Bupropion

The drug Bupropion is assigned to the drug class of antidepressants. It is also used to treat nicotine addiction.

What is bupropion?

Bupropion is a selective dopamine and norepinephrine reuptake inhibitor (NDRI). It also serves slightly to inhibit the uptake of serotonin.

Before 2000, bupropion was considered Amfebutamone known. The drug was approved in the USA since 1984. Since reports of sometimes fatal seizures increased after taking bupropion, the approval was withdrawn in 1986 and then re-issued in 1989 in a low dose. Bupropion has been approved in the United States for a single daily dose since 2003. In Germany, the drug was approved as an antidepressant in a retarded form in 2007. However, the drug was used as an antidepressant in off-label use even before this approval. For a long time, bupropion was only approved for smoking cessation in Switzerland. It has been used there since 2007 to treat depressive episodes. In Switzerland, however, bupropion therapy may only be initiated by a psychiatrist or a neurologist.

From a chemical point of view, bupropion belongs to the phenethylamines and to the subgroup of cathinones and amphetamines. The drug is closely related to the neurotransmitters dopamine, adrenaline and noradrenaline. Bupropion is a selective norepinephrine and dopamine reuptake inhibitor. The drug thus inhibits the uptake of noradrenaline and dopamine in the synaptic cleft.

Dopamine and norepinephrine are neurotransmitters. When an electrical impulse arrives at the synapse in front of a nerve cell, the presynaptic nerve cell releases the neurotransmitters into the so-called synaptic gap. The synaptic gap is a small gap between the two nerve cells. The neurotransmitters migrate from one nerve cell to the other. There they dock to a receptor on the postsynaptic neuron.

This triggers an electrical impulse. In a healthy person there is a balance between the neurotransmitters. In depressed people, the balance between the neurotransmitters is disturbed. The activity of the nerve cells that transmit the messenger substances norepinephrine and dopamine develops. Bupropion inhibits the uptake of noradrenaline and dopamine in the synaptic gap. As a result, the neurotransmitters remain in the synapse longer and the concentration of the neurotransmitters in the synaptic gap is increased with longer-term use. Thus, bupropion has a mood-enhancing and drive-boosting effect.

In addition, bupropion is also a so-called non-competitive antagonist on the cholinergic nicotine receptors. Non-competitive antagonists change the corresponding receptor in such a way that the original substance cannot trigger any or only a slight effect on the receptor.

Pharmacological effect

The main area of ​​application for bupropion is depression. Studies have shown that the effects of bupropion can be compared with the effectiveness of antidepressants from the class of active substances called selective serotonin reuptake inhibitors (SSRIs). Bupropion is more effective than SSRIs, especially in depression with psychological and physical fatigue.

In depression with anxiety symptoms, however, the SSRIs work better than bupropion. While sexual dysfunction is more common in treatment with SSRIs, these are very rarely observed in treatment with bupropion.

After therapy failure of the antidepressant citalopram, bupropion is also used in second-line therapy. It works just as well as venlafaxine, sertraline or buspirone. In a quarter of patients, treatment with the drug leads to a remission (temporary or permanent decrease in symptoms of the disease).

Bupropion is also used in smoking cessation. The effectiveness of the drug is comparable to the effectiveness of nicotine patches. However, the drug appears to be inferior to varenicline in the treatment of nicotine addiction.

Another indication for bupropion is attention deficit / hyperactivity disorder (ADHD). However, the drug has not been approved for this indication and has not been tested on patients under the age of 18 for its effectiveness or safety.

Manufacturer-financed studies also showed that bupropion leads to a reduction in appetite and thus leads to weight loss. It is not known whether the body weight will increase again after stopping the substance. In combination with the drug naltrexone, bupropion has proven to be an effective preparation for weight loss in obese patients. However, this combination product has not yet been officially approved.

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Risks & side effects

Common side effects of bupropion include insomnia and dry mouth. In addition, it can lead to headaches, muscle pain, loss of appetite, anxiety, difficulty concentrating and confusion. Bupropion can also cause priapism. Priapism is a painful permanent erection of the penis. Without treatment, this can lead to erectile dysfunction.

Bupropion must not be given together with MAOIs. Both drugs affect the catecholaminergic pathways, which can lead to severe interactions. If alcohol is consumed at the same time, the drug can cause neuropsychiatric side effects. If bupropion and drugs that lower the seizure threshold are administered at the same time, seizures can occur. These drugs include antidepressants, tramadol, systemic steroids, sedating antihistamines, and antimalarials.

The drug bupropion inhibits the CYP450-2D6 metabolic pathway. Since all tricyclics except Doxepin are metabolized in this way, blood levels can rise if the substances are taken at the same time. The effects of many pain relievers, antipsychotics, beta blockers, and antiarrhythmics can also be increased by bupropion. Despite a different metabolic pathway, the citalopram level also increases when taken at the same time.

Bupropion reduces the sedative effects of diazepam. If bupropion is used together with nicotine patches to quit smoking, the blood pressure can rise sharply.