Active substanceFosinoprilFosinopril
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  • Dosage form: & nbsppills
    Composition:
    In 1 tablet contains: active substance fosinopril sodium 10.0 mg / 20.0 mg; Excipients: lactose 146.2 mg / 136.2 mg, povidone-KZO 6.0 mg / 6.0 mg, crospovidone 5.0 mg / 5.0 mg, microcrystalline cellulose 20.0 mg / 20.0 mg, sodium lauryl sulfate 8 , 0 mg / 8.0 mg, glyceride dibehenate 4.8 mg / 4.8 mg.

    Description:
    Tablets 10 mg: white or almost white round flat-cylindrical tablets with a risk on both sides and with engraving on one side of the "F" and "10" on both sides of the risks.
    Tablets of 20 mg: white or almost white capsular biconvex tablets with engraving "93" on one side and "7223" on the other.

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

    C.09.A.A   ACE Inhibitors

    C.09.A.A.09   Fosinopril

    Pharmacodynamics:
    Fosinopril is a prodrug, the chemical structure is an ester. In the body, as a result of hydrolysis of fozyanopril under the action of enzymes, an active compound, fosinoprilate, is formed. The fosinopril molecule contains a phosphine group that binds to the active sites of the ACE molecule, prevents the conversion of angiotensin I decapeptide to octapeptide angiotensin II, which has a pronounced vasoconstrictor activity. As a result of lowering the level of angiotensin II and suppressing vasopressor activity, the secretion of aldosterone decreases. The latter effect can lead to an insignificant
    an increase in the content of potassium ions in the serum (an average of 0.1 meq / L) with the simultaneous loss of sodium and liquid ions by the body.
    Fosinopril inhibits the metabolic degradation of bradykinin, which has a powerful vasodilating effect; due to this, the antihypertensive effect of the drug can be enhanced.
    Reduction of blood pressure (BP) is not accompanied by significant changes in the volume of circulating blood, cerebral and renal blood flow, blood supply to internal organs, skeletal muscles, skin,reflex activity of the myocardium. After ingestion, the antihypertensive effect develops within 1 hour, reaches a maximum after 3-6 hours and persists for 24 hours. In some patients, the reduction in blood pressure to the optimal level is achieved only after 3-4 weeks of treatment. In heart failure, the positive effects of fosinopril are achieved mainly by suppressing the activity of the renin-angiotensin-aldosterone system (RAAS). Inactivation of ACE leads to a decrease in both preload and postload on the myocardium.
    The drug improves exercise tolerance, reduces the severity of heart failure and the frequency of hospitalizations. In patients with cirrhosis of the liver fosinopril does not affect the functions of the liver and kidneys.
    Pharmacokinetics:
    Suction. After ingestion, absorption from the gastrointestinal tract (GIT) 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.
    Fast and almost complete hydrolysis with the formation of pharmacologically active fosinoprilata occurs in the mucosa of the small intestine and liver.An hour after ingestion, the concentration of unchanged fosinopril in serum is less than 1%, fosinoprilat 75%, inactive fosinoprilate glucuronide 15-20%, active metabolite 4-hydroxyfosinoprilate - about 5%.
    The maximum concentration (Сmах) of fosinoprilat in blood plasma is reached after 3 hours and does not depend on the dose taken.
    Distribution and metabolism. Binding to plasma proteins is more than 95%. Therefore, fosinoprilat has a relatively small volume of distribution and is slightly associated with the cellular components of the blood.
    Excretion. Fosinoprilat from the body is equally excreted by the kidneys and through the intestines. In arterial hypertension in patients with normal renal and hepatic function, the half-life (T1 / 2) of fosinoprilata is about 11.5 hours. In heart failure, T 1/2 increases to 14 hours.
    In patients with impaired renal function (creatinine clearance less than 80 ml / min / 1.73 m2), the total clearance of fosinoprilat from the body is approximately twice lower than in patients with normal renal function. At the same time, absorption, bioavailability and binding to proteins are not significantly altered.Reduced excretion by the kidneys is compensated by increased excretion of the liver.
    A moderate increase in the area under the concentration-time curve (AUC) of fosinoprilat in blood plasma (less than twice the norm) was observed in patients with renal insufficiency of various degrees, including renal failure at the terminal stage (creatinine clearance less than 10 ml / min / 1.73 m2). The clearance of fosinoprilat in hemodialysis and peritoneal dialysis is 2% and 7%, respectively (relative to urea clearance values, respectively).
    In patients with impaired hepatic function (with alcoholic or biliary cirrhosis) there is no significant change in the degree of hydrolysis of fosinopril, but a decrease in the rate of this biochemical reaction may occur.
    The total clearance of fosinoprilata from the body of such patients is approximately twice lower than in patients with normal liver function.
    In men aged 65 to 74 years with clinically normal renal and hepatic function, no noticeable differences in the pharmacokinetic parameters of fosinoprilat are observed in comparison with younger patients (20-35 years).

    Indications:
    • Arterial hypertension;
    • chronic heart failure (as part of combination therapy).

    Contraindications:
    Hypersensitivity to fosinopril, other components of the drug and other ACE inhibitors; angioedema in history (hereditary, idiopathic or associated with the use of ACE inhibitors); pregnancy; the period of breastfeeding; age to 18 years; lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

    Carefully:
    Simultaneous use with diuretics, nitrates, vasodilators, potassium preparations, heparin, potassium-sparing diuretics, antacids, lithium preparations, non-steroidal anti-inflammatory drugs drugs (NSAIDs), insulin, hypoglycemic agents for oral administration, tricyclic antidepressants, antipsychotic drugs, opioid analgesics, drugs for general anesthesia, immunosuppressants, sympathomimetics, cytostatics, corticosteroids, procainamide, allopurinol; chronic heart failure (CHF) of III and IV functional class according to NYNA classification; state,accompanied by a decrease in the volume of circulating blood (BCC); ischemic heart disease (IHD); cerebrovascular diseases; Renovascular hypertension; bilateral stenosis of the renal arteries; stenosis of the artery of a single kidney; systemic connective tissue diseases (scleroderma, systemic lupus erythematosus); hyperkalemia; stenosis of the aortic valve; hypertrophic obstructive cardiomyopathy; uncontrolled diabetes mellitus; hemodialysis; plasmapheresis; when desensitizing or carrying out desensitization procedures; oppression of bone marrow hematopoiesis, elderly age, condition after kidney transplantation.

    Pregnancy and lactation:
    The drug Fosinopril-Teva is contraindicated in pregnancy. The use of ACE inhibitors in the P and III trimesters of pregnancy causes damage or even death of the developing fetus. If pregnancy is detected, treatment with fosinopril should be stopped immediately. For newborns whose mothers took ACE inhibitors during pregnancy, careful monitoring is recommended for the timely detection of arterial hypotension, oliguria and hyperkalemia.Because fosinoprilat is excreted in breast milk, if it is necessary to use Fosinopril-Teva, breast-feeding should be discontinued.

    Dosing and Administration:
    Inside. The tablet is swallowed without chewing, drinking a glass of water, regardless of the meal, preferably at the same time.
    If you miss one or more doses in the next dose, the drug Fosinopril-Teva should be taken in the usual dose; take a higher dose should not be.
    Arterial hypertension. The recommended initial dose is 10 mg once a day. Then the dose is selected depending on the dynamics of blood pressure lowering; in the absence of the desired therapeutic effect for 3-4 weeks, the dose may be increased. Supportive doses range from 10 mg to a maximum dose of 40 mg once daily. With the use of ACE inhibitors, patients receiving diuretic therapy may experience a sharp drop in blood pressure, for the prevention of which it is recommended to stop taking diuretics 2-3 days before the expected start of fosinopril therapy.
    If it is not possible to cancel diuretics, the drug Fosinopril-Teva should be used at an initial dose of 10 mg once a day.Patients with high RAAS activity (especially patients with renal vascular hypertension, water-electrolyte balance disorders, decompensated CHF, or severe arterial hypertension), it is recommended to start the treatment with Fosinopril-Teva because of the possibility of a sudden decrease in blood pressure under the supervision of a doctor.
    Chronic heart failure. The recommended initial dose is 10 mg once a day. Begin the treatment should be under the supervision of a doctor. With good tolerability, the dose is increased at a weekly interval, increasing it to 40 mg once a day. For the treatment of CHF, the preparation of Fosinopril-Teva is usually combined with diuretics and, if necessary, cardiac glycosides.
    Elderly patients
    Differences in efficacy and safety of drug treatment in elderly patients aged 65 years and older and young 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 of fosinopril.
    In patients with impaired renal or hepatic function, a dose reduction of Fosinopril-Teva is usually not required.

    Side effects:
    The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely (including isolated cases) - less than 0.01%.
    From the hemopoietic system and lymphatic system: infrequently - transient reduction of hemoglobin or hematocrit; rarely - eosinophilia, leukopenia, thrombocytopenia, neutropenia, lymphadenopathy; very rarely - agranulocytosis.
    From the side of metabolism: infrequently - a decrease in appetite, exacerbation of gout, hyperkalemia.
    From the side of the central nervous system: often - dizziness, headache; infrequently - depression, paresthesia, drowsiness, stroke, cerebral ischemia, tremor, sleep disturbance, taste disorders; rarely - speech disturbance, memory impairment, confusion, disorientation.
    From the side of the organ of vision: infrequently - visual disorders.
    From the organ of hearing and the vestibular apparatus: infrequently - noise in the ears, pain in the ears, dizziness.
    From the cardiovascular system: often - tachycardia,marked decrease in blood pressure, orthostatic hypotension; infrequently - angina, myocardial infarction, palpitations, cardiac arrest, arrhythmia, increased blood pressure, peripheral edema; rarely - "tides" of blood to the skin of the face, hemorrhage, violation of peripheral circulation.
    From the respiratory system: often - dry cough; infrequently - shortness of breath, rhinitis, pharyngitis, tracheobronchitis; rarely - bronchospasm, pneumonia, pulmonary infiltrates.
    From the side of the digestive tract: often - nausea, vomiting, diarrhea; infrequently - constipation, dryness of the oral mucosa, flatulence; rarely - stomatitis, pancreatitis, angioedema, dysphagia, abdominal pain; very rarely - angioedema, intestinal obstruction.
    From the liver and biliary tract: rarely - hepatitis; very rarely liver failure.
    From the skin and subcutaneous tissues: often - skin rash, angioedema, dermatitis; infrequently - increased sweating, itching, hives; rarely - hemorrhages in the skin (ecchymosis).
    A symptom complex including fever, vasculitis, muscle pain, joints or arthritis, antinuclear antibodies, increased erythrocyte sedimentation rate, eosinophilia and leukocytosis, rash, photosensitivity and other skin manifestations has been described.
    From the musculoskeletal system: infrequently - myalgia; rarely - arthralgia, arthritis.
    From the side of the urinary system: infrequently - proteinuria, development or aggravation of symptoms of chronic renal failure, violations of the prostate gland; rarely acute interstitial nephritis; very rarely acute renal failure.
    On the part of the reproductive system: infrequently - impotence, decreased libido.
    Other: often - general weakness, pain of unspecified localization; infrequently - fever, sudden death, weight gain; rarely - muscle weakness.
    On the part of laboratory indicators: often - increased activity of "liver" transaminases, lactate dehydrogenase and alkaline phosphatase, hyperbilirubinemia; infrequently - hypercreatininaemia, increased urea concentration, hyperkalemia;
    rarely - hyponatremia, a slight increase in hemoglobin. Fosinopril may underestimate the results of serum digoxin concentrations.

    Overdose:
    Symptoms: marked decrease in blood pressure, shock, stupor, bradycardia, abnormal water electrolyte balance, renal failure, temporary hyperventilation of the lungs, tachycardia, palpitation, dizziness, anxiety and cough.
    Treatment: the patient should be placed in the intensive care unit, with careful monitoring of serum electrolytes and creatinine. To reduce the absorption of the drug, it is necessary to wash the stomach, administer adsorbents and sodium sulfate within 30 minutes after taking fosinopril a. In case of a marked decrease in blood pressure, put the patient with raised legs on the bed and make a rapid intravenous (iv) injection of 0.9% sodium chloride solution, iv injection of catecholamines. With severe bradycardia - the administration of atropine sulfate, in some cases it may be necessary to use an artificial pacemaker. Fosinoprilat is not excreted during dialysis.
    Interaction:
    Diuretics, ethanol, nitroglycerine, other nitrates and vasodilators increase the antihypertensive effect of fosinopril.
    With the simultaneous use of fosinopril with potassium preparations, heparin, potassium-sparing diuretics (including amiloride, spironolactone, triamterene), with additives to food containing potassium, the risk of hyperkalemia increases, especially in patients with heart failure and diabetes mellitus.Simultaneous use of antacids (including aluminum hydroxide, magnesium hydroxide, simethicone) can reduce the absorption of an ACE inhibitor.
    With the use of ACE enzyme inhibitors with lithium preparations, a reversible increase in the concentration of lithium in the blood plasma and a corresponding increase in the risk of its toxic effect are possible.
    NSAIDs reduce the antihypertensive effect of ACE inhibitors, while providing a synergistic effect on the increase in potassium levels in the blood plasma, and can also cause renal dysfunction.
    Simultaneous use of ACE inhibitors and drugs that reduce the concentration of glucose in the blood (insulin, hypoglycemic agents for ingestion) can cause a further decrease in blood glucose and the risk of hypoglycemia, especially in the first weeks of treatment, and in patients with renal insufficiency.
    The simultaneous use of certain tricyclic antidepressants, antipsychotics, anesthetics (including opioid analgesics and drugs for general anesthesia) with ACE inhibitors may lead to a further decrease in blood pressure and the development of orthostatic hypotension.
    Sympathomimetics reduce the antihypertensive effect of ACE inhibitors.
    When used simultaneously with immunosuppressants, cytostatics, glucocorticosteroids for systemic use, procainamide and allopurinol, there is a risk of developing leukopenia.
    Fosinopril may underestimate the results of digoxin concentration in serum.

    Special instructions:
    Before using Fosinopril-Teva and during its administration, blood pressure, renal function, the number of blood elements, potassium content, creatinine concentration and glucose in blood serum should be closely monitored.
    A few days before the start of therapy with the drug Fosinoril-Teva, the previous antihypertensive treatment should be discontinued.
    In severe CHF III and IV functional class according to the classification of NYNA and also in patients from other risk groups, treatment should be started under the supervision of a doctor. Patients with violations of water-electrolyte balance are recommended to correct water-electrolyte disorders before starting treatment with the drug Fozinopril-Teva. Patients who use insulin or hypoglycemic agents for oral administration,while concurrent administration of ACE inhibitors, it is necessary to monitor the concentration of glucose in the blood, especially during the first month of use. In conditions accompanied by a decrease in BCC (diuretic intake, salt-free diet, vomiting, diarrhea, hemodialysis), renin-dependent hyponatremia, cerebrovascular diseases, IHD, the risk of a sharp decrease in blood pressure increases.
    With renovascular hypertension, bilateral stenosis of the renal arteries, or stenosis of the artery of a single functioning kidney, the risk of developing severe arterial hypotension and renal failure increases. In addition, during treatment with ACE inhibitors, the concentrations of urea and creatinine in serum can increase. These effects usually develop in patients with renal insufficiency, they are reversible and pass after discontinuation of treatment.
    With systemic diseases of connective tissue (systemic lupus erythematosus, scleroderma) and immunosuppressant therapy (including after kidney transplantation), the risk of developing neutropenia, agranulocytosis increases.
    With hyperkalemia, with stenosis of the aortic valve, hypertrophic obstructive cardiomyopathy,CHF III and IV of the functional class according to the classification of NYNA, when treating hypoglycemic drugs in patients with diabetes mellitus, the risk of developing hypoglycemia increases.
    Against the background of taking ACE inhibitors, potassium levels in the serum can be increased. Patients with a risk of hyperkalemia, namely, patients with renal insufficiency, uncontrolled diabetes mellitus, taking potassium-sparing diuretics, potassium preparations or other medications that may lead to an increase in serum potassium (eg, heparin) may cause hyperkalemia.
    When hemodialysis using high-flow polyacrylonitrile membranes, plasmapheresis with the use of dextran sulfate in patients with elevated levels of low-density lipoproteins, as well as specific desensitization to bee venom, the risk of allergic reactions increases. To prevent the development of anaphylactoid reactions in the conduct of plasmapheresis, the administration of an ACE inhibitor is temporarily stopped before the procedures are started.
    Angioedema, swelling of the face, limbs, lips, mucous membranes, tongue,vocal folds and / or larynx can develop with the use of ACE inhibitors, especially during the first few weeks of therapy. In rare cases, severe angioedema may occur with prolonged use of the drug. In such cases fosinopril should immediately be abolished and apply an antihypertensive drug of another pharmacological class.
    In patients with arterial hypertension, symptomatic arterial hypotension with ACE inhibitors most often develops after intensive treatment with diuretics, diets restricting table salt, against diarrhea, vomiting, or in patients on hemodialysis.
    In patients with heart failure with concomitant renal failure or without it, the risk of a sharp decrease in blood pressure on the background of hyponatremia, after previous intensive therapy with diuretics, as well as in elderly patients, increases.
    Temporary arterial hypotension is not a contraindication for the use of the drug after taking measures aimed at increasing the BCC.
    In order to reduce the risk of symptomatic arterial hypotension,who take diuretics, it is recommended to stop taking them 2-3 days before the start of treatment with the drug Fosinopril-Teva. If diuretics can not be canceled, the treatment should begin with a minimum dose of 10 mg. Further increase in the dose is carried out under the control of blood pressure.
    In some patients with heart failure who initially had normal or low blood pressure, with the onset of Fosinopril-Teva, a further moderate decrease in systemic blood pressure is possible, which is a common effect at the beginning of the drug.
    During the application of Fosinopril-Teva, a dry cough may appear, which disappears after the drug is withdrawn. If necessary, treatment can be continued.
    In the case of jaundice or a significant increase in the activity of "liver" enzymes, the use of an ACE inhibitor should be discontinued and the patient should be carefully monitored.
    During the administration of ACE inhibitors, edema of the intestinal mucosa was rarely seen, often in the absence of nausea and vomiting, which disappeared after the cessation of the use of ACE inhibitors. Swelling of the intestinal mucosa should be considered in differential diagnosis in patients withcomplaints of abdominal pain, developed against the background of treatment with ACE inhibitors.
    In surgical intervention (general anesthesia), the possibility of developing arterial hypotension increases.
    An anesthesiologist should be informed of the use of Fosinopril-Teva if an anesthetic or surgical procedure is planned for the patient. Treatment with an ACE inhibitor should be discontinued one day before surgery.
    Patients taking the drug Fosinopril-Teva should be careful when doing physical exercises or in hot weather because of the risk of dehydration and arterial hypotension due to a decrease in BCC.
    It is not recommended to use the drug Fosinopril-Teva concomitantly with preparations cast. If it is necessary to use such a combination, it is necessary to monitor the concentration of lithium in the blood plasma.
    Children and adolescents under the age of 18 years (safety and efficacy not established).

    Effect on the ability to drive transp. cf. and fur:
    Care should be taken during the application of the drug Fshinopril-Teva due to the possible development of adverse reactions,which can adversely affect the ability to drive vehicles and perform potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

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


    Packaging:
    For 10 tablets in a blister of PVC / aluminum foil or PVC / PVDC / acuminium foil. For 3 blisters per pack of cardboard along with instructions for use.
    For 7 tablets in blister pvc / aluminum foil or PVC / PVDC / alumina foil. For 2 or 4 blisters in a pack of cardboard along with instructions for use.
    Storage conditions:
    Store at a temperature of no higher than 25 ° C, in a place protected from light.
    Keep out of the reach of children.

    Shelf life:
    Tablets 10 mg - 1,5 years.
    Tablets 20 mg - 2 years.
    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001837
    Date of registration:13/09/2012
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Information update date: & nbsp25.10.2015
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