Gopten - instructions for use. Trandolapril: instructions for use and special recommendations Indications for use

ACE inhibitors are most commonly used to treat heart failure and hypertension.

Among the ACE inhibitors is the substance trandolapril.

This component, which has a hypotensive and vasodilating effect, is included in the composition of drugs for the secondary prevention of heart failure after myocardial infarction, treatment of hypertension and heart failure.

Trandolapril-based medicines are prescribed for adult patients. Prescription drugs are available from pharmacies.

pharmachologic effect

It is an ACE inhibitor. It has a vasodilating and hypotensive effect. It helps to suppress the formation of angiotensin II, reduce the release of aldosterone.

Expands veins to a lesser extent than arteries. Reduces post- and preload, BP, OPSS. There is no reflex increase in the heart rate. Increases the synthesis of propylene glycol, reduces the degradation of bradykinin.

There is no connection between plasma renin activity and the hypotensive effect: with normal or reduced hormone concentration, blood pressure decreases, which is due to the effect on tissue renin-angiotensin systems. With prolonged use, the severity of myocardial hypertrophy, the walls of resistive arteries, decreases.

Strengthens renal, coronary blood flow. It leads to an improvement in the blood supply to the ischemic myocardium. Increases the concentration of phosphocreatine in the reperfusion ischemic zones of the myocardium.

Delays the excretion of potassium, increases urine output. Reduces platelet aggregation. In people who have had myocardial infarction, it slows down the development of LV dysfunction. In patients with CHF, it increases life expectancy.

A noticeable decrease in blood pressure is observed within two days.

Absorption from the gastrointestinal tract is rapid. Bioavailability does not change when consumed with food. It is excreted in mother's milk. It is excreted by the kidneys (33%) and through the intestines (67%).

Indications for use

Trandolapril is prescribed for the treatment of CHF (as a component of combination therapy), arterial hypertension, as well as for the secondary prevention of heart failure after myocardial infarction.

Method of reception

Trandolapril capsules are taken regardless of the time of meals, with a liquid. Swallow them whole. No matter how many mg of Trandolapril the doctor prescribes, the drug is taken once a day at the same time.

A specialist should select an individual dose of the drug.

Arterial hypertension

LV dysfunction after myocardial infarction

In persons with hypertension who do not take diuretics, with normal liver and kidney function in the absence of CHF, the recommended starting dose ranges from 0.5 to 2 mg per day. The starting dose for black patients is usually 2 mg. The 0.5 mg dose has been effective in only a few people. You can double the dose after one to four weeks of therapy. The dose may be increased up to a maximum of 4-8 mg / day. In the absence of an effect or an adequate response to the drug at a dose of 4-8 mg / day, the possibility of combined treatment with calcium channel blockers and / or diuretics should be considered.

Treatment can be started from the third day after acute myocardial infarction. The therapy is started with 0.5-1 mg / day, after which the single daily dose is gradually increased to 4 mg. If therapy is poorly tolerated (the limiting point is the development of arterial hypotension), you can temporarily stop increasing the dose. With concomitant treatment with vasodilators, including diuretics and nitrates, the development of hypotension is a reason to reduce their dosage. As for the dosage of Trandolapril, it is reduced if it is impossible to change the concomitant treatment or if therapy is ineffective.

Release form, composition

Available in capsules or tablets. The active ingredient is trandolapril.

Interaction with other drugs

The effect of Trandolapril is enhanced by alcoholic beverages, diuretics, and other antihypertensive drugs, including beta-blockers.

NSAIDs, estrogens and drugs that activate the renin-angiotensin-aldosterone system weaken the effect of Trandolapril.

Myelodepressants increase the likelihood of agranulocytosis and / or lethal neutropenia; procainamide and allopurinol - neutropenia.

Potassium-sparing diuretics (triamterene, amiloride, spironolactone, etc.), potassium supplements and other potassium-containing agents, salt substitutes, and cyclosporine increase the likelihood of hyperkalemia.

Antacids enhance absorption.

Trandolapril potentiates the depressing effect of alcohol on the central nervous system, increases the toxic effect of lithium by increasing its concentration, reduces hypokalemia caused by diuretics and the symptoms of hyperaldosteronism.

Side effects

Blood (hemostasis, hematopoiesis), CCC	chest pain, a sharp decrease in blood pressure (especially when treated with diuretics, impaired water-salt metabolism), tachy- and bradycardia, palpitations, angina pectoris, decreased hematocrit and hemoglobin levels, neutro- and / or leukopenia, arrhythmias, myocardial infarction, agranulocytosis, anemia (sometimes hemolytic), thrombocytopenia, eosinophilia.
Sensory organs, nervous system	headaches, depression, dizziness, fainting, cerebral stroke, visual impairment, paresthesia, convulsions, imbalance and / or sleep, loss of taste.
Skin	psoriatic skin changes, bullous pemphigus, alopecia, allergic skin reactions, photosensitivity, rash.
Gastrointestinal tract	dyspepsia, glossitis, vomiting, abdominal pain, impaired hepatic function (fatal fulminant necrosis of the liver, cholestatic jaundice), constipation or diarrhea, pancreatitis, hepatitis, dry mouth, intestinal obstruction.
Respiratory system	dry cough, bronchospasm, sinusitis, infections of the lower and upper respiratory tract, dyspnea, rhinitis, bronchitis.
Genitourinary system	weakening of libido, impaired renal function (proteinuria, acute renal failure), impotence, edema.
Locomotor apparatus	arthralgia, convulsions, myalgia, arthritis.
Others	angioedema, hyponatremia, hyperproteinemia, development of infections, uratemia, hyperkalemia, increased concentration of bilirubin, creatinine, liver enzymes in the blood serum.

Overdose

Manifested by angioedema and acute arterial hypotension.

It is treated with a complete cancellation of the drug or a decrease in its dose, gastric lavage, transferring the patient to a horizontal position, taking measures to increase the BCC (transfusion of other blood-substituting fluids, administration of a physiological solution.

Symptomatic therapy involves the introduction of hydrocortisone (IV), epinephrine (IV or SC), as well as the appointment of antihistamines.

Contraindications

Trandolapril is not prescribed for pregnant women, people with hypersensitivity to trandolapril or other ACE inhibitors, nursing patients.

Caution requires the use of medication for:

During pregnancy

Prescribing to pregnant patients is unacceptable.

During therapy, breastfeeding is stopped.

Conditions and shelf life

Stored at temperatures up to 30 degrees for three years.

Price

The cost of a medicine is determined by its trade name. The approximate price of drugs containing trandolapril in Russia, is 500 p. per packing.

Preparations containing trandolapril, in Ukraine sold at a price of 60 to 850 UAH. for one pack.

Analogs

Analogs of Trandolapril include Gopten, Trandolapril Ratiopharm, as well as the combined drug Tarka, which additionally contains verapamil.

Gross formula

C 24 H 34 N 2 O 5

Pharmacological group of the substance Trandolapril

Nosological classification (ICD-10)

CAS code

87679-37-6

Characteristics of the substance Trandolapril

Colorless crystalline substance, soluble in chloroform, dichloromethane and methanol.

Pharmacology

pharmachologic effect - antihypertensive, vasodilatory, natriuretic, cardioprotective.

It inhibits ACE and inhibits the formation of angiotensin II, which has a vasoconstrictor effect. Reduces OPSS, systemic blood pressure and afterload on the myocardium, helps to reduce vascular hypertrophy (aorta, mesenteric and femoral arteries). By inhibiting the tissue renin-angiotensin system of the heart, it prevents the development of myocardial hypertrophy and left ventricular dilatation or promotes their regression (cardioprotective effect). Increases the level of phosphocreatinine in the ischemic reperfusion zones of the myocardium. Suppresses the synthesis of aldosterone in the adrenal glands, stabilizes bradykinin in tissues and blood (its degradation to inactive peptides decreases), increases the activity of the kallikrein-kinin system, increases the release of biologically active substances (PGE 2 and PGI 2, endothelial relaxing factor, atrial natriuretic factor), which provide natriuretic and vasodilating action and improving renal blood flow. Reduces the formation of arginine-vasopressin and endothelin-1, which have vasoconstrictor properties. The maximum inhibition of ACE in plasma is recorded after 2-4 hours, and after 24 hours, the enzyme activity remains 80% lower than the initial one. The antihypertensive effect develops approximately 1 hour after administration, reaches a maximum after 8-12 hours, lasts up to 24-36 hours. After discontinuation of therapy, ACE activity in the blood, lungs, heart and kidneys is normalized within 1 week, while in the wall arteries, it remains low for a long time. The high efficiency is due to the formation of a diacid metabolite (trandolaprilat), which is 2200 times more active than trandolapril. In patients with postinfarction left ventricular dysfunction (ejection fraction 35% or less), after a dose of 4 mg / day for 24-50 months, there was a decrease in overall mortality and mortality from cardiovascular diseases by 22 and 25%, the risk of developing severe heart failure by 29% and sudden death by 24%. According to calculations, life expectancy in this category of patients increases by an average of 15 months (27%). However, a significant improvement in survival after myocardial infarction was recorded only in patients with baseline blood pressure more than 125/90 mm Hg.

In experiments on mice and rats using doses up to 25 mg / kg / day and up to 8 mg / kg / day, respectively, no signs of carcinogenicity were found. Does not possess mutagenic and genotoxic properties. At doses up to 100 mg / kg / day (1250 times higher than the MRDC), it has no adverse effect on fertility in rats. When used in rabbits doses of 0.8 mg / kg / day, in rats - 1000 mg / kg / day and in monkeys - 25 mg / kg / day (10, 1250 and 312 times higher than the MRDC, respectively), no teratogenic effect was revealed ... However, it should be borne in mind that the appointment of other ACE inhibitors during pregnancy can cause an increase in fetal and neonatal mortality, and the introduction in the II and III trimesters of pregnancy is accompanied by a decrease in the mass of the placenta, a delay in skeletal ossification, the development of oligohydramnios (due to a decrease in renal function), anuria, renal failure in the fetus, up to death, hypoplasia of the lung tissue, contractures of the limbs and craniofascial deformities, non-closure of the Botallov duct and toxic effects on the mother's body.

After oral administration, it is rapidly absorbed from the gastrointestinal tract. The absolute bioavailability is 10% for trandolapril and about 40-60% for trandolaprilat. C max trandolapril is achieved after 1 hour, trandolaprilat - after 4-10 hours. It binds to plasma proteins by 80% (trandolapril) and 94% (trandolaprilat). It undergoes hydrolysis (deesterification) in the gastrointestinal tract and liver mucosa with the formation of active trandolaprilate, which has a pronounced lipophilicity, which causes a decrease in ACE activity not only in the blood, but also in the lungs, kidneys, and especially in the heart and adrenal glands. The plasma concentration decreases rapidly, T 1/2 is 0.7-1.3 hours. Trandolaprilat is excreted in 2 or 3 phases: T 1 / 2alpha is 3.3-4.5 hours, T 1 / 2beta is 16-24 h. Terminal T 1/2 of trandolaprilate exceeds 100 hours (probably reflects elimination after dissociation from the complex with membrane ACE). It is excreted from the body with bile (2/3) and urine (1/3). Against the background of renal failure, correction of the dosage regimen is necessary: \u200b\u200bat a glomerular filtration rate of less than 30 ml / min and against the background of hemodialysis, the initial and maintenance dose is reduced by 2 times. With severe liver damage, plasma concentrations of trandolapril are about 10 times higher than those in healthy people. Pharmacokinetic parameters do not depend on the patient's age.

Application of the substance Trandolapril

Arterial hypertension (mono- and combination therapy), heart failure (adjunctive treatment).

Contraindications

Hypersensitivity, a history of angioedema when using ACE inhibitors, pregnancy, breastfeeding.

Restrictions on use

Assessment of the risk-benefit ratio is necessary in the presence of an autoimmune disease (systemic lupus erythematosus, scleroderma, and other systemic collagenoses); violation of cerebral or coronary circulation; severe heart failure; aortic and mitral stenosis; hypertrophic cardiomyopathy; diabetes mellitus; dehydration of the body; hyponatremia; carrying out dialysis procedures; bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney; the presence of a transplanted kidney; impaired liver and kidney function; childhood (safety and effectiveness have not been determined).

Application during pregnancy and lactation

Contraindicated in pregnancy.

During treatment, breastfeeding should be discontinued.

Side effects of the substance Trandolapril

On the part of the cardiovascular system and blood (hematopoiesis, hemostasis): a sharp decrease in blood pressure (especially in patients with impaired water-salt metabolism, when treated with diuretics), chest pain, palpitations, brady- or tachycardia, arrhythmia, angina pectoris, myocardial infarction, a decrease in hemoglobin levels, hematocrit, leuko- and / or neutropenia , agranulocytosis, thrombocytopenia, anemia (in some cases - hemolytic), eosinophilia.

From the nervous system and sensory organs: dizziness, headache, fainting, depression, sleep and / or balance disturbance, cerebral stroke, paresthesia, loss of taste, visual impairment, convulsions.

From the digestive tract: glossitis, dry mouth, dyspepsia, vomiting, diarrhea or constipation, abdominal pain, liver dysfunction (cholestatic jaundice, fatal fulminant liver necrosis), hepatitis, pancreatitis, intestinal obstruction.

From the side of the skin: allergic skin reactions, psoriatic skin changes, rash, bullous pemphigus, photosensitivity, alopecia.

From the genitourinary system: impaired renal function (acute renal failure, proteinuria), edema, weakening of libido, impotence.

From the respiratory system: dry cough, dyspnea, bronchospasm, bronchitis, sinusitis, rhinitis, upper and lower respiratory tract infections.

From the side of the musculoskeletal system: myalgia, arthralgia, arthritis, convulsions.

Others: development of infections, angioedema, hyperkalemia, hyponatremia, uratemia, hyperproteinemia, increased concentration of creatinine, bilirubin and liver enzymes in the blood serum.

Interaction

The effect is enhanced (additive effect) by other antihypertensive drugs, including beta-blockers, incl. with significant systemic absorption from ophthalmic dosage forms, diuretics, alcohol; weaken - estrogens, NSAIDs, sympathomimetics, agents that activate the renin-angiotensin-aldosterone system. Potassium-sparing diuretics (spironolactone, amiloride, triamterene, etc.), cyclosporine, potassium supplements, salt substitutes, and other potassium-containing agents increase the risk of hyperkalemia. Myelodepressants increase the likelihood of lethal neutropenia and / or agranulocytosis; allopurinol and procainamide - neutropenia. Antacids enhance absorption. It potentiates the depressing effect of alcohol on the central nervous system, reduces the signs of hyperaldosteronism and hypokalemia caused by diuretics, increases the toxic effect (increases the concentration) of lithium.

Overdose

Symptoms: acute arterial hypotension, angioedema.

Treatment: dose reduction or complete withdrawal of the drug; gastric lavage, transferring the patient to a horizontal position, taking measures to increase the BCC (administration of saline, transfusion of other blood-substituting fluids), symptomatic therapy: epinephrine (s / c or i / v), antihistamines, hydrocortisone (i / v).

Route of administration

Inside.

Precautions for the substance Trandolapril

Treatment is carried out under regular medical supervision. To reduce the risk of symptomatic hypotension 1 week before starting treatment, antihypertensive therapy should be discontinued, incl. the appointment of diuretics (or significantly reduce the dose of the latter) and adjust the water-electrolyte balance. During therapy, it is necessary to monitor blood pressure, the composition of peripheral blood (before starting it, the first 3-6 months of therapy and then at periodic intervals up to 1 year, especially in patients with an increased risk of neutropenia), the level of protein, plasma potassium, urea nitrogen, creatinine, kidney function, body weight, diet. With the development of cholestatic jaundice and the progression of fulminant necrosis of the liver, treatment should be discontinued. Caution is required when performing surgical interventions (including dental), especially when using general anesthetics that have a hypotensive effect. Avoid hemodialysis through high-performance membranes made of polyacrylonitrile metaallyl sulfate (for example AN69), hemofiltration or LDL-apheresis (anaphylaxis or anaphylactoid reactions may develop). Hyposensitizing therapy may increase the risk of anaphylactic reactions. During treatment, it is recommended to exclude the use of alcoholic beverages. Use with caution during work for drivers of vehicles and people whose profession is associated with increased concentration of attention.

Part of preparations

ATX:

C.09.B.B.10 Verapamil and tradolapril

C.09.B.B ACE inhibitors in combination with calcium channel blockers

Pharmacodynamics:

The combination of substances has an antihypertensive effect.

Trandolapril

Trandolapril inhibits the activity of the renin-angiotensin-aldosterone system of blood plasma. Renin is an enzyme that is synthesized by the kidneys and enters the bloodstream, where it causes the conversion of angiotensinogen to angiotensin I (an inactive decapeptide). The latter turns under the influence(peptidyldipeptidase) into angiotensin II - a powerful vasoconstrictor that causes narrowing of the arteries and an increase in blood pressure, as well as stimulating the secretion of aldosterone by the adrenal glands.

Inhibition angiotensin converting enzymeleads to a decrease in the concentration of angiotensin II in the blood plasma, which is accompanied by a decrease in vasopressor activity and the secretion of aldosterone. Although aldosterone production is not significantly reduced, a slight increase in serum potassium concentration may be observed in combination with sodium and water loss.

A decrease in the level of angiotensin II by a feedback mechanism leads to an increase in renin activity in the blood plasma. Another functionangiotensin converting enzymeis the destruction of kinins (bradykinin), which have a powerful vasodilating property, to inactive metabolites. In this regard, suppressionangiotensin converting enzymeleads to an increase in circulating and tissue levels of kallikrein-kinins, which promotes vasodilation by activating the systemprostaglandins. This mechanism may partially determine the hypotensive effect of inhibitors.angiotensin converting enzymeand causes some side effects.

In patients with arterial hypertension, the use of inhibitorsangiotensin converting enzymeleads to a comparable decrease in blood pressure in the sitting and standing positions without compensatory increase heart rate... Peripheral vascular resistance decreases, cardiac output does not change or increases, renal blood flow increases, and glomerular filtration rate usually does not change. Abrupt discontinuation of therapy is not accompanied by a rapid increase in blood pressure. The hypotensive effect of trandolapril appears 1 hour after administration and lasts for at least 24 hours. In some cases, optimal blood pressure control can be achieved only a few weeks after the start of treatment. With prolonged therapy, the hypotensive effect persists. does not worsen the circadian profile of blood pressure.

Verapamil

Verapamil blocks the transmembrane flow of calcium ions into smooth muscle cells of the myocardium and coronary vessels. causes a decrease in blood pressure both at rest and during exercise due to the expansion of peripheral arterioles. As a result of the decrease(afterload) decreases myocardial oxygen demand and energy consumption. reduces myocardial contractility. The negative inotropic effect of the drug can be offset by a decreasetotal peripheral vascular resistance... The cardiac index does not decrease, except in patients with left ventricular dysfunction.

Verapamil does not affect the sympathetic regulation of cardiac activity, since it does not block beta-adrenergic receptors.

Pharmacokinetics:

Trandolapril

Suction

After oral administration, it is rapidly absorbed. The absolute bioavailability is about 10%. T max in blood plasma about 1 hour.

Distribution

The binding of trandolapril to blood plasma proteins is about 80% and does not depend on the concentration. V d trandolapril about 18 liters. Half-life< 1 ч. При многократном применении C ss достигается примерно через 4 дня, как у здоровых добровольцев, так и у пациентов молодого и пожилого возраста с артериальной гипертонией.

Metabolism

In blood plasma, it undergoes hydrolysis to the formation of an active metabolite trandolaprilate. T max of trandolaprilat in blood plasma is 4-10 hours. C max or AUC do not depend on food intake. The absolute bioavailability of trandolaprilat is about 70%. Binding to blood proteins depends on the concentration and varies from 65% at a concentration of 1000 ng / ml to 94% at a concentration of 0.1 ng / ml. Trandolaprilat has a high affinity forangiotensin converting enzyme.

Withdrawal

The renal clearance of trandolaprilat varies from 1 to 4 l / h depending on the dose. At C ss, the effectivehalf-lifetrandolaprilat, together with a small fraction of the drug taken, varies between 16 hours and 24 hours, which probably reflects binding to plasma and tissueangiotensin-converting enzyme... In the form of trandolaprilat, 10-15% of the dose of trandolapril is excreted by the kidneys,< 0,5 % дозы выводится почками в неизмененном виде. После приема меченого трандолаприла внутрь 33 % радиоактивности обнаруживают в моче и 66 %-в фекалиях.

The pharmacokinetics of trandolapril have not been studied in children under 18 years of age.

The concentration of trandolapril in blood plasma increases in elderly patients (over 65 years old). However, the plasma concentration of trandolaprilate and its ACE-inhibiting activity in elderly patients with arterial hypertension of both sexes are the same.

Renal failureCompared to healthy volunteers in hemodialysis patients and with creatinine clearance< 30 мл/мин плазменная концентрация трандолаприлата примерно в 2 раза выше, а почечный клиренс снижен приблизительно на 85 %.

Liver failure.Compared to healthy volunteers, in patients with non-severe alcoholic cirrhosis of the liver, the plasma concentration of trandolapril and trandolaprilat increases by 9 and 2 times, respectively, but the ACE inhibitory activity does not change.

Verapamil

Suction

After oral administration, about 90-92% of the dose of verapamil is rapidly absorbed in the small intestine. Bioavailability is only 22% due to the pronounced "first pass" effect through the liver. With repeated use, the average bioavailability can increase up to 30%. The time to reach C max in plasma is 4-15 hours.

Distribution

C ss with repeated use 1 time per day is achieved in 3-4 days. Plasma protein binding is about 90%.

Metabolism

One of the 12 metabolites found in urine is norverapamil, the pharmacological activity of which is 10-20% of that of verapamil; its share is 6% of the excreted drug. C ss norverapamil and verapamil are similar.

Withdrawal

Half-life with repeated use, it is on average 8 hours. 3-4% of the dose is excreted by the kidneys unchanged. Metabolites are excreted by the kidneys (70%) and through the intestines (16%).

Pharmacokinetics in special clinical situations

The pharmacokinetics of verapamil does not change with impaired renal function. Impaired renal function does not affect the excretion of verapamil.

Bioavailability andhalf-life verapamil increases in patients with liver cirrhosis. However, the pharmacokinetics of verapamil remains unchanged in patients with compensated liver dysfunction.

Indications:

Essential arterial hypertension (in patients for whom combination therapy is indicated).

IX.I10-I15.I10 Essential [primary] hypertension

IX.I10-I15.I15 Secondary hypertension

Contraindications:

History of angioedema associated with treatment with inhibitorsangiotensin converting enzyme;

Cardiogenic shock;

Chronic heart failure stage IIB and III;

Simultaneous use of beta-blockers;

AV block II and III degree (except for patients with an artificial pacemaker);

Acute myocardial infarction;

- sick sinus syndrome (except for patients with an artificial pacemaker);

Acute heart failure

Atrial fibrillation / flutter;

Wolff-Parkinson-White syndrome;

Laun-Ganong-Levin syndrome;

Severe bradycardia;

Severe arterial hypotension;

Renal dysfunction (creatinine clearance< 30 мл/мин.);

Pregnancy;

Breastfeeding period;

Age up to 18 years (efficacy and safety have not been established);

Known hypersensitivity to any component of the drug or to any other inhibitorangiotensin converting enzyme.

Carefully:

The drug should be used with caution in aortic stenosis, hypertrophic obstructive cardiomyopathy, impaired liver and / or kidney function, systemic connective tissue diseases (including systemic lupus erythematosus, scleroderma), inhibition of bone marrow hematopoiesis, AV-blockade of the 1st degree, bradycardia, arterial hypotension , conditions accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting), bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney, condition after kidney transplantation, in patients on a salt-restricted diet who are on hemodialysis, when used in combination with diuretics ...

Pregnancy and lactation:

The use of the drug during pregnancy and lactation is contraindicated.

The safety of using the drug in pregnant women has not been established. There are separate observations of pulmonary hypoplasia in newborns, intrauterine growth retardation, patent ductus arteriosus and cranial hypoplasia after using inhibitors.angiotensin converting enzyme during pregnancy. Inhibitorsangiotensin converting enzyme can cause arterial hypotension, accompanied by anuria in the fetus or newborn, or oligohydroamnion.

The risk of teratogenic effects is highest with the administration of inhibitorsangiotensin converting enzyme in the II and III trimesters of pregnancy. Information about possible teratogenicity or embryo / fetotoxicity of inhibitorsangiotensin converting enzyme in the first trimester of pregnancy is not available.

Verapamil is excreted in breast milk. During treatment with the drug, breastfeeding should be stopped.

Method of administration and dosage:

1 capsule (trandolapril 2 mg + verapamil 180 mg) once a day. The drug should be taken orally, preferably in the morning after meals. The capsule is swallowed whole with water.

Side effects:

Headache, dizziness; AV block I degree; increased cough; constipation, asthenia.

Infections: bronchitis.

System side hematopoiesis: leukopenia, neutropenia, lymphopenia, thrombocytopenia.

On the part of metabolism and nutrition: hyperkalemia, hyponatremia.

From the nervous system: balance disorders, insomnia, drowsiness, fainting, hypesthesia, paresthesia, anxiety, thought disorder.

On the part of the organ of vision: visual impairment, "fog in front of the eyes".

On the part of the organ of hearing and vestibular apparatus: dizziness, tinnitus.

complete AV block, angina pectoris, bradycardia, palpitations, tachycardia, bundle branch block, acute myocardial infarction, ventricular extrasystole, nonspecific changes in the ST-T segment on the ECG, marked decrease in blood pressure, "hot flushes" of blood to the face.

From the respiratory system: shortness of breath, sinus congestion.

From the digestive tract: nausea, diarrhea, dyspepsia, indigestion, dry mouth.

angioedema, pruritus, rash.

arthralgia, myalgia, gout (hyperuricemia).

frequent urination, polyuria, hematuria, proteinuria, nocturia.

From the reproductive system: impotence, endometriosis.

General and local reactions: chest pain, peripheral edema, fatigue.

Laboratory indicators: increased hepatic enzymes and / or bilirubin, serum creatinine, residual urea nitrogen.

Significant adverse events observed with verapamil

On the part of the cardiovascular system: AV blockade of I, II, III degrees, stopping the sinus node, AV dissociation, intermittent claudication, the onset or aggravation of heart failure, angina pectoris, arrhythmia, pulmonary edema, tachycardia, bradycardia, severe arterial hypotension, "hot flushes" of blood to the face.

From the nervous system: acute disturbance of cerebral circulation, confusion, drowsiness, psychotic symptoms, tremor, headache, dizziness, paresthesia.

On the part of the organ of hearing and balance: dizziness.

From the digestive tract: gingival hyperplasia, abdominal pain or discomfort, reversible non-obstructive intestinal obstruction, nausea, vomiting, constipation.

On the part of the skin and subcutaneous fat: angioedema, Stevens-Johnson syndrome, urticaria, purpura, pruritus, ecchymosis, bruising, hair loss, hyperkeratosis, increased sweating, erythema multiforme, maculopapular rash.

From the musculoskeletal system: muscle weakness, myalgia, arthralgia.

On the part of the reproductive system and mammary glands: gynecomastia, galactorrhea, impotence.

Immune disorders: hypersensitivity, allergic reactions.

From the kidneys and urinary tract: increased urination.

General reactions: peripheral edema, fainting, fatigue.

Laboratory indicators: hyperprolactinemia, increased activity of hepatic transaminases.

Significant adverse events observed with trandolapril

From the hematopoietic system: agranulocytosis.

From the digestive tract: vomiting, abdominal pain, pancreatitis.

On the part of the skin and subcutaneous fat: alopecia.

Immune disorders: hypersensitivity.

From the genitourinary system: decreased libido.

Common symptoms: fever.

Adverse events that have been reported with all inhibitors angiotensin converting enzyme

From the side of the central nervous system: transient cerebrovascular accident, headache.

On the part of the cardiovascular system: myocardial infarction, cardiac arrest, cerebral hemorrhage, arterial hypotension.

On the part of the skin and subcutaneous fat: exudative erythema multiforme, toxic epidermal necrolysis, angioedema, rash.

From the kidneys and urinary tract: acute renal failure.

Others: chest pain, cough.

Laboratory indicators: pancytopenia, decreased hemoglobin and hematocrit, neutropenia, agranulocytosis, hyperkalemia.

Overdose:

In clinical studies, the maximum dose of trandolapril was 16 mg. At the same time, there were no signs of his intolerance.

verapamil: marked reduction in blood pressure, AV blockade, bradycardia, asystole. Overdose deaths have been reported.

In case of an overdose of the drug, the following symptoms are possible caused by trandolapril: marked decrease in blood pressure, shock, stupor, bradycardia, electrolyte disturbances, renal failure.

Treatment: symptomatic. Treatment of an overdose of verapamil includes parenteral administration of calcium preparations, the use of beta-agonists, and gastric lavage. Given the slow absorption of the prolonged-release drug, the patient's condition should be monitored for 48 hours; hospitalization may be required during this period. not removed by hemodialysis.

Interaction:

Verapamil-mediated interactions

Research in vitro indicate that it is metabolized by the isoenzymes CYP3A4, CYP1A2, CYP2C8, CYP2C9 and CYP2C18.

Verapamil is a CYP3A4 inhibitor. A clinically significant interaction was noted with simultaneous use with CYP3A4 inhibitors, with an increase in the plasma level of verapamil, while CYP3A4 inducers reduced the concentration of verapamil in the blood plasma. Accordingly, the possibility of interaction should be taken into account when using such funds simultaneously.

Other possible interactions

With the simultaneous use of antiarrhythmics and beta-blockers with the drug, it is possible to increase the adverse effect on the cardiovascular system (more pronounced AV block, a more significant decrease in heart rate, development of heart failure and increased arterial hypotension).

With the simultaneous use of quinidine with the drug, the hypotensive effect is enhanced. Patients with hypertrophic obstructive cardiomyopathy may develop pulmonary edema.

With the simultaneous use of antihypertensive drugs, diuretics and vasodilators with the drug, the hypotensive effect is enhanced.

With simultaneous use with the drug prazosin, terazosin, the hypotensive effect is enhanced.

With simultaneous use with the drug, some drugs for the treatment of HIV infection () can inhibit the metabolism of verapamil, which leads to an increase in its concentration in the blood plasma. With the simultaneous use of the dose of verapamil should be reduced.

With the simultaneous use of carbamazepine with the drug, the level of carbamazepine in the blood plasma increases, which may be accompanied by the side effect characteristic of carbamazepine - diplopia, headache, ataxia or dizziness.

With the simultaneous use of lithium with the drug, the neurotoxicity of lithium increases.

With the simultaneous use of rifampicin with the drug, it is possible to reduce the hypotensive effect of verapamil.

With the simultaneous use of sulfinpyrazone with the drug, it is possible to reduce the hypotensive effect of verapamil.

With simultaneous use with the drug, the effect of muscle relaxants may increase.

With the simultaneous use of acetylsalicylic acid with verapamil, bleeding increases.

Patients receiving treatment with HMG-CoA reductase inhibitors (that is, simvastatin / lovastatin) should be started at the lowest possible dose with a gradual increase in the course of therapy. If it is necessary to prescribe to patients already receiving HMG-CoA reductase inhibitors, then their doses should be revised and reduced according to the serum cholesterol concentration. A similar tactic should be followed with the simultaneous appointment of verapamil with atorvastatin.

Fluvastatin, and are not metabolized by the CYP3A4 isoenzyme, so their interaction with verapamil is the least likely.

Interactions due to trandolapril

Diuretics or other antihypertensive drugs may enhance the antihypertensive effect of trandolapril. may reduce potassium loss when used together with thiazide diuretics.

Potassium-sparing diuretics (eg, amiloride, triamterene) or potassium preparations increase the risk of hyperkalemia when used concomitantly with trandolapril.

Concomitant use of trandolapril (as well as any inhibitorsangiotensin converting enzyme) with hypoglycemic agents (insulin or oral hypoglycemic agents) may increase the hypoglycemic effect and lead to an increased risk of hypoglycemia.

Trandolapril may impair lithium excretion. Serum lithium levels should be monitored.

Other interactions

When used simultaneously with verapamil, the concentration of colchicine in the blood can significantly increase, since the latter is a substrate for CYP3A and P-glycoprotein, which, in turn, inhibit the metabolism of verapamil.

In experiments on animals, it was shown that inhalation anesthetics reduce the flow of calcium into the cell, exerting a depressing effect on the cardiovascular system. With simultaneous use with verapamil, an increase in the inhibitory effect on the myocardium is possible.

The antihypertensive effect of some inhaled anesthetics can be enhanced by inhibitorsangiotensin converting enzyme.

When used during hemodialysis of high-flow polyacrylonitrile membranes in patients receiving inhibitorsangiotensin converting enzyme, anaphylactoid reactions have been described. In patients taking inhibitorsangiotensin converting enzymethe use of such membranes during hemodialysis should be avoided.

Non-steroidal anti-inflammatory drugsreduce the hypotensive effect of trandolapril.

Cytostatic or other immunosuppressive drugs andglucocorticosteroids increase the risk of developing leukopenia when used together with inhibitorsangiotensin converting enzyme.

Special instructions:

Patients with impaired liver function need careful monitoring during the period of drug treatment.

In patients with uncomplicated arterial hypertension after taking the first dose of trandolapril, as well as after its increase, the development of arterial hypotension was noted, accompanied by clinical symptoms. The risk of arterial hypotension is higher when the water-electrolyte balance is disturbed as a result of prolonged diuretic therapy, restriction of salt intake, dialysis, diarrhea or vomiting. In these patients, before starting trandolapril therapy, diuretic therapy should be discontinued and circulating blood volume and / or salt content should be replenished. It is necessary to monitor blood pressure especially carefully when prescribing or cancelingnonsteroidal anti-inflammatory drugs during the period of use of the drug. When treated with inhibitorsangiotensin converting enzyme described cases of agranulocytosis and suppression of bone marrow function. These adverse events are more common in patients with impaired renal function, especially with systemic connective tissue diseases. In such patients (for example, with systemic lupus erythematosus or scleroderma), it is advisable to regularly monitor the number of leukocytes in the blood and the protein content in the urine, especially in case of impaired renal function, treatment with glucocorticosteroids and cytostatic antimetabolites.

Trandolapril can cause angioedema of the face, tongue, pharynx and / or larynx.

It is part of the drug, therefore the use of the combined drug should be avoided in patients with severe left ventricular dysfunction (for example, with an ejection fraction< 30 %, повышением давления заклинивания легочных капилляров > 20 mmHg Art. or severe symptoms of heart failure) and in patients with any degree of left ventricular dysfunction if they receive a beta-blocker.

When examining patients with arterial hypertension, renal function should always be evaluated. Patients with chronic heart failure, bilateral renal artery stenosis or unilateral renal artery stenosis in patients with a single kidney (for example, after kidney transplantation) have an increased risk of impaired renal function, and in patients with renal failure, the risk of further deterioration of renal function.

In some patients with arterial hypertension who do not have kidney disease, when trandolapril is prescribed in combination with a diuretic, an increase in blood urea nitrogen and serum creatinine may be observed.

In patients with arterial hypertension, especially with impaired renal function, the drug may cause hyperkalemia.

During surgery or general anesthesia using drugs that cause arterial hypotension, it can block the formation of angiotensin II associated with compensatory renin release.

Care should be taken to select the dose of inhalation anesthetics when used simultaneously with verapamil.

With the simultaneous use of colchicine and verapamil, the development of tetraparesis was reported. Combined use is not recommended.

In some patients receiving diuretics, especially recently, after the appointment of trandolapril, a sharp decrease in blood pressure is observed.

Since there are no data on the interaction of verapamil and disopyramide, disopyramide should not be used within 48 hours before or 24 hours after taking verapamil.

Use in pediatrics

The use of the drug has not been studied in children under 18so its use in this age group is not recommended.

Influence on the ability to drive vehicles and use mechanisms

You should refrain from driving and operating machinery in the early stages of treatment, as the ability to drive or use complex equipment may deteriorate.

Instructions

Preparations containing Trandolapril (Trandolapril, ATC code C09AA10)

Gopten (Trandolapril) - official instructions for use. Prescription drug, information is intended only for healthcare professionals!

Clinical and pharmacological group:

Angiotensin Converting Enzyme (ACE) Inhibitor

pharmachologic effect

Non-peptide ACE inhibitor containing a carboxyl group, without a sulfhydryl group. After rapid absorption, trandolapril undergoes nonspecific hydrolysis to form trandolaprilate, a long-term circulating active metabolite. Trandolaprilat has a high affinity for ACE. Its interaction with this enzyme is a saturable process.

The use of the drug leads to a decrease in the concentration of angiotensin II, aldosterone and atrial natriuretic factor, as a result of which the activity of plasma renin and the concentration of angiotensin I increase.

Trandolapril, as a modulator of the RAAS, plays a significant role in the regulation of BCC and blood pressure, which to the greatest extent determines its antihypertensive effect.

The use of the drug in usual therapeutic doses in patients with arterial hypertension leads to a significant decrease in blood pressure, pre- and afterload on the heart. An obvious antihypertensive effect is observed already 1 hour after administration, reaches a maximum between 8 and 12 hours and lasts up to 24 hours.

Trandolapril reduces the severity of myocardial hypertrophy, slows down the progression of left ventricular dysfunction, which generally increases life expectancy in patients with heart failure.

Pharmacokinetics

Suction

After oral administration, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is 40-60% and does not depend on food intake. Cmax of trandolapril in blood plasma is noted after 30 minutes. Trandolapril very quickly disappears from the plasma, and its T1 / 2 is less than 1 hour. In plasma, trandolapril undergoes hydrolysis to trandolaprilat, which is an ACE inhibitor. The time to reach Cmax of trandolaprilat in plasma is 4-6 hours, and the amount of trandolaprilat formed does not depend on food intake.

Distribution

The binding of trandolaprilat to blood plasma proteins exceeds 80%. Most of the circulating trandoprilat binds to albumin; the binding is unsaturated.

When using the drug once a day, the equilibrium state in healthy volunteers, as well as young and elderly patients with arterial hypertension, is achieved after about 4 days.

Metabolism

It is metabolized in the liver with the formation of an active metabolite - trandolaprilate.

Withdrawal

The effective T1 / 2 is 16-24 hours, and the terminal T1 / 2 varies from 47 to 98 hours, depending on the dose. The terminal phase probably reflects the kinetics of the interaction of trandolapril with ACE and the dissociation of the resulting complex.

10-15% of a dose of trandolapril is excreted as unchanged trandolapril in the urine. After taking labeled trandolapril inside, 33% of radioactivity is found in urine and 66% in feces.

Pharmacokinetics in special clinical situations

The renal clearance of trandolaprilat is linearly correlated with CC. In patients with CC less than 30 ml / min, there is a significant increase in plasma trandolaprilat concentrations. With repeated use of the drug in patients with chronic renal failure, the equilibrium state is also achieved after 4 days, regardless of the degree of renal dysfunction.

Indications for the use of the drug GOPTEN®

• essential arterial hypertension;
• heart failure (secondary prevention after myocardial infarction with a decrease in the left ventricular ejection fraction on the 3rd day after its development).

Dosage regimen

Capsules should be taken with or without food, swallowed whole with plenty of fluids.

Regardless of the size of the dose, Gopten® is prescribed 1 time per day. The drug should be taken at the same time. The selection of an individual dose of the drug should be carried out by a doctor.

In patients with arterial hypertension, not taking diuretics, with normal renal and hepatic function and in the absence of chronic heart failure, the initial dose is from 0.5-1 mg to 2 mg per day. Only in a small number of patients was the 0.5 mg dose clinically effective. Doubling the dose is possible after 1-4 weeks of taking the drug to a maximum dose of 4-8 mg per day. If there is no effect on taking Gopten in doses of 4-8 mg per day, the possibility of combination therapy with diuretics and / or calcium channel blockers should be considered.

In patients with left ventricular dysfunction, treatment with Gopten can be started from 3 days after acute myocardial infarction. The initial dose is 0.5-1 mg per day, then a single daily dose is gradually increased to 4 mg. Depending on the tolerance of therapy (the limiting moment is the development of arterial hypotension), the dose increase can be temporarily stopped. The development of arterial hypotension with concomitant therapy with vasodilators, including nitrates and diuretics, causes a decrease in their dosage. The dose of Gopten should be reduced only in case of ineffectiveness or inability to change concomitant therapy.

In patients with chronic heart failure and arterial hypertension without or with impaired renal function, symptoms of arterial hypotension were observed after starting treatment with ACE inhibitors. In this group of patients, therapy should be started with taking Gopten at a dose of 0.5-1 mg per day in a hospital under close medical supervision.

In patients at risk of activation of the renin-angiotesin system (i.e., in patients with impaired water-salt metabolism), diuretics should be discontinued 2-3 days before the appointment of Gopten at a dose of 0.5 mg to reduce the possibility of arterial hypotension. Later, if necessary, diuretic therapy can be restarted.

In elderly patients with normal renal and hepatic function, dose adjustment is not required. With caution and under the control of blood pressure, the dose of Gopten should be increased in elderly patients with chronic heart failure, impaired liver and kidney function, taking diuretics.

In patients with moderate renal insufficiency (CC from 30 to 70 ml / min), it is recommended to take Gopten in the usual dose. With CC from 10 to 30 ml / min, the initial dose is 0.5 mg 1 time per day; the dose can be increased if necessary. With QC< 10 мл/мин начальная доза не должна превышать 0.5 мг в сутки, в дальнейшем доза не должна превышать 2 мг в сутки. Терапия Гоптеном у подобных больных должна проводиться под тщательным наблюдением врача.

The possibility of eliminating trandolapril or trandolaprilat during dialysis has not been precisely established, however, it can be expected that the concentration of trandolaprilat decreases during dialysis, which can lead to a loss of blood pressure control. Therefore, during dialysis, careful monitoring of blood pressure is recommended with possible adjustment (if necessary) of the dose of the drug.

In patients with severe hepatic impairment, due to a decrease in the metabolic function of the liver, an increase in the plasma level of both trandolapril and its active metabolite trandolaprilat (to a lesser extent) may be observed. Treatment begins with 0.5 mg per day, with close medical supervision.

Side effect

The table lists the adverse reactions that have been observed in long-term clinical studies of trandolapril. All reactions are distributed according to organ systems and frequency:

Other clinically significant adverse events reported in phase IV clinical trials or post-marketing practice:

From the hematopoietic system: agranulocytosis, leukopenia, pancytopenia.

Allergic reactions: hypersensitivity reactions, including itching and rash, angioedema.

From the respiratory system: dyspnea, bronchitis.

From the digestive system: nausea, vomiting, abdominal pain, diarrhea, dry mouth, increased activity of liver enzymes (including ACT and ALT).

Dermatological reactions: alopecia, increased sweating.

From the urinary system: increased residual urea nitrogen and serum creatinine.

Others: fever.

The following are the adverse events that have been reported with all ACE inhibitors:

From the hematopoietic system: pancytopenia.

From the side of the central nervous system: transient ischemic attacks, stroke.

From the side of the cardiovascular system: angina pectoris, myocardial infarction, AV blockade, bradycardia, cardiac arrest, tachycardia.

From the digestive system: pancreatitis.

Dermatological reactions: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the musculoskeletal system: myalgia.

On the part of laboratory tests: a decrease in the level of hemoglobin, a decrease in hematocrit.

Contraindications to the use of the drug GOPTEN®

• angioedema, incl. observed with previous treatment with ACE inhibitors;
• hereditary / idiopathic angioedema;
• pregnancy;
• lactation period (breastfeeding);
• children and adolescents up to 18 years old;
• hypersensitivity to the drug.

The drug should not be administered to patients with aortic stenosis or obstruction of the outflow tract of the left ventricle.

Use of the drug GOPTEN® during pregnancy and breastfeeding

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

It is necessary to exclude the presence of pregnancy before starting treatment with Gopten and avoid pregnancy during treatment. The use of ACE inhibitors in the middle or later stages of pregnancy led to oligohydramnios and neonatal hypotension, accompanied by anuria or renal failure.

Application for violations of liver function

In patients with hepatic impairment, treatment is started with a dose of 0.5 mg, and then, depending on clinical effectiveness, gradually increased.

Application for impaired renal function

In patients with moderate renal insufficiency (CC from 30 to 70 ml / min), it is recommended to take Gopten in the usual dose. With CC from 10 to 30 ml / min, the initial dose is 0.5 mg 1 time per day; it is gradually increased to 2 mg. With creatinine clearance<10 мл/мин начальная доза не должна превышать 0.5 мг в сутки, в дальнейшем доза не должна превышать 1 мг в сутки. Терапия Гоптеном у подобных больных должна проводиться под тщательным наблюдением врача.

special instructions

Trandolapril is a prodrug that converts to its active form in the liver, so special care must be taken in patients with impaired function, who should be closely monitored.

In patients with uncomplicated arterial hypertension after taking the first dose of Gopten, as well as after its increase, the development of arterial hypotension was noted, accompanied by clinical symptoms. The risk of developing hypotension is higher in patients with fluid and salt deficiencies resulting from prolonged diuretic therapy, salt restriction, dialysis, diarrhea or vomiting. In such patients, before starting therapy with Gopten, diuretic therapy should be discontinued and the BCC and / or salt content should be replenished.

When treated with ACE inhibitors, cases of agranulocytosis and bone marrow suppression have been described. These adverse events are more common with impaired renal function, especially in patients with diffuse connective tissue diseases. In such patients (for example, with SLE or systemic scleroderma), it is advisable to regularly monitor the number of leukocytes in the blood and the protein content in the urine, especially with impaired renal function and treatment with GCS and antimetabolites.

The use of trandolapril can cause angioedema of the face, extremities, tongue, pharynx and / or larynx.

In some patients receiving diuretics (especially recently), after the appointment of trandolapril, a sharp decrease in blood pressure is observed.

In severe renal failure, a dose reduction of trandolapril may be required; renal function should be closely monitored.

Patients with renal failure, chronic heart failure, bilateral renal artery stenosis, or unilateral arterial stenosis of a single functioning kidney are at increased risk of impaired renal function. In some patients with arterial hypertension without kidney disease, when trandolapril is prescribed in combination with a diuretic, an increase in blood urea nitrogen and serum creatinine levels may be observed. Proteinuria may occur.

Hyperkalemia may occur in patients with arterial hypertension with concomitant renal dysfunction while using Gopten.

During surgery or general anesthesia using drugs that cause arterial hypotension, trandolapril can block the secondary formation of angiotensin II associated with compensatory renin release.

When used during hemodialysis of highly permeable membranes of polyacrylonitrile in patients receiving ACE inhibitors, anaphylactoid reactions have been described. The use of such membranes should be avoided when prescribing ACE inhibitors to patients on hemodialysis.

Use in pediatrics

The safety and efficacy of Gopten in children has not been studied, therefore its use in children is not recommended.

Influence on the ability to drive vehicles and use mechanisms

Based on the pharmacological properties of trandolapril, the ability to drive vehicles or work with complex equipment should not change. However, in some patients, while taking alcoholic beverages, especially at the initial stages of treatment with ACE inhibitors or when replacing one drug with another, an increase in the level of ethanol in the blood may be observed and its excretion slows down. As a result, the effects of alcohol can increase. Therefore, when taken simultaneously with alcohol, after the first dose or with a significant increase in the dose of Gopten for several hours, it is not recommended to drive vehicles or work with mechanisms.

Overdose

Possible symptoms: marked decrease in blood pressure, shock, stupor, bradycardia, electrolyte disturbances, renal failure.

Drug interactions

Diuretics or other antihypertensive drugs, when used simultaneously, can enhance the hypotensive effect of trandolapril. Adrenergic blockers should be used in combination with trandolapril only with close supervision.

With the simultaneous use of trandolapril with potassium preparations, potassium-sparing diuretics (spironolactone, amiloride, triamterene), there is a significant increase in the concentration of potassium in the blood serum, especially with impaired renal function. Trandolapril may reduce potassium loss with thiazide diuretics.

The simultaneous use of trandolapril with hypoglycemic drugs (insulin or oral hypoglycemic drugs) can enhance the effect of the latter and lead to an increased risk of hypoglycemia.

With the simultaneous use of trandolapril with lithium preparations, the concentration of lithium in the blood serum increases due to the deterioration of its excretion.

With the simultaneous use of trandolapril with means for inhalation anesthesia, an increase in the hypotensive effect is noted.

With the simultaneous use of trandolapril with cytostatics, systemic corticosteroids and immunosuppressive drugs, the risk of developing leukopenia increases.

There were no clinically significant signs of the interaction of trandolapril with thrombolytics, acetylsalicylic acid, beta-blockers, calcium channel blockers, nitrates, anticoagulants or digoxin in patients with left ventricular failure who had undergone myocardial infarction.

Pharmacy dispensing conditions

The drug is available by prescription.

Storage conditions and periods

List B. The drug should be stored out of the reach of children at a temperature not exceeding 25 ° C. Shelf life is 4 years.

The drug Trandolapril has a hypotensive effect and is widely used to treat arterial hypertension. It can be used both as a single medication and in combination treatment. Before starting use, you should carefully read the instructions for use of the medicine.

Composition and form of release

Trandolapril is available in the form of red gelatin capsules. One capsule contains 2 milligrams of the active ingredient trandolapril. Additional substances are povidone, sodium stearyl, corn starch and lactose monohydrate. The capsules are located on blisters, which are packed in cardboard boxes.

Indicate your pressure

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Mechanism of action

The pressure stabilization effect lasts the whole day.

According to the instructions for use, the drug allows you to reduce the accumulation of angiotensin 2, aldosterone and increase the plasma activity of renin and the concentration of angiotensin 1. Due to this, the RAAS modulation occurs, which is responsible for the volume of circulating blood, and blood pressure values \u200b\u200bfall. The antihypertensive effect is observed one hour after application. The maximum effect is achieved after 12 hours and continues throughout the day.

Indications for use

The instructions for use indicate that Trandolapril is prescribed for the treatment of the following diseases:

• arterial hypertension;
• heart failure.

Instructions for the use of "Trandolapril"

The instructions for use indicate that Trandolapril is used according to the following scheme indicated in the table:

Contraindications

Instructions for use prohibit taking Trandolapril under the following conditions:

• quincke's edema, which developed due to the use of ACE inhibitors;
• genetic predisposition to Quincke's edema;
• aortic stenosis;
• period of pregnancy;
• lactation;
• age up to 18 years;
• individual intolerance to certain substances.

Side effects

The instructions for use indicate, "Trandolapril" sometimes causes the following side symptoms:

Areas of Potential Impact	Phenomena
Hematopoietic organs	decrease in cells from the group of leukocytes; violation of hematopoiesis of white blood cells; insufficiency of all types of blood; a decrease in the concentration of hemoglobin; aplastic anemia; reduced level of neutrophils in the general cellular composition of the blood; decrease in platelet concentration; anemia; an increase in the number of eosinophilic leukocytes in the blood.
Skin	rashes on the skin; itching and burning of the skin; quincke's edema; malignant exudative erythema; hypersensitivity to ultraviolet radiation; hair loss.
Respiratory system	dyspnea; bronchitis.
Gastrointestinal tract	bouts of nausea; vomiting; pain in the intestines; stool disorders; feeling of dryness in the mouth; pancreatitis; inflammatory lesion of the tongue; indigestion; failures in the liver; hepatitis.
Urinary system	malfunctioning of the kidneys; swelling; violation of potency.
central nervous system	vertigo; headache; loss of consciousness; loss of mood; sleep disturbance; stroke; violation of taste; violation of visual functions; disorders of sensitivity.
The cardiovascular system	excessive decrease in blood pressure; pain in the sternum; violation of the heartbeat; change in heart rate; myocardial infarction.
Locomotor apparatus	pain in the muscles; joint pain; convulsions.
Are common	increased concentration of potassium; decreased sodium levels; the presence of urates in urine; an increase in the level of total protein in the blood; bronchospasm; inflammation of the nasal mucosa.

Overdose

The instructions for use indicate that with an overdose of "Trandolapril", the following symptoms develop:

• a strong decrease in blood pressure;
• quincke's edema.

Gastric lavage should be done in the shortest possible time.

In cases of overdose, the patient's stomach should be flushed. In this case, the dosage of the drug should be reduced or completely canceled. If your blood pressure drops too much, doctors inject sodium chloride intravenously. In case of an overdose of "Trandolapril", for the beginning, the patient is placed in a horizontal position and his legs are raised, then an ambulance should be called immediately.