rub.

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special instructions

Nifedipine should be taken only under the strict supervision of doctors. Elderly patients are advised to reduce the dose. The medicine causes withdrawal symptoms, so it is discontinued gradually. It is necessary to discontinue the drug if the patient experiences chest pain.

If a person has stenosis of two coronary vessels, then the medicine cannot be administered intracoronarily into the third.

During the course of treatment it is forbidden to drink alcohol. It is advisable to refrain from working with machinery, driving a car or other types of transport, and also avoid dangerous work that requires great concentration.

Patient reviews

Anna, Moscow “I had to deal with Nifedipine at the 28th week of pregnancy, when the uterus became toned and there was a serious threat of miscarriage. I had previously heard about the drug that it should not be prescribed to pregnant women, as there is no data on this matter. Taking the medicine was quite alarming, but everything worked out and the baby was carried to term. I would like to advise expectant mothers to listen to doctors and under no circumstances self-medicate.”

Yulia, Sergiev Posad “I took Nifedipine in the late stages of pregnancy, as I developed late toxicosis, my blood pressure increased greatly, and I felt terrible. The leading doctor prescribed me Nifedipine, 1 tablet per day. Despite many negative reviews, the medicine had no effect on my child’s health. The drug relieved my blood pressure perfectly, there were no side effects.”

Svetlana, Ufa “After starting treatment with Nifedipine, the condition initially returned to normal, the pressure stabilized, but after a few days the headache began to hurt severely and rashes appeared in the face and neck. At that time I was in my seventh month. The drug had to be replaced. The doctor suggested that the medicine was not suitable for me individually, even though a sensitivity test was carried out.”

Valeria, Khimki “I was prescribed this drug several times throughout my pregnancy in short courses to relieve uterine tone. I was very afraid to take it, but the doctor assured me that the medicine was safe, saying that it was a new method of treatment. I didn’t argue with the specialist; fortunately, no side effects arose, I gave birth to a healthy baby on time.”

Analogs

The following drugs are complete or partial analogues of Nifedipine:

1. "Calcigard Retard".
2. "Cordaflex".
3. "Cordipin Retard."
4. "Kordipin HL".
5. "Corinfar".
6. "Corinfar Retard".
7. "Nifecard HL".
8. "Phenigidine."

The doctor may prescribe these drugs instead of Nifedipine. They have similar properties.