Fosinopril

When ATH:
C09AA09

Characteristic.

White or off-white crystalline powder, water-soluble (100 mg / ml), methanol, ethanol, and sparingly soluble in hexane.

Pharmacological action.
Gipotenzivnoe, vazodilatirtee, kardioprotektivnoe, natriuretic.

Application.

Arterial hypertension (mono- and combination therapy), heart failure (auxiliary treatment).

Contraindications.

Hypersensitivity, gipotenziya, severe renal insufficiency, severe hyperkalemia, pregnancy, lactation.

Restrictions apply.

Assessment of the risk-benefit ratio in the following cases: angioedema in history, severe autoimmune disease (systemic lupus erythematosus, scleroderma, and other systemic collagen), bone marrow depression (leukopenia, thrombocytopenia), cerebral or coronary circulation, severe heart failure, atherosclerosis of the lower extremities; aortic, mitral stenosis or other obstructive changes, impede the outflow of blood from the heart; diabetes, severe renal insufficiency (serum creatinine above 300 mmol / l) or hyperkalemia (more 5,5 mmol / l), hyponatremia or restriction of sodium in the diet, carrying out dialysis treatments, anesthesia and surgery, dehydration, bilateral renal artery stenosis or stenosis of the artery to a solitary kidney, the transplanted kidney, cirrhosis of the liver, hepatitis, chronic obstructive pulmonary disease, children's (Safety and efficacy have not determined) and old age.

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.

Cardio-vascular system and blood (hematopoiesis, hemostasis): heartbeat, arrhythmia, chest pain, angina, arrhythmias, myocardial infarction, orthostatic hypotension, gipertenzivnye crisis, fainting, flushing; sudden death, cardio-pulmonary insufficiency, cardiogenic shock, Beards- or tachycardia (Heart failure); anemia (hemolytic and aplastic), reduction in hemoglobin or hematocrit decrease, leukocytosis, lejko- or neutropenia, thrombocytopenia, eozinofilija.

From the nervous system and sensory organs: asthenia, weakness, headache, dizziness, syncope, cerebrovascular disorders, tremor, paraesthesia, mood disorders and / or sleep, vision and memory.

From the digestive tract: dry mouth, taste disturbance, loss of appetite, stomatitis, dysphagia, dyspepsia, nausea, vomiting, diarrhea / constipation, abdominal pain, pancreatitis, abnormal liver function (cholestatic jaundice, fulminant hepatic necrosis with fatal), changes in the level of transaminases.

For the skin: photosensitivity, hives, rash, itch, exfoliative dermatitis, bulezny pemphigus, and etc. hypersensitivity reactions.

With the genitourinary system: swelling, proteinuria, oligurija, renal failure, anurija.

From the respiratory system: cough, rhinitis, sinusitis, laringit, pharyngitis, traheobronhit, bronchospasm.

On the part of the musculoskeletal system: myalgia, arthralgia, arthritis, convulsions.

Other: weight loss, fever, chills, the development of infections, lymphadenopathy, hyperhidrosis, angioedema, increase in serum creatinine, urea, hyperkalemia, giponatriemiya, the weakening of the libido, impotence.

Cooperation.

Effect increase (additive effect) other antihypertensives, including beta-blockers, incl. in ophthalmic formulations at significant systemic absorption, diuretics, alcohol; weaken - estrogens, NSAIDs, sympathomimetic, funds, aktiviruyushtie renin-angiotensin-alydosteronovuyu sistemu. Are synergistic peripheral vasodilators (Minoxidil and others.). Potassium-sparing diuretics (spironolactone, amilorid, triamterene et al.), cyclosporine, kalievыe supplements, salt substitutes, kalisodergaszczye funds - increase the risk of hyperkalemia. Mielodepressanty increase the likelihood of a lethal neutropenia and / or agranulocytosis; allopurinol and procainamide - the syndrome of Stevens - Johnson and neutropenia. Antacids increase the absorption, probenecid reduces renal clearance. Potentiates the effect of oral hypoglycemic agents, and the inhibitory effect of alcohol on the central nervous system; reduces symptoms of hypokalemia and hyperaldosteronism, caused by diuretics; increases the toxic effect (increases the concentration) lithium. Compatible with thrombolytics, acetylsalicylic acid, beta-blockers, drugs tsentaralnogo action, vazodilatatorami, It does not alter pharmacokinetic parameters of warfarin.

Overdose.

Symptoms: severe hypotension.

Treatment: dose reduction or complete removal of the drug; gastric lavage, Transfer the patient to a horizontal position, introduce measures to increase BCC (a physiological solution, transfusions, etc.. blood liquids), simptomaticheskaya therapy: epinephrine (n / a or I /), antihistamines, gidrokortizon (I /).

Dosing and Administration.

Inside, adult hypertension the initial dose 10 mg, supports 20-40 mg / day once. The therapy of diuretics, the initial dose of 10 mg (under the control of blood pressure). The maximum daily dose - 80 mg.

Precautions.

Treatment is carried out under regular medical supervision. Held prior to the start of treatment antihypertensive therapy should be discontinued (for 1 Sun). When the previous diuretic therapy, to reduce the risk of symptomatic hypotension diuretic should be discontinued for 4-7 days prior to treatment (or significantly reduce the dose) and adjust the water and electrolyte balance. In order to reduce the risk of hypertension, symptomatic treatment is recommended to start with small doses and take medication the night. After myocardial infarction, treatment is initiated through 3 day. In patients with malignant hypertension therapy course is held under the control of blood pressure, with a gradual increase in dose every 24 h until the maximum effect. During therapy, blood pressure monitoring is necessary, continuous monitoring of peripheral blood (before its beginning, first 3-6 months of therapy and thereafter at periodic intervals to 1 year, especially in patients with an increased risk of neutropenia), protein levels, Plasma potassium, BUN, creatinine, renal function, body weight, diet. With the development of hyponatremia and dehydration correction dosing regimen (decreasing doses). Dose-related neutropenia develops over 3 Months of therapy, a frequency, depending on the degree of renal dysfunction, especially in scleroderma and systemic lupus erythematosus. Maximum reduction in the number of white blood cells is observed for 10-30 days and lasts about 2 weeks after discontinuation of the drug. Понижение уровня нейтрофилов до 1·109/l requires the preparation. Cough appears in the first week (from 24 hours to several weeks) therapy, It maintained during treatment and stopped a few days after discontinuation of the drug; taste disturbance, accompanied by a decrease in body weight, reversible, and goes through 2-3 months of therapy. With the development of cholestatic jaundice and progression of fulminant hepatic necrosis treatment should be discontinued. Maculopapular or urticaria (less often) rash occurs within the first 4 weeks of treatment, disappears at lower doses, administration of antihistamines or discontinuation of the drug. Care should be taken during surgical interventions (including dental), especially when used general anesthetics, hypotensive effect. Avoid hemodialysis through high capacity membranes poliakrilonitritmetallilsulfata (например АN69), gemofilytratsii or LDL apheresis (may develop anaphylaxis or anaphylactoid reactions). Giposensibilizatsionnaya therapy may increase the risk of anaphylactic reactions. At the time of treatment is recommended the use of alcohol. Be wary of during the drivers of vehicles and people, skills relate to the high concentration of attention.

Cautions.

When you miss a dose do not receive follow-doubles. During the radioimmunoassay available falsely low levels of digoxin in serum.

Cooperation

Active substanceDescription of interaction
AllopurinolFMR. Increases the likelihood of developing the syndrome of Stevens - Johnson and neutropenia.
BumetanidFMR: synergism. Strengthens (mutually) hypotensive effect.
VerapamilFMR: synergism. Strengthens (mutually) hypotensive effect.
GidroxlorotiazidFMR: synergism. Strengthens (mutually) hypotensive effect. Against the background of Fosinopril decreases the loss of potassium.
IbuprofenFMR. It weakens the hypotensive effect (consequently inhibiting prostaglandins decreases renal blood flow and renal retention of sodium and fluids); concomitant use increases the risk of renal impairment, especially in patients with hypovolemia.
IndapamidFMR. Strengthens (mutually) hypotensive effect. Against the background of fosinopril reduced loss of potassium.
Potassium chlorideFMR: synergism. Increases (mutually) the probability of hyperkalemia; In sharing recommended periodic monitoring of serum potassium.
Lithium carbonateFKV. FMR. Against the background of fosinopril increased risk of adverse events.
MinoksidilFMR: synergism. Strengthens (mutually) hypotensive effect.
ProkaynamydFMR. Increases the likelihood of developing neutropenia syndrome and Stevens - Johnson.
RisperidoneFMR: synergism. Enhances the hypotensive effect.
SpironolactoneFMR: synergism. Strengthens (mutually) hypotensive effect, It increases the risk of hyperkalemia; the combined use requires monitoring of serum potassium.
FurosemidFMR. Strengthens (mutually) hypotensive effect. Against the background of fosinopril reduced loss of potassium.
XlortalidonFMR: synergism. Strengthens (mutually) hypotensive effect. Against the background of fosinopril reduced loss of potassium.
CelecoxibFMR: antagonizm. It reduces the antihypertensive effect.
CyclosporineFMR. Increases (mutually) the risk of hyperkalemia.
EthanolFMR: synergism. Strengthens (mutually) effect; at the time of treatment should eliminate the use of alcohol.

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