Monopril pill 20mg №28

Active ingredient and dosage form

Pills: 1 pill contains Fosinopril sodium 10 or 20 mg;
Excipients: lactose, microcrystalline cellulose, crospovidone, povidone, sodium stearyl fumarate;
14 pcs. in a blister, 1 or 2 blisters in a carton box.

Mechanism of action

ACE inhibitor. Fosinopril is an ester from which the active compound fosinoplatat is formed in the body as a result of hydrolysis under the action of esterases.
Fozinopril, due to the specific connection of the phosphate group with ACE, prevents the conversion of angiotensin I into the vasoconstrictor substance angiotensin II, as a result of which vasopressor activity and aldosterone secretion are reduced. The latter effect can lead to a slight increase in the content of potassium ions in the serum (on average 0.1 mEq / l) with a simultaneous loss of sodium ions and fluid from the body.
Fosinopril inhibits the metabolic degradation of bradykinin, which has a powerful vasopressor effect; due to this, the antihypertensive effect of the drug may increase.
In heart failure, the positive effects of Monopril are mainly achieved by suppressing the renin-aldosterone system. Suppression of ACE leads to a decrease in both preload and afterload on the myocardium.
In patients with heart failure, the drug improves symptoms and increases tolerance to physical exertion, reduces the severity of heart failure, and reduces the frequency of hospitalizations for heart failure. The drug is effective without the simultaneous use of Digoxin.

Suction
After ingestion, absorption from the gastrointestinal tract is about 30-40%. The degree of absorption does not depend on food intake, but the rate of absorption can be slow. C_max fosinoprilata in plasma is reached after 3 hours and does not depend on the dose taken.
Distribution
Plasma protein binding and> = 95%. Fozinoprilat has a relatively small volume of distribution and is slightly associated with cellular components of blood.
Metabolism
Hydrolysis of fosinopril under the action of esterases with the formation of fosinoprilat occurs mainly in the liver.
Removal
Fosinopril is eliminated from the body equally by the kidneys and through the liver. In hypertension in patients with normal kidney function and liver T_1/2 Fosinoprilata is about 11.5 hours. With heart failure T_1/2 is 14 hours
Pharmacokinetics in special clinical situations
In patients with impaired renal function (CK and <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 plasma AUC values ​​(less than twice the norm) was observed in patients with various degrees of renal failure, including end-stage renal failure (CC and <10 ml / min / 1.73 m²).
The clearance of fosinoprilat during hemodialysis and peritoneal dialysis averages 2% and 7% (relative to the values ​​of urea clearance), respectively.
In patients with impaired liver function (with alcoholic or biliary cirrhosis), the rate of hydrolysis of fosinopril may decrease without changing its degree. 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 and usage

- arterial hypertension (for monotherapy or as part of combination therapy);
- heart failure (in combination with diuretics).

Contraindications

- angioedema for the use of ACE inhibitors in history;
- pregnancy;
- lactation (breastfeeding);
- Hypersensitivity to fosinopril and other components of the drug.

Dosage and administration

Before starting treatment hypertension It is necessary to analyze the previously conducted antihypertensive drug therapy, the degree of increase in blood pressure, restrictions on the amount of salt and / or liquid, and other clinical circumstances. If possible, antihypertensive treatment should be discontinued according to the previously used regimen a few days before the start of treatment with Monopril.
The recommended initial dose is 10 mg 1 time / day. The dose must be selected depending on the dynamics of lowering blood pressure. The average dose is 10-40 mg 1 time / day. In the absence of a sufficient hypotensive effect, an additional appointment of diuretics is possible.
If treatment with Monopril is started on the background of the therapy with a diuretic, then its initial dose should be no more than 10 mg with careful medical monitoring of the patient's condition. In order to reduce the risk of arterial hypotension, diuretics should be canceled 2-3 days before the start of Monopril.
In chronic heart failure The recommended initial dose is 10 mg 1 time / day. Depending on the therapeutic efficacy, the dose can be increased with a weekly interval, increasing it to a maximum of 40 mg 1 time / day. At the beginning and during treatment, careful medical observation is required. The development of arterial hypotension after the initial dose should not interfere with the 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.

Adverse reactions

Cardiovascular: dizziness, palpitations, chest pains.
Respiratory: cough.
Allergic reactions: skin rash, itching.
Nervous system: feeling tired, impaired sensitivity (including paresthesia).
Musculoskeletal system: myalgia
Gastrointestinal: nausea, vomiting, dyspepsia, a violation of taste sensitivity.
As a rule, adverse reactions when taking the drug Monopril are easy and temporary in patients both young and older.

Pregnancy and breastfeeding

Monopril is contraindicated in pregnancy. The use of the drug in the II and III trimesters of pregnancy causes damage or death of the developing fetus.
Since fosinoprilat is excreted in breast milk, if you need to use Monopril during lactation, breastfeeding should be stopped.

Special notes

With the development of angioedema with monopril taking the drug should be immediately canceled. Patients should be warned that when there is swelling in the face, eyes, lips and tongue, laryngeal muscle spasm or shortness of breath, you should immediately stop taking the drug and consult a doctor.In such cases, it is necessary to promptly administer adrenaline solution (1: 1000) and take other emergency treatment measures.
Care must be taken when prescribing the drug to patients receiving desensitization therapy, because There is a risk of anaphylactoid reactions.
Anaphylactoid reactions have also been reported during the administration of Monopril during hemodialysis through highly permeable membranes, as well as during the apheresis of LDL with adsorption on dextran sulfate. In such cases, the use of another type of dialysis membrane or other drug treatment should be considered.
In rare cases, patients with an uncomplicated form of arterial hypertension when using Monopril developed arterial hypotension. Symptomatic arterial hypotension with the use of ACE inhibitors is most likely in patients after intensive treatment with diuretics and / or diets with limited salt content, as well as during kidney dialysis. 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 an excessive antihypertensive effect, which can lead to oliguria or azotemia, and in rare cases to acute renal failure and death.Therefore, in the treatment with Monopril of chronic heart failure, it is necessary to carefully monitor the condition of patients, especially during the first 2 weeks of treatment, as well as with any increase in the dose of fosinopril or diuretic.
Patients with normal or lowered blood pressure who have previously received intensive diuretic therapy and with low sodium levels in the blood may require a reduction in diuretic dose. Hypotension is not a contraindication for the further use of the drug Monopril. Some reduction in systemic blood pressure is a common and desirable effect at the beginning of the use of the drug in heart failure. The extent of this decrease is maximum in the early stages of treatment and stabilizes within 1-2 weeks of therapy. BP usually returns to the values ​​typical for the period before treatment begins, without reducing therapeutic efficacy.
If during the treatment with Monopril there is a noticeable yellowness and a pronounced increase in the activity of liver enzymes, the drug should be canceled and appropriate treatment should be prescribed.
With arterial hypertension in patients with renal artery stenosis of one or both kidneys, as well as the simultaneous use of diuretics without signs of renal vascular disease during treatment with ACE inhibitors, blood urea nitrogen and serum creatinine may be elevated. These effects are usually reversible and disappear after discontinuation of treatment.May require a reduction in the dose of diuretic and / or drug 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 may lead to oliguria or to progressive azotemia and in rare cases to acute renal failure and / or death.
In patients with heart failure, diabetes, while taking potassium-saving diuretics, potassium dietary supplements and / or salt substitutes containing potassium salts, or other drugs that increase the content of potassium in the blood (eg, heparin), the use of ACE inhibitors increases the risk of hyperkalemia.
Since fosinopril is eliminated from the body in two ways, a dose reduction of Monopril is usually not required when treating hypertension and heart failure in patients with impaired renal or hepatic function.
There is no difference in the efficacy and safety of treatment with Monopril in patients aged 65 years and older and younger. However, in older patients, greater susceptibility to the drug cannot be ruled out.
Control of laboratory parameters
While taking Monopril, the number of leukocytes 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), becauseit has been reported that in rare cases, ACE inhibitors cause agranulocytosis and suppression of bone marrow function with a greater likelihood in this category of patients.
Use in pediatrics
Safety and efficacy of the drug Monopril in children have not been established.

Symptoms: may increase the manifestations of the described side effects.
Treatment: drug withdrawal, symptomatic and supportive therapy, control of the patient’s clinical condition.

The simultaneous use of antacids (including aluminum hydroxide, Magnesium hydroxide, simethicone) can reduce the absorption of fosinopril (Monopril and these drugs should be taken at least 2 hours apart).
In patients receiving monopril simultaneously with lithium salts, it is possible to increase the concentration of lithium in the blood plasma and the risk of developing intoxication with lithium (at the same time, use with caution).
When prescribing Monopril, it should be borne in mind that Indomethacin and other NSAIDs (including acetylsalicylic acid) can reduce the antihypertensive effect of ACE inhibitors, especially in patients with low rootin hypertension.
With the joint use of Monopril with diuretics or in combination with a strict diet, limiting salt intake, or with dialysis, severe arterial hypotension may develop, especially in the first hour after taking the initial dose of fosinopril.
When combined with Monopril with potassium-sparing diuretics (including spironolactone, amiloride, triamterene), with potassium supplements, the risk of hyperkalemia increases (at the same time with caution; frequent monitoring of serum potassium is required).
The bioavailability of Monopril does not change with the combined use of the drug with chlorthalidone, Nifedipine, propranolol, hydrochlorothiazide, cimetidine, Metoclopramide, propanthelin, digoxin, Acetylsalicylic acid and Warfarin.
ACE inhibitors can enhance the antihypertensive effect of drugs used for general anesthesia.

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