Description

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Pharmacological action

Antidepressant (tricyclic antidepressant). It also has some analgesic (of central origin), antiserotonin effect, helps to eliminate urinary incontinence and reduces appetite.

It has a strong peripheral and central anticholinergic effect due to its high affinity for m-cholinergic receptors; a strong sedative effect associated with affinity for H1-histamine receptors, and alpha-adrenoblocking effect.

It has the properties of a class IA antiarrhythmic drug, like quinidine in therapeutic doses, it slows down ventricular conduction (in case of overdose, it can cause severe intraventricular blockade).

The mechanism of antidepressant action is associated with an increase in the concentration of norepinephrine and / or serotonin in the central nervous system (CNS) (a decrease in their reabsorption).

The accumulation of these neurotransmitters occurs as a result of inhibition of their reuptake by the membranes of presynaptic neurons. With prolonged use, it reduces the functional activity of beta-adrenergic and serotonin receptors of the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems, disturbed in depressive states. In anxiety-depressive states, it reduces anxiety, agitation and depressive manifestations.

The mechanism of anti-ulcer action is due to the ability to have a sedative and m-cholinoblocking effect. The effectiveness in nocturnal urinary incontinence is apparently due to anticholinergic activity, leading to an increase in the ability of the bladder to stretch, direct beta-adrenergic stimulation, activity of alpha-adrenergic agonists, accompanied by an increase in the tone of the sphincter, and central blockade of serotonin uptake. It has a central analgesic effect, which is believed to be associated with changes in the concentration of monoamines in the central nervous system, especially serotonin, and the effect on endogenous opioid systems.

The mechanism of action in bulimia nervosa is unclear (may be similar to that in depression). A distinct effect of the drug is shown in bulimia in patients both without depression and in its presence, while a decrease in bulimia can be noted without concomitant weakening of depression itself.

During general anesthesia, it reduces blood pressure and body temperature. Does not inhibit monoamine oxidase (MAO).

The antidepressant effect develops within 2-3 weeks after the start of use.