Medication Description: Octadinum (Octadinum)
OCTADIN (Octadinum) b - (N-Azacyclooctyl) -ethylguanidine sulfate.
White crystalline powder bitter taste. Few soluble in water.
The sympatholytic effect of Octadine is due to the fact that it selectively accumulates in the granules of sympathetic nerve endings and displaces the adrenergic mediator, norepinephrine, from them. The part released by the mediator reaches the postsynaptic α -adrenoreceptors and has a short-term pressor effect, however, the main part of the mediator is destroyed by axonal monoamine oxidase. As a result of the depletion of norepinephrine in adrenergic endings, the transmission of nervous excitement to them decreases or stops.
Disturbance of transmission of nervous excitement is connected, moreover, with the fact that, accumulating in the nerve endings, octadine has a local anesthetic effect on them. Octadine affects the cardiovascular system in two phases: first a transient pressor reaction develops with tachycardia and an increase in cardiac output, then a progressive decrease in systolic and diastolic blood pressure occurs, the heart rate, minute volume and pulse pressure decrease, and later (after 2–3 days after oral administration) persistent hypotension occurs. The initial pressor reaction can last up to several hours. With prolonged use of the drug, the hypotensive effect may decrease due to a gradual increase in cardiac output.
Oktadin is used as an antihypertensive agent. The drug has a strong hypotensive effect and with proper dose selection can cause a decrease in blood pressure in patients with hypertension in various stages, including the severe forms with high and persistent pressure.
Octadine is effective when taken orally. Slowly sucked. Hypotensive effect in hypertension develops gradually; it begins to appear after 2 - 3 days after the start of the drug intake, reaches a maximum on the 7th - 8th day of treatment, and after stopping the administration, another 4 - 14 days is sold. The drug causes a decrease in heart rate, a decrease in venous pressure, and in some cases, peripheral resistance. At the beginning of treatment, there may be a decrease in the filtration function of the kidneys and renal blood flow, however, with further treatment and a steady decrease in blood pressure, these indicators level off (N. A. Ratner and others).
For the treatment of hypertension, octadine is administered orally in the form of tablets. Doses should be selected individually depending on the stage of the disease, the general condition of the patient, the tolerability of the drug, etc. Begin with a small dose - 0.01-0.0125 g (10-12, 5 mg) once a day, then gradually increase (usually weekly 10 12, 5 mg) to 0.05 - 0.075 g per day.