Benzohexonium

General characteristics:

international and chemical names: 1,6-Bis- (N-trimethyl-ammonium) -hexane dibenzenesulfonate;
basic physical and chemical properties: transparent, colorless solution;
composition: 1 ml contains 25 mg benzohexonium;
excipients: water for injection.

Release form.

Injection.

Pharmacotherapeutic group.

Ganglion blockers. ATS code С02В С02 **.

Pharmacological properties.

Bis-quaternary ammonium compound with a ganglion-blocking effect of long-term action.
The mechanism of action is due to the blocking of autonomic (sympathetic and parasympathetic) ganglia, which leads to inhibition of the transmission of nervous excitation from preganglionic to postganglionic fibers, dilatation of arterial and venous vessels, a decrease in the total peripheral resistance of blood vessels and a very rapid sharp decrease in blood pressure. The hemodynamic (vasodilating) effect is accompanied by a decrease in pressure in the pulmonary artery, deposition of blood in the dilated veins of the abdominal cavity and limbs, and a decrease in venous return to the heart.
It affects the carotid glomeruli and the chromaffin tissue of the adrenal glands, which contributes to the weakening of reflex pressor influences. Interrupting the conduction of nerve impulses through the autonomic nerve nodes, changes the functions of organs equipped with autonomic innervation. It causes a decrease in blood pressure, motility of the gastrointestinal tract, tone of the bladder, secretion of exocrine glands, disrupts accommodation, dilates the bronchi, increases the heart rate.
The antihypertensive effect begins 5-15 minutes after administration, reaches a maximum by the 30th minute and persists for 3-4 hours.
Pharmacokinetics After intravenous administration or local injection, it enters the extracellular fluid. It penetrates poorly through tissue barriers (including through the blood-brain and placental). It is excreted unchanged through the kidneys; within 24 hours, up to 90% of the drug is excreted. The maximum excretion rate in the first hours after injection.
With renal failure, cumulation may occur.
Pharmacokinetics is not fully understood.

Indications for use.

Spasms of peripheral vessels (endarteritis, intermittent claudication), hypertensive crisis (including complicated by left ventricular failure), peptic ulcer of the stomach and duodenum, bronchospasm; for controlled arterial hypotension.

Dosage and administration.

Assign intramuscularly, intravenously or subcutaneously. The dosing regimen is individual due to the large individual variability of the reactions of patients.
Controlled hypotension: 1–1.5 ml (25–37.5 mg) is administered intravenously for 2 minutes.
Hypertensive crisis. For relief, they are administered intramuscularly or subcutaneously in 0.5–1 ml (12.5–25 mg). If necessary, repeated injections (3-4 times a day) can be performed.
Spasms of peripheral vessels, peptic ulcer of the stomach and duodenum: injected intramuscularly or subcutaneously in 0.25-0.5 ml (6.25-12.5 mg) 1 hour before meals 2-4 times a day. Treatment is carried out in courses of 2–4–6 weeks with breaks of 1–3 weeks.
The maximum doses for adults with intramuscular and subcutaneous administration: single - 3 ml (75 mg), daily - 12 ml (300 mg).
Since the effect of benzohexonium with repeated administrations gradually decreases, treatment begins with the lowest doses, and then the doses are gradually increased.
Children in emergency pediatrics are given intramuscularly or intravenously. Intravenously administered slowly (within 6-8 minutes), diluted in 10-20 ml of an isotonic solution of sodium chloride or glucose. Single doses for children: up to 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), older than 5 years - 0.02 ml / kg (0.5 mg / kg).

Side effect.

From the central nervous system: weakness, dizziness, dilated pupils, short-term memory loss, dysarthria, respiratory depression. From the cardiovascular system: increased heart rate, orthostatic hypotension (up to the development of collapse), tachycardia, pain in the heart, vascular injection of the sclera. From the gastrointestinal tract: dry mouth, dysphagia, constipation; with prolonged use - atony of the intestine and paresis of the gallbladder. From the urinary system: with prolonged use - atony of the bladder, impaired urination with stagnation of urine, contributing to the development of cystitis.

Contraindications

Hypersensitivity to the drug, arterial hypotension, hypovolemia and shock, pheochromocytoma, acute myocardial infarction, ischemic stroke (up to 2 months), thrombosis (including cerebral arteries), angle-closure glaucoma, liver and / or renal failure, degenerative changes in the central nervous system.

Overdose.

With an overdose, orthostatic collapse may develop. Treatment: the patient is given a position with his head bowed and legs raised, the introduction of mesatone, fetanol or ephedrine in small doses, cordiamine, caffeine.

Features of the application.

Limitations to medical use are predisposition to thrombosis, old age (increased risk of side effects), pregnancy (risk of fetal hypoxia), lactation (there are no data on the use of the drug during lactation).
Treatment should be carried out under close medical supervision; with intravenous administration, blood pressure is constantly monitored.
To avoid the development of collapse, the patient should be in a horizontal position before administration and for 2–2.5 hours after it.
With the development of atony of the intestine or bladder, it is advisable to administer proserin, galantamine, or other cholinomimetic or anticholinesterase drugs.
Before starting therapy, it is necessary to conduct an individual sensitivity test, for which ½ an average dose is administered and the patients condition is monitored.
Addiction develops relatively quickly to benzohexonium, which requires an increase in dose.
During treatment, one should refrain from driving vehicles and performing potentially hazardous activities due to the possibility of developing side effects from the central and cardiovascular systems.

Interaction with other drugs.

The drug enhances the effectiveness of adrenomimetics (norepinephrine, mesatone, isadrine, etc.) and cholinomimetics (pilocarpine, carbocholine, etc.). Mutually enhances the action of venous vasodilators, antihistamines, narcotic, hypnotics, antipsychotics, tricyclic antidepressants, local anesthetics, antihypertensive drugs. When combined with MAO inhibitors, collapse may develop. Increases the sensitivity of patients with diabetes to insulin. Vomiting, anticholinesterase drugs and N-cholinostimulants reduce the effectiveness of the drug.

Terms and conditions of storage.

Store in a dark place at a temperature of 8 ° C to 25 ° C. Keep out of the reach of children.
Shelf life is 4 years.

Vacation terms.

On prescription.

Packaging.

10 ampoules of 1 ml per pack.