Depression being one of the most prevalent mental disorders worldwide and one of the major causes of disability, its treatment is an issue that the scientific community has taken into account for many years.
The suffering it generates requires sometimes immediate attention, since it is one of the disorders with the highest risk of suicide and that generates the most pain both for the person and their environment. The treatment of depression is carried out from different areas, one of them being psychopharmacology. One of the drugs used to treat depression is trazodone which we are going to talk about in this article.
Trazodone: what type of substance is it?
Trazodone is a psychotropic drug classified within antidepressants, substances that generate a neurochemical change at the brain level, causing the alteration of the levels of certain neurotransmitters, specifically serotonin. Among antidepressants, it is part and in fact the main representative of the group of serotonin-2A antagonists and reuptake inhibitors or SARIs, a type of atypical antidepressant. This drug was designed in Italy in 1966 under the assumption that depression could be based on the existence of low thresholds regarding the perception of pain and suffering, being a product of the lack of integration of aversive experiences.
Trazodone has proven to be an efficient and effective drug in the treatment of depression, reducing passivity and lack of activity as well as the discomfort and suffering associated with said ailment and facilitating an increase in mood. However, In addition, it also has an anxiolytic and tranquilizing action
This substance is considered a second-generation antidepressant, along with specific serotonin reuptake inhibitors (SSRIs), with which it shares part of its mechanism of action, and different dual antidepressants. In fact, sometimes trazodone is considered dual as it has two differentiated effects, although they focus on the same neurotransmission system, compared to the rest and in addition to an antidepressant effect it also has tranquilizing effects.
How does it work? Mechanism of action of the drug
As we have indicated previously, trazodone is classified as SARI, having a somewhat special mechanism of action among the rest of antidepressants. Trazodone acts at the serotonergic system (like most antidepressants) in two specific ways.
Firstly, this substance blocks the reuptake of brain serotonin, in such a way that This neurotransmitter remains in the synaptic space for a longer time This means that it has an agonist effect on the synthesis and maintenance of serotonin at the brain level, increasing its levels (which are decreased during depression and this is something that correlates with a decrease in mood). The aforementioned mechanism of action is the one used by SSRIs, which is why they and trazodone are related and the latter is sometimes included among the first.
However, trazodone has a second effect that differentiates it from other drugs, and that in fact seems contrary to the previous mechanism of action. And it also acts as an antagonist of the serotonin 5-HT2A receptors, preventing or making it difficult for these receptors to be activated. This second aspect is what makes trazodone have a slightly different profile and effects than other antidepressants.
Regarding its interaction with other neurotransmitter systems, does not present major anticholinergic effects, something that has made this drug a better option than tricyclics (although doses must still be regulated) in patients with cerebrovascular, cardiac, and dementia pathologies. However, it must be taken into account that it can generate arrhythmias. It also has a minor effect on the adrenergic system (blocking some receptors) and histaminergic, something that can contribute to the generation of side effects.
Main indications
The main indication for trazodone is obviously, as an antidepressant, major depression. Its effectiveness is also high in those depressions that appear together with anxious symptoms. It has also been observed its clinical usefulness in other disorders in which there are anxiety components or that are based on it, such as generalized anxiety disorder, Obsessive-Compulsive Disorder or bulimia.
In addition to this, it has also been observed to be useful for the treatment of substance addictions, being a good alternative for patients with benzodiazepine withdrawal syndrome, and in the treatment of alcoholism (including the presence of delirium tremens). Another of its indications is insomnia which effectively reduces increasing sleep time without greatly affecting the deep sleep phase.
Although most antidepressants can generally have the presence of erectile dysfunction or ejaculation problems as a side effect, this effect does not usually occur with trazodone, which in fact seems to generate an increase in libido and which It is even used as an indicated treatment for erectile dysfunction
Finally, trazodone has been applied (largely due to its relaxing properties) in some cases of schizophrenia, motor problems such as Gilles de la Tourette syndrome, the presence of manic episodes in bipolar disorder and the behavioral alterations of Alzheimer’s, although a greater amount of study is required regarding the latter.
On a medical level, it has also been used as a sedative in patients infected with HIV and diabetic neuropathies, as well as in other disorders that cause pain such as fibromyalgia. It has a very slight muscle relaxing effect.
Side effects and contraindications
Trazodone is a very useful drug that has been used in multiple pathologies and disorders, both mental and medical. However, it can have undesirable consequences in the form of side effects and is even contraindicated in some situations and pathologies.
Regarding secondary symptoms, Sedation and fatigue, the presence of headaches, nausea and vomiting, and gastric disorders are common (diarrhea or constipation), appetite disturbances, sweating, tremors (which may lead to convulsions in some cases), tinnitus, numbness and vision problems. In some cases it can also cause chest and muscle pain, alterations in consciousness, breathing problems and arrhythmias. Like other antidepressants, trazodone can also contribute to the development of suicidal ideation in the first moments of use.
Although, unlike other antidepressants, it does not seem to generate but actually contributes to improving cases of erectile dysfunction or ejaculatory problems, the use of trazodone has been observed and associated with the emergence of priapism, erections that do not disappear on their own. alone and that generate pain for those who suffer from them (and may require urgent and even surgical treatment).
Although it is sometimes used in dementia and has a lower risk than tricyclics of generating heart problems, great caution is required in its use and a dosage carefully prescribed by the doctor, since it can generate arrhythmias. It is contraindicated in patients who have just suffered a heart attack as well as in those who suffer from liver or kidney disease.
Caution should be taken in subjects with bipolarity, since if the medication is not regulated, the consumption of trazodone can cause a shift from a depressive to a manic phase. It is also contraindicated in people who have suffered from priapism or have Peyronie’s disease. Finally, it must be taken into account that trazodone can be excreted in breast milk and transmitted through the placenta, so its use is contraindicated in pregnant and lactating women.