Nefazodone: uses and side effects of this antidepressant

There have been multiple psychotropic drugs that have been developed throughout history in order 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 substance in order to combat its symptoms.

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

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Nefazodone: basic characteristics of the drug

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

It is part of the so-called atypical antidepressants, as its mechanism of action does not coincide with that of other antidepressants. Specifically, it would be part of the group of drugs known as

Weak serotonin, norepinephrine, and dopamine reuptake inhibitors or SDRI, just like mazindol. Other substances have a similar function 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 necessary brain changes to see a real effect. This drug is an effective antidepressant, which also has with the advantage of hardly producing alterations at the sexual level, weight gain or appetite disturbances.

However, although it is an effective antidepressant, its prescription is not common and, in fact, between 2003 and 2004 its commercialization was suspended in different countries. (including Spain and the United States) because it was shown that it could pose a high risk to health as it is highly toxic at the liver level, and can even lead to death.

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Mechanism of action

The main mechanism of action of nefazodone is its action on the receptors of the different monoamines: serotonin, dopamine and norepinephrine. In a similar way to the MAOS Non-selective, 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 the postsynaptic level while inhibiting its reuptake. This generates an increase in serotonin levels in the brain. It also helps to inhibit the reuptake of norepinephrine and dopaminealbeit at a much lower level. Lastly too has a slight effect on histamine and acetylcholine levels, but the latter are practically negligible.

Uses and applications of this medicine

Nefazodone is primarily known as an antidepressant, with major depression being its main indication. It is also used in premenstrual syndrome or in other types of depression, such as that associated with suffering from various pathologies. However, in addition to the 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 in the post traumatic stress disorder, as well as insomnia problems, although the latency of the REM sleep.

Side effects of this antidepressant

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

The most common side effects of nefazodon are dry mouth and drowsiness, along with nausea and dizziness. The presence of confusion, vision problems and asthenia are also relatively common. More rarely, hypotension and bradycardia have been observed, something dangerous especially for those subjects who already suffer from cardiac pathologies.

However, the most serious problem associated with this drug (and which in fact led to its marketing interruption) is its high hepatotoxicity. In some cases, liver failure has been observed that can even lead to death, or jaundice. That is why if prescribed (something not very common), a continuous control must be exercised on the state of liver health of the patient, performing tests periodically. It can also have renal effects, since the drug is eliminated mainly by this route.

Another aspect to take into account is the risk of suffering from serotonin syndrome, a problem derived from from an excess of serotonin (often caused by overdose or interactions with other drugs and drugs) that May cause anxiety, altered consciousness, hyperactivity, tremors, vomiting, tachycardia, incoordination, mydriasis, seizures, respiratory problems or even death.

contraindications

With regard to contraindications, one of the main ones occurs in those people who already suffer from liver problems, as well as coronary disorders. Also It is contraindicated for people who consume certain drugs and especially MAOIs, since it could generate serotonin syndrome and even cause death.

Its administration together with SSRIs is not recommended., since they interact. Likewise, some retrovirals such as those used with HIV interact with this substance, making it necessary that if used nefazodone (to treat depression associated with suffering from this disease) the doses and the possible interaction.

Minors and pregnant women should not take this medicine. In addition, people with epilepsy or a history of suicide attempts should not take this medicine either or do so with special caution. Generally not recommended in bipolar disorders.

Bibliographic references:

• Jufe, G. (2001). Practical Psychopharmacology. 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.