Nefazodone: uses and side effects of this antidepressant
There have been multiple psychopharmaceuticals 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 their symptoms.
One of them is nefazodone, a little-known antidepressant and used of 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 psychotropic drug, derived from phenylpiperazines and synthesized with the purpose of alleviating and treating the symptomatology of 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 inhibitors of the reuptake of serotonin, noradrenaline and dopamine or SDRI, like the Mazindol. Other substances have a similar functioning although they act through different mechanisms of action, such as ketamine, cocaine and ecstasy.
As with most antidepressants, it takes time to make the necessary brain changes to visualize a real effect, this time being around four weeks. This drug is an effective antidepressant, which also has with the advantage of not producing hardly alterations at a sexual level, weight increases or alterations of appetite.
However, although it is an effective antidepressant, its prescription is not usual and in fact between 2003 and 2004 its marketing was suspended in different countries (including Spain and the United States) because it was shown that it could pose a high risk to health Being highly toxic at the liver level, it 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 noradrenaline. In a similar way to non-selective MAOIs, the action of the three main monoamines increases but at a weaker and controlled level.
It mainly acts as an antagonist of the 5-HT2 receptors of serotonin at postsynaptic level at the same time that it inhibits the reuptake of the same. This generates an increase in brain serotonin levels. It also helps to inhibit the reuptake of noradrenaline and dopamine, although at a much lower level. Finally, also has a slight effect at the level of histamine and acetylcholine , but these last ones are practically inappreciable.
Uses and applications of this medicine
Nefazodone is mainly 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 the suffering of various pathologies. But nevertheless, 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 see that nefazodone is useful in the treatment of various anxiety problems and in post-traumatic stress disorder, as well as in the face of insomnia problems, although it increases the latency of REM sleep.
Side effects of this antidepressant
Despite its great utility, the consumption of nefazodone can generate various side effects and in some cases may have its risks, there are different contraindications.
The most common side effects of nefazodon they are dry mouth and drowsiness, along with nausea and dizziness. The presence of confusion, vision problems and asthenia are also relatively common. Rarely, hypotension and bradycardia have been observed, something dangerous especially for those subjects who already suffer cardiac pathologies.
However, the most serious problem associated with this drug (and which in fact led to interrupting its commercialization) is its high hepatotoxicity. In some cases liver failures have been observed that can even lead to death, or jaundice. That is why if prescribed (something not very usual), a continuous control over the state of hepatic health must be exercised of the patient, performing tests periodically. It can also have kidney effects, by eliminating the drug mainly by this route.
Another aspect to consider is the risk of suffering a serotonin syndrome, a problem derived from an excess of serotonin (often caused by overdose or interactions with other drugs and drugs) can cause anxiety, disturbances of consciousness, hyperactivity, tremors, vomiting , tachycardia, incoordination, mydriasis, seizures, respiratory problems or even death.
Regarding the contraindications, one of the main ones occurs in those people who already suffer from liver problems, as well as coronary disorders. As well is contraindicated to people who use certain drugs and especially MAOIs, as it could generate serotonin syndrome and even cause death.
Its administration with SSRI is not recommended , since they interact. Likewise, some retrovirals such as those used with HIV interact with this substance, being necessary that if nefazodone is used (to treat depressions associated with the condition of this disease) the doses and the possible interaction are regulated to a great extent.
Children and pregnant women should not take this medicine. In addition, people with epilepsy or a history of suicide attempts should not use this medicine or do so with special caution. Generally, it is not recommended in bipolar disorders.
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- 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.