FORFIVO XL

Bupropion is a racemic mixture. The pharmacologic activity and pharmacokinetics of the individual enantiomers have not been studied. Following single dosing under fasted conditions of FORFIVO XL tablets, the maximum peak plasma concentration (C max ), and the area under the plasma concentration versus time curve of bupropion from zero to infinity (AUC inf ), were 207.46 (± 59.40) ng/mL, and 2147.53 (± 664.12) ng

• hr/mL, respectively. The elimination half-life (± SD) of bupropion after a single do...

The efficacy of bupropion in the treatment of MDD was established with the immediate-release formulation of bupropion hydrochloride in two 4-week, placebo-controlled trials in adult inpatients with MDD and in one 6-week, placebo-controlled trial in adult outpatients with MDD. In the first study, the bupropion dose range was 300 to 600 mg/day administered in 3 divided doses; 78% of patients were treated with doses of 300 to 450 mg/day. The trial demonstrated the efficacy of bupropion as measured by the Hamilton Depression Rating Scale (HDRS) total score, the HDRS depressed mood item (item 1), a...

The following adverse reactions are discussed in greater detail in other sections of the labeling:

• Suicidal thoughts and behaviors in children, adolescents, and young adults [see Warnings and Precautions ( 5.1 )]
• Neuropsychiatric adverse events and suicide risk in smoking cessation treatment [see Warnings and Precautions ( 5.2 )]
• Seizure [see Warnings and Precautions ( 5.3 )]
• Hypertension [see Warnings and Precautions ( 5.4 )]
• Activation of mania or hypomania [see Warnings and Precauti...

• FORFIVO XL is contraindicated in patients with a seizure disorder [see Warnings and Precautions ( 5.3 )] .
• FORFIVO XL is contraindicated in patients treated currently with other bupropion products because the incidence of seizure is dose dependent [see Warnings and Precautions ( 5.3 )] .
• FORFIVO XL is contraindicated in patients with a current or prior diagnosis of bulimia or anorexia nervos...

Neuropsychiatric Adverse Events During Smoking Cessation: Postmarketing reports of serious or clinically significant neuropsychiatric adverse events have included changes in mood (including depression and mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, agitation, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide. Observe patients attempting to quit smoking with FORFIVO XL for the occurrence of such symptoms...

7 DRUG INTERACTIONS

• CYP2B6 Inhibitors: Ticlopidine or clopidogrel may increase bupropion exposure. Coadministration of FORFIVO XL with ticlopidine or clopidogrel is not recommended ( 7.1 ).
• CYP2B6 Inducers: Dose increase may be necessary if coadministered with CYP2B6 inducers (e.g., ritonavir, lopinavir, efavirenz, carbamazepine, phenobarbital, and phenytoin) based on clinical exposure, but sh...