Trazodone: uses and side effects of this drug
Depression being one of the most prevalent mental disorders worldwide and one of the major causes of disability, its treatment is a matter that the scientific community has taken into account for many years. The suffering that it generates requires immediate attention, since it is one of the disorders with the highest risk of suicide and that generates more pain for both the person and their environment. The treatment of depression is carried out from different areas, one being psychopharmacology. One of the drugs used in the treatment of depression is trazodone , which we are going to talk about in this article.
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Trazodone: what kind of substance is it?
Trazodone is a psychotropic drug classified as antidepressant , substances that generate a neurochemical change in the brain causing the alteration of the levels of certain neurotransmitters, specifically serotonin. Within antidepressants, it is part of and in fact is the main representative of the group of serotonin-2A antagonists and reuptake inhibitors or SARI, 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 in terms of the perception of pain and suffering, as a result of the lack of integration of aversive experiences.
Trazodone has been shown to be an effective and effective drug in the treatment of depression, reducing passivity and lack of activity, as well as the discomfort and suffering associated with this ailment and facilitating an increase in mood. But nevertheless, besides it also has an anxiolytic and tranquilizing action .
This substance is considered a second generation antidepressant, together with the specific inhibitors of serotonin reuptake (SSRI), with which it shares part of its mechanism of action, and different dual antidepressants. In fact, trazodone is sometimes considered to be dual in having two differentiated effects, although the same system of neurotransmission is centered, in comparison to the rest, and in addition to an antidepressant effect it also has tranquilizing effects.
How does it work? Mechanism of action of the medicine
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 level of serotonergic system (like most antidepressants) in two specific ways.
In the first place, this substance produces a blockade of the reuptake of cerebral serotonin, in such a way that said neurotransmitter remains in the synaptic space for longer . This supposes that it has an agonist effect on the synthesis and maintenance of serotonin in the brain, increases its levels (which are diminished during depression and this being something that correlates with the decrease in mood). The aforementioned mechanism of action is the one used by SSRIs, which is why these and trazodone are related and sometimes the second is included among the first.
However, trazodone has a second effect that differentiates it from other drugs, and 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 hindering these receptors are activated. This second aspect is what makes trazodone have a slightly different profile and effects than other antidepressants.
In regards to its interaction with other neurotransmitter systems, does not present great anticholinergic effects , something that has made this drug a better option than tricyclics (although the doses have to be regulated as well) in patients with cerebrovascular, cardiac and dementia pathologies. However, it must be borne in mind that it can generate arrhythmias. It also has a minor effect on the adrenergic system (blocking some receptors) and histaminergic, something that can converge in the generation of side effects.
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The main indication of trazodone is evidently, as an antidepressant that is, major depression. Its effectiveness is also high in those depressions that appear together with anxious symptoms. It has also been observed its clinical utility in other disorders in which anxiety components exist or that are based on it, such as generalized anxiety disorder, Obsessive-Compulsive Disorder or bulimia.
In addition, it has also been found useful for the treatment of addictions to substances, 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 by increasing the sleep time without greatly affecting the deep sleep phase.
Although the majority of antidepressants can have as a secondary effect the presence of erectile dysfunction or ejaculation problems, this effect does not usually occur in trazodone, which in fact seems to generate an increase in libido and that It is even used as the indicated treatment in 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 behavioral alterations of Alzheimer's, although a greater amount of study is required with respect to the latter.
At the 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 present with pain such as fibromyalgia. It has a very slight effect at the level of muscle relaxant.
Side effects and contraindications
Trazodone is a very useful drug that has been used in many 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.
With regard to secondary symptoms, sedation and fatigue, the presence of headaches, nausea and vomiting, gastric alterations are common (diarrhea or constipation), alterations of appetite, sweating, tremors (being able to reach convulsions in some cases), humming, numbness and problems in the vision. In some cases it can also cause chest and muscle pain, altered consciousness, breathing problems and arrhythmias. Like other antidepressants, trazodone can also contribute to the genesis of suicidal ideation in the first moments of consumption.
Although, unlike other antidepressants, it does not seem to generate, but actually contributes to improve the 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 to the sufferer (being able to get to require urgent treatment and even surgical).
Although it is sometimes used in dementia and has a lower risk than tricyclics of generating cardiac problems, it requires a high precaution in its use and a dosage carefully prescribed by the doctor, as it can generate arrhythmias. It is contraindicated in patients who have just suffered a heart attack , as well as in those who suffer a liver or kidney disease.
Caution should be exercised in subjects with bipolarity, because if the medication is not regulated, the consumption of trazodone can cause a change from the depressive phase to the manic phase. It is also contraindicated in people who have suffered priapism or have Peyronie's disease. Finally, it must be borne in mind that trazodone can be excreted in breast milk and transmitted through the placenta, with which pregnant and lactating women have contraindicated its use.
- Alcántara-López, M.G .; Gutiérrez-García, A.G .; Hernández-Lozano, M. & Contreras, C.M. (2009). Trazodone, an atypical antidepressant with anxiolytic and sedative properties. Arch. Neurocien (Mex), 14 (4): 249-257.