Iproniazid: uses and side effects of this psychotropic drug

It was one of the first Antidepressant drugs, and was discovered by chance.

Depression is a mental health problem that has accompanied human beings throughout history. Already in ancient Greece, melancholy was spoken of as a disease with characteristics similar to what we would consider depression today, with a sad and anhedonic mood. Being nowadays one of the most prevalent disorders worldwide, the search for an effective treatment has generated great interest over time and has become an increasingly pressing need.

Various methods have been employed to treat this condition, including psychopharmacology. One of the first drugs to be found and synthesized was iproniazid, which will be discussed below.which will be discussed in this article.

Iproniazid: the first MAOI

Iproniazid is a psychopharmaceutical classified as an antidepressant that is also of great historical importance. It is one of the first antidepressants synthesized, along with substances such as imipramine.

Its discovery was actually by chance, by serendipityIts synthesis was aimed at finding a drug that would be effective against tuberculosis. In trials with tuberculosis patients, it was observed that it had a mood elevating effect, something that would eventually be analyzed and applied to the population with depressive disorders (specifically, its use would be approved in 1958).

This drug is part of the group of monoamine oxidase inhibitors or MAOIs, which affect the nervous system by blocking the metabolization of certain neurotransmitters. Iproniazid is in fact the firstthe first of the MAOIs to be marketed and was, together with other substances derived from it, one of the treatments of choice for patients with depression. Its action is non-specific and irreversible, and its effects continue for at least fifteen days.

In terms of effects, its application generates an increase in mood and activation, being effective in the treatment of depressive symptomatology and reducing inactivity and passivity of those who use it.

However, the observation of the existence of strong side effects that put the health of those who consumed it at risk, among which the following stand out severe hepatic problems and the increase of arterial hypertension to dangerous levels.In the case of iproniazid, it is no longer marketed because it is very dangerous in terms of toxicity and can only be found in some countries. In the case of iproniazid in question, it is no longer marketed because it is very dangerous in terms of toxicity and can only be found in some countries.

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Mechanism of action.

Iproniazid is, as we have said, a non-selective irreversible monoamine oxidase inhibitor or MAOI. As an MAOI, it exerts its effects at brain level by inhibiting an enzyme, MAO, whose main function is to degrade monoamines by oxidation in order to eliminate the excess of neurotransmitters generated by monoaminergic neurons. (which are those that generate dopamine, noradrenaline and serotonin) in the synaptic space as well as tyramine.

Thus, inhibiting monoamine oxidase would not produce this destruction of monoamines, so that the levels of serotonin, noradrenaline and dopamine would increase in the brain. The action of iproniazid, therefore, would be fundamentally of the agonist type with respect to monoamines, favoring their action. This will generate an improvement of the depressive symptomatology by increasing neurotransmitters that are diminished in major depression.

It is important to take into account that there are two types of monoamine oxidase: MAO A and MAO B. The first is linked to and responsible for metabolizing and destroying excess noradrenaline, serotonin and tyramine, the first two being the substances most linked to depression. MAO B does the same with dopamine, influencing tyramine as well as the former.

The fact that it is considered irreversible and non-selective implies that iproniazid acts on all types of MAO, such that it is not just that monoamine oxidase is reduced but that it is completely destroyed from our brain. it is not only that monoamine oxidase is reduced but that it is completely destroyed from our brains until it synthesizes more again (something that can take about fifteen days). But the truth is that the enzyme in question is useful to the brain, and the increase of neurotransmitters that it generates (especially in the case of tyramine and noradrenaline) can have dangerous effects on health.

Main indications

Iproniazid is a drug that is not currently marketed due to the high level of risk it poses in terms of liver toxicity and the existence of much safer drugs with fewer side effects.

However, However, the main indication for this drug was in cases of major depression.It was effective in the treatment of mood symptoms (which it contributed to increase) and anhedonia and fatigue sensation. Likewise, occasionally it has also been used for the purpose for which it was in fact initially intended: the treatment of tuberculosis.

Side effects, contraindications and risks

Iproniazid is a drug that is very useful in the treatment of depressive symptomatology, but as we have mentioned, it has been withdrawn from the market due to its high level of risk and the side effects it has. In this regard, some of the best known side effects of iproniazid, which in fact it shares with some other MAOIs, are the following.

First and foremost, one of the main reasons for its withdrawal is the high level of toxicity that this drug can have on the liver.. Another of the possible side effects with the greatest risk is the appearance of severe hypertensive crises due to its interaction with a large number of foods rich in proteins, which can even contribute to the appearance of strokes or potentially fatal cardiac and vascular problems.

It can also cause kidney problems. Other less serious symptoms are the appearance of insomnia, weight gain and difficulties or impossibility to reach orgasm, delayed ejaculation or decreased libido.

All this means that there are certain types of people who are totally contraindicated for this medication. In this sense, all those people who suffer from some kind of pathology or liver damage, as well as those with heart disease or kidney problems stand out. People who need a high protein diet are also highly contraindicated.. People with diabetes and celiac disease should not take this drug either. Iproniazid and other MAOIs have a high level of interaction with other drugs, being also contraindicated its use with other antidepressants and other drugs.