Enafarm - instructions for use, doses, side effects, contraindications

Excipients: granulate Ludipress (lactose monohydrate, povidone, crospovidone), magnesium stearate or lactose monohydrate, povidone, crospovidone, magnesium stearate

Description:

White tablets are planocylindrical with a facet and a risk (Enafarm® 10 mg) or a cross-shaped risk (Enafarm® 20 mg). A slight unevenness of the surface is permissible.

Pharmacotherapeutic group:an angiotensin-converting enzyme (ACE) inhibitor

ATX: & nbsp

C.09.A.A.02 Enalapril

Pharmacodynamics:

Enalapril is an antihypertensive drug from the group of ACE inhibitors.

Enalapril is a "prodrug": as a result of its hydrolysis, a enalaprilate, which inhibits ACE. The mechanism of its action is associated with a decrease in the formation of angiotensin-1 angiotensin-P, a decrease in the concentration of which leads to a direct decrease in the release of aldosterone. This reduces overall peripheral vascular resistance, systolic and diastolic blood pressure (BP), post-and preload on the myocardium.

Expands arteries more than veins, with a reflex increase in the purity of the heart beats is not noted.

The hypotensive effect is more pronounced with a high plasma renin level than at a normal or reduced level of plasma. Decrease in 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 and against a background of low blood pressure.

Strengthens coronary and renal blood flow.

With prolonged use, hypertrophy of the left ventricle of the myocardium and myocytes of the arteries of the resistive type, prevents the progression of the cardiacsufficiency and slows down 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.

The time of the onset of the hypotensive effect with ingestion is 1 hour, reaches a maximum after 4-6 hours and lasts up to 24 hours. Some patients need therapy for several weeks to achieve the optimal blood pressure level. 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 enalapril. Enalapril up to 50% binds to blood proteins. Enalapril is rapidly metabolized in the liver to form an active metabolite of enalaprilat, which is a more active ACE inhibitor than enalapril. Bioavailability of the drug - 40%.The maximum concentration of enalapril in the blood plasma is achieved after 1 hour, enalaprilata - 3-4 hours. Enalaprilat easily passes through the histohematological barriers, excluding the blood-brain barrier, a small amount penetrates through the placenta and into breast milk.

The half-life of enalaprilat is about 11 hours. Displayed enalapril mainly kidneys - 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 enalaprilata).

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

Indications:

Arterial hypertension; chronic heart failure (as part of combination therapy).

Contraindications:

Hypersensitivity to enalapril and other ACE inhibitors, history of angioedema, associated with treatment with ACE inhibitors, and hereditary or idiopathic angioedema, porphyria, pregnancy, lactation, age under 18 years (efficacy and safety not established).

Carefully:

Apply for primary hyperaldosteronism, 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, oppression of bone marrow hematopoiesis, hyperkalemia, conditions accompanied by a decrease in the volume of circulating blood (including vomiting, diarrhea), coronary heart disease, cerebrovascular diseases, diabetes mellitus, renal insufficiency (proteinuria - more than 1 g / day), liver failure, in patients observing a diet with restriction of salt or silt on hemodialysis, while admission to immunosuppressants and saluretikami in the elderly (over 65 years).

Pregnancy and lactation:

The drug is contraindicated in pregnancy and during the period of feeding.

At the onset of pregnancy, the drug should be stopped immediately.

Dosing and Administration:

Enafarm 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 BP stabilizes. If necessary, and a fairly good tolerability dose can be increased to 40 mg / day in 2 divided doses. After 2-3 weeks pass to the maintenance dose 10-40 mg / day, divided into 1 - 2 doses. With moderate arterial hypertension, the average daily dose is about 10 mg. The maximum daily dose of the drug is 40 mg / day.

In the case of appointing patients who are simultaneously receiving diuretics, treatment with a diuretic should be stopped 2-3 days before the appointment of enalapril. If this is not possible, the initial dose of the drug should be 2.5 mg / day.

Patients with hyponatremia (concentration of sodium ions in the serum of blood less than 130 mmol / l) or serum creatinine concentration greater than 0.14 mmol / l, the initial dose - 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 per day.

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

In elderly people, more pronounced hypotensive effect and lengthening of the drug action time are more often, which is associated with a decrease in the rate of excretion of enalapril, so the recommended initial dose for the elderly is 1.25 mg.

In chronic renal failure cumulation occurs with a decrease in filtration of less than 10 ml / min. With the clearance of creatinine (CC) -80-30 ml / min, the dose is usually 5-10 mg / day, with QC up to 30-10 ml / min-2.5-5 mg / day, with CC less than 10 ml / min. - 1,25-2,5 mg / day. only during dialysis days.

The duration of treatment depends on the effectiveness of therapy. At too pronounced decrease in blood pressure, the dose of the drug is gradually reduced.

The drug is used in both monotherapy and in combination with other antihypertensive drugs.

Side effects:

Enafarm as a whole is well tolerated and in most cases does not cause adverse reactions that require drug discontinuation.

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

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

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

From the digestive tract: dry mouth, anorexia, dyspeptic

(nausea, diarrhea or constipation, vomiting, abdominal pain), intestinal obstruction, pancreatitis, impaired liver function and bile secretion, hepatitis, jaundice.

From the respiratory system: unproductive dry cough, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, pharyngitis.

Allergic reactions: skin rash, itching, urticaria, angioedema, extremely rare - dysphonia, polymorphic erythema, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, pemphigus, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis.

From the laboratory indicators: hypercreatinemia, increased urea levels, increased activity of "hepatic" enzymes, hyperbilirubinemia, hyperkalemia, hyponatremia. In some cases, a decrease in hematocrit, an increase in the rate of erythrocyte sedimentation (ESR), thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia are noted.

From the urinary system: impaired renal function, proteinuria. Other: alopecia, decreased libido, hot flashes.

Overdose:

Symptoms: marked reduction in blood pressure, up to the development of collapse, myocardial infarction, acute impairment of cerebral circulation 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 shown, in more severe cases, measures aimed at stabilizing blood pressure: intravenous injection of physiological solution, plasma substitutes, if necessary - the introduction of angiotensin II, hemodialysis (the rate of excretion of enalaprilate is 62 ml / min) .

Interaction:

With the simultaneous appointment of Enafarm with non-steroidal anti-inflammatory drugs (NSAIDs), it is possible to reduce the hypotensive effect of enalapril; with potassium-sparing diuretics (spironolactone, triamterene, amiloride) - can lead to hyperkalemia; with lithium salts - to slow down the excretion of lithium (shown control of the concentration of lithium in blood plasma).

Simultaneous administration with antipyretic and analgesic drugs may decrease the effectiveness of Enafarm.

Enafarm weakens the effect of drugs containing theophylline.

The hypotensive effect of the drug 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.

Hypotensive action strengthens medicines for general anesthesia. Strengthens the action of ethanol.

Special instructions:

Caution should be exercised when administering Enafarm to patients with reduced circulating blood volume (due to diuretic therapy, restriction of salt intake, hemodialysis, diarrhea and vomiting), the risk of a sudden and severe decrease in blood pressure after applying even an initial dose of an ACE inhibitor is increased. Transient arterial hypotension is not a contraindication for continuing treatment with the drug after BP stabilization. In the case of a re-expressed decrease in blood pressure should reduce the dose or cancel the drug.

The use of high permeability dialysis membranes increases the risk of developing an anaphylactic reaction. Correction of the dosing regimen on days free from dialysis should be performed depending on the level of blood pressure.

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

It should be carefully monitored for patients with severe heart failure, coronary heart disease and cerebrovascular disease, in which a sharp decrease in blood pressure can lead to myocardial infarction, stroke, or renal dysfunction.

Sudden abolition of treatment does not lead to the syndrome of "withdrawal" (a sharp rise in blood pressure).

For newborns and infants who have undergone intrauterine exposure to ACE inhibitors, careful monitoring is recommended in order to promptly detect a marked decrease in blood pressure, oliguria, hyperkalemia and neurological disorders, possibly due to a reduction in renal and cerebral blood flow with a decrease in renal and cerebral blood flow. of BP caused by ACE inhibitors. In oliguria it is necessary to maintain BP and renal perfusion by introducing appropriate fluids and vasoconstrictors. In the presence of renal failure, it is possible to reduce the excretion of the active metabolite, leading to an increase in its concentration in the blood plasma.

Such patients may require the administration of smaller doses of the drug.

In patients with hypertension and unilateral or bilateral stenosis of the renal arteries, an increase in urea and creatinine in the blood serum is possible.

These patients need to monitor kidney function during the first few weeks of therapy. You may need to reduce the dosage of the drug.

It is necessary to take into account the correlation of risk and potential benefit in the appointment of Enafarm to patients with coronary and cerebrovascular insufficiency, due to the danger of increasing ischemia in cases of excessive arterial hypotension.

The drug should be administered with caution to patients with diabetes because of the risk of developing hyperkalemia.

Patients with a history of anginaurotic edema may

have an increased risk of developing angioedema along with treatment with Enafarm.

In patients with severe autoimmune diseases, such as systemic lupus erythematosus or scleroderma, the risk of developing neutropenia or agranulocytosis with Enafarm is increased.

It is advisable to use caution in appointing Enafarm for the therapy of chronic heart failure in patients receiving cardiac glycosides and / or diuretics.

Before the study of the function of parathyroid glands Enafarm should be canceled. Alcohol enhances the hypotensive effect of the drug.

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:

At the beginning of treatment, before the end of the dose selection period, it is necessary to refrain from driving vehicles and practicing potentially dangerous activities requiring increased concentration and speed of psychomotor reactions, sincecan be dizzy, especially after the initial dose of an ACE inhibitor in patients taking diuretics.

Form release / dosage:

Tablets of 10 mg and 20 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

2 contour mesh packaging along with the instructions for use are placed in a pack of cardboard.

Storage conditions:In a dry place protected from light. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N001982 / 01

Date of registration:16.01.2008

The owner of the registration certificate:FARMAKOR PRODUCTION, LTD. FARMAKOR PRODUCTION, LTD. Russia

Manufacturer: & nbsp

FARMAKOR PRODUCTION, LTD. Russia

Information update date: & nbsp23.10.2015

Illustrated instructions

Instructions

Enafarm® (Enafarm®)