Company: Sanofi Aventis
Pharmacologic class: Antidepressant (aminoketone)
Active ingredient: Bupropion HBr 174 mg (equivalent to bupropion HCl 150 mg), 348 mg (equivalent to bupropion HCl 300 mg), 522 mg (equivalent to bupropion HCl 500 mg); extended- release tabs.
Indication: Major depressive disorder.
Pharmacology: Aplenzin is a once-daily, extended- release tablet formulation of bupropion HBr. The mechanism of action of bupropion in treating depression is not known, but it is likely mediated by its effects on norepinephrine and dopamine.
Clinical trials: The approval of Aplenzin was based on its bioequivalence to another form of bupropion, Wellbutrin XL. In a 10-day study comparing the use of Aplenzin 348 mg once daily to Wellbutrin XL 300 mg once daily, the peak levels and the extent of absorption for the parent drug and its metabolites were shown to be equivalent.
The effectiveness of bupropion in the treatment of depression was established using a short-acting formulation of bupropion HCl in two four-week placebo-controlled trials in adult inpatients and a six-week study in adult outpatients. These studies showed the effectiveness of bupropion HCl on the Hamilton Depression Rating Scale total score, the depressed mood item from that scale, and the Clinical Global Impressions severity score. In another trial, a 44-week study demonstrated the long-term efficacy of bupropion in responders.
Adults: Swallow whole. Take in the am. Initially 174 mg once daily; may increase to target maintenance 348 mg once daily on Day 4; may then increase to maximum 522 mg once daily if inadequate response after four weeks. Severe hepatic cirrhosis: maximum 174 mg/48 hours. Renal or mild-moderate hepatic dysfunction: reduce dose and/or frequency. Switching from other forms: use equivalent dose on once-daily basis. Re-evaluate periodically.
Children: Not recommended.
Contraindications: Seizure disorder. Bulimia. Anorexia nervosa. Within 14 days of monoamine oxidase inhibitors. Abrupt withdrawal of sedatives or alcohol. Concomitant other forms of bupropion (e.g., Zyban, Wellbutrin).
Precautions: Seizure risk or history. Discontinue if seizure occurs; do not restart. Bipolar disorder. Psychosis. Unstable heart disease. CHF. Recent MI. Hepatic or renal dysfunction. Suicidal tendencies (monitor). Maintain at lowest effective dose. Write prescription for smallest practical amount. Labor and delivery. Pregnancy (Cat. C). Nursing mothers: not recommended.
Interactions: See Contraindications. Avoid alcohol. May be potentiated by CYP2B6 substrates or inhibitors, efavirenz, fluvoxamine, nelfinavir, paroxetine, ritonavir, sertraline. Caution with drugs (e.g., antipsychotics) or factors (e.g., opiate addiction, excessive use of alcohol or sedatives, diabetes) that lower seizure threshold. Caution with levodopa, amantadine, and with drugs metabolized by CYP2B6 or CYP2D6, including tricyclic antidepressants, selective serotonin reuptake inhibitors, antipsychotics, beta blockers, class 1C antiarrhythmics; consider dose reduction. Antagonized by carbamazepine, phenobarbital, phenytoin. Monitor for hypertension with nicotine patches.
Adverse reactions: Central nervous system stimulation, dry mouth, GI upset, dizziness, pharyngitis, palpitations, abdominal pain, sweating, tinnitus, anorexia, urinary frequency, rash (may be serious, e.g., Stevens-Johnson syndrome), myalgia, neuropsychiatric effects.
How supplied: Tabs—30
For more information, call 800.446.6267 or visit www.Aplenzin.com.