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Wellbutrin: profile and news
I'm Bipolar Journal: December 2005-January 2006 17 May 2006 Policies on mentally troubled troops questioned 17 May 2006 Biovail 1st-Qtr Profit Rises Sixfold on Wellbutrin (Update3) May 11, 2006 Biovail 1st-Qtr Profit Rises Sixfold on Wellbutrin (Update1) May 11, 2006 Biovail Q1 Earnings Surge On Strong Sales Of Antidepressant ... May 11, 2006 Biovail Reports First-Quarter 2006 Financial Results; Company ... May 11, 2006 Biovail seeks acquisitions after US$64.5M Q1 profit driven by ... May 11, 2006 Biovail profit soars on strong sales, cost cuts May 11, 2006 Biovail Faces Generic Competition May 12, 2006 Biovail Sales Surge May 11, 2006 Biovail 1Q profit up nearly sixfold May 11, 2006 Morgan Stanley Keeps Glaxo Overweight May 12, 2006 TO THE POINT May 11, 2006 FDA approves Pfizer's smoking-cessation drug May 11, 2006 Anti-smoking pill is approved May 12, 2006 UPDATE 1-Biovail first-quarter profit soars, sales up May 11, 2006 FDA gives green light to Pfizer drug for quitting smoking May 11, 2006 FDA Approves New Smoking-Cessation Aid 10 Weeks After Rejecting ... May 11, 2006 Pfizer drug helps quit the habit May 12, 2006 Biovail Q1 profit tops expectations May 11, 2006 Biovail posts robust 1Q results May 11, 2006 Big quarter for Biovail May 11, 2006 Biovail Profit Skyrockets - Eyes Acquisitions May 11, 2006 Eight ways for Salt Lake Real to raise money for a new soccer ... May 10, 2006 Pfizer scores OK for new anti-smoking pill May 12, 2006 Laguna 'stepped out of his body' May 5, 2006 On the Radar: Biovail May 13, 2006 FDA OKs Pfizer Anti-Smoking Pill May 11, 2006 TSX slips on lower financial, tech stocks while NY falls on Fed ... May 11, 2006 Canadian Stocks Fall as Inflation Concerns Weigh on Financials May 11, 2006 Canadian Stocks Fall as Inflation Concerns Weigh on Financials May 11, 2006 Canadian Stocks Fall as Inflation Concerns Weigh on Market May 11, 2006 Toronto stocks set to bounce back on resources May 11, 2006 New drug could help smokers May 12, 2006 BlackBerry set for China debut May 11, 2006 Ex-phenom hits back at IMG, father in bid to regain her game May 9, 2006 Drugs giants hit heights on forecast-beating Q1 results Apr 27, 2006 Highlights of rising and falling US stocks May 11, 2006 DTC Takes a Back Seat May 10, 2006 Classen defense continues to make its case Apr 18, 2006 New drug wins approval in fight against smoking May 11, 2006 FDA approves Pfizer stop-smoking pill May 12, 2006 FDA approves new anti-smoking drug May 11, 2006 'Teachable' 9/11 Moment Helped Smokers Quit May 1, 2006 Generic Pharma Firms Stand To Benefit From Patent Expirations ... May 8, 2006 Trial asks 'why?' May 3, 2006 Suspect suicidal, says therapist May 5, 2006 Laguna trial begins May 1, 2006 Buried Sacrifice: Inside the Military Family May 3, 2006 Other information Indication For the treatment of depression and as aid to Smoking cessation. Pharmacology Bupropion, an antidepressant of the aminoketone class and a non-nicotine aid to smoking cessation, is chemically unrelated to tricyclic, tetracyclic, selective serotonin re-uptake inhibitor, or other known antidepressant agents. Compared to classical tricyclic antidepressants, Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine, serotonin, and dopamine. In addition, Bupropion does not inhibit monoamine oxidase. Bupropion produces dose-related central nervous system (CNS) stimulant effects in animals, as evidenced by increased locomotor activity, increased rates of responding in various schedule-controlled operant behavior tasks, and, at high doses, induction of mild stereotyped behavior. Mechanism Of Action Bupropion selectively inhibits the neuronal reuptake of dopamine, norepinephrine, and serotonin; actions on dopaminergic systems are more significant than imipramine or amitriptyline whereas the blockade of norepinephrine and serotonin reuptake at the neuronal membrane is weaker for bupropion than for tricyclic antidepressants. The increase in norepinephrine may attenuate nicotine withdrawal symptoms and the increase in dopamine at neuronal sites may reduce nicotine cravings and the urge to smoke. Bupropion exhibits moderate anticholinergic effects. Drug Category Antidepressants; Antidepressants; ATC:N07BA02 Brand Names/Synonyms Bupropion; Bupropion Hcl; Wellbatrin; Wellbutrin; Wellbutrin Sr; Wellbutrin Xl; Zyban Dosage Forms immediate and sustained release tablets Absorption for sustained release, peak plasma conc. are achieved within 3 hours. Interactions -->Interactions for Bupropion: Few systemic data have been collected on the metabolism of WELLBUTRIN following concomitant administration with other drugs or, alternatively, the effect of concomitant administration of WELLBUTRIN on the metabolism of other drugs. Because bupropion is extensively metabolized, the coadministration of other drugs may affect its clinical activity. In vitro studies indicate that bupropion is primarily metabolized to hydroxybupropion by the CYP2B6 isoenzyme. Therefore, the potential exists for a drug interaction between WELLBUTRIN and drugs that affect the CYP2B6 isoenzyme (e.g., orphenadrine and cyclophosphamide). The threohydrobupropion metabolite of bupropion does not appear to be produced by the cytochrome P450 isoenzymes. The effects of concomitant administration of cimetidine on the pharmacokinetics of bupropion and its active metabolites were studied in 24 healthy young male volunteers. Following oral administration of two 150-mg sustained-release tablets with and without 800 mg of cimetidine, the pharmacokinetics of bupropion and hydroxybupropion were unaffected. However, there were 16% and 32% increases in the AUC and Cmax, respectively, of the combined moieties of threohydrobupropion and erythrohydrobupropion. While not systematically studied, certain drugs may induce the metabolism of bupropion (e.g., carbamazepine, phenobarbital, phenytoin). Animal data indicated that bupropion may be an inducer of drug-metabolizing enzymes in humans. In one study, following chronic administration of bupropion, 100 mg 3 times daily to 8 healthy male volunteers for 14 days, there was no evidence of induction of its own metabolism. Nevertheless, there may be the potential for clinically important alterations of blood levels of coadministered drugs. Drugs Metabolized by Cytochrome P450IID6 (CYP2D6): Many drugs, including most antidepressants (SSRIs, many tricyclics), beta-blockers, antiarrhythmics, and antipsychotics are metabolized by the CYP2D6 isoenzyme. Although bupropion is not metabolized by this isoenzyme, bupropion and hydroxybupropion are inhibitors of the CYP2D6 isoenzyme in vitro. In a study of 15 male subjects (ages 19 to 35 years) who were extensive metabolizers of the CYP2D6 isoenzyme, daily doses of bupropion given as 150 mg twice daily followed by a single dose of 50 mg desipramine increased the Cmax, AUC, and t1/2 of desipramine by an average of approximately 2-, 5- and 2-fold, respectively. The effect was present for at least 7 days after the last dose of bupropion. Concomitant use of bupropion with other drugs metabolized by CYP2D6 has not been formally studied. Therefore, co-administration of bupropion with drugs that are metabolized by CYP2D6 isoenzyme including certain antidepressants (e.g., nortriptyline, imipramine, desipramine, paroxetine, fluoxetine, sertraline), antipsychotics (e.g., haloperidol, risperidone, thioridazine), beta-blockers (e.g., metoprolol), and Type 1C antiarrhythmics (e.g., propafenone, flecainide), should be approached with caution and should be initiated at the lower end of the dose range of the concomitant medication. If bupropion is added to the treatment regimen of a patient already receiving a drug metabolized by CYP2D6, the need to decrease the dose of the original medication should be considered, particularly for those concomitant medications with a narrow therapeutic index. MAO Inhibitors: Studies in animals demonstrate that the acute toxicity of bupropion is enhanced by the MAO inhibitor phenelzine . Levodopa and Amantadine: Limited clinical data suggest a higher incidence of adverse experiences in patients receiving bupropion concurrently with either levodopa or amantadine. Administration of WELLBUTRIN Tablets to patients receiving either levodopa or amantadine concurrently should be undertaken with caution, using small initial doses and small gradual dose increases. Drugs that Lower Seizure Threshold: Concurrent administration of WELLBUTRIN and agents (e.g., antipsychotics, other antidepressants, theophylline, systemic steroids, etc.) that lower seizure threshold should be undertaken only with extreme caution. Low initial dosing and small gradual dose increases should be employed. Nicotine Transdermal System: . Alcohol: In post-marketing experience, there have been rare reports of adverse neuropsychiatric events or reduced alcohol tolerance in patients who were drinking alcohol during treatment with WELLBUTRIN. The consumption of alcohol during treatment with WELLBUTRIN should be minimized or avoided (also see CONTRAINDICATIONS). |
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