Opipramol: operation and side effects of this drug

This psychotropic drug has the structure of antidepressants but is mainly used as an anxiolytic.

Moods of marked sadness most of the time, inability to enjoy oneself, hopelessness, lack of energy, sleeping problems and even suicidal ideation are some of the typical symptoms of depression or conditions in which depressive symptoms are present.

It is one of the most common mental disorders, which generates a high level of suffering and can be highly disabling.

But fortunately there are several treatments that allow us to fight against these symptoms, such as the use of Antidepressant drugs. And although the objective of most of them is the same, to combat depressive symptoms, they may differ greatly in the way they seek to achieve it. An example of this with an unusual mechanism of action is opipramolwhich we are going to talk about in this article.

What is opipramol?

Opipramol is a psychopharmaceutical of antidepressant and anxiolytic typeIt is an antidepressant and anxiolytic drug which, by altering brain chemistry and specifically the systems of certain neurotransmitters, combats the typical symptoms of depressive episodes and anxiety.

Within this large group of drugs, opipramol is structurally part of the group of tetracyclic antidepressants (in fact, structurally it is very similar to imipramine), although its functioning is very different in the organism.

This drug, developed in 1961 by Schindler and Blattner, is not yet approved or marketed in the United States but has been approved and is used in part of Europe. It is mainly marketed in Germany and Poland.

It has a biphasic effect, first provoking an increase in the levels of tension and anxiety and then generating an elevation of mood and eventually a reduction in the level of anxiety and tension. and over time a reduction in the level of anxiety and tension..

It is absorbed at gastrointestinal level and has a half-life of between 6 and 11 hours, being metabolized by the liver and eliminated through the kidneys. It is possible to find it in tablet form for oral administration.

Mechanism of action

Opipramol is an unusual psychopharmaceutical among antidepressants, since unlike most of them it does not base its action on blocking the reuptake of monoamines such as serotonin. (something that would cause serotonin levels to increase in the brain by not being reuptaken by the presynaptic neuron and held in the synaptic space).

Instead, opipramol acts as an agonist of sigma receptors receptors (i.e., it acts by triggering receptor activation), which are theoretically linked to the promotion of calcium ion release and inhibition of potassium ions.

The drug has a particularly relevant effect on sigma 1 receptors, an activity that is primarily responsible for the antidepressant effects of opipramol upon modification. Although with lower affinity, it also has an effect on sigma 2 receptors, which are more associated with its anxiolytic effects.

In addition, opipramol has an important antagonistic action with the histaminergic system, so that its anti-histaminergic action may have sedative effects and generate some side effects.. It also has a mild affinity with dopamine, serotonin and even more mildly with acetylcholine.

Main therapeutic indications

Opipramol is considered an antidepressant drug and an atypical anxiolytic. Although it is usually considered as an antidepressant because of its structure, in reality its main indication is for anxiety disordersand especially in the case of generalized anxiety disorder.

Another usual indication for this drug, and it is one of the few anxiolytics approved for this purpose, is found in the treatment of somatoform disorders. However, it is also used in the treatment of major depression and other depressive syndromes (especially neurotic depression).

Although it is not part of its approved indications, its usefulness in the treatment of various types of dementia, psychosomatic problems or schizophrenia has also been investigated.

Side effects

The use of opipramol, as with all other psychotropic drugs, may cause the following side effects undesirable and/or bothersome side effects and side effects (although some studies seem to indicate that in a smaller proportion than some SSRIs).

These include a high level of sedation, fatigue and drowsiness, especially in the first weeks of use, together with dry mouth, hypotension, dizziness, tremors, or urticaria. It can also cause stupor, weight gain, sexual symptoms such as erectile dysfunction or abnormal ejaculations or palpitations and tachycardia.

Although less frequently it may cause headaches, paresthesias, urination problems, taste alterations, edema, coronary problems, and even in some cases psychiatric symptoms such as manic episodes and hallucinations. and even in some cases psychiatric symptoms such as the appearance of manic episodes and hallucinations.

Hepatic damage, alopecia, comical crises or polyneuropathy have also been observed. If an overdose occurs, it can cause insomnia, coma, convulsions, respiratory depression and even cardiac arrest, among others.

Contraindications

The possible side effects of this drug and the way it affects the body can make its use dangerous or contraindicated for some people. In this sense, the contraindication for all those who are allergic to this drug or its components stands out in the first place.

Another important contraindication is given to those people with cardiac, renal or hepatic problems.. People with epilepsy, brain damage or cerebrovascular insufficiency should also be very cautious and should not use it. Patients with glaucoma, urinary problems such as urinary retention, paralytic ileus (paralysis of the intestinal muscles) or prostate hyperplasia should also avoid it.

Patients with bipolar disorder should be very cautious.Patients with bipolar disorder should be very cautious, since there have been cases in which the consumption of the drug has been associated with the appearance of manic episodes. Pregnant women and nursing mothers should also avoid taking the drug, since it is possible that it may be transmitted to the fetus or the baby through breast milk.

It is important to to avoid its use with alcoholIt is important to avoid its use with alcohol, MAOI antidepressants or other depressant substances.