Monopril, pills 20mg, 28pcs

Composition

Active ingredient: fosinopril sodium 20 mg

Pharmacological action

Monopril is hypotensive.

Pharmacodynamics

Fosinopril is an ester that is hydrolyzed in the body by enzymes to the active compound fosinoprilate. Due to the specific connection of the phosphinate group with ACE, it prevents the conversion of angiotensin I into the vasoconstrictor angiotensin II, which leads to vasodilation and a decrease in aldosterone secretion.

The latter effect can lead to a slight increase in the concentration of potassium ions in the serum (on average 0.1 mEq/l) and a decrease in the concentration of sodium ions and the volume of liquid. Fosinopril suppresses the metabolism of the bradykinin peptide, which has a powerful vasodilating effect, due to this, the antihypertensive effect of the drug may be enhanced.

Decline BP is not accompanied by changes in BCC, cerebral and renal blood flow, blood supply to internal organs, skeletal muscles, skin, and myocardial reflex activity. After oral use, the hypotensive effect develops within 1 hour, reaches a maximum in 3-6 hours and persists for 24 hours.

In heart failure, the positive effects of Monopril® They are achieved mainly by inhibiting the renin-aldosterone system. ACE inhibition leads to a decrease in both preload and afterload on the myocardium.

The drug helps to increase tolerance to physical activity, reduce the severity of heart failure.

Pharmacokinetics

After oral use, the absorption is approximately 30-40%. The degree of absorption does not depend on food intake, but its rate may slow down. Hydrolytic conversion of fosinopril under the action of enzymes to fosinoprilate occurs mainly in the liver and gastrointestinal mucosa.

With impaired liver function, the rate of hydrolysis may be slowed down, and the degree of conversion does not change significantly. _Cmax in blood plasma is reached after approximately 3 hours and does not depend on the dose taken. Fosinoprilate binds to blood proteins by ≥95%, has a relatively small volume of distribution and is slightly bound to the cellular components of the blood.

Fosinopril is excreted equally through the liver and kidneys. In hypertensive patients with normal renal and hepatic function, the T_1/2 of fosinoprilate is approximately 11.5 hours. In patients with heart failure, the value of T_1/2 is 14 hours. The clearance of fosinoprilate during hemodialysis and peritoneal dialysis is on average 2 and 7%, respectively, in relation to the values of urea clearance.

In patients with impaired renal function (creatinine clearance Reduced renal excretion is compensated for by increased liver excretion. A moderate increase in plasma AUC values (less than twice the normal value) is observed in patients with various degrees of renal insufficiency, including end-stage renal insufficiency (creatinine clearance 

In patients with impaired liver function (alcoholic or biliary cirrhosis), the rate of hydrolysis of fosinopril may be reduced, but the degree of hydrolysis does not significantly change. The total clearance of fosinoprilate from the body of such patients is approximately half that of patients with normal liver function.

Indications

Arterial hypertension, heart failure.

Contraindications

• hypersensitivity to fosinopril or any other substance included in the drug;
• a history of angioedema, including after taking other ACE inhibitors;
• pregnancy;
• lactation;
• age up to 18 years (efficacy and safety have not been established).

With caution:

• renal failure;
• hyponatremia (risk of dehydration, hypotension, chronic renal failure);
• bilateral renal artery stenosis or stenosis of the artery of a single kidney;
• aortic stenosis;
• condition after kidney transplantation;
• desensitization;
• systemic connective tissue diseases (including systemic lupus erythematosus, scleroderma) — increased risk of neutropenia or agranulocytosis;
• hemodialysis;
• cerebrovascular disease (including cerebrovascular insufficiency);
• coronary artery disease; congestive heart failure of III–IV grade (NYHA classification);
• diabetes mellitus;
• the oppression of bone marrow hematopoiesis;
• hyperkalemia;
• elderly patients;
• gout;
• when diet with restriction of salt;
• state, accompanied by a decrease in BCC (including diarrhea, vomiting, previous treatment with diuretics).

Side effects

From the cardiovascular system: dizziness, palpitation, chest pain.

Respiratory system disorders: cough.

Allergic reactions: skin rash, pruritus.

From the side of the central nervous system and peripheral nervous system: feeling tired, impaired sensitivity (including paresthesia).

Musculoskeletal disorders: myalgia.

From the digestive system: nausea, vomiting, dyspepsia, impaired taste sensitivity.

As a rule, adverse reactions when taking Monopril are mild and temporary in patients of both young and older age.

Interaction

Concomitant use of antacids (including aluminum hydroxide, magnesium hydroxide, simethicone) may reduce the absorption of fosinopril (Monopril and these drugs should be taken at intervals of at least 2 hours).

In patients receiving Monopril simultaneously with lithium salts, an increase in the concentration of lithium in blood plasma and the risk of lithium intoxication may occur (use with caution at the same time).

When prescribing Monopril, it should be taken into account that Indometacin and other NSAIDs (including acetylsalicylic acid) may reduce the antihypertensive effect of ACE inhibitors, especially in patients with low-renin hypertension.

When Monopril is co-administered with diuretics or in combination with a strict diet that restricts salt intake, or with dialysis, severe hypotension may develop, especially in the first hour after taking the initial dose of fosinopril.

When Monopril is co-administered with potassium-sparing diuretics (including spironolactone, amiloride, triamterene), with food supplements containing potassium, the risk of hyperkalemia increases (use with caution at the same time; frequent monitoring of serum potassium levels is required).

The bioavailability of Monopril does not change when the drug is co-administered with chlortalidone, nifedipine, propranolol, hydrochlorothiazide, cimetidine, metoclopramide, propantelin, digoxin, acetylsalicylic acid and warfarin.

ACE inhibitors may enhance the antihypertensive effect of drugs used for general anesthesia.

How to take, course of use and dosage

Before starting treatment for arterial hypertension, it is necessary to analyze the previous antihypertensive drug therapy, the degree of increase in blood pressure, restrictions on the amount of food salt and / or liquid, and other clinical circumstances. If possible, you should stop antihypertensive treatment according to the previously used scheme a few days before starting treatment with Monopril.

The recommended starting dose is 10 mg once a day. The dose should be selected depending on the dynamics of blood pressure reduction. The average dose is 10-40 mg 1 time/day. In the absence of a sufficient antihypertensive effect, additional diuretics may be prescribed.

If Monopril treatment is started against the background of diuretic therapy, then its initial dose should not exceed 10 mg with careful medical monitoring of the patient’s condition. In order to reduce the risk of hypotension, diuretics should be discontinued 2-3 days before starting Monopril.

In chronic heart failure, the recommended starting dose is 10 mg once a day. Depending on the therapeutic efficacy, the dose can be increased at weekly intervals, increasing it to a maximum of 40 mg 1 time/day. Careful medical supervision is required at the beginning and during treatment. The development of arterial hypotension after taking the initial dose should not interfere with careful selection of the dose of Monopril after effective relief of arterial hypotension. In case of heart failure, Monopril is recommended to be used in combination with a diuretic.

Overdose

Symptoms: marked decrease in blood pressure, bradycardia, shock, violation of the water-electrolyte state, acute renal failure, stupor.

Treatment: the drug should be discontinued, gastric lavage is indicated, taking sorbents (for example, activated carbon), vasopressors, infusions of 0.9% sodium chloride solution, and then symptomatic and supportive treatment. The use of hemodialysis is ineffective.

Special instructions

If angioedema develops while taking Monopril, the drug should be discontinued immediately. Patients should be warned that if they experience swelling of the face, eyes, lips and tongue, spasm of the laryngeal muscles or difficulty breathing, they should immediately stop taking the drug and consult a doctor.In such cases, rapid subcutaneous use of an epinephrine solution (1:1000) and other emergency measures are necessary.

Caution should be exercised when prescribing the drug to patients receiving desensitizing therapy, as there is a risk of developing anaphylactoid reactions.

Anaphylactoid reactions have also been reported with Monopril during hemodialysis through highly permeable membranes, as well as during LDL apheresis with adsorption on dextran sulfate. In such cases, a different type of dialysis membrane or other medical treatment should be considered.

In rare cases, patients with an uncomplicated form of arterial hypertension developed hypotension when using Monopril. Symptomatic hypotension with ACE inhibitors is most likely to occur in patients after intensive diuretic treatment and / or a salt-restricted diet, as well as during renal dialysis. A temporary hypotensive reaction is not a contraindication for the use of the drug after taking measures to hydrate the body.

In chronic heart failure with or without concomitant renal failure, treatment with ACE inhibitors can cause excessive antihypertensive effects, which can lead to oliguria or azotemia, and in rare cases, to acute renal failure and death. Therefore, when treating chronic heart failure with Monopril, patients should be carefully monitored, especially during the first 2 weeks of treatment, as well as with any increase in the dose of fosinopril or a diuretic.

Patients with normal or low blood pressure who have previously received intensive diuretic therapy, and with a low blood sodium content, may need to reduce the dose of the diuretic. Arterial hypotension is not a contraindication for further use of Monopril. Some reduction in systemic blood pressure is a common and desirable effect at the beginning of the drug use in patients with heart failure.

The degree of this decrease is maximal in the early stages of treatment and stabilizes within 1-2 weeks of therapy. Blood pressure usually returns to pre-treatment values without reducing therapeutic effectiveness.

If there is noticeable jaundice and a marked increase in liver enzyme activity during treatment with Monopril, the drug should be discontinued and appropriate treatment should be prescribed. In hypertensive patients with renal artery stenosis of one or both kidneys, as well as with the simultaneous use of diuretics without signs of renal vascular disease during treatment with ACE inhibitors, it is possible to increase the level of urea nitrogen in the blood and serum creatinine.

These effects are usually reversible and resolve after discontinuation of treatment. It may be necessary to reduce the dose of the diuretic and / or Monopril. In patients with severe chronic heart failure, in whom renal function may depend on the activity of the renin-angiotensin-aldosterone system, treatment with ACE inhibitors can lead to oliguria or progressive azotemia, and in rare cases to acute renal failure and / or death.

In patients with heart failure, diabetes mellitus, and concomitant use of potassium-sparing diuretics, potassium supplements and/or dietary salt substitutes containing potassium salts, or other drugs that increase the blood potassium content (for example, heparin), the use of ACE inhibitors increases the risk of hyperkalemia.

Since fosinopril is eliminated from the body in two ways, it is usually not necessary to reduce the dose of Monopril in the treatment of hypertension and heart failure in patients with impaired renal or hepatic function.

There are no differences in the efficacy and safety of Monopril treatment in patients aged 65 years and older and younger. However, in older patients, greater susceptibility to the drug cannot be excluded.

Monitoring of laboratory parameters While taking Monopril, the number of white blood cells in the peripheral blood should be periodically determined, paying attention to patients with impaired renal function, especially against the background of collagenosis (systemic lupus erythematosus or scleroderma), since it has been reported that in rare cases ACE inhibitors cause agranulocytosis and suppression of bone marrow function more likely in this category of patients.

Use in pediatricsafety and efficacy of Monopril in children have not been established.

Form of production

Tablets

Storage conditions

The drug should be stored in a dry place at room temperature.

Shelf life

3 years

Active ingredient

Fosinopril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Heart Failure, Hypertension