Uncommon Severe bupropion overdoses can mimic the findings of brain death. Some patients may present with drowsiness or obtundation, in the absence of sympathomimetic features. ECG Changes Sinus tachycardia QTc prolongation QRS interval prolongation may be delayed Right axis deviation Ventricular dysrhythmias after large overdoses can include ventricular tachycardia, ventricular fibrillation, and asystole.
Bupropion XL is the only form available in Canada. Peak levels are reached at 5 hours therapeutic use though may be substantially longer in overdose. Bupropion is suspected to form pharmacobezoars and clump within the upper GI system, further prolonging absorption.
Metabolites of bupropion are active and may be more toxic than the parent drug. Symptom onset is usually within hours, though severe toxicity may be delayed up to hours or longer. Severe cardiovascular toxicity may develop late, though usually within 24 hours. Symptoms usually resolve within 18 hours in mild cases, and up to 48 hours in severe cases.
Bupropion is a derivative of cathinone, and structurally similar to amphetamines and bath salts. Bupropion and its active metabolite inhibit reuptake of dopamine and norepinephrine minimally inhibits serotonin reuptake. There is no significant anticholinergic or monoamine oxidase inhibitor activity. The precise mechanism for seizures and cardiotoxicity is unclear. QRS widening may be due to cardiac myocyte gap junction inhibition rather than sodium channel blockade as with other antidepressants.
Not established. Doubling of therapeutic dosage as low as mg may result in seizures. Serum levels are not readily available and do not correlate with toxicity or outcome. False positive urine immunoassay for amphetamines has been reported with bupropion. It is strongly recommended that the BC Drug and Poison Information Centre DPIC be contacted at General Asymptomatic patients should have continuous cardiac monitoring and monitoring of vital signs for 18 hours.
An ECG should be done on presentation and prior to discharge. Symptomatic patients should be monitored for at least 12 hours after resolution of symptoms. If the patient needs to be intubated for management of agitation or seizures, Whole Bowel Irrigation should be started once airway is protected. It is strongly recommended that decontamination options be discussed with DPIC. Agitation, Seizures, Neurological toxicity Agitation and seizures should be treated aggressively with IV benzodiazepines.
Early intubation and sedation with propofol or midazolam infusions should be considered for patients with multiple seizures or severe agitation. Phenytoin should be avoided as it is ineffective and may worsen cardiac toxicity. Management of cardiovascular toxicity Sinus tachycardia and hypertension rarely requires treatment. QTc prolongation should be closely monitored and electrolytes corrected as needed. Immediate releasemg and mg. Sustained and extended release: mg, mg, mg, mg, mg, mg, mg, Aplenzin mg.
Mechanism of action:. Bupropion works by inhibiting the reuptake of dopamine and norepinephrine. It is structurally similar to amphetamines and can cause a false positive on urine drug screens-which means it has a structure like an amphetamine but is not actually an amphetamine.
Confirmation on the urine drug screen would be negative for amphetamines. It also antagonizes acetylcholine at nicotinic receptors. Bupropion crosses the blood brain barrier and is metabolized in the liver producing three major active metabolites hydroxybupropion, threohydrobupropion, erythrohydrobupropion which are present in higher concentrations in the plasma than the parent compound. It is the high concentration of active metabolite that causes delayed seizures. Toxic clinical effects:.
Nausea and vomiting can occur. Tachycardia is one of the most common side-effects. Other possible cardiovascular effects include QRS widening, QT prolongation, hypertension, and hypotension.
Seizures are the primary neurologic effect. Confusion, agitation, hallucination, and coma also occur. In confirmed SR Sustained Release or XL Extended Release formulations, seizure onset can be delayed due to the sustained production and accumulation of active metabolites. These patients should be observed for at least hours. If unable to confirm the formulation, consider using the longest observation period to ensure seizure risk has passed.
Bupropion overdoses can be difficult to manage with the combination of cardiac and central nervous system effects. Our advice is to call the Missouri Poison Center at where our specially trained nurses, pharmacists, and medical toxicologist can provide you with the most up-to-date management advice on common and uncommon exposures.
Call Now. Seizures: In very large overdose, it is often not a matter of if they will have a seizure but when they will have a seizure. Cardiovascular: Tachycardia is the most common CV symptom, occurring in almost every case. Share this Post. Legal Disclaimer Providing Your Information During your chat session, you may be asked to provide us some demographic information such as email address, zip code and age.
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