Fosinopril 10mg tabs 30 pcs Izvarino Pharma

Description

Composition
Active substance:
1 tablet contains: sodium fosinopril – 10.00 mg or 20.00 mg.
Excipients:
Glyceryl distearate; colloidal silicon dioxide; sodium carboxymethyl starch; sodium fumarate; trehalose dihydrate; microcrystalline cellulose.
Description:
10 mg Tablets: Tablets round, biconvex shape, a white or nearly white color, with the notch on one side.
20 mg Tablets: Tablets round, biconvex shape, a white or nearly white color, with the mark on one side and in the form of embossed symbol «f» on the other side.
Product form:
Tablets 10 mg, 20 mg. At 10 or 15 tablets in blisters of PVC film and aluminum foil printed patent.
1, 2, 3, 5, 6 or 9 contour cell packs of 10 tablets, or 2, 4 or 6 contour cell packs of 15 tablets together with instructions for use placed in a pile of cardboard.
Contraindications
Hypersensitivity to fosinopril and other ingredients; angioedema history (including on the background of other ACE inhibitors); pregnancy; lactation (breast feeding); age 18 years (effectiveness and safety have been established); hereditary / idiopathic angioedema; simultaneous application of aliskiren and aliskirensoderzhaschimi drugs in patients with diabetes and / or moderate to severe renal impairment (GFR of less than 60 ml / min / 1.73 m2) (see. the sections “Interaction with the other medicaments,” and “special instructions” ).
Carefully.
Applied with renal failure; hyponatremia (risk of dehydration, hypotension, chronic renal failure); bilateral renal artery stenosis or stenosis of the artery to a solitary kidney; aortic stenosis; mitral stenosis; hypertrophic obstructive cardiomyopathy; condition after kidney transplantation; during desensitization; systemic connective tissue diseases (including systemic lupus erythematosus, scleroderma), due to increased risk of neutropenia and agranulocytosis; hemodialysis; cerebrovascular diseases (including cerebrovascular insufficiency); coronary heart disease; chronic heart failure III-IV NYHA functional class classification; diabetes; suppression of bone marrow hematopoiesis; hyperkalemia; in elderly patients; gout, against a diet with restriction of salt; under conditions involving reduction bcc (including diarrhea, vomiting, diuretics previous treatment); Use in patients blacks (see. section “Special Instructions”).
Dosage
10 mg
Indications
Hypertension – in monotherapy or in combination with other antihypertensive drugs (in particular with thiazide diuretics).
Chronic heart failure – as part of combination therapy.
Interaction with other drugs
The simultaneous use of antacids (including aluminum hydroxide, magnesium hydroxide, simethicone), may reduce the absorption of fosinopril (fosinopril and these drugs should be taken at intervals of not less than 2 hours).
Patients receiving fosinopril concurrently with lithium salts, lithium may increase the plasma concentrations and the risk of lithium toxicity (simultaneous use with caution).
When assigning fosinopril should be noted that indomethacin and other non-steroidal anti-inflammatory drugs (including aspirin (more than 3 g / day)) can reduce the antihypertensive effect of ACE inhibitors, particularly in patients with low-renin hypertension.
When the joint application of fosinopril with diuretics or in combination with a strict diet, limiting salt intake, dialysis or may develop severe arterial hypotension, particularly in the first hour after taking the initial dose of fosinopril.
When the joint application of fosinopril with potassium preparations, potassium-sparing diuretics (including with amiloride, spironolactone, eplerenone (a derivative of spironolactone), triamterene), with food supplements containing potassium, increases the risk of hyperkalemia. In patients with heart failure, diabetes, simultaneously receiving potassium-sparing diuretics, potassium, kalisodergaszczye edible salt substitutes or other means for causing hyperkalemia (e.g., heparin), ACE inhibitors increase the risk of increasing the content of potassium in serum.
Fosinopril enhances hypoglycemic effect sulfonylureas, insulin.
While the use of allopurinol, cytostatic agents, immunosuppressants, procainamide there is a risk of leucopenia.
Estrogens weaken the antihypertensive effect of fosinopril because of its ability to hold up liquid.
Antihypertensive drugs, opioid analgesics, drugs for general anesthesia increase the antihypertensive effect of fosinopril.
Bioavailability fosinopril while the use of chlorthalidone, nifedipine, propranolol, hydrochlorothiazide, cimetidine, metoclopramide, propantheline bromide, digoxin, aspirin as antiplatelet agents and warfarin does not change.
The literature reported that patients diagnosed with atherosclerotic disease, heart failure or diabetes with end-organ damage, dual blockade of the RAAS using angiotensin II receptor antagonists (ARA II), ACE or aliskiren inhibitors (direct renin inhibitor) is associated with an increased frequency occurrence of hypotension, syncope, hyperkalemia, and renal dysfunction (including acute renal failure) as compared with the use of one drug affecting on the RAAS. Dual blockade (e.g., appointment with an ACE inhibitor aliskiren or ARA II) should be conducted only in certain specific cases, regular monitoring of renal function.
Overdose
Symptoms: marked reduction of blood pressure, bradycardia, shock, disorders of water and electrolyte balance, acute renal failure, stupor.
Treatment: the drug should be stopped, shown gastric lavage, adsorbents (e.g., activated carbon), vasopressor agents, infusion of 0.9% sodium chloride solution and more symptomatic and supportive treatment. The use of hemodialysis ineffective.
pharmachologic effect
Pharmacological group:
Angiotensin converting enzyme (ACE).
Pharmacodynamics:
ACE inhibitor. Fosinopril – ester from which the body by hydrolysis by the enzymes formed fozinoprilat active compound.
Fosinopril, through specific binding of the phosphate groups with ACE prevents the conversion of angiotensin I to the vasoconstrictor compound angiotensin II, resulting vasopressor activity and reduced aldosterone secretion. The latter effect can lead to a slight increase in the content of potassium ions in serum (mean 0.1 mEq / L) with a simultaneous loss of body fluids and sodium ions.
Fosinopril inhibits metabolic degradation of bradykinin, which has powerful vasopressor action, due to this antihypertensive effect of the drug can be enhanced.
Lowering blood pressure (BP) is not accompanied by changes in the circulating blood volume (CBV), cerebral and renal blood flow, blood supply to the internal organs, skeletal muscle, skin and reflex activity of the myocardium. After oral antihypertensive effect develops over 1 hour, reaching a maximum after 3-6 hours and lasts 24 hours.
In heart failure, fosinopril positive effects are achieved mainly by suppressing the renin-angiotensin-aldosterone (RAAS) system. ACE suppression leads to a reduction in both preload and afterload on the myocardium.
The drug enhances exercise tolerance, reducing the severity of heart failure.
Pharmacokinetics:
Suction.
After oral absorption from the gastrointestinal tract (GIT) is about 30-40%. The degree of absorption depends not mealtime, but the rate of absorption may be delayed. The maximum concentration (Cmax) in plasma fozinoprilata achieved after 3 hours and is independent of the dose.
Distribution.
Binding to plasma proteins is greater than 95%. Fozinoprilat has a relatively small volume of distribution (Vd) and is connected to a small extent with the cellular components of blood.
Metabolism.
Hydrolysis of fosinopril by the enzymes to form fozinoprilata occurs mainly in the liver and gastrointestinal mucosa.
Withdrawal.
Fosinopril excreted equally through the liver and kidneys. When hypertension patients with normal renal function and liver half-life (T1 / 2) fozinoprilata is about 11.5 hours. In heart failure, T1 / 2 is 14 hours.
Pharmacokinetics in special clinical situations.
Patients with impaired renal function (glomerular filtration rate (GFR) of less than 80 ml / min / 1.73 m2) fozinoprilata total clearance from the body is approximately twice lower than in patients with normal renal function. At the same time, absorption, bioavailability and protein binding is not appreciably changed. Reduced renal excretion is compensated by an increased excretion by the liver. A moderate increase in the area under the curve “concentration-time» (AUC) in the blood plasma (less than half compared with the norm) was observed in patients with renal insufficiency varying severity, including kidney failure in the terminal stage (GFR of less than 10 ml / min / 1 , 73 m2). Fozinoprilata Clearance in hemodialysis and peritoneal dialysis averages 2% and 7% (with respect to the values ​​of the urea clearance), respectively. Patients with impaired liver function (in alcoholic or biliary cirrhosis) may decrease the rate of hydrolysis of fosinopril without significant changes in its extent. Total clearance from the body fozinoprilata such patients is approximately twice lower than in patients with normal liver function.
Pregnancy and breast-feeding
Fosinopril is contraindicated in pregnancy. Of newborns whose mothers took ACE inhibitors during pregnancy, it is recommended to carry out careful monitoring for early detection of arterial hypotension, oliguria and hyperkalemia.
Use of the drug in the II and III trimester of pregnancy causes damage or death of the developing fetus. Fozinoprilat which crosses the placenta is removed from neonatal circulation by peritoneal dialysis with some clinical benefit and, theoretically, can be removed by exchange transfusion.
If during treatment with ACE inhibitors established pregnancy, treatment must be stopped immediately and, if necessary, alternative therapy should be instituted, which has an established safety profile of use during pregnancy. Patients undergoing therapy of ACE inhibitors and planning pregnancy should also be assigned to an alternative therapy.
Since fozinoprilat excreted in breast milk and breastfeeding should be discontinued if necessary applying Fosinopril during lactation.
Conditions of supply of pharmacies
On prescription.
side effects
To evaluate the incidence of adverse events using the following classification of the World Health Organization:
Very common (> 1/10)
Often (> 1/100 and 1/1000 and 1/10 000 and 1/10 000)
Frequency unknown (can not be calculated on the basis of the available data).
Cardio-vascular system:
often – tachycardia, marked reduction in blood pressure, orthostatic collapse;
rarely – angina, myocardial infarction, palpitations, cardiac arrest, arrhythmia, cardiac conduction disturbances, increased blood pressure, shock, sudden death;
rare – “tides” of blood to the skin, bleeding, peripheral vascular disease.
From the urinary system:
rarely – renal failure, proteinuria;
seldom – a pathology of the prostate (hyperplasia, BPH), polyuria, oliguria;
very rarely – acute renal failure.
On the part of genitals and mammary gland:
rarely – sexual dysfunction.
On the part of the central and peripheral nervous system:
often – dizziness, headache;
seldom – cerebral infarction, paraesthesia, somnolence, stroke, syncope, transient ischemic attack, tremor, insomnia, depression, confusion;
rarely – impaired memory, dysphasia, impaired orientation, alarm.
From the senses:
infrequently – hearing and visual impairment, tinnitus, ear pain, taste disturbance.
From the digestive system:
often – nausea, vomiting, diarrhea;
rarely – constipation, dry mouth, flatulence;
rarely – defeat the oral mucosa, pancreatitis, glossitis, bloating, dysphagia, hepatitis, cholestatic jaundice, abdominal pain, anorexia;
very rarely – angioneurotic edema of the intestine, (partial), intestinal obstruction, liver failure.
The respiratory system:
often – cough;
rarely – dyspnea, rhinitis, sinusitis, tracheobronchitis;
rarely – bronchospasm, epistaxis, laryngitis / hoarseness, pneumonia, pulmonary infiltrates.
From the side of hematopoiesis:
infrequently – a temporary reduction in hemoglobin concentration, hematocrit reduction;
rarely – anemia, eosinophilia, leukopenia, lymphadenitis, neutropenia, thrombocytopenia;
very rarely – agranulocytosis.
On the part of the musculoskeletal system:
rarely – myalgia;
rarely – arthritis.
From a metabolism:
infrequently – decreased appetite, exacerbation of gout, hyperkalemia;
Allergic reactions:
often – skin rash, angioedema, dermatitis;
seldom – rash, pruritus, urticaria;
rarely – ecchymosis.
General disorders and the site of injection:
often – chest pain (non-cardiac), weakness;
rarely – fever, peripheral edema;
rarely – weakness in one limb, viral infections.
From the laboratory parameters:
often – increasing the activity of alkaline phosphatase, hyperbilirubinemia, increased lactate dehydrogenase activity, increased activity of “liver” transaminases;
infrequently – body weight increase, increase of urea concentration in the blood, hypercreatininemia, hyperkalemia;
rarely – hyponatremia.
Effect on the fetus: fetal developmental disorder of the kidneys, lowering blood pressure of the fetus and newborn renal dysfunction, hyperkalemia, hypoplasia of the skull bones, oligohydramnios, limb contractures, pulmonary hypoplasia.
Reported symptom of various manifested alone or in combination of the following symptoms: fever, myalgia, arthralgia / arthritis, increased titer of antinuclear antibodies, increased erythrocyte sedimentation rate, leukocytosis and eosinophilia, skin rash, photosensitivity or other dermatologic reactions.
With simultaneous use of ACE inhibitors, including fosinopril, patients receiving the drug gold (sodium aurothiomalate) / w is described symptom, including facial flushing, nausea, vomiting and reduced blood pressure.
special instructions
Before treatment requires an analysis of earlier antihypertensive therapy, a degree of increase in blood pressure, limit salt diet and / or liquid, and other clinical circumstances.
If possible, stop the wire before antihypertensive treatment a few days before the start of treatment fosinopril.
To reduce the likelihood of hypotension diuretic should be discontinued for 2-3 days prior to initiation of treatment fosinopril. Before and during the treatment is necessary to control blood pressure, renal function, the content of potassium ions, creatinine, urea, electrolytes and Activity “liver” enzymes in the blood.
It reported on the development of angioedema in patients while taking fosinopril. Edema tongue, pharynx or larynx may develop airway obstruction which can be fatal. In the case of such reactions patients should terminate reception and acceptance of drug therapy emergency measures, including subcutaneous administration of epinephrine solution (epinephrine) (1: 1000).
While receiving ACE inhibitors rarely observed swelling of the intestinal mucosa. In such cases, patients complained of abdominal pain (with nausea and vomiting could be), in some cases, swelling of the intestinal mucosa arose without facial edema, C1-esterase levels were normal. Symptoms disappeared after discontinuation of ACE inhibitors. Intestinal bowel edema should be considered in the differential diagnosis in patients with complaints of abdominal pain during treatment with ACE inhibitors.
The therapy of ACE inhibitors of anaphylactic reactions may develop during hemodialysis through highly permeable membrane, as well as during low-density lipoprotein apheresis adsorption on dextran sulfate. In such cases, you should consider using another type of dialysis membrane or other medication.
Possible development of agranulocytosis and bone marrow suppression during treatment with ACE inhibitors. These cases are more common in patients with impaired renal function, especially in the presence of systemic diseases of connective tissue (systemic lupus erythematosus or scleroderma). Before therapy of ACE inhibitors and in the treatment process is carried out determination of the total number of leukocytes and leukocyte formula (1 once a month during the first 3-6 months of treatment and in the first year of the drug in patients with an increased risk of neutropenia).
In patients with uncomplicated hypertension may develop hypotension in connection with the use of the drug Fosinopril.
Symptomatic hypotension when used ACE inhibitors most often develops in patients after intensive treatment with diuretics, diet restriction salt or during kidney dialysis. Temporary hypotension is not a contraindication for the use of the drug after the measures the body’s hydration.
Patients with chronic heart failure treatment with ACE inhibitors may cause excess antihypertensive effect, which can lead to oliguria or azotemia fatal. Therefore, in the treatment of chronic heart failure, fosinopril should monitor their patients closely, especially during the first 2 weeks of treatment, as well as any increase in the dose of fosinopril or diuretic.
May need to reduce the dose of diuretics in patients with hyponatremia and patients previously heavily treated with diuretics. Transient hypotension is not a contraindication for further use Fosinopril formulation. Some decrease in systemic blood pressure is a common and desired effect at the start of the drug in heart failure. The degree of this reduction is maximal in the early stages of treatment and stabilized within 1-2 weeks of starting treatment. АД обычно возвращается к значениям периода до начала лечения без снижения терапевтической эффективности.
При появлении заметной желтушности и выраженном повышении активности ферментов печени лечение Фозиноприлом следует прекратить и назначить соответствующие лечение.
У пациентов с артериальной гипертензией с двусторонним стенозом почечных артерий или стенозом артерии единственной почки, а также при одновременном применении диуретиков без признаков заболевания почечных сосудов во время лечения ингибиторами АПФ может повышаться концентрация азота мочевины крови и креатинина сыворотки крови. Эти эффекты обычно обратимы и проходят после прекращения лечения. Может потребоваться снижение дозы диуретика и/или Фозиноприла.
У пациентов с тяжелой хронической сердечной недостаточностью, с измененной активностью РААС лечение ингибиторами АПФ может привести к олигурии, прогрессирующей азотемии, в редких случаях к острой почечной недостаточности и возможному летальному исходу.
Как и другие препараты группы ингибиторов АПФ, Фозиноприл следует с осторожностью применять у пациентов с митральным и аортальным стенозом, а также при гипертрофической обструктивной кардиомиопатии.
Ингибиторы АПФ могут усиливать антигипертензивное действие средств, применяющихся для проведения общей анестезии. Перед хирургическим вмешательством (включая стоматологию) необходимо предупредить врача о применении ингибиторов АПФ. Следует соблюдать осторожность при выполнении физических упражнений или при жаркой погоде из-за риска дегидратации и артериальной гипотензии вследствие уменьшения ОЦК.
На основании эпидемиологических исследований предполагается, что одновременный прием ингибиторов АПФ и инсулина, а также гипогликемических лекарственных препаратов для приема внутрь может приводить к развитию гипогликемии. Наибольший риск развития наблюдается в течение первых недель комбинированной терапии, а также у пациентов с нарушением функции почек. У пациентов с сахарным диабетом требуется тщательный контроль концентрации глюкозы в крови, особенно во время первого месяца терапии ингибитором АПФ.
Существует доказательство того, что одновременное применение ингибиторов АПФ, АРА II или алискирена увеличивает риск артериальной гипотензии, гиперкалиемии и снижает функцию почек (в т.ч. вызывая острую почечную недостаточность). В связи с этим двойная блокада РААС одновременным применением ингибиторов АПФ, АРА II или алискирена не рекомендуется. Если терапия с применением двойной блокады РААС считается необходимой, лечение должно происходить под наблюдением специалиста с регулярным мониторингом функции почек, содержания электролитов и АД. Применение ингибиторов АПФ и АРАII у пациентов с диабетической нефропатией не рекомендовано.
Фозиноприл (как и другие ингибиторы АПФ), оказывает менее выраженное антигипертензивное действие у пациентов негроидной расы по сравнению с представителями других рас.
Влияние на способность к управлению автотранспортными средствами и механизмами.
Необходимо соблюдать осторожность при управлении транспортными средствами или выполнении другой работы, требующей повышенного внимания, т.к. возможно развитие головокружения, особенно после приема начальной дозы ингибитора АПФ у пациентов, принимающих диуретики.
Storage conditions
In the dark place at a temperature not higher than 25 ° C.
Keep out of the reach of children.
Dosing and Administration
Inside. Дозировка препарата должна подбираться индивидуально.
Arterial hypertension.
Рекомендуемая начальная доза препарата Фозиноприл составляет 10 мг один раз в сутки. Дозу необходимо подбирать в зависимости от динамики снижения АД. Обычная доза составляет от 10 мг до 40 мг один раз в сутки. При отсутствии достаточного антигипертензивного эффекта возможно дополнительное назначение диуретиков.
Если лечение препаратом Фозиноприл начинают на фоне проводимой терапии диуретиком, то его начальная доза должна составлять не более 10 мг при тщательном врачебном контроле состояния пациента.
Хроническая сердечная недостаточность.
Рекомендованная начальная доза составляет 5 мг (1/2 таблетки по 10 мг) 1 или 2 раза в сутки. В зависимости от терапевтической эффективности дозу можно повышать с недельным интервалом вплоть до максимальной дозы – 40 мг 1 раз в сутки.
Артериальная гипертензия и сердечная недостаточность при нарушенной функции почек или печени.
Поскольку выведение препарата из организма происходит двумя путями, снижения доз пациентам с нарушенной функцией почек или печени обычно не требуется.
Elderly patients.
Различий в эффективности и безопасности лечения препаратом пациентов в возрасте 65 лет и старше и молодых пациентов не наблюдается. Однако нельзя исключить большую восприимчивость у некоторых пациентов пожилого возраста к препарату, в связи с возможными явлениями передозировки.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist