Fosinap tablets 10mg, No. 28

- arterial hypertension (in monotherapy or as part of combination therapy);
- chronic heart failure (as part of combination therapy).

The drug is administered orally, regardless of food intake. Take without chewing with 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 reduction. Doses range from 10 to 40 mg 1 time / day. The maximum daily dose is 40 mg.

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

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

1 tablet contains:
active substance: sodium fosinopril 10.00 mg
excipients: colloidal silicon dioxide (aerosil) 0.7 mg, croscarmellose sodium (primellose) 5.0 mg, lactose (milk sugar) 66.8 mg macrogol (polyethylene glycol 4000) 0.5 mg; sodium stearyl fumarate 1.0 mg, povidone (kollidon 30) 7.0 mg, microcrystalline cellulose 49.0 mg,

- hypersensitivity to fosinopril and other components of the drug;
- hereditary or idiopathic angioedema;
- angioedema with the use of other ACE inhibitors (in history);
- pregnancy;
-period of lactation (breastfeeding);
- age up to 18 years (efficacy and safety have not been established);
-lactose intolerance, lactase deficiency or glucose-galactase malabsorption.

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

Trade name Fosinap

International non-proprietary name fosinopril

Dosage form Tablets

Composition:
1 tablet contains:
active substance: sodium fosinopril 10.00 mg
excipients: colloidal silicon dioxide (aerosil) 0.7 mg, croscarmellose sodium (primellose) 5.0 mg, lactose (milk sugar) 66.8 mg macrogol (polyethylene glycol) 4000) 0.5 mg; sodium stearyl fumarate 1.0 mg, povidone (kollidon 30) 7.0 mg, microcrystalline cellulose 49.0 mg,

Description
Tablets are white or almost white, flat-cylindrical, with a bevel.

Pharmacotherapeutic group:

an angiotensin converting enzyme (ACE) inhibitor.

Pharmacological properties
Pharmacodynamics
ACE inhibitor. It has hypotensive, vasodilating, diuretic and potassium-sparing effects. Fosinopril prevents the conversion of angiotensin I into the vasoconstrictor angiotensin II, as a result of which vasopressor activity and aldosterone secretion decrease, which can lead to a slight increase in the content of potassium ions in the blood serum with a simultaneous loss of sodium ions and fluid by the body. As a result, the total peripheral vascular resistance and systemic arterial pressure (BP) decrease. Suppresses the synthesis of aldosterone, inhibits tissue ACE.

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

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

In chronic heart failure, the beneficial 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 afterload on the myocardium.

Fozinopril helps to increase exercise tolerance, reduce the severity of chronic heart failure.

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

Metabolism of fosinopril under the action of enzymes with the formation of fosinoprilat occurs mainly in the liver and in the mucous membrane of the gastrointestinal tract.

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

The connection with blood plasma proteins is 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 equally by the kidneys and through the liver. With arterial hypertension in patients with normal renal and hepatic function, the half-life of fosinoprilat is about 11.5 hours. In chronic heart failure, the half-life is 14 hours.

Indications for use
- arterial hypertension (in monotherapy or as part of combination therapy);
- chronic heart failure (as part of combination therapy).

Contraindications
- hypersensitivity to fosinopril and other components of the drug;
- hereditary or idiopathic angioedema;
- angioedema with the use of other ACE inhibitors (in history);
- pregnancy;
-period of lactation (breastfeeding);
- age up to 18 years (efficacy and safety have not been established);
-lactose intolerance, lactase deficiency or glucose-galactase malabsorption.

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

Application during pregnancy and lactation
Fosinopril is contraindicated for use during pregnancy. The use of the drug in the II and III trimesters of pregnancy causes damage or death of the developing fetus. For newborns whose mothers took ACE inhibitors during pregnancy, it is recommended to conduct close monitoring for the timely detection of arterial hypotension, oliguria and hyperkalemia.
Since fosinoprilat is excreted in breast milk, if it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Method of administration and dosage
The drug is administered orally, regardless of food intake. Take without chewing with 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 reduction. Doses range from 10 to 40 mg 1 time / day. The maximum daily dose is 40 mg.

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

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

Side effect
From the side of the cardiovascular system: a marked decrease in blood pressure, orthostatic hypotension, collapse, tachycardia, palpitations, arrhythmias, angina pectoris, myocardial infarction, 'flushing' of blood to the skin of the face, fainting, cardiac arrest.

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

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

From the senses: hearing and visual impairment, tinnitus.

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

From the respiratory system: 'dry' cough, pulmonary infiltrates, bronchospasm, shortness of breath, rhinorrhea, pharyngitis, dysphonia, nosebleeds.

From the side of the hematopoietic organs: lymphadenitis.

From the musculoskeletal system: arthritis.

Metabolic: gout.

Allergic reactions: skin rash, itching, angioedema.

On the part of laboratory parameters: hypercreatininemia, increased concentration of urea, increased activity of 'hepatic' transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia; a decrease in the concentration of hemoglobin and hematocrit, an increase in the erythrocyte sedimentation rate, leukopenia, neutropenia, eosinophilia.

Effect on the fetus: impaired development of the fetal kidneys, decreased blood pressure of the fetus and newborns, impaired renal function, hyperkalemia, hypoplasia of the bones of the skull, oligohydramnios, contractures of the extremities, hypoplasia of the lungs.

Overdose
Symptoms: marked decrease in blood pressure, bradycardia, shock, disturbance of the water-electrolyte state, acute renal failure, stupor.
Treatment: taking the drug should be discontinued, gastric lavage is indicated, taking sorbents (for example, activated carbon), vasopressors, infusion of 0.9% sodium chloride solution, and then symptomatic and supportive treatment. The use of hemodialysis is ineffective.

Interaction with other drugs The
simultaneous use of antacids (including aluminum hydroxide, magnesium hydroxide) can reduce the absorption of fosinopril (fosinopril and these drugs should be taken at least 2 hours apart).

In patients receiving fosinopril concurrently with lithium preparations, it is possible to increase the concentration of lithium in the blood plasma and the risk of developing 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 (including acetylsalicylic acid in a dose exceeding 3 g and cyclooxygenase-2 inhibitors) can reduce the antihypertensive effect of ACE inhibitors, especially in patients with low-grade arterial hypertension.

With the combined use of fosinopril with diuretics or in combination with a strict diet that restricts sodium intake, or with hemodialysis, severe arterial hypotension may develop, especially in the first hour after taking the initial dose of fosinopril.

With the combined use of fosinopril with potassium preparations, potassium-sparing diuretics (including amiloride, spironolactone, triamterene), with food supplements containing potassium, the risk of hyperkalemia increases. In patients with chronic heart failure, diabetes mellitus, who are simultaneously taking potassium-sparing diuretics, potassium, potassium-containing salt substitutes, or other drugs that cause hyperkalemia (for example, heparin), ACE inhibitors increase the risk of hyperkalemia.

Fozinopril enhances the hypoglycemic effect of sulfonylurea derivatives, insulin.

With simultaneous use with allopurinol, cytostatic agents, immunosuppressants, procainamide, the risk of developing leukopenia increases.

Estrogens weaken the hypotensive effect of fosinopril due to its ability to retain fluid.

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

The bioavailability of fosinopril when used simultaneously with chlorthalidone, nifedipine, propranolol, hydrochlorothiazide, cimetidine, metoclopramide, propantheline bromide, digoxin, acetylsalicylic acid and warfarin does not change.

Special instructions
Before starting treatment, it is required to analyze the previously conducted antihypertensive therapy, the degree of increase in blood pressure, restriction of the diet in salt and / or liquid and other clinical situations.

If possible, previous antihypertensive treatment should be discontinued a few days before starting treatment with Fosinap.

To reduce the likelihood of arterial hypotension, diuretics should be discontinued 2-3 days before starting treatment with Fosinap.

Before and during treatment with Fosinap, it is necessary to control blood pressure, renal function, the content of potassium ions, creatinine, urea, electrolyte concentrations and the activity of 'hepatic' transaminases in the blood.

It was reported about the development of angioedema in patients while taking fosinopril. With spreading swelling of the tongue, pharynx, or larynx, airway obstruction may develop, with a possible fatal outcome. If such reactions develop, it is necessary to stop taking the drug and take emergency measures, incl. subcutaneously inject a solution of epinephrine (adrenaline) (1: 1000).

During the administration of ACE inhibitors, in rare cases, swelling of the intestinal mucosa was noted. Edema of the intestinal mucosa should be considered in the differential diagnosis in patients with complaints of abdominal pain during treatment with ACE inhibitors. Symptoms disappeared after discontinuation of ACE inhibitors.

Against the background of therapy with ACE inhibitors, it is possible to develop anaphylactic reactions during hemodialysis through high-flow membranes, as well as during plasmapheresis of low-density lipoproteins with adsorption on dextran sulfate. In such cases, consideration should be given to using a different type of dialysis membrane or other medical treatment.

Perhaps the development of agranulocytosis and suppression of bone marrow function during treatment with ACE inhibitors. These cases are more common in patients with impaired renal function, especially in the presence of systemic connective tissue diseases (including systemic lupus erythematosus or scleroderma). Before starting therapy with ACE inhibitors and during treatment, the total number of leukocytes and the leukocyte formula are monitored (once a month in the first 3-6 months of treatment and in the first year of using the drug in patients with an increased risk of neutropenia).

Symptomatic hypotension with the use of ACE inhibitors most often develops in patients after intensive diuretic treatment, a diet that restricts the intake of salt, or during renal dialysis. Transient arterial hypotension is not a contraindication for further use of the drug.

In patients with arterial hypertension with bilateral stenosis of the renal arteries or stenosis of an artery of a single kidney, as well as with the simultaneous use of diuretics in patients with unchanged renal function, the concentration of urea nitrogen and serum creatinine may increase during treatment with ACE inhibitors. If these effects persist after stopping treatment, then it is necessary to reduce the dose of the drug Fosinap and / or the diuretic.

In some cases, in patients with severe chronic heart failure, treatment with ACE inhibitors can cause a more pronounced antihypertensive effect, which can lead to fatal oliguria or azotemia. Therefore, in the treatment of chronic heart failure with Fosinap, monitoring of patients is necessary, especially during the first 2 weeks of treatment, as well as with any increase in the dose of Fosinap or a diuretic.

With the appearance of noticeable yellowness and a pronounced increase in the activity of 'hepatic' transaminases, therapy with Fosinap should be discontinued and appropriate treatment should be prescribed.

ACE inhibitors can enhance the antihypertensive effect of drugs used for general anesthesia. Before surgery (including dentistry), it is necessary to warn the anesthesiologist about the use of ACE inhibitors.

Care should be taken when exercising or in hot weather due to the risk of dehydration and arterial hypotension due to a decrease in circulating blood volume.

Influence on the ability to drive vehicles and use mechanisms

Care must be taken when driving vehicles or performing other work requiring increased attention, since dizziness may develop, especially after taking the initial dose of Fosinap.

Release form
Tablets of 10 mg and 20 mg.
On 7, 10, 15 or 30 tablets in a blister strip packaging from a film of polyvinyl chloride and printed aluminum foil varnished.
1, 2, 4, 8 blister packs of 7 tablets or 1, 3 blister packs of 10 tablets or 1, 2 blister packs of 15 tablets or 1 blister pack of 30 tablets, together with instructions for use, are placed in a pack of cardboard.

Storage conditions
In a dry, dark place at a temperature not exceeding 25 ? C. Keep out of the reach of children.

Shelf life is
2 years. Do not use after the expiration date.

Terms of dispensing from pharmacies
Prescription.