Iproclozide: Characteristics And Secondary Uses Of This Drug

Iproclozide

There are many psychotropic drugs that throughout history have been developed for the treatment of depression, from the accidental discovery (in reality 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 or have continued to be manufactured. And some of them have shown a relevant danger that has caused them to stop being used or have been withdrawn from sale.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 that was once effective but was discontinued due to its high hepatotoxicity.

What is iproclozide?

Iproclozide is an antidepressant drug 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 antidepressants, iproclozide is part of 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 type A and type B.

This group of drugs It is highly effective in the treatment of depressive symptoms, but whose potency can have dangerous effects on health and that can interact not only with other medications but also with different foods (which implies that its use requires exhaustive control and monitoring). That is why, over time, other safer drugs have been developed that have superseded both the medication that gives its name to this article and the rest of the MAOIs: first they were the tricyclics and later the specific serotonin reuptake inhibitors.

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Iproclozide is, as we have said, an effective drug in the treatment of depression, but As an irreversible MAOI, its use can generate dangerous side effects and has the potential to cause severe damage to the body, to the point of being associated with possible fulminant liver failure, with fatal potential, and even with several deaths. That is why it was withdrawn from sale and is no longer sold.

Mechanism of action

The mechanism of action of iproclozide is based on the destruction or blocking of the enzyme monoamine oxidase or MAO, a type of enzyme responsible for eliminating excess monoamine neurotransmitters (among which we find norepinephrine, serotonin and dopamine) that are generated. during nerve conduction through oxidation processes. There are two types of MAO, A, which is responsible for metabolizing serotonin and norepinephrine, and B, which does the same with dopamine.

The fact that this enzyme is inhibited will prevent said elimination from occurring, in such a way that monoamine levels in the brain increase: Thus, MAOIs are agonists of the different monoamines. Since norepinephrine and serotonin are essential in depression, this is very helpful in combating depressive symptoms.

As we have said, iproclozide is an irreversible and non-selective MAOI. The fact that it is irreversible means that it is not a blockade of MAO, but rather that it completely destroys the enzyme and its functioning in the brain (although it is synthesized again 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 rather it 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, can generate an alteration in blood pressure that sometimes becomes dangerous or even generate fatal cardiovascular events.

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Main indication

Although iproclozide is currently withdrawn from sale due to its high risk, it is a drug whose main indication was treatment of major depression and other alterations that cause depressive symptoms.

It also has a sedative and anxiolytic effect that helps combat anxiety states, which sometimes led to it being applied in cases of panic disorder. It has also been observed that it has 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 must be taken into account that it is highly dangerous. In fact, even other MAOIs that are still in force They 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 its effect in preventing the degradation of tyramine by MAO. And the fact is that the non-degradation of tyramine and its accumulation means that extreme hypertension can occur suddenly and unexpectedly, and even lead to cardiovascular problems, strokes and other similar problems. The risk of serotonin syndrome is also relevant.

Another of the riskiest aspects of iproclozide and one of the reasons why its production was paralyzed is because its strong hepatotoxicity having been found that in some cases it can cause severe liver problems such as fulminant liver failure and has even been linked to some deaths.

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Contraindications

Although iproclozide is a drug that has stopped being used and sold, it is worth keeping in mind that if it were used, its consumption would be contraindicated in different types of population (or constant monitoring of their status would be required).

To begin with, its effect on tyramine means that the consumption of certain foods rich in this substance should be avoided, such as cheese, meat, beer or sardines, among many others, given the risk of increased blood pressure. I would also totally be contraindicated in people with liver problems, as well as in those with cardiac or cardiovascular disorders. Pregnant and lactating women should also avoid it.

It is also contraindicated in people who are under treatment with other drugs such as analgesics, other antidepressants, drugs used in chemotherapy such as doxorubicin or products to relieve the respiratory tract such as aminophylline, among many others. This is because the interactions between these drugs They can excessively enhance the effects of one or alter its action on the body. Another sector that should avoid it is obviously those people who have an allergy to the drug or any of its components.