On September 30, 2013, a new antidepressant, vortioxetine (Brintellix) was approved by the Food and Drug Administation in the United States. The recommended starting dose is 10mg / day to be taken by mouth once a day with no preference on the timing of administration. The dose can be increased up to 20mg / day, but doses of 5mg have been shown to be effective in intolerant subjects at higher doses.
When a new drug is approved, there are questions to ask as psychiatrists: how much this new molecule differs from those already on the market in terms of tolerability and efficacy and how it can therefore constitute an additional opportunity for our patients. Since the discovery of tricyclics and MAOIs, new classes of antidepressants have been developed and approved over time, such as SSRIs (serotonin reuptake inhibitors), SNRIs (serotonin and norepinephrine inhibitors), bupropion (dopamine and noradrenaline), mirtazapine (adrenaline, noradrenaline, serotonin and histamine) and lately agomelatine (melatonin) in Europe.
Molecules with different mechanisms of action have been tested but most of them have failed. One exception is the great attention that has recently been pouring into ketamine and the N-Methyl-D-aspartate receptor antagonist which seems to promise pretty well.
Vortioxetine is considered a multimodal antidepressant: it acts as an antagonist on 5-HT3A and 5-HT7 receptors, partial agonist on 5-HT1B receptors and 5-HT1A agonist, determining a potent inhibition of serotonin reuptake. Pre-clinical data suggest that these multiple and unique effects on different serotonin receptors result in increased regional transmission of norepinephrine, dopamine and glutamate.
Vortioetine is metabolised by several liver enzymes (e.g. CYP2D6, CYP2C9, CYP3A4 / 5, CYP2A6 and CYP2C19) and blood levels do not appear to be significantly affected by concomitant intake of other drugs. The half-life is approximately 57 hours and withdrawal symptoms after a missed dose or abrupt discontinuation of treatment are uncommon. The most frequently reported side effects were nausea (10-20%), headache (15%), diarrhea (7-11%), xerostomia and hyperhidrosis (less frequent). The alleged benefits from the use of this drug would be low sleepiness and insomnia, low tendency to weight gain, fewer side effects on the sexual sphere compared to serotonergics.
At the end of last December, vortioxetine received marketing approval from the European Commission. There is currently no information on the fate of the drug in Italy.
25 comments
# 1
User 215XXX
February 07, 2015
a new hope for those suffering from this pathology that would seem not to affect sleep
one thing I do not understand, being depression, often accompanied by insomnia problems, because there are so few antidepressants that can also treat this problem
# 2
Insomnia is generally a symptom of depression does not cause it: In general, if the antidepressant works, sleep is one of the first symptoms to return so it is often possible to avoid the use of hypnotics which over time can cause addiction. The sedation that some antidepressants cause is to be considered a side effect and is attributable to an antihistamine action. Although this effect can sometimes be exploited (as in the case of mirtazapine, trazodone or many of the tricyclics) the risk is to pay a price in terms of cognitive performance which in cases of depression is often affected (deficit of concentration and memory e.g.).
#3
Insomnia is generally a symptom of depression does not cause it: In general, if the antidepressant works, sleep is one of the first symptoms to return so it is often possible to avoid the use of hypnotics which over time can cause addiction. The sedation that some antidepressants cause is to be considered a side effect and is attributable to an antihistamine action. Although this effect can sometimes be exploited (as in the case of mirtazapine, trazodone or many of the tricyclics) the risk is to pay a price in terms of cognitive performance which in cases of depression is often affected (deficit of concentration and memory e.g.).
# 4
User 215XXX
February 12, 2015
so it can be said that if after 2/3 months of therapy with an antidepressant, if the patient continues to suffer from insomnia, and therefore continues to need, another category of drugs in order to to sleep, the antidepressant used is not good and it is necessary to look for another molecule ..
I ask you on this topic because, some time ago, I talked about it with my family doctor, who told me that it is difficult with the antidepressant alone (I refer to ssri) the problem of insomnia is solved, even when the mood improves (she was referring precisely to a therapeutic experience she lived in the first person) ..
Thanks for the explanations Doctor Bova
# 5
# 6
User 234XXX
February 28, 2015
It would be interesting to know how much it affects weight gain and male sexuality (delayed ejaculation and desire)
# 7
User 152XXX
01 May 2015
Dear Dr Francesco Bova, I suffer from chronic endogenous depression and I would like to ask you if the new antidepressant that it will have to come out and different from the current ones only for the fact that it should have an almost immediate effect or above all because it could be effective where the current drugs have had “not enough”
I have been treated with several antidepressants but they have never been “enough”, the penultimate was cipralex, the current one is duloxetine which, compared to cipralex, gives me more results but with important side effects especially at a sexual / orgasmic / ejaculation level / libido and also urination;
I read that the new molecule should also have quite less negative effects on libido, ejaculation, etc. but, I wonder: if the duloextine that acts on seretonin and noradrenaline gives me these important side effects, then the vortioxetine that would act not only on seretonin and noradrenaline also on dopamine and perhaps other neurotransmitters … …. then it shouldn’t cause me even more sexual side effects
I understand that, as I have been told, clinical practice has some differences with the literature but in light of how much “little” is still known, it is possible to have some answers on what I ask above (always taking into account that it may not be so on my person)
Thank you and best regards
# 8
Unfortunately, I cannot answer you precisely. You know that the reported effect of drugs is an average effect that is derived from statistical data. It is therefore not possible to make a reliable prediction on a single case. The literature data promises a greater tolerability than the drugs currently on the market, but my experience of recent years advises me to be cautious. In any case, new drugs with an alternative profile are always a new opportunity and inevitably constitute a hope for those who have not managed to have a satisfactory effect with current therapies. So let’s wait for vortioxetine to prove itself.
# 9
User 152XXX
May 13, 2015
Thank you so much for your kind reply. Dr. Francesco Bova,
I understand what he says, in any case, reading in American forums I see that with vortioxetine few have complained of sexual problems and this gives me hope, but not a few have claimed to have had severe itching or severe nausea which, if they will be transient and only to start treatment then a bit of sacrifice until they disappear will not be the end of the world, but in the hope that precisely if there will be that then they will go away and do not cause the suspension of the treatment as happened for some.
However, many have written that at the level of depression they have had good results and some of them, like me, had first tried other antidepressants but with poor or unsatisfactory results ……….. so even if I understand that in any case and if, I like to hope that this new drug in me can produce effective antidepressant effects and few or very few unwanted sexual effects ………… always if in Italy it will ever be available, why not I hide, dear doctor, that the fact that it is not yet on the market makes me quite angry, I do not understand why it takes so long and why those in duty take it so easy.
To date, we still have no idea when we will be able to use it. It may
be that it will be available next month as well as in December or 2016
Thanks again and best regards
# 10
User 128XXX
05 June 2015
Hello, I have been suffering from panic attacks for many years, I would like to know if this new drug “VORTIOXETINA” is also indicated for my pathology.
Thanks
# 11
I have no direct experience but in general I would say no. However, it has no specific indication other than for depression.
# 12
User 128XXX
June 08, 2015
Thanks for answering me; I still take this opportunity to ask you which drug or molecule is more effective for panic attacks and which one has fewer side effects, in particular weight gain and sexual disorders.
Greetings
# 13
User 383XXX
June 13, 2015
Dear Doctor Bova, I understand that the drug is currently available in Italy, you can confirm this.
If I’m wrong, I apologize and ask you when it will be available in our pharmacies. Thank you for your attention,
Best regards.
Alex
# 14
I am not aware that the drug is currently on the market. The authorization was granted a few months ago. I’m afraid there are issues with mutability …
# 15
User 383XXX
June 13, 2015
Thank you very much Dr. Bovia for your quick reply. I am very hopeful towards this new drug having tried various antidepressants that promptly gave me not negligible effects in my sexual life. What do you think about it Finally an
antidepressant has arrived with more
tolerable
side
effects on the sexual sphere
. and disorders of the sexual sphere.
Greetings
# 17
It is difficult to elect a drug as the best for a given pathology. The best drug is the most effective for the individual patient. As a guideline, we know that increased appetite is correlated with antihistamine effects and that in panic the drug is more manageable and usually not very activating. The least activating drugs are those that have higher antihistamine activity. As you see, it is not easy to answer your question. Speaking with his patient, the psychiatrist generally formulates a hypothesis of therapy that seems to be the best possible in this specific case. With the collaboration of the patient himself, he will make the necessary adjustments to have the best tolerability profile. Psychiatry as he sees it is not a field of competition but a healthy exercise in patience. Best regards.
# 18
User 128XXX
May 12, 2016
Good morning after being treated (panic attacks) with paroxetine and having found that despite being an effective drug for my pathology, it caused me side effects related to the sexual sphere and weight gain, my The doctor prescribed me fluoxetine which improved the unwanted effect on a sexual level, but not the one related to weight, on the contrary it made it worse. Give me some advice to improve this aspect as well, maybe some drugs that compensate for this effect.
thanks
# 19
User 240XXX
May 31, 2016
I have been on brintellix 10mg for 8 days. You understand that the drug may cause tiredness, sleepiness or insomnia
The most appropriate time of intake which would be
You already have experience with patients treated with this molecule
Greetings
# 20
I do not yet have direct experience (which derives from the use of the drug on a sufficient number of patients). The drug should be taken electively in the morning and should be free of sedative effects. This means that a possible evening intake can cause some difficulty in sleeping. In 8 days any prediction is difficult because as you know insomnia and drowsiness can be symptoms of different depressive pictures as well as fatigue. Be patient and consult your psychiatrist who knows the drug as much as I do and your patient much better.
Sincerely
# 21
User 240XXX
May 31, 2016
Thanks doctor I ask you one last thing, I measured the pressure 107/65 it seems to me a bit low it may be due to the drug
Thanks
# 22
Psychiatrist
June 09 2016
# 23
User 420XXX
August 17 2016
good morning
I have been using it for two months now 5mg Brintellix every morning, the nausea that was supposed to be transient continues, my doctor is temporarily unavailable and I, frankly, exasperated by this nausea (I also noticed a weight gain) I would like to stop it! can you kindly tell me how I should behave to do it .
Sincerely
# 24
Dear lady, I think that a momentary absence of your trusted psychiatrist leads us to assume a prompt return. After two months of therapy, I think she can afford to wait for her return to decide on alternative strategies. Having a trusted specialist is a fundamental prerequisite for a successful treatment outcome. Sincerely
# 25
User 648XXX
February 05, 2022
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