Captopril 25 mg tablets № 20

Author Ольга Кияница

2017-05-11

Amount in a package -
Product form Pills
Manufacturer Ternoparm Ltd. (Ukraine, Ternopil)
Registration certificate UA/8912/01/01
The main medicament -
morion code 137824

Captopril (CAPTOPRIL) instructions for use

Composition

active ingredient: 1 tablet contains captopril 25 mg (0.025 g)
auxiliary substances: potato starch, lactose, microcrystalline cellulose, povidone, magnesium stearate, silicon dioxide colloidal

Dosage form

Pills.

Pharmacological group

ACE inhibitors (ACE). The code of automatic telephone exchange С09А А01.

Indications

Arterial hypertension.
Heart failure. Captopril is prescribed for the treatment of chronic heart failure with a decrease in systolic function of the ventricles, and also in combination with diuretics and, if necessary, with digitalis and beta-blockers.
Myocardial infarction
for a short-term (4 weeks) treatment, captopril may be administered within 24 hours after myocardial infarction has been transferred to patients with a stable condition;
for prolonged prevention of symptomatic heart failure, the drug is indicated in patients with clinically stable condition with asymptomatic left ventricular dysfunction (ejection fraction ≤ 40%).
Diabetic nephropathy in patients with type 1 diabetes mellitus is manifested by macroproteinuria.

Contraindications

  • Hypersensitivity to captopril or to excipients of the drug, as well as to other ACE inhibitors, the case of angioedema in the use of ACE inhibitors in an anamnesis
  • narrowing of the aorta or mitral stenosis, other obstructions to outflow of blood from the left ventricle of the heart;
  • hypertrophic cardiomyopathy with low cardiac output;
  • primary hyperaldosteronism;
  • hyperkalemia;
  • severe renal dysfunction, bilateral narrowing of the renal arteries, or narrowing of the artery of a single kidney state after kidney transplantation
  • congenital (idiopathic) angioedema
  • porphyria.

Dosing and Administration

Captopril should be taken before, during, or after meals. You should take the drug regularly, at the same time every day.If a pill is missed, it should be taken as soon as possible; However, if there are several hours left before the next dose, the next dose is recommended to be taken according to the schedule and not to take the missed dose. Do not take 2 doses of captopril at the same time.

Arterial hypertension. The recommended initial dose is 25-50 mg daily, in 2 divided doses per day. After 2-4 weeks of treatment, titration of the dose can be performed depending on the blood pressure achieved, up to 100-150 mg per day, divided into 2 doses. Captopril can be used alone or with other antihypertensive drugs, especially with thiazide diuretics.Dosing regimen once a day can be used when such a concomitant antihypertensive drug as a thiazide diuretic is added.

Patients with increased activity of renin-angiotensin (hypovolemia, renovascular hypertension, decompensated heart failure), it is advisable to start therapy with a single dose of 6.25 mg or 12.5 mg. The beginning of such treatment should be carried out under careful medical supervision with the subsequent application of the drug 2 times a day. Dosage can be gradually increased to 50 mg or 100 mg per day for 1 or 2 doses.

Heart failure . The initial dose is 6.25-12.5 mg 2 or 3 times a day. Titration to a maintenance dose (75-150 mg per day) should be based on the patient's response (objective examination and drug tolerability) in response to treatment. The dose should be increased gradually, at intervals of at least 1 time in 2 weeks in order to assess the response of the patient in response to treatment. The maximum daily dose is 150 mg divided into 2 divided doses.

Myocardial infarction.

Short-term treatment. The administration of the drug in the first 24 hours after myocardial infarction is carried out according to the following scheme: the initial dose is 6.25 mg, after 2:00 appoint 12.5 mg and after 12:00 take another 25 mg of captopril. From the next day for 4 weeks, captopril should be taken at a dose of 100 mg per day, divided into 2 doses. At the end of the 4-week treatment, a reassessment of the patient's condition should be made to make a decision on the treatment at a stage after a previous myocardial infarction.

Prolonged treatment. If captopril is not started during the first 24 hours of the acute myocardial infarction stage, it is recommended to begin treatment between the third and the sixteenth days after the infarction from the moment when the necessary treatment conditions are provided (stable hemodynamics and treatment of any residual ischemia).Treatment should begin in the hospital under strict control (in particular, blood pressure) until the dose reaches 75 mg per day. The initial dose should be low (see Section "Features of application"), in particular, if the patient has normal or low blood pressure at the beginning of therapy. Treatment should begin with a dose of 6.25 mg, then go to a dose of 12.5 mg 3 times a day for 2 days, then - to a dose of 25 mg 3 times a day in the absence of adverse hemodynamic reactions. The recommended dose for an effective cardiothoracic during a prolonged treatment is 75-150 mg daily, which should be divided into 2 or 3 divided doses. In case of symptomatic hypotension, as in heart failure, the dose of diuretics and / or other vasodilating drugs can be reduced to achieve a stable dose of captopril. If necessary, the dose of captopril can be adjusted depending on the clinical response of the patient. Captopril can be used in combination with other types of treatment for myocardial infarction, for example, with thrombolytic drugs, beta-blockers and acetylsalicylic acid.

Diabetic nephropathy in patients with type I diabetes mellitus. Captopril is used in a dose of 75-100 mg per day in 2 divided doses. If necessary, combine with other antihypertensive drugs.

Impaired renal function. Since captopril is mainly excreted by the kidneys, if the kidney function is impaired, either reduce the dose of the drug or increase the interval between its use. If concomitant therapy with diuretics is needed, loop diuretics (furosemide) should be preferred, and not thiazide.

Patients with impaired renal function are recommended the following scheme of dosing captopril to prevent its cumulation in the body.

KK (ml / min / 1.73 m 2)

Initial daily dose

(Mg)

The maximum daily dose (mg)
> 40 25-50 150
21-40 25 100
10-20 12.5 75
<10 6.25 37.5

Children. The effectiveness and safety of the use of captopril to children have not been adequately studied. The use of captopril for children should be started under close medical supervision. The initial dose of captopril is 0.3 mg / kg body weight. For special groups of patients (children with renal insufficiency, premature neonates, newborns and infants due to immaturity of the urinary system), the initial dose should be 0.15 mg / kg body weight. Usually captopril is prescribed to children 3 times a day, but the interval between injections must be selected individually, depending on the patient's reaction to the administration of the drug.

Patients of advanced age. As with other antihypertensive drugs, it is necessary to start captopril therapy at a dose of 6.25 mg 2 times a day, since elderly patients may have impaired renal function and other organs and systems. Dose titrated depending on the response of blood pressure to the drug, while prescribing a minimum dose that can adequately control the pressure.

Adverse Reactions

From the cardiovascular system: orthostatic hypotension tachycardia, tachyarrhythmia, angina pectoris, tachycardia, cardiogenic shock, cardiac arrest; Arterial hypotension, Raynaud's syndrome, hot flashes, pallor;

from the respiratory system: dry cough, shortness of breath, bronchospasm, rhinitis, allergic alveolitis / eosinophilic pneumonia

from the digestive system: nausea, decreased appetite abdominal pain, diarrhea, increased activity of hepatic transaminases, vomiting, stomach irritation, constipation, dry mouth, stomatitis / appearance of aphthous ulcers, glossitis, ulcer, pancreatitis

from the digestive system: a violation of liver function of cholestasis, including jaundice; hepatitis, including necrotizing hepatitis, increased levels of liver enzymes and bilirubin

from the central nervous system: dizziness, headache, fatigue, asthenia

neurological disorders: taste disorders, drowsiness, paresthesia, cerebrovascular manifestations, ataxia, including stroke and loss of consciousness;

from the hemopoietic system: neutropenia, in patients with autoimmune diseases - agranulocytosis, leukopenia, pancytopenia (in particular in patients with impaired renal function), anemia (including aplastic and hemolytic), thrombocytopenia, lymphadenopathy, eosinophilia;

from the immune system: autoimmune diseases and / or a positive test for antinuclear antibodies;

metabolic and digestive disorders: anorexia, acidosis, hypoglycaemia

mental disorders: sleep disorders, confusion, depression

from the side of the organs of vision: blurring of vision;

changes in the skin and subcutaneous tissue: itching, rash, alopecia, urticaria, Stevens-Johnson syndrome, polymorphic erythema, photosensitivity, erythroderma, pemphigoid reactions and exfoliative dermatitis, angioedema, facial edema, eyelids, tongue, interstitial angioedema

from the musculoskeletal system and connective tissue: myalgia, arthralgia

from the urinary tract: renal failure, impaired renal function, polyuria, oliguria and frequent urination, nephrotic syndrome

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

common disorders: chest pain, weakness, fever

changes in laboratory parameters: hyperkalemia, proteinuria, hyponatremia (most often observed with a salt-free diet with simultaneous use of diuretics), elevated levels of urea, creatinine in the blood serum, as well as reduced hemoglobin, hematocrit and increased erythrocyte sedimentation rate (ESR), increased titer antinuclear antibodies.Captopril may result in a chemically positive urine test result for acetone.

Overdose

It manifests a pronounced arterial hypotension with the development of shock, stupor, bradycardia, electrolyte imbalance and renal insufficiency.

Treatment: the presence of severe arterial hypotension requires withdrawal of the drug. the patient should be given a horizontal position, wash the stomach and conduct therapy aimed at normalizing blood pressure. In case of severe symptoms of overdose, the patient is urgently hospitalized for intensive detoxification methods, including hemodialysis, and measures aimed at increasing the volume of circulating blood, normalizing the functions of the cardiovascular, respiratory and nervous systems, restoring the kidney function. It is necessary to avoid hemodialysis through high-performance membranes from polyacrylonitrite-methyl sulphate, (AN69), hemofiltration because of the possibility of developing anaphylactoid reactions. Peritoneal dialysis is ineffective.

Use during pregnancy or lactation

Do not use during pregnancy and lactation.

Children

The efficacy and safety of captopril in children have not been adequately studied. The use of captopril in children should be carried out under careful medical supervision.

Application features

Arterial hypotension. Rarely arterial hypotension may occur in patients with hypertension who have reduced blood volume and / or reduced sodium levels as a result of diuretic therapy, limited consumption of table salt, and also due to diarrhea, vomiting, or hemodialysis. Before the appointment of ACE inhibitors should adjust the volume of circulating blood (BCC), as well as decide on the appointment of a minimum effective optimal dose of the drug.

Patients with heart failure are also at risk of symptomatic hypotension with ACE inhibitors. Therefore, these patients are recommended to administer captopril with a low initial dose. An increase in the dose of ACE inhibitors and diuretics should be performed under the supervision of a physician.

Excessive reduction in blood pressure in patients with cerebrovascular and ischemic heart disease increases the risk of myocardial infarction and stroke. In case of hypotension, the patient should take a horizontal position (put on his back), and if necessary - increase the BCC due to the introduction of 0.9% sodium chloride solution.

Renovascular hypertension. There is an increased risk of hypotension and kidney failure when patients with bilateral renal artery stenosis or with a single kidney stenosis take ACE inhibitors. In this case, it is possible to stop the kidney function with very small changes in serum creatinine, so it is recommended that such patients start with small doses of captopril and under the supervision of a doctor, and during the treatment, titrate the dose and constantly monitor the kidney function.

Impaired renal function. Patients with impaired renal function (creatinine clearance ≤40 ml / min) require individual dose selection (see Section "Method of administration and dose"). When using captopril, such patients should constantly monitor the level of potassium and creatinine in the blood serum.

Angioedema. Rarely with treatment with ACE inhibitors, in particular during the first weeks of treatment, it is possible to develop angioedema of the extremities, face, lips, mucous membranes, tongue, larynx and / or glottis. However, extremely rarely angioedema may develop as a result of long-term treatment with ACE inhibitors. In such cases, it should be stopped immediately. Angioneurotic edema of the tongue, glottis and / or larynx can be lethal, so immediate purchase of such reactions should be made immediately, followed by hospitalization and observation of at least 12-24 hours until the symptoms disappear completely.

Cough. There have been reports of the occurrence of cough in the treatment with ACE inhibitors. The cough was characterized as continuous, dry, unproductive, which ceases after the withdrawal of therapy.

Liver failure. ACE inhibitors in rare cases were associated with a syndrome that begins with cholestatic jaundice, progresses to sudden necrotic hepatitis and sometimes leads to death. The mechanism of development of this syndrome remains unclear. Therefore, if during treatment with ACE inhibitors jaundice or increased liver enzymes occurs, treatment should be stopped immediately and the patient's condition carefully monitored.

Hyperkalemia. The risk of hyperkalemia is increased in patients with renal insufficiency, diabetes, in those who simultaneously take potassium-sparing diuretics, potassium supplements or salt substitutes containing potassium or other drugs that can cause hyperkalemia (eg, heparin). If simultaneous reception of these drugs is considered necessary, it is recommended to regularly check the level of potassium in the blood serum.

Stenosis of the aorta or mitral valve / hypertrophic cardiomyopathy. ACE inhibitors should be taken with caution in patients with stenosis of the aorta or mitral valve and obstruction of the left ventricular outflow tract. It is necessary to avoid the use of captopril in the development of cardiogenic shock and significant hemodynamic disorders.

Lithium. The combination of lithium and captopril is not recommended (see Section "Interaction with Other Drugs and Other Interactions").

Neutropenia / agranulocytosis. There have been reports of the occurrence of neutropenia / granulo-cytosis, thrombocytopenia and anemia in patients taking ACE inhibitors. In patients with normal renal function and without other aggravating factors, neutropenia occurs rarely. Captopril should be used with caution in patients with vascular lesions with collagenoses (for example, systemic lupus erythematosus, scleroderma), with antidepressants, allopurinol or procainamide, or a combination of these factors, especially if there are already violations of kidney function. In some of these patients, a serious infection can develop, which sometimes does not respond to intensive antibiotic therapy. If such patients need to use captopril, it is recommended to check the amount of white blood cells in the blood and check the detailed blood test before treatment, every 2 weeks during the first 3 months of treatment and periodically thereafter.For patients should be instructed about the need to immediately inform the doctor about any signs of infection (eg, sore throat, fever) and further analysis of blood with an expanded leukocyte formula. Captopril and other concomitant medication (see. Section "interaction with other drugs and other types of interactions") to be immediately canceled if detected or suspected neutropenia (neutrophils less than 1000 / mm 3).

In most patients neutrophil counts rapidly return to normal after discontinuation of captopril.

Proteinuria. Proteinuria may occur in patients with impaired kidney function or with high doses of ACE inhibitors. Total protein in the urine of more than 1 g per day is observed in approximately 0.7% of patients receiving captopril. Most of these patients had evidence of previous kidney disease or receive relatively high doses of captopril (more than 150 mg per day), or both of these factors are available. Nephrotic syndrome is observed in 1/5 patients with proteinuria. In most cases, proteinuria decreases or disappears within 6 months regardless of captopril. Patients with proteinuria rarely change parameters such as the level of kidney function urea and serum creatinine.

For patients undergoing renal disease should be conducted in urine protein assay (test strip analysis of first morning urine samples) before treatment and periodically thereafter.

Anaphylactoid reactions during desensitizing allergen Hymenoptera venom may occur in patients while receiving ACE inhibitors, which in rare cases can be life threatening. Such reactions can be avoided by temporarily discontinuing therapy with ACE inhibitors before each desensitization, but the reaction may occur at random again repeated antigenic stimulation of the preparation. Therefore, caution is recommended with the therapy of ACE inhibitors in patients who have tested such desensitisation procedures.

There have been reports of the occurrence of anaphylactoid reactions in patients during dialysis using membranes with high permeability / LDL apheresis with dextran sulfate. For such patients should take the decision to use another type of dialysis membrane preparations or other group.

Surgery / anesthesia. In patients with major surgery in the application of anesthesia can occur hypotension. By reducing blood pressure recommended recharge BCC.

Diabetes. Diabetic patients taking oral antidiabetic agents or insulin, during the first month of combined use of ACE inhibitors should be carefully check the level of glucose in the blood.

Ethnic features. Like other ACE inhibitors, captopril less effective antihypertensive agent for blacks patients, possibly due to a greater prevalence of low-renin essential hypertension.

The ability to influence the reaction rate when driving vehicles or other mechanisms

During the period of treatment must be careful when driving and implementation of potentially hazardous activities that require concentration and an increased rate of psychomotor reactions, because there may be dizziness and drowsiness, especially at the beginning of therapy.

Interaction with other drugs and other interactions

Potassium-sparing diuretics and potassium supplements. ACE inhibitors reduce the loss of potassium caused by diuretics. Potassium-sparing diuretics (e.g., spironolactone, triamterene or amiloride), potassium supplements or salt substitutes containing potassium can cause hyperkalemia. While the appointment through existing hypokalaemia they should be used with caution and with frequent monitoring of potassium concentration in the blood serum.

Diuretics (thiazide and loop diuretics). Pre-treatment with diuretics in high doses may lead to a reduction of the bcc and increased risk of significant hypotension (see. Section "Properties application"). Hypotonic effect can be reduced by stopping the diuretic, an increase of salt intake and the liquid or starting therapy with low-dose captopril. However, it is not revealed any clinically relevant interactions with hydrochlorothiazide or furosemide.

Other antihypertensive drugs. The simultaneous use of captopril with other antihypertensive agents (e.g., beta blockers and calcium channel blockers prolonged action) is safe, and concomitant drugs may enhance the antihypertensive effect of captopril. Caution should be used to treat nitroglycerin, other nitrates, or other vasoconstrictor agents.

Treatment of acute myocardial infarction. Patients with myocardial infarction captopril can be taken together with acetylsalicylic acid (at cardiological doses), thrombolytics, beta-blockers and / or nitrates.

Lithium. The simultaneous use of ACE inhibitors and lithium can cause a temporary increase in the level of lithium in blood serum and lithium intoxication. The simultaneous use of ACE inhibitors and thiazide diuretics may further increase the levels of lithium in blood serum and increase the risk of lithium intoxication. Therefore it is not recommended simultaneous application of captopril with lithium. If this combination of drugs is required, it is necessary to closely monitor the level of lithium in blood serum.

Tricyclic antidepressants / antipsychotics. Simultaneous use of certain tricyclic antidepressants and neuroleptics with ACE inhibitors may lead to a further decrease in blood pressure (cm. "Application Features" section). You may experience postural hypotension.

Allopurinol, procainamide, cytostatic or immunosuppressive drugs. Their simultaneous use with ACE inhibitors may lead to increased risk of leukopenia, especially when the latter are used in doses higher than recommended.

Nonsteroidal anti-inflammatory drugs (NSAIDs). It discloses that ACE inhibitors and NSAIDs exert additional effect on improving the level of potassium in blood serum which may lead to renal dysfunction. Usually, this effect is reversible. Rarely possible acute renal failure, especially in patients with impaired renal function, such as elderly patients or patients suffering from dehydration. Long term administration of NSAIDs may reduce the antihypertensive effect of the ACE inhibitors.

Sympathomimetics. May reduce the antihypertensive effect of ACE inhibitors, therefore, should be carefully monitored for indicators of blood pressure in a patient.

Antidiabetic drugs. ACE inhibitors, including captopril, antiglikemichny can enhance the effect of insulin and other oral antidiabetic drugs (sulfonylurea) in patients with diabetes. This effect is very rare, but when it occurs it becomes necessary to reduce the dose of antidiabetic drugs with simultaneous treatment with ACE inhibitors.

Pharmacological properties

Pharmacological.

Captopril - ACE inhibitor (ACE) reduces the concentration of angiotensin II and aldosterone blood, prevents the inactivation of endogenous vasodilators - bradykinin and prostaglandin E 2. As a result of gradually decreasing blood pressure, total peripheral vascular resistance, and post-preload on the heart, the pressure in the pulmonary circulation and pulmonary vascular resistance, increase cardiac output, without changing the heart rate, left ventricular hypertrophy decreases (when long-term therapy), increased tolerance physical stress.

Antihypertensive action is shown through 15-60 min after oral administration, reaching a maximum in 60-90 minutes and lasts 6-12 hours. The duration of the antihypertensive effect is dose dependent and reaches optimum values for several weeks under continuous use. In patients with moderate hypertension captopril when used in doses of 25-50 mg 2 times a day increases the quality and duration of life improves overall health, sleep and emotional status. In patients with hypertension combined with diabetes reduces the incidence of cardiovascular complications. Angioprotective exhibits properties against microvasculature that increases the diameter of the major peripheral arteries (from 13% to 21%), slowing the progression of renal failure in diabetic nephropathy.

Pharmacokinetics.

Rapidly and completely absorbed from the gastrointestinal tract, the minimum absorption is 60-75%. In applying fasting maximum blood concentration is reached after 30-90 min. Biotransformation in the liver. It passes through the blood-tissue barriers, with the exception of the blood-brain penetrates through the placenta and into breast milk (concentration reaches approximately 1% of the level in the mother's blood). The half-life of 2-3 hours, in patients with chronic heart failure and renal failure is increased to 3,5-32 hours. Excreted mainly by the kidneys (2/3 dose excreted within 4:00, more than 95% of the dose - for 24 hours) as metabolites and unaltered (40-50%). Cumulated with chronic renal failure.

Basic physical and chemical properties

Tablets white or almost white color with a flat surface, and the notch chamfer, with a specific smell.

Shelf life

2 years.

Storage conditions

Store in a dry, dark place at a temperature not higher than 25 ° S.Hranit the reach of children.

Packaging

№ 20 (10'2) in a blister pack.

Category of leave

On prescription.


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