Enap

Enap is an antihypertensive drug that contains an element of enalapril that inhibits ACE activity, as a result of which angiotensin-2 production is reduced.

[1], [2],

Indications Enap

It is used in the following conditions:

• primary hypertension;
• complex therapy for CHF;
• prevention of the development of heart failure expressed in people who have been diagnosed with left ventricular dysfunction without symptoms (a comprehensive treatment course);
• to reduce the incidence of  myocardial infarction ;
• to reduce the incidence of hospitalization in patients with unstable angina.

[3]

Release form

The release of drugs is sold in tablets with a different volume of active ingredient - 2.5, 5, and in addition 10 and 20 mg. Inside the cell packaging contains 10 such tablets. In the box - 2, 3 or 6 packs.

Pharmacodynamics

The enalapril component is a derivative of amino acids (such as L-proline and L-alanine). After applying the drug inside, the component hydrolyzes, turning into enalaprilat, which slows down the action of ACE. The activity of the component leads to a decrease in the production of angiotensin-2 from angiotensin-1. Due to the decrease in its plasma values, there is an increase in plasma renin activity and a decrease in aldosterone production.

Because ACE is similar to kininase-2, enalapril is able to block the destruction of bradykinin (peptide having vasopressor properties). It is not yet definitively determined to what therapeutic result the similar effect of enalapril leads.

The hypotensive effect of the component is based on the suppression of the activity of the RAAS, which is extremely important in the regulation of blood pressure values. But in individuals with increased blood pressure and low renin levels, the hypotensive effect of enalapril is also recorded.

The use of medication reduces the level of blood pressure, without taking into account the position in which the patient's body resides. Significant increase in heart rate is not observed.

Symptomatic orthostatic collapse develops only occasionally. In some cases, to get a pronounced decrease in blood pressure, you need to take the drug for several weeks. Abrupt cancellation Enap did not lead to an increase in blood pressure values.

In patients with primary hypertension, in the event of a decrease in blood pressure, there is a weakening of peripheral vascular resistance and an increase in cardiac output values. But a noticeable change in the level of heart rate is not recorded. The blood circulation inside the kidneys increases, and the filtration rate of the glomeruli does not change. But at the same time, this indicator increases in individuals with low filtration rates.

In people with nephropathy with a diabetic or nondiabetic nature, the use of enalapril resulted in a weakening of proteinuria or albuminuria and a decrease in renal excretion of IgG.

In patients treated with CHF, at the stage of therapy with SG and diuretic drugs, and with enalapril, there is a decrease in cardiac output or BPP and HR (usually in people with CHF, this figure is increased).

There is a decrease in capillary wedging inside the lungs. Prolonged use of the drug increases the tolerance of physical exertion and reduces the severity of symptoms of HF. In patients with moderate or mild CHF, the drug inhibits the progression of the disease and reduces the rate of development of left ventricular dilatation.

In patients with left ventricular dysfunction, drugs reduce the risk of symptoms of the most frequent ischemic outcomes (a decrease in the incidence of myocardial infarction along with the number of hospitalizations associated with angina).

[4], [5]

Pharmacokinetics

A pronounced retarding effect on ACE is usually recorded after 2-4 hours after oral administration of the drug. The hypotensive effect often develops after 60 minutes have passed since the oral intake of the substance, and Cmax values occur after 4-6 hours. The duration of influence is determined by the size of the therapeutic portion. When used as recommended by the doctor, the hypotensive and hemodynamic effect is maintained for at least 24 hours.

Accepted active element is rapidly absorbed, with a degree of absorption of approximately 60%. Peak blood parameters of a substance are noted after 60 minutes from the moment of administration; eating does not affect the degree of absorption. The drug is subjected to active hydrolysis, which is formed enalaprilat, slowing down the activity of APF. Values of Cmax enalaprilat are recorded after 3-4 hours from the time of ingestion. After a multiple dose, the half-life of enalapril is 11 hours.

Substance does not undergo significant transformation inside the body, except for transformation into enalaprilat.

Excretion occurs mostly through the kidneys. Inside urine, 40% enalaprilat is recorded, as well as 20% enalapril in an unchanged state.

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Dosing and administration

Use the medication should be inside, without reference to the reception of food. It is necessary to take drugs at the same time of the day, drinking a small amount of any liquid.

To reduce elevated blood pressure indicators, the drug is first prescribed in a serving of 5–20 mg, 1 time per day (a more accurate dosage amount is determined by the severity of the disorder). In the mild form of hypertension should be consumed daily for 5 or 10 mg of the substance.

In individuals with a pronounced increase in the activity of the RAAS, the blood pressure level may sharply decrease. In such cases, it is required to use small medicinal portions - 5 mg per day. Therapy is carried out under medical supervision.

Before using Enap, it should be borne in mind that in the case of previous therapy with diuretic drugs (in large portions), dehydration may develop and the likelihood of a drop in blood pressure may increase already at the beginning of the treatment course. You should take a maximum of 5 mg medication per day. It is necessary to stop the use of diuretic drugs for 2-34 days before using the medication. During therapy, you need to monitor the work of the kidneys and determine the blood parameters of potassium.

The size of the maintenance dosage is 20 mg, with a single dose per day. When needed, an increase in daily portion up to 40 mg is allowed. Dosing sizes are generally personalized.

During treatment of CHF or left ventricular dysfunction, you must first use 2.5 mg of the drug per day. In the treatment of heart failure, sometimes combined use is prescribed with hypertension, diuretic drugs, and β-blockers.

By adjusting the elevated values of blood pressure, the portion can be gradually increased - by 2.5-5 mg with 3-4-day intervals, until it is brought to a supporting level of 20 mg per day. The maximum allowable daily dosage is 40 mg.

Due to the fact that during therapy, the level of blood pressure can be greatly reduced and renal function deficiency develops, during the treatment cycle, it is necessary to closely monitor the work of the kidneys and pressure values. If the pressure drops sharply after taking the first batch, you do not need to cancel the medication.

Persons with kidney disease should increase the intervals between doses of drugs or reduce its dosage.

Elderly patients should take an initial dose of 1.25 mg, because they have slowed down the excretion of enalapril.

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Use Enap during pregnancy

It is forbidden to prescribe Enap during pregnancy, because there is a likelihood of teratogenic effects. When diagnosing pregnancy, it is necessary to immediately stop the use of drugs.

When using an ACE inhibitor in pregnant women, you should periodically undergo an ultrasound examination - to assess the performance of amniotic fluid. In addition, ultrasound of the kidneys and cranial bones of the fetus is performed.

The active component of Enapa is found inside the mother's milk, therefore for the period of therapy it is required to refuse breastfeeding.

Contraindications

Among the contraindications:

• the presence of patient intolerance regarding the component enalapril, and in addition other elements of the drug;
• a history of angioedema that appeared during therapy with an ACE inhibitor;
• Quincke's edema of idiopathic or hereditary nature;
• porphyria;
• use in combination with aliskiren in people with renal disease or diabetes mellitus;
• malabsorption of glucose-galactose, hypolactasia and lactase deficiency (because the drug contains lactose).

With caution, the drug is used in such cases:

• stenosis associated with arteries within the kidneys;
• gingivitis;
• people who have had a kidney transplant;
• Conn's syndrome;
• lower BCC values;
• obstructive cardiomyopathy of hypertrophic type;
• stenosis of the aortic or mitral valve;
• diabetes;
• IBS;
• general lesions of connective tissue;
• suppression of hematopoietic processes;
• cerebrovascular pathology;
• renal failure.

Caution is also required when used in individuals who follow a dietary regime with reduced consumption of salt, and in addition, people who use immunosuppressants or diuretic drugs, and those who undergo hemodialysis.

Persons over the age of 65 should consult a doctor before taking the drug.

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Side effects Enap

Therapy may be accompanied by the development of the following side effects:

• disorders of hematopoietic processes: thrombocyte, neutro or pancytopenia, anemia, and in addition, agranulocytosis, lymphadenopathy, autoimmune diseases, decrease in hemoglobin values with hematocrit and suppression of blood formation;
• metabolic disorders: hypoglycemia;
• problems with the work of NA: headaches, paresthesias, vertigo, depression, insomnia, disorders of consciousness, a feeling of strong excitability or drowsiness and sleep disorders;
• lesions affecting the function of the cardiovascular system: a sharp drop in blood pressure, dizziness, angina, pain in the sternum, heart rhythm disorder, myocardial infarction or stroke, palpitations and Raynaud's disease;
• signs associated with the senses: ear noise, change in taste and visual impairment;
• disorders of the digestive processes: nausea, pain in the abdominal area, constipation, vomiting, bloating, diarrhea, intestinal blockage, and in addition dyspepsia, pancreatitis, dry oral mucosa and anorexia. In addition, stomatitis, peptic ulcers, glossitis, disorder in the liver and biliary excretion, as well as aphthous ulcers, liver necrosis, hepatitis and cholestasis;
• problems with respiratory activity: pain in the throat, dyspnea, cough, hoarseness, bronchial spasm, rhinorrhea, rhinitis, eosinophilic pneumonia of an alveolitis and allergic nature;
• epidermis lesions: angioedema, pruritus, intolerance symptoms, rashes, hyperhidrosis, urticaria, erythroderma, and in addition alopecia, erythema polyforma, pemphigus, PET, and exfoliative form of dermatitis;
• disorders of the urogenital system: proteinuria, oliguria, renal failure, gynecomastia, renal impairment and impotence;
• ODA dysfunction: muscle cramps;
• indications of laboratory tests: hyponatremia or hyperkalemia, increased serum values of creatinine, blood levels of urea, activity of liver enzymes, as well as blood levels of bilirubin;
• other symptoms: myalgia, Parkhon's syndrome, leukocytosis, fever, vasculitis, and in addition, myositis, serositis, increased ESR, arthritis and signs of photosensitivity.

Overdose

With intoxication after about 6 hours there is a strong drop in blood pressure values. The development of collapse and disorder of EBV indicators are possible, and besides this there is a lack of kidney function, hyperventilation, convulsions, bradycardia with a strong heartbeat, tachycardia and dizziness.

In case of an overdose, it is required to position the victim horizontally so that the head is at the level of the body. For mild poisoning, gastric lavage is performed and activated charcoal is given to the patient. For severe disorders, 0.9% NaCl is injected intravenously, and in addition, catecholamines or plasma substitutes can be used in / in.

Enalaprilat can be excreted through hemodialysis at a rate of 62 ml / minute.

A pacemaker is installed for people with bradycardia. In case of poisoning, it is necessary to carefully monitor the electrolyte values inside the serum and creatinine values.

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Interactions with other drugs

In the case of a double blockade of the RAAS activity (when combining ACE inhibitors with angiotensin-2 end antagonists or aliskiren), the probability of a decrease in blood pressure level increases. If such a combination of drugs is necessary, it is necessary to closely monitor the values of EBV, renal function and blood pressure indicators.

You can not combine the drug with aliskiren people with kidney disease or diabetics.

ACE inhibitors reduce the loss of potassium under the influence of diuretic drugs. The use of enalapril together with potassium-containing substitutes or potassium-sparing type diuretics can lead to hyperkalemia. With this combination, you need to track the values of potassium inside the serum.

After previous treatment with the administration of diuretic drugs, the volume of the BCC may decrease and the risk of a decrease in the blood pressure level when using enalapril may increase. This effect can be weakened by abolishing the use of diuretics, increasing the daily amount of taken salt and water, as well as reducing the amount of enalapril.

Combining Enap with methyldopa, nitroglycerin, α-, as well as β-blockers, ganglioblokiruyuschimi drugs, BKK or other nitrates can further reduce the level of blood pressure.

Use with lithium products leads to a temporary increase in the level of lithium, and in addition to lithium poisoning. The introduction of a diuretic thiazide character can increase the values of lithium inside the serum. It is better not to use such combinations, and when you need such a combination, it is important to carefully monitor the lithium values inside the serum.

The introduction of drugs with some anesthetics, antipsychotics or tricyclics can further reduce the values of blood pressure.

Combined use with NSAIDs may weaken the antihypertensive activity of the drug. Possible weakening of the renal activity (especially in individuals with pathologies of the kidneys). Such an effect is curable.

Combined use with insulin and antidiabetic drugs can activate antidiabetic activity and increase the likelihood of hypoglycemia.

Enapa's antihypertensive properties are potentiated by using ethyl alcohol.

Sympathomimetics reduce the hypotensive activity of an ACE inhibitor.

Enalapril reduces the effects of medications containing theophylline component.

The introduction of cytostatics, immunosuppressants or allopurinol together with the drug increases the risk of leukopenia. In individuals with disorders of renal activity, the use of ACE inhibitors with allopurinol increases the likelihood of allergies.

Cyclosporine increases the risk of hyperkalemia.

The level of bioavailability of ACE inhibitors decreases with the introduction of antacids.

[10], [11], [12]

Storage conditions

Enap must be kept in a place closed to small children. Temperature marks - not more than 25 ° C.

Shelf life

Enap can be used within a 36-month period from the moment of manufacture of a drug.

Application for children

The drug is not used in pediatrics (up to 18 years of age).

[13], [14],

Analogs

Analogues of the therapeutic element are drugs Renipril, Enap R, Ednit and Bagopril with Invoril, and besides Berlipril, Enalapril with Vasolapril and so on.

[15]

Reviews

Enap receives mostly positive reviews from physicians. It is believed that with proper use of the drug, the patient's quality of life is significantly improved. But keep in mind that the drug often causes the appearance of side effects. In the comments of patients often noted the development of dry-type cough and so on. It is required to remember that if the condition begins to worsen, you should immediately consult a doctor to change the dose of medication or prescribe a different medication.