Enalapril recipe in Latin. Enalapril - instructions for use. Latest update of the description by the manufacturer

Let's find out at what blood pressure levels you should take it medicine Lorista - instructions for use of the drug will help us with this. The medicine is used for hypertension. This disease is characterized by an increase in blood pressure, which after some time can lead to damage to the kidneys, heart, and brain. Indications for use of Lorista include wide range action of the drug.

• general description
• Indications for use
• Contraindications
• How to take: dosage
• What is better to take: analogues
• Lorista or Lorista N
• Lorista or Lisinopril
• Lorista or Enalapril

general description

Lorista is a medicine in tablet form. The main active ingredient is losartan. There is a drug with different amounts of the active component - from 12.5 to 100 mg. One pack may contain from 7 to 14 tablets. average price Lorista in the pharmacy chain ranges from 140 to 490 rubles. The cost depends on the dosage and number of tablets.

The manufacturer of the drug is KRKA-RUS, which is located in Russia. After purchase, the tablets should be stored at an air temperature not exceeding +30°C. The shelf life of the medication is 2 years from the date of manufacture, and for 50 mg tablets – a little longer (5 years).

The active component of this medication is capable of blocking angiotensin II receptors, which are located in the heart, adrenal glands and other organs. The action of losartan leads to a decrease in the diameter of the arteries, which can significantly reduce blood pressure.

This drug is also indicated in the presence of heart failure. When used, patients experience increased endurance to physical activity. In patients with this pathology, the risk of hypertrophy of cardiac muscle tissue is reduced several times.

Maximum main concentration active substance After taking the medication, it is observed 1 hour later. Metabolites that are formed by liver cells begin their effect on the body of a sick person only after 2.5 hours. The decrease in pressure level with a decrease in the concentration of losartan (it is observed 6 hours after administration) occurs by 70-80% of the indicator that is characteristic of the peak concentration active substance. There is no withdrawal syndrome after stopping the drug.

Lorista does not affect the number of heart contractions, which must be taken into account when taking it. This drug It is highly effective for patients of different genders and age groups, including elderly patients.

Indications for use

Lorista blood pressure tablets are used in the following cases:

• hypertension of varying degrees;
• reducing the risk of stroke in patients with hypertension who also have ventricular hypertrophy. This should be confirmed with an ECG;
• to reduce blood pressure in patients with type 2 diabetes;
• treatment of heart failure. This disease is most often of a chronic type, which is typical for patients over 60 years of age. Lorista is used in patients who, for some reason, cannot take traditional medications (ACE inhibitors).

Contraindications

Tablets from high blood pressure Lorista is prohibited from use in the following cases:

• the presence of hypersensitivity to one of the components of the drug;
• low pressure;
• intolerance to the absorption of certain substances (glucose, galactose);
• hyperglycemia, dehydration;
• period of pregnancy and lactation, childhood;
• presence of lactose intolerance.

How to take: dosage

The drug is used orally according to a certain scheme, regardless of food consumption. The method of therapy depends on the diagnosis made to the sick person. It is recommended to adhere to the following rules:

• in the presence of hypertension, 50 mg of the drug is prescribed once a day. Stabilization of blood pressure occurs a month after the start of treatment. To achieve a better effect, the daily dose may be increased to 100 mg;
• for heart failure, therapy begins with a minimum dose of the drug – 12.5 mg. Next week, the use of a medication is already indicated, where one tablet contains 25 mg of the active substance. After another 7 days, the dosage is increased to 50 mg;
• to reduce the risk of stroke in the corresponding category of patients, the recommended daily dose of the drug is 50 mg. If hydrochlorothiazide is not additionally administered for treatment in the future, the number of tablets is doubled - up to 100 mg;
• for diabetes mellitus accompanied by high blood pressure, the use of 50 mg of Lorist per day is indicated. If necessary, this amount can be doubled.

What is better to take: analogues

Let's consider the main analogues of the drug and their features.

Lorista or Lorista N

What does Lorista N help with? This drug also has a pronounced hypotensive effect. In addition to losartan, it contains hydrochlorothiazide. This substance is a diuretic, the action of which occurs due to the disruption of the reabsorption of chloride, sodium, potassium and other ions. Hydrochlorothiazide provokes dilation of arterioles. Because of this, there is a decrease in performance blood pressure.

The diuretic effect of hydrochlorothiazide is observed 1 hour after entering the human body. The maximum concentration of this substance is observed after 4 hours. Stabilization of blood pressure occurs 3 days after the start of treatment combination drug. A lasting therapeutic effect occurs only after a month of treatment.

If necessary, its substitutes can be used instead of Lorist. Lozap is considered such a drug. Given medicine also contains losartan, which produces an antihypertensive effect.

This drug is used in the same way as Lorista. When used in patients with kidney or liver problems, in some cases it is recommended to reduce daily dose up to 25 mg.

Lorista or Lisinopril

The analogue has lisinopril in an amount of 10 or 20 mg as the main active ingredient. It is used for high blood pressure, including those caused by diabetes and heart failure.

This drug is used with caution in the presence of renal failure, autoimmune diseases, aortic stenosis and other pathological conditions.

Losartan is one of the analogues of Lorist. This substitute is used in the same way as the main medication. It is taken as the main component of treatment or as part of complex therapy.

This remedy is used according to a special scheme depending on the disease. It is recommended to take 1 tablet of Losartan per day, but with different dosages.

Lorista or Enalapril

Enalapril is an ACE inhibitor. Used to reduce blood pressure, in heart failure, and to prevent the development of ischemia. At first, the dose of the drug is 2.5 mg. After some time, the amount of the drug is increased to 10–20 mg per day.

This drug is contraindicated for pregnant and lactating women, children and adolescents. It is not used for stenosis of the hepatic arteries, hyperkalemia, porphyria.

Lorist's analogues are a worthy replacement. The best drug will be able to select a doctor who is able to take into account all the characteristics of the sick person. Choosing treatment on your own is dangerous to your health.

Captopril

Captopril is the first representative of drugs from the group of ACE inhibitors. Synthesized in 1973-75. and has since been used to treat hypertension, and subsequently heart failure. The emergence of captopril and other ACE inhibitors has significantly changed approaches to the treatment of diseases of cardio-vascular system.

ACE inhibitors - including captopril - have become the cornerstone of the treatment of heart failure. This was influenced by the impressive results of studies that assessed the effectiveness of drugs in this class.

Important for patients! Effective treatment captopril - this is only possible if you take the medicine regularly, 3-4 times a day, as prescribed by your doctor. This medicine is well suited for emergency treatment of hypertensive crisis. But its main purpose is the systemic treatment of hypertension and cardiovascular diseases.

Captopril and capoten are the same medicine. Later in the article we sometimes write “captopril” and sometimes “capoten”. It should be remembered that this is the same drug for hypertension and heart failure.

The dosage that is suitable for you personally can only be selected by experienced doctor. An overdose of capoten can excessively lower blood pressure, which can lead to a heart attack. Therefore, do not self-medicate! Get tested, and then consult with a competent specialist.

Captopril - instructions

This article consists of instructions for the drug captopril, which is supplemented by information from domestic and foreign medical journals. Official instructions on the use of captopril (Capoten) 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.

• Effective treatment of hypertension without drugs
• The best way to recover from hypertension (quickly, easily, healthy, without “chemical” drugs and dietary supplements)
• Hypertonic disease - folk way recover from it at stages 1 and 2

The instructions for the drug captopril, as well as any other materials on the Internet or printed publications, are intended for specialists. Patients - do not use this information for self-medication. The side effects of self-medication with blood pressure pills can cause irreparable harm to your health. Take capoten or captopril only as prescribed by a doctor. Read the section “Contraindications and precautions”.

• Causes of hypertension and how to eliminate them. Tests for hypertension

Indications for use

Indications for use of captopril:

• Hypertension, including its forms that are resistant to the action of other classes of drugs for hypertension;
• Malignant hypertension, especially when hypertension is combined with angina or congestive heart failure;
• Renovascular hypertension - due to problems with the blood vessels of the kidneys;
• Emergency assistance for hypertensive crises (chew the tablet and hold it under the tongue, read more in “How to provide emergency assistance during hypertensive crisis");
• Renoparenchymal hypertension in chronic or rapidly progressive glomerulonephritis (primary and secondary);
• High blood pressure in bronchial asthma;
• Diabetic nephropathy;
• Congestive heart failure, especially if the effect of cardiac glycosides or their combination with diuretics is insufficient;
• Conn's syndrome is primary hyperaldosteronism.

Benefits of captopril

Captopril has significant benefits in the treatment of hypertension and heart failure:

1. Reliably reduces the mortality rate from cardiovascular diseases;
2. Lowers blood pressure no worse than drugs from other major classes of hypertension drugs;
3. Capoten is very safe for the treatment of elderly and senile patients;
4. Has the ability to slow down the development of nephropathy - kidney damage - including diabetic;
5. Does not affect male potency;
6. Has antioxidant activity;
7. Proven to reduce frequency oncological diseases more effective than other classes of drugs;
8. Treatment with these tablets is often cheaper in cost, with approximately equal effectiveness.

All this makes it possible to classify captopril as the gold standard for the treatment of cardiovascular diseases.

Captopril tablets - how effective are they?

Captopril tablets have been used to treat hypertension and heart failure since the 1970s. Millions of patients know that they help well when they need to quickly “bring down” the pressure during a hypertensive crisis. Unfortunately, a very small part of these people take the trouble to go to the doctor and then take the medicine for hypertension as prescribed regularly, 2-4 times a day.

Newer and more “advanced” blood pressure pills are sartans, from the group of angiotensin-II receptor blockers. These drugs appeared on the market in the late 1990s. However, large studies from 2001-2003 showed that captopril lowered blood pressure and mortality from cardiovascular disease no worse than the new, more expensive pills.

These studies involved tens of thousands of patients. To obtain reliable results, patients did not know which pills they were actually taking. This is called a “double-blind, placebo-controlled study.” It turned out that at the beginning of the 21st century, captopril remains an attractive option among drugs for hypertension and heart failure.

This drug works very well and, importantly, is usually cheaper than alternative medications. Patients just don’t like that they have to take pills 3-4 times a day, and not once a day, like newer medications.

Proven effective and cost-effective supplements for normalizing blood pressure:

• Magnesium + Vitamin B6 from Source Naturals;
• Taurine from Jarrow Formulas;
• Fish oil from Now Foods.

Read more about the technique in the article “Treatment of hypertension without drugs“. How to order hypertension supplements from the USA - download instructions. Bring your blood pressure back to normal without harmful side effects, which cause "chemical" tablets. Improve your heart function. Become calmer, get rid of anxiety, sleep like a baby at night. Magnesium with vitamin B6 works wonders for hypertension. You will have excellent health, the envy of your peers.

Treatment of congestive heart failure

Captopril is recommended for the treatment of patients who have congestive heart failure due to left ventricular diastolic dysfunction. The dosage should be selected by a doctor, preferably in a hospital setting. Read more about this in the section “How to take captopril (dosage)”.

Capoten significantly reduces the risk sudden death by 20-30% for patients who have heart disease or heart failure. But only on condition that it is taken for a long time and regularly, and not “from time to time.” Side effects rarely make it necessary to stop this medication. Although sometimes severe intolerance to captopril occurs in patients.

The patient may experience improvement in well-being no earlier than a few weeks after the start of therapy. However, this drug quickly begins to inhibit the development of heart disease, already from the first week of use.

Also watch a video about the treatment of heart failure prepared by the friendly website Centr-Zdorovja.Com.

Captopril for blood pressure

Captopril for blood pressure can be used independently, but more often it is prescribed along with other medications for hypertension. These may be thiazide and thiazide-like diuretics, beta blockers, calcium antagonists or other drugs. If you want to lower your blood pressure to normal, then carefully study the article “Treating hypertension with combined tablets.”

With long-term and continuous use in patients with high blood pressure, capoten reduces hypertrophy of the left ventricle of the heart and inhibits the development of heart failure. It has been proven to reduce mortality, especially in patients who have suffered a myocardial infarction.

What is very important, captopril protects the kidneys from damage due to hypertension of any origin. It reduces proteinuria - the excretion of protein in the urine - and is a means of preventing nephrosclerosis and renal failure. This drug does not worsen blood cholesterol levels.

• Perindapril (Prestarium)
• Diroton (Lisinopril)
• Fosinopril (Monopril)
• Indapamide (Arifon)
• Bisoprolol (Concor)
• Nolriprel (combined, most powerful)

According to reviews from thousands of patients, captopril is considered one of the best means to quickly reduce blood pressure when it rises suddenly.

The author of the review should get tested and consult a doctor to determine and treat the cause of his hypertension. Otherwise, next time you won’t get off so easily. The pressure readings are very high. The risk of sudden heart attack or stroke is significant, despite feeling well.

Individual allergic reactions occur in 5-8% of people who start taking capoten. You need to agree with your doctor and switch to a medication for hypertension from a different group. For example, it could be a beta blocker or an angiotensin II receptor antagonist. Your doctor will decide which drug to prescribe depending on the other symptoms you have besides high blood pressure. Don't self-medicate! Concerning allergic reaction on captopril, then it was impossible to predict it in advance; you shouldn’t blame the doctor. Over time it will pass.

Anaprilin (propranolol) is an outdated medicine that, although it lowers blood pressure, does not reduce, and even increases, mortality. Your doctor is dense and does not follow the news at all. I strongly recommend that you contact another specialist. And, of course, try our method of treating hypertension without drugs.

This is probably the most that can be done in your situation. Treatment of hypertension in older people is complicated by their monstrous stubbornness. If you can convince an elderly person to take pills regularly, that’s good. It’s almost impossible to go to the clinic to get examined, get tested, normalize your diet and move more. But retirement years can be one of the happiest periods in life. Today's old people simply don't know what they are missing. I hope that at their age you and I will live differently, more fully.

Use of captopril for hypertension caused by kidney problems

If a patient is diagnosed with renovascular or renoparenchymal hypertension, it means that he has a serious kidney problem that causes hypertension. Although in most cases the opposite happens - first hypertension damages the kidneys, and then a vicious circle is formed.

In the case of renovascular (problems with the blood vessels of the kidneys) or renoparenchymal (problems with the filtering elements of the kidneys) hypertension, treatment with captopril begins with lower doses. Then the dosage is carefully adjusted based on the results of a blood test for creatinine. It is also advisable to monitor serum potassium levels.

How to take captopril (dosage)

The official instructions for the drug captopril for chronic heart failure recommend starting with a dosage of 6.25 mg 2-3 times a day. This dosage can then be gradually increased at intervals of at least 2 weeks.

After taking the first dose of 6.25 mg, it is recommended that the patient's blood pressure be measured every 30 minutes for the first 3 hours to assess the effect of the medication. The average maintenance dose of captopril for heart patients is 25 mg 2-3 times a day.

For hypertension, the instructions recommend starting to take capoten with a dosage of 25 mg 2 times a day. The second option is 12.5 mg 3 times a day. The dosage of tablets is determined based on the results of blood pressure monitoring, at home and in the hospital.

The maximum dosage of captopril for hypertension is 50 mg 3 times a day. Increasing the dose beyond this does not provide an additional decrease in blood pressure, but sharply increases the likelihood of side effects. We remind you that captopril for blood pressure is usually used as part of combination therapy. Read more in the article “Treating hypertension with combination medications”

For elderly patients, the initial dosage of captopril is 6.25 mg 2 times a day. If possible, it is advisable to maintain it at this level. The article “What medications for hypertension are prescribed to elderly patients” may also be useful for you.

Captopril dosage for patients with renal failure

With moderate renal impairment (glomerular filtration rate of 30 or more ml/min/1.73 m2), patients can take captopril up to 75-100 mg per day. If kidney disease is more severe (glomerular filtration rate less than 30 ml/min/1.73 m2), then start with a dosage of 6.25 mg 2-3 times a day. And then they try to carefully increase it, monitoring the test results. If diuretics are also required, loop diuretics rather than thiazide diuretics are prescribed.

pharmachologic effect

Angiotensin II is a hormone that causes contraction blood vessels, and also increases sodium retention in the body. It is formed from angiotensin-I by the angiotensin-converting enzyme. Captopril belongs to the group of drugs called ACE inhibitors. This means that it inhibits the activity of angiotensin-converting enzyme, reducing the concentration of angiotensin II in the blood.

As a result of this, total peripheral vascular resistance decreases, cardiac output and load tolerance increase. Capoten tablets increase blood flow in the vessels feeding the heart and kidneys. With long-term use, it reduces the severity of hypertrophy of the myocardium and blood vessel walls.

How captopril lowers blood pressure:

• Inhibits the activity of angiotensin-converting enzyme.
• Stimulates the synthesis of bradykinin - a natural vasodilator (relaxes blood vessels).
• Promotes increased synthesis of nitric oxide in tissues.
• Reduces the release of adrenaline and norepinephrine.
• Inhibits aldosterone synthesis.
• Strengthens the elasticity of the arteriolar wall.
• Stabilizes cerebral circulation in patients hypertension with symptoms of cerebrovascular insufficiency.

How this medicine protects the heart:

• Helps reduce the mass of hypertrophied left ventricular myocardium, which in to a greater extent expressed when combined with calcium channel blockers.
• Reduces pre- and afterload of the myocardium.
• Reduces the frequency of ventricular arrhythmias.
• Improves the condition of coronary circulation.
• Increases exercise tolerance in patients with angina pectoris.
• When combined with calcium channel blockers, it helps reduce cholesterol, low-density lipoproteins and very low-density lipoproteins.

Protection of blood vessels from damage in diabetes mellitus:

• Captopril inhibits aldosterone synthesis.
• Does not affect carbohydrate metabolism and tissue sensitivity to insulin.
• Increases natriuresis (sodium excretion in urine).
• Helps prevent stroke development.
• Prevents the development of renal hyperfiltration.
• Has an antiproteinuric effect (reduces protein excretion in urine).

How captopril is absorbed and acts in the body (pharmacokinetics)

After oral administration, captopril is rapidly absorbed, begins to act within 15-60 minutes, and peak concentrations in the blood are reached within an hour. Eating together with the drug reduces its content in the blood by up to 30-40%, so capoten tablets should be prescribed 1 hour before meals or 1-1.5 hours after meals.

The duration of the effect on lowering blood pressure depends on the dose and frequency of administration. For the development of complete pharmacological effect it takes several weeks.

Contraindications and precautions

Contraindications to the use of captopril:

• pregnancy and breastfeeding;
• bilateral renal artery stenosis;
• stenosis of the artery of the only functioning kidney;
• severe azotemia - increased content in the blood of nitrogenous metabolic products excreted by the kidneys;
• severe liver dysfunction;
• arterial hypotension;
• increased sensitivity to ACE inhibitors.

In patients autoimmune diseases, including with systemic lupus erythematosus, the level of leukocytes in the blood in the first 3 months of captopril therapy should be monitored every 2 weeks, and then once every 2 months. If this level decreases by 2 times from the original level, then the drug should be discontinued.

Special instructions for patients undergoing therapy with captopril or capoten:

1. At the first symptoms of any infection, consult a doctor immediately.
2. You cannot arbitrarily interrupt the medication, change its dosage or frequency of administration. This can be done only after agreement with the doctor - a personal visit or by phone.
3. You should see a doctor immediately if there is vomiting, diarrhea, increased sweating. Because due to increased loss of fluid by the body, severe hypotension can occur, i.e. an excessive decrease in blood pressure, which causes myocardial infarction.

Side effects and overdose

From the cardiovascular system: excessive decrease in blood pressure, tachycardia (increased heart rate), swelling of the legs.

Orthostatic hypotension is a sharp decrease in blood pressure when the patient gets up from a lying or sitting position. It manifests itself as dizziness and even fainting.

From the urinary system: proteinuria (excretion of protein in the urine), development of renal dysfunction - increased blood levels of urea and creatinine.

From the hematopoietic system (very rarely):

• neutropenia - decreased number of neutrophils
• anemia - decreased hemoglobin content in red blood cells
• thrombocytopenia - decreased platelet count
• agranulocytosis - the absence or sharp decrease in the content of granulocytes in the blood.

From the central side nervous system: dizziness, headache, ataxia (disorder of movement coordination), sensitivity disorders of the limbs, drowsiness, blurred vision, feeling of chronic fatigue.

From the outside respiratory system: dry cough that goes away after discontinuation of the drug, as well as very rarely bronchospasm and pulmonary edema.

Dermatological reactions: rash, itchy skin, increased sensitivity to light.

From the outside gastrointestinal tract, liver, pancreas: taste disturbances, dry mouth, inflammation of the oral mucosa, nausea, weak appetite, rarely - diarrhea, abdominal pain, increased activity of liver transaminases (enzymes), increased bilirubin, hepatitis.

Laboratory indicators:

• hyperkalemia - increased level of potassium in the blood;
• hyponatremia - sodium deficiency in the blood;
• acidosis - a change in the acid-base balance towards increased acidity.

Interaction with other drugs

If captopril is taken concomitantly with potassium-sparing diuretics or with potassium supplements, this can lead to hyperkalemia - increased level potassium in the blood.

With the simultaneous administration of lithium salts, the concentration of lithium in the blood serum may increase.

If capoten is taken simultaneously with allopurinol or procainamide, this increases the likelihood of developing neutropenia and/or Stevens-Johnson syndrome.

Use of this drug in patients receiving immunosuppressant therapy (such as cyclophosphacine or azathioprine) increases the risk of developing hematologic disorders (diseases of the blood system).

With the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate), a complex of symptoms was described, which included facial flushing, nausea, vomiting and a decrease in blood pressure.

Concomitant use of insulin or diabetes pills that lower blood sugar increases the risk of hypoglycemia.

The following drugs weaken or slow down the blood pressure lowering effect of captopril:

• indomethacin (and possibly other non-steroidal anti-inflammatory drugs);
• estrogens;
• clonidine (clonidine).

The effectiveness of captopril in lowering blood pressure is enhanced by diuretics, as well as vasodilators - drugs that relax and dilate blood vessels.

How safe is the use of captopril?

In 2009-2010, on the basis of the regional clinical hospital Ukrainian city of Rivne conducted a frequency study adverse reactions from taking captopril. The study involved patients with mild to moderate arterial hypertension. These were 500 people who were treated in a hospital, and another 499 patients who took Capoten on an outpatient basis, that is, at home.

What daily doses did these patients receive:

Daily dose of captopril (Capoten), mg

Place of treatment

Some of them received monotherapy with captopril, and the rest - as part of a combination of drugs for hypertension.
Distribution of patients by type of treatment with blood pressure pills (monotherapy or combination):

Of the 500 patients who were treated in a hospital, side effects from treatment with captopril were found in only 5 people (1%):

• flushes of blood to the skin (hyperemia) - 1 person. (0.2%);
• heartbeat - 1 person (0.2%);
• decreased appetite and taste disturbances - 2 people. (0.4%);
• dry mouth - 1 person. (0.2%).

These are not serious side effects that quickly disappeared after discontinuation of the drug. They didn't demand additional expenses for treatment and did not increase the time that patients spent in the hospital.

Of the 499 patients who took captopril for blood pressure on an outpatient basis, according to the survey results, 72 people (14%) complained of side effects. The list of side effects included:

• dry cough - 16 people. (3.2%);
• dry mouth - 8 people. (1.6%);
• taste disturbances - 1 person. (0.2%);
• heartbeat - 3 people (0.6%);
• flushes of blood to the skin (hyperemia) - 4 people. (0.8%);
• rash on the body - 5 people. (1.0%);
• dizziness - 10 people. (2.0%);
• headache - 6 people (1.2%);
• itchy skin - 2 people. (0.4%);
• hypotension (excessive decrease in blood pressure) - 3 people. (0.6%);
• vomiting - 2 people (0.4%);
• nausea - 8 people (1.6%);
• increased blood pressure - 2 people. (0.4%);
• swelling of the legs - 1 person. (0.2%);
• inflammation of the oral mucosa - 1 person. (0.2%).

Of these 72 people, 52 stopped taking the drug, and 20 continued to take it despite side effects because they felt it provided more health benefits.

It was found that the risk of side effects of capoten increases significantly in patients over the age of 70 years. And the more experience a patient has with hypertension, the higher the likelihood side effect medicines. At the same time, the study authors were unable to track the relationship between the dosage of tablets and blood pressure and the frequency of adverse reactions.

Attracts attention high level side effects in patients who took captopril on an outpatient basis. The study authors explained this as follows. 13.8% of these patients additionally took adelphan, and another 16.01% took clonidine. And these are only those who admitted to the doctor at the appointment... This situation is explained by the low culture of patients, their tendency to self-medicate and their reluctance to spend money on more expensive high-quality drugs for hypertension. It is worth emphasizing that none of the 999 people who were treated for high blood pressure with Capoten experienced severe side effects.

Release form

The release form of captopril is tablets of 25 and 50 mg. They are packaged in contour cells of 10 pcs. IN cardboard box there can be from 1 to 10 contour cells, i.e. from 10 to 100 Capoten tablets.

See also the article “ACE inhibitors: side effects”.

• ACE inhibitors - general information
• Enalapril
• Lisinopril
• Moexpril
• Perindopril (Prestarium)
• Spirapril (quadropril)
• Fosinopril (monopril)

Characteristics of the substance Enalapril

An ACE inhibitor, related to drugs that affect the RAAS. It is a derivative of the amino acids L-alanine and L-proline.

Pharmacology

Pharmacodynamics

Antihypertensive drug used for the treatment of essential hypertension (primary arterial hypertension of any severity) and renovascular hypertension, both in monotherapy and in combination with others antihypertensive drugs, in particular diuretics. Enalapril is also used to treat or prevent the development of heart failure.

After oral administration, enalapril is rapidly absorbed and hydrolyzed into enalaprilat, which is a highly specific and long-acting ACE inhibitor that does not contain a sulfhydryl group.

ACE (peptidyl dipeptidase A) catalyzes the conversion of angiotensin I to the vasopressor peptide angiotensin II. ACE inhibition leads to a decrease in the concentration of angiotensin II in the blood plasma, which entails an increase in the activity of plasma renin (due to the elimination of negative feedback in response to the release of renin) and a decrease in aldosterone secretion. At the same time, SBP and DBP, OPSS decrease, post- and preload on the myocardium decrease.

Enalapril dilates arteries more than veins, but there is no reflex increase in heart rate.

ACE is identical to the enzyme kininase II, so enalapril can also block the destruction of bradykinin, a peptide that has a pronounced vasodilating effect. The significance of this effect in the therapeutic action of enalapril requires clarification. The main mechanism of the antihypertensive effect of enalapril is considered to be suppression of the activity of the RAAS, which plays an important role in regulating blood pressure, but enalapril exhibits an antihypertensive effect even in patients with arterial hypertension and with reduced plasma renin activity. The antihypertensive effect is more pronounced at high renin concentrations than at normal or low levels.

The use of enalapril in patients with arterial hypertension leads to a decrease in blood pressure both in a standing position and in a lying position without significant increase Heart rate. Symptomatic orthostatic (postural) hypotension rarely develops during treatment with enalapril.

Effective inhibition of ACE activity usually develops 2-4 hours after a single oral dose of enalapril. The antihypertensive effect develops within 1 hour, the maximum decrease in blood pressure is observed 4-6 hours after taking enalapril. The duration of action depends on the dose. When using recommended doses, the antihypertensive effect and hemodynamic effects persist for 24 hours after administration.

In some patients, achieving optimal blood pressure reduction may require several weeks of therapy. Interruption of enalapril therapy does not cause a sharp rise in blood pressure.

Antihypertensive therapy with enalapril leads to a significant regression of left ventricular hypertrophy and preservation of its systolic function.

In patients with essential hypertension, a decrease in blood pressure is accompanied by a decrease in peripheral vascular resistance and an increase in cardiac output, while heart rate does not change or changes slightly.

After taking enalapril, an increase in renal blood flow is observed. At the same time, GFR does not change, and there are no signs of sodium or fluid retention. However, in patients with initially reduced glomerular filtration rate, its rate usually increases.

Enalapril reduces intraglomerular hypertension, slowing the development of glomerulosclerosis and the risk of developing chronic renal failure.

Long-term use of enalapril in patients with essential hypertension and renal failure may lead to improved renal function, as evidenced by an increase in GFR.

In patients with renal failure and diabetes mellitus or without it, there is a decrease in albuminuria, renal excretion of IgG, as well as a decrease in total protein in the urine after taking enalapril.

With simultaneous use of enalapril and thiazide diuretics, a more pronounced antihypertensive effect is observed. Enalapril reduces or prevents the development of hypokalemia caused by taking thiazide diuretics.

Enalapril therapy is not usually associated with adverse effects on concentration. uric acid in blood plasma.

Enalapril therapy is accompanied by a beneficial effect on the ratio of lipoprotein fractions in the blood plasma and no effect or a beneficial effect on the concentration of total cholesterol.

In patients with CHF during therapy with cardiac glycosides and diuretics, taking enalapril causes a decrease in peripheral vascular resistance and blood pressure. Cardiac output increases, while heart rate (usually elevated in patients with CHF) decreases. Wedge pressure in the pulmonary capillaries is also reduced. Tolerance to physical activity and severity of heart failure, as assessed by NYHA criteria, improve. These effects are observed with long-term therapy with enalapril.

In patients with mild to moderate heart failure, enalapril slows the progression of cardiac dilatation and heart failure, as evidenced by a decrease in diastolic and systolic volumes and an improvement in left ventricular ejection fraction.

In case of left ventricular dysfunction, enalapril reduces the risk of major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).

Enalapril reduces the incidence of ventricular arrhythmias in patients with heart failure, although the underlying mechanisms and clinical significance of this effect are unknown.

With CHF noticeable clinical effect observed with long-term treatment for 6 months or more.

Pharmacokinetics

Suction. After oral administration, enalapril is rapidly absorbed into the gastrointestinal tract. Cmax of enalapril in blood serum is achieved within 1 hour after oral administration. The degree of absorption when taken orally is approximately 60%. Concomitant food intake does not affect the absorption of enalapril.

After absorption, enalapril is rapidly hydrolyzed to form the active metabolite enalaprilat, a strong ACE inhibitor. Cmax of enalaprilat in the blood serum is observed approximately 4 hours after taking an oral dose of enalapril. The duration of absorption and hydrolysis of enalapril is similar for various recommended therapeutic doses. In healthy volunteers with normal renal function, C ss of enalaprilat in the blood serum is achieved by 4 days from the start of taking enalapril.

Distribution. In the range of therapeutic doses, the binding of enalaprilat to plasma proteins does not exceed 60%.

Enalaprilat easily penetrates histohematic barriers, excluding the blood-brain barrier; a small amount penetrates the blood-brain barrier and into breast milk.

Metabolism. There is no data on other significant pathways of metabolism of enalapril other than hydrolysis to enalaprilat. The rate of hydrolysis of enalapril may be reduced in patients with impaired liver function without reducing the therapeutic effect.

Excretion. Excretion of enalaprilat is carried out mainly by the kidneys - 60% (20% - unchanged and 40% - in the form of enalaprilat), through the intestines - 33% (6% - unchanged and 27% - in the form of enalaprilat). The main metabolites detected in urine are enalaprilat, accounting for approximately 40% of the dose taken, and unchanged enalapril. There are no data on other metabolites of enalapril. The plasma concentration profile of enalaprilat has a long terminal phase, apparently due to its binding to ACE. T1/2 of enalaprilat is about 11 hours.

Special patient groups

Renal dysfunction. The AUC of enalapril and enalaprilat is increased in patients with renal impairment.

In patients with mild to moderate renal impairment (creatinine clearance 40-60 ml/min) after taking enalapril 5 mg once daily, the steady-state AUC value of enalaprilat is approximately 2 times higher than in patients with unchanged renal function.

In patients with severe renal failure (Cl creatinine ≤30 ml/min), after repeated use of enalapril, the AUC value of enalaprilat increases approximately 8 times, T 1/2 increases, and the achievement of C ss is delayed.

Enalaprilat can be removed from the general circulation using hemodialysis. Clearance during hemodialysis is 62 ml/min (1.03 ml/s).

Breast-feeding. After a single oral administration of enalapril at a dose of 20 mg in patients in postpartum period the average C max of enalapril in breast milk is 1.7 mcg/l (0.54-5.9 mcg/l) 4-6 hours after administration. The average Cmax of enalaprilat is 1.7 mcg/l (1.2-2.3 mcg/l) and is observed at various times within 24 hours after administration. Based on data on maximum concentrations in breast milk, the estimated maximum intake of enalapril for a full-term infant breastfeeding, is 0.16% of the dose calculated taking into account the mother’s body weight.

After taking enalapril orally at a dose of 10 mg once a day for 11 months, the C max of enalapril in breast milk is 2 μg/l 4 hours after administration, enalaprilat is 0.75 μg/l approximately 9 hours after administration. The average concentration in breast milk within 24 hours after taking enalapril is 1.44 mcg/l and enalaprilat is 0.63 mcg/l.

Use of the substance Enalapril

Essential hypertension of any severity; renovascular hypertension; heart failure of any severity (in patients with clinical manifestations of heart failure, enalapril is also indicated to increase patient survival, slow the progression of the disease, and reduce the frequency of hospitalizations for heart failure); prevention of the development of clinically significant heart failure (in patients without clinical symptoms heart failure with left ventricular dysfunction enalapril is indicated to slow the development clinical manifestations diseases, reducing the frequency of hospitalizations for heart failure); prevention of coronary ischemia in patients with left ventricular dysfunction to reduce the incidence of myocardial infarction and reduce the frequency of hospitalizations for unstable angina.

Contraindications

Hypersensitivity to enalapril or other ACE inhibitors; angioedema history associated with previous use of ACE inhibitors, as well as hereditary or idiopathic angioedema; simultaneous use with aliskiren or aliskiren-containing drugs in patients with diabetes mellitus and/or impaired renal function (GFR<60 мл/мин/1,73 м 2) (см. «Взаимодействие»); возраст до 18 лет (безопасность и эффективность применения не изучены); беременность и период грудного вскармливания; наследственная непереносимость лактозы, дефицит лактазы, синдром глюкозо-галактозной мальабсорбции.

Restrictions on use

Bilateral renal artery stenosis or stenosis of the artery of a single kidney; condition after kidney transplantation; aortic or mitral stenosis (with impaired hemodynamic parameters); hypertrophic obstructive cardiomopathy; IHD; cerebrovascular diseases (including cerebrovascular insufficiency); renal failure (Cl creatinine<80 мл/мин); угнетение костномозгового кроветворения; системные заболевания соединительной ткани (в т.ч. склеродермия, системная красная волчанка), иммуносупрессивная терапия, лечение с применением аллопуринола или прокаинамида или комбинация указанных осложняющих факторов; печеночная недостаточность; сахарный диабет; гиперкалиемия; одновременное применение калийсберегающих диуретиков, препаратов калия, калийсодержащих заменителей поваренной соли и препаратов лития; проведение процедуры афереза ЛПНП с использованием декстрана сульфата; отягощенный аллергологический анамнез или ангионевротический отек в анамнезе; состояния, сопровождающиеся снижением ОЦК (в т.ч. при терапии диуретиками, соблюдении диеты с ограничением поваренной соли, диализе, диарее или рвоте); проведение десенсибилизации аллергеном из яда перепончатокрылых; у пациентов, находящихся на диализе с применением высокопроточных мембран (таких как AN 69 ®); после больших хирургических вмешательств или при проведении общей анестезии; у пациентов негроидной расы; пожилой возраст (>65 years old); primary aldosteronism.

Use during pregnancy and breastfeeding

If pregnancy occurs, enalapril should be discontinued immediately unless it is considered essential for the mother.

Epidemiological data indicate a possible teratogenic effect on the fetus of ACE inhibitors in the first trimester of pregnancy. If ACE inhibitor therapy is not vital, then women planning pregnancy should use other antihypertensive drugs approved during pregnancy that have proven safety.

ACE inhibitors can cause disease or death of the fetus or newborn when used in the second and third trimesters of pregnancy. The use of ACE inhibitors during these periods was accompanied by negative effects on the fetus and newborn, including the development of arterial hypotension, renal failure, hyperkalemia and/or hypoplasia of the skull bones in the newborn. Prematurity, intrauterine growth restriction, and patent ductus arteriosus have also been reported, but it is unclear whether these cases were associated with ACE inhibitors. In cases where the use of an ACE inhibitor during pregnancy is considered necessary, periodic ultrasound should be performed to assess the amniotic fluid index; if oligohydramnios is detected, enalapril should be discontinued unless its use is considered vital for the mother. However, both the patient and the physician should be aware that oligohydramnios occurs when there is irreversible damage to the fetus. If ACE inhibitors are used during pregnancy and the development of oligohydramnios is observed, then, depending on the stage of pregnancy, a stress test, a non-stress test or determination of the biophysical profile of the fetus may be necessary to assess the functional status of the fetus.

It is possible that the development of oligohydramnios occurs due to a decrease in fetal renal function. This complication can lead to contracture of the limbs, deformation of the bones of the skull, including the facial part, and hypoplasia of the lungs. When using enalapril, the patient must be informed of the potential risk to the fetus. Neonates whose mothers took enalapril should be closely monitored for hypotension, oliguria, and hyperkalemia.

Enalapril, which crosses the placenta, can be partially removed from the neonatal circulation by peritoneal dialysis; theoretically it can be removed through exchange transfusion.

Enalapril and enalaprilat are excreted in breast milk in trace concentrations. If it is necessary to use enalapril during lactation, breastfeeding should be discontinued.

Side effects of the substance Enalapril

The frequency of adverse reactions is given in accordance with the WHO classification: very often (>1/10); often (>1/100,<1/10); нечасто (>1/1000, <1/100); редко (>1/10000, <1/1000); очень редко (<1/10000, включая отдельные сообщения); частота неизвестна (определить частоту возникновения по имеющимся данным невозможно).

From the blood and lymphatic system: infrequently - anemia (including aplastic and hemolytic); rarely - neutropenia, decreased hemoglobin and hematocrit levels, thrombocytopenia, agranulocytosis, suppression of bone marrow hematopoiesis, pancytopenia, lymphadenopathy, autoimmune diseases.

Metabolic and nutritional disorders: uncommon - hypoglycemia (see "Precautions").

From the side of the central nervous system: very often - dizziness; often - headache, depression; uncommon - confusion, drowsiness, insomnia, increased excitability, paresthesia, vertigo; rarely - unusual dreams, sleep disturbances.

Hearing and labyrinth disorders: infrequently - tinnitus.

From the side of the organ of vision: rarely - blurred vision.

From the SSS side: often - marked decrease in blood pressure, fainting, chest pain, heart rhythm disturbances, angina pectoris, tachycardia; uncommon - orthostatic hypotension, palpitations, myocardial infarction or stroke (possibly caused by a sharp decrease in blood pressure in high-risk patients) (see "Precautions"); rarely - Raynaud's syndrome.

From the respiratory system, chest and mediastinal organs: very often - cough; often - shortness of breath; uncommon - rhinorrhea, sore throat, hoarseness, bronchospasm/bronchial asthma; rarely - pulmonary infiltrates, rhinitis, allergic alveolitis/eosinophilic pneumonia.

From the digestive system: very often - nausea; often - diarrhea, abdominal pain, taste disturbance; uncommon - intestinal obstruction, pancreatitis, vomiting, dyspepsia, constipation, anorexia, stomach irritation, dry oral mucosa, gastric and duodenal ulcers; rarely - stomatitis/aphthous ulcers, glossitis; very rarely - intestinal edema.

From the liver and biliary tract: rarely - liver failure, hepatitis (hepatocellular or cholestatic), including hepatic necrosis, cholestasis (including jaundice).

For the skin and subcutaneous tissues: often - hypersensitivity reactions/angioedema of the face, limbs, lips, tongue, vocal folds and/or larynx, skin rash; uncommon - increased sweating, itching, urticaria, alopecia; rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis, pemphigus, erythroderma.

The development of a symptom complex has been reported, which may be accompanied by some and/or all of the following symptoms: fever, serositis, vasculitis, myalgia/myositis, arthralgia/arthritis, positive antinuclear antibody test, increased ESR, eosinophilia and leukocytosis. Skin rash, photosensitivity, or other skin reactions may also occur.

From the kidneys and urinary tract: uncommon - renal dysfunction, renal failure, proteinuria; rarely - oliguria.

From the endocrine system: frequency unknown - syndrome of inappropriate ADH secretion.

From the genital organs and breast: uncommon - erectile dysfunction; rarely - gynecomastia.

Deviations in laboratory and instrumental research data: often - hyperkalemia, increased creatinine concentration in the blood serum; uncommon - hyponatremia, increased urea concentration in the blood; rarely - increased activity of liver transaminases, increased concentration of bilirubin in the blood serum.

Common disorders: very often - asthenia; often - increased fatigue; uncommon - muscle cramps, flushing of the face, discomfort, fever.

In rare cases, with the simultaneous use of ACE inhibitors (including enalapril) and intravenous administration of gold preparations (sodium aurothiomalate), a symptom complex has been described, including redness of the facial skin, nausea, vomiting and arterial hypotension.

Adverse events that were observed during post-marketing use of enalapril (a cause-and-effect relationship has not been established): urinary tract infection, upper respiratory tract infection, bronchitis, cardiac arrest, atrial fibrillation, herpes zoster, melena, ataxia, pulmonary embolism and pulmonary infarction, hemolytic anemia, including cases of hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency.

Interaction

Other antihypertensive drugs. With simultaneous use of enalapril and other antihypertensive therapy, an additive effect may be observed.

When enalapril is used concomitantly with other antihypertensive drugs, especially diuretics, an enhanced antihypertensive effect may be observed.

Simultaneous use with beta-blockers, methyldopa or CCB increases the severity of the antihypertensive effect.

Concomitant use with alpha-, beta-blockers and ganglion blockers should be carried out under close medical supervision.

Concomitant use with nitroglycerin, other nitrates or vasodilators enhances the antihypertensive effect.

Serum potassium. In patients with arterial hypertension who took enalapril monotherapy for more than 48 weeks, there was an increase in serum potassium by an average of 0.2 mmol/l.

With the simultaneous use of enalapril with diuretics that cause the loss of potassium ions (thiazide or loop diuretics), hypokalemia caused by the action of diuretics is usually weakened due to the effect of enalapril.

Risk factors for the development of hyperkalemia include renal failure, diabetes mellitus, concomitant use of potassium-sparing diuretics (eg spironolactone, eplerenone, triamterene or amiloride), as well as potassium supplements and salts. The use of potassium supplements, potassium-sparing diuretics, or potassium-containing salts, especially in patients with impaired renal function, can lead to a significant increase in serum potassium levels. If necessary, simultaneous use of the above potassium-containing or potassium-increasing drugs should be used with caution and regularly monitor the potassium level in the blood serum.

Hypoglycemic agents. The simultaneous use of ACE inhibitors and hypoglycemic agents (insulin, hypoglycemic drugs for oral administration) may enhance the hypoglycemic effect of the latter with the risk of developing hypoglycemia. This effect is usually most often observed during the first weeks of combination therapy, as well as in patients with impaired renal function. In patients with diabetes mellitus taking oral hypoglycemic drugs or insulin, blood glucose concentrations should be regularly monitored, especially during the first month of simultaneous use with ACE inhibitors.

Lithium preparations. Like other drugs that affect sodium excretion, ACE inhibitors can reduce the excretion of lithium by the kidneys, therefore, when using lithium preparations and ACE inhibitors simultaneously, it is necessary to regularly monitor the concentration of lithium in the blood serum.

Tricyclic antidepressants/neuroleptics/general anesthesia. The simultaneous use of certain anesthetic drugs, tricyclic antidepressants and antipsychotics with ACE inhibitors can lead to a further decrease in blood pressure (see “Precautions”).

Ethanol. Ethanol enhances the antihypertensive effect of ACE inhibitors.

Acetylsalicylic acid, thrombolytics and beta-blockers. Enalapril can be used simultaneously with acetylsalicylic acid (as an antiplatelet agent), thrombolytics and beta-blockers.

Sympathomimetics. Sympathomimetics may reduce the antihypertensive effect of ACE inhibitors.

NSAIDs. NSAIDs, including selective COX-2 inhibitors, may reduce the effect of diuretics and other antihypertensive drugs. As a result, the antihypertensive effect of ARA II or ACE inhibitors may be weakened when used simultaneously with NSAIDs, incl. with selective COX-2 inhibitors.

In some patients with impaired renal function (for example, in elderly patients or patients with dehydration, including those taking diuretics), receiving therapy with NSAIDs, including selective COX-2 inhibitors, the simultaneous use of ARB II or ACE inhibitors may cause further deterioration of kidney function, including the development of acute renal failure. These effects are usually reversible, so simultaneous use of these drugs should be carried out with caution in patients with impaired renal function.

Double blockade of the RAAS. Dual blockade of the RAAS using ARB II, ACE inhibitors or aliskiren (renin inhibitor) is associated with an increased risk of arterial hypotension, syncope, hyperkalemia and renal dysfunction (including acute renal failure) compared with monotherapy. Regular monitoring of blood pressure, renal function and electrolyte levels in the blood is necessary in patients taking enalapril and other drugs that affect the RAAS at the same time. Enalapril should not be used concomitantly with aliskiren or aliskiren-containing drugs in patients with diabetes mellitus and/or impaired renal function (GFR<60 мл/мин/1,73 м 2).

The simultaneous use of ACE inhibitors with ARA II in patients with diabetic nephropathy is contraindicated.

Gold preparations. In rare cases, with the simultaneous use of gold preparations for parenteral administration (sodium aurothiomalate) and ACE inhibitors, including enalapril, a symptom complex (nitrate-like reactions) is observed, including a rush of blood to the facial skin, nausea, vomiting and arterial hypotension.

mTOR inhibitors. In patients using both an ACE inhibitor and an enzyme inhibitor mTOR (mammalian target of rapamycin- target of rapamycin in mammalian cells) (for example, temsirolimus, sirolimus, everolimus), therapy may be accompanied by an increased risk of angioedema.

Allopurinol, cytostatics and immunosuppressants. Concomitant use with ACE inhibitors may increase the risk of developing leukopenia.

Cyclosporine. Concomitant use with ACE inhibitors may increase the risk of developing hyperkalemia.

Antacids. May reduce the bioavailability of ACE inhibitors.

Theophylline. Enalapril weakens the effect of drugs containing theophylline.

Other medicines. There are no clinically significant pharmacokinetic drug interactions observed between enalapril and the following drugs: hydrochlorothiazide, furosemide, digoxin, timolol, methyldopa, warfarin, indomethacin, sulindac and cimetidine. With the simultaneous use of enalapril and propranolol, the concentration of enalaprilat in the blood serum decreases, but this effect is not clinically significant.

Overdose

Symptoms: pronounced decrease in blood pressure (begins approximately 6 hours after administration), up to the development of collapse, myocardial infarction, acute cerebrovascular accident or thromboembolic complications, water and electrolyte imbalance, renal failure, increased breathing, tachycardia, palpitations, bradycardia, dizziness, anxiety, fear, convulsions, cough, stupor. Enalaprilat plasma concentrations 100-200 times higher than after therapeutic doses were observed after oral administration of 300 and 440 mg of enalapril, respectively.

Treatment: transfer the patient to a horizontal position with a low headboard. In mild cases, gastric lavage and ingestion of activated charcoal are indicated; in more serious cases, measures aimed at normalizing blood pressure (IV administration of 0.9% sodium chloride solution, plasma expanders, and, if necessary, IV administration of catecholamines), hemodialysis (excretion rate) are indicated. enalaprilat - 62 ml/min). In patients with bradycardia that is resistant to therapy, pacemaker placement is indicated.

Routes of administration

Inside.

Precautions for the substance Enalapril

Symptomatic arterial hypotension. Symptomatic hypotension is rarely observed in patients with uncomplicated hypertension. In patients with arterial hypertension taking enalapril, arterial hypotension develops more often against the background of dehydration, which occurs, for example, as a result of diuretic therapy, restriction of salt intake, in patients on dialysis, as well as in patients with diarrhea or vomiting (see " Side effects", "Interaction"). Symptomatic hypotension is also observed in patients with heart failure with or without renal failure.

Arterial hypotension occurs more frequently in patients with more severe heart failure with hyponatremia or impaired renal function in whom higher doses of loop diuretics are used. In these patients, treatment with enalapril should be started under medical supervision, which should be especially careful when changing the dose of enalapril and/or diuretic. Similarly, patients with coronary artery disease or cerebrovascular disease should be monitored, in whom an excessive decrease in blood pressure may lead to the development of myocardial infarction or stroke.

If arterial hypotension develops, the patient should be laid down and, if necessary, a 0.9% sodium chloride solution should be administered. Transient arterial hypotension when taking enalapril is not a contraindication to further use and increasing the dose; therapy can be continued after fluid volume is replenished and blood pressure is normalized.

In some patients with heart failure and normal or low blood pressure, enalapril may cause an additional decrease in blood pressure. This reaction to taking enalapril is expected and is not a reason to stop treatment. In cases where arterial hypotension becomes stable, the dose should be reduced and/or treatment with a diuretic and/or enalapril should be discontinued.

Aortic or mitral stenosis/hypertrophic obstructive cardiomyopathy. Like all drugs that have a vasodilating effect, ACE inhibitors should be prescribed with caution to patients with left ventricular outflow tract obstruction.

Renal dysfunction. In some patients, hypotension that develops after initiation of treatment with ACE inhibitors may lead to further deterioration of renal function. In some cases, the development of acute renal failure, usually reversible, has been reported.

In patients with renal failure, a reduction in the dose and/or frequency of enalapril may be required. In some patients with bilateral renal artery stenosis or arterial stenosis of a solitary kidney, increases in blood urea and serum creatinine concentrations were observed. The changes were usually reversible, and indicators returned to baseline values ​​after cessation of treatment. This pattern of changes is most likely in patients with renal failure.

In some patients who did not have renal disease before treatment, enalapril in combination with diuretics usually caused a slight and transient increase in blood urea and serum creatinine concentrations. In such cases, it may be necessary to reduce the dose and/or discontinue the diuretic and/or enalapril.

Kidney transplantation. Treatment with enalapril is not recommended in patients after kidney transplantation due to the lack of experience with such use.

Liver failure. The use of ACE inhibitors is rarely associated with the development of a syndrome that begins with cholestatic jaundice or hepatitis and progresses to fulminant liver necrosis, sometimes fatal. The mechanism of this syndrome has not been studied. If jaundice appears or a significant increase in the activity of liver transaminases during the use of ACE inhibitors, enalapril should be discontinued and appropriate auxiliary therapy should be prescribed; the patient should be under appropriate supervision.

Neutropenia/agranulocytosis. Neutropenia/agranulocytosis, thrombocytopenia and anemia are observed in patients taking ACE inhibitors. Neutropenia occurs rarely in patients with normal renal function and no other complicating factors.

Enalapril should be used with extreme caution in patients with systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, etc.) taking immunosuppressive therapy, allopurinol or procainamide, or a combination of these complicating factors, especially if there are pre-existing renal impairments. Some of these patients develop serious infections, which in some cases do not respond to intensive antibiotic therapy. If enalapril is used in such patients, regular monitoring of white blood cell and lymphocyte counts is recommended and patients should be warned to report any signs of infectious disease.

Hypersensitivity reactions/angioedema. When using ACE inhibitors, including enalapril, rare cases of angioedema of the face, extremities, lips, tongue, vocal folds and/or larynx have been observed, occurring during different periods of treatment. In very rare cases, intestinal edema may develop. In such cases, you should immediately stop taking enalapril and carefully monitor the patient's condition in order to monitor and correct clinical symptoms. Even in cases where only swelling of the tongue is observed without the development of respiratory distress syndrome, patients may require long-term observation, since therapy with antihistamines and corticosteroids may not be sufficient.

Very rarely, deaths due to angioedema associated with swelling of the larynx or tongue have been reported. Swelling of the tongue, vocal folds, or larynx can lead to airway obstruction, especially in patients who have undergone respiratory surgery. In cases where swelling is localized in the area of ​​the tongue, vocal folds or larynx and can cause airway obstruction, appropriate treatment should be immediately prescribed, which may include subcutaneous injection of 0.1% epinephrine solution (0.3-0.5 ml ) and/or ensure airway patency.

In black patients taking ACE inhibitors, angioedema is observed more often than in patients of other races.

Patients with a history of angioedema not associated with taking ACE inhibitors may be at greater risk of developing angioedema during therapy with ACE inhibitors (see "Contraindications").

Anaphylactoid reactions during desensitization with an allergen from Hymenoptera venom. In rare cases, patients taking ACE inhibitors develop life-threatening anaphylactoid reactions during desensitization with hymenoptera venom allergen. Adverse reactions can be avoided if you temporarily stop taking the ACE inhibitor before starting desensitization.

Enalapril is a drug from the group of ACE inhibitors, used to treat arterial hypertension and heart failure. Enalapril is an inactive prodrug, its active metabolite is enalaprilat.

Enalapril is used alone (monotherapy) and in combination with other antihypertensive drugs (combination therapy). Combinations with or calcium channel blockers are especially common.

Enalapril reliably prolongs life in chronic heart failure - more details: . And is used to treat arterial hypertension.

Unlike some other ACE inhibitors, such as ramipril, enalapril has not shown any effectiveness in preventing myocardial infarction.

Mechanism of action

Enalapril inhibits ACE, which leads to a decrease in the formation of angiotensin 2 from angiotensin 1. A lower concentration of angiotensin 2 causes a decrease in blood vessel tone and, consequently, a drop in blood pressure levels

Mechanism of action of ACE inhibitors

A decrease in angiotensin 2 levels also leads to a decrease in the release of aldosterone from the adrenal cortex. Thus enalapril affects water and electrolyte balance(through the renin-angiotensin-aldosterone system).

Side effects

The main side effects of enalapril are related to its mechanism of action. ACE inhibition leads to a slowdown in metabolism and accumulation of bradykinin. Due to this, various skin reactions occur, such as exanthema, urticaria, and the possible development of Quincke's edema.

However, severe allergic reactions are extremely rare.

Side effects from the respiratory system include dry cough, sore throat and hoarseness. Asthma attacks and shortness of breath occur very rarely.

As a result of the main effect of enalapril, an excessive drop in blood pressure may occur. This causes dizziness, headaches and drowsiness.

Severe side effects from the cardiovascular system, such as angina pectoris, myocardial infarction and syncope, occur only in isolated cases.

Since enalapril, by inhibiting ACE, interferes with the body's water-salt metabolism, renal dysfunction may occur. Proteinuria is rare.

Enalapril during pregnancy causes serious side effects that interfere with the normal development and growth of the child's skeletal system, and also increases the risk of antenatal mortality. That's why enalapril is contraindicated during pregnancy and should be replaced with other drugs.

Interactions

Enalapril enhances the hypoglycemic effect of insulin and oral antidiabetic agents, as well as the effects of immunosuppressants.

Since enalapril interferes with water and electrolyte balance, problems with removing electrolytes from the body may occur. This should be taken into account when used together with lithium preparations.

When used with other antihypertensive agents, the possibility of an excessive decrease in blood pressure should be considered.

Enalapril recipe in Latin

The enalapril prescription in Latin is prescribed in the form of tablets (more details) with a dosage of 2.5; 5, 10 and 20 mg. For example, we will prescribe 5 mg of enalapril in the amount of 60 tablets, and we will prescribe it to be taken orally 2 times a day.

Rp.: Enalaprili 5 mg
D.t.d. N 60 in tab.
S. Orally, 1 tablet 2 times a day.

You can also write a prescription for enalapril using the trade name. In this case, the pharmacist does not have the right to change the drug at his discretion; he will issue exactly the one that is written in the prescription. For example, let’s write out a prescription for Renitec with a dosage of 10 mg and a quantity of 30 tablets, prescribed in the morning and evening.

Rp.: Tab. “Renitec” 10 mg
D.t.d. N 30
S. 1 tablet orally morning and evening

Here is a small list of trade names for enalapril prescription with dosages:

• Berlipril 5, 10, 20 mg;
• Enahexal 5 mg;
• Corvo 5 mg;
• Invoril 10 mg;
• Enap, Enarenal, Renitec 5, 10 and 20 mg;
• Enam 2.5 mg;
• Vasotec 2.5; 5, 10, 20 mg;
• Enam-LM 10.20 mg.

List of combination drugs containing enalapril:

• In combination with: Co-Acepril (CH), Co-Renitec (A), Co-Mepril (A), Co-Renistad (A), Coenytyrol (A), Elpradil HCT (CH), Epril plus (CH), Renitec plus (A), Reniten plus (CH).
• In combination with lercanidipine: Carmen ACE (D), Zaneril (D), Zanipress (D), Zanipril (A).
• In combination with nitrendipine: Baroprine (A), Cenipress (A), Eneas (D).

• Latin name: Enalapril
• ATX code: C09AA02
• Active substance: Enalapril
• Manufacturer: Hexal AG (Germany)

Compound

The tablets contain the active ingredient enalapril in the amount of 5, 10, 20 mg, as well as excipients: gelatin, lactose monohydrate, magnesium stearate, magnesium carbonate and crospovidone.

Release form

Tablets, 10 pieces in a blister, 2 blisters in a pack.

It is produced by different pharmaceutical companies, as a result of which the name of the company is added to the name of the active substance in the name of the drug, for example: Enalapril-Health.

pharmachologic effect

The medication reduces blood pressure, expands the lumen of blood vessels, and has cardioprotective And natriuretic action. The drug belongs to the group of angiotensin-converting enzyme inhibitors.

Pharmacological group: ACE inhibitors.

Pharmacodynamics and pharmacokinetics

According to the abstract, the mechanism of action is the inhibition of angiotensin-converting enzyme (ACE) by Enalapril, from which a decrease in the biosynthesis of angiothepsin II leads to vasodilation, the production of PGE2 and bradykinin, which are powerful vasodilators.

In patients with heart failure, with long-term use (6 months or more), there is an increase in the heart's tolerance to physical activity, a decrease in heart size, and a decrease in the number of deaths. Under the influence of the drug, the pulmonary circulation is unloaded, the pressure in the pulmonary capillaries decreases, the peripheral resistance decreases, and the cardiac output (Heart rate does not increase.)

The absorption of the drug Enalapril reaches 60%, regardless of the intake and presence of food in the gastrointestinal tract. The maximum concentration of the active substance enalaprilat is observed 1 hour after use. Biotransforms in the liver to enalaprilata . It easily passes through the placenta and histohematic barriers. Excreted by the kidneys. The hypotensive effect is recorded 1 hour after drug administration and lasts for a day. To achieve optimal blood pressure results, several weeks of regular use of Enalapril are required.

Indications for use of Enalapril

What are Enalapril tablets for?

Indications for the use of Enalapril are as follows: , Raynaud's disease, heart failure, symptomatic arterial hypertension, diabetic nephropathy , scleroderma , secondary hyperaldosteronism . Enalapril is prescribed as part of complex therapy for the treatment of tension and chronic renal failure. Use tablets for high blood pressure.

Contraindications

Hypersensitivity to ACE inhibitors, renal artery stenosis, azotemia , hyperaldosteronism, hyperkalemia , renal dysfunction, (hereditary), aortic stenosis, childhood. Enalapril is not prescribed.

Side effects

The drug has the following side effects: increased fatigue, dizziness, headache, convulsions, nervousness, insomnia, glossitis, tinnitus, nausea, orthostatic hypotension, palpitations, dyspepsia, disorders of the liver, kidneys, hyperkalemia, Quincke's edema , neutropenia, increased levels of bilirubin in the blood, hair loss, pain in the heart, increased concentrations of liver transaminases.

Enalapril tablets, instructions for use (Method and dosage)

The medicine is taken orally. The initial dosage is 5 mg per day, the drug is taken once a day. In case of pathology of the renal system or taking diuretics, the dose is reduced to 2.5 mg. To achieve an effect, depending on individual characteristics, the dose of the drug can be increased to 10-40 mg per day (can be divided into 2 doses).

Instructions for use Enalapril Hexal

The drug is used regardless of meals.

For arterial hypertension, you should take 5 mg of enalapril maleate in the morning. The maintenance dose is 10 mg. You should not take more than 40 mg of the drug per day.

For chronic heart failure, take 2.5 mg of the medication in the morning. The maintenance dose is 5-10 mg. You should not take more than 20 mg of the drug per day.

For left ventricular dysfunction, take 2.5 mg twice daily. The maintenance dose is 10 mg twice daily.

How to take if you have kidney problems? In this situation, take 2.5 mg per day. The maintenance dose is usually 5-10 mg. The maximum dose is 20 mg per day.

Instructions for use Enalapril Acri

Anytime. Initially, take 2.5–5 mg once every 24 hours. The maintenance dose is 10–20 mg once every 24 hours. The maximum dose is 40 mg in 1–2 doses.

Instructions for Enalapril FPO

Similar to the dosage method of the previous drug.

Enalapril N dosage regimen

1-2 tablets every 24 hours, regardless of meals.

Overdose

Excessive drop in blood pressure, myocardial infarction , stroke, thromboembolic complications as a consequence of a sharp decrease in blood pressure. Treatment: intravenous administration of NaCl (isotonic solution). There is no specific antidote.

Interaction

Absorption of the drug does not depend on food intake. When taken simultaneously with beta-adrenergic blockers, nitrates , methyldopa, calcium antagonists, , hydralazines Enalapril potentiates the hypotensive effect. Cimetidine increases T1/2 of the drug. NSAIDs increase nephrotoxicity, reduce the effectiveness of Enalapril. Potassium supplements and potassium-sparing diuretics when taken with drugs lead to hyperkalemia. Enalapril reduces the half-life theophylline , reduces lithium clearance. LS does not interact with cardiac glycosides .

Terms of sale

Requires a prescription.

Storage conditions

At temperatures up to 25 degrees Celsius in a dry place out of reach of children.

Best before date

No more than 3 years.

special instructions

In the first hours of taking Enalapril can lead to a pronounced decrease in blood pressure. This is especially evident in people taking an antihypertensive drug for the first time, in patients with chronic renal failure, severe heart failure, hypovolemia, and hyponatremia. To prevent a sharp decrease in blood pressure, the salt-free diet is also canceled 2-3 days before taking Enalapril. If angioedema develops on the face and neck, it is necessary to stop taking medications and prescribe antihistamines. In severe cases, intubation and tracheotomy are performed. It is not recommended to prescribe potassium-sparing diuretics at the same time. Regular monitoring is required hemostasis. Enalapril is not prescribed to women planning pregnancy.

The medicine is registered by WHO according to the Vidal reference book.

Often used with hydrochlorothiazide as a combination drug.

Recipe in Latin: Tab. Enalaprili 0.01

INN: Enalapril.

Enalapril's analogs

Lisinopril or Enalapril - which is better?

Based on research, lisinopril lowers blood pressure more effectively and also lasts for a longer period of time. Both drugs are tolerated approximately equally.

Enap and Enalapril - what is the difference?

In fact, the drugs are no different, since they have the same active substance. However, the price of Enap is much higher than its analogue.

Enalapril and Enalapril Hexal

The drug is also produced by Hexal, which is why it has the corresponding addition in the name.

Reviews of Enalapril

Reviews from doctors boil down to the fact that this is a very effective, widely used, high-quality drug for blocking ACE. It does reduce blood pressure, however, it has a number of contraindications and side effects, for example, cough.

Reviews about Enalapril Hexal on forums are generally also positive. The drug effectively lowers blood pressure, is inexpensive, but has frequent side effects.

Enalapril price, where to buy

The medicine is sold for 15-20 rubles.

How much does Enalapril 10 mg cost? About 15 rubles.

The price of Enalapril Hexal is 85 rubles per pack of 20 pieces of 20 mg.

• Online pharmacies in Russia Russia
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Enalapril tablets 10 mg No. 20 Organic JSC Organika

Enalapril tab. 20 mg No. 20JSC Obolenskoe farm. company

Enalapril hexal tab. 10mg n20 Salutas Pharma GmbH

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Enalapril-hexal 5 mg No. 20 tabletSalutas Pharma GmbH.

Enalapril-hexal 20 mg No. 20 tabletSalutas Pharma GmbH

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Drugs belonging to the group of angiotensin-converting enzyme inhibitors began to be widely used in medical practice more than 40 years ago and to this day are one of the most effective means for combating arterial hypertension. A widely used member of this group is Enalapril. Instructions for use of Enalapril include a detailed description of the indications, contraindications, method of use of the medicine, its side effects and other features of use.

Description and clinical properties

Enalapril is produced in the form of tablets for oral use. Externally, the tablets have a white or grayish tint and are available in dosages of 5, 10 and 20 mg. The product is packaged in blisters. The cardboard package contains 2-3 plates.

The main active ingredient of the drug is enalapril maleate. Its concentration in one tablet depends on the form of production and is 0.005, 0.01 and 0.02 g, respectively.

Indications for use

Instructions for use of Enalapril include rather limited indications for use. This is explained by the specific and rather strong effect of the drug, as well as a large list of side effects and contraindications.

In medical practice, the drug is prescribed to patients for the following conditions:

• various stages of hypertensive heart disease. The strength of the drug is adjusted by decreasing or increasing the dosage individually for each patient;
• arterial hypertension of various etiologies. Many years of experience show that Enalapril is one of the most effective means in the fight against high blood pressure;
• chronic heart failure, as well as severe forms of pathology, in particular during the recovery period after a myocardial infarction to restore the functioning of the left ventricle of the heart;
• heart failure accompanied by congestive processes;
• Enalapril is used as a complex treatment for bronchospastic conditions;
• treatment of left ventricular dysfunction occurring in a latent form;
• IHD, accompanied by attacks of angina and other manifestations.

Mode of application

How to take Enalapril? The tablets are intended for oral use, that is, ingestion. The drug should be washed down only with clean water, since in combination with juices, tea, coffee and other drinks, the drug sometimes has a negative effect.

To achieve faster results, the tablet can be placed under the tongue and held until completely dissolved. Typically, this method is indicated for patients with a hypertensive crisis to quickly reduce blood pressure.

How long does it take for the product to work?

The therapeutic effect of Enalapril occurs approximately 60 minutes after administration. It is during this period that the highest concentration of the active component of the drug in the blood is observed.

The duration of the hypotensive effect is about 24 hours. The duration of action of the drug increases in patients with heart failure, as well as in patients with kidney and liver diseases.

The effect of the medicine is enhanced when taken twice. In most cases, the initial dose is 5 mg and is increased gradually if the drug is well tolerated.

How long does the medication last? The half-life is up to 5 hours. After this, the effect of Enalapril decreases slightly.

The therapeutic effect of the drug is enhanced when used simultaneously with calcium antagonists and thiazide diuretics.

How many times a day

The number of doses and dosage of the medication is determined by the leading physician based on the patient’s medical history and complaints. Enalapril is usually prescribed as monotherapy at 10–20 mg twice a day.

For complex treatment of one or another condition, the doctor prescribes 1 tablet in the morning or evening. The duration of treatment is individual for each patient.

Take before or after meals

The instructions for use of Enalapril N and other brands of medicine do not indicate clear restrictions on taking tablets before or after meals. The drug can be taken both before and after meals. This has virtually no effect on the therapeutic effect of the drug.

At what pressure

Many patients are interested in what pressure should they take the drug? The use of Enalapril is indicated for patients with even a slight increase in blood pressure against the background of essential hypertension, since this leads to impaired blood circulation in the brain and heart muscle.

For hypertension, it is recommended to take Enalapril when the mercury level rises above 120/90.

If a person’s working pressure is 100/60, the product is used when the readings increase to 120/90.

Dosage of the drug

The annotation for Enalopril indicates that the drug is taken before, after or during meals in the dosage prescribed by the doctor depending on the diagnosis. Treatment with the drug is carried out both as independent and complex therapy.

Self-therapy

At the initial stages of treatment, patients are usually prescribed ¼ tablet of 20 mg. If there is no effect within 7–14 days and the pressure does not decrease to normal levels, the dosage is gradually increased. In this case, the daily dose should not exceed 40 mg of the drug.

Complex treatment

In the treatment of heart failure and other conditions as a means of complex therapy, Enalapril is prescribed 2.5 mg once a day. The dosage of the drug is gradually increased, but not more than 2–2.5 mg every 7 days.

For chronic heart failure, the dosage is 2.5 mg in the first stages. The rate increases gradually, once a week by 2–2.5 mg.

For renovascular type hypertension, the daily dose of the drug cannot exceed 20 mg. At the initial stage, the patient is advised to take ¼ tablet twice a day.

Alcohol compatibility

Combining Enalapril and alcohol is prohibited in any dosage. This effect can cause a number of serious complications that are dangerous to the health and life of the patient. The fact is that while drinking alcohol, the effect of the drug may increase, which will lead to a severe form of arterial hypotension.

The compatibility of Enalapril and alcohol is extremely undesirable for patients suffering from kidney and liver diseases. Negative consequences include persistent hypotension, disorders of the central nervous, respiratory, and cardiovascular systems.

In addition, strong drinks increase the risk and intensity of possible side effects of the drug. The patient may experience severe headaches, nausea, dizziness and other unpleasant symptoms.

If kidney function is impaired

In case of severe kidney pathologies, the drug is completely contraindicated. Using the product can lead to dangerous complications that are incompatible with life.

For moderate organ dysfunction, Enalapril can be used in an initial dosage of 2.5 mg per day. The maximum amount of medication should not exceed 20 mg throughout the day.

In case of severe kidney dysfunction, the patient is prescribed the drug at a dosage of 2.5 mg per day, the permissible daily amount of the drug does not exceed 10 mg.

If the renal artery is narrowed unilaterally or bilaterally, Enalapril is not used.

In case of liver dysfunction

Liver diseases are a direct contraindication to the use of Enalapril. In extremely rare cases, a specialist may decide to prescribe the drug in limited doses if other medications do not provide the desired therapeutic effect.

Prescription in old age

For elderly patients, the drug is prescribed after a complete examination in a hospital setting. In this case, it is necessary to monitor the dynamics of blood pressure, urine and blood tests.

The initial dosage for patients over 65 years of age should be 2.5 mg. No more than 10 mg of the drug is allowed per day.

Use during pregnancy and lactation

The instructions for use state that during pregnancy and breastfeeding, treatment with Enalapril is strictly contraindicated. If the need to take the drug does arise, the babies of such mothers should be under close medical supervision and undergo regular tests.

Impact on the ability to control complex mechanisms

Patients undergoing treatment with Enalapril should be careful when engaging in work activities that require increased concentration and rapid mental and physical reactions. In some cases, the development of individual reactions of the body is possible, in particular, after taking large doses or combining the drug with alcohol.

Prescription in childhood

There is no data on the safety of the drug among children under 18 years of age, so in pediatrics the drug is used only when absolutely necessary in emergency situations.

Drug interactions

When including Enalapril in a prescription, the specialist must take into account its interaction with other drugs:

• the hypotensive effect of the drug decreases when combined with analgesics and non-steroidal anti-inflammatory drugs;
• in combination with diuretic tablets, the vasodilating effect of Enalapril is enhanced;
• vitamin complexes, including potassium, potassium-sparing diuretics, when used simultaneously with Enalapril, increase the risk of excess potassium in the body - hyperkalemia;
• agents including sodium chloride reduce the hypotensive effect of the drug;
• the antihypertensive effect is enhanced when the drug is combined with narcotic drugs used for anesthesia;
• when taking drugs containing insulin, their hypoglycemic effect increases against the background of Enalapril;
• Cases of leukopenia have been reported when the described drug is combined with cytostatics, immunosuppressants, and some hormones.

Conditions for storage and sale from pharmacies

When purchasing Enalapril at a pharmacy, you must present a prescription. The medicine should be stored in places protected from children at a temperature not exceeding 25 degrees. Shelf life from the date of production is 3 years. After this period, using the product is strictly not recommended.

Use of Bisoprolol for hypertension

Bisoprolol, a selective β-adrenergic blocker, was discovered in 1967, but even compared to today’s analogues, it stands out for its high selectivity and potency of action. Treating hypertension or angina with this drug provides significant benefits to patients.

In a comparative analysis of the effects of Bisoprolol and similar β-blockers, they equally quickly reduced blood pressure. But when monitoring it daily, it turned out that only Bisoprolol maintained its performance the next morning. At the same time, it was possible to normalize blood pressure not only at rest, but also during exercise. The stability and uniform effect of a single tablet throughout the day have provided Bisoprolol with well-deserved popularity.

Pharmacology of Bisoprolol - mechanism of action

The drug has hypotensive (lowers blood pressure), antiarrhythmic (normalizes heart rate) and antianginal (reduces symptoms of coronary artery disease) effects. The therapeutic dosage does not have intrinsic symptomatic activity and does not have significant membrane-stabilizing capabilities.

Under the influence of minimal doses of the drug (active substance - bisoprolol fumarate):

With an increase in dosage, significantly exceeding the norm (from 0.2 g), as indicated in the annotation, the drug can cause blockade of β 2-adrenergic receptors of the bronchi and smooth muscles of the vascular walls. Immediately after use, cardiac output decreases.

The therapeutic dosage does not have a cardiodepressive effect, does not affect the body's absorption of glucose, and does not retain sodium. The maximum effect appears 1-3 hours after consumption and lasts 24 hours.

The active component binds to blood molecules by 30%. To some extent, Bisoprolol fumarate can cross the placenta of the fetus. Partially passes into breast milk.

Forms of release of the drug

Photo: to enlarge, click on the description of release forms.

Pharmacokinetics: composition and principle of action

Each Bisoprolol tablet includes 0.005 or 0.01 g of bisoprolol fumarate and several excipients in the form of magnesium stearate, silicon dioxide, crospovidone, starch and cellulose. In the drug Bisoprolol, the composition of the shell covering the capsule is alcohol, macrogol, talc, titanium dioxide and several yellow dyes.

Bisoprolol is available in the form of round beige and yellow tablets of 20, 30 or 50 pieces in each package.

The drug is absorbed by 90% regardless of food, half of it is transformed in the liver, 98% is excreted by the kidneys, the remainder is eliminated in bile.

Bisoprolol: indications for use

Bisoprolol tablets: what do they really help with? Among the common indications:

• Hypertension (persistently high blood pressure);
• Angina pectoris (IHD);
• Heart failure (in combination with other medications).

Bisoprolol is prescribed with particular care:

1. For psoriasis and anyone who has a family history of patients diagnosed with psoriasis.
2. For diabetes mellitus (stage of decompensation).
3. With a predisposition to allergies.
4. Patients whose profession involves a high reaction rate or may threaten their health. At the first stage of treatment, the speed of psychomotor reactions decreases. A similar effect is observed under the influence of alcohol, since the drug Bisoprolol and alcohol have poor compatibility.

For patients diagnosed with pheochromocytoma, Bisoprolol is prescribed after completion of a course of α-blocker therapy.

Bisoprolol during pregnancy

In general, the medication is not recommended for use by pregnant or nursing mothers. An exception may be in a situation where the effectiveness of Bisoprolol for the mother exceeds the expected risk for the child. If a pregnant woman nevertheless undergoes a course of therapy with Bisoprolol, the drug is discontinued no later than three days before giving birth.

If this condition is not met, the newborn runs the risk of acquiring a bunch of diseases - hypotension, hypoglycemia, bradycardia, hypoxia. If health indications do not allow stopping Bisoprolol, the condition of the newborn must be constantly monitored during the first week of life.

Contraindications for use

Bisoprolol is not prescribed if the patient suffers from:

• Hypersensitivity to any ingredient in the composition;
• Acute or chronic form of cardiac pathology, when inotropic therapy is performed;
• Cardiogenic shock;
• Weakening of the sinus node;
• Neoplasms in the lungs;
• Sinoatrial block;
• Severe bradycardia;
• AV blockade 2 and 3 stages;
• Severe stage of arterial hypertension with systolic blood pressure limits up to 100 mm Hg. Art.;
• Uncompensated diabetes mellitus;
• Pheochromocytoma (if α-blockers are prescribed in parallel);
• Bronchial asthma in severe form;
• Metabolic acidosis;
• Impaired peripheral blood flow;
• Refractory hypokalemia, hypercalciemia or hyponatremia;
• Hypolactasia;
• Lactose intolerance (the drug contains lactose).

No studies have been conducted on the effectiveness of the drug in minors. Do not use the drug in patients who are prescribed a course of therapy with MAO inhibitors (with the exception of parallel use with B-type monoamine oxidase inhibitors).

Side effects

Bisoprolol: what should you protect against? The annotation also states some undesirable manifestations in the form of:

• Headache and loss of coordination;
• Feelings of fatigue, loss of strength;
• A sharp flow of blood to the head, redness of the face;
• Insomnia;
• Mental disorders of depressive and hallucinogenic type;
• Paresthesia of the arms and legs, sensations of cold extremities;
• Reduced secretion of the lacrimal glands;
• Developing conjunctivitis;
• Abdominal pain, nausea and vomiting;
• Intestinal disorders;
• Muscle weakness;
• Frequent seizures;
• Orthostatic hypotension;
• Signs of bronchial obstruction (if there is a predisposition);
• Increased sweating;
• Slow heartbeat;
• AV conduction disorders.

A decrease in glucose tolerance is possible (most often in patients diagnosed with diabetes mellitus, including its latent form, which usually does not manifest itself). The product gives a positive reaction during doping control. Bisoprolol exhibits side effects in rare cases; the instructions warn, first of all, doctors to clarify the dosage and compatibility.

Bisoprolol: instructions for use

The medicine is intended for oral use. Take it in the morning, before breakfast or during meals. Swallow whole and wash down with water. The daily norm for an adult is 20 mg. If there are no special instructions, for patients with hypertension or patients with angina pectoris, 10 mg of the drug for a single dose is enough.

At the very beginning of the course, you can limit yourself to a more moderate dose - 5 mg / day. Exceeding the norm is possible only in the most extreme cases. When the daily intake increases, the rules of admission remain the same. The standard treatment regimen with Bisoprolol tablets according to the instructions is presented in the table.

An individual treatment regimen is drawn up by the therapist, taking into account pulse indicators and the body’s reaction. Patients with minor dysfunction of the kidneys, adrenal glands or liver, as well as adults, do not need to adjust the dose. In severe forms of the listed pathologies, the daily dose is limited to 10 mg of the drug. The medicine is designed for long-term use. Will the drug really help control blood pressure over many years?

Bisoprolol is produced by many pharmaceutical companies, but the origin of the medicine does not affect the regimen of use. Bisoprolol-Prana has instructions identical to analogues from the Lugansk Chemical Plant or the Israeli company Teva.

Overdose

Overdose manifests itself as:

• Pronounced bradycardia;
• Arrhythmias;
• Ventricular extrasystoles;
• AV block;
• Significant drop in blood pressure;
• Heart failure;
• Cyanosis (blue discoloration) of the hands;
• Shortness of breath;
• Dizziness;
• Bronchospasms;
• Syncope;
• Convulsive attacks.

When treating the consequences of an overdose, gastric lavage is performed, adsorbent drugs and symptomatic therapy are prescribed:

1. Atropine or epinephrine (1-2 g intravenously) for AV block. Sometimes the problem is solved by installing a temporary pacemaker.
2. For ventricular extrasystole - lidocaine (intravenously). In parallel, class IA medications are not used.
3. When blood pressure drops, the patient is moved to the Trendelenburg position (head and shoulders below the level of the pelvis by 30-45º).
4. Plasma replacement solutions are injected into a vein if symptoms of pulmonary edema do not appear. If there is a further drop in blood pressure, epinephrine and dobutamine are added if there is insufficient effectiveness.
5. Cardiac glycosides, diuretics, glucagon.
6. Diazepam is injected into a vein to relieve seizures.
7. Inhalation of β-adrenergic stimulants for bronchospasm.

This convincing list once again proves that before taking Bisoprolol, it is important not only to study the instructions, but also to agree on the dosage with the doctor.

Bisoprolol is absolutely incompatible with Floctafenine and Sultopride. It is not recommended to combine it with calcium antagonists, antihypertensive drugs, and MAO inhibitors. Bisoprolol and drugs should be combined with caution:

• Against arrhythmia;
• Calcium antagonists;
• Anticholinesterase agents and local β-blockers;
• Insulin-based drugs and other medications for diabetics;
• β-sympathomimetics, which can enhance the activity of α- and β-adrenergic receptors;
• Cardiac glycosides (based on digitalis);
• Ergotamine derivatives;
• Pain relievers;
• Anti-inflammatory non-steroidal drugs;
• Antihypertensive medications that increase the likelihood of hypotension (antidepressants, barbiturates);
• Baclofen;
• Amifostine;
• Parasympathomimetics.

Normal interaction of Bisoprolol with Mefloquine and corticosteroids was noted.

Terms of sale and storage

Bisoprolol, a medicine, is sold in pharmacies only with a prescription written in Latin: “Rp.: Tab. Bisoprololi 0.005 No. 20. D.S. 1 tab. per day (AH, IHD).”

While the instructions for use are the same for any of the representatives of Bisoprolol, the price of the drug is different for each manufacturer: for example, Bisoprolol-Ratiopharm (0.005 g) can be purchased in Russian pharmacies for 350 rubles, a similar package of generic Bisoprolol-Prana costs from 32 rubles.

The drug is listed in class B. It is recommended to store it at temperatures up to 25º C in a dry and dark room, out of reach of children. The period of safe use is 36 months.

Analogues of Bisoprolol

Structural analogues of Bisoprolol include the medications Bisogamma, Biprol, Bisoprolol-Prana, Niperten, Bisoprolol-Ratiopharm, Bisoprolol-Teva, Bisoprolol-Lugal, Concor, Bisomor, Concor Cor, Corbis, Aritel Cor, Bioscard, Bidop, Bisomore.

The drugs Atenolol, Betalok, Betacard, Nebilet, Binelol, Lokren, Egilok, Metocor, Kordanum, Lidalok, Metoprolol, Metozok, Nebivator, Nebilong, OD-Neb, Estekor have a similar mechanism of therapeutic effect.

The question is often discussed on forums: which medicine is better - Bisoprolol or Concor?

Concor is the name of the brand under which the original Bisoprolol is produced. Manufacturer: Merck KGaA from Germany. Unfortunately, the patent for the drug Bisoprolol Concor has already expired, so on our market today you can find many alternative options - generics of Bisoprolol, quite effective substitutes that are affordable.

Benefits of Bisoprolol

Compared to similar beta blockers, Bisoprolol has a number of advantages:

1. For effective blood pressure control, 1 tablet of the drug per day is enough - it remains active both day and night.
2. The product works both when taken on an empty stomach and after taking it with meals.
3. The drug has high selectivity. Compared to the previous generation of β-blockers, this provides it with a lower percentage of side effects.
4. The medicine does not have a negative effect on men's health. The findings come from a placebo-controlled study in which the control group was not told which drug they were given.
5. Bisoprolol is a metabolically neutral agent that does not worsen metabolic processes (cholesterol, triglycerides and blood glucose).
6. The drug is available to patients with type 2 diabetes and members of the risk group for this disease.
7. The medicine is constantly prescribed even in adulthood, since the likelihood of side effects is less than that of its analogues.
8. The pharmaceutical market is full of generics of Bisoprolol - analogues that are produced by many competing companies. This makes the treatment not only effective, but also financially accessible, since the price of the artificial medicine Bisoprolol is much lower.

Bisoprolol: patient reviews

Bisoprolol is quite popular on thematic forums. Bisoprolol tablets are discussed most often; reviews relate to the duration of treatment and its discontinuation. Upon abrupt cessation of drug use, many experience withdrawal symptoms.

Its main manifestations are attacks of hypertension, increased heart rate. Some patients experienced noticeable loss of vision during treatment. But since treatment with the drug is very long-term, and for some, lifelong, all the described symptoms may not be related to the use of Bisoprolol. The risk of side effects is quite real: some users did not notice any obvious violations, while for others they were noticeable.

Summarizing all the opinions, we can come to the conclusion that self-medication with such a serious drug as Bisoprolol can be extremely dangerous. If you don't get the dose right, you can get a bunch of side effects, including cardiac arrest. The prescription, treatment regimen and time of drug withdrawal should be solely within the competence of physicians.