Amprilan tablets user manual
Amprilan is an antihypertensive agent that belongs to the group of angiotensin converting enzyme (ACE) inhibitors. Has vasodilator effect, lowers arterial pressure. The drug is effective in the therapy of chronic heart failure. After a heart attack, Amprilan reduces the risk of sudden death, prevents the development of chronic heart failure. Reduces the likelihood of developing nephropathy.
Form of issue and composition
The main active ingredient of Amprilan is ramipril.
The auxiliaries contained in the tablets are: croscarmellose sodium; pregelatinized starch; sodium stearyl fumarate; sodium bicarbonate, lactose monohydrate, colorants.
Dosage: 1.25 mg, 2.5 mg, 5 mg and 10 mg of ramipril in one tablet.
Amprilan produced in tablets (7 or 10 tablets in a blister) oval shape with a flat surface and bevel. The color of the tablets differs depending on the dosage of the drug: white or almost white (1.25 mg and 10 mg each), light yellow (2.5 mg), pink with patches (5 mg each),
Pharmacodynamics. Amprilan - long-acting ACE inhibitor. Angiotensin-converting enzyme accelerates the conversion of angiotensin II from angiotensin I, is identical to a kinase enzyme that accelerates the breakdown of bradykinin. As a result of the blockade of ACE by Amprilan, the concentration of angiotensin II decreases, the renin activity in the blood plasma increases, the action of bradykinin and aldosterone production increases, which leads to an increase in the potassium content in the blood.
Amprilan has antihypertensive and hemodynamic effects due to the expansion of blood vessels and reduction of their total peripheral resistance. At the same time, the heart rate does not change. Decrease in pressure after a single dose of Amprilan is observed after 1-2 hours, after 3-6 hours the therapeutic effect reaches a maximum and lasts 24 hours.
With prolonged treatment with the drug, left ventricular hypertrophy decreases, while there is no adverse effect on the function of the heart.
Pharmacokinetics. The active substance is quickly absorbed from the digestive tract (speed does not depend on the intake of food). An hour after application, the maximum concentration of the active substance in the blood is reached. Blood plasma proteins bind up to 73% of ramipril.
The drug is cleaved in the liver, forming an active metabolite ramiprilate (the activity of the latter is 6 times greater than that of ramipril itself) and an inactive diketopiperazine compound. The maximum concentration of ramiprilate in the blood is detected 2-4 hours after the application of the drug, a stable and constant therapeutic concentration - on the 4th day of treatment. About 56% of ramiprilata binds to blood plasma proteins.
Up to 60% of ramipril and ramiprilate are excreted by the kidneys in the form of metabolites, less than 2% of ramipril is removed from the body in an unchanged form. The half-life of ramiprilata is from 13 to 17 hours, ramipril - 5 hours.
If the renal function is impaired, the rate of excretion of ramipril and metabolites is reduced. In patients with hepatic insufficiency the process of transformation of ramipril into ramiprilat is slowed down, the content of ramipril in serum is increased.
Indications for use
In accordance with the instructions, indications for the use of Amprilan are:
- chronic heart failure;
- in complex supportive treatment after myocardial infarction;
- arterial hypertension;
- diabetic nephropathy;
- nephropathy due to chronic diffuse kidney disease;
- acute violation of arterial peripheral circulation (occlusion of arteries);
- prevention of stroke, heart attack and reduction of mortality from cardiovascular pathologies;
- after coronary bypass.
According to the instructions, the drug is contraindicated in the following pathologies and conditions:
- the transferred angioedema (idiopathic, resulting from the administration of ACE inhibitors, hereditary);
- kidney failure;
- a transplanted kidney transplant operation;
- mitral or aortic stenosis;
- bilateral stenosis of the renal arteries or stenosis of one renal artery in the presence of only one kidney;
- cardiomyopathy (inflammation of the muscular tissue of the heart);
- heart defects;
- low pressure;
- hyperaldosteronism (excessive synthesis of aldosterones);
- age younger than 18 years;
- pregnancy and lactation.
Dosing and Administration
Tablets are taken orally regardless of food intake, do not chew, drink a sufficient amount of liquid.
The dosage of the drug is selected by the doctor individually for each patient, taking into account the indications, drug tolerance, concomitant diseases and the patient's age. When choosing a dose, the blood pressure index must be taken into account. The maximum permissible dosage of the drug for all types of pathology is 10 mg per day. The course of treatment is usually lengthy, also set by the doctor.
With arterial hypertension, the initial recommended dosage is 2.5 mg once daily. If necessary, the dose can be doubled after 7-14 days.
In chronic heart failure, the initial recommended dose of the drug is 1.25 mg (can be doubled after 1-2 weeks).
With heart failure , which occurred 2-9 days after acute myocardial infarction, it is recommended to take 5 mg of Amprilan per day - 2, 5 mg in the morning and in the evening. If the pressure is greatly reduced during treatment, the dosage is halved (1.25 mg twice a day). After 3 days, the dose rises again. If taking the drug at a dose of 2.5 mg twice a day is again badly tolerated by the patient, Amprilan treatment should be reversed.
Nephropathy (with diffuse kidney pathologies and diabetic). The recommended initial dose is 1.25 mg per day. Every 14 days, the dosage is doubled before reaching a maintenance dose of 5 mg per day.
Prevention of heart failure after myocardial infarction. At the initial stage of the therapeutic course, Amprilan is administered 2.5 mg per tablet per day. After a week, the dosage is increased to 5 mg per day, after another 2-3 weeks - to a maintenance dose of 10 mg once a day.
In arterial occlusion and after coronary shunting, Amprilan is taken 2.5 mg once a day for 7 days. Then 2-3 weeks the drug is taken at 5 mg per day, after it dosage is doubled - up to 10 mg per day.
The drug is well tolerated. But there are likely to be side effects from various body systems.
From the cardiovascular system:
- marked decrease in blood pressure, especially at the initial stages of treatment, with complex use with diuretics or with increasing doses (often);
- development of arrhythmia, angina pectoris, peripheral edema (rarely);
- circulatory disorders, tachycardia , vasculitis , increased circulatory disorders, ischemia and myocardial infarction (extremely rare).
From the nervous system:
- weakness and headache (often);
- nervousness and fatigue, depression, confusion and impaired consciousness, dizziness, anxiety, sleep disorder (rarely);
- decreased ability to concentrate, impaired perception of odors, cerebral ischemia, ischemic stroke (extremely rare).
From the excretory system:
- functional impairment of kidney function, renal failure, increased proteinuria, increased urea levels (rarely);
- gynecomastia (very rarely).
On the part of the respiratory tract:
- dry cough, worse at night and lying down, sinusitis, bronchitis (often);
- pharyngitis , bronchospasm, exacerbation of bronchial asthma (rarely).
From the side of the skin:
- skin rash (often);
- skin itching, increased sweating (rarely);
- erythema, exacerbation of psoriasis, alopecia, urticaria , dermatitis, photosensitivity (extremely rare).
From the digestive system:
- inflammation of the mucosa of the digestive tract, discomfort in the epigastric region, indigestion, nausea, vomiting, diarrhea (often);
- increased bilirubin concentration and liver enzyme activity, cholestatic jaundice and hepatitis, hepatic insufficiency, gastritis , pancreatitis , dryness of the oral mucosa (rarely);
- glossitis, stomatitis, anorexia, angioedema (extremely rare).
From the musculoskeletal system:
- myalgia and muscle cramps (often);
- arthralgia (rarely).
When an overdose of the drug is noted:
- marked decrease in blood pressure;
- bradycardia (slowing of the heart rate);
- acute renal insufficiency;
- violation of water-electrolyte metabolism;
In case of an overdose in mild cases, the stomach is washed, sodium sulfate is administered (for 30 minutes after applying a high dose of amprilan), the use of sorbents. With a marked decrease in pressure, the administration of catecholamines, angiotensin II, alpha-1-adrenomimetics intravenously is required.
- For patients with functional disorders of the kidneys, the initial dose of Amprilan should be 1.25 mg, and the maximum daily dosage should be 5 mg.
- For patients with hepatic insufficiency, the initial dose is 1.25 mg, the maximum daily dose is 2.5 mg.
- If Amprilan is prescribed to patients taking diuretics, it is necessary to cancel or reduce the dosage of diuretics. It also requires constant monitoring of the condition of such patients, especially elderly patients (over 65 years of age).
- Amprilan is taken with caution in patients with systemic connective tissue diseases, diabetes mellitus, unstable angina.
- The drug has a negative effect on the fetus (hypoplasia of the lungs and bones of the skull, hyperkalemia, disruption of the kidneys) and is contraindicated in pregnant women. Before discharge Amprilan women of childbearing age it is important to exclude pregnancy.
- When taking Amprilan during lactation, breastfeeding should be canceled.
Terms and conditions of storage
The drug should be stored at a temperature not higher than 25 ° C, protected from moisture and sunlight, and difficult to reach for children. The shelf life of Amprilan tablets is 3 years. After the onset of the date indicated on the package, the drug should not be taken.
Structural analogues of Amprilan (preparations with a similar active ingredient) are:
Price for Amprilan
Amprilan tablets 1.25 mg, 30 pcs. - from 165 rubles.
Amprilan tablets 2.5 mg, 30 pcs. - from 217 rubles.
Amprilan tablets 5 mg, 30 pcs. - from 283 rubles.
Amprilan tablets 10 mg, 30 pcs. - from 345 rubles.