Captopril

When ATH:
C09AA01

Characteristic.

White or off-white crystalline powder with a faint odor of sulfur, sulfhydryl containing residue. Soluble in water (160 mg / ml), methanol and ethanol (96%). Poorly soluble in chloroform and etilazette, insoluble in ether.

Pharmacological action.
Gipotenzivnoe, vazodilatirtee, kardioprotektivnoe, natriuretic.

Application.

Arterial hypertension (mono- and combination therapy), congestive heart failure, cardiomyopathy, left ventricular dysfunction in a stable condition in patients post-myocardial infarction, diabetic nephropathy on background of diabetes mellitus type 1 (if albuminuria more 30 mg / day).

Contraindications.

Hypersensitivity, the presence of anamnestic information about developing angioedema when preceding the appointment of ACE inhibitors, hereditary or idiopathic angioedema, primary hyperaldosteronism, pregnancy, lactation.

Restrictions apply.

Assessment of the risk-benefit ratio in the following cases: leukopenia, thrombocytopenia, aortic stenosis or other obstructive changes, impede the outflow of blood from the heart; hypertrophic cardiomyopathy with low cardiac ejection; expressed by the human kidney; bilateral renal artery stenosis or stenosis of the artery to a solitary kidney; the transplanted kidney; hyperkalemia; childhood.

Pregnancy and breast-feeding.

Contraindicated in pregnancy.

Category actions result in FDA - C (I trimester). (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Category actions result in FDA - D (II and III trimesters).

At the time of treatment should stop breastfeeding.

Side effects.

From the nervous system and sensory organs: fatiguability, dizziness, headache, CNS depression, drowsiness, confusion, depression, ataxia, convulsions, numbness or tingling in the extremities, Visual impairment and/or smell.

Cardio-vascular system and blood (hematopoiesis, hemostasis): gipotenziya, incl. orthostatic, angina, myocardial infarction, heart rhythm disturbance (pryedsyerdnaya Rituals- or bradycardia, atrial fibrillation), heartbeat, acute ischemic stroke, peripheral edema, lymphadenopathy, anemia, chest pain, pulmonary embolism, neutropenia, agranulocytosis (0,2% -in patients with impaired renal function, 3,7% — kollagenozov), thrombocytopenia, eozinofilija.

From the respiratory system: bronchospasm, breathlessness, interstitial pneumonitis, bronchitis, nonproductive cough.

From the digestive tract: anorexia, taste disturbance, stomatitis, ulcerative lesions of the mucous membranes of the oral cavity and stomach, xerostomia, glossitis, difficulty weight management, nausea, vomiting, dyspepsia, flatulence, abdominal pain, constipation or diarrhea, pancreatitis, liver (cholestasis, cholestatic hepatitis, hepatocellular necrosis).

With the genitourinary system: violation of kidney function, oligurija, proteinuria, impotence.

For the skin: redness of the skin, rash, itch, exfoliative dermatitis, toxic epidermal necrolysis, pemphigus, shingles, alopecia, photodermatitis.

Allergic reactions: Syndrome Stevens - Johnson, hives, angioedema, anaphylactic shock, etc..

Other: fever, chills, sepsis, arthralgia, hyperkalemia, gynecomastia, serum sickness, increase of liver enzymes in the blood, BUN, Acidosis, test positive for antibodies to nuclear antigen.

Cooperation.

Possible increases gipotenzivny effect of anaesthetics. Reduces the secondary hyperaldosteronism and hypokalemia, caused by diuretics. Increases concentration of lithium and digoxin in plasma. Effects increase gipotenzivee funds other, including beta-blockers, incl. When systemic vsasavanii ophthalmic dosage forms of, diuretics, klonidin, narcotic analgesics, antipsychotics, alcohol, weaken - estrogens, NSAIDs, sympathomimetic, antacids (reduce the bioavailability of 45%). Potassium-sparing diuretics, cyclosporine, kalisodergaszczye medicines and supplements, salt substitutes, milk with a low salt content increase the risk of hyperkalemia. Preparations, depressing the bone marrow (immunosuppressants, cytostatics and/or allopurinol), increase the risk of neutropenia and / or fatal agranulocytosis. Dampening effect of alcohol on the central nervous system. Probenecid slows excretion of captopril in the urine.

Overdose.

Symptoms: severe hypotension, cerebrovascular accident, myocardial infarction, thromboembolism, angioedema.

Treatment: dose reduction or complete removal of the drug; gastric lavage, Transfer the patient to a horizontal position, introduce measures to increase BCC (isotonic sodium chloride solution, transfusions, etc.. blood liquids), simptomaticheskaya therapy: epinephrine (n / a or I /), antihistamines, gidrokortizon (I /). A kidney dialysis, If necessary, the use of artificial pacemaker.

Dosing and Administration.

Inside, for 1 hour before meals. When hypertension: the initial dose - 12,5 mg 2 once a day, the single dose increase to 50 mg 3 times a day at intervals of 2-4 weeks; maintenance dose 25 mg 2-3 times a day; The maximum daily dose - 150 mg. When it renovskularna hypertension and renal: the initial dose - 6,25 mg 3 once a day, supporting — 25 mg 3 once a day. In chronic heart failure, in postinfarctne period: initial dose is on 6,25 mg 3 times per day with a subsequent increase in (every 2-3 weeks) until maintenance dose 25 mg 2-3 times a day or to 50 mg 3 once a day (in postinfarctne period). The maximum daily dose - 150 mg. If the kidney function: the initial dose 6,25 mg 2-3 times a day with a consequent increase in, the maximum dose depends on creatinine clearance: When clearance 35-130 ml/min/1.73 m² - 150 mg, 20-35 mL/min/1.73 m² - 75 mg, less 20 mL/min/1.73 m² - 37,5 mg.

Precautions.

Treatment is carried out under regular medical supervision. Before treatment (for 1 Sun) prior to antihypertensive therapy should be abolished. In patients with malignant hypertension over every 24 h gradually increase the dose to achieve maximum effect under the supervision of ad. During treatment requires monitoring of blood pressure, peripheral blood (before treatment, in the first 3-6 months of treatment and at periodic intervals thereafter until 1 year, especially in patients with an increased risk of neutropenia), protein levels, Plasma potassium, BUN, creatinine, renal function, body weight, diet. In developing giponatriemii, Dehydration is a correction mode (dose reduction). Maculopapular or urticaria (less often) rash occurs during the first 4 weeks of treatment, disappears at the same time reducing the dose, the preparation and introduction of antigistaminnah funds. Dose-related neutropenia develops over 3 months after initiation of therapy (the maximum decrease in the number of cells is observed within 10-30 days and is about 2 weeks after discontinuation of the drug). Cough (most commonly seen in women) often appears in the first week (from 24 h to several months) therapy, persists during treatment and ends a few days after the end of therapy. Taste and lowering body weight reversible and recovered through 2-3 months of therapy. Care should be taken during surgical interventions (including dental), especially when used general anesthetics, hypotensive effect. With the development of cholestatic jaundice and progression of fulminant hepatic necrosis treatment should be discontinued. It is necessary to avoid dialysis through high-performance membrane of poliakrilonitritmetallilsul'fata (eg, An69), gemofilytratsii or LDL apheresis (may develop anaphylaxis or anaphylactoid reactions). Hyposensitization therapy can increase the risk of anaphylactic reactions. It is recommended that the use of alcohol during treatment. Be wary of during the drivers of vehicles and people, skills relate to the high concentration of attention.

Cautions.

In case of skipping the dose of subsequent dose double. When conducting a test on acetonuriju possible positive result.

Cooperation

Active substance	Description of interaction
Allopurinol	FMR. Increases the risk of neutropenia and/or agranulozitoza (incl. Fatal).
Amylnitrite	FMR. Strengthens (mutually) hypotensive and antianginalny effects.
Atenolol	FMR: synergism. Strengthens (mutually) hypotensive effect.
Betaksolol	FMR: synergism. Strengthens (mutually) hypotensive effect.
Bisoprolol	FMR: synergism. Strengthens (mutually) hypotensive effect.
Bumetanid	FMR: synergism. Enhances the hypotensive effect.
Verapamil	FMR: synergism. Strengthens (mutually) hypotensive effect.
Gidroxlorotiazid	FMR: synergism. Strengthens (mutually) hypotensive effect. Against the backdrop of captopril reduced potassium loss.
Digoxin	FKV. Against the backdrop of captopril increases concentration in plasma.
Ibuprofen	FMR. Inhibits renal prostaglandins, reduces kidney bloodstream sodium delay, fluid and weakens gipotenzivny effect. Combined use may increase the risk of renal impairment, especially in patients with hypovolemia.
Isosorbide dinitrate	FMR. Strengthens (mutually) hypotensive effect.
Izosorʙida mononitrat	FMR. Strengthens (mutually) hypotensive effect.
Indapamid	FMR: synergism. Strengthens (mutually) hypotensive effect (, severe hypotension).
Indomethacin	FMR: antagonizm. It weakens the hypotensive effect.
Potassium chloride	FKV. Against the backdrop of captopril in serum potassium achieves higher values.
Lithium carbonate	FKV. FMR. Against the backdrop of captopril increases concentration in plasma and increases the risk of toxic manifestations.
Metoprolol	FMR: synergism. Strengthens (mutually) hypotensive effect.
Minoksidil	FMR. Strengthens (mutually) hypotensive effect.
Nadolol	FMR: synergism. Strengthens (mutually) hypotensive effect.
Nitroglycerin	FMR. Strengthens (mutually) hypotensive and antianginalny effects.
Pentaэritritila tetranitrate	FMR. Strengthens (mutually) hypotensive effect.
Pindolol	FMR: synergism. Strengthens (mutually) hypotensive effect.
Prazosin	FMR: synergism. Strengthens (mutually) hypotensive effect; the combined appointment of caution.
Propranolol	FMR: synergism. Strengthens (mutually) hypotensive effect.
Risperidone	FMR: synergism. Enhances the hypotensive effect.
Sotalol	FMR: synergism. Strengthens (mutually) hypotensive effect.
Terazosin	FKV: synergism. FMR: synergism. Strengthens (mutually) hypotensive effect. Against the backdrop of captopril increases (C)max.
Timolol	FMR: synergism. Strengthens (mutually) hypotensive effect.
Phenylbutazone	FMR: antagonizm. It weakens the hypotensive effect.
Furosemid	FMR. Strengthens (mutually) hypotensive effect. Against the backdrop of captopril reduced potassium loss.
Xlortalidon	FKV. FMR. Strengthens (mutually) hypotensive effect. Against the backdrop of captopril reduced potassium loss.
Celecoxib	FMR: antagonizm. It weakens the hypotensive effect.
Cyclosporine	FMR. Increases (mutually) the risk of hyperkalemia.
Esmolol	FMR: synergism. Strengthens (mutually) hypotensive effect.
Ethacrynic acid	FMR: synergism. Strengthens (mutually) hypotensive effect. Against the backdrop of captopril reduced potassium loss.
Ethanol	FMR: synergism. Enhances hypotension; at the time of treatment should abandon alcohol.