Bupropion is a selective inhibitor of dopamine and norepinephrine reuptake (ISRN). He was authorized in Spain by the Spanish Medicines Agency (AEMPS) in 2000 as an adjuvant in the detoxification of smoking.
Since 2007, it has also been included as an antidepressant and is currently funded by the national health system for the treatment of major depression.
- The mechanism of action of bupropion is not yet well defined; works by selectively inhibiting neuronal reuptake of dopamine (EA) and norepinephrine (NA).
- Thus increasing its concentration in synaptic space; However.
- The effect on Serotonin reuptake is less.
- Minimum.
It has also been observed that bupropion has an affinity for nicotine receptors. He would act as a non-competitive antagonist. Its action on NA may be related to nicotine withdrawal. Also, its effect on EA can influence the brain’s reward mechanisms.
Bupropion, also marketed as Elontril, is indicated as an antidepressant for major depression and is generally not a world-class drug.
Several studies have compared its efficacy and safety with certain selective serotonin reuptake inhibitors (SSRS) and venlafaxine, and conclude that their efficacy is similar to that of other antidepressants, but has been linked to a lower incidence of sexual disorders.
The starting dose is 150 mg per day. If no improvement is observed, after 4 weeks it can be increased to 300 mg per day in a single intake. Studies indicate that it begins to take effect within 14 days of treatment, although it takes several weeks to see the full antidepressant effect. It is recommended that treatment last at least 6 months.
Bupropion can be seen as an additional alternative in the treatment of major depression, especially for patients for whom sexual function is a relevant aspect.
Bupropion, marketed as Zyntabac, is indicated in patients with nicotine dependence. It aims to help them quit smoking. It should always be accompanied by motivational support.
It is recommended to start treatment before quitting smoking, you have to set a date for it in the first two weeks, the starting dose is 150 mg a day for 6 days, increasing to 300 mg (150 mg twice daily) on the seventh day. .
It is the first nicotine-free drug that has proven its effectiveness against smoking.
In 2016, the drug Mysimba was authorized: a combination of bupropion and naltrexone. It is indicated for weight management in obese adults, always accompanied by a reduced calorie diet and increased physical activity.
Another possible future therapeutic application of this drug is Attention Deficit Hyperactivity Disorder (ADHD), which could be an effective non-stimulant therapeutic option, as some studies show, so further research is needed.
In 2001, AEMPS issued an informative note warning of the risk of possible seizures with bupropion treatment. This is the most important side effect.
Most cases involve patients with risk factors, so before starting treatment it is important to evaluate them, as well as take precautions with the use of drugs that lower the crisis threshold, for example: antipsychotics, antidepressants, tramadol, theophiline. Etc.
Caution is recommended when administering other medicines simultaneously, due to the possibility of interactions.
The use of bupropion is contraindicated in combination with monoamine oxidase inhibitors (MAOI). The most common side effects of bupropion treatment are:
Quitting smoking is often related to many of these side effects due to nicotine withdrawal.
In 2009, the U. S. Regulatory Agency (FDA) warned of the risk of severe psychiatric symptoms when treated with this drug, for example: behavioral changes, suicidal thoughts, manic episodes, but other subsequent studies have failed to observe this relationship.
Finally, remember that bupropion is a drug that requires a prescription and requires medical supervision.