Bupropion Hydrochloride

Indications

Bupropion Hydrochloride is used for: Depression, smoking cessation

Adult Dose

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 wk. To discontinue treatment if abstinence is not achieved by 7th wk. Max: 300 mg/day. Elderly: 150 mg/day. Hepatic impairment: Mild to moderate: 150 mg once daily. Severe hepatic cirrhosis: Contraindicated. 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 wk 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 wk if needed. Max: 450 mg as a single dose. Elderly: As immediate-release tab: Initially, 37.5 mg bid. As sustained-release tab: Initially, 100 mg daily. Dose may be increased by 37.5-100 mg every 3-4 days as tolerated. Max: 300 mg daily in divided doses. Hepatic impairment: Mild to moderate: Reduce dose or dosing frequency. Severe: As immediate-release preparation: Max: 75 mg once daily. As modified-release preparation: Max: 100 mg once daily or 150 mg every other day.

Child Dose

Renal Dose

Renal impairment: Use caution; consider dose reduction

Administration

Swallow extended/sustained-release tablets whole; do not chew, crush, or split; this may lead to adverse effects including seizures

Contra Indications

It is contraindicated in patients with a seizure disorder. Bupropion Hydrochloride is contraindicated in patients treated with other medications that contain Bupropion because the incidence of seizure is dose dependent. Bupropion may induce seizure and consequently its use is contraindicated in patients with epilepsy. The drug is also contraindicated in patients with a current or prior diagnosis of bulimia or anorexia nervosa because of a higher incidence of seizures noted in such patients treated for bulimia with Bupropion Hydrochloride. The concurrent administration of Bupropion Hydrochloride and a monoamine oxidase (MAO) inhibitor is contraindicated. At least 14 days should elapse between discontinuation of MAO inhibitor and initiation of treatment with Bupropion Hydrochloride. Bupropion Hydrochloride is contraindicated in patients who have shown an allergic response to Bupropion or the other ingredients that make up Bupropion Hydrochloride.

Precautions

It should be used with extreme caution, in patients with history of seizure disorders or in patients with other predisposing factors such as severe hepatic cirrhosis or a CNS tumour, and in those undergoing abrupt withdrawal from alcohol or Benzodiazepines. The use of Bupropion in patients with other risk factors for seizures (for example, alcohol abuse, a history of head trauma, diabetes, and drugs known to lower the seizure threshold) should only be undertaken when there are compelling clinical reasons. Bupropion should be used with caution in patients with bipolar depression or psychoses and in patients with a recent history of myocardial infarction or unstable heart disease and in hepatic or renal impairment. Lactation: Enters breast milk; use caution

Pregnancy-Lactation

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.

Adverse Effects

Side effects of Bupropion Hydrochloride : >10% Headache (25-34%),Dry mouth (17-28%),Nausea (1-18%),Weight loss (15-20%),Insomnia (11-20%),Agitation (2-32%),Dizziness (6-22%),Pharyngitis (3-13%) 1-10% Constipation (5-10%),Infection (8-9%),Abdominal pain (2-9%),Anxiety (5-7%),Diarrhea (5-7%),Tinnitus (3-6%),Tremor (3-6%),Nervousness (3-5%),Anorexia (3-5%),Palpitation (2-6%),Myalgia (2-6%),Sweating (2-5%),Rash (1-5%),Sinusitis (1-5%),Weight gain (4%),Chest pain (3-4%),Urinary frequency (2%),Vaginal hemorrhage (2%),Pruritus (2-4%),Vomiting (2-4%),Arthralgia (1-4%),Flushing (1-4%),Migraine (1-4%),Decreased memory (<3%),Irritability (2-3%),Somnolence (2-3%),Dysphagia (<2%),Arthritis (2%),Paresthesia (1-2%),Fever (1-2%),Twitch (1-2%),Seizures (0.4% [<450 mg/day], >3% [>450 mg/day]; may be increased risk with concomitant ECT) Frequency Not Defined Confusion,Cystitis,Erythema,,Ataxia,Coma,EEG abnormality,Euphoria,Gastric reflux

Mechanism of Action

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.