Discover the contraindications and side effects of Bupropion.

This psychotropic drug is used both to treat depressive symptoms and in tobacco addiction.

A drug belonging to the IRND.

Tobacco is one of the substances with psychoactive effects that have been used the most legally since its discovery.

Even though today smoking is prohibited in establishments and closed public spaces and its price has risen based on taxes, millions of people still have the habit of smoking.

But many of these people, at some point, need to stop. Although it is possible to do it voluntarily, in some cases they may require psychological and even pharmacological help.

In the latter case, one of the existing drugs used to quit smoking is bupropion, a drug that originated as an antidepressant.

What is bupropion?

Bupropion is a well-known antidepressant drug, although more than in its application for depression it is more common and distinctive due to its efficacy in the treatment of tobacco addiction.

In this sense, it is a treatment that does not include nicotine and that is recommended together with some type of therapy or psychological treatment.

This shows that psychotropic drugs are not designed following a plan from scratch, but rather that there is a certain process of trial and error in their development, and that sometimes there are benefits for the drug that were not even taken into account at first.

Bupropion is a specific dopamine and norepinephrine reuptake inhibitor, or NRDI , that works by increasing the levels of these neurotransmitters in the brain.

Compared with other drugs in the group of antidepressants, bupropion has the advantage of not causing sexual dysfunctions, although, on the other hand, its effectiveness alone seems less compared to other drugs on the market.

Thus, bupropion is an example that molecules related to other substances used for a certain class of disorder may be more useful in different health conditions, no matter how similar their structure is.

Mechanism of action

The function of bupropion and its mechanism of action is based on its role as a selective inhibitor of dopamine and norepinephrine reuptake.

This implies that bupropion works by preventing these two transmitters (associated with gratification and energy) from being re-uploaded by the presynaptic neuron, in such a way that they are available to postsynaptic neurons for a longer time.

Furthermore, it appears to stimulate the secretion of these neurotransmitters.

Thus, dopamine and norepinephrine levels and their transport increase at the brain level, something that can alter the mood.

Likewise, it has also been observed that it has an effect at the level of acetylcholine, binding to nicotinic receptors and exerting a non-competitive antagonistic effect.

Although there is no total security for this, this element is one of the possible explanations for its role in smoking cessation.

However, it must be taken into account that the exact way in which the mechanism of action of bupropion and psychotropic drugs in general works is still unknown.

Its use does not guarantee that it will work to alleviate the symptoms of the disorder to be treated, and its efficacy is only slightly better than that of a placebo.

That does not mean that in many cases it is very useful, simply that the percentage of patients who try this treatment and do not obtain any benefit is relatively high.

Indications: uses in disorders

Bupropion is a drug that has had various uses throughout its history. Although it was born as an antidepressant and today it is still used to treat this condition both as monotherapy (single therapy) and combined therapy (more common, to enhance some specific antidepressants when first-line drugs are not effective), the truth is is that by itself it is generally considered less effective than other antidepressants.

Where this drug stands out and has the greatest use is in smoking cessation, being effective in reducing the consumption habit and the urge to smoke.

In this sense, its mechanism of action seems to contribute to stopping craving (possibly due, on the one hand, to its antagonism of nicotinic receptors and its interaction with brain dopamine, although the exact mechanism is not fully known).

Another disorder in which it is used is seasonal affective disorder, in which depressive episodes appear associated with certain times of the year.

In addition to the above, it has sometimes been used in the treatment of bipolar disorder, especially during the depressive episodes that can occur in this disorder (although this use requires caution since there is a risk of turning the disorder into a manic crisis).

Also in ADHD. But in any case, further research is required and possible risks must be taken into account.

Side effects of Bupropion

Bupropion is a drug that is very useful in smoking cessation and is used in cases of depression, but as with other drugs, its clinical utility is not free of risks and possible side effects.

This occurs because the active substance in bupropion affects many areas of the body, not just the areas that could produce an improvement in symptoms.

This unwanted interaction generates a chain reaction of consequences to some extent unpredictable, which can lead to new health disorders (although they tend to disappear as the substance leaves the body). Therefore, its use should always be supervised and indicated by doctors.

In this sense, among the main side effects of bupropion, we can find the cause of insomnia (being one of the most frequent), dry mouth and dizziness, headaches, nausea, constipation, rapid heartbeat, tremors, skin rashes, agitation, and nervousness. It can also cause a decrease in appetite.

In more serious cases it can generate seizures (this being one of the most well-known serious risks), arrhythmias, hallucinations, panic or difficulties in breathing or feeding, or inflammations being necessary to see a doctor. In some cases, it can cause irritability, hostility, depression, suicidal thoughts.

Contraindications of Bupropion

In addition to these side effects, this drug is contraindicated in some sections of the population.

People who are allergic to it or any of its components (something obvious on the other hand), those who consume certain medications (especially MAOS), dependence on substances other than tobacco (such as alcohol, drugs, and pharmaceuticals), and those who suffer from epilepsy, brain tumors and anorexia nervosa or bulimia (since it reduces the appetite).

It is also not recommended, although it can sometimes be used if the benefits are considered greater than the risks, in cases of people with kidney or liver failure, head trauma, insomnia, or the use of other medications that may interact with bupropion.

Diabetics, alcoholics, hypertensive or people with psychiatric disorders (since it can contribute to the appearance of mania in bipolar or psychotic crisis in schizophrenia, among others) also have it contraindicated (or at least the treatment should be done with a high level of control of the patient’s condition and the doses administered) due to the risk of seizures and other side effects.

Finally, it is not recommended for pregnant and lactating women either