Etoperidone: Uses, Characteristics And Side Effects
Etoperidone is an atypical antidepressant, or second-generation tricyclic, used to treat depressive disorders and which was developed decades ago, although it is currently discontinued. Currently, other new generation antidepressants are used that have fewer side effects than those of the drugs in the family of this medication.
In this article we explain what etoperidone is and what effects it produces, what is its mechanism of action and that of tricyclic antidepressants, what side effects it causes and what are the main contraindications if this drug is going to be used.
What is etoperidone and what effects does it have?
Etoperidone is a drug from the group of atypical antidepressants (second-generation tricyclic) that was developed in the 1970s by the Italian pharmaceutical company Angelini and is currently no longer marketed.
It belongs to the group of phenylpiperazines and has a chemical structure similar to other medications such as trazodone and nefazodone, both also second-generation antidepressants that act as antagonists and serotonin reuptake inhibitors, with anxiolytic and hypnotic effects.
Although etoperidone has certain sedative effects, it differs from other minor tranquilizers in some fundamental aspects: in its interaction with the main brain amines; due to the absence of anticonvulsant effects; and in its different spectrum of effects at a behavioral level when consumed in high doses.
Etoperidone, however, It is similar in some aspects to neuroleptic drugs (medicines used to treat psychoses and states of extreme agitation), such as chlorpromazine, since it produces analgesic and sedative effects at low doses; although unlike these, it does not block dopamine receptors at a central level.
Etoperidone acts as a drug antagonist of several receptors, including serotonin and adrenergic receptors It also seems to have a slight affinity for blocking dopamine, histamine and acetylcholine (muscarinic type) receptors.
In addition to blocking these receptors, this medication also has a weak affinity for the monoamine transporters: serotonin, norepinephrine, and dopamine. The administration of this type of antidepressants in the acute phase mainly increases the availability of norepinephrine and, to a certain extent, that of 5-HT, by blocking its reuptake in the synaptic cleft.
Prolonged use downregulates alpha-adrenergic receptors on the postsynaptic membrane a possible final common pathway of the antidepressant activity of these drugs.
On the other hand, etoperidone, in its metabolization, produces an active substance or metabolite called mCPP, probably responsible for the serotonergic effects; a substance that can cause unwanted and unpleasant effects in subjects who consume or consumed this antidepressant.
Second-generation atypical or tricyclic antidepressants
Etoperidone belongs to the group of atypical or tricyclic antidepressants, frequently used in patients suffering from major depression and who respond inadequately or endure intolerable side effects during first-line treatment with serotonin reuptake inhibitor antidepressants.
Tricyclic antidepressants have been used for decades and have certain chemical and, to a lesser extent, pharmacological similarity with phenothiazines, used to treat serious mental and emotional disorders. Although initially it was thought that this type of antidepressants were useful as antihistamines, over time their use was limited to the treatment of depression and other similar pathologies.
These types of antidepressants are highly effective although due to the number of side effects they produce, it is usually recommended to start the treatment with a low dose and increase it depending on the tolerance that each patient has and the antidepressant effect achieved, until a balance is found between the greatest effectiveness possible and the fewest side effects.
Given its sedative profile, this type of drugs can also be used to treat patients with depression who have a high level of anxiety helping them calm the nervousness and agitation that they usually present in certain circumstances.
Currently, this type of antidepressants have been replaced by new generation ones, with fewer side effects and a more specific and selective mechanism of action, such as venlafaxine or mirtazapine, two serotonin and norepinephrine reuptake inhibitors.
Side effects
The most common side effects When drugs from the group of atypical or heterocyclic antidepressants are consumed, such as etoperidone, they include a whole series of effects at the somatic level, such as the following:
Contraindications
Although these types of antidepressant drugs were effective in their day and when they were developed, they are currently used less and less, since Their overdose is toxic and they have more adverse effects than the most modern antidepressants These side effects are mainly due to muscarinic and histamine blockades, and alpha-adrenergic actions.
Many of the atypical antidepressants have strong anticholinergic properties and are therefore not suitable for the elderly or for patients suffering from benign prostatic hypertrophy, glaucoma or chronic constipation. Besides, The vast majority of drugs of this type lower the seizure threshold, with the consequent danger for people prone to seizures.
Specific contraindications for the use of etoperidone include the following:
