Definition
Bupropion is a selective catecholamine (norepinephrine and dopamine) reuptake inhibitor. It has only a small effect on serotonin reuptake. It does not inhibit MAO. The antidepressant effect of bupropion is considered to be mediated by its dopaminergic and noradrenergic action. Bupropion has also been shown to act as a competitive alpha-3-beta-4- nicotinic antagonist, the alpha-3-beta-4-antagonism has been shown to interrupt addiction in studies of other drugs such as ibogaine. This alpha-3-beta-4-antagonism correlates quite well with the observed effect of interrupting addiction.; A unicyclic, aminoketone antidepressant. The mechanism of its therapeutic actions is not well understood, but it does appear to block dopamine uptake. The hydrochloride is available as an aid to smoking cessation treatment; Bupropion is a selective catecholamine (norepinephrine and dopamine) reuptake inhibitor. It has only a small effect on serotonin reuptake. It does not inhibit MAO. The antidepressant effect of bupropion is considered to be mediated by its dopaminergic and noradrenergic action. Bupropion has also been shown to act as a competitive alpha-3-beta-4-nicotinic antagonist, the alpha-3-beta-4-antagonism has been shown to interrupt addiction in studies of other drugs such as ibogaine. This alpha-3-beta-4-antagonism correlates quite well with the observed effect of interrupting addiction. Bupropion (amfebutamone) (brand names Wellbutrin and Zyban) is an antidepressant of the aminoketone class, chemically unrelated to tricyclics or selective serotonin reuptake inhibitors (SSRIs). It is similar in structure to the stimulant cathinone, and to phenethylamines in general. It is a chemical derivative of diethylpropion, an amphetamine-like substance used as an anorectic. Bupropion is both a dopamine reuptake inhibitor and a norepinephrine reuptake inhibitor. It is often used as a smoking cessation aid. [HMDB]
Description
Bupropion is a selective catecholamine (norepinephrine and dopamine) reuptake inhibitor. It has only a small effect on serotonin reuptake. It does not inhibit MAO. The antidepressant effect of bupropion is considered to be mediated by its dopaminergic and noradrenergic action. Bupropion has also been shown to act as a competitive alpha-3-beta-4- nicotinic antagonist, the alpha-3-beta-4-antagonism has been shown to interrupt addiction in studies of other drugs such as ibogaine. This alpha-3-beta-4-antagonism correlates quite well with the observed effect of interrupting addiction. A unicyclic, aminoketone antidepressant. The mechanism of its therapeutic actions is not well understood, but it does appear to block dopamine uptake. The hydrochloride is available as an aid to smoking cessation treatment; Bupropion is a selective catecholamine (norepinephrine and dopamine) reuptake inhibitor. It has only a small effect on serotonin reuptake. It does not inhibit MAO. The antidepressant effect of bupropion is considered to be mediated by its dopaminergic and noradrenergic action. Bupropion has also been shown to act as a competitive alpha-3-beta-4-nicotinic antagonist, the alpha-3-beta-4-antagonism has been shown to interrupt addiction in studies of other drugs such as ibogaine. This alpha-3-beta-4-antagonism correlates quite well with the observed effect of interrupting addiction. Bupropion (amfebutamone) (brand names Wellbutrin and Zyban) is an antidepressant of the aminoketone class, chemically unrelated to tricyclics or selective serotonin reuptake inhibitors (SSRIs). It is similar in structure to the stimulant cathinone, and to phenethylamines in general. It is a chemical derivative of diethylpropion, an amphetamine-like substance used as an anorectic. Bupropion is both a dopamine reuptake inhibitor and a norepinephrine reuptake inhibitor. It is often used as a smoking cessation aid.
Top Gene Interactions
Related Pathways
General Information
- Metabolism:
Reduction of the carbonyl groupand/or hydroxylation of the tert-butyl group of bupropion. Route of Elimination: Bupropion is extensively metabolized in humans. Oxidation of the bupropion side chain results in the formation of a glycine conjugate of metachlorobenzoic acid, which is then excreted as the major urinary metabolite. Following oral administration of 200 mg of 14C-bupropion in humans, 87% and 10% of the radioactive dose were recovered in the urine and feces, respectively. However, the fraction of the oral dose of bupropion excreted unchanged was only 0.5%, a finding consistent with the extensive metabolism of bupropion. Half Life: 24 hours
- Uses/Sources:
For the treatment of depression and as aid to smoking cessation.
- Symptoms:
Symptoms of overdose include seizures, hallucinations, loss of consciousness, tachycardia, and cardiac arrest.
- Treatment:
Ensure an adequate airway, oxygenation, and ventilation. Monitor cardiac rhythm and vital signs. EEG monitoring is also recommended for the first 48 hours post-ingestion. General supportive and symptomatic measures are also recommended. Induction of emesis is not recommended. Activated charcoal should be administered. There is no experience with the use of forced diuresis, dialysis, hemoperfusion, or exchange transfusion in the management of bupropion overdoses. No specific antidotes for bupropion are known. Due to the dose-related risk of seizures with Bupropion, hospitalization following suspected overdose should be considered. Based on studies in animals, it is recommended that seizures be treated with intravenous benzodiazepine administration and other supportive measures, as appropriate. (L1712)
- Route of Exposure:
For sustained release, peak plasma concentrations are achieved within 3 hours.
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Neuronal acetylcholine receptor subunit alpha-4 Neuronal acetylcholine receptor subunit alpha-7 Muscarinic acetylcholine receptor M1 Muscarinic acetylcholine receptor M2 Muscarinic acetylcholine receptor M3 Muscarinic acetylcholine receptor M4 Neuronal acetylcholine receptor subunit alpha-3 5-hydroxytryptamine receptor 2C 5-hydroxytryptamine receptor 1A Sodium-dependent serotonin transporter Alpha-2A adrenergic receptor Histamine H1 receptor |
12431845 9537821 19821577 12723940 20509659 8100134 9862757 16033252 10991997 20158204 21058665 7855217 |
|
Sodium-dependent dopamine transporter Sodium-dependent noradrenaline transporter |
Bupropion selectively inhibits the neuronal reuptake of dopamine, norepinephrine, and serotonin; actions on dopaminergic systems are more significant than imipramine or amitriptyline whereas the blockade of norepinephrine and serotonin reuptake at the neuronal membrane is weaker for bupropion than for tricyclic antidepressants. The increase in norepinephrine may attenuate nicotine withdrawal symptoms and the increase in dopamine at neuronal sites may reduce nicotine cravings and the urge to smoke. Bupropion exhibits moderate anticholinergic effects. |
12909199 12431845 9537821 14550679 15787205 12183670 12589396 19821577 12723940 20509659 11752352 19442525 8302271 20158204 16893531 21058665 12185406 |
Bupropion (Wellbutrin, Zyban) Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Reperfusion Injury | 12.33 |
|
Major Affective Disorder 1 | 11.19 |
|
Protein Deficiency | 9.43 |
|
Hepatitis, Chronic | 9.31 |
|
Turner Syndrome | 9.16 |
|
Status Epilepticus | 9.12 |
|
Asphyxia Neonatorum | 8.92 |
|
Glioma | 8.64 |
|
TOBACCO ADDICTION, SUSCEPTIBILITY TO | 8.38 |
|
Myocardial Reperfusion Injury | 8.16 |
|
Marfan Syndrome | 8.1 |
|
Brain Ischemia | 7.88 |
|
Retinal Detachment | 7.59 |
|
Nervous System Diseases | 7.54 |
|
Ureteral Calculi | 7.3 |
|
Major Depression | 7.19 |
|
Diabetes Mellitus, Experimental | 7.14 |
|
Trigeminal Neuralgia | 7.01 |
|
Diabetes Mellitus, Type 2 | 6.85 |
|
Amphetamine-Related Disorders | 6.59 |