Active substanceFosinoprilFosinopril
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  • Dosage form: & nbsppills
    Composition:
    Tablets 10 mg Each tablet contains:
    Active substance:
    Fosinopril sodium 10 mg
    Excipients: lactose, microcrystalline cellulose, crospovidone, povidone, colloidal silicon dioxide, talc.
    Tablets 20 mg
    Each tablet contains:
    Active substance:
    Fosinopril sodium 20 mg
    Excipients: lactose, microcrystalline cellulose, crospovidone, povidone, colloidal silicon dioxide, talc.

    Description:
    Tablets 10 mg
    White to almost white in color, an oval shaped tablet with a separation risk on both sides and engraved "F" and "10" on one side of the tablet on both sides of the separation hazard.
    Tablets 20 mg
    White to almost white,oblong tablets with a separation risk on both sides and engraved "F" and "20" on one side of the tablet on either side of the dividing risk.

    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. Is a prodrug. In the body of fosinopril formed active metabolite - fosinoprilat, which prevents the conversion of angiotensin I into the vasoconstrictor substance angiotensin II, this leads to vasodilation and a decrease in the secretion of aldosterone. Has hypotensive, 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.
    In chronic heart failure (CHF), the positive effects of fosinopril are achieved mainly by suppressing the renin-angiotensin aldosterone system. Suppression of the angiotensin-converting enzyme leads to a reduction in both preload and post-loading on the myocardium.
    The hypotensive effect is also due to the suppression of the metabolism of bradykinin, which has a pronounced vasodilating effect. The hypotensive effect of the drug persists with long-term treatment, tolerance to the drug does not develop. After ingestion, the hypotensive effect develops within 1 hour, reaches a maximum after 2-6 hours, and lasts 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.
    Connection with blood plasma proteins - 95%. Fosinopril has a relatively small volume of distribution. Does not penetrate the blood-brain barrier.
    In the mucosa of the gastrointestinal tract and, in part, in the liver fosinopril it is hydrolyzed to fosinoprylate.
    Fosinoprilat is excreted through the intestines and kidneys.
    In patients with arterial hypertension with normal renal and hepatic function, the half-life (T1 / 2) of fosinoprilat is approximately 11.5 hours.In patients with CHF T1 / 2 is 14 hours. The clearance of fosinoprilat for hemodialysis and peritoneal dialysis is on average 2% and 7%, respectively, relative to the values ​​of urea clearance.
    In patients with impaired renal function (creatinine clearance less than 80 ml / min), the total clearance of fosinoprilat is approximately half that of patients with normal renal function. At the same time, both absorption, bioavailability and association with plasma proteins are not significantly altered.
    In patients with impaired liver function (with alcoholic or biliary cirrhosis), the rate of hydrolysis of fosinopril may be reduced, but the degree does not change significantly.
    The total clearance of fosinoprilat in these patients is approximately half that of patients with normal liver function.

    Indications:
    Arterial hypertension.
    Chronic heart failure (as part of combination therapy).

    Contraindications:
    • hypersensitivity to fosinopril or other components of the drug;
    • hereditary or idiopathic angioedema, including in the anamnesis, after taking other ACE inhibitors;
    • pregnancy and lactation;
    • age to 18 years;
    • deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

    Carefully:
    The drug should be taken with caution in renal 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 desensitisation, systemic connective tissue diseases including systemic lupus erythematosus, scleroderma) - increased risk of developing neutropenia or agranulocytosis; hemodialysis, cerebrovascular diseases (including cerebral circulatory insufficiency), ischemic heart disease, chronic cardiac insufficiency III and IV functional class according to the NYHA classification, diabetes mellitus, oppression of bone marrow hematopoiesis, hyperkalemia, old age, diet with restriction of table salt, conditions , accompanied by a decrease in the volume of circulating blood (BCC) (including diarrhea, vomiting).

    Pregnancy and lactation:
    The use of the drug Fozinotek is contraindicated in pregnancy.The use of ACE inhibitors in the II and III trimester can cause damage or even death of the fetus (possibly development of violations of kidney fetus, lowering blood pressure, hypoplasia of the skull bones, oligohydramnia, limb contracture, lung hypoplasia).
    Fosinopril is excreted in breast milk. If you need to use the drug Fosinotek during lactation, breastfeeding should be discontinued.

    Dosing and Administration:
    Inside. The dose should be selected individually.
    In the treatment of hypertension, it is necessary, if possible, to stop taking antihypertensive drugs several days before starting taking Fosinotek. The initial dose is 10 mg once a day. The further dose of the drug is selected depending on the dynamics of lowering blood pressure. The maintenance dose is 10-40 mg once a day. In the absence of a sufficient hypotensive effect from monotherapy with Fosinotek, additional diuretics may be prescribed.
    If treatment with Fosinotek begins with a diuretic, the initial dose of the drug Fosinotek should not exceed 10 mg with careful medical supervision.
    In the treatment of chronic heart failure, the initial dose of the drug Fozinotek is 10 mg 1 time per day. Then the dose of the drug is selected in accordance with the dynamics of therapeutic effectiveness, increasing by 10 mg with a weekly interval. The maximum dose is 40 mg per day. Possible additional appointment of a diuretic.
    Dose adjustments in patients with impaired renal and / or liver function are usually not required.

    Side effects:
    On the part of the cardiovascular system: lowering blood pressure, orthostatic hypotension, tachycardia, palpitations, arrhythmias, angina pectoris, myocardial infarction, chest pain.
    On the part of the digestive system: nausea, vomiting, constipation, intestinal obstruction, pancreatitis, hepatitis, stomatitis, glossitis, dyspepsia, abdominal pain, anorexia, cholestatic jaundice, intestinal angioedema.
    On the part of the respiratory system: dry cough, shortness of breath, pharyngitis, laryngitis, sinusitis, pulmonary infiltrates, bronchospasm, dysphonia.
    From the urinary system: development or aggravation of symptoms of chronic renal failure, proteinuria, oliguria.
    From the central nervous system: stroke, cerebral ischemia, dizziness, headache, weakness; when used in high doses - insomnia, anxiety, depression, confusion, paresthesia.
    From the sense organs: hearing and vision impairment, noise in the ears, disturbances from the vestibular apparatus.
    Allergic reactions: skin rash, itching, angioedema.
    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, agranulocytosis, increased erythrocyte sedimentation rate (ESR).
    Other: musculo-articular pain.
    There have been reports of cases of hypoglycemia in patients with diabetes who took insulin and hypoglycemic agents for oral administration.

    Overdose:
    Symptoms: marked decrease in blood pressure, bradycardia, shock, violation of water
    electrolyte balance, acute renal failure, stupor.
    Treatment: stop taking the drug, lay the patient with legs elevated.In mild cases of overdose - gastric lavage, the introduction of sorbents within 30 minutes after an overdose. With a pronounced decrease in blood pressure, intravenous administration of catecholamines, angiotensin II; at a bradycardia - application of the artificial driver of a rhythm. Hemodialysis is ineffective.

    Interaction:
    Hypotensive drugs, diuretics, narcotic analgesics, means for general anesthesia, ethanol, alprostadil, antidepressants, anxiolytics and hypnotics, nitrates increase the hypotensive effect of fosinopril.
    Potassium preparations, potassium-sparing diuretics, epoetins increase the risk of hyperkalemia.
    With simultaneous administration with lithium preparations, an increase in the concentration of lithium in the blood is possible.
    The drug enhances the hypoglycemic effect of derivatives of sulfonylurea, insulin, the risk of developing leukopenia with simultaneous use with allopurinol, cytostatic agents, immunosuppressants, procainamide.
    Nonsteroidal anti-inflammatory drugs and estrogens reduce the severity of the hypotensive effect.
    Antacids reduce the absorption of ACE inhibitors in the gastrointestinal tract.Bioavailability of the drug with simultaneous use with chlorthalidone, nifedipine, propranolol, hydrochlorothiazide, cimetidine, metoclopramide, propanthelin bromide, digoxin, acetylsalicylic acid and warfarin does not change.
    With simultaneous use of ACE inhibitors and preparations of gold (sodium aurotomy malate) describes a symptom complex, which includes flushing of the facial skin, nausea, vomiting and a decrease in blood pressure.

    Special instructions:
    Patients with severe course of arterial hypertension or concomitant CHF in decompensation should begin treatment with Fosinotek in a hospital setting.
    In rare cases, it is possible to develop arterial hypotension. Symptomatic arterial hypotension with ACE inhibitors is most likely in patients after intensive treatment with diuretics and / or restriction of salt intake or during hemodialysis. Transient arterial hypotension is not a contraindication for further use of the drug, after correction of the BCC.
    In patients with CHF in the presence or absence of impaired renal function, therapy with ACE inhibitors can cause an excessive hypotensive effect,which can lead to oliguria or azotemia, and in rare cases to acute renal failure and death. Therefore, in the treatment of CHF with Fosinotek, monitoring of the patient's condition is necessary, especially during the first two weeks of therapy, as well as with any increase in dose and / or diuretic.
    Patients with bilateral renal artery stenosis, renal artery stenosis or a single kidney, and while the use of diuretics ACE during therapy can increase the content of urea nitrogen and serum creatinine inhibitors. These effects are usually reversible and pass after discontinuation of therapy. You may need to reduce the dose of a diuretic and / or Fosinotek.
    Before and during the treatment with Fozinotek necessary to monitor blood pressure, renal function, the content of potassium ions, hemoglobin, creatinine, urea, electrolytes and activity concentration "liver" enzymes in the blood.
    While taking Fozinotek drug should periodically monitor the total number of leukocytes and leukocyte formula (1 once a month during the first 3-6 months of therapy.), Especially in patients with an increased risk of neutropenia: with impaired renal function and systemic connective tissue diseases, as well as first signs of infection.
    In patients with CHF, diabetes mellitus, concurrently taking potassium-sparing diuretics, potassium supplements, potassium-containing salt substitutes, or other agents that increase serum potassium levels (eg, heparin), ACE inhibitors increase the risk of hyperkalemia.
    Because of the increased risk of developing arterial hypotension, care should be taken when prescribing the drug to patients on a low-salt or salt-free diet.
    The safety and effectiveness of the use of the drug Fosinotek in children under 18 years of age is not established.
    Caution should be exercised when performing physical exercises or in hot weather due to the risk of dehydration and a decrease in blood pressure due to a decrease in BCC.
    Before surgery (including dentistry), an anesthesiologist should be warned about the use of an ACE inhibitor.
    Caution should be exercised when treating patients with ACE inhibitors during desensitization procedures.
    Care must be taken when driving vehicles or performing any work that requires increased attention, especially after taking the initial dose of the drug in patients,taking diuretic drugs.

    Effect on the ability to drive transp. cf. and fur:Care must be taken when driving vehicles or performing any work that requires special attention, especially after taking the initial dose of the drug in patients taking diuretics.
    Form release / dosage:
    Tablets of 10 mg and 20 mg.

    Packaging:
    10 tablets in a blister of aluminum foil, PVC film and polyamide.
    2, 3 or 10 blisters with instructions for use in a cardboard bundle.

    Storage conditions:
    List B.
    Store in a dry 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 expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-009022/10
    Date of registration:31.08.2010
    The owner of the registration certificate:Ranbaxy Laboratories LimitedRanbaxy Laboratories Limited India
    Manufacturer: & nbsp
    Representation: & nbspRABBAYS LABORATORY LIMITEDRABBAYS LABORATORY LIMITED
    Information update date: & nbsp26.10.2015
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