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Bupropion-used as an antidepressant and smoking cessation aid

Bupropion is a medication primarily used as an antidepressant and smoking cessation aid. It is marketed as Wellbutrin and Zyban among other trade names. More

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Description

Bupropion is a medication primarily used as an antidepressant and smoking cessation aid. It is marketed as Wellbutrin and Zyban among other trade names.

Generic Name

Bupropion-used as an antidepressant and smoking cessation aid

Chemical names

Amfebutamone; Amfebutamon; 2-(tert-butylamino)-1-(3-chlorophenyl)propan-1-one; Amfebutamonum

Brand names

Bupdep, Bupep, Bupisure, Bupron-SR, Bupron-XL, Ession-ER, Nicotex, Smoquit-SR, Zyban

IUPAC name

2-(tert-butylamino)-1-(3-chlorophenyl)propan-1-one

Pharmacokinetics

Well absorbed

Actions

Bupropion, an antidepressant of the aminoketone class and a non-nicotine aid to smoking cessation, is chemically unrelated to selective serotonin re-uptake inhibitor, tetracyclic, tricyclic, or other known antidepressant agents. Bupropion is a relatively weak inhibitor of the neuronal uptake of serotonin, norepinephrine and dopamine. 

Dosage/Dosage form

Oral route

  • Initially, 100 mg bid increased to 100 mg tid after 3 days if necessary to treat depression.
  • Initially, 150 mg once daily for 6 days then increased to 150 mg bid used for smoking cessation.

Therapeutic uses

For the treatment of depression and as aid to smoking cessation.

Adverse effects/Side effects

Facial oedema; nausea, dry mouth, constipation, diarrhoea, anorexia; mouth ulcer; thirst; myalgia, arthralgia; insomnia, abnormality, dream, anxiety, dizziness, disturbed concentration, nervousness, dysphoria; tremor, rhinitis, increased cough, pharyngitis, sinusitis; dyspnoea, epistaxis, agitation, insomnia, tremor, headache, weight loss, vomiting, skin rash. Stevens-Johnson syndrome.

Interaction

  • Concurrent use with MAO inhibitors may cause acute toxicity symptoms and increased risk of fatality.
  • Reduced hepatic clearance with fluoxetine.
  • Neuroleptics, lithium and TCAs, benzodiazepine, alcohol, drugs that lower seizure threshold.
  • Increased risk of side effects when co-admin with levodopa.
  • Caution when administering with agents that will affect hepatic drug metabolizing enzymes.
  • Increased risk of toxicity when used with ritonavir.

Contraindications

Epilepsy; eating disorders (e.g. bulimia or anorexia nervosa); hypersensitivity

Storage

Store at 15-25°C.

Information

Molecular weight

239.741

Molecular formula

C13H18ClNO

CAS number

34911-55-2

Precautions

  • History of seizure disorders, bipolar disorders
  • Renal or hepatic impairment.
  • MI or unstable heart disease
  • Pregnancy
  • Monitor BP before and after treatment
  • May impair ability to drive and operate machinery.
  • Avoid use within 2 weeks of MAO inhibitor withdrawal.