Ebrantil (urapidil) solution for injections 25 mg. 5 ml. ampoules №5

Description

Ebrantil solution Storage
active substance: urapidil;

1 ml of solution contains 5 mg of urapidil, which corresponds to 5.47 mg of urapidil hydrochloride;

Ebrantil solution excipients: propylene glycol; sodium hydrogen phosphate, dihydrate; sodium dihydrogen phosphate, dihydrate; water for injections.

Ebrantil solution Dosage form
Solution for injection.

Basic physical and chemical properties: transparent, colorless solution.

Pharmacotherapeutic group
Antihypertensive agent. Alpha-adrenoceptor blockers. ATX code C02C A06.

Pharmacological properties

Pharmacodynamics.

Urapidil reduces systolic and diastolic blood pressure by reducing peripheral resistance.

The heart rate remains virtually unchanged. Cardiac output also remains unchanged; cardiac output, which decreases as a result of increased postload, may increase.

Mechanism of action. Urapidil has central and peripheral mechanisms of action.

At the peripheral level, urapidil blocks mainly postsynaptic alpha-1-adrenoceptors, thus inhibiting the vasoconstrictive effect of catecholamines.

At the central level, urapidil modulates the activity of the center of blood circulation regulation, which prevents a reflex increase in the tone of the sympathetic nervous system or a decrease in sympathetic tone.

Pharmacokinetics.

Absorption. After intravenous administration of 25 mg of urapidil there is a two-phase decrease in the concentration of the drug in the blood (initial phase of distribution, terminal phase of elimination). The half-life is approximately 35 minutes. The half-life of the drug from serum after intravenous bolus administration is 2.7 hours (1.8-3.9 hours).

The binding of urapidil to plasma proteins (human serum) in vitro is 80%. This relatively low binding of urapidil to plasma proteins may explain why the interactions of urapidil and drugs with strong binding to plasma proteins are still unknown.

Distribution. The volume of distribution is 0.77 l / kg body weight. The substance crosses the blood-brain barrier and enters the placenta.

Metabolism. Urapidil is metabolized mainly in the liver. The main metabolite is hydroxylated urapidil in the 4th position of the phenolic ring, which has no significant antihypertensive activity. The O-dimethylated metabolite of urapidil has almost the same biological activity as urapidil, but is formed in very small quantities.

Excretion and elimination. Elimination of urapidil and its metabolites in the human body up to 50-70% renal, of which about 15% of the applied dose – pharmacologically active urapidil; the rest, primarily para-hydroxylated urapidil, which has no antihypertensive effect, is excreted in the feces.

Special groups. In elderly patients, as well as in patients with progressive hepatic and / or renal insufficiency, the volume of distribution and clearance of urapidil is reduced and the half-life from plasma is prolonged.

Indication
Hypertensive crisis.
Severe or very severe hypertension.
Refractory hypertension.
For controlled reduction of blood pressure in case of its increase during and / or after surgery.

Contraindication
Hypersensitivity to any of the components of the drug.
Aortic stenosis.
Arteriovenous shunt (except for patients with hemodynamically insignificant dialysis shunt).