Universal reference book for medicines
Name of the preparation: EHRANTIL ® (EBRANTIL ® )

Active substance: urapidil

Type: Alpha 1- blocker

Manufacturer: TAKEDA (Germany) manufactured by TAKEDA (Germany) manufactured by TAKEDA AUSTRIA (Austria)
Composition, form of production and packaging

The solution for intravenous administration is clear, colorless.

1 ml of 1 amp.

urapidil hydrochloride 5.47 mg 27.35 mg,

which corresponds to the content of urapidil 5 mg 25 mg

Excipients: propylene glycol - 100 mg, sodium hydrogen phosphate dihydrate - 0.42 mg, sodium dihydrogen phosphate dihydrate - 2.22 mg, water d / and - up to 1 ml.

5 ml - ampoules (5) - packings contour mesh plastic (1) - packs cardboard.

The solution for intravenous administration is clear, colorless.

1 ml of 1 amp.

urapidil hydrochloride 5.47 mg 54.7 mg,

which corresponds to the content of urapidil 5 mg 50 mg

Excipients: propylene glycol - 100 mg, sodium hydrogen phosphate dihydrate - 0.42 mg, sodium dihydrogen phosphate dihydrate - 2.22 mg, water d / and - up to 1 ml.

10 ml - ampoules (5) - packings contour mesh plastic (1) - packs cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2017.

PHARMACHOLOGIC EFFECT

Alpha 1- adrenoblocker.
Ebrantil ® refers to drugs that block postsynaptic? 1- adrenoreceptors, thereby reducing the peripheral resistance. In addition, Egrantil ®regulates the central mechanism of maintaining vascular tone and has a weak beta-adrenergic blocking effect. Heart rate, cardiac output when it is administered does not change. Low cardiac output may be increased by decreasing vascular resistance. Orthostatic phenomena, as a rule, Ebrantil ® does not cause. Ebrantil ® blocks vasoconstriction, caused? 2- adrenoreceptors, and does not cause reflex tachycardia due to vasodilation.
Ebrantil ® balances systolic and diastolic blood pressure, reducing peripheral resistance and does not cause reflex tachycardia.

Urapidil reduces pre- and postnagruzku on the heart, increases the efficiency of cardiac contraction, thus, in the absence of arrhythmia, the drug increases the reduced minute volume of the heart.

Mechanism of action

Ebrantil ® has a central and peripheral mechanism of action.
Primarily blocks peripheral postsynaptic? 1- adrenoreceptors, thus, the drug blocks the vasoconstrictive effect of catecholamines. In the central nervous system, urapidil affects the activity of the vasomotor center, which is manifested in preventing reflex increase (or decrease) in the tone of the sympathetic nervous system.
Urapidil does not affect the parameters of carbohydrate metabolism, the exchange of uric acid and does not cause fluid retention in the body.

PHARMACOKINETICS

Distribution

After intravenous administration of 25 mg of urapidil, a two-phase decrease in drug concentration is observed: first, a rapid decrease in the (? -phase), and then a slow (? -phase).

The period of distribution of the drug is about 35 minutes.
V d - 0.8 l / kg (0.6-1.2 l / kg).
Binding to blood plasma proteins - 80%.
The relatively low degree of binding to blood plasma proteins explains that it is not known the possible interaction of urapidil with drugs strongly binding to plasma proteins.
Urapidil penetrates through blood-brain and placental barriers.

Metabolism

Most of the urapidil is metabolized in the liver.
The main metabolite is the hydroxylated derivative in the 4-position of the benzene ring, which has practically no antihypertensive activity.
O-demethylated metabolite is formed in very small amounts and almost as active as urapidil.

Excretion

50-70% of urapidil and its metabolites (15% in the form of an active drug) is excreted by the kidneys, the rest is excreted through the intestines in the form of metabolites (mainly in the form of inactive n-hydroxylated urapidil).

T 1/2 after IV bolus is 2.7 hours (1.8-3.9 hours).

Pharmacokinetics in special clinical cases

In elderly patients, as well as in patients with severe hepatic and / or renal insufficiency, V d and clearance of urapidil are reduced, and T 1/2 is increased.

INDICATIONS

- hypertensive crisis;

- refractory arterial hypertension;

- severe degree of arterial hypertension;

- controlled arterial hypotension during and / or after a surgical operation.

DOSING MODE

Ebrantil ® is administered intravenously or by long-term infusion (the patient should be lying down).

With hypertensive crisis, severe degree of hypertension, refractory hypertension, the drug
administered at a dose of 10-50 mg IV slowly under the control of blood pressure. Reduction of blood pressure is expected within 5 minutes after administration. Depending on the therapeutic effect, the repeated administration of the drug Egrantil ® is possible.
In / in drip or continuous infusion is carried out using a perfusion pump.
The maintenance dose is an average of 9 mg / h, i.e. 250 mg of Ebrantil ® (10 amp 5 ml or 5 amp 10 ml) in 500 ml of the infusion solution (1 mg = 44 drops = 2.2 ml). The maximum allowable ratio is 4 mg of Egrantil ® per ml of solution for infusion. The recommended maximum initial speed is 2 mg / min. The rate of drip administration depends on the indices of the patient's blood pressure.
A drip infusion solution for maintaining blood pressure is prepared as follows: 250 mg of the preparation (10 ampoules of 5 ml or 5 ampules of 10 ml) are added to 500 ml of the infusion solution, for example saline, 5% or 10% dextrose solution (glucose).

If a perfusion pump is used to administer the maintenance dose, 100 mg of the drug (4 ampoules of 5 ml or 2 10 ml ampoules) are injected into the syringe of the perfusion pump and diluted to 50 ml with saline, 5% or 10% dextrose (glucose) solution.

For controlled (controlled) reduction of blood pressure during its increase during and / or after surgery , Ehrnantil ® is administered iv in a dose of 25 mg.
Reduction of blood pressure is expected within 2 minutes after administration. Then, stabilize the blood pressure with infusion (the initial dose of up to 6 mg in 1-2 minutes, then reduce the dose).
If this does not happen, i. E.
BP does not change, then after 2 minutes, repeat intravenous injection of the drug Egrantil ® in a dose of 25 mg. Reduction of blood pressure is expected within 2 minutes after administration. Then, stabilize the blood pressure with infusion (the initial dose of up to 6 mg in 1-2 minutes, then reduce the dose).
If this does not happen, i. E.
BP does not change, then after 2 minutes a slow intravenous injection of the drug Ehrantil® at a dose of 50 mg is performed. Blood pressure decreases after 2 minutes. Then, stabilize the blood pressure with infusion (the initial dose of up to 6 mg in 1-2 minutes, then reduce the dose).
Continuous infusion using a perfusion pump or drip infusion is used to maintain blood pressure at the level achieved by IV.

If other antihypertensives have previously been used, then Egrantil ® can be administered only after a period of time sufficient to effect the previously administered drug (s).
The dose of Egrantil ® should be adjusted accordingly.
Care should be taken when using antihypertensive drugs in elderly patients .
The initial dose should be reduced compared to the recommended one, since the sensitivity in elderly patients to drugs of this series is often changed (V d is reduced, and T 1/2 is increased).
The administration of the drug can be single or multiple.
Injection administration of the drug can be combined with subsequent drip infusion. Parenteral therapy can be repeated with a new increase in blood pressure.
SIDE EFFECT

Most of the following side effects are caused by a sharp decrease in blood pressure, but clinical experience shows that they disappear within a few minutes, even after drip infusion of the drug Ebrantil ® .
Severe side effects may require discontinuation of treatment.
Determination of the frequency of adverse events according to WHO: very often (> 10%), often (? 1% and <10%), infrequently (? 0.1% and <1%), rarely (≥0.01% and <0.1%), very rarely (<0.01%), the frequency is unknown (the frequency can not be determined from the available data).

From the side of the psyche: very rarely - an excited state (a feeling of anxiety).

From the nervous system: often - dizziness, headache.

From the side of the cardiovascular system: infrequent - palpitations, tachycardia, bradycardia, a feeling of constriction or pain in the chest (complaints of an anginous nature), dyspnea, arrhythmia, a decrease in blood pressure when the position of the body changes, for example, when going to a vertical position from the prone position orthostatic hypotension).

From the respiratory system: rarely - nasal congestion.

From the digestive system: often - nausea;
infrequently - vomiting.
From the skin and subcutaneous tissues: infrequently - increased sweating.

Allergic reactions: rarely - skin itching, redness of the skin, exanthema;
unknown - angioedema, urticaria.
From the urinary system: often - proteinuria;
rarely - nephropathy, nephrotic syndrome.
From the side of the reproductive system: rarely - priapism.

General reactions: infrequent - increased fatigue.

From the laboratory: very rarely - thrombocytopenia *.

* Very rarely there was a decrease in the number of platelets during the administration of urapidil.
However, it was impossible to establish any causal relationship with therapy with the drug Ebrantil ® , for example, through immunohematological studies.
CONTRAINDICATIONS

- aortic stenosis;

- open the bottles of the duct;

- arteriovenous fistula (with the exception of the hemodynamically inactive dialysis shunt);

- age under 18 years (effectiveness and safety not established);

- lactation period (efficacy and safety not established);

- Hypersensitivity to the drug.

Carefully:

- elderly age;

- impaired liver and / or kidney function;

- hypovolemia;

- in patients with heart failure, which is caused by a violation of the mechanical function (for example, stenosis of the aortic or mitral valve), with pulmonary embolism or cardiac disorders due to pericardial diseases;

- simultaneous application with cimetidine;

- concomitant use with ACE inhibitors (concurrent clinical data with urapidil are limited).

PREGNANCY AND LACTATION

Egrantil ® solution for intravenous administration is not recommended for use in pregnancy due to the fact that urapidil penetrates the placental barrier, except when the potential benefit to the mother exceeds the potential risk to the fetus.

Clinical data on its use in I and II trimesters of pregnancy are absent, data on the use of the drug in the III trimester are limited.
Studies carried out on animals showed no signs of fetal damage.
At present, it is not known whether urapidil is excreted in breast milk, so during treatment with urapidil breastfeeding should be discontinued.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution should prescribe the drug in violation of kidney function.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution should prescribe the drug to patients with a violation of liver function.

APPLICATION FOR CHILDREN

Contraindicated in children and adolescents under 18 years.

APPLICATION IN ELDERLY PATIENTS

Caution should be given to elderly patients.

SPECIAL INSTRUCTIONS

Possible simultaneous use with other internal antihypertensives.

If previously prescribed antihypertensive drugs, the drug Egrantil ® , solution for intravenous administration, should not be used until enough time has elapsed to develop the effect of taking the previous drug (s) drug (s) .
The dose of Egrantil ® should be appropriately reduced.
An excessively rapid drop in blood pressure can cause bradycardia or cardiac arrest.

In elderly patients, the drug should be used with caution and initially administered in small doses, because
sensitivity in this category of patients is higher or changed to such drugs.
Patients on a sodium-restricted diet should bear in mind that the Ebrantil® solution, an intravenous solution, contains sodium in an amount not exceeding 1 mmol (23 mg) in 5 ml of the preparation and 2 mmol (46 mg ) in 10 ml of the preparation.

There are cases of development of prolonged erection and priapism against the background of therapy with alpha 1- adrenoblockers.
If the erection persists for more than 4 hours, you should immediately seek medical help. If priapism therapy has not been carried out immediately, it can lead to damage to the tissues of the penis and an irreversible loss of potency.
Impact on the ability to drive vehicles and manage mechanisms

The drug may affect the ability to drive vehicles or work with various mechanisms.
This is especially true at the beginning of treatment, with an increase in the dose of the drug or the replacement of the drug, as well as the use of alcohol during the treatment period.
OVERDOSE

Symptoms: dizziness, orthostatic collapse, fatigue, retardation.

Treatment: with a sharp decrease in blood pressure, it is necessary to lift the patient's legs and begin infusion therapy to increase the BCC.
If these measures are ineffective, infusion of vasoconstrictors, under the control of blood pressure, can be started. In very rare cases, intravenous catecholamines (0.5-1.0 mg epinephrine (epinephrine) diluted in 10 ml of physiological saline) are needed.
DRUG INTERACTION

The antihypertensive effect of urapidil can be enhanced by joint admission with alpha-adrenoblockers, vasodilators or other antihypertensive agents, as well as in conditions associated with a decrease in body fluid (diarrhea, vomiting) and with the intake of ethanol (alcohol).

With simultaneous administration of cimetidine C max, urapidil in blood plasma can increase by 15%.

It is not recommended to use with ACE inhibitors, because data on such a combination is not enough.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of no higher than 30 ° C.
Shelf life - 2 years.
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