Fozinopril tablets 20mg, No. 30

Arterial hypertension (as monotherapy or as part of combination therapy).

Chronic heart failure (as part of combination therapy).

It is taken internally.

With arterial hypertension, the initial dose is 10 mg 1 time / day. The maintenance dose is 10-40 mg 1 time / day. In the absence of a sufficient therapeutic effect, additional use of diuretics is possible.

In chronic heart failure, the initial dose is 5 mg 1-2 times / day. Depending on the therapeutic efficacy, the dose can be increased at weekly intervals up to a maximum daily dose of 40 mg 1 time / day.

The tablets are white or off-white, round, biconvex, scored on one side and 'f' embossed on the other.

1 tab.

fosinopril sodium 20 mg

Excipients: glyceryl distearate - 3 mg, colloidal silicon dioxide - 3 mg, sodium carboxymethyl starch - 6 mg, sodium stearyl fumarate - 6 mg, trehalose dihydrate - 15 mg, microcrystalline cellulose - 247 mg.

• Pregnancy,

• lactation (breastfeeding),

• hypersensitivity to ACE inhibitors.

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, preventing the breakdown of bradykinin.

Due to the vasodilating effect, it reduces the OPSS (afterload), the pressure of wedging 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. Food intake may reduce the rate, but not the extent of absorption. It is metabolized in the liver and in the gastrointestinal mucosa by hydrolysis with the formation of fosinoprilat, due to the pharmacological activity of which the hypotensive effect is realized. Plasma protein binding of fosinoprilat 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%.

Side effect

From the side of the cardiovascular system: a marked decrease in blood pressure, orthostatic hypotension, tachycardia, palpitations, arrhythmias, angina pectoris, myocardial infarction, chest pain, hot flushes 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, appetite disturbance, changes in body weight, dry mucous membranes membranes of the oral cavity, increased activity of hepatic 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 aggravation 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 visual impairment, tinnitus.

Allergic reactions: skin rash, itching, angioedema.

From the hematopoietic system: neutropenia, leukopenia, eosinophilia, lymphadenitis, decreased hemoglobin and hematocrit.

From the musculoskeletal system: arthritis.

From the side of metabolism: exacerbation of the course of gout, hyperkalemia, hyponatremia, increased ESR.

Application during pregnancy and lactation

Use during pregnancy is contraindicated.

During treatment, women of childbearing age should use reliable contraception.

Fozinopril is excreted in breast milk. If it is necessary to use fosinopril during lactation, the issue of stopping breastfeeding should be resolved.

Application in children

The safety of use in children has not been established.

Use in elderly patients

No special correction of the dosage regimen of fosinopril in elderly patients is required.

special instructions

It is used with caution in renovascular hypertension, heart failure, hyperkalemia, history of Quincke's edema, hypovolemia and / or low plasma osmolarity of various etiologies, as well as in patients on hemodialysis.

2-3 days before starting treatment with fosinopril, previous diuretic therapy is recommended to be canceled, with the exception of patients with malignant or difficult to treat arterial hypertension. In such cases, therapy with fosinopril should be started immediately, at a reduced dose, with close medical supervision and a careful increase in the dose.

Symptomatic arterial hypotension with the use of ACE inhibitors most often develops in patients after intensive diuretic treatment, a diet that restricts the intake of table salt, or during renal dialysis. Transient arterial hypotension is not a contraindication for continuing treatment after taking measures to restore the BCC.

In patients with chronic heart failure, treatment with ACE inhibitors can cause an excessive antihypertensive effect, which can lead to oliguria or fatal azotemia. 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 a diuretic.

ACE inhibitors rarely cause swelling of the intestinal mucosa. At the same time, patients have abdominal pain (sometimes without nausea and vomiting), swelling of the face may also be absent, the level of C1-esterases is normal. After stopping the use of ACE inhibitors, the symptoms disappear. Edema of the intestinal mucosa should be considered in the differential diagnosis in 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 to dextran sulfate, anaphylactic reactions may develop. In these cases, consideration should be given to using a different type of dialysis membrane or other antihypertensive therapy.

Perhaps the development of agranulocytosis and suppression of bone marrow function during treatment with ACE inhibitors. These cases are more common 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).

With the appearance of noticeable yellowness and a pronounced increase in the activity of liver enzymes by treatment with fosinopril, you should cancel and prescribe appropriate treatment.

With arterial hypertension in patients with bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney, as well as with the simultaneous use of diuretics without signs of impaired renal function during treatment with ACE inhibitors, the concentration of blood urea nitrogen and serum creatinine may increase. These effects are usually reversible and go away after treatment is stopped. A dose reduction of the 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, to acute renal failure and possible death.

During therapy with fosinopril, the patient should be careful when performing physical exercises or in hot weather due to the risk of dehydration and arterial hypotension due to a decrease in the BCC.

No special correction of the dosage regimen of fosinopril in elderly patients is required. The safety of use in children has not been established.

Before and during treatment with the drug, it is necessary to control blood pressure, kidney function, potassium content, hemoglobin, creatinine, urea, electrolyte concentration and hepatic transaminase activity in the blood.

Influence on the ability to drive vehicles and use mechanisms

Caution is required when driving or performing other work requiring increased attention, as dizziness is possible, especially after the initial dose of fosinopril.

Drug interactions

With simultaneous use with antacids, it is possible to increase the absorption of fosinopril.

With simultaneous use with antihypertensive drugs, an increase in the antihypertensive effect is possible.

With simultaneous use with diuretics, severe arterial hypotension may develop.

With simultaneous use with potassium-sparing diuretics, potassium preparations, an increase in the concentration of potassium in the blood plasma is possible.

With simultaneous use with lithium carbonate, it is possible to increase the concentration of lithium in the blood plasma and increase the risk of developing intoxication.

With simultaneous use with drugs used in anesthesia, analgesics, an increase in the antihypertensive effect is possible.

With simultaneous use with acenocoumarol, a case of bleeding has been described.

With simultaneous use with indomethacin, other NSAIDs (acetylsalicylic acid), it is possible to reduce the effectiveness of ACE inhibitors.