Composition
Active ingredient:
enalapril maleate 20 mg.
Auxiliary substances:
lactose monohydrate,
hydroxypropyl cellulose,
corn starch,
sodium bicarbonate,
talc,
magnesium stearate.
Pharmacological action
Antihypertensive drug, ACE inhibitor. The mechanism of action is associated with inhibition of ACE activity, which leads to a decrease in the formation of angiotensin II.
Enalapril is a derivative of two amino acids: L-alanine and L-proline. After absorption, oral enalapril is hydrolyzed to enalalrylate, which inhibits ACE. The mechanism of its action is associated with a decrease in the formation of angiotensin II from angiotensin I, a decrease in the content of which in blood plasma leads to an increase in the activity of plasma renin (by eliminating the negative feedback to changes in renin production) and a decrease in aldosterone secretion. Since ACE is identical to the enzyme kininase II, enalapril can also block the breakdown of bradykinin, a peptide that has a powerful vasopressor effect. The significance of this effect in the mechanism of action of enalapril has not been definitively established.
The antihypertensive effect of enalapril is primarily associated with the suppression of RAAS activity, which plays an important role in the regulation of blood pressure. Despite this, enalapril has an antihypertensive effect even in patients with arterial hypertension and low renin concentrations.
When using enalapril, the blood pressure level decreases regardless of the body position (both in the supine and standing positions) without a significant increase in heart rate. Symptomatic orthostatic hypotension is rare. In some patients, achieving optimal BP reduction may require several weeks of therapy. Abrupt withdrawal of enalapril was not accompanied by an increase in blood pressure.
Effective ACE inhibition usually occurs 2-4 hours after a single oral dose of enalapril. The time of onset of antihypertensive action when taken orally is usually 1 hour, reaches a maximum – after 4-6 hours. The duration of action depends on the dose. When used at the recommended doses, the antihypertensive effect and hemodynamic effects are maintained for at least 24 hours.
In patients with essential hypertension, a decrease in blood pressure is accompanied by a decrease in OPSS and an increase in cardiac output, while the heart rate does not change or changes slightly. Renal blood flow increases, but the glomerular filtration rate does not change. However, in patients with an initially low glomerular filtration rate, its level usually increased.
In patients with diabetic/non-diabetic nephropathy, enalapril decreased albuminuria / proteinuria and renal excretion of IgG.
In patients with chronic heart failure (CHF) on the background of therapy with cardiac glycosides and diuretics, the use of enalapril is accompanied by a decrease in OPSS and BP, an increase in cardiac output, while the heart rate decreases (usually in patients with chronic heart failure, the heart rate is increased). The pressure of jamming of pulmonary capillaries is also reduced. Long-term use of enalapril increases exercise tolerance and reduces the severity of heart failure (assessed according to NYHA criteria). Enalapril in patients with mild to moderate heart failure slows its progression, as well as slows the development of left ventricular dilation. In patients with left ventricular dysfunction, enalapril reduces the risk of major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).
Indications
- arterial hypertension,
- heart failure,
- asymptomatic left ventricular dysfunction (as part of combination therapy).
Contraindications
- hypersensitivity to amlodipine or other components of the drug,
- hypersensitivity to other ACE inhibitors,
- a history of angioedema, including those associated with the use of ACE inhibitors (an allergic reaction with a sharp swelling of the lips, face, neck and, might of arms and legs, accompanied by dyspnea and hoarseness),
- porphyria,
- patients who have ever observed angioedema.
Side effects
- dry cough,
- pharyngitis,
- laryngitis,
- dizziness when sitting upright, palpitations, chest pain,
- impaired kidney function and blood picture,
- nausea, vomiting, abdominal pain,
- allergic skin reactions,
- headache, depression, sleep disorders,
- increased potassium in the blood.
Interaction
The patient should refrain from taking alcoholic beverages, as ethanol increases the reduction in blood pressure (BP) by enalapril.
Concomitant use of enalapril and diuretics or other antihypertensive agents increases the effectiveness of these drugs.
Interactions with drugs used to treat heart failure (cardiac glycosides) are not clinically relevant.
Before surgery, the doctor should be informed that the patient is taking enalapril, as there is a risk of hypotension during general anesthesia.
Concomitant use of enalapril and nonsteroidal anti-inflammatory drugs (NSAIDs) or acetylsalicylic acid (aspirin), as well as estrogens, may reduce the effectiveness of enalapril and increase the risk of impaired renal function.
Concomitant use of certain diuretics (spironolactone, amiloride, or triamterene) and / or additional use of potassium-containing tablets may cause an increase in serum potassium levels (hyperkalemia).
Drugs that cause bone marrow suppression increase the risk of developing neutropenia and / or agranulocytosis.
Immunosuppressants, allopurinol, cytostatics increase hematotoxicity.
Enalapril weakens the effect of drugs containing theophylline. Concomitant use of lithium medications may increase the side effects of lithium.
Concomitant use of Enap with cimetidine increases the half-life (T 1/2) of Enap. If the patient is already taking the above medications or is advised to take any of them, they should inform their doctor that they are taking Enap.
How to take, course of use and dosage
The drug Enap is prescribed orally, regardless of the time of food intake. The initial dose of Enap is 10-20 mg per day (once).
In the future, the dose is selected individually for each patient-usually 20 mg per day once.
The maximum daily dose should not exceed 40 mg.
In case of heart failure, it is prescribed starting from 2.5 mg, then the dose is gradually increased to 10-20 mg (in one or two doses).
Solution for intravenous use.
Enap is administered at a dose of 1.25 mg (1 ml) every 6 hours, including patients who have previously taken enalapril orally. Treatment is carried out only in a hospital setting.
The drug is administered intravenously in a slow jet (for 5 minutes) or dropwise in dilution in 20-50 ml of 5% dextrose (glucose) solution or 0.9% sodium chloride solution.
If the therapeutic effect is unsatisfactory 1 hour after use, the drug at a dose of 1.25 mg (1 ml) can be re-administered, and after 6 hours treatment is continued according to the usual scheme (1.25 mg every 6 hours).
In patients taking diuretics, the initial dose of the drug is reduced to 0.625 mg (0.5 ml). If the therapeutic effect is unsatisfactory 1 hour after use, the same dose can be re-administered, and after 6 hours treatment with the full dose (1.25 mg every 6 hours) is continued.
In mild to moderate chronic renal failure with creatinine clearance > 30 ml/min (serum creatinine does not exceed 265.2 mmol/L), the dose of Enap P is 1.25 mg (1 ml) every 6 hours, i. e. no dose adjustment is required.
At CC/l) the initial dose is 0.625 mg (0.5 ml), followed by monitoring for 1 hour to detect an excessive decrease in blood pressure.
If there is no effect after 1 hour, the dose of 0.625 mg is repeated and the treatment is continued at a dose of 1.25 mg every 6 hours. For patients undergoing hemodialysis, the Enap P dose is 0.625 mg (0.5 ml) every 6 hours for 48 hours.
Overdose
If the patient has taken too many pills at one time, call a doctor immediately.
Symptoms: Â excessive decrease in blood pressure (BP) up to the development of collapse, myocardial infarction, acute cerebrovascular accident or thromboembolic complications, convulsions, stupor.
Treatment: Â the patient is placed in a horizontal position with a low headboard. In mild cases, gastric lavage and ingestion of saline solution are indicated, in more serious cases-measures aimed at stabilizing blood pressure (BP), intravenous use of saline solution, plasma substitutes, if necessary – intravenous use of angiotensin II, hemodialysis (the rate of elimination of enalaprilat is 62 ml/min).
Special instructions
Use with caution Enap for car drivers. When used concomitantly with diuretics, beta-blockers effect of the drug Enap is enhanced, and with nonsteroidal anti-inflammatory drugs, the effect is reduced.
Hypotension (a sharp decrease in blood pressure) may occur (even a few hours after the first dose) in patients with severe heart failure or severe renal impairment, as well as in patients with impaired water and electrolyte balance due to diuretic treatment, a salt-free diet, diarrhea, vomiting, or who are on hemodialysis. A marked decrease in blood pressure (BP) usually manifests itself in the form of nausea, increased heart rate (HR), and fainting.
If hypotension develops, the patient should take a horizontal position, with a low headboard, and call a doctor.
Form of production
Tablets
Storage conditions
Store in a dark place at a temperature not exceeding 25°C.
Active ingredient
Enalapril
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Purpose
For adults as directed by your doctor
Indications
Hypertension, Heart Failure
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