FOSINOPRIL PILLS 20MG

Release form

Pills

Packaging

30 pieces

Pharmacology

Pharmacodynamics
Fosinopril is a prodrug, the chemical structure is an ester. In the body, as a result of the hydrolysis of fosinopril, an active compound is formed by the action of enzymes - fosinoprilat. The fosinopril molecule contains a phosphine group that binds to the active sites of the ACE molecule. prevents the conversion of the decapeptide angiotensin I into the octapeptide angiotensin ||, which has a pronounced vasoconstrictor activity. As a result of a decrease in the level of angiotensin II and the suppression of vasopressor activity, the secretion of aldosterone decreases. The latter effect can lead to a slight increase in the content of potassium ions in the serum (average of 0.1 mEq / l) with the simultaneous loss of sodium ions and fluids 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 may increase.
A decrease in 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, and reflex activity of the myocardium.After ingestion, the antihypertensive effect develops within 1 hour, reaches a maximum after 3-6 hours and lasts for 24 hours.
In some patients, a 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 mainly achieved 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 helps to increase exercise tolerance, reduce the severity of heart failure and the frequency of hospitalizations.
In patients with liver cirrhosis, fosinopril has no effect on liver and kidney function.

Pharmacokinetics
Suction. After ingestion, absorption from the gastrointestinal tract (GIT) is about 30-40%. The degree of absorption does not depend on food intake, but the rate of absorption may be slow.
Fast and almost complete hydrolysis with the formation of pharmacologically active fosinoprilat occurs in the mucosa of the small intestine and liver. One hour after ingestion, the concentration of unchanged fosinopril in serum is less than 1%. fosinoprilata - 75%, inactive fosinoprilat glucuronide - 15-20%, active metabolite 4-hydroxyphosinoprilat - about 5%.
Maximum concentration (Cmaxa) fosinoprilat in 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 cellular components of the blood.
Inference. Fozinoprilat is equally excreted by the kidneys and through the intestines. With arterial hypertension in patients with normal renal function and liver, the half-life (T1 / 2) of fosinoprilat is about 11.5 hours. In heart failure, T1 / 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 fosinoprilata is about half the body than in patients with normal renal function. At the same time, absorption, bioavailability and protein binding are not markedly changed. Reduced renal excretion is compensated by increased excretion by the liver. A moderate increase in the area under the concentration-time curve (AUC) of plasma fosinoprilat (less than twice the norm) was observed in patients with various degrees of renal failure, including end-stage renal failure (creatinine clearance less than 10 ml / min / 1.73 m2).
The clearance of fosinoprilat during hemodialysis and peritoneal dialysis is on average 2% and 7%, respectively (relative to the values ​​of urea clearance).
In patients with impaired liver function (with alcoholic or biliary cirrhosis), there is no significant change in the degree of hydrolysis of fosinopril, however, a decrease in the rate of progress of this biochemical reaction is possible.
The total clearance of fosinoprilat from the body of these patients is about half that of patients with normal liver function.
In men aged 65 to 74 years with clinically normal renal and liver function, there are no noticeable differences in the pharmacokinetic parameters of fosinoprilat compared with younger patients (20-35 years).

Indications

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

Contraindications

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

Carefully
Simultaneous use with diuretics, nitrates, vasodilators. with potassium, heparinic, potassium-sparing, diuretic, procainamide, Allopurinol; chronic heart failure (XCH) III and IV functional class according to the classification of NYNA; states thataccompanied by a decrease in circulating blood volume (BCC); ischemic heart disease (CHD); 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; aortic valve stenosis; hypertrophic obstructive cardiomyopathy: uncontrolled diabetes mellitus; hemodialysis; plasma exchange; desensitization or desensitization procedures; oppression of bone marrow hematopoiesis, old age, condition after kidney transplantation.

Pregnanacy and breastfeeding

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

Special notes

Before using the drug Fosinogril-Teva and during its administration, blood pressure should be carefully monitored, indicators of kidney function, the number of blood cells, potassium content, serum creatinine and glucose levels.
A few days before the start of therapy with Fozinoril-Teva, the previous antihypertensive treatment should be stopped.
In severe CHF III and IV functional class according to the classification of NYNA, as well as in patients from other risk groups, treatment should begin under the supervision of a physician.
Correction of water electrolyte disturbances is recommended for patients with impaired water-electrolyte balance before starting treatment with Fosinopril-Teva. Patients using insulin or hypoglycemic agents for oral administration, while taking ACE inhibitors, it is necessary to control the concentration of glucose in the blood, especially during the first month of use..
When conditions are associated with a decrease in bcc (diuretic intake, salt-free diet, vomiting, diarrhea, hemodialysis), renin-dependent hyponatremia, cerebrovascular diseases, ischemic heart disease, the risk of a sharp decrease in blood pressure increases, in renovascular hypertension, an arthropod artery, or a stenotic arteriography, an arthropod artery, or a stenotic arthropodia, an arthritis, a stenotic artery severe hypotension and acupuncture. In addition, during treatment with ACE inhibitors may increase the concentration of urea nitrogen and creatinine in the serum. These effects usually develop in patients with renal insufficiency, they are reversible and disappear after cessation of treatment.
In systemic diseases of the connective tissue (systemic lupus erythematosus, scleroderma) and therapy with immunosuppressants (including after kidney transplantation), the risk of developing neutropenia and agranulocytosis increases.
With hyperkalemia.with aortic valve stenosis, hypertrophic obstructive cardiomyopathy, III and IV CHF functional class according to the NYNA classification, with the treatment of hypoglycemic drugs in patients with diabetes increases the risk of hypoglycemia.
While taking ACE inhibitors, an increase in serum potassium is possible, in patients at risk for hyperkalemia, namely in patients with renal insufficiency, uncontrolled diabetes mellitus, who take potassium-sparing diuretics, potassium preparations or other drugs, which can lead to an increase in serum levels potassium (for example, heparin), may cause hyperkalemia.
When conducting hemodialysis using high-flow polyacrylonitrile membranes, plasmapheresis using 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 during plasma pulp, the use of an ACE inhibitor is temporarily stopped before the start of the procedure.
Angioedema of the face, extremities, lips, mucous membranes, tongue, vocal folds and / or larynx may develop with the use of ACE inhibitors, especially during the first few weeks of therapy. In rare cases, severe angioedema can occur during prolonged use of the drug.In such cases, fosinopril should be immediately discontinued and the antihypertensive drug of another pharmacological class should be used.
In patients with arterial hypertension, symptomatic arterial hypotension most often develops after the use of ACE inhibitors after intensive treatment with diuretics, a diet limiting table salt, diarrhea, vomiting, or patients on hemodialysis.
In patients with heart failure with or without concomitant renal failure, there is an increased risk of developing a sharp decrease in blood pressure on the background of hyponatremia after previous intensive diuretic therapy, as well as in elderly patients.
Temporary arterial hypotension is not a contraindication for the use of the drug after carrying out measures aimed at increasing the BCC. In order to reduce the risk of developing symptomatic arterial hypotension, patients taking diuretics are advised to stop taking them 2-3 days before the start of treatment with Fosinopril-Teva. If diuretics cannot be canceled, treatment should be started 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 start of taking 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 use of the drug Fosinopril-Teva may cause dry cough, which disappears after discontinuation of the drug. 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 stopped and the patient should be carefully monitored by medical supervision.
While taking ACE inhibitors, edema of the intestinal mucosa was rarely observed, often in the absence of nausea and vomiting, which disappeared after discontinuation of the use of ACE inhibitors. Swelling of the intestinal mucosa should be considered in the differential diagnosis of patients with complaints of abdominal pain, which developed during the treatment with ACE inhibitors.
With surgical intervention (general anesthesia) the possibility of arterial hypotension increases.
The anesthesiologist should be informed about the use of the drug Fosinopril-Teva, if the patient is planned to undergo anesthesia or surgery. Treatment with an ACE inhibitor should be discontinued one day prior to surgery.
Patients taking the drug Fosinopril-Teva, should be careful when performing physical exercises or in hot weather because of the risk of dehydration and hypotension due to a decrease in BCC.
It is not recommended to use the drug Fozinopril-Teva simultaneously with lithium preparations.If it is necessary to use such a combination, it is necessary to control the concentration of lithium in the blood plasma.
In children and adolescents under the age of 18 years (safety and efficacy have not been established).

Influence on ability to manage transport and work with equipment
Caution should be exercised during the use of the drug Fosinopril-Teva due to the possible development of adverse reactions that may adversely affect the ability to drive vehicles and perform potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Composition

1 tablet contains:
active substance: fosinopril sodium 20.0 mg;
Excipients: lactose 136.2 mg, povidone-KZO 6.0 mg, crospovidone 5.0 mg, microcrystalline cellulose 20.0 mg, sodium lauryl sulfate 8.0 mg, glyceride dibehenag 4.8 mg.

Dosage and administration

Inside A pill is swallowed without chewing, drinking a glass of water, regardless of the meal, preferably at the same time.
When you skip taking one or more doses in the next dose, 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 1 time per day. Then the dose is selected depending on the dynamics of blood pressure reduction; in the absence of the desired therapeutic effect within 3-4 weeks, the dose may be increased.Maintenance doses range from 10 mg to a maximum dose of 40 mg 1 time per day. When using ACE inhibitors in patients receiving diuretic therapy, a sharp drop in blood pressure may be noted, for the prevention of which it is recommended to stop taking diuretics 2-3 days before the expected start of therapy with fosinopril.
If it is impossible to cancel diuretics, Fosinopril-Teva should be used in an initial dose of 10 mg 1 time per day. Patients with high RAAS activity (especially patients with renovascular hypertension, impaired water-epectrolyte balance, decompensated CHF or severe arterial hypertension) are advised to begin treatment with Fosinopril-Teva under the supervision of a physician because of a sudden decrease in blood pressure.
Chronic heart failure. The recommended initial dose is 10 mg 1 time per day. Treatment should begin under the supervision of a physician. With good tolerance, the dose is increased with a weekly interval, increasing it to 40 mg 1 time per day. For the treatment of CHF, Fosinopril-Teva is usually combined with diuretics and, if necessary, cardiac glycosides.
Elderly patients
There are no differences in the efficacy and safety of drug treatment in elderly patients aged 65 and older and younger patients. However, we cannot exclude a greater susceptibility in some elderly patients to the drug, due to possible overdose events due to the delayed elimination of fosinopril,
In patients with renal impairment or the liver dose reduction of the drug Fosinopril-Teva is usually not required.

Side effects

The incidence of side effects is classified in accordance with 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 hematopoietic system and lymphatic system: infrequently - transient decrease in hemoglobin or hematocrit; rarely, eosinophilia, leukopenia, thrombocytopenia, neutropenia, lymphadenopathy; very rarely - agranulocytosis.
Metabolism: infrequently - loss of appetite, aggravation of the course 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 disturbances; rarely - impaired speech, impaired memory, confusion, disorientation.
On the part of the organ of vision: infrequent visual disturbances.
From the organ of hearing and vestibular apparatus: infrequently - tinnitus, pain in the ears, dizziness.
Since the cardiovascular system: often - tachycardia, marked reduction in blood pressure, orthostatic hypotension; infrequently - angina pectoris, myocardial infarction, palpitations, cardiac arrhythmia, arterial hypertension, increased blood pressure, peripheral edema; rarely - "tides" of blood to the skin of the face, hemorrhage, impaired peripheral circulation.
On the part of the respiratory system: often - dry cough; infrequently - shortness of breath, rhinitis, pharyngitis, tracheobronchitis; rarely - bronchospasm, pneumonia, pulmonary infiptrata.
From the digestive tract: often - nausea, vomiting, diarrhea; infrequently - constipation, dryness of the oral mucosa, flatulence; rarely - stomatitis, pancreatitis, angioedema of the tongue, dysphagia, abdominal pain; very rarely - angioedema, intestinal obstruction.
On the part of the liver and biliary tract: rarely - hepatitis; very rarely, hepatic failure.
Skin and Subcutaneous Tissues: often - skin rash, angioedema, dermatitis; infrequently - increased sweating, itching, urticaria; rarely - hemorrhages in the skin (ecchymosis).
Symptom complex was described. including fever, vasculitis, muscle or joint pain or arthritis, antinuclear antibodies, increased erythrocyte sedimentation rate, eosinophilia and leukocytosis, rash, photosensitivity and other skin manifestations.
From the musculoskeletal system: infrequently - myalgia; rarely arthralgia, arthritis.
From the urinary system: infrequently - proteinuria, the development or aggravation of the symptoms of chronic renal failure, disorders of the prostate gland; rarely, acute interstitial nephritis; very rarely, acute renal failure.
From the reproductive system: infrequently - impotence, decreased libido.
Other: often - general weakness, pain of unspecified localization; infrequently - fever, sudden death, weight gain; rarely, muscle weakness.
From the laboratory indicators: often - increased activity of liver transaminases, lactate dehydrogenase and alkaline phosphatase, hyperbilirubinemia; infrequently - hypercreatininemia, increased concentration of urea, hyperkalemia; rarely - hyponatremia, a slight increase in hemoglobin, Fosinopril may underestimate the results of serum Digoxin concentrations.

Drug interaction

Diuretics, ethanol, Nitroglycerin, other nitrates and vasodilators enhance the antihypertensive effect of the drug fosinopril.

With simultaneous use of fosinopril with potassium preparations, Heparin, potassium-sparing diuretics (including amiloride, spironolactone, triamterene), with potassium supplements, the risk of hyperkalemia increases, especially in patients with heart failure and diabetes.

The simultaneous use of antacids (including aluminum hydroxide, Magnesium hydroxide, simethicone) can reduce the absorption of an ACE inhibitor.

When using ACE inhibitors of the enzyme with lithium preparations, a reversible increase in the concentration of lithium in the blood plasma and, accordingly, an increase in the risk of its toxic action is possible.

NSAIDs reduce the antihypertensive effect of ACE inhibitors, while providing a synergistic effect on the increase in potassium in the blood plasma, and can also cause kidney dysfunction.

The simultaneous use of ACE inhibitors and drugs that reduce the concentration of glucose in the blood (insulin, hypoglycemic agents for oral administration) can cause a further decrease in the concentration of glucose in the blood and the risk of hypoglycemia, especially in the first weeks of treatment, and in patients with renal insufficiency.

The simultaneous use of some tricyclic antidepressants, antipsychotics, anesthetics (including opioid analgesics and drugs for general anesthesia) with ACE inhibitors can lead to a further decrease in blood pressure and the development of orthostatic hypotension,

Sympathomimetics reduce the antihypertensive effect of ACE inhibitors. With simultaneous use with immunosuppressants, cytostatics: glucocorticosteroids for systemic use, procainamide and allopurinol, there is a risk of leukopenia.

Fosinopril may underestimate the results of serum digoxin concentration.

Symptoms: pronounced decrease in blood pressure, shock, stupor, bradycardia, impaired water and electrolyte balance, renal failure, temporary hyperventilation of the lungs, tachycardia, feeling of palpitations, dizziness, anxiety and cough.

Treatment: The patient should be placed in an intensive care unit, with careful control of serum electrolytes and creatinine. To reduce the absorption of the drug is necessary gastric lavage, the appointment of adsorbents and sodium sulfate within 30 minutes after taking fosinopril.In the case of a pronounced decrease in blood pressure, put the patient with raised legs on the bed and make a quick intravenous (IV) injection of 0.9% sodium chloride solution, IV injection of catecholamines. With severe bradycardia - the introduction of atropine sulfate, in some cases, you may need to use an artificial pacemaker. Fozinoprilat is not displayed during dialysis.

Store at a temperature not higher than 25 ° С, protected from the light of the place.