Eneas

Eneas is a complex drug that lowers blood pressure.

The drug contains a component of enalapril, which is an ACE inhibitor, and has an impact by suppressing the activity of the RAAS. The drug prevents the transformation of angiotensin-1 into the angiotensin-2 vasodilating peptide, which allows you to get rid of its stimulating effect on the adrenal glands, as well as on the secretion of aldosterone.

In addition, the drug 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 vessel membranes.

[1]

Indications Eneas

It is used for high blood pressure indicators, as an integral component of complex treatment.

[2], [3]

Release form

The release of drugs produced in tablets - 10 pieces inside the cellular packaging. In a pack - 3 such packages.

Pharmacodynamics

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

Prolonged use of enalapril in people with essential hypertension and kidney failure may improve renal activity by increasing the rate of CF.

Nitrendipine is a 1,4-dihydropyridine derivative. It lowers calcium inside the cells, resulting in reduced contractility of the vascular muscles; due to the expansion of peripheral arteries, systemic peripheral resistance is weakened, and an excessively increased blood pressure level is also reduced.

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

[4], [5], [6], [7],

Pharmacokinetics

Enalapril is absorbed at high speed inside the gastrointestinal tract, and the presence of food does not affect its absorption. Inside the serum, Cmax values are noted after the 1st hour.

Intlasma protein synthesis is 50-60%. After absorption, the component is hydrolyzed at high speed to form enalaprilat. It reaches the values of serum Cmax after 3-4 hours from the moment of taking the medicine inside.

Excretion is done mostly through the kidneys (unchanged, as well as enalaprilat (40%)). In addition to the transformation into enalaprilat, there are no other noticeable manifestations of metabolic transformations of the substance. Enalaprilat inside blood serum has a prolonged terminal stage associated with ACE synthesis processes.

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

The effective half-term of cumulation of enalaprilat with multiple administration of the drug inside is 11 hours. The level of hydrolysis and absorption of enalapril is identical with the introduction of portions from the recommended dosing spectrum.

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

The level of bioavailability is in the range of 20-30%. Synthesis of the component with intraplasma protein is 96-98%.

Almost all nitrendipine undergoes intrahepatic metabolism through oxidative processes.

The term half-life is in the range of 8-12 hours. Cumulation of the active element and its metabolic components was not observed.

People with problems in the liver of a chronic nature increase the plasma levels of nitrendipine.

The excretion of an element is mostly realized through the kidneys in the form of non-active metabolic components (approximately 77%), as well as through the biliary tract.

[8], [9], [10], [11]

Dosing and administration

Eneas should be taken orally (at the same time, it is recommended to do it in the morning). The use of drugs is not tied to a meal. Usually for the day, take the first tablet of the drug.

[14]

Use Eneas during pregnancy

Eneas can not be used during breastfeeding or pregnancy, as well as at the planning stage of conception.

Contraindications

The main contraindications:

• severe sensitivity or allergy associated with active elements or auxiliary components of drugs;
• unstable hemodynamics (especially after the transfer of a shock condition, stroke, AHF or coronary in the active phase);
• porphyria;
• Quincke edema associated with the use of an ACE inhibitor in history;
• renal transplantation;
• bilateral stenosis affecting both renal arteries, or stenosis affecting the arteries of a single kidney;
• hypertrophic cardiomyopathy;
• Conn's syndrome;
• lack of hepatic function in severe;
• anuria or renal pathology in the chronic phase (4-5 stage).

Caution is needed when prescribing in such situations:

• diabetes;
• CHF;
• elderly people;
• lower bcc rates;
• severe aortic stenosis or stenosis affecting the subaortic region, and having a hypertrophic idiopathic form and obstructive nature;
• cerebrovascular diseases and ischemic heart disease;
• periods after renal transplantation.

[12]

Side effects Eneas

Enalapril.

Main adverse events:

• damage to the CVS function: sometimes there is an orthostatic collapse or a decrease in blood pressure indicators with such signs as weakness, visual disturbance and dizziness. Occasionally, syncope is noted (especially at the initial stage of therapy, in the case of increased portions of enalapril maleate or diuretic in patients with EBV disorders, as well as HF or elevated renal blood pressure). Singly due to a sharp drop in blood pressure is observed palpitation, angina, tachycardia, pain retrosternal area, arrhythmia, stroke, pulmonary edema, and in addition to bradycardia, myocardial infarction, atrial fibrillation, cerebral circulation disorder, transitory disorder of blood flow inside the brain, pulmonary infarction and pulmonary embolism;
• disorders associated with the urethra and kidneys: sometimes there are disorders in the work of the kidneys or their exacerbation, and also develops a lack of renal function. Occasionally there is proteinuria or oliguria, and people with disorders of renal activity may develop pain in the lumbar region. FPN is observed sporadically;
• problems with respiratory activity: often marked dyspnea. Sometimes there are wheezing, pain in the throat, rhinorrhea, dry-type cough or bronchitis. Occasionally, a runny nose, sinusitis, eosinophilic pneumonia, or an allergic alveolitis occurs. There is a single case of stomatitis, pneumonia, asthma or bronchial spasm, infiltration in the lung area, dry oral mucosa, glossitis and angioedema in the pharyngeal zone with larynx or tongue (sometimes this can cause obstruction of the respiratory ducts, and the main risk group in this case are representatives of the race Negroids);
• disorders of the liver and gastrointestinal tract: sometimes there is pain in the upper abdominal region, peptic ulcer, gastric irritation, nausea, and digestive disorders. Occasionally diarrhea, loss of appetite, obstipation or vomiting. Hepatitis (cholestatic or hepatocellular varieties), intestinal angioedema, problems with liver function, insufficiency of its function, cholestasis (with jaundice), necrosis, stomatitis, intestinal blockage, pancreatitis and glossitis;
• lesions of endocrine function: gynecomastia appears singly. Perhaps the development of the syndrome disorders of the allocation of ADH;
• problems associated with the work of the National Assembly: drowsiness, headaches, fatigue and insomnia are sometimes noted. Depression, imbalance or sleep disturbance, dizziness, polyneuropathy with paresthesia, impotence, and also nervousness, cramps, muscle injuries, abnormal dreams and confusion;
• symptoms associated with the epidermis and vessels: often rash appears. Sometimes there are signs of allergies. Occasionally, urticaria, itching, Erythroderma, or Quincke’s edema develop, affecting the tongue, limbs, lips with the face, larynx, or glottis. Epidermal reactions of a severe nature (SJS, pemphigus, exfoliative dermatitis, TEN and erythema multiforme), hyperhidrosis, photosensitivity, Raynaud's syndrome, alopecia and onycholysis develop individually. Skin fever can be observed on the background of myositis or myalgia, arthritis or arthralgia, serositis, vasculitis, leukocytosis, eosinophilia, and in addition to this increase in erythrocyte sedimentation rate and a positive sample for the presence of antinuclear antibodies;
• metabolic disorders: sometimes there is hypoglycemia;
• disorders associated with the senses: occasionally there is a visual impairment, ear ringing, loss of smell, a change or a short loss of taste, tearing or eye dryness;
• systemic disorders: asthenia usually occurs. Sometimes tides appear;
• changes in test results: sometimes there is a decrease in hematocrit or hemoglobin, or platelet count with leukocytes.

Nitrendipin.

Among the side effects are:

• systemic lesions: flu-like manifestations or asthenia are sometimes observed;
• Dysfunction of the cardiovascular system: sometimes cardiac palpitation, hyperemia, arrhythmia, peripheral edema, tachycardia or vasodilation occur. A single case of angina, a decrease in blood pressure or pain in the retrosternal zone;
• problems with the work of the digestive tract: sometimes develop diarrhea or nausea. Occasionally, there is vomiting, pain in the abdominal area, dyspepsia, or constipation. A single occurrence of gingivitis, which is hypertrophic;
• endocrine disorders: gynecomastia appears singly;
• manifestations affecting the hematopoietic system: Agranulocytosis or leukopenia may occur singly;
• lesions in the NA: sometimes there are headaches. Occasionally, tremor, nervousness, dizziness, or paresthesia develop;
• disorders associated with the respiratory system: dyspnea is rarely observed;
• problems with muscles and the epidermis: occasionally develop urticaria, itching, myalgia or rash;
• disorders associated with the senses: rarely noted visual impairment;
• lesions of the urogenital tract: polyuria rarely develops, or urination becomes more frequent;
• Changes in laboratory test values: an increase in liver enzymes is rare.

[13],

Overdose

Manifestations of intoxication: arrhythmia, cough, convulsions, decrease in blood pressure, bradycardia and potentiation of diuresis, and in addition, failure of renal function, disorder of consciousness and EBV level or acid-base values.

It is necessary to lay the victim horizontally, and then eliminate the drug from the body (reception of sorbents, gastric lavage). Also, the BCC balance is replenished and the work of the organs important for life is monitored (with subsequent correction), and besides, the indices of potassium urea and creatinine inside the blood are determined and hemodialysis is performed.

[15], [16], [17], [18], [19]

Interactions with other drugs

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

Combinations of enalapril maleate and other drugs requiring careful use.

Use with diuretic potassium-sparing forms, substances that increase the plasma values of potassium (for example, heparin), and potassium supplements can increase the plasma level of potassium, especially in people with kidney problems. In the case of their combination, you need to track the K level inside the blood plasma.

The combination with lithium drugs can lead to a delay in the excretion of lithium, which increases the likelihood of developing toxic and adverse symptoms. With such combinations of medicines, it is necessary to closely monitor the plasma indicators of lithium, because of what they are not prescribed together.

Using together with NSAIDs can weaken the anti-hypertensive effect of ACE inhibitors and further increase the plasma values of potassium with a simultaneous weakening of the renal activity. For individuals with kidney problems, this combination may cause further deterioration of this pathology.

Enalapril is able to enhance the antidiabetic effect of hypoglycemic drugs taken orally, which is why blood sugar values should be monitored.

Amifostine with baclofen potentiate the antihypertensive activity of drugs, therefore, dosage adjustment and control of blood pressure levels is required.

Introduction together with tricyclics or neuroleptics can provoke orthostatic collapse.

Use in conjunction with cytostatics, procainamide, allopurinol, as well as common GCS and immunosuppressants can cause leukopenia.

Combinations of nitrendipine and other drugs that require caution.

Nitrendipin is able to increase the plasma values of digoxin, so when combined, these indicators should be monitored.

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

Grapefruit juice slows down the oxidation of a substance during metabolic processes, increasing its plasma level, which is why the anti-hypertensive effect of Eneas is potentiated.

The metabolism of nitrendipine develops within the hepatic and intestinal mucosa with the help of the 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. Drugs that inhibit the activity of this enzyme system (antimycotics - intraconazole, etc.) increase the plasma level of the substance.

Nitrendipine, together with β-adrenoreceptor blockers, have synergistic properties.

[20], [21],

Storage conditions

Eneas must be maintained at a temperature in the range of 15-25 ° C.

Shelf life

Eneas can be used within a 36-month period from the date of sale of the drug.

[22], [23]

Application for children

There is no information about the safety of the use of drugs in pediatrics, as well as its effectiveness, so children do not prescribe it.

[24]

Analogs

Analogues of drugs are the substances Amapine, Enadipine, Gipril with Bi-prestirium, Enap Combi, Bi-Ramagus and the Equator with Rami-azomex.

[25], [26], [27]