Enalapril, tablets 10 mg 20 pcs

Enalapril is an antihypertensive drug from the ACE inhibitor group. Enalapril is a “prodrug”: as a result of its hydrolysis enalaprilat is formed, which inhibits ACE. Its mechanism of action is related to the reduction of angiotensin I and angiotensin II, the reduction of which leads to a direct reduction of aldosterone secretion. This reduces total peripheral vascular resistance, systolic and diastolic blood pressure (BP), post- and preload on the myocardium. It dilates arteries to a greater extent than veins, and there is no reflex increase in heart rate.
Hypotensive effect is more pronounced at high plasma renin levels than at normal or reduced levels. Decrease in BP within therapeutic limits does not affect the cerebral blood flow, blood flow in the brain vessels is maintained at a sufficient level even against the background of reduced blood pressure. It increases coronary and renal blood flow.
Long-term use reduces myocardial hypertrophy of the left ventricle and myocytes of the walls of the resistive arteries, prevents the progression of heart failure and slows the development of dilatation of the left ventricle.
Improves blood supply to ischemic myocardium. Reduces platelet aggregation. Has some diuretic effect. Time of onset of hypotensive effect when taken orally -1 hour reaches a maximum after 4-6 hours and lasts up to 24 hours. In some patients, therapy for several weeks is necessary to achieve optimal blood pressure levels.
With heart failure noticeable clinical effect is observed with long-term use – 6 months or more.

Indications

Arterial hypertension (symptomatic, renovascular, including in scleroderma, etc.), CHF of I-III stage; prevention of coronary ischemia in patients with LV dysfunction, asymptomatic LV dysfunction.

Active ingredient

Composition

1 tablet contains: enalapril maleate – 10 mg.
Excipients: lactose monohydrate, magnesium carbonate, gelatin, crosspovidone, magnesium stearate.

How to take, the dosage

In monotherapy of arterial hypertension, the initial dose is 5 mg once daily. If there is no effect, the dose is increased by 5 mg after 1-2 weeks. After the initial dose, patients should be under medical supervision for 2 hours and an additional 1 hour until BP stabilizes. If necessary and tolerated well enough, the dose can be increased to 40 mg/day at 1-2 doses. After 2-3 weeks, switch to a maintenance dose of 10-40 mg/day divided into 1-2 doses. In moderate hypertension, the average daily dose is about 10 mg. The maximum daily dose of the drug is 40 mg.
If prescribed to patients simultaneously receiving diuretics, diuretic treatment should be discontinued 2-3 days before enalapril administration. If this is not possible, the initial dose of enalapril should be 2.5 mg/day.
Patients with hyponatremia (serum Na+ concentration less than 130 mmol/l) or serum creatinine concentration more than 0.14 mmol/l should take an initial dose of 2.5 mg once daily.
Renovascular hypertension: the initial dose is 2.5-5 mg/day. The maximum daily dose is 20 mg.
In severe arterial hypertension it is possible to administer by intravenous injection (see Enalaprilat) only in hospital.
In CHF the initial dose is 2.5 mg once and then the dose is increased by 2.5-5 mg every 3-4 days according to the clinical response to maximum tolerated doses (depending on BP), but not more than 40 mg/day, once or in 2 doses. In patients with low systolic blood pressure (less than 110 mmHg), therapy should be started with a dose of 1.25 mg. The dose should be adjusted over 2-4 weeks or at shorter intervals. The average maintenance dose is 5-20 mg/day at 1-2 doses.
More severe hypotensive effect and prolongation of action time are more often observed in elderly patients due to decreased elimination rate of enalapril, therefore the recommended initial dose for elderly patients is 1.25 mg.
In asymptomatic LV dysfunction – 2.5 mg 2 times a day. The dose is adjusted for tolerance to 20 mg/day, divided into 2 doses.
In CKD, cumulation occurs when filtration is less than 10 ml/min. With a CK of 80-30 ml/min, the dose is usually 5-10 mg/day, with a CK of 30-10 ml/min, 2.5-5 mg/day, and less than 10 ml/min, 1.25-2.5 mg/day on dialysis days only.
The duration of treatment depends on the effectiveness of therapy. If BP decreases too significantly, the drug dose is gradually decreased.

Interaction

The decrease of hypotensive effect is determined by NSAIDs, including selective COX-2 inhibitors, estrogens, increase is determined by diuretics and other hypotensive drugs (beta-adreno-blockers, methyldopa, nitrates, BICC, hydralazine, prazosin). The effect of hypotensive drugs (beta-adrenoblockers, methyldopa, nitrates, NSAIDs, hydralazine, prazosin), drugs for general anesthesia, ethanol.
Potassium-saving diuretics and potassium-containing drugs increase the risk of hyperkalemia.
Drugs that cause bone marrow suppression increase the risk of neutropenia and/or agranulocytosis.
Concurrent use of ACE inhibitors and gold drugs for parenteral use (sodium aurothiomalate) is described symptomcomplex including facial hyperemia, nausea, vomiting and decreased blood pressure.
Simultaneous use with insulin and oral hypoglycemic agents increases the risk of hypoglycemia.
Immunosuppressants, allopurinol, cytostatics increase hematotoxicity.

Special Instructions

Caution should be exercised when prescribing to patients with decreased blood pressure (as a result of diuretic therapy, restriction of table salt intake, hemodialysis, diarrhea and vomiting) – the risk of sudden and pronounced BP decrease after using even the initial dose of ACE inhibitor is increased. Transient hypotension is not a contraindication for continuation of treatment with the drug after BP stabilization. In case of recurrent marked BP decrease the dose should be reduced or the drug should be discontinued.
In case of development of excessive BP decrease the patient should be transferred to the horizontal position with low headrest, if necessary 0.9% NaCl solution and plasma exchange drugs should be administered.
The use of high-flow dialysis membranes (including AN69) increases the risk of anaphylactic reaction. The dosage regimen adjustment during the days free of dialysis should be made depending on the blood pressure.
Blood pressure, blood parameters (Hb, K+ concentration, creatinine, urea, liver enzymes activity), protein in urine should be controlled before and during the treatment with ACE inhibitors.
Patients with decompensated CHF, coronary artery disease and cerebrovascular disease should be closely monitored as rapid decrease of BP may result in myocardial infarction, stroke or renal impairment. Sudden treatment withdrawal does not lead to “withdrawal” syndrome (a sharp rise in BP).
Patients with a history of angioedema have an increased risk of its development when taking ACE inhibitors.
Newborns and infants who have had intrauterine exposure to ACE inhibitors should be closely monitored for the timely detection of marked BP decline, oliguria, hyperkalemia, and neurologic disorders that may result from decreased renal and cerebral blood flow with ACE inhibitor-induced BP decline. In oliguria it is necessary to maintain BP and renal perfusion by administering appropriate fluids and vasoconstrictors.
In patients with reduced renal function the single dose should be reduced or the intervals between doses should be increased.
Enalapril should be discontinued before parathyroid function tests.
Caution should be exercised or in hot weather (risk of dehydration and excessive BP decrease due to decreased BCC).
Before surgical interventions (including dentistry) the surgeon/anesthesiologist should be advised about the use of ACE inhibitors.
During the treatment period caution should be exercised while driving motor transport and engaging in other potentially dangerous activities requiring increased concentration and rapid psychomotor reactions (dizziness is possible, especially after the initial dose of ACE inhibitor in patients taking diuretic drugs).

Contraindications

Hypersensitivity to enalapril or other ACE inhibitors, pregnancy, lactation.
With caution. Angioneurotic edema in past history of ACE inhibitor therapy, hereditary or idiopathic angioedema, aortic stenosis, cerebrovascular diseases (including cerebrovascular insufficiency), CHD, coronary artery disease, severe autoimmune systemic connective tissue diseases (including scleroderma scleroderma). SLE, scleroderma), suppression of medullary hematopoiesis, diabetes mellitus, hyperkalemia, bilateral stenosis of renal arteries, stenosis of artery of single kidney, conditions after kidney transplantation, renal and/or hepatic insufficiency, Na+-restricted diet, conditions accompanied with OBC reduction (including diarrhea, vomiting), elderly age, age under 18 years (safety and efficacy of administration have not been studied).

Side effects

System adverse reactions: excessive BP decrease, orthostatic collapse, rarely – chest pain, angina pectoris, myocardial infarction (usually associated with marked BP decrease), arrhythmias (atrial bradycardia or tachycardia, atrial fibrillation), palpitation, pulmonary artery thromboembolism.
Nervous system disorders: dizziness, fainting spells, headache, weakness, insomnia, anxiety, confusion, increased fatigability, somnolence (2-3%), very rarely in high doses – nervousness, depression, paresthesia.
The sensory system: disorders of the vestibular system, hearing and vision disorders, tinnitus.
The digestive system: oral mucosa dryness, decreased appetite, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), bowel obstruction, pancreatitis, liver function and bile excretion disorders, hepatitis, jaundice.
Respiratory system: unproductive “dry” cough, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, pharyngitis.
Allergic reactions: skin rash, angioedema of the face, small intestine (very rare), extremities, lips, tongue, vocal cleft and/or larynx, dysphonia, exfoliative dermatitis, erythema multiforme exudative (including Stevens-Johnson syndrome).Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), pemphigus, pruritus, urticaria, photosensitization, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis.
Laboratory data: hypercreatininemia, increased urea, increased liver transaminase activity, hyperbilirubinemia, hyperkalemia, hyponatremia, decreased Hb and hematocrit, increased sedimentation, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia.
Urinary system: renal dysfunction, proteinuria.
Other: alopecia, decreased libido, blood flushes to the face. Cases of hypoglycemia have been reported in patients with diabetes mellitus who have taken insulin and oral hypoglycemic drugs.

Overdose

Symptoms: excessive BP decrease, up to the development of collapse, myocardial infarction, acute violation of cerebral circulation or thromboembolic complications; convulsions, stupor.
Treatment: the patient is transferred to a horizontal position with a low headboard. In mild cases gastric lavage and oral intake of saline solution are indicated, in more severe cases – measures aimed at BP stabilization: intravenous infusion of 0.9% NaCl solution, plasma substitutes, if necessary – intravenous angiotensin II, hemodialysis (elimination rate of enalaprilat 62 ml/min).

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