Bupropion; Uses, Dosage, Side Effects, Drug Interactions

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Bupropion is an aminoketone antidepressant that is widely used in therapy of depression and smoking cessation. Bupropion therapy can be associated with transient, usually asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.This agent does not inhibit monoamine oxidase and, compared to classical tricyclic antidepressants, is a weak blocker of the neuronal uptake of serotonin and norepinephrine. Buproprion also weakly inhibits the neuronal reuptake of dopamine.

Bupropion is a medication primarily used as an antidepressant and smoking cessation aid.  It is one of the most frequently prescribed antidepressants in the United States and Canada, although in many countries this is an off-label use. It is an effective antidepressant on its own but is also popular as an add-on medication in cases of incomplete response to first-line SSRI antidepressants. Bupropion is taken in tablet form and is available only by prescription in most countries.

Mechanism of action of Bupropion

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.

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Indications of Bupropion

Contra-Indications of Bupropion

  • Spread of cancer to the brain
  • Tumor of the brain or spinal cord
  • Symptoms from alcohol withdrawal
  • Mild degree of Mania
  • Manic-depression
  • Mental disorder with loss of normal personality & reality
  • Having thoughts of suicide
  • Alcoholism
  • Narcotic addiction
  • Anorexia nervosa
  • Bulimia
  • Feeling anger toward something
  • Lower seizure threshold
  • Closed angle glaucoma
  • high blood pressure
  • Heart attack
  • Severe liver disease
  • Seizures
  • Weight loss
  • Seizure caused by sudden withdrawal of benzodiazepine
  • Stimulant drug dependence
  • Sedative drug dependence
  • risk of angle-closure glaucoma due to narrow angle of anterior chamber of eye

Dosage of Bupropion

Strengths: 75 mg; 100 mg; 150 mg;  200 mg ;300mg; 400mg; 450mg.

Smoking Cessation

Sustained-release tablets

  • Initial dose: 150 mg orally once a day for 3 days, increased to 150 mg orally twice a day
  • Maintenance dose: 150 mg orally twice a day
  • Maximum dose: 300 mg/day; maximum single dose should not exceed 150 mg
  • Duration of therapy: 7 to 12 weeks

Depression

Immediate-release tablets

  • Initial dose: 100 mg orally twice a day, increase if necessary after 3 days to 100 mg orally three times a day.
  • Maintenance dose: 100 mg orally three times a day
  • Maximum dose: 450 mg/day in up to 4 divided doses; single doses should not exceed 150 mg

Sustained-release tablets

  • Initial dose: 150 mg orally once a day in the morning, increase if necessary after 3 days to 150 mg orally twice a days
  • Maintenance dose: 150 mg orally twice a day
  • Maximum dose: 400 mg/day; maximum single dose should not exceed 200 mg
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Extended-release tablets

  • Initial dose: 150 mg orally once a day in the morning, increase if necessary after 4 days to 300 mg orally once a day.
  • Maintenance dose: 300 mg orally once a day
  • Maximum dose: 450 mg/day

Seasonal Affective Disorder

Extended-release tablets

  • Initial dose: 150 mg orally once a day in the morning, increased if necessary after 7 days to 300 mg orally once a day
  • Maintenance dose: 150 to 300 mg orally once a day
  • Maximum dose: 300 mg/day

Side Effects of Bupropion

The most common

 Common

Rare

  • Buzzing or ringing in the ears
  • headache (severe)
  • skin rash, hives, or itching
  • Confusion
  • false beliefs that cannot be changed by facts
  • having extreme distrust of people
  • seeing, hearing, or feeling things that are not there
  • seizures
  • trouble concentrating

Drug Interactions of Bupropion

Bupropion may interacts with following drugs, supplyments & may change the efficacy of drugs

This is not a complete list of all drug interactions of bupropion. Ask your doctor for more information.

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Pregnancy & Lactation of Bupropion

FDA Pregnancy Catagory C

Pregnancy

This medication falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Lactation

Limited information indicates that maternal bupropion doses of up to 300 mg daily produce low levels in breast milk and would not be expected to cause any adverse effects in breastfed infants. However, there is little-reported use in breastfed newborn infants and case reports of a possible seizure in partially breastfed 6-month-old. If bupropion is required by a nursing mother.

References

 

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