Bupropion

Bupropion - Use | Dose | Side Effects

Bupropion is a drug that belongs to a group of medicines called norepinephrine and dopamine reuptake inhibitors. It exhibits a very weak effect on the serotonin reuptake inhibition and it does not exhibit an inhibitory effect on an enzyme called monoamine oxidase.

Bupropion is used to treat major depression and for smoking cessation.

Contraindications and precautions

Bupropion is contraindicated in the following conditions:

  • In patients with epilepsy. Bupropion may cause grand mal seizures and convulsions1,2 and must not be used in patients that suffer from epilepsy.
  • In patients with cirrhosis or liver failure. Bupropion can lead to acute hepatitis and must be avoided in these patients.3
  • In patients suffering from eating disorders (anorexia and bulimia nervosa)
  • In patients who are taking (or have taken in the past two weeks) medicines called MAO inhibitors (also used to treat depression)

Never apply a higher dose than recommended by your doctor, because the use of high doses increases the risk of seizures. Studies have shown that every 1,000th patient who is taking 450 mg of Bupropion per day experience convulsions.

Patients who have an increased risk of seizures (e.g. patients who have experienced head trauma, patients with a history of alcohol abuse or diabetics) must use this drug with extra precautions, because the risk of Bupropion-induced seizures is higher in these patients.

Some clinical studies have suggested that Bupropion may cause hypertension (which can be severe) and the blood pressure should be checked at the start of the treatment and periodically (every 7th day for the first two months of therapy).

Bupropion, pregnancy and breastfeeding

Some epidemiological studies have shown that administration of Bupropion during pregnancy may increase the risk of congenital heart malformations in newborns. On the other hand, one prospective study that included 136 pregnant women who used Bupropion in the first trimester revealed no increased incidence of malformations as compared to the control group.4 Risk/benefit ratio should be considered before a decision is made on the use of this drug during pregnancy.

Bupropion and its metabolites are excreted into breast milk, and breastfeeding should be avoided while taking this drug.

Dosage

Bupropion exists in the form of modified release tablets at a dose of 150 mg and 300 mg and in the form of a sustained release tablets at a dose of 150 mg.

Recommended dosage for Bupropion modified release tablets

The starting dose is 150 mg once a day. If this dose does not improve your symptoms within a month, the dose may be increased to 300 mg daily.

Symptoms improvement is expected within two weeks of starting the Bupropion.

The tablet should be taken in the morning, because taking this drug in the evening increases the risk of insomnia.

It can be taken regardless of meals. Swallow the tablet with 200 ml of water. Do not crush, chew or divide the tablet because it can affect its efficacy.

The therapy usually lasts 6 months or longer.

This drug should not be used in patients younger than 18 years.

Interactions

Bupropion enter into major interaction with about 400 different drugs! Therefore, it is very important that you tell your doctor about all medications you're using.

Use of the Bupropion with the following drugs increases the risk of seizures:

  • Hydrocodone, dezocine, alfentanil, and fentanyl (medicines used to treat pain)
  • Aminophylline (a drug used to treat asthma)
  • Aripiprazole, clozapine, olanzapine and prochlorperazine (antipsychotics)
  • Corticosteroids, such as: methylprednisolone, hydrocortisone, prednisone and triamcinolone.
  • Tricyclic antidepressants, such as: amitriptyline, nortriptyline, imipramine, clomipramine and desipramine.
  • Amphetamine (a drug used to treat attention deficit disorder)
  • Blockers of potassium channels in the central nervous system, such as: dalfampridin - a drug that has been approved by FDA for multiple sclerosis treatment.
  • Muscle relaxants, such as: cyclobenzaprine.
  • Antihistamines, such as: promethazine - a drug used in the treatment of allergic reactions and in the treatment of motion sickness.
  • Chloroquine - drug used in the treatment of malaria.
  • Buprenorphine - a drug used in the treatment of opioid addiction.
  • Cycloserine - a drug used in the treatment of tuberculosis.
  • Duloxetine - a selective inhibitor of serotonin and noradrenaline (used to treat depression)

Side effects

Bupropion may cause the following side effects:

  • Anorexia (occurs frequently)
  • Agitation
  • Anxiety
  • Ataxia
  • Depression
  • Depersonalisation
  • Delusion
  • Dystonia
  • Paranoid ideas
  • Suicidal thoughts
  • Seizures
  • Tremor
  • Weight loss
  • Taste disturbances
  • Rapid heartbeat
  • Frequent urination
  • Fluid retention
  • Allergy

References