Pharmacological properties of the drug Fozinopril
ACE inhibitor. Reduces the formation of angiotensin II from angiotensin I, which leads to a decrease in peripheral vascular resistance and systemic blood pressure. Suppresses the synthesis of aldosterone in the adrenal glands. The onset of therapeutic action is observed 1 hour after oral administration, the maximum reduction in blood pressure is achieved within 3–6 hours. The hypotensive effect persists for 24 hours, however, it may take 2–3 weeks to achieve a stable hypotensive effect in some patients. During long-term treatment, the effect persists. After oral administration, about 36% of fosinopril is absorbed in the digestive tract; the degree of absorption does not depend on food intake. Hydrolysis of fosinopril with the formation of pharmacologically active fosinoprilat occurs in the mucous membrane of the digestive tract and partially in the liver. The maximum concentration of fosinoprilat in blood plasma is achieved after 3 hours. Plasma protein binding is 95%. Does not penetrate the BBB. Fosinoprilat is excreted unchanged in urine and bile. The half-life is 11.5 hours. In patients with renal failure, there is no noticeable change in the pharmacokinetics of fosinopril due to a compensatory increase in its excretion by the liver. In patients with impaired liver function, a slight decrease in the hydrolysis of fosinopril is possible. There is evidence of a compensatory increase in the excretion of fosinopril by the kidneys with a simultaneous decrease in the hepatic clearance of fosinopril in this category of patients.
Fosinopril
Fosinopril tablet 20 mg x30 ATX code: C09AA09 (Fosinopril) Active substance: fosinopril (fosinopril) Rec.INN registered by WHO
Dosage form
Fosinopril
Tab. 20 mg: 7, 10, 14, 20, 21, 28, 30 or 40 pcs.reg. No.: LP-002622 dated 09/15/14 - Valid
Release form, packaging and composition of the drug Fozinopril
Tablets are white or white with a yellow tint, round, biconvex.
1 tab.
fosinopril sodium 20 mg
Excipients: lactose monohydrate - 0.3668 g, croscarmellose sodium - 0.0012 g, colloidal silicon dioxide - 0.008 g, magnesium stearate - 0.004 g.
Clinical-pharmacological group: ACE inhibitor Pharmaco-therapeutic group: ACE blocker
pharmachologic effect
ACE inhibitor. It is a prodrug from which the active metabolite fosinoprilat is formed in the body. It is believed that the mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I to angiotensin II, which is a powerful vasoconstrictor. As a result of a decrease in the concentration of angiotensin II, a secondary increase in plasma renin activity occurs due to the elimination of negative feedback during the release of renin and a direct decrease in aldosterone secretion. In addition, fosinoprilat appears to have an effect on the kinin-kallikrein system, inhibiting the breakdown of bradykinin.
Thanks to its vasodilating effect, it reduces roundabout percentage (afterload), wedge pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels, increases cardiac output and exercise tolerance.
Pharmacokinetics When taken orally, it is slowly absorbed from the gastrointestinal tract. Taking with food may reduce the rate, but not the extent, of absorption. Metabolized in the liver and in the mucous membrane of the gastrointestinal tract by hydrolysis with the formation of fosinoprilat, due to the pharmacological activity of which a hypotensive effect is realized. The binding of fosinoprilat to plasma proteins is 97-98%. T1/2 of fosinoprilat is 11.5 hours. It is excreted by the kidneys - 44-50% and through the intestines - 46-50%.
Indications of the active substances of the drug Fosinopril
Arterial hypertension (as monotherapy or as part of combination therapy).
Chronic heart failure (as part of combination therapy).
Open list of ICD-10 codes
ICD-10 code Indication
I10 Essential [primary] hypertension
Dosage regimen
Taken orally.
For arterial hypertension, the initial dose is 10 mg 1 time / day. Maintenance dose - 10-40 mg 1 time / day. In the absence of a sufficient therapeutic effect, additional use of diuretics is possible.
For chronic heart failure, the initial dose is 5 mg 1-2 times a day. Depending on the therapeutic effectiveness, the dose can be increased at weekly intervals up to a maximum daily dose of 40 mg 1 time / day.
Side effect
From the cardiovascular system: marked decrease in blood pressure, orthostatic hypotension, tachycardia, palpitations, arrhythmias, angina pectoris, myocardial infarction, chest pain, flushes of blood to the skin of the face, cardiac arrest, fainting.
From the digestive system: nausea, vomiting, constipation, intestinal obstruction, pancreatitis, hepatitis, stomatitis, glossitis, dyspepsia, abdominal pain, anorexia, intestinal edema, cholestatic jaundice, dysphagia, flatulence, loss of appetite, changes in body weight, dry mucous membranes membranes of the oral cavity, increased activity of liver transaminases, hyperbilirubinemia.
From the respiratory system: dry cough, shortness of breath, pharyngitis, laryngitis, sinusitis, pulmonary infiltrates, bronchospasm, dysphonia, shortness of breath, nosebleeds, rhinorrhea.
From the urinary system: development or worsening of symptoms of chronic renal failure, proteinuria, oliguria, hypercreatininemia, increased urea concentration.
From the nervous system: stroke, cerebral ischemia, dizziness, headache, weakness, when used in high doses - insomnia, anxiety, depression, confusion, paresthesia, drowsiness.
From the senses: hearing and vision impairment, tinnitus.
Allergic reactions: skin rash, itching, angioedema.
From the hematopoietic system: neutropenia, leukopenia, eosinophilia, lymphadenitis, decrease in hemoglobin and hematocrit.
From the musculoskeletal system: arthritis.
From the metabolic side: exacerbation of gout, hyperkalemia, hyponatremia, increased ESR.
Contraindications for use Pregnancy, lactation (breastfeeding), hypersensitivity to ACE inhibitors.
Use during pregnancy and breastfeeding
Use during pregnancy is contraindicated.
During treatment, women of childbearing age should use reliable contraception.
Fosinopril is excreted in breast milk. If it is necessary to use fosinopril during lactation, the issue of stopping breastfeeding should be decided.
Use in children Safety of use in children has not been established.
Use in elderly patients No special adjustment of the fosinopril dosage regimen is required in elderly patients.
special instructions
Use with caution in cases of renovascular hypertension, heart failure, hyperkalemia, a history of angioedema, hypovolemia and/or reduced plasma osmolarity of various etiologies, as well as in patients on hemodialysis.
2-3 days before starting treatment with fosinopril, it is recommended to discontinue previous diuretic therapy, with the exception of patients with malignant or difficult-to-treat hypertension. In such cases, fosinopril therapy should be started immediately, at a reduced dose, with close medical supervision and careful dose escalation.
Symptomatic hypotension with the use of ACE inhibitors most often develops in patients after intensive treatment with diuretics, a diet limiting salt intake, or during renal dialysis. Transient arterial hypotension is not a contraindication for continuing treatment after measures to restore blood volume.
In patients with chronic heart failure, treatment with ACE inhibitors may cause excessive antihypertensive effects, which can lead to oliguria or azotemia, which can be fatal. Therefore, when treating patients with chronic heart failure with fosinopril, careful clinical monitoring is necessary, especially during the first 2 weeks of treatment, as well as with any increase in the dose of fosinopril or diuretic.
ACE inhibitors rarely cause swelling of the intestinal mucosa. In this case, patients experience abdominal pain (sometimes without nausea and vomiting), facial swelling may also be absent, and the level of C1-esterases is normal. After stopping taking ACE inhibitors, symptoms disappear. Swelling of the intestinal mucosa should be taken into account in the differential diagnosis of patients with abdominal pain while taking ACE inhibitors.
During treatment with ACE inhibitors during hemodialysis using highly permeable membranes, as well as during LDL apheresis with adsorption on dextran sulfate, anaphylactic reactions may develop. In these cases, the use of a different type of dialysis membrane or other antihypertensive therapy should be considered.
It is possible to develop agranulocytosis and suppression of bone marrow function during treatment with ACE inhibitors. These cases occur more often in patients with impaired renal function, especially in the presence of systemic connective tissue diseases (systemic lupus erythematosus or scleroderma). Before starting therapy with ACE inhibitors and during treatment, the total number of leukocytes and the leukocyte formula are determined (once a month in the first 3-6 months of treatment and in the first year of treatment in patients with an increased risk of neutropenia).
If noticeable jaundice and a marked increase in liver enzyme activity occur, fosinopril treatment should be discontinued and appropriate treatment should be prescribed.
In case of arterial hypertension in patients with bilateral renal artery stenosis or stenosis of the artery of a single kidney, as well as with the simultaneous use of diuretics without signs of renal impairment during treatment with ACE inhibitors, the concentration of blood urea nitrogen and serum creatinine may increase. These effects are usually reversible and disappear after treatment is stopped. A dose reduction of diuretic and/or fosinopril may be required.
In patients with severe chronic heart failure with altered RAAS activity, treatment with ACE inhibitors can lead to oliguria, progressive azotemia and, in rare cases, acute renal failure and possible death.
During fosinopril therapy, the patient should be careful when performing physical exercise or in hot weather due to the risk of dehydration and hypotension due to a decrease in blood volume.
No special adjustment of the fosinopril dosage regimen is required in elderly patients. Safety of use in children has not been established.
Before and during treatment with the drug, it is necessary to monitor blood pressure, kidney function, potassium levels, hemoglobin levels, creatinine, urea, electrolyte concentrations and the activity of liver transaminases in the blood.
Impact on the ability to drive vehicles and operate machinery
Caution is required when driving vehicles or performing other work that requires increased attention, because Dizziness may occur, especially after the initial dose of fosinopril.
Drug interactions
When used simultaneously with antacids, the absorption of fosinopril may be increased.
When used simultaneously with antihypertensive drugs, the antihypertensive effect may be enhanced.
When used simultaneously with diuretics, severe arterial hypotension may develop.
When used simultaneously with potassium-sparing diuretics and potassium preparations, it is possible to increase the concentration of potassium in the blood plasma.
When used simultaneously with lithium carbonate, it is possible to increase the concentration of lithium in the blood plasma and increase the risk of developing intoxication.
When used simultaneously with drugs used in anesthesia and analgesics, the antihypertensive effect may be enhanced.
When used simultaneously with acenocoumarol, a case of bleeding has been described.
When used simultaneously with indomethacin and other NSAIDs (acetylsalicylic acid), the effectiveness of ACE inhibitors may decrease.
Side effects of the drug Fozinopril
from the digestive system: rarely - nausea, vomiting, dyspepsia, increased activity of liver transaminases; cases of pancreatitis and hepatitis have been described; from the respiratory system: cough, rarely - pharyngitis, laryngitis, sinusitis, bronchospasm; from the cardiovascular system: palpitations, chest pain, rarely - orthostatic hypotension, collapse, hot flashes, arrhythmia; allergic and immunological reactions - skin rash, itching, photosensitivity, angioedema, myalgia, arthralgia; from the urinary system - proteinuria, oliguria, disorders of excretory function, accompanied by an increase in the concentration of creatinine and urea in the blood plasma; other reactions - dizziness, fatigue, impaired taste and other types of sensitivity.
Fosinopril tablet 10 mg x30
Fosinopril tablet 10 mg x30 ATX code: C09AA09 (Fosinopril) Active substance: fosinopril (fosinopril) Rec.INN registered by WHO
Dosage form
Fosinopril
Tab. 10 mg: 7, 10, 14, 20, 21, 28, 30 or 40 pcs.reg. No.: LP-002622 dated 09/15/14 - Valid
Release form, packaging and composition of the drug Fozinopril
Tablets are white or white with a yellow tint, round, biconvex.
1 tab.
fosinopril sodium 10 mg
Excipients: lactose monohydrate - 0.1834 g, croscarmellose sodium - 0.0006 g, colloidal silicon dioxide - 0.004 g, magnesium stearate - 0.002 g.
Clinical-pharmacological group: ACE inhibitor Pharmaco-therapeutic group: ACE blocker
pharmachologic effect
ACE inhibitor. It is a prodrug from which the active metabolite fosinoprilat is formed in the body. It is believed that the mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I to angiotensin II, which is a powerful vasoconstrictor. As a result of a decrease in the concentration of angiotensin II, a secondary increase in plasma renin activity occurs due to the elimination of negative feedback during the release of renin and a direct decrease in aldosterone secretion. In addition, fosinoprilat appears to have an effect on the kinin-kallikrein system, inhibiting the breakdown of bradykinin.
Thanks to its vasodilating effect, it reduces roundabout percentage (afterload), wedge pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels, increases cardiac output and exercise tolerance.
Pharmacokinetics When taken orally, it is slowly absorbed from the gastrointestinal tract. Taking with food may reduce the rate, but not the extent, of absorption. Metabolized in the liver and in the mucous membrane of the gastrointestinal tract by hydrolysis with the formation of fosinoprilat, due to the pharmacological activity of which a hypotensive effect is realized. The binding of fosinoprilat to plasma proteins is 97-98%. T1/2 of fosinoprilat is 11.5 hours. It is excreted by the kidneys - 44-50% and through the intestines - 46-50%.
Indications of the active substances of the drug Fosinopril
Arterial hypertension (as monotherapy or as part of combination therapy).
Chronic heart failure (as part of combination therapy).
Open list of ICD-10 codes
ICD-10 code Indication
I10 Essential [primary] hypertension
Dosage regimen The method of administration and dosage regimen of a particular drug depend on its release form and other factors. The optimal dosage regimen is determined by the doctor. The compliance of the dosage form of a particular drug with the indications for use and dosage regimen should be strictly observed.
Taken orally.
For arterial hypertension, the initial dose is 10 mg 1 time / day. Maintenance dose - 10-40 mg 1 time / day. In the absence of a sufficient therapeutic effect, additional use of diuretics is possible.
For chronic heart failure, the initial dose is 5 mg 1-2 times a day. Depending on the therapeutic effectiveness, the dose can be increased at weekly intervals up to a maximum daily dose of 40 mg 1 time / day.
Side effect
From the cardiovascular system: marked decrease in blood pressure, orthostatic hypotension, tachycardia, palpitations, arrhythmias, angina pectoris, myocardial infarction, chest pain, flushes of blood to the skin of the face, cardiac arrest, fainting.
From the digestive system: nausea, vomiting, constipation, intestinal obstruction, pancreatitis, hepatitis, stomatitis, glossitis, dyspepsia, abdominal pain, anorexia, intestinal edema, cholestatic jaundice, dysphagia, flatulence, loss of appetite, changes in body weight, dry mucous membranes membranes of the oral cavity, increased activity of liver transaminases, hyperbilirubinemia.
From the respiratory system: dry cough, shortness of breath, pharyngitis, laryngitis, sinusitis, pulmonary infiltrates, bronchospasm, dysphonia, shortness of breath, nosebleeds, rhinorrhea.
From the urinary system: development or worsening of symptoms of chronic renal failure, proteinuria, oliguria, hypercreatininemia, increased urea concentration.
From the nervous system: stroke, cerebral ischemia, dizziness, headache, weakness, when used in high doses - insomnia, anxiety, depression, confusion, paresthesia, drowsiness.
From the senses: hearing and vision impairment, tinnitus.
Allergic reactions: skin rash, itching, angioedema.
From the hematopoietic system: neutropenia, leukopenia, eosinophilia, lymphadenitis, decrease in hemoglobin and hematocrit.
From the musculoskeletal system: arthritis.
From the metabolic side: exacerbation of gout, hyperkalemia, hyponatremia, increased ESR.
Contraindications for use Pregnancy, lactation (breastfeeding), hypersensitivity to ACE inhibitors.
Use during pregnancy and breastfeeding
Use during pregnancy is contraindicated.
During treatment, women of childbearing age should use reliable contraception.
Fosinopril is excreted in breast milk. If it is necessary to use fosinopril during lactation, the issue of stopping breastfeeding should be decided.
Use in children Safety of use in children has not been established.
Use in elderly patients No special adjustment of the fosinopril dosage regimen is required in elderly patients.
special instructions
Use with caution in cases of renovascular hypertension, heart failure, hyperkalemia, a history of angioedema, hypovolemia and/or reduced plasma osmolarity of various etiologies, as well as in patients on hemodialysis.
2-3 days before starting treatment with fosinopril, it is recommended to discontinue previous diuretic therapy, with the exception of patients with malignant or difficult-to-treat hypertension. In such cases, fosinopril therapy should be started immediately, at a reduced dose, with close medical supervision and careful dose escalation.
Symptomatic hypotension with the use of ACE inhibitors most often develops in patients after intensive treatment with diuretics, a diet limiting salt intake, or during renal dialysis. Transient arterial hypotension is not a contraindication for continuing treatment after measures to restore blood volume.
In patients with chronic heart failure, treatment with ACE inhibitors may cause excessive antihypertensive effects, which can lead to oliguria or azotemia, which can be fatal. Therefore, when treating patients with chronic heart failure with fosinopril, careful clinical monitoring is necessary, especially during the first 2 weeks of treatment, as well as with any increase in the dose of fosinopril or diuretic.
ACE inhibitors rarely cause swelling of the intestinal mucosa. In this case, patients experience abdominal pain (sometimes without nausea and vomiting), facial swelling may also be absent, and the level of C1-esterases is normal. After stopping taking ACE inhibitors, symptoms disappear. Swelling of the intestinal mucosa should be taken into account in the differential diagnosis of patients with abdominal pain while taking ACE inhibitors.
During treatment with ACE inhibitors during hemodialysis using highly permeable membranes, as well as during LDL apheresis with adsorption on dextran sulfate, anaphylactic reactions may develop. In these cases, the use of a different type of dialysis membrane or other antihypertensive therapy should be considered.
It is possible to develop agranulocytosis and suppression of bone marrow function during treatment with ACE inhibitors. These cases occur more often in patients with impaired renal function, especially in the presence of systemic connective tissue diseases (systemic lupus erythematosus or scleroderma). Before starting therapy with ACE inhibitors and during treatment, the total number of leukocytes and the leukocyte formula are determined (once a month in the first 3-6 months of treatment and in the first year of treatment in patients with an increased risk of neutropenia).
If noticeable jaundice and a marked increase in liver enzyme activity occur, fosinopril treatment should be discontinued and appropriate treatment should be prescribed.
In case of arterial hypertension in patients with bilateral renal artery stenosis or stenosis of the artery of a single kidney, as well as with the simultaneous use of diuretics without signs of renal impairment during treatment with ACE inhibitors, the concentration of blood urea nitrogen and serum creatinine may increase. These effects are usually reversible and disappear after treatment is stopped. A dose reduction of diuretic and/or fosinopril may be required.
In patients with severe chronic heart failure with altered RAAS activity, treatment with ACE inhibitors can lead to oliguria, progressive azotemia and, in rare cases, acute renal failure and possible death.
During fosinopril therapy, the patient should be careful when performing physical exercise or in hot weather due to the risk of dehydration and hypotension due to a decrease in blood volume.
No special adjustment of the fosinopril dosage regimen is required in elderly patients. Safety of use in children has not been established.
Before and during treatment with the drug, it is necessary to monitor blood pressure, kidney function, potassium levels, hemoglobin levels, creatinine, urea, electrolyte concentrations and the activity of liver transaminases in the blood.
Impact on the ability to drive vehicles and operate machinery
Caution is required when driving vehicles or performing other work that requires increased attention, because Dizziness may occur, especially after the initial dose of fosinopril.
Drug interactions
When used simultaneously with antacids, the absorption of fosinopril may be increased.
When used simultaneously with antihypertensive drugs, the antihypertensive effect may be enhanced.
When used simultaneously with diuretics, severe arterial hypotension may develop.
When used simultaneously with potassium-sparing diuretics and potassium preparations, it is possible to increase the concentration of potassium in the blood plasma.
When used simultaneously with lithium carbonate, it is possible to increase the concentration of lithium in the blood plasma and increase the risk of developing intoxication.
When used simultaneously with drugs used in anesthesia and analgesics, the antihypertensive effect may be enhanced.
When used simultaneously with acenocoumarol, a case of bleeding has been described.
When used simultaneously with indomethacin and other NSAIDs (acetylsalicylic acid), the effectiveness of ACE inhibitors may decrease.
Special instructions for the use of the drug Fozinopril
Prescribe with caution to patients with renovascular hypertension, heart failure, patients on hemodialysis, as well as patients with hypovolemia and/or reduced plasma osmolarity of any etiology due to the increased risk of developing side effects from the kidneys. In order to reduce the risk of arterial hypotension, diuretics should be discontinued 2-3 days before fosinopril is prescribed and the water and electrolyte balance should be corrected. In patients with left ventricular hypertrophy, long-term use of fosinopril leads to a decrease in left ventricular mass and a decrease in the thickness of the interventricular septum. After discontinuation of fosinopril, no withdrawal syndrome (sharp increase in blood pressure) is observed. The safety and effectiveness of fosinopril in pediatric practice has not been established. No special adjustment of the fosinopril dosage regimen is required in elderly patients. Women of reproductive age receiving fosinopril should use reliable contraception.
Fosinopril, 20 mg, tablets, 28 pcs.
2-3 days before starting treatment with fosinopril, it is recommended to discontinue previous diuretic therapy, with the exception of patients with malignant or difficult-to-treat hypertension. In such cases, fosinopril therapy should be started immediately, at a reduced dose, with close medical supervision and careful dose escalation.
Symptomatic hypotension with the use of ACE inhibitors most often develops in patients after intensive treatment with diuretics, a diet limiting salt intake, or during renal dialysis. Transient arterial hypotension is not a contraindication for continuing treatment after measures to restore blood volume.
In patients with chronic heart failure, treatment with ACE inhibitors may cause excessive antihypertensive effects, which can lead to oliguria or azotemia, which can be fatal. Therefore, when treating patients with chronic heart failure with fosinopril, careful clinical monitoring is necessary, especially during the first 2 weeks of treatment, as well as with any increase in the dose of fosinopril or diuretic.
ACE inhibitors rarely cause swelling of the intestinal mucosa. In this case, patients experience abdominal pain (sometimes without nausea and vomiting), facial swelling may also be absent, and the level of C1-esterases is normal. After stopping taking ACE inhibitors, symptoms disappear. Swelling of the intestinal mucosa should be taken into account in the differential diagnosis of patients with abdominal pain while taking ACE inhibitors.
During treatment with ACE inhibitors during hemodialysis using highly permeable membranes, as well as during LDL apheresis with adsorption on dextran sulfate, anaphylactic reactions may develop. In these cases, the use of a different type of dialysis membrane or other antihypertensive therapy should be considered.
It is possible to develop agranulocytosis and suppression of bone marrow function during treatment with ACE inhibitors. These cases occur more often in patients with impaired renal function, especially in the presence of systemic connective tissue diseases (systemic lupus erythematosus or scleroderma). Before starting therapy with ACE inhibitors and during treatment, the total number of leukocytes and the leukocyte formula are determined (once a month in the first 3-6 months of treatment and in the first year of treatment in patients with an increased risk of neutropenia).
If noticeable jaundice and a marked increase in liver enzyme activity occur, fosinopril treatment should be discontinued and appropriate treatment should be prescribed.
In case of arterial hypertension in patients with bilateral renal artery stenosis or stenosis of the artery of a single kidney, as well as with the simultaneous use of diuretics without signs of renal impairment during treatment with ACE inhibitors, the concentration of blood urea nitrogen and serum creatinine may increase. These effects are usually reversible and disappear after treatment is stopped. A dose reduction of diuretic and/or fosinopril may be required.
In patients with severe chronic heart failure with altered RAAS activity, treatment with ACE inhibitors can lead to oliguria, progressive azotemia and, in rare cases, acute renal failure and possible death.
During fosinopril therapy, the patient should be careful when performing physical exercise or in hot weather due to the risk of dehydration and hypotension due to a decrease in blood volume.
No special adjustment of the fosinopril dosage regimen is required in elderly patients. Safety of use in children has not been established.
Before and during treatment with the drug, it is necessary to monitor blood pressure, kidney function, potassium levels, hemoglobin levels, creatinine, urea, electrolyte concentrations and the activity of liver transaminases in the blood.
Influence on the ability to drive vehicles and operate machinery.
Caution is required when driving vehicles or performing other work that requires increased attention, because Dizziness may occur, especially after the initial dose of fosinopril.
