Bupropion adverse effects

Patients taking bupropion may require dose adjustments if they also take elopidogrel or tielopidine. Until more is known about this interaetion it would seem prudent to monitor for inereased bupropion adverse effects (lightheadedness, gastrointestinal effeets) and effieaey. 

Side effects. The primary side effects reported with bupropion administration in cigarette smokers are headache, dry mouth, nausea and vomiting, insomnia, and activation. Although most of these adverse effects occur during the first week of treatment, insomnia can persist. Seizures are of exceedingly low occurrence (<0.5%) at doses of 300 mg daily or less, but a prior history of seizures or a seizure disorder contraindicate its use. 

Bupropion causes insomnia, nightmares, decreased appetite, anxiety, and tremors, but the most concerning adverse effect is seizures. Because of the risk for seizures, patients who should not receive the drug include those with a CNS lesion or those with a history of seizures, head trauma, or bulimia. The daily dose of bupropion should not exceed 450 mg/day, and any single dose of the immediate-release formulation should not exceed 150 mg/day Occurrences of insomnia and/or nightmares often respond to moving the last daily dose from bedtime to late afternoon.7,9,22,23... 

Sexual function One of the potential benefits of hypericum is the apparent reduced or lack of adverse effects upon sexual function, compared to pharmaceutical antidepressants. The SSRIs are particularly notorious for inhibition of sexual function, whereas antidepressants with dopaminergic actions (e.g., bupropion) do not, and may actually enhance sexual function (Rosen et al. 1999 Piazza et al. 1997). Anecdotal reports and the fact that there are no clinical reports of sexual dysfunction with hypericum is encouraging, but it remains to be tested empirically. 

One of the more worrisome adverse effects of bupropion is seizures. At dosages of 450 mg/day or less, the rate of seizures is 0.4% for individuals without risk factors (Davidson, 1989). Because of this risk, a single dose of bupropion should not exceed 150 mg and a second dose should be separated in time by a minimum of 8 hours. Also, patients who are metabolically unstable (i.e., have bulimia) should be carefully assessed for the risk of seizures before initiating medication. Finally, bupropion is not associated with sexual side effects. 

Bupropion appears to be relatively free of adverse effects on sexual function, in contrast to the SSRIS or venlafaxine (168). 

Patients with cardiovascular disorders or those predisposed to anticholinergic adverse effects (e.g., elderly or diabetic patients) probably do best on drugs low in these effects (e.g., an SSRI, venlafaxine, or bupropion). 

As a results of these studies, clinicians have proposed that switching to reboxetine or bupropion might a useful strategy given that these antidepressants share the ability with desipramine and imipramine to block NE uptake. Nevertheless, only one small open label study has been done to test this possibility ( 365). If bupropion is to be used in patients switched from an ineffective trial of fluoxetine, the dose should be kept low for several weeks to allow for the clearance of fluoxetine and norfluoxetine. Case reports indicate that fluoxetine can elevate levels of the active metabolites of bupropion, which, in turn, could mediate an increase risk of adverse effects (366). 

Bupropion, the only marketed aminoketone antidepressant, also has a side-effect profile different from the other classes of antidepressants. It is essentially devoid of anticholinergic, antihistaminic, and orthostatic hypotensive effects. Its principal adverse effects are consistent with its indirect agonism of dopamine and NE via uptake inhibition and include the following ... 

These adverse effects bear some similarity to those of the SSRIs. Although these adverse effects rarely require discontinuation, aggravation of psychosis and seizures caused by this agent do (427, 462, 463 and 464). In contrast to the SSRIs and venlafaxine, bupropion usually does not cause sexual dysfunction. As such, bupropion may be an alternative for patients bothered by these adverse effects (465). Bupropion may also be a useful antidote for SSRI-induced sexual dysfunction (4 53, 455, 466, 467). 

In humans, bupropion undergoes extensive biotransformation to three metabolites that have pharmacological activity ( 469). During treatment, these metabolites accumulate in concentrations several times higher than the parent compound (352). High plasma levels of these metabolites, particularly hydroxybupropion, may be associated with an increased incidence of serious adverse effects, as well as poorer antidepressant response ( 314). These observations form the basis of the possible utility of using TDM to guide dose adjustment with bupropion. 

Bupropion falls between TCAs and SSRIs in terms of safety in overdose. Death is a rare possibility with an overdose of bupropion alone because there are no adverse effects on the cardiovascular or the respiratory systems (461). Seizures may occur but are readily treatable in a hospital setting. 

The SSRis may avoid some of the more serious adverse effects seen with the TCAs. Thus, if expense is not a major concern, the SSRIs are increasingly considered an appropriate first choice (290, 291). Trazodone and bupropion are also appealing because of their milder anticholinergic and cardiovascular effects ( 292). With milder mood disturbances, a brief trial with psychostimuiants, such as methyiphenidate, can be attempted. 

T effects OF amiodarone, astemizole, atorvastadn, barbiturates, bepridil, bupropion, cerivastatin, cisapride, clorazepate, clozapine, clarithromycin, desipramine, diazepam, encainide, ergot alkaloids, estazolam, flecainide, flurazepam, indinavir, ketoconazole, lovastatin, meperidine, midazolam, nelfinavir, phenytoin, pimozide, piroxicam, propafenone, propoxyphene, quinidine, rifabutin, saquinavir, sildenafil, simvastatin, SSRIs, TCAs, terfenadine, triazolam, troleandomycin, zolpidem X effects W/ barbiturates, carbamazepine, phenytoin, rifabutin, rifampin, St. John s wort, tobacco X effects OF didanosine, hypnotics, methadone, OCPs, sedatives, theophylline, warfarin EMS T Effects of amiodarone, diazepam, midazolam and BBs, may need X- doses concurrent use of Viagra-type drugs can lead to hypotension X- effects of warfarin concurrent EtOH use can T adverse effects T glucose ODs May cause an extension of adverse SEs symptomatic and supportive Rivasrigmine (Exelon) [Cholinesterase Inhibitor/Anri ... 

Oxcarbazepine can also cause hyponatremia, but in this case the hyponatremia appeared to correlate with the prescription of bupropion rather than oxcarbazepine and was also reproduced by amfebutamone re-challenge. This case suggests that amfebutamone can also cause hyponatremia, although it is possible that the presence of oxcarbazepine was necessary for the adverse effect to occur. 

FLUOXETINE, FLUVOXAMINE, PAROXETINE, SERTRALINE BUPROPION t plasma concentrations of bupropion and risk of adverse effects Inhibition of CYP2B6 Warn patients about adverse effects, and use alternatives when possible... 

CHLORPROMAZINE, CLOZAPINE, HALOPERIDOL, OLANZAPINE BUPROPION T plasma concentrations of these drugs with risk of toxic/adverse effects Smoking induces mainly CYP1A2 and CYP2E1. Thus de-induction takes place following cessation of smoking Be aware and watch for early features of toxicity. Consider reducing the dose... 

BUPROPION 1. ANTICANCER DRUGS - thiotepa 2. ANTIDEPRESSANTS-fluoxetine, fluvoxamine, paroxetine, sertraline 3. ANTIVIRALS - efavirenz, protease inhibitors t plasma concentrations of bupropion and risk of adverse effects Inhibition of CYP2B6 Warn patients about adverse effects and use alternatives when possible. Avoid co-administration of bupropion with protease inhibitors. Co-adminis-ter efavirenz and bupropion with caution. A retrospective study showed that two patients received a combination without reported adverse effects. Potential T risk of seizures... 

PROTEASE INHIBITORS BUPROPION t adverse effects of bupropion with nelfinavir and ritonavir (with or without lopinavir) Possibly inhibition of CYP2B6-mediated metabolism of bupropion Avoid co-administration... 

Bupropion is a well-tolerated antidepressant. It is non-sedating and lacks the cardiovascular and anticholinergic side effects of tricyclic antidepressants. Bupropion s most commonly observed adverse effects are insomnia and dry mouth. The drug is also known to be associated with a low rate of seizures however, no seizure incidents were reported in the smoking cessation clinical trials. Other less frequently occurring side effects include nervous system disturbances (mainlytremor) and skin rashes (170,182). 

Bupropion s adverse effects and their management are hsted in Table 61-5 and include nausea, which may resolve over time or with slower dosage titration, and rash, which may require discontinuation of therapy if severe. Bupropion can cause or exacerbate tics and therefore should be used with caution in individuals with tics or a family history of tics. " ... 

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