Amprilan application. Impact on the ability to operate machinery

Composition and release form of the drug

Pills white or almost white, oval, flat, chamfered.

Excipients: sodium carbonate, lactose monohydrate, croscarmellose sodium, pregelatinized starch, sodium stearyl fumarate.

10 pcs. - blisters (3) - cardboard packs.

Pharmacological action

ACE inhibitor. It is a prodrug from which the active metabolite ramiprilat is formed in the body. It is believed that the mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I to angiotensin II, which is a powerful vasoconstrictor. As a result of a decrease in the concentration of angiotensin II, a secondary increase in renin activity occurs due to the elimination of negative feedback upon the release of renin and direct reduction aldosterone secretion. Thanks to its vasodilating effect, it reduces roundabout percentage (afterload), wedge pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases cardiac output and exercise tolerance.

In patients with signs of chronic heart failure after myocardial infarction, ramipril reduces the risk sudden death, progression of heart failure to severe/resistant heart failure and reduces hospitalizations for heart failure.

Ramipril is known to significantly reduce the incidence of myocardial infarction, stroke and cardiovascular death in patients with increased cardiovascular risk due to vascular diseases(CHD, previous stroke or peripheral vascular disease) or diabetes mellitus with at least one additional factor risk (microalbuminuria, arterial hypertension, increased levels total cholesterol, low level HDL, smoking). Reduces overall mortality and the need for revascularization procedures, slows the onset and progression of chronic heart failure. As in patients with diabetes mellitus, and without it, ramipril significantly reduces existing microalbuminuria and the risk of developing nephropathy. These effects are observed in patients with both high and normal blood pressure.

The hypotensive effect of ramipril develops after approximately 1-2 hours, reaches a maximum within 3-6 hours, and lasts for at least 24 hours.

Pharmacokinetics

When taken orally, absorption is 50-60%; food does not affect the degree of absorption, but slows down absorption. Cmax is reached after 2-4 hours. It is metabolized in the liver to form the active metabolite ramiprilat (6 times more active in inhibiting ACE than ramipril), inactive diketopiperazine and glucuronidated. All metabolites formed, with the exception of ramiprilat, pharmacological activity don't have. Plasma protein binding for ramipril is 73%, ramiprilat is 56%. Bioavailability after oral administration of 2.5-5 mg of ramipril is 15-28%; for ramiprilat - 45%. After daily intake ramipril at a dose of 5 mg/day, a steady-state concentration of ramiprilat in plasma is achieved by day 4.

T1/2 for ramipril - 5.1 hours; in the distribution and elimination phase, a drop in the concentration of ramiprilat in the blood serum occurs with T 1/2 - 3 hours, followed by a transition phase with T 1/2 - 15 hours, and a long final phase with very low concentrations of ramiprilat in plasma and T 1/2 - 4-5 days. T1/2 increases in chronic renal failure. V d ramipril - 90 l, ramiprilat - 500 l. 60% is excreted by the kidneys, 40% is excreted through the intestines (mainly in the form of metabolites). If renal function is impaired, the excretion of ramipril and its metabolites slows down in proportion to the decrease in CC; if liver function is impaired, the conversion to ramiprilat slows down; in heart failure, the concentration of ramiprilat increases by 1.5-1.8 times.

Indications

Arterial hypertension; chronic failure; heart failure that developed in the first few days after acute heart attack myocardium; diabetic and non-diabetic nephropathy; reducing the risk of myocardial infarction, stroke and cardiovascular mortality in patients with high cardiovascular risk, including patients with confirmed coronary artery disease (with or without a history of infarction), patients who underwent percutaneous transluminal coronary angioplasty, coronary bypass surgery, with a history of stroke and patients with occlusive lesions peripheral arteries.

Contraindications

Severe renal and liver dysfunction, bilateral stenosis renal arteries or stenosis of the artery of a single kidney; condition after kidney transplantation; primary hyperaldosteronism, hyperkalemia, aortic stenosis, pregnancy, lactation ( breast-feeding), children's and adolescence under 18 years of age, hypersensitivity to ramipril and other ACE inhibitors.

Dosage

Taken orally. The initial dose is 1.25-2.5 mg 1-2 times/day. If necessary, a gradual increase in dose is possible. The maintenance dose is set individually, depending on the indications for use and the effectiveness of treatment.

Side effects

From the outside cardiovascular system: arterial hypotension; rarely - chest pain, tachycardia.

From the side of the central nervous system: dizziness, weakness, headache; rarely - sleep disturbances, mood disorders.

From the digestive system: diarrhea, constipation, loss of appetite; rarely - stomatitis, pancreatitis, cholestatic jaundice.

From the outside respiratory system: dry cough, bronchitis, sinusitis.

From the side of urine excretory system: rarely - proteinuria, increased concentrations of creatinine and urea in the blood (mainly in patients with impaired renal function).

From the hematopoietic system: rarely - neutropenia, agranulocytosis, thrombocytopenia, anemia.

From the laboratory parameters: hypokalemia, hyponatremia.

Allergic reactions: skin rash, angioedema and other hypersensitivity reactions.

Others: rarely - muscle spasms, impotence, alopecia.

Drug interactions

At simultaneous use Potassium-sparing diuretics (including triamterene, amiloride), potassium preparations, salt substitutes and dietary supplements containing potassium may develop hyperkalemia (especially in patients with impaired renal function), because ACE inhibitors reduce the content of aldosterone, which leads to potassium retention in the body while limiting the excretion of potassium or its additional intake into the body.

When used simultaneously with NSAIDs, the hypotensive effect of ramipril may be reduced and renal function may be impaired.

When used simultaneously with loop or thiazide diuretics, the antihypertensive effect is enhanced. Severe arterial hypotension, especially after taking the first dose of a diuretic, appears to occur due to hypovolemia, which leads to a transient increase in the hypotensive effect of ramipril. There is a risk of developing hypokalemia. The risk of kidney dysfunction increases.

When used simultaneously with agents that have hypotensive effect, the hypotensive effect may be enhanced.

When used simultaneously with insulin, hypoglycemic agents, sulfonylurea derivatives, and metformin, hypoglycemia may develop.

When used simultaneously with cystostatics, immunosuppressants, procainamide, the risk of developing leukopenia may increase.

When used simultaneously with lithium carbonate, it is possible to increase the concentration of lithium in the blood serum.

Special instructions

In patients with concomitant renal impairment, doses are selected individually in accordance with CC values. Before starting treatment, all patients must undergo a kidney function test. During treatment with ramipril, renal function, blood electrolyte composition, levels of liver enzymes in the blood, as well as blood patterns are regularly monitored. peripheral blood(especially in patients with diffuse diseases connective tissue, in patients receiving , allopurinol). Patients who have fluid and/or sodium deficiency must have their fluid and electrolyte imbalances corrected before starting treatment. During treatment with ramipril, hemodialysis should not be performed using polyacrylonitrile membranes (the risk of anaphylactic reactions is increased).

For liver dysfunction

Contraindicated in cases of severe liver dysfunction.

KRKA KRKA d.d. KRKA, d.d., Novo mesto KRKA, d.d., Novo mesto, JSC

Country of origin

Slovakia Slovenia

Product group

Cardiovascular drugs

Angiotensin-converting enzyme inhibitor

Release forms

• pack of 30 tablets pack of 30 tablets

Description of the dosage form

• Tablets 1.25 mg tablets are oval, flat, white or almost white tablets with a bevel. Pills

Pharmacological action

amipril is a prodrug that is metabolized after absorption into ramiprilat in the liver. Ramipril is a long-acting angiotensin-converting enzyme (ACE) inhibitor. ACE catalyzes the conversion of angiotensin I to α-angiotensin II. ACE is identical to kinase, an enzyme that catalyzes the breakdown of bradykinin. ACE blockade leads to a decrease in the concentration of angiotensin II, an increase in renin activity in the blood plasma, an increase in the effect of bradykinin and an increase in the secretion of aldosterone, which may cause an increase in the level of potassium in the blood serum. The antihypertensive and hemodynamic effects of ramipril in patients with arterial hypertension are the result of dilation of resistive vessels and a decrease in total peripheral resistance, which in turn gradually reduces blood pressure (BP). Heart rate usually does not change. At long-term treatment left ventricular hypertrophy decreases without negative influence on heart function. The hypotensive effect of a single dose appears 1-2 hours after administration, reaches a maximum after 3-6 hours and lasts 24 hours. Ramipril is also effective for the treatment of chronic heart failure. In patients with signs of chronic heart failure after myocardial infarction, the drug reduces the risk of sudden death, progression of heart failure to severe/resistant heart failure and reduces the number of hospitalizations for heart failure. According to the literature, ramipril significantly reduces the incidence of myocardial infarction, stroke and cardiovascular death in patients with increased cardiovascular risk due to vascular disease (such as coronary heart disease, previous stroke or peripheral vascular disease) or diabetes mellitus who have at least one additional risk factor (microalbuminuria, arterial hypertension, increased total cholesterol, low lipoprotein levels high density, smoking). The drug also reduces overall mortality and the need for revascularization procedures, and slows the onset and progression of chronic heart failure. In both patients with and without diabetes mellitus, the drug significantly reduces existing microalbuminuria and the risk of developing nephropathy. These effects are observed in patients with both high and normal blood pressure.

Pharmacokinetics

After oral administration, ramipril is rapidly absorbed from gastrointestinal tract 50-60% of the drug, food intake does not slow down absorption. The maximum concentration in blood serum is reached after 1 hour. Ramipril is metabolized in the liver to form an active metabolite - ramiprilat, the activity of which is 6 times higher than ramipril and inactive diketopiperazine, which is then glucuronidated. The maximum concentration of ramiprilat in the blood serum is achieved 2-4 hours after administration, the equilibrium concentration is achieved by the 4th day of taking the drug. About 73% of ramipril and 56% of ramiprilat are bound to plasma proteins. Ramipril and ramiprilat are excreted from the body mainly in the urine (about -60%), mainly in the form of metabolites, less than 2% of the dose taken is excreted as unchanged ramipril. Ramipril is eliminated in several stages. The half-life after administration of a therapeutic dose is 13-17 hours for ramiprilat, 5.1 hours for ramipril. Animal studies have not revealed secretion of the drug into milk. Studies conducted in healthy volunteers aged 65 to 76 years showed that the pharmacokinetics of ramipril in them did not differ from the pharmacokinetics in young healthy volunteers. If renal function is impaired, the elimination of ramipril and its metabolites slows down in proportion to the decrease in creatinine clearance. In patients with liver failure the metabolism of ramipril to ramiprilat may be slowed and ramipril serum concentrations may be increased.

Special conditions

Ramipril Renal function should be assessed at the start of treatment. It is necessary to carefully monitor renal function during treatment with ramipril, especially in patients with weakened renal function, with damage to the renal vessels (for example, clinically insignificant renal artery stenosis or hemodynamically significant stenosis of the artery of a solitary kidney); heart failure. Risk hypersensitivity and allergy-like (anaphylactoid) reactions are increased in patients concomitantly taking ACE inhibitors and undergoing hemodialysis procedures using AN 69 dialysis membranes. Similar reactions have been identified with LDL apheresis using dextran sulfate, therefore the use of ACE inhibitors should be avoided this method. During treatment with ramipril in patients with impaired renal function, especially simultaneous treatment diuretics, the level of urea and creatinine in the blood serum may increase. In this case, treatment should be continued with lower doses of ramipril or the drug should be discontinued. In patients with impaired renal function, the risk of hyperkalemia increases. In patients with impaired liver function due to a decrease in the activity of liver enzymes, the metabolism of ramipril and the formation of an active metabolite may be slowed down. In this regard, treatment of such patients should be started only under strict medical supervision. Caution must be exercised when prescribing ramipril to patients on low-salt or salt-free diet (increased risk development of arterial hypotension). In patients with reduced blood volume (as a result of diuretic therapy), symptomatic hypotension may develop during dialysis, with diarrhea and vomiting. Transient arterial hypotension is not a contraindication for continuing treatment after stabilization of blood pressure. If severe arterial hypotension reoccurs, the dose should be reduced or the drug discontinued. In patients undergoing major surgery or receiving other drugs that cause hypotension during general anesthesia, ramipril may cause a blockade of angiotensin II formation due to compensatory release of renin. If the physician associates the development of arterial hypotension with the mechanism mentioned above, arterial hypotension can be corrected by increasing blood plasma volume. IN in rare cases During treatment with ACE inhibitors, agranulocytosis, erythrocytopenia, thrombocytopenia, hemoglobinemia or depression are observed bone marrow. At the beginning and during treatment, it is necessary to monitor the number of white blood cells to detect possible neutropenia/agranulocytosis. More frequent monitoring is recommended in patients with renal failure, with connective tissue diseases (including SLE or scleroderma) and in patients taking concomitant medicines, affecting hematopoiesis.

Compound

• ramipril 1.25 mg Excipients: sodium bicarbonate 1.25 mg, lactose monohydrate 79.50 mg mg, croscarmellose sodium 2.00 mg, pregelatinized starch 15.00 mg mg, sodium stearyl fumarate 1.00 mg mg, dye mixture PB 22886 yellow* -/ 4.00 ramipril 1.25 mg Excipients: sodium bicarbonate, lactose monohydrate, croscarmellose sodium, pregelatinized starch, sodium stearyl fumarate. ramipril 10 mg Excipients: sodium bicarbonate, lactose monohydrate, croscarmellose sodium, pregelatinized starch, sodium stearyl fumarate. ramipril 2.5 mg Excipients: sodium bicarbonate, lactose monohydrate, croscarmellose sodium, pregelatinized starch, sodium stearyl fumarate, yellow iron oxide (E172 ramipril 2.5 mg hydrochlorothiazide 12.5 mg Excipients: sodium bicarbonate, lactose monohydrate, croscarmellose sodium, pregelatinized starch ( starch 1500) , sodium stearyl fumarate ramipril 5 mg Excipients: sodium bicarbonate, lactose monohydrate, croscarmellose sodium, pregelatinized starch, sodium stearyl fumarate, red iron oxide (E172 ramipril 5 mg hydrochlorothiazide 25 mg Excipients: sodium bicarbonate, lactose monohydrate, croscarmellose sodium, starch isolated ( starch 1500), sodium stearyl fumarate.

Amprilan indications for use

• Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs, for example, diuretics and slow blockers calcium channels). Chronic heart failure (as part of combination therapy, in particular, in combination with diuretics). Diabetic nephropathy or non-diabetic nephropathy, preclinical and clinically pronounced stages, including with severe proteinuria, especially when combined with arterial hypertension. Reducing the risk of myocardial infarction, stroke or cardiovascular mortality in patients with high cardiovascular risk: - in patients with confirmed coronary disease heart, with or without a history of myocardial infarction, including patients who have undergone percutaneous transluminal coronary angioplasty, coronary artery bypass surgery; - in patients with a history of stroke; - in patients with a history of occlusive lesions of peripheral arteries; - in patients with diabetes mellitus with NS less than one

Amprilan contraindications

• - history of angioedema (including those associated with previous therapy with ACE inhibitors); - hemodynamically significant bilateral renal artery stenosis; - stenosis of the artery of the only kidney; - condition after kidney transplantation; - hemodialysis; - renal failure (KR

Amprilan dosage

• 1.25 1.25 mg 10 mg 2.5 mg 2.5 mg + 12.5 mg 5 mg 5 mg+25 mg

Amprilan side effects

• Ramipril From the cardiovascular system: decreased blood pressure, orthostatic hypotension, orthostatic collapse, tachycardia; rarely - arrhythmia, palpitations, exacerbation of Raynaud's syndrome. With an excessive decrease in blood pressure, mainly in patients with coronary artery disease and clinically significant narrowing of cerebral vessels, myocardial ischemia (angina pectoris, myocardial infarction) and cerebral ischemia (possibly with dynamic impairment) may develop. cerebral circulation or stroke). From the outside digestive system: nausea, vomiting, diarrhea or constipation, pain in epigastric region, intestinal obstruction, flatulence, pancreatitis, hepatitis, cholestatic jaundice, cholecystitis (in the presence of cholelithiasis), liver dysfunction with the development of liver failure, melena, ileus, dry mouth, thirst, loss of appetite, stomatitis, glossitis, inflammation salivary glands. From the central nervous system and peripheral nervous system: dizziness, headache, weakness, drowsiness, peripheral neuropathy (paresthesia), nervous irritability, anxiety, tremor, muscle spasm, mood disorders, apathy; when used in high doses - insomnia, anxiety, depression, ataxia, confusion, fainting. From the respiratory system: dry cough, bronchospasm, shortness of breath, rhinorrhea, rhinitis, sinusitis, pharyngitis, hoarseness, bronchitis, interstitial pneumonia, embolism pulmonary artery, pulmonary infarction, pulmonary edema. From the urinary system: development or intensification of symptoms

Drug interactions

Ramipril enhances the inhibitory effect of ethanol on the central nervous system. With the simultaneous use of ramipril and other drugs that lower blood pressure (diuretics, nitrates, tricyclic antidepressants, anesthetics), it leads to an increase in the hypotensive effect of ramipril. The simultaneous administration of ramipril and potassium supplements or potassium-sparing diuretics can cause hyperkalemia. Vasopressor sympathomimetics (adrenaline, norepinephrine) can reduce the hypotensive effect of ramipril. In this regard, during simultaneous treatment, blood pressure levels should be carefully monitored. The simultaneous administration of ramipril and allopurinol, immunosuppressants, corticosteroids, procainamide, cytostatics increases the likelihood of changes in the peripheral blood picture. The simultaneous administration of ramipril and lithium preparations leads to a decrease in lithium excretion. Therefore, it is necessary to monitor the concentration of lithium in the blood serum to eliminate the risk of developing toxic effects.

Overdose

marked decrease in blood pressure, bradycardia, shock, water-electrolyte imbalance, acute renal failure, stupor, dry mouth, weakness, drowsiness

Storage conditions

• store in a dry place
• store at room temperature 15-25 degrees
• keep away from children

Information provided

INSTRUCTIONS
For medical use drug
Amprilan

(Amprilan)

Pharmacological action:
The active component is a prodrug. In the body, its metabolic transformations occur to ramiprilat. It acts as an angiotensin-converting enzyme inhibitor. The substance has long action. The drug blocks the synthesis of angiotensin II from angiotensin I. This provokes a decrease in plasma levels of angiotensin II, causes an increase in renin activity, leads to a potentiation of the effect of bradykinin molecules, and increased production of aldosterone molecules. As a result of these effects, vasodilation and a decrease in peripheral vascular resistance with a natural decrease in blood pressure are observed. This determines the implementation of the antihypertensive effect and hemodynamic effect. The effect of ramipril on myocardial rhythm is usually not observed.

Long-term therapy with ramipril causes regression of hypertrophic changes in the left ventricle. The development of the therapeutic effect to reduce blood pressure is observed after 60-120 minutes. after consumption dosage form. The action lasts up to a day. Maximum therapeutic effect develops after 3.5 weeks of therapy. This action can be maintained during long courses. With abrupt withdrawal, no significant hypertension is observed.

When treating CHF, ramipril ensures greater survival of patients, stops the progress of myocardial failure, and reduces the risk of hospitalization in patients with CHF. Ramipril reduces the likelihood of fatal complications in patients with cardiovascular pathologies, in diabetic patients with associated factors risk. It is recommended to use ramipril-containing drugs in parallel with revascularization to reduce the risk of death. Amprilan improves the patient's condition with microalbuminuria and reduces the risk of developing nephropathic changes. Influences negative character there is no effect on myocardial function.

Indications for use:
Amprilan is indicated for:
- arterial hypertension;
- nephropathy associated with diabetes;
- myocardial failure chronic;
- nephropathy associated with kidney pathologies;
- prevention of myocardial infarction;
- stroke prevention;
- myocardial failure in the post-infarction period;
- therapy of patients after coronary angioplasty, coronary bypass surgery;
- therapy of patients with arterial occlusion in the periphery;
- therapy to reduce mortality from cardiovascular pathologies.

Directions for use:
The dosage form is taken orally. The tablet must not be chewed. The medication can be taken regardless of food. Dosage is selected individually. The tablet must be taken with clean water in sufficient quantity. Long-term courses of therapy with Amprilan are indicated.

Amprilan dosage regimens:
Condition, indication Initial dosage, mg Maintenance dosage, mg Special instructions
Arterial hypertension 2.5 2.5-10 The dose is taken 1 time/day. The dose is increased after 1-2 weeks. During therapy with diuretics, it is necessary to reduce the dose of diuretics three days before starting therapy with the drug Amprilan
CHF 1.25 2.5-10
Myocardial failure in the post-infarction period (2-9 days) 2.5-5 5-10 The dose is divided into two doses. Doubling of doses is carried out every few days. At poor tolerance dosage of 5 mg/day, the drug is discontinued
Nephropathy associated with diabetes, diffuse chronic kidney pathologies 1.25 5 Dosage doubling is carried out 1 time/14 days. The dose is taken once a day
Reducing the risk of fatal cardiovascular complications 2.5 10 Dosage doubling every week
Indications for patients with kidney pathologies (creatinine clearance less than 30 ml/min) 1.25 5
Indications for patients with kidney pathologies 1.25 2.5
Indications in elderly patients Dosage depends on blood pressure values ​​Monitoring the condition of patients during diuretic therapy is important

Side effects:
The use of Amprilan tablets may be accompanied by:
- severe hypotension;
- imbalance;
- nasal congestion;
- disorders of concentration;
- ischemia of myocardial tissue;
- asthenic syndrome;
- motor agitation;
- erythema;
- syncope;
- myocardial infarction;
- gynecomastia;
- muscle cramps;
- orthostatic hypotension;
- arrhythmia;
- exanthema;
- ischemia of cerebral tissues;
- vasculitis;
- transient ischemic attacks;
- anxiety;
- headache;
- sleep disorders;
- tachycardia;
- fatigue;
- impotence;
- circulatory disorders;
- decreased libido;
- increase in creatinine concentration;
- tachycardia;
- shortness of breath;
- photosensitivity;
- myalgia;
- acute insufficiency liver;
- bronchospasm;
- increased excitability;
- paresthesias;
- peripheral edema;
- angina pectoris;
- bronchitis;
- maculopapular rash;
- increased proteinuria;
- depressive states;
- kidney disorders;
- dizziness;
- tides;
- urticaria;
- exacerbation of gout;
- vomiting;
- exacerbation of psoriasis;
- anorexia;
- parosmia;
- Stevens-Johnson syndrome;

- disorders of consciousness;
- exfoliative dermatitis;
- alopecia;
- loss of appetite;
- polyuria;
- nausea;
- dry cough;
- deterioration in asthmatic patients;
- inflammation of the gastrointestinal mucosa;
- tremor;
- aphthous stomatitis;
- hearing impairment;
- neutropenia;
- increased liver activity. enzymes;
- hyperhidrosis;
- erythropenia;
- pemphigoid rashes;
- pharyngitis;
- ischemic stroke;
- itching;
- proteinuria;
- sinusitis;
- toxic epidermal necrolysis;
- hyperkalemia;
- gastritis;
- Raynaud's syndrome;
- dyspepsia;
- alopecia
- pemphigus;
- hyperbilirubinemia;
- hyperthermia;
- psoriasiform rashes;
- lichenification of the skin;
- epigastric discomfort;
- pancytopenia;
- pancreatitis;
- distortion of taste perception;
- vision disorders;
- cholestatic hepatitis;
- onycholysis;
- cholestatic jaundice;
- hepatocellular lesions;
- diarrhea;
- conjunctivitis;
- hemolytic anemia;
- arthralgia;
- angioedema;
- dryness of the oral mucosa;
- thrombocytopenia;
- activation of pankeoenzymes;
- increase in ANA titer;
- glossitis;
- febrile conditions;
- hyponatremia;
- impaired sense of smell;
- inhibition of bone marrow hematopoiesis;
- increased diuresis;
- agranulocytosis;
- hypohemoglobinemia;
- anaphylaxis.

Contraindications:
Amprilan is not prescribed for:
- hypersensitivity to ramipril;
- obstructive cardiomyopathy associated with myocardial hypertrophy;
- hemodialysis;
- galactose intolerance;
- indications for pregnant women;
- angioedema of various origins in the anamnesis;
- indications for nursing;
- lactase deficiency;
- renal artery stenosis with significant hemodynamic disturbances;
- hypersensitivity to ACE inhibitors;
- hypertension with blood pressure readings less than 90 mmHg;
- kidney failure with creatinine clearance less than 20 ml/minute;
- indications for patients after kidney transplantation;
- hypersensitivity to additive components of tablets;
- malabsorption syndrome of simple sugars;
- aortic stenosis with a significant effect on hemodynamics;
- stenosis of the renal artery in the presence of one kidney in the patient;
- mitral stenosis with a significant effect on hemodynamics;
- primary hyperaldosteronism;
- indications in pediatrics;
- nephropathy, for the therapeutic correction of which cytostatic drugs, immunomodulatory agents, glucocorticosteroids, and NSAIDs are used;
- decompensated myocardial failure of a chronic nature.

Caution is necessary when prescribing Amprilan for:
- pathologies coronary arteries difficult character;
- kidney failure;
- diabetes mellitus;
- hyperkalemia;
- unstable angina;
- systemic pathologies of connective tissue;
- hyponatremia;
- arterial hypertension of a malignant nature;
- liver failure;
- inhibition of bone marrow functions;
- severe myocardial rhythm disturbances;
- CHF of the fourth functional class;
- indications in elderly patients;
- pathologies cerebral vessels difficult character;
- decrease in BCC;
- hemodialysis using membranes based on polyacrylonitrile;
- pulmonary heart in the stage of decompensation;
- carrying out desensitization based on the venom of Hymenoptera;
- the need to prescribe the drug before LDL apheresis.

Pregnancy:
Ramipril can disrupt the functioning of the fetal kidneys, provoke the development of hyperkalemia, and cause hypoplasia of the cranial bones and lung tissue. Because of this, the drug is contraindicated for pregnant women. Before use, women must undergo a test to exclude pregnancy. If a patient is pregnant during ramipril therapy, therapy should be discontinued as soon as possible.

Interaction with other drugs:
Preparation, group affiliation medicine Possible result interactions with ramipril
Ethanol-containing drugs Significant potentiation of the effect of ethanol-containing drugs
Procainamide Development of leukopenia
Allopurinol Risk of developing leukopenia
Opiates Potentiation of antihypertensive effects
Nimodipine Heart rhythm disturbances, development of congestive heart failure
Antihypertensives Risk of hypotension
Cytostatics Risk of developing leukopenia
Antidiabetic drugs Increased hypoglycemic effect. Dosage adjustment of hypoglycemic drugs is necessary
Lithium preparations Increased plasma lithium concentration. Toxic Hazard
Alpha blockers Increased hypotension. You can combine drugs to achieve the required blood pressure levels
Digitalis preparations Threat of arrhythmia, risk of complications due to changes in potassium levels
Lisinopril Increased development of the hypotensive effect
Beta blockers Increased hypotension. You can combine drugs to achieve the required blood pressure levels
Diuretics Increased hypotension. Dosages of medications need to be adjusted
Immunosuppressants Risk of developing leukopenia
Organic nitrates Increased hypotension
Potassium-containing drugs Risk of hyperkalemia
Systemic anesthetics Significant reduction in blood pressure
NSAIDs Reduced antihypertensive effect, risk of developing acute renal failure
Epinephrine Decreased antihypertensive effect
Tricyclic antidepressants Risk of hypotension (including orthostatic)
GCS Reduced antihypertensive effect due to fluid retention
Gold preparations Development of nitrate-like reactions
Neuroleptics Increased hypotension, orthostatic hypotension
Tetracosactide Reduced antihypertensive effect due to fluid retention
Methyldopa Mutual enhancement of antihypertensive effect
Nitroglycerin Increased hypotension

Overdose:
Excess therapeutic doses accompanied by:
- significant hypotension;
- bradycardia;
- pathological change water and electrolyte balance;
- acute renal failure;
- states of shock.

Measures are taken to cleanse the gastrointestinal tract; administration of drugs with adsorbing properties, sodium sulfate, is indicated. For severe hypotension, catecholamines are administered. The patient's position is head below body. BCC is replenished by administering physical. solution. When bradycardia manifests itself, the use of pacemakers is indicated. The doctor is obliged to monitor plasma potassium concentration and blood pressure levels. The use of hemodialysis is not recommended.

Release form:
Amprilan is available in tablet form in four dosages. For each dosage the packaging is as follows:
- 14 tablets/pack;
- 28 tablets/pack;
- 30 tablets/pack;
- 56 tablets/pack;
- 60 tablets/pack;
- 84 tablets/pack;
- 90 tablets/packaging;
- 98 tablets/pack.

Storage conditions:
The storage temperature of Amprilan tablets is up to 25 degrees Celsius. The shelf life of Amprilan 1.25 is 2 years, all other dosages are 3 years.

Compound:
1 tablet of Amprilan 1.25 contains ramipril 1.25 mg. Additive components: starch, sodium stearyl fumarate, croscarmellose sodium, sodium bicarbonate, lactose (in the form of monohydrate).

1 tablet of Amprilan 2.5 contains ramipril 2.5 mg. Additive components: starch, sodium stearyl fumarate, croscarmellose sodium, sodium bicarbonate, lactose (in the form of monohydrate), pigment PB 22886.

1 tablet Amprilan 5 contains ramipril 5 mg. Additive components: starch, sodium stearyl fumarate, croscarmellose sodium, lactose (in the form of monohydrate), sodium bicarbonate, pigment PB 24899.

1 tablet of Amprilan 10 contains ramipril 10 mg. Additive components: starch, sodium stearyl fumarate, croscarmellose sodium, sodium bicarbonate, lactose (in the form of monohydrate).

Pharmacological group:
Cardiovascular drugs
Level-regulating drugs blood pressure
Antihypertensive drugs
Medicines affecting the renin-angiotensin system

ATX: C09AA05

Amprilan - antihypertensive drug, belonging to the group of ACE inhibitory agents, intended to compensate for conditions accompanied by high blood pressure. It is no secret that many people, especially older people, suffer from this pathology, which, first of all, is fraught with its own complications, including conditions such as myocardial infarction and cerebral strokes. But can they all be used? Let's find out by reading what the instructions for use write about Amprilan, and we'll find out what analogues it has.

Composition and release form

The active component of the drug is ramipril, which is an angiotensin-converting enzyme inhibitor. Its content, depending on the dosage, is: 1.25; 2.5; 5; 10 milligrams.

Auxiliary components: yellow iron oxide, lactose monohydrate, sodium stearyl fumarate, pregelatinized corn starch, croscarmellose sodium, sodium bicarbonate, lactose monohydrate, as well as a mixture of multi-colored dyes.

It is produced in blisters, each of which contains 7 or 10 tablets. Sold in strict accordance with the doctor's prescription.

Pharmacological action

As I already mentioned, the drug Amprilan, or rather its active component, is an angiotensin-converting enzyme inhibitor. How does it work? It's all about suppressing the biological transformation of a special substance, angiotensin I, into angiotensin II. The latter has a pronounced effect on the tone of smooth muscle fibers located in vascular wall, resulting in increased blood pressure.

Decline blood pressure helps reduce the load on the heart muscle, which ultimately results in a decrease in the heart's need for oxygen. This circumstance, firstly, has a positive effect on the frequency and severity of heart attacks. Secondly, it helps to reduce compensatory hypertrophy of the left ventricle of the heart, which also has a positive effect on the patient’s health.

Ramipril improves the course of diseases complicated by heart failure, reduces the likelihood of sudden death of the patient, and reduces the need for hospitalization for inpatient treatment.

The effect of Amprilan begins 1 to 2 hours after taking the medicine. The maximum effect is achieved after 3 hours, and the hypotensive effect itself lasts about 24 hours, which means that you need to take this medicine only once a day, which makes its use very convenient.

Indications for use

The purpose of this medication performed in the presence of the following pathological conditions:

High blood pressure;
Pathology accompanied by chronic heart failure;
Diabetic kidney damage;
Prevention of myocardial infarction, as well as sudden death of the patient.

I remind you that this kind of medication should be taken only after approval from a cardiologist who has comprehensively studied the patient’s health condition. Uncontrolled use of such drugs promises very sad consequences.

Contraindications for use

Below is a list of conditions in the event of which Amprilan should not be prescribed:

Angioedema;
Renal artery stenosis;
Need for hemodialysis;
Any pathology caused by insufficient function of the excretory system;
Obstructive cardiomyopathy of hypertrophic origin;
Decompensated heart failure;
Pregnancy;
Lactation;
Low blood pressure;
Hyperaldosteronism;
The patient's age is less than 18 years, in the form of unknown effectiveness of the drug in this group;
Hypersensitivity;
Nephropathic conditions.

Use with a fair amount of caution in the presence of malignant hypertension, in case of damage cerebral arteries, with the simultaneous use of diuretics, as well as during the implementation of desensitizing therapy carried out after poisoning with the venom of certain Hymenoptera.

Application and dosage

The choice of an adequate dose of the drug is carried out in strict accordance with the diagnosis, age, body weight of the patient and other factors. So, when treating arterial hypertension, you should take 2.5 mg once a day. If necessary, the dosage can be increased to 2.5 - 5 mg. Maximum - 10 mg per day.

To correct chronic heart failure, 1.25 mg per day is prescribed. If the patient’s body responds adequately, the dose should be doubled every 2 weeks until a therapeutic effect is achieved. For the treatment of nephropathic conditions, the application regimen is similar.

Prevention of myocardial infarction consists of using 2.5 mg of the drug, increasing the dose every week until the desired effect is achieved. The maximum daily dose is 10 mg.

Drug overdose

In case of unintentional overdose, the following symptoms may occur: sharp drop pressure, tachycardia, weakness, sweating. In this case, you need to rinse the patient’s stomach and take all measures aimed at maintaining basic vital signs.

Side effects

From the cardiovascular system: drop in blood pressure, increase in heart rate, orthostatic manifestations, edema, heart attacks, flushes, Raynaud's syndrome.

From the digestive system: inflammation of the mucous membrane of the gastrointestinal tract, dyspepsia, nausea, vomiting, diarrhea, constipation, stomatitis, loss of appetite and some others.

From the peripheral and central nervous system: weakness, fatigue, depressive states, anxiety, dizziness, parosmia, memory impairment and motor coordination.

Others unwanted effects: allergic reactions, suppression of libido, visual disturbances, changes in hemogram.

Analogues

The following drugs are analogues of the drug: Hartil, Tritace, Ramicardia, Ramigamma, Pyramil, Korpril, Dilaprel, Vazolong.

Conclusion

You found out what the drug Amprilan is in practice, instructions, use, analogues, indications and contraindications, as well as composition. Successful treatment cardiac diseases depends on how punctually the patient follows all the doctor’s instructions, both in terms of taking medications and in terms of daily routine and dietary habits.

The drug "Amprilan" belongs to the class ACE inhibitors(angiotensin-converting enzyme), which dilate blood vessels and lower blood pressure. The drug is recommended for hypertension and heart failure, as well as for prophylactic use patients who have had a heart attack, in order to reduce the risk of mortality and complications.

"Amprilan": instructions for use, at what pressure and how exactly to take the drug, its use for certain indications, nature of action and metabolic features.

Compound

The active component of the tablets is ramipril. The drug is available with different dosages ramipril per tablet at 1.25, 2.5, 5 and 10 mg.

Composition of fillers and excipients in the drug varies depending on the dosage of the active component, since according to the manufacturer’s idea, tablets with different dosages should have different colors.

Important! Tablets of any strength include lactose monohydrate, pregelatinized starch and sodium compounds (croscarmellose, bicarbonate and stearyl fumarate). Due to the lactose content, patients intolerant milk sugar the drug is contraindicated.

Tablets with a dosage of 5 mg, in addition to all the indicated substances, also contain a mix of dyes “RV 24899 pink”, and 2.5 mg - “RV 24886 yellow”. Other dosages do not contain dyes and have white and differ in size (the smallest and the largest).

The drug "Amprilan" in tablets of 10 mg

Release form

The drug is available only in tablet form. The tablets are packaged in blisters of 7 or 10 pieces. The blisters, together with the attached instructions for use, are placed in a cardboard box.

The tablets have an oblong shape, a flat surface and are chamfered. Tablets with a dosage of 1.25 mg and 10 mg have natural color ingredients (close to white), differing only in size. 2.5 mg tablets have light yellow color, 5 mg tablets – pink with lighter inclusions.

"Amprilan ND" (active ingredients: 5 mg ramipril and 25 mg hydrochlorothiazide)

Pharmacodynamics and pharmacokinetics

Ramipril is an angiotensin-converting enzyme inhibitor (ACEI), whose function is to accelerate the transformation of angiotensin I to angiotensin II. After initial appointment the patient may already experience a decrease in blood pressure after 2 hours (sometimes earlier). The maximum therapeutic effect is observed 4-6 hours after administration and lasts throughout the day. Taking the medication for 2-3 months reduces hypertrophy of the left cardiac ventricle, while there is no negative impact on organ function.

The drug prevents the development of nephrotic diseases (including in patients with diabetes). He also gives strong effect in the treatment of heart failure. If signs of this disease are detected in a patient, suffered a heart attack, the use of the drug reduces the risk of mortality associated with diseases of the cardiovascular system. Listed positive effects observed in patients both with and without signs of hypertension.

About 70% active ingredient binds to plasma albumin. Regardless of whether the drug was taken with food or not, ramipril has very rapid absorption: within an hour after taking the tablets, its highest plasma concentration can be recorded. In the liver, it is broken down into metabolites - active (ramiprilat - its activity is 6 times higher than the activity of the original substance) and inactive (diketopiperazine).

The highest concentration of ramiprilat is recorded 3-4 hours after administration. A stable therapeutic concentration accumulates in the blood after 4 days of treatment. About 55% of the active metabolite is bound to plasma proteins.

Rampril and its active metabolite are excreted by the kidneys, with up to two percent of the former being excreted unchanged. Its half-life is just over 5 hours. For ramiprilat, its duration is up to 17 hours. Moreover, in patients with kidney disease, these indicators increase in proportion to the decrease in creatinine clearance. In patients with liver failure, laboratory tests show increased levels of unchanged ramipril in the blood. This is because deteriorating liver function affects its metabolic capacity.

During laboratory comparative study Features of ramipril metabolism in young and elderly healthy people no significant differences were found.

Ramipril

Indications for use

• Hypertension;
• Nephropathy (including those caused by diabetes mellitus);
• Glomerulonephritis with increased content protein in urine;
• Chronic heart failure;
• For patients who have suffered a stroke or myocardial infarction, as a means of maintenance therapy for general relief of the condition, reducing the likelihood of mortality and preventing the development of recurrent manifestations;
• In case of occlusive arterial circulation disorder;
• Patients who have undergone coronary bypass surgery or other surgical interventions on the arteries.

Hypertension

Contraindications

Contraindications to taking amipril are such conditions and diseases as:

• Renal failure (creatinine clearance value less than 20 ml/min);
• Stenosis of the aorta and heart valves, as well as stenosis of the renal arteries;
• Hypotensive conditions;
• Increased synthesis of aldosterones;
• Presence in anamnesis angioedema any etiology;
• Inflammation of heart tissue;
• The presence of transplanted kidneys in the body;
• Hemodialysis;
• Intolerance to lactose, galactose and high sensitivity to the active component of the drug;
• Therapy of nephropathy with immunomodulators, non-steroidal anti-inflammatory drugs, cytostatics, glucocorticoids;
• Minor age;
• Pregnancy (at any stage) and breastfeeding.

Caution should also be exercised when prescribing the drug to patients with the following pathologies:

• Angina;
• Systemic lupus erythematosus;
• Heart rhythm disturbances;
• Serious damage to the brain and heart arteries (as a decrease in blood pressure due to taking the drug can lead to a dangerously reduced blood supply to the heart or brain);
• Diabetes mellitus;
• Decompensated cor pulmonale;
• Conditions that accompany diarrhea and vomiting;
• Excess potassium and sodium deficiency in the body.

Blood pressure measurement process

Side effects

Typically, patients tolerate treatment with the drug calmly, but in clinical studies The following side effects have been reported.

• Too much pressure reduction (especially if the patient is taking diuretics);
• Nausea, diarrhea, vomiting;
• Muscle pain and cramps;
• Inflammation of the mucous membranes of the gastrointestinal tract;
• Bronchitis and sinusitis;
• Skin rash;
• Dry cough;
• Migraine.

• Peripheral cardiac edema;
• Violations heart rate;
• Joint pain;
• Dizziness;
• Increased fatigue, nervousness, anxiety;
• Insomnia;
• Kidney dysfunction;
• Increased protein and urea content in urine;
• Pancreatitis, jaundice, liver inflammation;
• Increased sweating.

Very rare:

• Myocardial infarction;
• Coronary heart disease and ischemic stroke;
• Tachycardia;
• Gynecomastia;
• Stomatitis;
• Baldness;
• Urticaria and dermatitis.

Migraine

How to take and at what pressure, dosage

The dosage of the drug is selected by the doctor taking into account the assessment of the patient’s general health profile and condition various systems body. It is permissible to take no more than 10 mg per day active substance. Tablets are taken without reference to meals. They are swallowed and washed down with at least 50 g of liquid. The duration of treatment is also prescribed by the doctor for each specific case.

Limitations on daily dosage:

• If the patient has kidney pathologies, you should not take more than 5 mg of the active ingredient per day;
• The same applies to patients with liver failure, only for them the maximum daily dose is already 2.5 mg per day;
• When creatinine clearance is less than 30 ml/min, the initial daily dose active substance should be 1.25 mg. Over time it is increased, but it should not exceed 5 mg;
• Taking the drug by pregnant women has a negative effect on the fetus, contributing to improper formation skeleton of the skull and underdevelopment of the lungs, therefore, taking Amprilan is strictly contraindicated for pregnant women, and if a woman childbearing age prescribed to take the drug, she needs to first take a pregnancy test.

At high blood pressure It is recommended to take 2.5 mg of ramipril once a day. In case of severe hypertension, if the state of the body allows, daily dose increase to 5 mg one to two weeks after starting treatment. If the patient is taking diuretics, their dose should be reduced 3 days before starting the drug (if possible, discontinued completely).

Heart patients are prescribed a dosage of 1.25 mg once daily. They, like the previous group of patients, need to stop diuretics (or reduce the dose) if they are taken. In the post-infarction state, 2.5 mg twice a day is first prescribed. If there is an excessive drop in pressure, single dose reduced to 1.25 mg (also taken twice a day). To prevent the development of heart failure after suffered a heart attack 2.5 mg tablets are prescribed: first one tablet per day, after a week the dose is doubled, after a month it is doubled again - as maintenance therapy the patient begins to receive 10 mg of the active substance per day.

For nephropathy of various etiologies the patient starts with a dose of 1.25 mg per day. After two weeks it is doubled, then after two weeks of taking 2.5 mg per day it is doubled again. The patient stops at a maintenance dosage of 5 mg.

"Amprilan NL"

Overdose

Signs of a drug overdose:

• Slowing heartbeat;
• Severe drop in blood pressure;
• Problems with water and electrolyte balance (excess potassium, lack of sodium);
• Phenomena of renal failure;

If a pronounced drop in pressure is observed, the patient is placed on his back (there should be no pillow under the head) and catecholamines, dopamine, and angiotensinamide are administered intravenously. If your heart rate is very low, you can consider implanting a pacemaker.

To relieve the consequences of an overdose, it is advisable as early as possible (within half an hour after taking disproportionately high dose drug) give the victim a gastric lavage and take a sorbent (enterosgel, activated carbon). The administration of sodium sulfate is indicated. There are no clinical data on the effectiveness of hemodialysis.

Patients taking ramipril need to monitor their kidney function, the concentration of potassium ions in the blood and blood pressure.

Interaction

ACE inhibitors, including ramipril, increase the inhibitory nervous system alcohol effect. Drinking alcohol while taking the drug puts a significant burden on the liver, so when treating with this drug, the use of products containing ethanol should be avoided.

Concomitant use of ATP inhibitors and non-steroidal anti-inflammatory drugs worsens renal function and may contribute to the development of acute renal failure.

Drugs based on epinephrine neutralize the ability of Amprilan to reduce blood pressure.

Tricyclic antidepressants, on the contrary, increase hypotensive effect drug.

When ramipril was used with lithium-based drugs, a strong increase in plasma lithium levels was observed, approaching concentrations that have a toxic effect.

A number of drugs for joint reception with ramipril may contribute to the development of leukopenia. These include:

• Cytostatics;
• Procainamide;
• Immunosuppressants;
• Allopurinol;
• Glucocorticoids.

Analogues

Analogs of the drug are medications with the same active ingredient, for example:

• "Pyramid";
• "Hartil";
• "Dilaprel";
• "Vazolong".

Dilaprel

The use of Amprilan (in the absence of contraindications) is advisable for hypertensive conditions, as well as for the prevention and relief of heart failure, including that developed after a heart attack and stroke. However, the drug imposes very large number restrictions on use. Only the attending physician should prescribe the regimen and dosage.