Capoten, pills 25mg, 56pcs

Composition

One tablet contains: Active ingredient: captopril in terms of 100% substance – 25 mg; excipients: microcrystalline cellulose, corn starch, stearic acid, lactose monohydrate.

Pharmacological action

Captopril is a highly specific competitive first-generation angiotensin-converting enzyme (ACE) inhibitor containing a sulfhydryl group (SH-group). Reduces the activity of the renin-angiotensin-aldosterone system (RAAS). By inhibiting ACE, captopril reduces the conversion of angiotensin I to angiotensin II and eliminates the vasoconstrictor effect of the latter on arterial and venous vessels. As a result of a decrease in the concentration of angiotensin II, a secondary increase in plasma renin activity occurs (due to the elimination of negative feedback) and a decrease in the secretion of aldosterone by the adrenal cortex. The antihypertensive effect of captopril is independent of plasma renin activity. A decrease in blood pressure is noted with normal or even reduced hormone activity, which is due to the effect on the tissue RAAS.

Captopril reduces ACE-mediated degradation of bradykinin and increases its content in body tissues. As a result of ACE inhibition, the activity of the circulating and tissue kallikrein-kinin system increases, which contributes to peripheral vasodilation due to the accumulation of bradykinin (a peptide with a pronounced vasodilating effect) and increases the synthesis of prostaglandin E 2. This mechanism may contribute to the antihypertensive effect of captopril 2, and also causes some adverse reactions (in particular, dry cough).

In patients with arterial hypertension, captopril reduces blood pressure (BP) without compensatory increases in heart rate (HR), fluid retention and sodium ions in the body. After a single oral dose, the maximum antihypertensive effect is observed in 60-90 minutes. The degree of reduction in blood pressure is the same when the patient is “standing” and “lying down”. The duration of the antihypertensive effect depends on the dose of the drug. The antihypertensive effect of captopril may increase over time and reaches optimal values after a few weeks of therapy. Orthostatic hypotension is rare, mainly in patients with reduced circulating blood volume. Sudden discontinuation of captopril usually does not lead to the development of withdrawal symptoms.

In patients with arterial hypertension, captopril increases renal blood flow, while the glomerular filtration rate usually does not change. With prolonged use, it reduces left ventricular myocardial hypertrophy.

When sublingual use of captopril in patients with uncomplicated hypertensive crisis, the onset of antihypertensive action is noted in 10-20 minutes; the maximum antihypertensive effect is observed in 45-60 minutes.

In patients with chronic heart failure (CHF), captopril significantly reduces total peripheral vascular resistance (OPSS) and increases venous volume (thus reducing pre – and post-load on the heart), reduces pressure in the right atrium and small circle of blood circulation, increases the minute volume of the heart and improves exercise tolerance.

In placebo-controlled clinical trials in patients with left ventricular dysfunction (left ventricular ejection fraction < 40%) after a previous myocardial infarction, captopril increased survival, slowed the development of clinically significant heart failure, and reduced the frequency of hospitalizations for heart failure.

In a clinical study in patients with type I diabetes mellitus, diabetic nephropathy, retinopathy, and proteinuria ≥ 500 mg/day, captopril reduced proteinuria and reduced the rate of progression of diabetic nephropathy. The efficacy and safety of captopril in children have not been established.

Indications

-arterial hypertension, including renovascular hypertension (including uncomplicated hypertensive crisis);- chronic heart failure (as part of combination therapy);- acute myocardial infarction: within the first 24 hours from the moment of infarction in a clinically stable condition;- left ventricular dysfunction (left ventricular ejection fraction < 40%) after a previous myocardial infarction in a clinically stable condition to reduce the incidence of clinically pronounced heart failure, increase survival and reduce the frequency of hospitalizations for chronic heart failure; – diabetic nephropathy against the background of type 1 diabetes mellitus (with albuminuria more than 30 mg / day).

Contraindications

Hypersensitivity in the anamnesis (including to other ACE inhibitors), angioedema (hereditary or associated with the use of ACE inhibitors in the anamnesis), severe renal and hepatic dysfunction, hyperkalemia, bilateral renal artery stenosis or stenosis of the artery of a single kidney with progressive azotemia, condition after kidney transplantation, aortic stenosis and similar obstructive changes that hinder blood flow, pregnancy, breastfeeding.

Side effects

From the cardiovascular system:  orthostatic hypotension, tachycardia, peripheral edema.

Respiratory system disorders:  dry cough, bronchospasm, pulmonary edema.

Allergic reactions:  angioedema of the extremities, face, lips, mucous membranes, tongue, pharynx or larynx.

From the side of the water-electrolyte balance:  hyperkalemia (most likely with renal failure), hyponatremia (most often with a salt-free diet and simultaneous use of diuretics.

From the urinary system:  proteinuria, increased urea nitrogen and creatinine levels in blood plasma, acidosis.

From the hematopoietic system:  in rare cases-neutropenia, agranulocytosis, thrombocytopenia and anemia, a positive test for antibodies to the nuclear antigen. In patients with normal renal function (creatinine clearance less than 1.6 mg/dl) in the absence of other complicating factors, neutropenia was observed in 0.02% of cases.

From the digestive system:  reversible and usually self-passing taste disorders, dry mouth, aphthous stomatitis; rarely-abdominal pain, diarrhea, gum hyperplasia, hepatitis, increased levels of hepatic transaminases in blood plasma, hyperbilirubinemia.

Dermatological reactions:  macular-papular rash, usually accompanied by pruritus and in rare cases-an increase in body temperature; hyperemia, vesicular or bullous rashes, erythema (including Stevens-Johnson syndrome), photosensitization.

From the central nervous system and peripheral nervous system:  headache, dizziness, ataxia, paresthesia, drowsiness, visual disturbances.

Interaction

Diuretics, vasodilators, ganglioblockers, and adrenoblockers when used simultaneously enhance the antihypertensive effect of Kapoten.

Indometacin and other NSAIDs, as well as clonidine, may reduce the antihypertensive effect of Kapoten.

Neutropenia and/or Stevens-Johnson syndrome may occur when Capoten is co-administered with allopurinol and procainamide, but the causal relationship between these phenomena is not clear.

Concomitant use of immunosuppressants (e. g. azathioprine and cyclophosphamide) with Capoten increases the risk of developing hematological disorders.

With the simultaneous use of probenecid, captopril excretion in the urine decreases.

The simultaneous use of lithium salts and Capotene may lead to an increase in the concentration of lithium in the blood serum. This increases the risk of side effects and toxic effects of lithium preparations.

Concomitant use of Capoten with potassium-sparing diuretics (triamterene, amiloride and spironolactone) or potassium preparations may lead to hyperkalemia.

How to take, course of use and dosage

Capoten doses should be selected by your doctor.

Inside, an hour before meals,25-50 mg 2-3 times a day (but not more than 450 mg per day), for children the initial dose is 0.15-0.3 mg/kg (but not more than 6 mg/kg per day).

Overdose

Symptoms:  marked decrease in blood pressure.

Treatment:  use of plasma-substituting drugs and hemodialysis are effective.

Special instructions

Caution should be exercised when using Capoten for collagenosis due to the increased risk of neutropenia and agranulocytosis. When prescribing the drug to patients with severe disorders of the water-electrolyte balance, this condition should be corrected. During treatment with Kapoten, it is not recommended to take potassium-sparing diuretics or potassium preparations, especially in patients with severe renal impairment.

Angioedema of the extremities, face, lips, mucous membranes, tongue, pharynx or larynx is observed in patients with ACE inhibitors, including captopril. If the swelling is limited to the face and lips, this condition usually resolves after discontinuation of the drug. Antihistamines may be used to relieve clinical symptoms. Patients should be monitored by a doctor until symptoms disappear. If the edema covers the tongue, pharynx or larynx with the threat of airway obstruction,0.5 ml of 0.1% epinephrine solution should be administered subcutaneously.

During treatment with Kapoten, a low-sodium diet is indicated.

Kapoten may cause a false positive reaction in the urine test for acetone.

Use in pediatrics

The safety and efficacy of the drug in children have not been studied.

Form of production

Tablets

Storage conditions

In a dry place, at a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Captopril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets