Benzogexonium-zdorovya

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT BENZOHHEXONY-ZDOROV'YA (BENZOHEXONY-ZDOROVYE)

Composition:

Active ingredient: 1 ml of solution contains 25 mg of benzohexonium;

Excipient: water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear, colorless solution.

Pharmacotherapeutic group. Antiadrenergic agents, ganglion blockers. ATC code C02BC.

Pharmacological Properties.

Pharmacodynamics.

A quaternary ammonium compound having a long-acting ganglion-blocking effect.

The mechanism of action is due to blockade of autonomic (sympathetic and parasympathetic) ganglia, resulting in inhibition of nerve impulse transmission from preganglionic to postganglionic fibers, dilation of arterial and venous vessels, reduction of total peripheral vascular resistance, and a very rapid, sharp decrease in arterial blood pressure. The hemodynamic (vasodilating) effect is accompanied by reduced pressure in the pulmonary artery, pooling of blood in the dilated veins of the abdominal cavity and extremities, and decreased venous return to the heart.

It affects carotid body chemoreceptors and chromaffin tissue of the adrenal glands, thereby attenuating reflex pressor responses. By interrupting nerve impulse conduction through autonomic ganglia, it alters the function of organs innervated by the autonomic nervous system. It causes reduction in arterial pressure, gastrointestinal motility, bladder tone, exocrine gland secretion, impairs accommodation, dilates bronchi, and increases heart rate.

The hypotensive effect begins 5–15 minutes after administration, reaches its maximum by the 30th minute, and lasts for 3–4 hours.

Pharmacokinetics.

After intravenous administration or local injection, the drug enters the extracellular fluid. It poorly penetrates tissue barriers (including the blood-brain and placental barriers). It is excreted unchanged by the kidneys; up to 90% of the administered dose is eliminated within 24 hours. The rate of excretion is highest during the first hours after injection.

Accumulation may occur in renal insufficiency.

Pharmacokinetics has not been fully studied.

Clinical Characteristics.

Indications.

For controlled arterial hypotension, hypertensive crisis (including complicated by left ventricular failure), peripheral vascular spasms (endarteritis, intermittent claudication).

Contraindications.

Hypersensitivity to components of the drug; arterial hypotension, hypovolemia and shock, pheochromocytoma, acute myocardial infarction, ischemic stroke (within 2 months), thromboses (including cerebral arteries), closed-angle glaucoma, hepatic and/or renal insufficiency, degenerative changes of the central nervous system.

Interaction with other medicinal products and other types of interactions.

The drug enhances the effects of adrenoblockers and cholinoblockers. Mutually enhances the action of venous vasodilators, antihistamines, narcotics, sedatives, neuroleptics, tricyclic antidepressants, local anesthetics, antihypertensive agents. When used concomitantly with monoamine oxidase inhibitors (MAO inhibitors), collapse may occur. Increases insulin sensitivity in patients with diabetes mellitus. The effectiveness of the drug is reduced by anticholinesterase agents, N-cholinomimetics, and drugs that induce vomiting.

Special precautions.

Contraindications for medical use include predisposition to thrombosis and advanced age (increased risk of adverse effects).

Treatment must be carried out under strict medical supervision; arterial pressure must be continuously monitored during intravenous administration.

To prevent collapse, the patient must remain in a horizontal position before administration and for 2–2.5 hours after it.

In case of intestinal or urinary bladder atony, administration of proserin, galantamine, or other cholinomimetic or anticholinesterase agents is advisable.

Tolerance to benzohexonium develops relatively quickly, requiring dose escalation.

Use during pregnancy or breastfeeding.

The drug is contraindicated during pregnancy. If use of the drug is necessary, breastfeeding should be discontinued.

Ability to affect reaction rate when driving or operating machinery.

During treatment, patients should refrain from driving and engaging in potentially hazardous activities due to the possible occurrence of adverse effects on the nervous and cardiovascular systems.

Administration and Dosage.

Administer intramuscularly, intravenously, or subcutaneously. The dosage regimen is individual due to high individual variability in patient responses.

Prior to initiating therapy, a test for individual sensitivity should be performed by administering ½ of the standard dose (via the intended route of administration), followed by monitoring of the patient's condition.

Adults.

Controlled arterial hypotension: administer intravenously 1–1.5 mL (25–37.5 mg) over 2 minutes.

Hypertensive crisis: to control, administer intramuscularly or subcutaneously 0.5–1 mL (12.5–25 mg). If necessary, repeated injections may be given (3–4 times daily).

Peripheral vascular spasms: administer intramuscularly or subcutaneously 0.25–0.5 mL (6.25–12.5 mg) once an hour before meals, 2–4 times daily. Treatment should be administered in courses of 2–4–6 weeks with 1–3 week intervals between courses.

Maximum doses for adults for intramuscular and subcutaneous administration: single dose – 3 mL (75 mg), daily dose – 12 mL (300 mg).

Since the effect of benzohexonium gradually decreases with repeated administration, treatment should begin with the lowest doses, which should then be gradually increased.

Children. In emergency situations, administer intramuscularly or intravenously. For intravenous administration, slowly (over 6–8 minutes), after dilution in 10–20 mL of 0.9% sodium chloride or glucose solution. Single doses for children by age: under 2 years – 0.04–0.08 mL/kg (1–2 mg/kg); 2–4 years – 0.02–0.08 mL/kg (0.5–2 mg/kg); from 5 years – 0.02 mL/kg (0.5 mg/kg).

Children. The medicinal product should be administered to children in doses according to body weight (see section "Administration and Dosage").

Overdose.

In case of overdose, orthostatic collapse may develop.

Treatment: place the patient in a horizontal position with head lowered and legs elevated; administration of mesaton (phenylephrine) or ephedrine in small doses, cordiamine, caffeine is indicated.

Adverse reactions.

Cardiac side effects: increased pulse rate, tachycardia, chest pain.

Nervous system side effects: weakness, dizziness, pupillary dilation, accommodation disorders, transient memory impairment, dysarthria, respiratory depression.

Gastrointestinal side effects: dry mouth, dysphagia, constipation; with prolonged use – intestinal atony and gallbladder paresis.

Urinary system side effects: with prolonged use – bladder atony, urinary retention and impaired micturition, predisposing to cystitis.

Vascular side effects: orthostatic hypotension (up to collapse), injection of scleral vessels.

Shelf life. 4 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. 1 ml in ampoules: pack of 10 in a box; packs of 5, 5×2, 10 in blister packs in a box.

Supply category. Prescription only.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROV'YA".

Manufacturer's location and address of business activity.

Ukraine, 61013, Kharkiv region, Kharkiv city, Shevchenka street, building 22.