Ramipril
Ramipril: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Drug interactions
- 10. Analogs
- 11. Terms and conditions of storage
- 12. Terms of dispensing from pharmacies
- 13. Reviews
- 14. Price in pharmacies
Latin name: Ramipril
ATX code: C09AA05
Active ingredient: Ramipril (Ramipril)
Manufacturer: Hechst AG (Germany)
Description and photo update: 2019-07-08
Prices in pharmacies: from 83 rubles.
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Ramipril is a long-acting angiotensin-converting enzyme (ACE) inhibitor.
Release form and composition
Dosage form - tablets: almost white or white, round flat-cylindrical shape, with a chamfer and a dividing line (in a blister strip: 10 pcs., 3 packs in a cardboard box; 14 pcs., 1 or 2 packs in a cardboard box) …
The active ingredient of Ramipril is ramipril, in 1 tablet - 2.5 mg, 5 mg or 10 mg.
Auxiliary components: lactose, microcrystalline cellulose, aerosil (colloidal silicon dioxide), magnesium stearate, primogel (sodium carboxymethyl starch).
Pharmacological properties
Pharmacodynamics
Ramipril has a hypotensive, natriuretic, cardioprotective effect, being a prodrug, from which the active metabolite ramiprilat is synthesized in the body.
This substance slows down the formation of angiotensin II from circulating angiotensin I and the production of angiotensin II in tissues, and also inhibits the renin-angiotensin system in tissues, including the vascular wall. Ramipril suppresses the release of norepinephrine from neuronal endings and minimizes vasoconstrictor reactions resulting from increased neurohumoral activity. The drug reduces the degradation of bradykinin and the production of aldosterone.
The drug provides for the expansion of the renal vessels, as well as the induction of reversion of left ventricular hypertrophy and pathological remodeling in the cardiovascular system. The pronounced cardioprotective effect is explained by the influence of ramipril on the biosynthesis of prostaglandins and the stimulation of the production of nitric oxide in the endothelium.
Treatment with ramipril decreases the total peripheral vascular resistance (mainly in the renal vessels). This phenomenon is less pronounced in internal organs, including the skin and liver, and slightly in the brain and muscle tissue. Also, the drug increases regional blood flow in these organs, increases the level of fibrinogen and tissue sensitivity to insulin, promotes the production of tissue plasminogen activator, providing thrombolysis.
Pharmacokinetics
When taken orally, absorption reaches 50-60%. Food intake does not affect the degree of absorption, but reduces the rate of absorption. The maximum concentration of ramipril is reached 2–4 hours after administration. In the liver, the compound is metabolized, forming the active metabolite ramiprilat (the intensity of ACE inhibition is 6 times higher than that for ramipril) and the inactive metabolite diketopiperazine. Then ramipril undergoes glucuronidation. With the exception of ramiprilat, all the metabolites formed do not exhibit pharmacological activity.
Ramipril binds to plasma proteins by 73%, and ramiprilat by 56%. Bioavailability after oral administration of 2.5-5 mg of the drug is 15-28%, in the case of ramiprilat - 45%. With a daily intake of the drug in a daily dose of 5 mg, a stable level of ramiprilat in blood plasma is achieved by the 4th day.
The half-life of ramipril is 5.1 hours. The concentration of ramiprilat in the blood serum decreases in the phase of distribution and elimination with a half-life of 3 hours, in the transition phase, the half-life is 15 hours and in the prolonged final phase, which is characterized by a very low content of ramiprilat in plasma - 4-5 days. The half-life is increased in patients with chronic renal failure.
The volume of distribution of ramipril is 90 liters, ramiprilat is 500 liters. The substance is excreted through the kidneys in the amount of 60% of the dose taken, and through the intestines in the amount of 40% (mainly in the form of metabolites). With renal dysfunction, the rate of excretion of ramipril and its metabolites decreases in proportion to the decrease in creatinine clearance, with liver dysfunctions, its conversion to ramiprilat is inhibited, and with heart failure, the content of ramiprilat increases by 1.5-1.8 times.
Indications for use
- Combination therapy of chronic heart failure (including diuretics);
- Arterial hypertension;
- Heart failure, which occurred in the period from the second to the ninth day after acute myocardial infarction;
- Clinically pronounced and preclinical stages of diabetic or nondiabetic nephropathy (especially with severe proteinuria) when combined with arterial hypertension;
- Reducing the risk of stroke, myocardial infarction or cardiovascular mortality in patients with high cardiovascular risk: with confirmed coronary heart disease (with or without myocardial infarction), including patients after coronary artery bypass grafting, percutaneous transluminal coronary angioplasty; with a history of stroke, occlusive lesions of the peripheral arteries.
In addition, the use of Ramipril is indicated in patients with diabetes mellitus in the presence of at least one additional risk factor: arterial hypertension, microalbuminuria, an increase in plasma concentrations of total cholesterol, smoking, a decrease in plasma concentrations of high-density lipoprotein cholesterol (HDL-C).
Contraindications
- Chronic heart failure in the stage of decompensation;
- Hypertrophic obstructive cardiomyopathy, hemodynamically significant stenosis of the mitral or aortic valve;
- Arterial hypotension (systolic blood pressure (BP) below 90 mm Hg) or pathology with unstable hemodynamic parameters;
- Hereditary or idiopathic angioedema (including history, including during previous therapy with ACE inhibitors);
- Glucose-galactose malabsorption syndrome, lactase deficiency, lactose intolerance;
- Severe renal failure (creatinine clearance (CC) less than 20 ml / min);
- Liver failure;
- Bilateral hemodynamically significant renal artery stenosis (in the presence of only one kidney, unilateral);
- Hemodialysis using high-flow membranes with a negatively charged surface;
- Primary hyperaldosteronism;
- Low density lipoprotein apheresis using dextran sulfate;
- Simultaneous use of glucocorticosteroids, non-steroidal anti-inflammatory drugs, immunosuppressants, cytotoxic drugs for the treatment of nephropathy;
- Concomitant hyposensitizing therapy of hypersensitivity reactions to the venoms of bees, wasps and other insects;
- Combination therapy with angiotensin II receptor antagonists in diabetic nephropathy;
- Combination with drugs containing aliskiren in patients with renal insufficiency (CC less than 60 ml / min) and diabetes mellitus;
- Age under 18;
- The period of pregnancy and breastfeeding;
- Hypersensitivity to drug components or other ACE inhibitors.
In addition, the use of Ramipril is contraindicated in the acute stage of myocardial infarction:
- NYHA functional class IV heart failure;
- Pulmonary heart;
- Unstable angina;
- Life-threatening ventricular arrhythmias.
It is recommended to prescribe the drug with caution to patients with atherosclerotic lesions of the cerebral or coronary arteries; in pathologies associated with a risk of a sharp decrease in blood pressure with impaired renal function during ACE inhibition: severe hypertension (especially malignant arterial hypertension), chronic heart failure (especially severe stage or when taking other antihypertensive drugs for it), hemodynamically significant unilateral renal stenosis arteries in patients with two kidneys, previous diuretic therapy, disturbances in water and electrolyte balance (against the background of vomiting, diarrhea, insufficient intake of sodium chloride and liquid, profuse sweating); with impaired liver and / or kidney function (CC more than 20 ml / min), diabetes mellitus, hyperkalemia, hyponatremia,systemic diseases of the connective tissue (including scleroderma, systemic lupus erythematosus, concomitant therapy with drugs acting on the peripheral blood picture (risk of inhibition of bone marrow hematopoiesis, development of agranulocytosis or neutropenia)); with the simultaneous use of angiotensin II receptor antagonists and / or aliskiren preparations with double blockade of the renin-angiotensin-aldosterone system (RAAS), in a condition after kidney transplantation.with the simultaneous use of angiotensin II receptor antagonists and / or aliskiren preparations with double blockade of the renin-angiotensin-aldosterone system (RAAS), in a condition after kidney transplantation.with the simultaneous use of angiotensin II receptor antagonists and / or aliskiren preparations with double blockade of the renin-angiotensin-aldosterone system (RAAS), in a condition after kidney transplantation.
Instructions for the use of Ramipril: method and dosage
The tablets are taken orally before or after meals, swallowing whole with water.
The doctor prescribes the dose on the basis of clinical indications, taking into account the individual tolerance and therapeutic effect of the drug.
Recommended dosage:
- Arterial hypertension: initial dose - 2.5 mg once a day (in the morning) or in 2 divided doses. To achieve the desired therapeutic effect, a multiple dose increase is possible after 2-3 weeks of treatment. The usual maintenance dose is 2.5-5 mg, the maximum is 10 mg per day. With previous diuretic therapy, they should be canceled or the dose reduced no later than 3 days before starting Ramipril. The initial dose for patients taking diuretics, patients with renal failure or with arterial hypertension and heart failure is 1.25 mg once a day. Use should be started under the strict supervision of a physician. For patients with impaired water-electrolyte balance or risk of hypotensive reaction, the initial daily dose should not exceed 1.25 mg;
- Chronic heart failure: the initial dose is 1.25 mg once, if necessary, the dose can be doubled after 1-2 weeks. The daily dose should not exceed 10 mg. With the simultaneous administration of diuretics, their dose should be reduced before starting therapy;
- Heart failure that occurs within 2-9 days after acute myocardial infarction: the initial dose is 2.5 mg 2 times a day (morning and evening) and after two days of therapy - 5 mg 2 times a day. The maintenance dose is 2.5-5 mg 2 times a day. If the drug is poorly tolerated (arterial hypotension), the initial dose should be reduced to 1.25 mg 2 times a day, then after 2 days it can be increased to 2.5 mg, after another 2 days - up to 5 mg 2 times a day. The daily dose should not exceed 10 mg. If the dose is poorly tolerated, 2.5 mg 2 times a day, the drug should be discontinued. Due to insufficient experience in the use of Ramipril in patients with severe heart failure III-IV functional class (according to the NYHA classification), which arose immediately after acute myocardial infarction, the initial dose for this category of patients should not exceed 1,25 mg once a day. Dose escalation should be carried out under medical supervision;
- Nephropathy in chronic diffuse kidney pathologies, diabetic nephropathy: initial dose - 1.25 mg once. If the drug is well tolerated, the dose can be doubled every 2 weeks until a maintenance dose of 5 mg is reached once a day;
- Reducing the risk of stroke, myocardial infarction, or cardiovascular mortality in patients with high cardiovascular risk: the initial dose is 2.5 mg once. A gradual increase in the dose is shown: after 1 week, then after 2-3 weeks - up to a maintenance dose of 10 mg once a day.
The recommended dosage regimen of Ramipril for patients with renal insufficiency:
- CC less than 30 ml / min: initial dose - 1.25 mg per day, maximum - 5 mg;
- CC 30-60 ml / min: initial dose - 2.5 mg per day, maximum - 5 mg;
- CC more than 60 ml / min: initial dose - 2.5 mg per day, maximum - 10 mg.
In liver failure, the initial dose should not exceed 1.25 mg, the maximum dose should be 2.5 mg once.
The initial dose for elderly patients is 1.25 mg per day.
Special monitoring is required for patients over 65 years of age, taking diuretics, for patients with chronic heart failure with impaired renal and liver function. The dose is selected depending on the target blood pressure level.
Side effects
- Cardiovascular system: often - orthostatic hypotension, fainting (syncope), a strong decrease in blood pressure; infrequently - peripheral edema, palpitations, flushing of the skin of the face, myocardial ischemia (including the development or intensification of arrhythmias, the development of myocardial infarction or an attack of angina pectoris, tachycardia); rarely - vasculitis, increase or appearance of peripheral circulatory disorders; frequency unknown - Raynaud's syndrome;
- Respiratory system: often - sinusitis, bronchitis, shortness of breath, dry cough (worse lying down and at night); infrequently - nasal congestion, bronchospasm, worsening of the clinical course of bronchial asthma;
- Nervous system: often - a feeling of lightness in the head, headache; infrequently - ageusia, dizziness, dysgeusia; rarely - imbalance, tremor; frequency unknown - impaired psychomotor reactions, cerebral ischemia, cerebrovascular accident (transient), ischemic stroke, paresthesia, parosmia;
- Digestive system: often - discomfort in the abdomen, nausea, vomiting, inflammatory reactions in the stomach and intestines, dyspepsia, diarrhea, indigestion; infrequently - abdominal pain, pancreatitis (in rare cases with a fatal outcome), intestinal angioedema, dryness of the oral mucosa, increased activity in the blood plasma of pancreatic enzymes, gastritis, constipation; rarely - glossitis; frequency unknown - aphthous stomatitis;
- Mental disorders: infrequently - anxiety, drowsiness, depressed mood, nervousness, sleep disturbances, motor restlessness; rarely - confusion of consciousness; frequency unknown - attention disorders;
- Hearing organ: rarely - ringing in the ears, hearing impairment;
- Organ of vision: infrequently - blurred image, visual impairment; rarely - conjunctivitis;
- Hepatobiliary system: infrequently - an increase in the content of conjugated bilirubin in the blood plasma, an increase in the activity of hepatic enzymes; rarely - hepatocellular lesions, cholestatic jaundice; frequency unknown - acute hepatic failure, cytolytic or cholestatic hepatitis (extremely rarely fatal);
- Urinary system: infrequently - functional kidney disorder, development of acute renal failure, increased urine output, increased proteinuria (pre-existing), increased content of creatinine and urea in the blood;
- Lymphatic system and blood system: infrequently - eosinophilia; rarely - neutropenia, leukopenia, agranulocytosis, a decrease in the content of erythrocytes in the peripheral blood, a decrease in the level of hemoglobin concentration, leukocytosis, thrombocytopenia; frequency unknown - pancytopenia, hemolytic anemia, inhibition of bone marrow hematopoiesis;
- Breasts and reproductive system: infrequently - transient impotence, decreased libido; frequency unknown - gynecomastia;
- Musculoskeletal system: often - myalgia, muscle cramps; infrequently - arthralgia;
- Dermatological reactions: often - skin rash, infrequently - hyperhidrosis, pruritus, angioedema (including fatal); rarely - onycholysis, urticaria, exfoliative dermatitis; very rarely - photosensitivity; frequency unknown - erythema multiforme, toxic epidermal necrolysis, pemphigus, Stevens-Johnson syndrome, psoriasis-like dermatitis, aggravation of the course of psoriasis, alopecia, lichenoid or pemphigoid exanthema or enanthema;
- Immune system: frequency unknown - anaphylactoid or anaphylactic reactions (including to insect poisons), increased levels of antinuclear antibodies;
- Metabolism, laboratory parameters, nutrition: often - an increase in the level of potassium in the blood serum; infrequently - decreased appetite, anorexia; frequency unknown - decrease in blood sodium levels;
- General disorders: often - feeling tired, chest pain; infrequently - an increase in body temperature; rarely asthenia.
Overdose
Symptoms of an overdose of Ramipril are thromboembolic complications, acute arterial hypotension, angioedema, cerebrovascular accident, myocardial infarction.
As a treatment, it is necessary to reduce the dose or completely cancel the drug, rinse the stomach and transfer the patient to a horizontal position. Also, measures are taken to increase the BCC (administration of isotonic sodium chloride solution, transfusion of other blood-substituting fluids) and symptomatic therapy is prescribed, including subcutaneous or intravenous administration of epinephrine, intravenous administration of hydrocortisone, and taking antihistamines.
special instructions
According to the instructions, Ramipril should be prescribed only after a thorough assessment of the patient's renal function. Treatment should be accompanied by monitoring of renal function, especially in patients with renal vascular disease.
Before and during the period of use of Ramipril, regular monitoring of blood pressure, renal function (urea, creatinine), levels of potassium and other electrolytes, hemoglobin, and liver enzyme activity is required.
The first intake and each dose increase should be carried out under the supervision of a physician, this will avoid the development of uncontrolled hypotension and other undesirable effects.
Patients with malignant arterial hypertension are recommended to start treatment in a hospital setting.
In case of an increase in the concentration of creatinine and urea in the blood serum in patients with impaired renal function, it is necessary to reduce the dose or cancel the drug, since hyperkalemia may develop.
With significant activity of liver enzymes or jaundice, the use of Ramipril should be canceled.
If transient arterial hypotension occurs, the drug should be temporarily discontinued, after stabilization of blood pressure, treatment can be continued, the repetition of severe hypotension is the basis for dose reduction or drug withdrawal.
In case of planned surgery, including dental surgery, the patient should inform the surgeon and the anesthesiologist about the treatment with ramipril in order to prevent a sharp decrease in blood pressure by means of general anesthesia. It is recommended to stop taking pills 12 hours before the start of the operation.
During treatment, it is necessary to regularly monitor the level of blood leukocytes for the timely detection of the possible development of agranulocytosis or neutropenia.
The risk of developing hyperkalemia in patients with arterial hypertension increases with chronic heart failure, the appointment of potassium preparations, the simultaneous administration of amiloride, spironolactone, triamterene (potassium-sparing diuretics).
If the patient develops abdominal pain with nausea and vomiting during the differential diagnosis, the possibility of developing intestinal angioedema should be considered.
In the case of desensitizing therapy for poisonous insect bites, ACE inhibitors must be replaced with antihypertensive drugs from other groups.
The appearance of a dry cough during the treatment period may be associated with taking the drug.
Patients are advised to avoid physical activity and exposure to high air temperatures.
During the period of taking Ramipril, patients should not drive vehicles and mechanisms.
Drug interactions
When prescribing Ramipril, the doctor should warn the patient about the need for prior consultation before starting the simultaneous use of any drugs.
Analogs
Ramipril analogs are: Ramipril-SZ, Vasolong, Amprilan, Dilaprel, Hartil, Corpril, Pyramil, Ramigamma, Tritace, Ramikardia.
Terms and conditions of storage
Store at temperatures up to 25 ° C out of reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Ramipril
Many patients leave positive reviews about Ramipril when treating with the original drug, and not with cheaper analogues. However, in some cases, they complain that the drug has a wide range of side effects.
Ramipril price in pharmacies
In most cases, the price of Ramipril with a dosage of 2.5 mg does not exceed 104–120 rubles (30 pcs per pack). A drug with a dosage of 5 mg can be purchased for 120–135 rubles, and with a dosage of 10 mg for 136–155 rubles (30 pcs per pack).
Ramipril: prices in online pharmacies
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Drug name Price Pharmacy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
