Composition, form of production and packaging
Tablets 1 tab.
captopril 25 mg
- "- 50 mg
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
10 pieces. - packings cellular planimetric (10) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
The mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I into angiotensin II and eliminates its vasoconstrictive effect.
As a result of a decrease in the concentration of angiotensin II, a secondary increase in renin plasma activity occurs by eliminating the negative feedback during the release of renin and directly reducing the secretion of aldosterone. Due to the vasodilator effect, reduces the overall peripheral vascular resistance (afterload), wedging pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases the minute volume of the heart and tolerance to the load. Does not affect lipid metabolism.
It causes a decrease in the degradation of bradykinin (one of the effects of ACE) and an increase in the synthesis of Pg.
The hypotensive effect does not depend on the plasma renin activity, the decrease in blood pressure is noted with a normal and even reduced concentration of the hormone, which is due to the effect on tissue RAAS. Strengthens coronary and renal blood flow.
With prolonged use reduces the severity of myocardial hypertrophy and the walls of arteries of resistive type. Improves the blood supply of the ischemic myocardium.
Reduces the aggregation of platelets.
PHARMACOKINETICS
Suction and distribution
After ingestion, at least 75% of the drug is rapidly absorbed and C max is observed in the blood after 50 minutes.
The binding with proteins, mainly albumin, is 25-30%.
Metabolism and excretion
Captopril is metabolized in the liver.
T 1/2 is about 3 hours. More than 95% of the drug is excreted in the urine, of which 40-50% in unchanged form, the rest is in the form of metabolites. The duration of the drug is about 5 hours.
INDICATIONS
- arterial hypertension (including renovascular);
- chronic heart failure (as part of combination therapy).
DOSING MODE
Captopril is prescribed an hour before meals. The dosage regimen is set individually. To ensure the following dosing regimen, it is possible to use the drug Captopril in dosage form: tablets of 12.5 mg.
With arterial hypertension, the drug is prescribed in an initial dose of 25 mg 2 times / day. If necessary, the dose gradually (with an interval of 2-4 weeks) is increased to achieve the optimal effect. With mild or moderate arterial hypertension, the usual maintenance dose is 25 mg 2 times / day; the maximum dose is 50 mg 2 times / day. With severe arterial hypertension, the maximum dose is 50 mg 3 times / 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 initial dose is 6.25 mg 2-3 times / day, which is then gradually (with an interval of at least 2 weeks) increase. The average maintenance dose is 25 mg 2-3 times / day. In the future, if necessary, the dose gradually (with an interval of not less than 2 weeks) is increased. The maximum dose is 150 mg / day.
Patients with impaired renal function: with a moderate degree of renal dysfunction (KK not less than 30 ml / min / 1.73 m 2 ) captopril can be administered at a dose of 75-100 mg / day. With a more pronounced degree of renal dysfunction (CC less than 30 ml / min / 1.73 m 2 ), the initial dose should not exceed 12.5-25 mg / day; Further, 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.
In the elderly, the dose of Captopril is selected individually, it is recommended to start therapy with a dose of 6.25 mg 2 times / day and, if possible, maintain it at this level.
If necessary, additionally prescribed loop diuretics, and not diuretics thiazide series.
SIDE EFFECT
From the cardiovascular system: a marked decrease in blood pressure, tachycardia, orthostatic hypotension, peripheral edema.
On the part of the urinary system: proteinuria, impaired renal function (increased levels of urea and creatinine in the blood).
From the hemopoietic system: rarely - neutropenia, anemia, thrombocytopenia, agranulocytosis.
From the side of the central nervous system: dizziness, headache, ataxia, paresthesia, drowsiness, visual impairment, fatigue, asthenia.
On the part of the respiratory system: dry cough, which occurs after withdrawal of the drug, bronchospasm, pulmonary edema.
Allergic and immunopathological reactions: angioedema of the extremities, face, lips, mucous membranes, tongue, throat and larynx, as well as intestinal edema (very rarely), serum sickness, lymphadenopathy, in rare cases - the appearance of antinuclear antibodies in the blood.
Dermatological reactions: a rash, usually macular-papular, less often of a vasicular or bullous nature, itching, increased photosensitivity.
On the part of the gastrointestinal tract, liver, pancreas: a violation of taste, dry mouth, stomatitis, nausea, decreased appetite, rarely - diarrhea, abdominal pain, increased activity of hepatic transaminases, hyperbilirubinemia, hepatitis.
Laboratory indicators: hyperkalemia, hyponatremia, acidosis. There have been reports of cases of hypoglycemia in patients with diabetes who took insulin and oral hypoglycemic drugs.
Other: paresthesia.
CONTRAINDICATIONS
- angioedema, incl. hereditary, in the anamnesis (including in the anamnesis after application of other ACE inhibitors);
- severe renal dysfunction, azotemia, hyperkalemia, bilateral stenosis of the renal arteries or stenosis of a single kidney with progressive azotemia, a condition after kidney transplantation, primary hyperaldosteronism;
- stenosis of the aortic aorta, mitral stenosis, presence of other obstructions to outflow of blood from the left ventricle of the heart;
- pronounced violations of the liver function;
- arterial hypotension;
- cardiogenic shock;
- pregnancy and lactation;
- age under 18 years (efficiency and safety not established).
- Hypersensitivity to captopril and other ACE inhibitors.
With caution apply: severe autoimmune diseases (including systemic lupus erythematosus, scleroderma), oppression of bone marrow circulation (risk of developing neutropenia and agranulocytosis), cerebral ischemia, diabetes mellitus (increased risk of hyperkalemia), patients on hemodialysis, diet with sodium restriction, ischemic heart disease, conditions accompanied by a decrease in bcc (including diarrhea, vomiting), elderly age.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with impaired renal function: with a moderate degree of renal dysfunction (KK not less than 30 ml / min / 1.73 m 2 ) captopril can be administered at a dose of 75-100 mg / day. With a more pronounced degree of renal dysfunction (CC less than 30 ml / min / 1.73 m 2 ), the initial dose should not exceed 12.5-25 mg / day; Further, 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.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindications: marked violations of the liver.
APPLICATION FOR CHILDREN
Contraindication: age under 18 years (efficacy and safety not established).
APPLICATION IN ELDERLY PATIENTS
With caution apply: the elderly.
SPECIAL INSTRUCTIONS
Before the start, and also regularly during the treatment with the drug captopril, kidney function should be monitored.
In chronic heart failure, the drug is used under conditions of careful medical supervision.
With exceptional caution appoint captopril to patients with diffuse connective tissue diseases or systemic vasculitis; patients receiving immunosuppressants, especially in the presence of violations of kidney function (the risk of serious infections that are not amenable to antibiotic therapy). In such cases, monitor the pattern of peripheral blood before using captopril, every 2 weeks for the first 3 months of therapy, and periodically - in the subsequent treatment period.
The drug is used with caution on the background of treatment with allopurinol or procainamide, as well as against the background of treatment with immunosuppressants (including, azathioprine, cyclophosphamide), especially in patients with impaired renal function.
Caution is used in patients with a history of kidney disease, as the risk of developing proteinuria increases. In such cases, during the first 9 months of treatment with captopril, the amount of protein in the urine should be monitored on a monthly basis. If the level of protein in the urine exceeds 1 g / day, it is necessary to decide whether further use of the drug is advisable. With caution appoint captopril to patients with stenosis of the renal arteries, tk. there is a risk of kidney dysfunction; In the case of increased levels of urea or creatinine in the blood, a reduction in the dose of captopril or withdrawal of the drug may be required.
When hemodialysis in patients receiving captopril, the use of dialysis membranes with high permeability (including AN69) should be avoided. this increases the risk of anaphylactoid reactions.
The likelihood of developing arterial hypotension in the course of treatment can be reduced if stopping the use of diuretics or significantly reducing their dose 4 to 7 days before the start of treatment with captopril.
In the 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 observed with IV administration of an isotonic sodium chloride solution.
In the case of angioedema, the drug is withdrawn and carefully monitored. If the edema is localized on the face, special treatment is usually not required (to reduce the severity of symptoms can be used antihistamines); if the swelling spreads to the tongue, throat or larynx and there is a threat of development of airway obstruction, epinephrine (epinephrine) should be injected immediately (0.5 ml at 1: 1000 dilution).
Impact on the ability to drive vehicles and manage mechanisms
During the treatment with captopril it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions. possibly dizziness, especially after taking the initial dose.
OVERDOSE
Symptoms: a marked decrease in blood pressure, including collapse, myocardial infarction, acute impairment of cerebral circulation, thromboembolic complications.
Treatment: to lay the patient with raised lower limbs; measures aimed at restoring blood pressure (increased BCC, including intravenous infusion of saline), symptomatic therapy. Possible use of hemodialysis; peritoneal dialysis is ineffective.
DRUG INTERACTION
Diuretics and vasodilators (eg, minoxidil) potentiate the hypotensive effect of captopril.
With the combined use of captopril with indomethacin (and, possibly, with other NSAIDs), there may be a decrease
hypotensive action.
The hypotensive effect of captopril may decrease estrogen (Na + delay).
The hypotensive effect of captopril can be slowed down when administered to patients receiving clonidine.
Simultaneous use with potassium-sparing diuretics or with potassium preparations can lead to hyperkalemia.
With the simultaneous use of lithium salts, it is possible to increase the concentration of lithium in the blood serum.
The use of captopril in patients taking allopurinol or procainamide increases the risk of developing neutropenia and / or Stevens-Johnson syndrome.
The use of captopril in patients taking immunosuppressants (eg, cyclophosphacin or azathioprine) increases the risk of hematological disorders.
With the simultaneous use of ACE inhibitors and gold preparations (sodium aurotyomalate), a symptom complex is described, including facial hyperemia, nausea, vomiting and a decrease in blood pressure.
Simultaneous use of insulin and oral hypoglycemic drugs increases the risk of developing hypoglycemia.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. Store in a dry place at a temperature below 30 В° C. Keep out of the reach of children. Shelf life - 3 years.
