ЭNAP P
Active material: Enalapril
When ATH: C09AA02
CCF: ACE inhibitor
ICD-10 codes (testimony): I10, I67.4
When CSF: 01.04.01.03
Manufacturer: KRKA d.d. (Slovenia)
Pharmaceutical form, composition and packaging
Solution for / in the clear, colorless.
| 1 ml | |
| Enalaprilat | 1.25 mg |
Excipients: benzyl alcohol, sodium chloride, Sodium hydroxide, water d / and.
1 ml – ampoule (5) – blisters (1) – packs cardboard.
Pharmacological action
ACE inhibitor. Enalaprilat, of the drug Enap® P, is a metabolite of enalapril. Reduces the formation of angiotensin II from angiotensin I, reduces the concentration of aldosterone in blood, increases the release of Renin, It stimulates the release of prostaglandins and endotelialnogo relaksirutego factor veins, inhibits sympathetic nervous system. Reduces PR, FROM, before- and the postnagruzku miocard, widens the arteries in a greater degree, than veins.
Antigipertenzivny effect is more pronounced at high plasma Renin level, than the normal or reduced its level. Reduction of blood pressure is not within a therapeutic effect on cerebral blood flow. It improves blood flow to ischemic myocardium.
Therapeutic effect after in/in the introduction is a 5-15 m, reaches through 1-4 no, is about 6 no.
Pharmacokinetics
Absorption and distribution
Ènalaprilat poorly absorbed after administration inwards and almost inactive, Therefore, it is injected only/in. Cmax After the on/in the introduction is achieved through 15 m.
Binding to plasma proteins is 50-60%. Circulates in the blood in an unmodified form. Poor penetrate the BBB.
Metabolism and excretion
Not metabolizmu. T1/2 is 4 no. Excreted unaltered, more 90% – urine. Clearance englaprilata in hemodialysis – 38-62 ml / min, englaprilata concentration in the serum after 4-hour hemodialysis is reduced by 45-75%.
Testimony
-hypertonic Kriz;
-arterial hypertension in cases, When taking the drug inside is impossible;
-hypertensive encephalopathy.
Dosage regimen
Enap® R injected in a dose 1.25 mg (1 ml) every 6 no, including patients, taking enalapril earlier inside. Treatment is carried out only in a hospital environment. The drug is injected in/in struino slowly (during 5 m) or drip in the breeding in 20-50 ml 5% dextrose (Glucose) or 0.9% sodium chloride solution.
If after 1 h after the introduction of the therapeutic effect of unsatisfactory, the drug dose 1.25 mg (1 ml) can be repeated again, and after 6 h continue treatment as usual (1.25 mg every 6 no).
Patients, taking diuretics, the initial dose of the drug is reduced to 0.625 mg (0.5 ml). If after 1 h after the introduction of the therapeutic effect of unsatisfactory, the same dose can be entered again, and then 6 h continue treatment full dose (1.25 mg every 6 no).
At chronic renal failure mild when QC > 30 ml / min (serum creatinine does not exceed 265.2 mmol / l) dose Ènapa® R is 1.25 mg (1 ml) every 6 no, that is, no dose adjustment is required. At CC < 30 ml / min (serum creatinine is greater than 265.2 mmol / l) starting dose is 0.625 mg (0.5 ml) with subsequent monitoring during 1 h to identify excessive loss AD. In the absence of effect in 1 no, dose 0.625 mg repeated and treatment continues in the dose 1.25 mg every 6 no. To patients, hemodialysis, dose Ènapa® R is 0.625 mg (0.5 ml) every 6 h for 48 no.
When switching to ingesting the recommended initial dose of enalapril is 5 mg/day for patients, previously injected Enap® R/in the dose 1.25 mg / ml. The dose for the intake can be increased.
Patient, which Enap® R injected in/in a dose of 0.625 mg, the recommended dose of the drug when you switch on reception inside is 2.5 mg / day.
Side effect
Cardio-vascular system: excessive reduction of blood pressure, Orthostatic hypotension, angina, myocardial infarction (usually associated with excessive decline ad), heartbeat, Arrhythmia (predserdnaya beards- or tachycardia, auricular fibrillation), acute left ventricular failure, embolism of pulmonary arteries, cerebrovascular disorders.
From the central and peripheral nervous system: dizziness, headache, weakness, fatiguability, asthenia, drowsiness, insomnia, anxiety, depression, confusion, paresthesia, noise in ears.
From the digestive system: nausea, vomiting, diarrhea or constipation, abdominal pain, ileus, decreased appetite, stomatitis, glossitis, transient increase in liver transaminases.
The respiratory system: nonproductive cough, breathlessness, rhinorrhea, pharyngitis, disfonija.
From the water-electrolyte balance: hyperkalemia, giponatriemiya.
From the hematopoietic system: anemia, neutropenia, thrombocytopenia, agranulocytosis, decrease in hematocrit, increased erythrocyte sedimentation rate.
From the urinary system: proteinuria, impairment of renal function, tranzithornoe increase in serum creatinine and urea.
Allergic reactions: skin rash, angioneurotic edema of the face, limbs, lips, language, glottis and / or larynx, exfoliative dermatitis, erythema multiforme, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), pemphigus (pemphigus), itch, hives, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis, eozinofilija.
Other: alopecia, decreased libido.
Contraindications
- Angioedema, (incl. in history and in the treatment of ACE inhibitors);
- Porphyria;
— a kidney dialysis, using polyacrylonitrile membranes, Apheresis on dextran sulphate;
— immediately before the desensitization of Hornet's or bee venom;
- Pregnancy (especially II and III trimester);
- Lactation;
- Childhood and adolescence up 18 years;
- Hypersensitivity to the drug.
FROM caution assign the primary giperaldosteronizme, aortic stenosis, mitral stenosis, bilateral renal artery stenosis, stenosis of the artery to a solitary kidney, hyperkalemia, condition after kidney transplantation, systemic connective tissue diseases, cerebrovascular diseases, diabetes, chronic heart failure, hypertrophic obstructive cardiomyopathy, mielosupression (leukopenia, thrombocytopenia), CHD, renal failure (proteinuria more 1 g / day), giponatriemii, and patients, observing diet with restriction of table salt or in gemodialise, elderly patients (more 65 years).
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation.
For newborns or babies, who were in utero effects of ACE inhibitors, It is recommended to monitor for the timely identification of expressed AD decline, oligurii, giperkaliemii and neurological disorders, possible due to reduced renal and cerebral blood flow at lower HELL, called ACE inhibitors. If oliguria need to maintain blood pressure and renal perfusion through the introduction of appropriate fluids and vasoconstrictor.
Cautions
Arterial gipotenzia may occur (even a few hours after the first dose) in patients with chronic heart failure and hyponatremia, as well as in patients with renal failure and in patients with arterial hypertension, especially against the background of hypovolemia as a result of treatment dioretikami, salt-free diet, diarrhea, vomiting or hemodialysis.
Treatment of patients with an increased risk of hypotension after the first dose should be started with half a dose of enalaprilat (0.625 mg). If hypotension the patient should be given a horizontal position with a low headboard and, if necessary, adjust the volume of the plasma by infusion 0.9% sodium chloride. Hypotension and its consequences are rare and are transient in nature. Transient hypotension is not a contraindication to further treatment Enap® P. After correction of HELL and BCC patients usually tolerate well the subsequent introduction of the drug. In the case of symptomatic arterial hypotension should reduce the dose or stop treatment Ènapom® P.
Ènapom treatment should be avoided® R patients with stenosis bilateral renal artery or artery only kidneys, Since this may cause deterioration in kidney function and even acute kidney failure, that usually has a reversible.
Since the treatment Ènapom® R may increase potassium in serum, especially in patients with chronic renal failure, the simultaneous appointment Ènapa® R and kalisberegath dioretikov, such as spironolactone, amiloride and triamterene, not recommended.
With a history of angioneuroticeski pain (not even associated with the acquisition of ACE inhibitors) There is an increased risk of re-development in the face of treatment Ènapom® P.
Before surgical interventions (including dentistry) must notify the surgeon / anesthesiologist on the use of ACE inhibitors.
Enap® R can be used in conjunction with drugs naperstanki, beta-blockers, methyldopa, nitratami, blockers of slow calcium channels, Hydralazine and prazosinem.
Overdose
Symptoms: excessive reduction of blood pressure until the development of collapse, myocardial infarction, acute stroke and thromboembolic complications, convulsions, stupor.
Treatment: ingesting salt solution, epinephrine (n / a or I /), antihistamines, GCS (I /), in/in the introduction plazmozamenitelei, angiotensin II, hemodialysis (introduction rate – 62 ml / min).
Drug Interactions
The simultaneous use of Enap® R with dioretikami, other hypotensive means, opioid analgesics, funds for general anesthesia increases the risk of arterial hypotension.
With simultaneous use of NSAIDs, Estrogens, adrenostimulyatorov, drugs, aktiviruyushtie renin-angiotensin-alydosteronovuyu sistemu, acceptance of common salt in excess, ethanol weaken gipotenzivny effect drug.
Drugs potassium, potassium-sparing diuretics (spironolactone, amilorid, triamterene), ciclosporin together with the application Ènapom® R increase the risk giperkaliemii.
The simultaneous appointment Ènapa® R and drugs lithium can cause reversible lithium intoxication, which takes place after the termination of the use of both drugs.
Ènalaprilat enhances gipoglikemiceski effect derived sulfonylureas, insulin.
In an application Enap® R with allopurinolom, cytotoxic funds, immunosuppressants, prokainamidom increases the risk of neutropenia and/or agranulozitoza.
Conditions of supply of pharmacies
The drug is released under the prescription. Applies only in the hospital.
Conditions and terms
List B. The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.
