Buy Ebrantil ampoules 5 mg/ml 5 ml, 5 pcs

Ebrantil® [Urapidil]

Brand Takeda GmbH

In stock 1993 Items

Available since: 2019-09-19

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Clinical Pharmacology

Ebrantil refers to drugs that block postsynaptic α₁-adrenoretseptory, thereby reducing peripheral resistance. In addition, the drug Ebrantil regulates the central mechanism for maintaining vascular tone and has a weak β-adrenergic blocking effect. Heart rate, cardiac output with its introduction do not change. Low cardiac output may increase due to a decrease in vascular resistance. Orthostatic phenomena, as a rule, the drug Ebrantil does not cause. Blocks vasoconstriction caused by α₂-adrenoreceptors, and does not cause reflex tachycardia due to vasodilation.

The drug Ebrantil balanced reduces SBA and DBP, reducing peripheral resistance.

Urapidil reduces the pre- and afterload of the heart, increases the efficiency of the heartbeat, thereby, in the absence of arrhythmia, the drug increases the reduced minute volume of the heart.

Mechanism of action. The drug Ebrantil has a central and peripheral mechanisms of action.

Preferentially blocks peripheral postsynaptic α₁- adrenergic receptors, so the drug blocks the vasoconstrictor action of catecholamines.

In the central nervous system, urapidil affects the activity of the vasomotor center, which is manifested in the prevention of reflex changes in the tone of the sympathetic nervous system.

Urapidil does not affect the carbohydrate metabolism, the exchange of uric acid and does not cause fluid retention in the body.

Pharmacokinetics

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

The period of distribution of the drug is about 35 minutes.

V_d - 0.8 l / kg (0.6–1.2 l / kg). Most of the urapidil is metabolized in the liver. The main metabolite is a derivative hydroxylated at the 4th position of the benzene ring, which has practically no antihypertensive activity.

O-demethylated metabolite is formed in very small quantities and is practically as active as urapidil. 50–70% of urapidil and its metabolites (15% in the form of an active drug) are excreted by the kidneys, the rest is excreted through the intestines in the form of metabolites (mainly in the form of inactive para-hydroxylated urapidil).

T_1/2 after intravenous bolus administration is 2.7 hours (1.8–3.9 hours). Binding to plasma proteins - 80%. A relatively low degree of binding to plasma proteins minimizes the likelihood of urapidil interacting with drugs that bind strongly to plasma proteins.

In elderly patients, as well as in patients with severe hepatic and / or renal insufficiency. V_d and clearance of urapidil reduced, and T_1/2 is increased.

Urapidil penetrates the BBB and placental barrier.

Indications

hypertensive crisis;
refractory hypertension or severe severity;
controlled hypotension during and / or after surgery.

Composition

1 ml solution for intravenous administration contains:
active substance: urapidil hydrochloride 5.47 mg (corresponds to 5 mg of urapidil),
Excipients: propylene glycol; sodium hydrogen phosphate dihydrate; sodium dihydrophosphate dihydrate; water for injections.

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Dosage and Administration

Enter the jet or by long-term infusion in the patient lying down.

Hypertensive crisis, severe arterial hypertension, refractory hypertension

1. ATnutrivenno: 10-50 mg of the drug Ebrantil slowly administered under the control of blood pressure. A decrease in blood pressure is expected within 5 min after administration. Depending on the therapeutic effect, repeated administration of the drug Ebrantil is possible.

2. ATnutrivennaya drip or continuous infusion using a perfusion pump. Maintenance dose is on average 9 mg / h, i.e. 250 mg of the drug Ebrantil (10 vials of 5 ml or 5 vials of 10 ml) in 500 ml of solution for infusion (1 mg = 44 drops = 2.2 ml).

The maximum allowable ratio is 4 mg of the drug Ebrantil per 1 ml solution for infusion.

The recommended maximum initial speed is 2 mg / min.

The rate of drip depends on the patient's blood pressure.

The solution for drip infusions, designed to maintain blood pressure, is prepared as follows.

Typically, 250 mg of the drug (10 vials of 5 ml or 5 amp. 10 ml) of the drug Ebrantil are added to 500 ml of solution for infusion, for example, saline, 5 or 10% dextrose (glucose) solution.

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

Controlled (controlled) decrease in blood pressure with its increase during and / or after surgery. Continuous infusion using a perfusion pump or drip infusion is used to maintain blood pressure at the level achieved using IV injection.

The dosing scheme is shown in the figure.

Notes:

- if other antihypertensive drugs were previously used, then the drug Ebrantil can be administered only after a period of time sufficient for the previously administered drug (s) to work (s); dose of the drug Ebrantil should be adjusted accordingly;

- when using antihypertensive drugs in elderly patients, caution must be exercised; the initial dose should be reduced in comparison with the recommended, since the sensitivity in elderly patients to drugs of this series is often changed (V_d reduced and T_1/2 enlarged).

The introduction of the drug can be single or multiple. Injection can be combined with the subsequent drip infusion. Parenteral therapy can be repeated with a new increase in blood pressure.

Adverse reactions

Most of the following side effects are due to a sharp drop in blood pressure, but clinical experience shows that they disappear within a few minutes even after a drip infusion of Ebrantil. For severe side effects, discontinuation of treatment may be required.

The list of side effects with an indication of the frequency of their development is presented in the tables.

Side effects of the drug Ebrantil (solution for intravenous administration)

Organ system	Frequency
Organ system	Often (≥ 1: 100, Sometimes (≥1: 1000, <1: 100="" rarely="" 1:="" 10000="" very="" td="">
From the CCC		Palpitations, tachycardia, bradycardia, chest pressure, shortness of breath, arrhythmias
From the gastrointestinal tract	Nausea	Vomiting
Laboratory values				Thrombocytopenia^*
From the side of the central nervous system	Dizziness, headache, fatigue			Anxiety
Reproductive system and mammary glands			Priapism
On the part of the urinary system	Proteinuria		Nephropathy, nephrotic syndrome
On the part of the skin		Excessive sweating	Allergic reactions (pruritus, skin redness, rash)

Carefully: advanced age, impaired liver and / or kidney function, hypovolemia.

Drug interactions

The antihypertensive effect of urapidil may be enhanced when taken together with α-blockers or other antihypertensive drugs, as well as with hypovolemia (nausea, vomiting) and with ethanol.

While taking cimetidine C_max urapidil in plasma can increase by 15%.

Special instructions

It may be used simultaneously with other oral antihypertensive drugs.

There is no clinical data on the use of the drug in children under 18 years.

Overdosage

Symptoms: dizziness, orthostatic collapse, fatigue, lethargy.

Treatment: with a sharp drop in blood pressure, it is necessary to raise the patient's legs and begin infusion therapy to increase the BCC. With the ineffectiveness of these measures, you can begin the infusion of vasoconstrictors under the control of blood pressure. In very rare cases, it is necessary to / in the introduction of catecholamines (0.5–1 mg of epinephrine (adrenaline), diluted in 10 ml of saline).