Pharmacodynamics and pharmacokinetics
The drug has a pronounced antihypertensive and vasodilating effect. Its main component is metabolized within the body, resulting in the formation of a pharmacologically active substance - fosinoprilate . The mechanism of therapeutic action is manifested by inhibition of the activity of angiotensin-converting enzyme , which helps prevent the transition of angiotensin-I to angiotensin-II , which has a noticeable vasoconstrictor effect. bradykinin , also slows down . At the same time, the total peripheral vascular resistance decreases, blood pressure , and pre- and afterload on the myocardium .
These tablets are well absorbed from the gastrointestinal tract. The development of the therapeutic effect occurs within an hour, the maximum concentration is reached after 2-6 hours and lasts about 24 hours even with a single use. Long-term use does not contribute to the development of tolerance to fosinopril . This substance is characterized by an increased degree of binding to plasma proteins, about 95%. Excretion of fosinoprilat occurs through the kidneys and liver. On average, the half-life reaches 11.5 hours.
Pharmacological properties of the drug Fosicard
fosinopril is a prodrug, an ester of fosinoprilat, a long-acting ACE inhibitor. After oral administration, fosinopril is quickly and completely converted by hydrolysis into fosinoprilat, which is an active ACE inhibitor. In hypertension (arterial hypertension), the effect of fosinopril is mainly due to its effect on the renin-angiotensin-aldosterone system (RAAS). Inhibition of ACE and a decrease in the concentration of angiotensin II leads to vasodilation, a decrease in sodium and water retention due to inhibition of aldosterone secretion. There may be a slight increase in serum potassium. Inhibition of ACE slows down the breakdown of bradykinin, which is a powerful vasodilator, which also contributes to the therapeutic effect. When taking fosinopril once a day, blood pressure begins to decrease after 1 hour, the maximum effect occurs after 2–6 hours, the hypotensive effect persists for 24 hours. In heart failure, the effect of fosinopril is due to inhibition of the RAAS. ACE inhibition reduces both pre- and afterload. The hemodynamic effect persists for 24 hours when using fosinopril once a day. Treatment with fosinopril improves the performance of patients with heart failure within 24 hours after administration. Treatment with fosinopril reduces the need to increase the dose of diuretics to relieve symptoms of heart failure.
Contraindications for use
It is not recommended to take this drug if:
- hypersensitivity to fosinopril and other components;
- hereditary or idiopathic angioedema ;
- lactation, pregnancy;
- under 18 years of age.
Caution is necessary when:
- renal failure;
- hyponatremia;
- bilateral stenosis of the renal arteries and the artery of the only kidney;
- condition after kidney transplantation, desensitization, some systemic connective tissue diseases;
- hemodialysis;
- cerebrovascular diseases, for example, cerebrovascular insufficiency;
- diabetes mellitus;
- aortic stenosis;
- inhibition of bone marrow hematopoiesis;
- old age and so on.
Fosicard
Before starting treatment, it is necessary to analyze previous antihypertensive therapy, the degree of increase in blood pressure, dietary restrictions on salt and/or liquid, and other clinical circumstances.
Patients with severe arterial hypertension or concomitant decompensated CHF should begin treatment with Fosicard in a hospital setting.
Before and during treatment with the drug, it is necessary to monitor blood pressure, kidney function, potassium content, hemoglobin, creatinine, urea, electrolyte concentrations and the activity of “liver” transaminases in the blood.
Angioedema
The development of angioedema has been reported in patients using the drug Fosicard. Swelling of the tongue, pharynx, or larynx can cause airway obstruction, which can be fatal. If such reactions develop, patients must stop taking the drug and subcutaneously administer a solution of epinephrine (adrenaline) (1:1000), as well as take other emergency treatment measures.
There is a risk of anaphylactic reactions during desensitization with hymenoptera venom while taking an ACE inhibitor. The simultaneous use of APS inhibitors with the combination of valsartan + sacubitril is contraindicated due to the increased risk of angioedema. Taking Fosicard should not be started before 36 hours after taking the last dose of this combination, just as taking the combination of valsartan + sacubitril should not be started before 36 hours after taking the last dose of Fosicard.
Concomitant use of ACE inhibitors with racecadotril, mTOR inhibitors (such as sirolimus, everolimus, temsirolimus) and vildagliptin may lead to an increased risk of developing angioedema (see section "Interaction with other drugs").
Swelling of the intestinal mucosa
Swelling of the intestinal mucosa has rarely been observed while taking ACE inhibitors. These patients complained of abdominal pain (there may have been no nausea and vomiting), in some cases swelling of the intestinal mucosa occurred without swelling of the face, and the level of C1-esterases was normal. Symptoms disappeared after stopping the use of ACE inhibitors. Edema of the intestinal mucosa should be included in the differential diagnosis of patients taking ACE inhibitors who complain of abdominal pain.
Anaphylactic reactions during dialysis using high-permeability membranes Anaphylactic reactions may develop in patients who used ACE inhibitors during hemodialysis through high-permeability membranes, as well as during apheresis of low-density lipoproteins with adsorption to dextran sulfate. In these cases, the use of a different type of dialysis membrane or other antihypertensive therapy should be considered.
Neutropenia/agranulocytosis
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 use of the drug in patients with an increased risk of neutropenia).
Arterial hypotension
In patients with uncomplicated arterial hypertension, arterial hypotension may develop due to the use of the drug Fosicard.
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 the use of the drug after measures to restore blood volume.
In patients with CHF, treatment with ACE inhibitors may cause excessive antihypertensive effects, which can lead to oliguria or azotemia, which can be fatal. Therefore, when treating CHF with Fosicard, it is necessary to carefully monitor patients, especially during the first 2 weeks of treatment, as well as with any increase in the dose of Fosicard or a diuretic.
A reduction in the diuretic dose may be required in patients with hyponatremia and in patients previously intensively treated with diuretics. Arterial hypotension is not a contraindication for further use of the drug Fosicard. Some reduction in systemic blood pressure is a common and desirable effect when starting the drug for heart failure. The extent of this reduction is greatest early in treatment and stabilizes within one or two weeks of starting treatment. Blood pressure usually returns to pre-treatment values without a decrease in therapeutic efficacy.
Liver dysfunction
If noticeable jaundice appears and a marked increase in the activity of liver enzymes, Fosicard should be discontinued and appropriate treatment should be prescribed.
In rare cases, when using ACE inhibitors, a syndrome is observed, the first manifestation of which is cholestatic jaundice. This is followed by fulminant liver necrosis, sometimes fatal. The mechanism of development of this syndrome has not been studied.
In patients with impaired liver function, increased plasma concentrations of fosinopril may be observed. In liver cirrhosis (including alcoholic cirrhosis), the apparent total clearance of fosinopril is reduced, and the AUC is approximately 2 times higher than in patients without liver dysfunction.
Renal dysfunction
In patients with arterial hypertension with bilateral renal artery stenosis or stenosis of the artery of a single kidney, as well as with simultaneous use of diuretics without signs of renal impairment, the concentration of blood urea nitrogen and serum creatinine may increase during treatment with ACE inhibitors. These effects are usually reversible and disappear after treatment is stopped. It may be necessary to reduce the dose of the diuretic and/or Fosicard.
In patients with severe CHF, with altered activity of the renin-angiotensin-aldosterone system, treatment with ACE inhibitors can lead to oliguria, progressive azotemia and, in rare cases, acute renal failure and possible death.
Hyperkalemia
Increases in serum potassium levels have been observed in some patients receiving ACE inhibitor therapy, including fosinopril. Patients at increased risk of developing hyperkalemia include: patients with impaired renal function or diabetes mellitus, patients taking potassium-sparing diuretics, potassium supplements or potassium-containing salt substitutes, and patients taking other drugs that may increase serum potassium levels (eg heparin, trimethoprim or co-trimoxazole, also known as a combination of trimethoprim and sulfamethoxazole) and especially aldosterone antagonists or angiotensin receptor blockers. If the simultaneous use of these drugs is considered necessary, it is recommended to periodically monitor the level of potassium in the blood serum (see section "Interaction with other drugs").
Cough
When using ACE inhibitors, including fosinopril, some patients may experience a nonproductive, persistent cough that resolves after discontinuation of therapy. When cough occurs in patients taking ACE inhibitors, this therapy should be considered as a possible cause in the differential diagnosis.
Surgery/general anesthesia
ACE inhibitors may enhance the antihypertensive effect of drugs used for general anesthesia. Before surgery (including dentistry), the surgeon/anesthesiologist must be warned about the use of ACE inhibitors.
Special patient groups
Fosinopril (like other ACE inhibitors) has a less pronounced antihypertensive effect and has a higher risk of developing angioedema in black patients compared to representatives of other races.
There is no experience with the use of fosinopril in patients who have recently undergone kidney transplantation.
The drug should be used with caution in patients with obstruction of the blood outflow tract from the left ventricle (aortic or mitral stenosis/hypertrophic obstructive cardiomyopathy).
Caution should be exercised when performing work requiring increased attention, as dizziness may occur, especially after the initial dose of an ACE inhibitor in patients taking diuretics. Caution should be exercised when performing physical exercise or in hot weather due to the risk of dehydration and hypotension due to a decrease in blood volume.
The safety and effectiveness of Fosicard in children has not been established.
Side effects
When treated with Fosicard, side effects may occur that affect the activity of all systems and organs. For example, the cardiovascular system may respond with decreased blood pressure, orthostatic hypotension, tachycardia, palpitations, arrhythmia, angina pectoris, myocardial infarction, and chest pain.
Deviations in the functioning of the digestive system in the form of nausea, vomiting, constipation, intestinal obstruction, pancreatitis, hepatitis, stomatitis, glossitis, dyspepsia, abdominal pain, anorexia and so on are also possible.
In addition, it is possible that disorders associated with the activities of the respiratory, urinary and nervous systems .
There is still a possibility of damage to the sensory organs, the development of allergic reactions and changes in laboratory parameters .
Phosicard - instructions for use (Method and dosage)
Fosicard tablets are intended for oral administration. Usually the dosage and duration of treatment are selected individually, but there are a number of standard rules.
According to the instructions for use of Fosicard, during the treatment of arterial hypertension it is recommended to stop taking any antihypertensive drugs in advance.
The initial daily dosage of this drug is 1 time 10 mg. In the future, dose selection is required taking into account blood pressure indicators. In this case, the maintenance daily dose can be 10–40 mg once. If monotherapy with Fosicard does not bring a positive effect, then adding a diuretic .
When starting to take this drug along with a diuretic , an initial dose of up to 10 mg is prescribed, with careful medical monitoring of the patient’s condition.
During the treatment of chronic heart failure, an initial daily dose of 10 mg is set. Gradually increase the dose by 10 mg weekly. In this case, the maximum dosage should not be higher than 40 mg/day. It is also possible to additionally take a diuretic .
Use of the drug Fosicard
For hypertension (arterial hypertension), the initial dose is 10 mg/day. If necessary, the dose can be increased to 20–40 mg/day. If monotherapy does not lead to the expected effect, a thiazide diuretic can be added. For symptomatic heart failure, the initial dose is 5 mg/day with a gradual increase to a maximum dose of 40 mg/day. Since fosinoprilat is excreted both through the kidneys and through the liver, if renal or liver function is impaired, there is no need for dose adjustment.
Interaction
Simultaneous use of the drug with antihypertensive drugs, diuretics, narcotic analgesics, and general anesthesia can enhance the hypotensive effect of fosinopril.
Combination with potassium supplements and some potassium-sparing diuretics increases the likelihood of developing hyperkalemia . Simultaneous use with lithium salts increases the concentration of lithium in the blood.
Fosicard increases the hypoglycemic effect of sulfonylurea derivatives, insulin, the risk of leukopenia increases in cases of simultaneous use with allopurinol , immunosuppressants, cytostatic drugs, procainamide . Combination with NSAIDs and estrogens reduces the severity of the hypotensive effect.
special instructions
Treatment with Fosicard for patients suffering from severe arterial hypertension or decompensated chronic heart failure is recommended to begin in the hospital. In this case, the therapeutic process requires monitoring of blood pressure, kidney function, hemoglobin, urea and creatinine , concentrations of electrolytes and potassium, and the activity of liver enzymes in the blood.
It is also necessary to periodically monitor the number of leukocytes , especially if there is a risk of neutropenia , for example, in cases of impaired renal function or systemic connective tissue diseases.
A possible increase in the development of arterial hypotension requires caution when the drug is prescribed to patients who are on a salt-free or low-salt diet.
Taking this drug may cause dizziness, usually at the beginning of treatment when combined with diuretics , so caution should be used in activities requiring special attention or when driving.
Special instructions for the use of the drug Fosicard
Treatment with fosinopril should not be initiated in patients with acute myocardial infarction who are at risk of further severe hemodynamic deterioration after use of vasodilators. These are patients with systolic blood pressure ≤100 mm Hg. Art. or patients with cardiogenic shock. During the first 3 days after myocardial infarction, the dose should be reduced if systolic blood pressure is ≤120 mmHg. Art. The maintenance dose should be reduced to 5–2.5 mg if systolic blood pressure ≤100 mm Hg. Art. For persistent hypotension (systolic blood pressure ≤90 mm Hg), fosinopril should be discontinued. During treatment with fosinopril in combination with diuretics in patients without signs of renal vascular disease, there may be a slight increase in serum urea and serum creatinine. This effect, however, is more often noted in patients with pre-existing renal failure. A dose reduction of fosinopril may be necessary. Regular monitoring of potassium and creatinine levels is part of standard medical monitoring in these patients. In patients with heart failure, hypotension at the start of treatment with ACE inhibitors may lead to additional impairment of renal function. In such cases, acute renal failure may develop, usually reversible. In acute myocardial infarction, treatment with fosinopril should not be started in patients with diagnosed renal dysfunction, with a serum creatinine concentration of 177 µmol/l and/or proteinuria exceeding 500 mg/24 hours. If renal dysfunction develops during treatment with fosinopril (serum creatinine concentration of 265 µmol/ l or if serum creatinine levels are 2 times higher than before treatment), the doctor should consider discontinuing treatment with fosinopril. There is evidence of anaphylactic reactions in patients receiving ACE inhibitors during hemodialysis using high-permeability membranes. In such cases, the possibility of using a different type of dialysis membrane or the use of antihypertensive drugs of a different group should be considered. There is evidence of the appearance of cough after the use of ACE inhibitors. Usually the cough is non-productive, persistent and stops after discontinuation of the drug. During the first month of treatment with an ACE inhibitor, strict monitoring of blood glucose levels is necessary in patients taking oral antidiabetic agents or insulin. During pregnancy and breastfeeding. It is not known whether fosinopril passes into breast milk. The use of fosinopril during pregnancy and breastfeeding is not recommended. Ability to drive vehicles and operate machinery. Fosinopril has no or negligible effect on the ability to drive vehicles or operate machinery. Drivers should be aware that dizziness or fatigue may sometimes occur.
Fozikard's analogues
Level 4 ATC code matches:
Dilaprel
Prenesa
Enap
Diroton
Lipril
Renipril
Parnavel
Fozinap
Tritace
Enam
Zokardis
Fosinopril
Lisinopril
Captopril
Monopril
Renitek
Hartil
Amprilan
Ramipril
Perindopril
The main analogues are represented by the drugs Monopril, Fozinotec and Fosicard N. Also have a similar effect: Enalapril, Prestarium , Captopril and Lisinopril.
Reviews about Fosicard
This drug is usually prescribed for hypertension , but it should be understood that such treatment does not bring complete recovery. At the same time, reviews of Physicard show that complex therapy with this drug is carried out for patients who have been bothered by this disease for several years.
According to experts, treating hypertension requires the right approach and perseverance. Therefore, patients must comply with the doctor’s prescriptions without violating the therapeutic regimen and without stopping treatment on their own. In addition to taking medications, it is necessary to adhere to a healthy lifestyle and perform procedures that will strengthen blood vessels.
Overdose of the drug Fosicard, symptoms and treatment
When using doses significantly higher than recommended, severe arterial hypotension, circulatory shock, stupor, bradycardia, electrolyte disturbances and renal failure may develop. Treatment is carried out by gastric lavage (within 30 minutes after taking the drug) and accelerating elimination. Treatment with angiotensin II should be considered. Bradycardia and pronounced vagal reactions can be relieved by administering atropine. If necessary, the use of a temporary pacemaker should be considered.
Phosicard price, where to buy
The price of Fosicard varies between 107-237 rubles and depends on the content of the active substance in the tablets.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Phosicard tablets 10 mg 28 pcs. Zdravle JSC HFZ
328 rub. order - Phosicard tablets 20 mg 28 pcs. Zdravle JSC HFZ
RUB 354 order
- Phosicard tablets 5 mg 28 pcs. Zdravle JSC HFZ
RUB 212 order
Pharmacy Dialogue
- Fosicard N (tab. 20/12.5 mg No. 28) Actavis
RUB 377 order
- Phosicard (tab. 20 mg No. 28) Actavis
RUB 346 order
- Phosicard (tab. 5 mg No. 28)Zdravlje
210 rub. order
- Phosicard (tab. 10 mg No. 28)Zdravlje
RUR 326 order
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Pharmacy24
- Phosicard 20 mg No. 30 tablets Actavis AT.Islandiya/Pharmac.i Chemical Industry, Zdravle AT, Serbia/Balkanfarma-Dupnitsa AT, Bulgaria
204 UAH.order - Phosicard 10 mg No. 30 tablets Actavis AT.Icelandia/Pharmaceutical and Chemical Industry, Zdravle AT, Serbia
158 UAH order
PaniPharmacy
- Fosicard H tablets Fosicard N tablets. 20/12.5 mg No. 30 Iceland, Actavis
174 UAH order
- Phosicard tablets Phosicard tablets. 20 mg No. 30 Serbia, Zdravlje
205 UAH order
- Phosicard tablets Phosicard tablets. 10mg No. 30 Serbia, Zdravlje
152 UAH order
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