Description
Release form
Tablets.
Packing
20 pcs.
Pharmacological action
Captopril is a competitive inhibitor of the angiotensin-converting enzyme, an enzyme that promotes the conversion of angiotensin I to angiotensin II.
The drug has an antihypertensive effect, reduces total peripheral vascular resistance (afterload), preload and resistance in the pulmonary vessels increases cardiac output and exercise tolerance.
With prolonged use, it reduces the severity of left ventricular myocardial hypertrophy, prevents the progression of heart failure and slows down the development of left ventricular dilatation.
Pharmacokinetics
Absorption
After oral administration, at least 75% of the dose taken is rapidly absorbed from the gastrointestinal tract. Cmax in blood plasma is reached after 1 hour. A simultaneous meal slows down the absorption of the drug by 30 – 40%.
Distribution of
Binding to blood proteins is 25 – 30%.
Excretion of
T1 / 2 is less than 3 hours. More than 95% of the drug is excreted in the urine, 40 – 50% unchanged, the rest – in the form of metabolites.
The pharmacokinetics of
in special clinical cases, fT1 / 2 increases with renal failure.
Indications
arterial hypertension (as monotherapy and in combination with other antihypertensive drugs, for example, with thiazide diuretics)
chronic heart failure (as part of combination therapy)
coronary heart disease (dysfunction of the left ventricle after myocardial infarction in patients with a stable clinical condition)
diabetic nephropathy (microalbuminuria more than 30 mg / day) with insulin-dependent diabetes mellitus.
Contraindications
hypersensitivity to captopril and other inhibitors of the angiotensin-converting enzyme
Quincke’s edema (hereditary or associated with the use of inhibitors of angiotensin-converting enzyme in the anamnesis)
severe dysfunction of red stenosis -venous kidney with progressive azotemia
condition after kidney transplantation
stenosis of the aortic orifice and similar obstructive changes that make it difficult the flow of blood from the left ventricle
II and III trimester pregnancy
lactation (breast feeding).
Special instructions
Before starting, as well as regularly during treatment with Captopril, kidney function should be monitored.
In chronic heart failure, the drug is used subject to close medical supervision.
With extreme caution, captopril is prescribed to patients with diffuse connective tissue diseases or systemic vasculitis to patients receiving immunosuppressants, especially in the presence of impaired renal function (risk of serious infections that are not amenable to antibiotic therapy). In such cases, the peripheral blood picture should be monitored before captopril is used, every 2 weeks during the first 3 months of therapy and periodically in the subsequent treatment period.
The drug is used with caution during treatment with allopurinol or procainamide, as well as during treatment with immunosuppressants (including azathioprine, cyclophosphamide), especially in patients with impaired renal function.
The likelihood of developing arterial hypotension during treatment can be reduced if you stop using diuretics 4-7 days before starting Captopril or significantly reduce their dose. In case of symptomatic arterial hypotension after taking Captopril, the patient should take a horizontal position with raised legs.
In the case of severe arterial hypotension, a positive effect is noted with the intravenous administration of an isotonic sodium chloride solution. In the case of the development of angioedema, the drug is canceled and a thorough medical observation is carried out. If the edema is localized on the face, special treatment is usually not required (antihistamines can be used to reduce the severity of symptoms) if the edema extends to the tongue, pharynx or larynx, and there is a risk of developing airway obstruction, adrenaline should be immediately injected subcutaneously (0.5 ml at a dilution of 1: 1000).
Use in patients with impaired renal function: Use with caution in patients with a history of kidney disease, since there is an increased risk of developing proteinuria. In such cases, the amount of protein in the urine should be monitored monthly during the first 9 months of captopril treatment. If the protein level in the urine exceeds 1 g / day, it is necessary to decide on the appropriateness of further use of the drug. With caution, Captopril is prescribed to patients with renal artery stenosis, as there is a risk of impaired renal function in the event of an increase in the level of urea or creatinine in the blood, a dose reduction of Captopril or withdrawal of the drug may be required.
Composition
active substance: 100 mg nitrofurantf35 pfrrdfufo354 Active substance: 50 mg captopril.
Dosage and administration of
captopril is prescribed one hour before a meal. The dosage regimen is set individually.
For arterial hypertension: The drug is prescribed in an initial dose of 25 mg 2 times a day. If necessary, the dose is gradually (with an interval of 2-4 weeks) increased until the optimal effect is achieved.
– For mild or moderate arterial hypertension, the usual maintenance dose is 25 mg 2 times a day. The maximum dose is 50 mg 2 times a day.
– In severe arterial hypertension, the maximum dose is 50 mg 3 times a day. The maximum daily dose is 150 mg.
For the treatment of chronic heart failure, captopril is prescribed in cases where the use of diuretics does not provide an adequate effect. The average maintenance dose is 25 mg 2-3 times a day. In the future, if necessary, the dose is gradually increased (with an interval of at least 2 weeks). The maximum dose is 150 mg per day.
Use in patients with impaired renal function Patients with impaired renal function with a moderate degree of impaired renal function (creatinine clearance of at least 30 ml / min / 1.73 m 2) Captopril can be prescribed at a dose of 75-100 mg / day. With a more pronounced degree of impaired renal function (creatinine clearance less than 30 ml / min / 1, 73 m 2) the initial dose should be no more than 12.5-25 mg / day in the future, if necessary, with sufficiently long intervals, the dose of Captopril is gradually increased, but a smaller than usual daily dose of the drug is used.
Side effects
From the cardiovascular system and blood (hematopoiesis, hemostasis): orthostatic hypotension, tachycardia, neutropenia, agranulocytosis.
From the digestive tract: nausea, anorexia, taste disturbance, dry mouth.
Metabolism: electrolyte imbalance (especially in patients with renal failure), hyponatremia (with the simultaneous use of diuretics).
Allergic reactions: skin rash, itching, erythema, urticaria, photosensitivity, vasomotor edema.
Other: dry cough.
Drug interactions
Diuretics and vasodilators (e.g. minoxidil) potentiate the hypotensive effect of captopril.
When combined with captopril and indomethacin (and possibly with other non-steroidal anti-inflammatory drugs), a decrease in hypotensive effect may be noted.
The antihypertensive effect of captopril may be slowed when prescribed to patients receiving clonidine.
Concomitant use with potassium-sparing diuretics or potassium preparations can lead to hyperkalemia.
With the simultaneous use of lithium salts, an increase in serum lithium concentration is possible. The use of captopril in patients taking allopurinol or procainamide increases the risk of neutropenia and / or Stevens-Johnson syndrome.
The use of captopril in patients taking immunosuppressants (e.g. cyclophosphacin or azathioprine) increases the risk of hematologic disorders.
Overdose
Symptoms: severe arterial hypotension, up to collapse, myocardial infarction, acute cerebrovascular accident, thromboembolic complications.
Treatment: lay down a patient with raised lower limbs measures aimed at restoring blood pressure (increase in circulating blood volume, including intravenous infusion of isotonic sodium chloride solution), symptomatic therapy. Perhaps the use of hemodialysis, peritoneal hemodialysis is ineffective.
Storage conditions
Store in a dry, dark place at a temperature not exceeding 25 ° C.
Form of Treatment
tablets
Pharmacore Production, Russia
