Fosinap - instructions for use, dose, side effects, contraindications

Excipients: silicon colloid dioxide 0.7 mg, croscarmellose sodium 5 mg, lactose monohydrate 66.8 mg, macrogol (polyethylene glycol 4000) 0.5 mg, sodium stearyl fumarate 1 mg, povidone 7 mg, cellulose microcrystalline 47.88 mg, calcium stearate 1.12 mg.

Dosage of 20 mg

1 tablet contains: active substance: fosinopril sodium 20.0 mg

auxiliary substances: silicon dioxide colloidal 1 mg, croscarmellose sodium 5.7 mg, lactose monohydrate 97.3 mg, macrogol (polyethylene glycol 4000) 1 mg, sodium stearyl fumarate 1.5 mg, povidone 10.5 mg, cellulose microcrystalline 71.32 mg, calcium stearate 1.68 mg.

Description:

Pills round, planocylindrical, with a facet and a risk (a dosage of 10 mg); round, planocylindrical with chamfer (dosage of 20 mg), white or almost white colors. Marble is allowed.

Pharmacotherapeutic group:inhibitor of angiotensin-converting enzyme (ACE).

ATX: & nbsp

C.09.A.A ACE Inhibitors

C.09.A.A.09 Fosinopril

Pharmacodynamics:

ACE inhibitor. Has hypotensive, vasodilating, diuretic and potassium-sparing effect. Fosinopril prevents the conversion of angiotensin I into a vasoconstrictor substance, angiotensin II, as a result of which vasopressor activity and secretion of aldoheterone decrease, which can lead to a slight increase in the potassium ion concentration in the blood serum with simultaneous loss of sodium and liquid ions. As a result, the overall peripheral vascular resistance and systemic arterial pressure (BP) decrease. Suppresses the synthesis of aldo-heteron, inhibits tissue ACE.

Fosinopril inhibits the metabolic degradation of bradykinin, which has a powerful vasopressor effect; due to this, the antihypertensive effect of the drug can be enhanced.

Reduction of blood pressure is not accompanied by a change in the volume of circulating blood, cerebral and renal blood flow, blood supply of internal organs, skeletal muscles, skin, reflex activity of the myocardium. With arterial hypertension and left ventricular hypertrophy, treatment results in a decrease in left ventricular mass and a decrease in the thickness of the interventricular septum. Long-term therapy does not lead to metabolic disorders. After ingestion, the hypotensive effect develops within 1 hour, reaches a maximum after 3 to 6 hours, and persists for 24 hours.

In chronic heart failure, the positive effects of fosinopril are achieved mainly by suppressing the activity of the renin-aldosterone system. Inhibition of ACE leads to a decrease in both preload and postload on the myocardium.

Fosinopril promotes increased tolerance to physical activity, reducing the severity of chronic heart failure.

Pharmacokinetics:

After ingestion, absorption from the gastrointestinal tract is about 30-40%. The degree of absorption does not depend on the intake of food, but the rate of absorption can be slowed down.

Metabolism of fosinopril under the action of enzymes with the formation of fosinoprilata occurs mainly in the liver and in the mucosa of the gastrointestinal tract.

The time to reach the maximum concentration of fosinoprilat in blood plasma is 3 hours and does not depend on the dose taken.

Link with blood plasma proteins - more than 95%. Fosinoprilat has a relatively small volume of distribution and is slightly associated with the cellular components of the blood. Does not penetrate the blood-brain barrier.

Fosinopril is excreted from the body in equal parts by the kidneys and through the liver. With arterial hypertension in patients with normal renal and hepatic function, the half-life of fosinoprilata is about 11.5 hours. In chronic heart failure, the elimination half-life is 14 hours.

Indications:

arterial hypertension (in monotherapy or as part of combination therapy);

chronic heart failure (as part of combination therapy).

Contraindications:

increased sensitivity to fosinopril and other components of the drug;
hereditary or idiopathic angioedema;
angioedema with use of other ACE inhibitors (in the anamnesis);
pregnancy;
-period of lactation (breastfeeding);
age under 18 years (effectiveness and safety not established);
-lactose intolerance, lactase deficiency or glucose-galactase malabsorption.

Carefully:

apply for kidney failure; hyponatremia (risk of dehydration, arterial hypotension, chronic renal failure); bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney; aortic stenosis; condition after kidney transplantation; with desensitization; systemic diseases of connective tissue (including systemic lupus erythematosus, scleroderma) due to increased risk of developing neutropenia or agranulocytosis; with hemodialysis; with cerebrovascular diseases (including cerebral circulatory insufficiency); ischemic heart disease; chronic heart failure of III-IV functional class according to NYHA classification; diabetes mellitus; oppression of bone marrow hematopoiesis; hyperkalemia; in elderly patients; gout; on a background of a diet with salt restriction; at conditions accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting, previous treatment with diuretics).

Pregnancy and lactation:

Fozinap® contraindicated for use during pregnancy.

The use of the drug in the II and III trimesters of pregnancy causes damage or the death of a developing the fetus. For newborns whose mothers took ACE inhibitors during pregnancy, it is recommended to carry out careful monitoring for the timely detection of arterial hypotension, oliguria and hyperkalemia.

Because the fosinoprilat is excreted in breast milk, if necessary, the use of the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

The drug is administered orally, regardless of food intake. Take without chewing, squeezed a small amount of liquid. The dose is set individually.

With arterial hypertension, the recommended initial dose is 10 mg 1 time / day. The dose should be selected depending on the dynamics of blood pressure lowering. Doses vary from 10 to 40 mg once a day. The maximum daily dose is 40 mg.

In chronic heart failure, the recommended initial dose is 5 mg (1/2 tablet 10 mg) 1 or 2 times / day. The maximum daily dose is 40 mg / day.

Patients with impaired renal and / or liver function, as well as patients of advanced age, do not need to adjust the dosage regimen.

Side effects:

From the cardiovascular system. a pronounced decrease in blood pressure, orthostatic hypotension, collapse, tachycardia, palpitations, arrhythmias, angina pectoris, myocardial infarction, blood flushes to the skin of the face, fainting, cardiac arrest.

From the side of the urinary system: the development or aggravation of the symptoms of chronic renal failure, proteinuria.

From the central and peripheral nervous system: stroke, cerebral vascular ischemia, dizziness, headache, weakness, memory impairment; when used in high doses - insomnia, anxiety, depression, confusion, drowsiness, paresthesia.

From the senses: hearing and vision impairment, tinnitus.

On the part of the digestive system: nausea, diarrhea, intestinal obstruction, pancreatitis, hepatitis, cholestatic jaundice, abdominal pain, vomiting, constipation, anorexia, stomatitis, glossitis, dysphagia, flatulence, impaired appetite, weight change, dry mouth; intestinal edema (very rarely).

On the part of the respiratory system: "dry" cough, pulmonary infiltrates, bronchospasm, dyspnea, rhinorrhea, pharyngitis, dysphonia, nosebleeds.

On the part of the organs of hematopoiesis: lymphadenitis.

From the musculoskeletal system: arthritis.

From the side of metabolism: gout.

Allergic reactions: skin rash, itching, angioedema.

From the laboratory indicators: hypercreatinemia, increased

urea concentration, increased activity of "hepatic" transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia; a decrease in the concentration of hemoglobin and hematocrit, an increase in the rate of erythrocyte sedimentation, leukopenia, neutropenia, eosinophilia.

Influence on the fetus: impaired fetal kidney development, decreased fetal and newborn infants, impaired renal function, hyperkalemia, hypoplasia of the skull bones, oligohydramnion, limb contractures, lung hypoplasia.

Overdose:

Symptoms: marked decrease in blood pressure, bradycardia, shock, disturbance of the water electrolyte state, acute renal failure, stupor.

Treatment: the drug should be discontinued, gastric lavage, sorbents (eg, activated charcoal),vasopressor agents, infusion of 0.9% sodium chloride solution and further symptomatic and supportive treatment. The use of hemodialysis is ineffective.

Interaction:

Simultaneous use of antacids (including aluminum hydroxide, magnesium hydroxide) can reduce the absorption of fosinopril (fosinopril and these agents should be taken at intervals of not less than 2 hours).

In patients receiving fosinopril simultaneously with lithium preparations, it is possible to increase the concentration of lithium in the blood plasma and the risk of lithium intoxication (it is necessary to control the concentration of lithium in the blood plasma).

When prescribing fosinopril, it should be borne in mind that indomethacin and other non-steroidal anti-inflammatory drugs (incl. acetylsalicylic acid in a dose exceeding 3 g and inhibitors of cyclooxygenase-2) can reduce the antihypertensive effect of ACE inhibitors, especially in patients with low-renin hypertension.

When combined with fosinopril with diuretics or in combination with a strict diet that limits sodium intake or hemodialysis, it is possible to develop severe arterial hypotension, especially in the first hour after taking the initial dose of fosinopril.

When combined fosinopril with potassium preparations, potassium-sparing diuretics (including amiloride, spironolactone, triamterene), with additives to food containing potassium, increases the risk of hyperkalemia. In patients with chronic heart failure, diabetes mellitus, concomitantly taking potassium-sparing diuretics, potassium, potassium-containing salt substitutes, or other agents that cause hyperkalemia (eg, heparin), ACE inhibitors increase the risk of developing hyperkalemia.

Fosinopril enhances the hypoglycemic effect of derivatives of sulfonylurea, insulin.

With simultaneous use with allopurinol, cytostatic agents, immunosuppressants, procainamide, the risk of developing leukopenia increases. Estrogens weaken the hypotensive effect of fosinopril because of its ability to retain fluid.

Antihypertensive drugs, opioid analgesics, medicines for general anesthesia increase the hypotensive effect of fosinopril.

Bioavailability of fosinopril with simultaneous application with chlorthalidone, nifedipine, propranolol, hydrochlorothiazide, cimetidine, metoclopramide.propantheline bromide, digoxin, acetylsalicylic acid and warfarin does not change.

Special instructions:

Before the beginning of treatment it is required to conduct an analysis of previous antihypertensive therapy, the degree of increase in blood pressure, the restriction of diet for salt and / or fluid and other clinical situations.

If possible, the ongoing previously antihypertensive treatment several days before the start of treatment with the drug Fozinap®.

To reduce the likelihood of arterial

hypotension diuretics should be canceled 2-3 days before the start of treatment with Fozinap®.

Before and during drug treatment Fozinap® must be controlled AD, kidney function, content potassium ions, creatinine, urea, concentration of electrolytes and activity of "liver" transaminases in blood.

The development angioedema patients on admission fosinopril.

With the spreading edema of the tongue, pharynx or larynx can develop airway obstruction with possible fatal outcome. AT if such reactions develop you must stop receiving and take immediate action therapy, incl.subcutaneously enter epinephrine solution (epinephrine) (1:1000).

During the administration of ACE inhibitors in rare cases of edema the intestinal mucosa. Edema of the intestinal mucosa should be considered when differential diagnosis of patients with complaints about abdominal pain in the background of treatment ACE inhibitors. Symptoms disappeared after termination use of ACE inhibitors.

Against therapy with ACE inhibitors it is possible to develop anaphylactic reactions during hemodialysis through high-density membranes, as well as during plasmapheresis lipoproteins of low density with adsorption on dextran sulfate.

In such cases, the use of dialysis membranes of a different type or other medication should be considered. Perhaps the development of agranulocytosis and suppression of bone marrow function during treatment with ACE inhibitors. These cases are more often observed in patients with impaired renal function, especially in the presence of systemic diseases connective tissue (including systemic lupus erythematosus or scleroderma). Before the beginning of therapy with ACE inhibitors and during the treatment, the total number of leukocytes and leukocyte formula(Once a month in the first 3-6 months of treatment and in the first year of use in patients with an increased risk of neutropenia).

Symptomatic arterial hypotension in use ACE inhibitors most often develops in patients after intensive treatment with diuretics, a diet that restricts entry salt, or when performing kidney dialysis. Transient arterial hypotension is not contraindication for further application of the drug. In patients with arterial hypertension with bilateral renal stenosis arteries or with arteries tenesis single kidney, as well as simultaneous application diuretics in patients with unchanged kidney function; time of treatment with ACE inhibitors can increase the concentration of nitrogen urea and serum creatinine blood. If these effects do not pass after discontinuation of treatment, then it is necessary to reduce the dose of the drug Fosinap® and / or diuretic.

In some cases, patients with severe cardiac insufficiency treatment ACE inhibitors can cause more pronounced antihypertensive effect, which can lead to oliguria or azotemia with fatal outcome. Therefore, in the treatment of chronic heart failure Fosinap requires monitoring of patients, especially during the first 2 weeks of treatment, as well as with any increase in the dose of the drug Fosinap® or diuretic. When there is noticeable jaundice and a marked increase in the activity of "liver" transaminases, therapy with Fosinap® should be discontinued and prescribed appropriate treatment.

ACE inhibitors can enhance the antihypertensive effect of the drugs used for general anesthesia. Before surgical intervention (including dentistry), it is necessary to warn an anesthesiologist about the use of ACE inhibitors. Caution should be exercised when performing physical exercises or in hot weather due to the risk of dehydration and arterial hypotension due to a decrease in the volume of circulating blood.

Effect on the ability to drive transp. cf. and fur:

Care must be taken when driving a vehicle or doing other work that requires increased attention, because possibly the development of dizziness, especially after taking the initial dose of the drug Fozinap®.

Form release / dosage:

Tablets of 10 mg and 20 mg.

Packaging:

By 7, 10, 15 or 30 tablets in the endcell packing from polyvinyl chloride and aluminum foil foilcoded. By 1, 2, 4, 8 contour cell packs of 7 tablets or 1, 3 contouring cells packs of 10 tablets or 1, 2 contourcell packings by 15 tablets or 1 loop cell pack of 30 tablets together with instructions for use in a pack of cardboard.

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000834/10

Date of registration:09.02.2010

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp26.10.2015

Illustrated instructions

Instructions

Fozinap (Fosinap)