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N-Cholinolytics
Last reviewed: 08.07.2025

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Gangleron. The drug has ganglionic blocking, central anticholinergic, antispasmodic and anesthetic effects.
Gangleron is a stable substance that slowly hydrolyzes in the body. It dilates blood vessels, causing a hypotensive effect.
In cardiovascular pathology, the use of gangleron in a dose of 1-3 mg/kg of body weight significantly suppresses reflexes from the heart, normalizes pathological shifts in the electrocardiogram, improves myocardial nutrition, and reduces the flow of vasoconstrictor impulses to the coronary vessels. The use of gangleron in hypertension is also very effective.
In a series of studies of the effect of ganglerone on the body's oxygen supply, it was shown that at a dose of 0.5-1 mg/kg, the drug gradually increases the oxygen content by 7.1 ± 1.8% in arterial blood by the 20-30th minute. At the same time, a sharp but brief increase in the oxygen content in venous blood (9.4 ± 1.6%) is observed at doses of 2-3 mg/kg, as well as an increase in the volumetric velocity of venous blood flow by 9.4 ± 3.1%. Arterial pressure decreases gradually, decreasing by 18.0 ± 7.4 % 60 minutes after the administration of ganglerone at a dose of 2-3 mg/kg. With the administration of ganglerone at a dose of 2-5 mg/kg, a fairly significant increase in the oxygen content in the blood was noted - by 20-70% of the initial level. Thus, the use of gangleron leads to a significant increase in arterial blood oxygenation, a decrease in dyspnea and an increase in tissue oxygen consumption. This is probably what causes its beneficial effect in the treatment of angina and other diseases.
It has been established that gangleron has a stimulating effect on the uterus. It selectively blocks impulse conduction in the parasympathetic ganglia. The drug has thus been found to have an acetylcholine-like effect. Consequently, along with ganglionic blocking activity, the substance also has a cholinergic effect, and this effect is manifested at the level of postganglionic cholinergic synapses.
Gangleron is used 2-4 ml intramuscularly or intravenously: single dose (4 ml of 1.5% solution - 60 mg), daily (12 ml of 1.5% solution).
Kvateron. The drug blocks the conduction of excitation in the parasympathetic and, to a lesser extent, sympathetic ganglia, and has some coronary dilating action. It has a hypotensive effect and, which is very important for obstetric practice, normalizes arterial pressure in pituitrin hypertension. Kvateron is especially indicated for conditions accompanied by increased tone of the parasympathetic nerves and smooth mucosa.
When taking kvateron, side effects are possible - dizziness, tendency to constipation, moderate tachycardia. There are no specific contraindications to the use of kvateron.
In experimental studies conducted on cats and rabbits, it was established that intravenous administration of kvateron in doses of 0.02-0.05 mg/kg stimulates the motor activity of the uterus, causing an increase and more frequent waves of contractions of the uterine muscles lasting up to 2 hours. The following fact established by the author is very important - with simultaneous recording of contractions from the horn and cervix, along with an increase in the motor activity of the neuromotor apparatus of the horn, relaxation of the cervix occurs. When determining some biochemical indices, along with an increase in contractile activity of the uterus, a decrease in cholinesterase activity of tissues and an increase in the content of acetylcholine were noted. In addition, it was shown that N-cholinolytics (gangleron, kvateron), when used to stimulate uterine contractions during weakness of labor, have a pronounced labor-stimulating effect.
Dosage: 30-40 mg orally 3 times a day. Higher doses for adults: orally single - 0.05 g, daily - 0.2 g.
Pentamin. The most characteristic feature of the action of pentamin is its ability to block the transmission of impulses in the autonomic ganglia.
Indications are basically the same as for other similar ganglionic blockers. There is considerable experience in using pentamin in hypertensive crises, spasms of peripheral vessels, spasms of the intestine and biliary tract, renal colic, bronchial asthma (relief of acute attacks), eclampsia, causalgia, pulmonary edema, cerebral edema.
Anticholinergics have found wide application for regulation of labor activity. Complete ganglionic block is achieved by using pentamine at a dose of 2 mg/kg.
The drug reduces the secretion of catecholamines by the adrenal glands, peripheral vascular tone, promotes hemodynamic stabilization, improves oxidative processes, prevents the development of traumatic shock and pulmonary edema.
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