Iproclozide: characteristics and side uses of this drug.
A type of antidepressant of the MAOI group, with dangerous side effects.
Many psychotropic drugs have been developed throughout history for the treatment of depression, since the accidental discovery (in fact a drug against tuberculosis was being sought) and the subsequent use of the first of them in subjects with depression.
But although we currently have a wide variety of them, the truth is that not all of those that were created have seen the light of day or have continued to be manufactured. And the fact is that some of them have shown a relevant danger that has caused them to stop being used or have been withdrawn from sale. This is the case of iproclozide, an antidepressant in its original form.an antidepressant that was once effective but was no longer marketed due to its high hepatotoxicity.
What is iproclozide?
Iproclozide is an antidepressant drugIt is a psychoactive substance whose properties and effects on the body are very useful to combat the symptoms of depression, such as low mood, anhedonia, fatigue and passivity.
Among the antidepressants, iproclozide belongs to the group of monoamine oxidase enzyme inhibitors or MAOIs, the first of the types of antidepressants that were synthesized. Specifically, it is a non-selective and irreversible MAOI, which means that it completely destroys the monoamine oxidase enzyme, both in its type A and type B.
This group of drugs is highly effective in the treatment of depressive symptoms.but whose potency can have dangerous effects on health and which can interact not only with other drugs but also with different foods (which means that their use requires exhaustive control and monitoring). For this reason, over time other safer drugs have been developed that have replaced both the drug that gives its name to this article and the rest of the MAOIs: first the tricyclics and later the specific serotonin reuptake inhibitors.
Iproclozide is, as we have said, an effective drug in the treatment of depression, but as an irreversible MAOI that is irreversible. as an irreversible MAOI, its use can generate dangerous side effects and has the potential to cause severe harm. and has the potential to cause severe damage to the organism, to the point of being associated with possible fulminant hepatic failure, potentially fatal, and even with several deaths. For this reason, it was withdrawn from sale and is no longer marketed.
Mechanism of action
The mechanism of action of iproclozide is based on the destruction or blockage of the enzyme monoamine oxidase or MAO, a type of enzyme responsible for eliminating excess monoamine neurotransmitters (including noradrenaline, serotonin and dopamine) that are generated during nerve conduction by oxidation processes. There are two types of MAO, the A that is in charge of metabolizing serotonin and noradrenaline and the B that does the same with dopamine.
The fact that this enzyme is inhibited means that this elimination does not take place, in such a way that the levels of monoamines in the brain are increased.Thus, MAOIs are agonists of the different monoamines. Since noradrenaline and serotonin are essential in depression, this is of great help in combating depressive symptoms.
As we have said, iproclozide is an irreversible and non-selective MAOI. The fact that it is irreversible implies that it is not an MAO blockade, but that it completely destroys the enzyme and its functioning in the brain (although it is re-synthesized and regenerated after two weeks). And with regard to its non-selectivity, we mean that its action is not restricted to a single type of MAO, but eliminates all types of this enzyme in the brain.
It also has an effect on tyramine, a substance that is part of many foods and whose excess is also eliminated by MAO. However, since there is no MAO after the action of iproclozide or other MAOIs, it accumulates, This can generate an alteration in blood pressure that can sometimes be dangerous, or even generate cardiovascular events.or even generate fatal cardiovascular events.
Main indication
Although iproclozide is currently withdrawn from sale because of its high risk, it is a drug whose main indication was for the treatment of major depression and other disorders with depressive symptomatology.
It also has a sedative and anxiolytic effect that helps to combat states of anxiety, which sometimes led it to be used in cases of panic disorder. It has also been observed to have a certain Anticonvulsant and anesthetic effect.
Risks and side effects
Iproclozide is a highly potent drug that affects our brain chemistry in a non-specific and irreversible way (temporarily). Although it has positive effects on disorders such as depression, it should be noted that it is very dangerous. In fact, even other MAOIs that are still in use today are only used in atypical depressions. and when other drugs have had no effect due to the large number of side effects and risks they have.
Some common and low-risk side effects would be drowsiness or insomnia, dizziness, dry mouth, gastric problems such as nausea and vomiting, constipation or diarrhea, weight gain, decreased libido or problems with urination.
But beyond that, they can also cause serious effects. One of the most relevant risks has to do with their effect in preventing the degradation of tyramine by MAO. The fact is that the non-degradation of tyramine and its accumulation can suddenly and unexpectedly cause extreme hypertension, and even lead to cardiovascular problems, strokes and other similar problems. The risk of serotonin syndrome is also relevant.
Another of the most risky aspects of iproclozide and one of the reasons why its production was stopped is its strong hepatotoxicity. its strong hepatotoxicityIt has been found that in some cases it can cause severe hepatic problems such as fulminant hepatic failure and has even been linked to some deaths.
Contraindications
Although iproclozide is a drug that is no longer used and sold, it is worth bearing in mind that if it were used, its consumption would be contraindicated in different types of population (or constant monitoring of their condition would be required).
To begin with, its effect on tyramine means that the consumption of certain foods rich in this substance, such as cheese, meat, beer or sardines among many others, should be avoided, given the risk of increased blood pressure. It would also be totally contraindicated in people with liver problems.as well as in those with cardiac or cardiovascular alterations. Pregnant women and nursing mothers should also avoid it.
It is also contraindicated in people who are under treatment with other drugs such as analgesics, other antidepressants, chemotherapy drugs such as doxorubicin or products to relieve the respiratory tract such as aminophylline, among many others. This is because interactions between these drugs the effects of one drug or alter its action on the organism. Another sector that should be avoided is obviously those who are allergic to the drug or to any of its components.
(Updated at Apr 12 / 2024)