Eneas

Eneas is a complex medication that lowers blood pressure.

The composition of the drug contains the component enalapril, which is an ACE inhibitor and exerts its effect by suppressing the activity of the RAAS. The drug prevents the transformation of angiotensin-1 into the vasodilating peptide angiotensin-2, which allows eliminating its stimulating effect on the adrenal glands, as well as the secretion of aldosterone.

In addition, the medication contains a calcium antagonist, the substance nitrendipine. It is active by blocking the passage of calcium ions through the smooth muscle cell membranes of blood vessels.

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Indications Eneasa

It is used for elevated blood pressure as an integral component of complex treatment.

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Release form

The drug is produced in tablets - 10 pieces in a blister pack. There are 3 such packs in a pack.

Pharmacodynamics

The main effect of enalapril is aimed at suppressing the activity of the RAAS, which is an important element in the processes of blood pressure regulation, due to which the component can demonstrate a hypotensive effect in people with low-renin hypertension.

Long-term use of enalapril in patients with essential hypertension and renal insufficiency may improve renal function by increasing the glomerular filtration rate.

Nitrendipine is a derivative of 1,4-dihydropyridine. It lowers intracellular calcium levels, resulting in decreased vascular muscle contractility; by dilating peripheral arteries, systemic peripheral resistance is reduced, and excessively elevated blood pressure is reduced.

Nitrendipine has moderate natriuretic activity, especially at the initial stage of therapy.

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Pharmacokinetics

Enalapril is absorbed at high speed in the gastrointestinal tract, and its absorption is not affected by the presence of food. In serum, Cmax values are noted after 1 hour.

Intraplasmic protein synthesis is 50-60%. After absorption, the component is hydrolyzed at high speed to form enalaprilat. It reaches serum Cmax values 3-4 hours after oral administration.

Excretion occurs mainly through the kidneys (unchanged state, as well as enalaprilat (40%)). Apart from transformation into enalaprilat, no other noticeable manifestations of metabolic transformations of the substance are observed. Enalaprilat in the blood serum has an extended terminal stage associated with the processes of ACE synthesis.

In individuals with healthy renal function, stable enalaprilat values are observed by the 4th day of drug use.

The effective half-term of enalaprilat accumulation with multiple oral administration of the drug is 11 hours. The level of hydrolysis and absorption of enalapril is identical when administering portions from the recommended dosage range.

Nitrendipine is absorbed almost completely (88%) and at high speed, reaching serum Cmax values 1-3 hours after taking the drug.

The bioavailability level is within 20-30%. Synthesis of the component with intraplasmic protein is 96-98%.

Almost all nitrendipine undergoes intrahepatic metabolism through oxidative processes.

The half-life is in the range of 8-12 hours. No accumulation of the active element and its metabolic components was observed.

In people with chronic liver problems, plasma levels of nitrendipine increase.

Excretion of the element is mainly carried out through the kidneys in the form of inactive metabolic components (approximately 77%), as well as through the bile ducts.

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Dosing and administration

Eneas should be taken orally (at the same time, it is recommended to do this in the morning). The use of the drug is not tied to food intake. Usually, 1 tablet of the drug is taken per day.

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Use Eneasa during pregnancy

Eneas should not be used during breastfeeding or pregnancy, or when planning to conceive.

Contraindications

Main contraindications:

• severe sensitivity or allergy associated with active ingredients or auxiliary components of the drug;
• unstable hemodynamics (especially after experiencing a state of shock, stroke, acute heart failure or coronary heart disease in the active phase);
• porphyria;
• history of angioedema associated with ACE inhibitor use;
• kidney transplant;
• bilateral stenosis affecting both renal arteries, or stenosis affecting the arteries of a single kidney;
• cardiomyopathy of a hypertrophic nature;
• Conn's syndrome;
• severe liver failure;
• anuria or renal pathology in the chronic phase (stages 4-5).

Caution is required when prescribing in the following situations:

• diabetes mellitus;
• CHF;
• elderly people;
• decrease in BCC indicators;
• severe form of aortic stenosis or stenosis affecting the subaortic region and having a hypertrophic idiopathic form and obstructive nature;
• cerebrovascular diseases and coronary heart disease;
• periods after kidney transplantation.

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Side effects Eneasa

Enalapril.

Main side effects:

• CVS dysfunction: orthostatic collapse or decreased blood pressure with symptoms such as weakness, visual impairment, and dizziness may sometimes occur. Syncope may occasionally occur (especially at the initial stage of therapy, when the dose of enalapril maleate or diuretics is increased in patients with EBV disorders, as well as heart failure or elevated renal blood pressure). Occasionally, a sharp drop in blood pressure may cause palpitations, angina with tachycardia, chest pain, arrhythmia, stroke, pulmonary edema, and also bradycardia, myocardial infarction, atrial fibrillation, cerebral blood flow disorders, transient intracerebral blood flow disorder, pulmonary infarction, and pulmonary artery embolism;
• urinary tract and kidney disorders: sometimes kidney dysfunction or exacerbation occurs, and renal failure develops. Proteinuria or oliguria are occasionally observed, and people with renal dysfunction may develop lumbar pain. Acute renal failure is observed occasionally;
• respiratory problems: dyspnea is often observed. Sometimes wheezing, sore throat, rhinorrhea, dry cough or bronchitis occur. Occasionally, rhinitis, sinusitis, eosinophilic pneumonia or allergic alveolitis occur. Stomatitis, pneumonia, asthma or bronchial spasm, infiltrate in the lungs, dry mouth mucosa, glossitis and Quincke's edema in the pharynx with larynx or tongue are observed alone (at times this can cause obstruction of the respiratory tract, and the main risk group in this case are representatives of the Negroid race);
• disorders affecting the liver and gastrointestinal tract: sometimes there are pains in the upper abdominal region, peptic ulcers, gastric irritation, nausea and indigestion. Rarely, diarrhea, loss of appetite, constipation or vomiting are observed. Isolated hepatitis (cholestatic or hepatocellular type), intestinal Quincke's edema, problems with liver function, liver failure, cholestasis (along with jaundice), necrosis, stomatitis, intestinal obstruction, pancreatitis and glossitis develop;
• endocrine function disorders: gynecomastia appears occasionally. Development of ADH secretion disorder syndrome is possible;
• problems related to the functioning of the nervous system: sometimes drowsiness, headaches, severe fatigue and insomnia are observed. Occasionally, depression, balance or sleep disorders, dizziness, polyneuropathy with paresthesia, impotence develop, as well as nervousness, cramps affecting muscles, abnormal dreams and confusion;
• Symptoms related to the epidermis and blood vessels: a rash often appears. Sometimes signs of allergy are observed. Rarely, urticaria, itching, erythroderma or Quincke's edema develop, affecting the tongue, extremities, lips with face, larynx or glottis. Isolated severe epidermal reactions (SSD, pemphigus, exfoliative dermatitis, TEN and erythema multiforme), hyperhidrosis, photosensitivity, Raynaud's syndrome, alopecia and onycholysis develop. Skin heat can be observed against the background of myositis or myalgia, arthritis or arthralgia, serositis, vasculitis, leukocytosis, eosinophilia, as well as an increase in the erythrocyte sedimentation rate and a positive test for the presence of antinuclear antibodies;
• metabolic disorders: sometimes hypoglycemia occurs;
• sensory disturbances: occasionally blurred vision, tinnitus, loss of smell, change or temporary loss of taste, lacrimation or dry eyes;
• systemic disorders: asthenia usually occurs. Hot flashes sometimes occur;
• changes in test results: sometimes there is a decrease in hematocrit or hemoglobin values or the number of platelets and leukocytes.

Nitrendipine.

Side effects include:

• systemic lesions: sometimes flu-like symptoms or asthenia are observed;
• dysfunction of the cardiovascular system: sometimes cardiac palpitations, hyperemia, arrhythmia, peripheral edema, tachycardia or vasodilation occur. Angina pectoris, decreased blood pressure or pain in the chest area are observed sporadically;
• problems with the gastrointestinal tract: sometimes diarrhea or nausea develops. Vomiting, abdominal pain, dyspepsia or constipation are occasionally observed. Gingivitis of a hypertrophic nature occurs sporadically;
• endocrine disorders: gynecomastia appears occasionally;
• manifestations affecting the hematopoietic system: agranulocytosis or leukopenia may occur occasionally;
• lesions in the NS area: headaches are sometimes observed. Rarely, tremor, nervousness, dizziness or paresthesia develop;
• Respiratory system disorders: dyspnea is occasionally observed;
• problems with muscles and epidermis: occasionally urticaria, itching, myalgia or rashes develop;
• disorders associated with the sense organs: visual disturbances are occasionally noted;
• lesions of the urogenital tract: polyuria develops occasionally or urination becomes more frequent;
• changes in laboratory test values: occasionally, there is an increase in liver enzyme levels.

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Overdose

Manifestations of intoxication: arrhythmia, cough, convulsions, decreased blood pressure, bradycardia and increased diuresis, as well as renal failure, impaired consciousness and decreased EBV levels or acid-base values.

It is necessary to lay the victim horizontally, and then eliminate the drug from the body (taking sorbents, gastric lavage). Also, the balance of the BCC is replenished and the work of vital organs is monitored (with subsequent correction), and in addition, the indicators of urea potassium, creatinine in the blood are determined and hemodialysis is performed.

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Interactions with other drugs

The antihypertensive effect of the drug is potentiated when combined with other antihypertensive drugs (including β-blockers, diuretics and α-blockers, including prazolin).

Combinations of enalapril maleate and other drugs that require careful use.

Use with potassium-sparing diuretics, substances that increase plasma potassium levels (eg, heparin), and potassium supplements may increase plasma potassium levels, especially in people with kidney problems. When combined, plasma K levels should be monitored.

Combination with lithium drugs may lead to delayed lithium excretion, which increases the likelihood of toxic and adverse effects. With such combinations of drugs, plasma lithium levels should be closely monitored, which is why they are not prescribed together.

Use together with NSAIDs may weaken the antihypertensive effect of ACE inhibitors and further increase plasma potassium values with simultaneous weakening of renal function. In some individuals with kidney problems, such a combination may cause further deterioration of this pathology.

Enalapril may enhance the antidiabetic effect of oral hypoglycemic drugs, which is why blood sugar levels should be monitored.

Amifostine and baclofen potentiate the antihypertensive activity of the drug, therefore dosage adjustment and blood pressure monitoring are required.

Administration together with tricyclics or neuroleptics may provoke orthostatic collapse.

Use in combination with cytostatics, procainamide, allopurinol, as well as general GCS and immunosuppressants may cause leukopenia.

Combinations of nitrendipine and other drugs that require caution.

Nitrendipine can increase plasma digoxin levels, so when they are combined, these parameters should be monitored.

Nitrendipine potentiates the effectiveness and duration of action of muscle relaxants, including pancuronium bromide.

Grapefruit juice slows down the oxidation of the substance during metabolic processes, increasing its plasma level, which potentiates the antihypertensive effect of Eneas.

The processes of nitrendipine metabolism develop inside the liver and intestinal mucosa with the help of hemoprotein P450. Substances that stimulate the activity of this system (anticonvulsants - phenobarbital with phenytoin and carbamazepine), as well as rifampicin, can lead to a significant decrease in the bioavailability of nitrendipine. Medicines that inhibit the activity of the specified enzyme system (antimycotics - intraconazole, etc.) increase the plasma level of the substance.

Nitrendipine together with β-adrenergic receptor blockers have synergistic properties.

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Storage conditions

Eneas should be stored at temperatures between 15-25°C.

Shelf life

Eneas can be used within 36 months from the date of sale of the medicine.

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Application for children

There is no information regarding the safety of the drug in pediatrics, as well as its effectiveness, so it is not prescribed to children.

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Analogues

The analogs of the drug are Amapin, Enadipine, Gipril with Bi-prestarium, Enap combi, Bi-ramag and Ekvator with Rami-azomex.

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