Captopres Darnytsia tablets 2 blisters of 10 pcs

Pharmacodynamic parameters. Captopril is a specific competitive inhibitor of ACE, which is responsible for the transformation of angiotensin I into angiotensin II (the latter is a regulator of blood pressure and a key component of the renin-angiotensin-aldosterone system).

The affinity of captopril for ACE is approximately 30,000 times higher than that of angiotensin I. A decrease in the content of angiotensin II in the body and, accordingly, the severity of its pressor effects, leads to a decrease in blood pressure.

Due to the relative absence of negative feedback on renin release caused by the decrease in angiotensin II, plasma renin activity increases.

The content of aldosterone in the blood and urine decreases (and, as a result, the level of potassium in the blood serum increases slightly, along with the excretion of sodium and fluid from the body).

The thiazide diuretic hydrochlorothiazide inhibits water reabsorption in the distal convoluted tubules of the nephron. Administration of hydrochlorothiazide leads to increased excretion of sodium and chloride (in approximately equivalent amounts) and secondary loss of potassium and bicarbonate.

Normal blood pressure values ​​do not change when taking hydrochlorothiazide.

Pharmacokinetic parameters

Captopril. Rapidly absorbed in the gastrointestinal tract (with food intake, the absorption rate decreases by 30-40%). 70-75% of the orally administered dose is absorbed, bioavailability is about 65%. C _max in the blood is reached 45-60 minutes after administration. Captopril contains sulfhydryl groups and easily binds to albumin and other blood plasma proteins. T _½ of unchanged captopril is about 2 hours. The main route of excretion is with urine (within 24 hours 95% of the dose taken). Renal clearance of unchanged captopril exceeds the glomerular filtration rate due to active tubular secretion of the drug.

Hydrochlorothiazide. Rapidly absorbed from the gastrointestinal tract, bioavailability is 68-78%. C _max in the blood is reached 1-2 hours after administration. About 58% binds to plasma proteins. T _½ ≈3-4 h (increases in patients with CHF and renal failure). Rapidly excreted by the kidneys (20-75% of the unchanged dose).

Hypertension.

Orally 1 hour before meals once a day. The dose is selected individually.

Starting dose (including patients with creatinine clearance 30-80 ml/min): 25 mg captopril + 12.5 mg. If necessary, the dose is increased to 50 mg captopril + 25 mg hydrochlorothiazide. If the patient’s condition does not require a rapid change in dose, it is adjusted at intervals of 6 weeks.

When taking captopril:

• pallor, decreased blood pressure (90/60 mm Hg), postural hypotension, Raynaud’s syndrome, angina pectoris, hot flashes, increased heart rate (90 beats/min), tachyarrhythmia, rapid heartbeat, cardiogenic shock, cardiac arrest;
• nonproductive cough, bronchospasm, dyspnea, rhinitis, laryngitis, allergic alveolitis/eosinophilic pneumonia;
• dry mouth, nausea, vomiting, constipation, diarrhea, epigastric discomfort, abdominal pain, stomatitis/aphthous ulcers, glossitis, peptic ulcer, pancreatitis;
• liver dysfunction and cholestasis, hepatitis, increased bilirubin levels, liver enzyme activity;
• decreased renal function (including renal failure), proteinuria, polyuria, pollakiuria, oliguria, nephrotic syndrome;
• anorexia, hypoglycemia, decreased blood sodium levels, increased blood potassium levels;
• dysgeusia, drowsiness, headache, dizziness, paresthesia, cerebral circulation disorders;
• depression, sleep disturbances, confusion;
• blurred vision;
• eosinophilia, pancytopenia, decreased platelet count (150 x 10 ⁹ / l), anemia, decreased white blood cell count (4⋅10 ⁹ / l), decreased neutrophil content (1000 / ml ³) /agranulocytosis;
• pruritus (with or without rash), alopecia, angioedema, peripheral edema, urticaria, erythema multiforme, Stevens-Johnson syndrome, photosensitivity reactions, erythroderma, pemphigoid reactions, exfoliative dermatitis, autoimmune disorders, fever;
• pain in muscles and joints;
• erectile dysfunction, gynecomastia;
• lymphadenopathy, fatigue, weakness;
• increased blood plasma creatinine and urea levels, increased ESR, decreased hematocrit and hemoglobin levels, increased antinuclear antibody levels, false-positive urine acetone test.

When taking hydrochlorothiazide:

• orthostatic hypotension, cardiac arrhythmias; necrotizing vasculitis;
• respiratory disorders;
• sialoadenitis, decreased appetite, thirst, dry mouth, nausea, vomiting, stomach irritation, diarrhea, constipation, pancreatitis;
• jaundice, cholecystitis;
• deterioration of renal function, interstitial nephritis;
• anorexia, hyperglycemia, glucosuria, decreased glucose tolerance, hyperuricemia, electrolyte imbalance (including hypochloremic alkalosis); acidosis; decreased blood sodium, potassium, magnesium, increased blood calcium, increased cholesterol and triglyceride levels;
• drowsiness, headache, paresthesia, seizures, dizziness, vertigo;
• sleep disturbances, mood changes, depression, nervousness, anxiety, disorientation, confusion;
• transient blurred vision, acute myopia, xanthopsia, glaucoma (acute angle-closure);
• decrease in the number of leukocytes (4⋅10 ⁹ / l), neutropenia / agranulocytosis, decreased platelet count (150⋅10 ⁹ / l), anemia (aplastic, hemolytic), bone marrow dysfunction;
• urticaria, anaphylactic reactions, anaphylactic shock;
• photosensitivity reactions, rash, eczema, lupus-like syndrome, reactivation of cutaneous lupus erythematosus, purpura, Lyell’s syndrome, Stevens-Johnson syndrome;
• muscle pain, muscle spasm;
• sexual disorders;
• fever, weakness, exhaustion.

captopril

Enhances CNS depression when taken simultaneously with alcohol.

Enhances the hypoglycemic effect of oral hypoglycemic agents.

Enhances the possible decrease in blood pressure when using anesthetics.

Reduces the manifestations of secondary hyperaldosteronism and hypokalemia due to the use of diuretics.

Increased plasma levels of digoxin and lithium preparations.

The hypotensive effect is enhanced by simultaneous use with ethanol, other antihypertensive or diuretic agents, antipsychotics, clonidine, and narcotic analgesics.

The hypotensive effect is weakened when taken simultaneously with antacids, estrogens, sympathomimetics, and NSAIDs.

Concomitant use with cyclosporine, potassium-sparing diuretics, potassium-containing dietary supplements or salt substitutes increases the risk of developing hyperkalemia.

The risk of neutropenia and/or agranulocytosis increases with the simultaneous use of captopril with immunosuppressants, cytostatics and/or allopurinol.

Renal excretion of captopril is slowed by concomitant use with probenecid.

Hydrochlorothiazide

Concomitant use of alcohol, barbiturates, or narcotics may potentiate orthostatic hypotension.

In case of combined use with antidiabetic drugs, their dose should be adjusted.

In case of simultaneous use with other antihypertensive drugs – additive effect or potentiation of action.

The absorption of hydrochlorothiazide is sharply reduced when cholestyramine or colestipol are used (by 85 and 43%, respectively).

Simultaneous use with corticosteroids and ACTH leads to electrolyte balance disorders and severe hypokalemia.

There may be a decrease in the response to pressor amines.

Increased sensitivity to non-polarizing muscle relaxants is possible.

Concomitant use with NSAIDs may reduce the diuretic effect.

Simultaneous administration with lithium preparations (due to a decrease in its renal clearance) increases the risk of toxic effects of these drugs.

Captopril. Overdose is manifested by headache, increased heart rate (90 beats / min), severe arterial hypotension, decreased appetite, dysgeusia, development of skin allergic reactions, agranulocytosis. In rare cases, arrhythmia, decreased heart rate (40 beats / min), paresis, convulsions, stupor, shock, renal failure, fluid and electrolyte balance disorders in the body are possible.

Therapy is symptomatic.

Hydrochlorothiazide. Overdose is manifested by diarrhea, nausea, vomiting, weakness. It is possible to develop paresthesias, muscle spasms, dizziness, hypotension, increased heart rate (90 beats / min), shock, impaired consciousness, cachexia, poly-, oligo-, anuria, decreased blood potassium, sodium, chlorine, alkalosis. In patients with renal insufficiency – increased blood urea nitrogen. In severe cases – a pronounced disorder of fluid and electrolyte balance in the body, coma.

Overdose therapy: artificially induced vomiting; gastric lavage, sorbents. Severe cases require intensive detoxification (hemodialysis), normalization of vital functions, fluid and electrolyte balance in the body, restoration of renal function.

At a temperature ≤25 °C in the original packaging.