Ebrantil (urapidil) capsules 60 mg. №50

$36.90

Manufacturer: Germany

Of hypertensive crisis. Severe or very severe hypertension. Refractory arterial hypertension. For a controlled decrease in blood pressure if it increases during / or after surgery.

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Description

Ebrantil Storage
active substance: urapidil;

1 capsule of Ebrantil 30 mg contains 30 mg of urapidil;

1 capsule of Ebrantil 60 mg contains 60 mg of urapidil;

excipients: methacrylate copolymer (type B); diethyl phthalate; talc; hypromellose; fumaric acid; ethylcellulose; hypromellose phthalate; stearic acid; spherical sugar;

shell for capsules of 30 mg: gelatin; titanium dioxide (E 171); iron oxide yellow (E 172); purified water; black ink (for marking);

shell for capsules of 60 mg: gelatin; titanium dioxide (E 171); erythrosine (E 127); indigo carmine (E 132); iron oxide red (E 172); purified water; black ink (for marking).

Ebrantil Dosage form
Prolonged-release capsules are hard.

Basic physical and chemical properties:

30 mg capsules: hard gelatin capsules (№4) with an opaque yellow body and a yellow cap with the black inscription “Ebr 30” printed on the body. Capsule content – yellow granules;

60 mg capsules: hard gelatin capsules (№2) with an opaque pink body and a bright red cap with a black “Ebr 60” inscription on the body. The content of the capsules is yellow granules.

Ebrantil 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 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 oral administration, more than 80-90% of urapidil is absorbed in the gastrointestinal tract. Peak plasma concentration of sustained release dosage form is reached 4-6 hours after application; the half-life from plasma is approximately 4.7 hours (3.3-7.6 hours).

Bioavailability. The relative bioavailability of sustained-release capsules compared to orally administered solution is 92 (83–103)%. The absolute bioavailability of prolonged-release capsules compared to the intravenous standard is 72 (63-80)%.

The binding of urapidil to plasma proteins (human serum) in vitro is 80%. This relatively low plasma protein binding of urapidil may explain why the interactions of urapidil and drugs with strong plasma protein binding 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 benzene 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 hypotensive para-hydroxylated urapidil, 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
Hypertension.

Contraindication
Hypersensitivity to the active substance or to any of the excipients.