Active substanceFosinoprilFosinopril
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  • Dosage form: & nbsppills
    Composition:

    1 tablet of 5 mg contains:

    active substance: fosinopril sodium 5 mg;

    Excipients: lactose monohydrate 59 mg, sodium croscarmellose 2 mg, starch corn pregelatinized corn (starch 1500) 12 mg, cellulose microcrystalline 20 mg, glycerol dibechenate 2 mg.

    1 tablet of 10 mg contains:

    active substance fosinopril sodium 10 mg; ; Excipients: lactose monohydrate 118 mg, croscarmellose sodium 4 mg, corn pregelatinized starch (starch 1500) 24 mg, cellulose microcrystalline 40.1 mg, glycerol dibehenate 4 mg.

    1 tablet of 20 mg contains: active substance fosinopril sodium 20 mg; auxiliary substances: lactose monohydrate 108 mg, croscarmellose sodium 4 mg, corn starch pregelatinized starch (starch 1500) 24 mg, microcrystalline cellulose 40 mg, glycerol dibenate 4 mg.


    Description:
    Round tablets are flat-cylindrical, white or almost white, labeled "FL 5" for a dosage of 5 mg, "FL 10" for a dosage of 10 mg, "FL 20" for a dosage of 20 mg.

    Pharmacotherapeutic group:angiotensin-converting enzyme (ACE) inhibitor
    ATX: & nbsp

    C.09.A.A   ACE Inhibitors

    C.09.A.A.09   Fosinopril

    Pharmacodynamics:
    ACE inhibitor. Refers to prodrugs. In the body of fosinopril formed active metabolite - fosinoprilat, which prevents the conversion of angiotensin-I into a vasoconstrictor substance, angiotensin. II, this leads to vasodilation and a decrease in the secretion of aldosterone. Has antihypertensive, vasodilating, diuretic and potassium-sparing effect. Reduces the overall peripheral vascular resistance and systemic blood pressure (BP). The drug inhibits the synthesis of aldosterone, inhibits tissue ACE. Antihypertensive effect is also due to the suppression of bradykinin metabolism, which has a pronounced vasodilating effect. Reduction of blood pressure is not accompanied by a change in the volume of circulating blood (BCC), cerebral and renal blood flow, blood supply to internal organs, skeletal muscles, skin, reflex activity of the myocardium.Antihypertensive effect persists with long-term treatment, tolerance does not develop. After ingestion, the antihypertensive effect develops within 1 hour, reaches a maximum after 2-6 hours, and persists for 24 hours. .

    Pharmacokinetics:
    After oral administration fosinopril absorbed from the gastrointestinal tract. Absorption averages 30 - 40%. The degree of absorption is not dependent on food intake, but its speed can be slowed down. The time to reach the maximum concentration in the blood plasma is 3 hours and does not depend on the dose taken.
    Communication with plasma proteins of fozinoprilat is 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 through the liver and kidneys.
    In patients with arterial hypertension with normal renal and hepatic function, the half-life (T 1/2) of fosinoprilata is approximately 11.5 hours. In patients with heart failure, the value of T 1/2 is 14 hours. The clearance of fosinoprilat in hemodialysis and peritoneal dialysis is, on average, 2% and 7%, respectively, with respect to the values ​​of urea clearance.
    In patients with impaired function; (creatinine clearance less than 80 ml / min / 1.73 m2), total clearance of fosinoprilite from the body is approximately twice lower than in patients with normal renal function. While absorption, bioavailability and association with proteins do not change noticeably. Reduced excretion through the kidneys is compensated by increased excretion through the liver. A moderate increase in the area under the curve / concentration-time (AUC) in the blood plasma (less than twice the norm) is observed in patients with renal insufficiency of various degrees, including renal failure in the terminal stage. (SC less than 10 ml / min / 1.73 m2).
    In patients with impaired function. liver (with alcoholic or biliary cirrhosis), the rate of hydrolysis of fosinopril may be reduced, but the degree of hydrolysis does not change noticeably. The total clearance of fosinoprilata from the body of such patients is approximately half as compared with patients with normal function, liver
    Indications:
    • Arterial hypertension (in monotherapy, or in combination with other antihypertensive drugs (in particular, with thiazide diuretics)).
    • Chronic heart failure (as part of combination therapy).

    Contraindications:Hypersensitivity to fosinopril or other components of the drug, hereditary and / or idiopathic angioedema, including in history, after taking other ACE inhibitors, pregnancy, lactation, age under 18 years (efficacy and safety not established), lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
    Carefully:kidney failure; hyponatremia (risk of dehydration, arterial hypotension, chronic renal failure), bilateral stenosis of the renal arteries or stenosis of the single kidney artery, aortic stenosis, condition after kidney transplantation, desensitization; systemic diseases of connective tissue (including systemic lupus erythematosus, scleroderma), increased risk of developing neutropenia or agranulocytosis, hemodialysis, cerebrovascular diseases (including cerebral circulatory insufficiency), coronary heart disease, chronic heart failure (III and IV functional class in NYHA classification),diabetes mellitus, oppression of bone marrow hematopoiesis, hyperkalemia, advanced age, diet with restriction of table salt, conditions accompanied by a decrease in BCC (including diarrhea, vomiting).
    Pregnancy and lactation:
    Fosicard is contraindicated for use during pregnancy. The use of ACE inhibitors in the second and third trimester of pregnancy causes damage or even death of the developing fetus. For newborns, mothers who were taking ACE inhibitors during pregnancy, careful monitoring is recommended for the timely detection of arterial hypotension of oliguria and hyperkalemia.
    Fosinopril is excreted in breast milk, so taking the drug during lactation is not recommended. If the drug is used during this period, breastfeeding should be discontinued.


    Dosing and Administration:
    Inside. Dosage should be selected individually.
    Arterial hypertension,
    The recommended initial dose of the drug is 10 mg once a day. The dose of the drug should be selected depending on the dynamics of blood pressure.
    The maintenance dose is 10-40 mg once a day.In the absence of a sufficient therapeutic effect, additional prescription of diuretics is possible.
    If treatment with Fosicard is initiated against a background of diuretic therapy, then its initial dose should not exceed 10 mg, with careful medical monitoring of the patient's condition.
    Chronic heart failure
    The recommended initial dose is 5 mg 1 or 2 times a day. Depending on the therapeutic effectiveness, the dose can be increased at a weekly interval up to a maximum daily dose of 40 mg once a day.
    Use in cases of impaired renal and / or liver function
    Correction of the dose is not required.
    Elderly patients
    Differences in efficacy and safety of drug treatment in patients aged 65 years and older and younger patients are not observed. However, it is impossible to exclude a greater susceptibility in some elderly patients to the drug, due to possible overdose phenomena due to delayed excretion
    preparation.
    Side effects:
    From the side of the cardiovascular system: a marked decrease in blood pressure, orthostatic hypotension, tachycardia, palpitations, arrhythmias, angina pectoris,myocardial infarction, chest pain, blood flushes to the skin of the face, hypertensive crisis, cardiac arrest / fainting.
    From the digestive tract: nausea, vomiting, constipation, intestinal obstruction, pancreatitis, hepatitis, stomatitis, glossitis, dyspepsia, abdominal pain, anorexia, intestinal edema, cholestatic jaundice, dysphagia, flatulence, anorexia, weight loss, dryness of the oral mucosa.
    On the part of the respiratory system: dry cough, shortness of breath, pharyngitis, laryngitis, sinusitis, pulmonary infiltrates, bronchospasm, dysphonia, dyspnea, nosebleeds, rhinorrhea.
    From the side of the urinary system: the development or aggravation of symptoms of chronic renal failure, proteinuria, oliguria.
    From the side of the central nervous system: stroke, cerebral ischemia, dizziness, headache, weakness; insomnia, anxiety, depression, confusion in high doses; paresthesia, drowsiness.
    From the sense organs; hearing and vision impairment, tinnitus.
    Allergic reactions: skin rash, itching, angioedema.
    On the part of the organs of hematopoiesis: inflammation of the lymph nodes.
    From the musculoskeletal system: arthritis. .
    From the side of metabolism: exacerbation of gout.
    On the part of laboratory indicators: hypercreatininaemia, increased urea concentration, increased activity of hepatic transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia; reduction of hemoglobin, and hematocrit, neutropenia, leukopenia, eosinophilia, accumulation of erythrocyte sedimentation rate (ESR).
    Influence on the fetus: impaired fetal kidney development, decreased fetal and newborn infants, impaired renal function, hyperkalemia, hypoplasia of the skull bones, oligohydramnion, limb contracture, lung hypoplasia.
    Overdose:
    Symptoms: marked decrease in blood pressure, bradycardia, shock, disturbance of water-electrolyte balance, acute renal failure, stupor.
    Treatment: the drug should be discontinued, gastric lavage, intake of sorbents (eg activated charcoal), vasodepressor agents, infusion of 0.9% sodium chloride solution and further symptomatic and supportive treatment.
    The use of hemodialysis is ineffective.

    Interaction:
    Antacids. The simultaneous use of antacids (eg, aluminum or magnesium hydroxide, simethicone) can reduce the absorption of the drug Fosicard. Therefore, it is necessary to apply these means with an interval of at least 2 hours.
    Lithium. With the simultaneous use of ACE inhibitors with lithium salts, the concentration of lithium in the blood serum and the risk of lithium intoxication may increase, so at the same time use Fosicard and lithium preparations with caution.
    Non-steroidal anti-inflammatory drugs (NSAIDs). NSAIDs can reduce the antihypertensive effect of other ACE inhibitors, especially in patients with hypertension and low renin plasma concentrations.
    Diuretics. With simultaneous use of diuretics, in combination with a strict diet that limits consumption of table salt or with dialysis, a marked decrease in blood pressure may develop, especially in the first hour after taking the initial dose of the drug Fosicard.
    Potassium preparations, potassium-sparing diuretics (amiloride, spironolactone, triamterene) increase the risk of hyperkalemia. In patients with heart failure, diabetes mellitus,simultaneously taking potassium-sparing diuretics, potassium, potassium-containing cleavers or other agents that cause hyperkalemia (eg, heparin), ACE inhibitors increase the risk of increasing serum potassium.
    Fosinopril enhances the hypoglycemic effect of sulfonylurea derivatives, insulin, the risk of developing leukopenia with simultaneous applications with allopurinol, cytostatic agents, immunosuppressants, procainamide. Estrogens weaken the antihypertensive effect of fosinopril because of its ability to retain water.
    Hypotensive, narcotic analgesics, drugs for general anesthesia increase the antihypertensive effect of the drug Fosicard.
    Bioavailability of the drug with simultaneous application, with chlorthalidone, nifedipine, propranolol, hydrochlorothiazide, cimetidine, metoclopramide, propanthelin 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, restriction of ration for salt and / or fluid and other clinical circumstances.
    Patients with severe hypertension or concomitant decompensated chronic heart failure should begin treatment with Focicard in a hospital setting.
    Before and during treatment, the drug requires control of blood pressure, kidney function, potassium content, hemoglobin, creatinine, urea concentration, electrolyte concentration and activity of "hepatic" transaminases in the blood.
    Angioedema
    It was reported on the development of angioedema in patients with Fozicard. With edema of the tongue, throat or larynx, it can develop - airway obstruction with possible fatal outcome. In case of development of similar reactions, patients should stop taking the drug and subcutaneous injection of epinephrine (adrenaline) solution (1: 1000), as well as taking other measures of emergency therapy.
    Swelling of the intestinal mucosa .
    During the administration of ACE inhibitors, edema of the intestinal mucosa was rarely observed. These patients complained of abdominal pain (with nausea and vomiting may not be), in some cases, edema of the intestinal mucosa appeared without edema of the face, the level of Cl-esterases was normal.Symptoms disappeared after the cessation of the use of ACE inhibitors. Swelling of the intestinal mucosa should be included in the differential diagnosis of patients taking ACE inhibitors who complain of abdominal pain.
    Anaphylactic reactions during dialysis using high-permeability membranes can lead to anaphylactic reactions in patients using ACE inhibitors during hemodialysis through high-permeability membranes, as well as during apheresis of low-density lipoproteins adsorbed to dextran sulfate.
    In these cases, one should consider the possibility of using dialysis membranes of a different type or other antihypertensive therapy.
    Neutropenia / agranulocytosis
    Perhaps the development of agranulocytosis and suppression of bone marrow function during treatment with ACE inhibitors. These cases are noted more often in patients with impaired renal function, especially in the presence of systemic connective tissue diseases (systemic lupus erythematosus or scleroderma). Before the beginning of therapy with ACE inhibitors, and during the treatment, the total number of leukocytes and the leukocyte formula is determined (once a month for the first 3-6 months of treatment and the firstyear of use of the drug in patients with an increased risk of neutropenia).
    Arterial hypotension
    Patients with uncomplicated form of hypertension may develop arterial hypotension due to the use of the drug Fozicard.
    Symptomatic arterial hypotension with ACE inhibitors most often develops in patients after intensive treatment with diuretics, a diet limiting intake of table salt; or with renal dialysis. Transient arterial hypotension is not a contraindication for the use of the drug after taking measures to restore BCC.
    In patients with chronic heart failure, treatment with ACE inhibitors can cause an excessive antihypertensive effect, which can lead to oliguria or azotemia with a fatal outcome. Therefore, in the treatment of chronic heart failure with Fosicard, patients should be closely monitored, especially during the first 2 weeks of treatment, as well as with any increase in the dose of the drug Fosicard or diuretic.
    It may be necessary to reduce the dose of diuretic in patients with hyponatremia and patients previously intensively treated with diuretics.Arterial hypotension is not a contraindication for further use of the drug Fosicard. Some, lowering systemic BP is a common and desirable effect at the beginning of the drug in heart failure. The degree of this decrease is maximal at early stages of treatment and stabilizes within one or two weeks from the start of treatment. BP usually returns to the values ​​of the period before the start of treatment without decreasing the therapeutic effectiveness.
    Impaired liver function
    If there is a noticeable icterus and a marked increase in the activity of liver enzymes, treatment with Fosicard should be discontinued and appropriate treatment should be prescribed. .
    Impaired renal function
    In patients with arterial hypertension with bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney, and also with the simultaneous use of diuretics without signs of renal dysfunction during treatment with ACE inhibitors, concentration of blood urea nitrogen and serum creatinine may result. These effects are usually reversible and pass after discontinuation of treatment. You may need to reduce the dose of a diuretic and / or Fosicard.
    In patients with severe chronic heart failure, with altered activity of the renin-angiotensin-aldosterone system, treatment with ACE inhibitors can lead to oliguria, progressive azotemia and, in rare cases, acute renal failure and possible fatal outcome.
    Surgical interventions / general anesthesia
    ACE inhibitors can enhance the antihypertensive effect of agents used for general anesthesia. Before surgery (including dentistry), it is necessary to alert the surgeon / anesthesiologist about the use of ACE inhibitors.
    Care must be taken when driving vehicles or doing other work that requires increased attention, since it may cause dizziness; especially after the initial dose of an ACE inhibitor in patients taking diuretics. 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 BCC.
    Safety and efficacy of Fosicard in children is not established.
    Effect on the ability to drive transp. cf. and fur:
    Care must be taken when driving vehicles and working with mechanisms that require a high concentration of attention and speed of psychomotor reactions.

    Form release / dosage:
    Tablets 5 mg, 10 mg and 20 mg. .

    Packaging:
    For 7, 10 or 14 tablets in a blister pack. For 4 blisters for 7 tablets or 3 blisters for 10 tablets or 2 blisters for 14 tablets together with instructions for use in a cardboard bundle.

    Storage conditions:
    At a temperature of no higher than 30 ° C.
    Keep out of the reach of children!

    Shelf life:
    2 years.
    The drug should not be used after the expiry date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-000839
    Date of registration:31.08.2010
    The owner of the registration certificate:Actavis PTS ehf GroupActavis PTS ehf Group Iceland
    Manufacturer: & nbsp
    Information update date: & nbsp26.20.2015
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