Bupropion Hydrochloride information from DrugsUpdate
P - Caution when used during pregnancy
L - Bupropion and its metabolites are secreted in breast milk
Bupropion is a typical antidepressant that acts as a norepinephrine and dopamine reuptake inhibitor, and nicotinic antagonist. Bupropion belongs to the chemical class of aminoketones and is similar in structure to the stimulant cathinone, to the anorectic diethylpropion, and to phenethylamines in general.
Initially researched and marketed as an antidepressant, bupropion was subsequently found to be effective as a smoking cessation aid. In 2007 it was the fourth-most prescribed antidepressant in the United States retail market, with 20.184 million retail prescriptions.
Bupropion lowers seizure threshold and its potential to cause seizures was widely publicized. However, at the recommended dose the risk of seizures is comparable to that observed for other antidepressants. Bupropion is an effective antidepressant on its own but it is particularly popular as an add-on medication in the cases of incomplete response to the first-line SSRI antidepressant. In contrast to many psychiatric drugs, including nearly all antidepressants, bupropion does not cause weight gain or sexual dysfunction.
Pharmacodynamics
Pharmacokinetics
Bupropion HCl is a relatively weak inhibitor of the neuronal uptake of norepinephrine, serotinin and dopamine. The mechanism by which it aids in smoking cessation is presumed to be mediated by its noradrenergic and/or dopaminergic actions.
Absorption
Well absorbed from the GI tract but undergoes extensive first pass effect.
Distribution
=80% bound to plasma proteins. Crosses the placenta and distributed into breast milk.
Excretion
Terminal half-life of immediate-release preparation: about 14 hours. Mainly excreted in the urine as metabolites.
Bupropion Hydrochloride Indications / Bupropion Hydrochloride Uses
Information Not Available
Bupropion Hydrochloride Adverse Reactions / Bupropion Hydrochloride Side Effects
Facial oedema; nausea, dry mouth, constipation, diarrhoea, anorexia; mouth ulcer; thirst; myalgia, arthralgia; insomnia, dream, abnormality, anxiety, disturbed concentration, dizziness, nervousness, tremor, dysphoria; rhinitis, increased cough, pharyngitis, sinusitis; dyspnoea, epistaxis, agitation, insomnia, tremor, headache, weight loss, vomiting, skin rash.
Potentially Fatal: Stevens-Johnson syndrome.
Precautions
Information Not Available
Special Precautions
History of seizure disorders, bipolar disorders; MI or unstable heart disease; pregnancy; renal or hepatic impairment. Monitor BP before and after treatment; monitor weekly if used with nicotine products. May impair ability to drive and operate machinery. Avoid use within 2 weeks of MAO inhibitor withdrawal.
Other Drug Interactions
Neuroleptics, lithium and TCAs, benzodiazepine, alcohol, drugs that lower seizure threshold. Increased risk of side effects when co-admin with levodopa. Reduced hepatic clearance with fluoxetine. Caution when administering with agents that will affect hepatic drug metabolizing enzymes. Increased risk of toxicity when used with ritonavir.
Potentially Fatal: Concurrent use with MAO inhibitors may cause acute toxicity symptoms and increased risk of fatality.
Other Interactions
Information Not Available
Dosage
Oral
Smoking cessation
Adult: Modified-release preparation: Initially, 150 mg once daily for 6 days then increased to 150 mg bid.
Period of treatment: 7-12 weeks. To discontinue treatment if abstinence is not achieved by 7th weeks.
Max: 300 mg/day.
Elderly: 150 mg/day.
Oral
Depression
Adult: Initially, 100 mg bid increased to 100 mg tid after 3 days if necessary. Increased further to 150 mg tid if no improvement has been observed after several weeks of therapy.
Max: 150 mg tid. As a modified-release preparation: 150 mg once daily in the morning, increased to 150 mg bid after 3 days if necessary, may further increase to 200 mg bid after several weeks if needed.
Max: 450 mg as a single dose.
Food(before/after)
May be taken with or without food
List of Contraindications
Bupropion Hydrochloride and Pregnancy
Caution when used during pregnancy
Bupropion Hydrochloride and Lactation
Bupropion and its metabolites are secreted in breast milk
Bupropion Hydrochloride and Children
Safety and efficacy not established
Bupropion Hydrochloride and Geriatic
Use with caution. Because elderly patients are more likely to have decreased renal function, use care in dose selection and consider monitoring renal function.
Bupropion Hydrochloride and Other Contraindications
Epilepsy; eating disorders (e.g. bulimia or anorexia nervosa); hypersensitivity
Storage
Oral
Store at 15-25°C.
Lab interference
Oral
Store at 15-25°C.
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