Bupropion is administered orally, in the form of immediate-release, sustained-release (SR), and extended-release (XL).
Immediate-Release: Usually taken three times a day, this type of bupropion releases the medication into the bloodstream quickly.
Sustained-Release (SR): Usually taken twice a day, this type of bupropion releases the medication slowly.
Extended-Release (XL): This type of formulation is taken once a day and provides a steady release of the medication over the course of the day, leading to a more consistent effect.
Patients should strictly follow the healthcare provider’s prescription on the specific dose and frequency because the dose is based on the illness to be treated.
Smoking cessation: In smoking cessation, bupropion, or Zyban, is usually initiated one to two weeks before the quit date. The usual dose is 150 mg per day for the first three to six days then increased to 300 mg per day.
Depression: For the treatment of major depressive disorder, bupropion commonly begins at 150 mg a day for the first 3–4 days and then can be raised to 300 mg a day or, in a few cases, up to 400 mg a day in divided doses.
It is essential to take bupropion exactly as prescribed and to avoid taking more than the recommended dose, as higher doses can increase the risk of seizures (a rare but serious side effect).
Bupropion acts on the neurotransmitters that control mood, energy, and emotional activities, including dopamine and norepinephrine. The specific mechanism through which bupropion treats depression and anxiety is not well understood; it is believed to:
Inhibit the reuptake of norepinephrine and dopamine: Bupropion blocks the reabsorption of these neurotransmitters in the brain, which increases their levels and activity in synapses. This leads to improved mood and increased energy for individuals with depression or anxiety.
Unlike SSRIs and SNRIs: While other antidepressants primarily affect serotonin, a neurotransmitter which plays a role in mood, bupropion’s pharmacological profile is different by virtue of its action on dopamine and norepinephrine; it is often better for people who have not responded to other antidepressants.
Smoking cessation: Bupropion reduces the urge and withdrawal symptoms of smoking cessation through the action on dopamine. This medication may correct the imbalanced dopamine caused by smoking that contributes to nicotine addiction.
Although bupropion is usually well tolerated, it may also lead to side effects. Among them are common and dangerous ones as follows:
Seizures: One of the most dangerous adverse effects of bupropion is seizure, especially at high dosages. This effect occurs more frequently in those suffering from other conditions, such as an eating disorder (e.g., anorexia or bulimia) or who have experienced seizures in the past.
Suicidal Thoughts: Like many other antidepressants, there is an increased risk of suicidal thoughts or behavior in children, adolescents, and young adults. They must be closely monitored, especially within the first few weeks of initiating treatment or if their dosage is changed.
Risk of Seizure: Bupropion increases the risk of seizure, especially among individuals with a history of seizures, eating disorders, alcohol or drug withdrawal, or concomitant therapy with drugs that decrease the seizure threshold.
Liver and Kidney Function: People with liver or kidney impairment should be cautious with bupropion since it is metabolized in the liver. Dosage adjustment may be necessary.
Alcohol Use: Alcohol consumption should be minimized or avoided during treatment with bupropion, as it may increase the risk of seizures and other side effects.
Pregnancy: Bupropion is classified as a Category C drug during pregnancy, meaning that it should be used only if the potential benefits outweigh the risks.
- Monoamine Oxidase Inhibitors (MAOIs): Combining bupropion with MAOIs (e.g., phenelzine or tranylcypromine) can increase the risk of serious side effects like hypertensive crisis and serotonin syndrome. A 14-day gap is recommended between discontinuing an MAOI and starting bupropion.
- CYP2B6 Inhibitors: Drugs like ticlopidine or clopidogrel, which inhibit CYP2B6, can increase bupropion levels, raising the risk of side effects like seizures or agitation, which is a known risk with bupropion.
- Alcohol: Bupropion combined with alcohol can increase the risk of neuropsychiatric side effects like seizures and may lower the seizure threshold, particularly in high alcohol consumption.
- Other Antidepressants: Using bupropion with other antidepressants, especially SSRIs or SNRIs (like fluoxetine or venlafaxine), may increase the risk of serotonin syndrome, a serious condition caused by excessive serotonin.
These interactions highlight the importance of monitoring and possibly adjusting doses when combining bupropion with other medications.
Bupropion is supplied in several formulations; dosage is determined by indication; for Depression (Wellbutrin): an initial dose is 150 mg/day, best taken in the morning; a higher dose can be initiated to 300 mg/day following days 3–4 of the dosing regimen and may, in fact, go up to 400 mg in divided doses; for Smoking Cessation (Zyban): the first dose should be 150 mg per day and commenced one to two weeks prior to quitting smoking.
Maintenance dose: After 3 to 6 days, the dose can be titrated up to 300 mg/day.
For Weight Loss (Contrave)
The usual dosage is 8 to 12 mg of bupropion per day combined with naltrexone.
Bupropion is a prescription-only medication. It should be prescribed only by a licensed healthcare provider after proper assessment of the patient’s medical history and weighing of the risks and benefits of treatment.