Enalapril-FPO - instructions for use, dose, side effects, contraindications

1 tablet contains: active substance enalapril 5 mg, 10 mg and 20 g, excipients: sugar milk, potato starch, talc, magnesium stearate, aerosil, microcrystalline cellulose

Description:tablets white with a yellowish hue of color, flat-cylindrical shape.

ATX: & nbsp

C.09.A.A.02 Enalapril

Pharmacodynamics:

Enalapril-FPO is an antihypertensive drug, the mechanism of its action is associated with a decrease in the formation of angiotensin II from angiotensin I, a decrease in its content leads to a direct decrease in the release of aldosterone. This reduces overall peripheral vascular resistance, systolic and diastolic blood pressure, post- and preload on the myocardium. Expands arteries more than veins, with a reflex increase in heart rate is not noted. Reduces the degradation of bradykinin, increases the synthesis of prostaglandin. The hypotensive effect is more pronounced with a high plasma renin level, than a normal or reduced level of plasma.

Reduction of blood pressure within the therapeutic limits does not affect cerebral circulation, blood flow in the vessels of the brain is maintained at a sufficient level against the background of reduced pressure. Strengthens coronary and renal blood flow. With prolonged use, hypertrophy of the left ventricle of the myocardium and myocytes of the artery wallsresistant type, prevents the progression of heart failure and slows the development of dilatation of the left ventricle. Improves the blood supply of the ischemic myocardium.

Reduces the aggregation of platelets. Has some diuretic effect. Enalapril is a "prodrug": as a result of its hydrolysis, a enalaprilate, which inhibits ACE.

The time of onset of the hypotensive effect with oral administration is 1 hour, reaches a maximum after 4-6 hours and lasts up to 24 hours. In some patients, in order to achieve the optimal level of blood pressure, therapy is needed for several weeks. With heart failure, a noticeable clinical effect is observed with prolonged use - 6 months or more.

Pharmacokinetics:

After ingestion, 60% of the drug is absorbed. Eating does not affect the absorption of enalaryl.

Enalapril binds up to 50% with plasma proteins. Enalapril is rapidly metabolized in the liver to form an active metabolite of enalaprilate, which is a more active ACE inhibitor than enalapril. Bioavailability of the drug is 40%.

The maximum concentration of enalapril in the blood plasma is reached after 1 hour, enalaprilata - after 3-4 hours. Enalaprilat easily passes through the histohematological barriers, excluding the blood-brain barrier, a small amount penetrates the placenta and into the breast milk.

The half-life of enalaprilat is about 11 hours. Displayed enalapril mainly through the kidneys of 60% (20% in the form of enalapril and 40% in the form of enalaprilata), through the intestine - 33% (6% in the form of enalapril and 27% in the form of enalaprilate).

It is removed during hemodialysis (rate 62 ml / min) and peritoneal dialysis.

Indications:

Enalapril-FPO is prescribed for various forms of hypertension, including renovascular hypertension. The drug is also effective in chronic heart failure (as part of combination therapy).

Contraindications:

Enalapril-FPO is contraindicated in cases of increased sensitivity to enalapril and other angiotensin-converting enzyme (ACE) inhibitors, with a history of angioedema, associated with treatment with ACE inhibitors, porphyria, pregnancy, lactation, under the age of 18 years.

Carefully:With caution should be used Enalapril-FPO in primary aldosteronism, bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney, hyperkalemia, condition after kidney transplantation, aortic stenosis, mitral stenosis (with hemodynamic disorders), idiopathic hypertrophic subaortic stenosis, systemic connective tissue diseases, ischemic heart disease, cerebrovascular diseases, diabetes mellitus, renal failure (proteinuria more than 1 g / day), liver failure , in patients who follow a diet with salt restriction or who are on hemodialysis, with simultaneous reception with immunosuppressants and saluretic, in the elderly (over 65 years).

Dosing and Administration:

Enalapril-FPO is administered orally regardless of the time of ingestion.

At monotherapy of an arterial hypertensia the initial dose - 5 mg once a day. If there is no clinical effect, after 1-2 weeks the dose is increased by 5 mg. After taking the initial dose, patients should be under medical supervision for 2 hours and an additional 1 hour until blood pressure stabilizes.If necessary and fairly well tolerated, the dose can be increased to 40 mg per day for 1 -2 admission. After 2-3 weeks pass to a maintenance dose of 10-40 mg per day, divided into 1 -2 admission. With moderate hypertension, the average daily dose is about 10 mg. The maximum daily dose is 40 mg.

In the event that it is necessary to appoint Enalapril-FPO to a patient who takes diuretics, treatment with diuretics should be discontinued 2-3 days before enalapril-FPO is started. If this is not possible, the initial dose of Enalapril-FPO should be 2.5 mg / day.

Patients with hyponatremia (concentration of sodium ions in the serum of less than 130 mmol / l) or with an increase in serum creatinine concentration of more than 0.14 mmol / l are given Enalapril-FPO at an initial dose of 2.5 mg once a day.

With Renovascular hypertension, the initial dose is 2.5 - 5 mg / day. The maximum daily dose is 20 mg.

In chronic heart failure, the initial dose of Enalapril-FPO is 2.5 mg once, then the dose is increased by 2.5 to 5 mg every 3-4 days according to the clinical response to the maximum tolerated dose, depending on the blood pressure values, but not above 40 mg / day once or in 2 divided doses.In patients with low systolic pressure (less than 110 mm Hg), therapy should be started at a dose of 1.25 mg / day. Selection of the dose should be carried out within 2-4 weeks or if necessary and the opportunity in a shorter time. The average maintenance dose is 5-20 mg / day for 1-2 doses.

In elderly people, the more pronounced hypotensive effect and lengthening of the action time of enalapril are more frequent, which is associated with a decrease in the rate of excretion of the drug, therefore the recommended initial dose for elderly patients is 1.25 mg / day. In chronic renal failure, cumulation of enalapril occurs with a decrease in filtration of less than 10 ml / min. When creatinine clearance (CC) is 80-30 ml / min, the dose of enalapril should be 5-10 mg / day, with a decrease in CK to 30-10 ml / min - 2.5-5 mg / day, with a CC less than 10 ml / min - 1,25-2,5 mg / day only on dialysis days.

The duration of treatment depends on the effectiveness of therapy. If the blood pressure is too low, the dose of Enalapril-FPO is gradually reduced. The drug is used in both monotherapy and in combination with other antihypertensive agents.

Side effects:

From the cardiovascular system: excessive decrease in blood pressure, orthostatic collapse, rarely - chest pain, stenocardia,myocardial infarction (usually associated with a marked decrease in blood pressure), arrhythmias (atrial brady or tachycardia, atrial fibrillation), palpitations, thromboembolism of the pulmonary artery branches, pain in the heart, fainting.

From the nervous system: dizziness, headache, weakness, insomnia, anxiety, confusion, fatigue, drowsiness (2-3%), very rarely with high doses of nervousness, depression, paresthesia.

From the sense organs: violations of the vestibular apparatus, hearing and vision impairment, tinnitus.

On the part of the gastrointestinal tract: dry mouth, anorexia, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), intestinal necessity, pancreatitis, impaired liver function and bile secretion, hepatitis, jaundice.

On the part of the respiratory system: unproductive dry cough, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, pharyngitis.

Allergic reactions: skin rash, angioedema, swelling of the face, limbs, lips, tongue, glottis and / or larynx, dysphonia, polymorphic erythema, exfoliative dermatitis, Stephen-Johnson syndrome,toxic epidermal necrolysis, pemphigus, pruritus, urticaria, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis.

On the part of laboratory indicators: hypercreatininaemia, increased urea levels, increased activity of "hepatic" transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia. In some cases, a decrease in hematocrit and hemoglobin content, an increase in ESR, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia are noted.

From the urinary system: a violation of kidney function, proteinuria. Other side effects: alopecia, decreased libido, hot flushes.

Overdose:

Symptoms: marked reduction in blood pressure until the development of collapse, myocardial infarction, acute cerebrovascular accident or thromboembolic complications, convulsions, stupor.

Treatment: patient is transferred to a horizontal position with a low headboard. In mild cases, gastric lavage and ingestion of saline are indicated. In more severe cases,aimed at stabilizing blood pressure: intravenous injection of physiological solution, plasma substitutes, and if necessary - angiotensin II, hemodialysis (the rate of enalapril removal is an average of 62 ml / min).

Interaction:

With the simultaneous administration of Enalapril-FPO with non-steroidal anti-inflammatory drugs, it is possible to reduce the hypotensive effect. Use of the drug in conjunction with potassium-sparing diuretics (spironolactone, triamterene, amiloride) can lead to hyperkalemia, with lithium salts, to a delay in the removal of lithium in the blood plasma (control of the concentration of lithium in blood plasma is shown). Simultaneous reception of Enalapril-FPO with antipyretic and analgesic drugs may decrease the effectiveness of enalapril. Enalapril weakens the effect of medicines containing theophylline.

The hypotensive effect of enalapril is enhanced by diuretics, beta-blockers, methyldopa, nitrates, blockers of "slow" calcium channels, hydralazine, prazozin. Immunosuppressants, allopurinol, cytotoxic drugs increase hematotoxicity.Drugs that cause bone marrow depression, increase the risk of developing neutropenia and / or agranulocytosis up to death.

Special instructions:

Care should be taken when prescribing patients with reduced circulating blood volume (as a result of diuretic therapy, limiting intake of salt, hemodialysis, diarrhea and vomiting) - the risk of a sudden and pronounced decrease in blood pressure after applying even an initial dose of an ACE inhibitor is increased. Transient hypotension is not a contraindication for continuing treatment with the drug after stabilizing blood pressure, should reduce the dose or cancel the drug.

With the development of excessive reduction in blood pressure, the patient is transferred to a horizontal position with a low headboard, if necessary, physiological saline and plasma-substituting drugs are administered.

The use of high-flow dialysis membranes increases the risk of developing an anaphylactic reaction. Correction of the dosing regimen on days free from dialysis should be carried out depending on the level of arterial pressure.

Before and after treatment with ACE inhibitors, control of blood pressure, blood counts (hemoglobin, potassium, creatinine, urea, activity of "liver" enzymes), protein in the urine is necessary.

It should be carefully monitored for patients with severe heart failure, coronary heart disease and cerebrovascular diseases, in which a sharp drop in blood pressure can lead to myocardial infarction, stroke, or renal dysfunction. Sudden withdrawal of treatment does not lead to the syndrome of "withdrawal" (a sharp rise in blood pressure).

Patients with a history of angioedema have an increased risk of developing it with ACE inhibitors.

For newborns and infants who have been exposed to the intrauterine effect of ACE inhibitors, careful monitoring is recommended to detect the pronounced decrease in arterial pressure, oliguria, hyperkalemia and neurological disorders that are possible due to a decrease in renal and cerebral blood flow while lowering the arterial pressure caused by ACE inhibitors.In oliguria, maintenance of arterial pressure and renal perfusion is necessary by the introduction of appropriate fluids and vasoconstrictors.

In patients with reduced renal function, a single dose should be reduced or intervals between doses should be increased.

Before the study of the function of parathyroid glands Enalapril-FPO should be abolished.

During the period of treatment it is not recommended to drink alcoholic beverages, since alcohol enhances the hypotensive effect of the drug.

Care should be taken when doing physical exercises in hot weather (the risk of dehydration and excessive reduction in blood pressure due to a decrease in the volume of circulating blood).

During the treatment period, it is necessary to refrain from driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions, since dizziness is possible, especially after the initial dose of an ACE inhibitor in patients taking diuretics.

Before surgery (including dentistry), it is necessary to alert the surgeon / anesthesiologist about the use of ACE inhibitors

Effect on the ability to drive transp. cf.and fur:

Form release / dosage:Tabletki by 0.005, 0.01 and 0.02 g.

Packaging:

Up to 10 tablets into a contiguous packaging. For 2, 3, 5 or 10 contour packs, together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

List B. Store in a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002143 / 01-2003

Date of registration:10.08.2009

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp18.10.2015

Illustrated instructions

Instructions

Enalapril-FPO (Enalapril-FPO)