Nefazodone: uses and side effects of this antidepressant

This drug is relatively little used, although it has proven useful in treating certain disorders.

Many psychotropic drugs have been developed throughout history to treat different disorders and diseases, both physical and mental. Among the different mental disorders, depression is one of the most common, which has led to the synthesis of multiple types of substances to combat its symptoms.

One of them is nefazodone, a little-known and little-used antidepressant. and used of which we are going to talk about in this article.

Nefazodone: basic characteristics of the drug

Nefazodone is an antidepressant-type psychotropic drug, derived from phenylpiperazines. and synthesized for the purpose of alleviating and treating the symptoms of depression: low mood, lack of motivation, anhedonia, passivity and sleep problems, among others.

It is one of the so-called atypical antidepressants, since its mechanism of action does not coincide with that of other antidepressants. Specifically, it would form part of the group of drugs known as weak serotonin, norepinephrine and dopamine reuptake inhibitors, or SDRIs, as does the or SDRIs, like mazindol. Other substances function similarly although they act through different mechanisms of action, such as ketamine, cocaine and ecstasy.

As with most antidepressants, it takes about four weeks to effect the brain changes necessary to visualize a real effect. This drug is an effective antidepressant, which also has the following features with the advantage of not producing hardly any sexual alterations, weight gain or appetite alterations. or appetite alterations.

However, although it is an effective antidepressant, its prescription is not habitual and in fact between 2003 and 2004 its commercialization was suspended in different countries (including Spain and the United States) due to the fact that it was demonstrated that it could suppose a high risk for health as it is highly toxic at hepatic level, and could even lead to death.

Mechanism of action

The main mechanism of action of nefazodone is its action on the receptors of different monoamines: serotonin, dopamine and noradrenaline. In a similar way to non-selective MAOIs, it increases the action of the three main monoamines but at a weaker and more controlled level.

It mainly acts as an antagonist of serotonin 5-HT2 receptors at postsynaptic level while inhibiting the reuptake of serotonin. This generates an increase in serotonin levels in the brain. It also contributes to inhibit the reuptake of norepinephrine and dopamine, although at a much lower level. Finally, it also has a slight effect at the level of histamine and acetylcholinebut the latter are practically inappreciable.

Uses and applications of this drug

Nefazodone is mainly known as an antidepressant, being major depression its main indication. It is also used in premenstrual syndrome or in other types of depression, such as that associated with various pathologies. However, in addition to its activity on depressive disordersHowever, in addition to its activity on depressive disorders, this drug can be useful in the treatment of other psychopathologies and problems.

Among them we can observe that nefazodone is useful in the treatment of various anxiety problems and post-traumatic stress disorder, as well as insomnia problems, although it increases REM sleep latency.

Side effects of this antidepressant

Despite its great usefulness, the consumption of nefazodone can generate several side effects and in some cases it can have its risks, with different contraindications.

The most common side effects of nefazodone are dry mouth and dry mouth. are dry mouth and drowsiness, along with Nausea and dizziness. Confusion, vision problems and asthenia are also relatively common. More rarely, hypotension and bradycardia have been observed, which is dangerous especially for those subjects already suffering from cardiac pathologies.

However, the most serious problem associated with this drug (and which in fact led to the discontinuation of its commercialization) is its high hepatotoxicity. In some cases, hepatic failures that can even lead to death, or jaundice, have been observed. For this reason, if prescribed (which is not very common), continuous monitoring of the patient's hepatic health status should be exercised, with periodic tests of the patient's liver health, with periodic tests. It can also have renal effects, as the drug is eliminated mainly by this route.

Another aspect to be taken into account is the risk of suffering from serotonin syndrome, a problem derived from an excess of serotonin (often caused by overdose or interactions with other drugs and medicines) that can cause anxiety, alterations of consciousness, hyperactivity, tremors, vomiting, tachycardia, tachycardia, despondency, tremors, tachycardiatachycardia, incoordination, mydriasis, convulsions, respiratory problems or even death.

Contraindications

Regarding contraindications, one of the main ones is for those people who already suffer from liver problems, as well as coronary disorders. Also It is also contraindicated for people who consume certain drugs, especially and especially MAOIs, as it could generate serotonergic syndrome and even cause death.

Its administration together with SSRIs is not recommended.as they interact. Likewise, some retrovirals such as those used with HIV interact with this substance, being necessary that in case of using nefazodone (to treat depressions associated to the suffering of this disease) the doses and the possible interaction should be regulated to a great extent.

Minors and pregnant women should not take this drug. In addition, people with epilepsy or a history of suicide attempts should also not take this drug or should do so with special caution. Por lo general, no se recomienda en trastornos bipolares.

Referencias bibliográficas:

• Jufe, G. (2001). Psicofarmacología Práctica. Buenos Aires, Editorial Polemos.
• McConville, B.J.; Chaney, R.O.; Browne, K.L. et al. (1998). Newer antidepressants-beyond selective serotonin reuptake inhibitor antidepressants. Ped Clin North Am. 45:1157-71.
• Tatsumi, M.; Groshan, K.; Blakely, R.D. & Richelson, E. (1997). «Pharmacological Profile of Antidepressants and Related Compounds at Human Monoamine Transporters.». Eur J Pharmacol.340 (2–3): 249-258.