Overdosage
Lethal Doses in Animals:
In rats the acute oral LD50 values were 607 mg/kg (males) and 482 mg/kg (females). Respective values for mice were 544 mg/kg and 636 mg/kg. Signs of acute toxicity included labored breathing, salivation, arched back, ptosis, ataxia,
and convulsions.
Human Overdose Experience:
There has been limited clinical experience with overdosage of bupropion. Thirteen overdoses occurred during clinical trials. Twelve patients ingested 850 to 4200 mg and recovered without significant sequelae. Another patient who ingested 9000
mg of bupropion and 300 mg of tranylcypromine experienced a grand mal seizure and recovered without further sequelae.
Since introduction, overdoses of bupropion up to 17,500 mg have been reported. Seizure was reported in approximately one-third of all cases. Other serious reactions reported with overdoses of bupropion alone included hallucinations, loss of
consciousness, and tachycardia. Fever, muscle rigidity, rhabdomyolysis, hypotension, stupor, coma, and respiratory failure have been reported when bupropion was part of multiple drug overdoses.
Although most patients recovered without sequelae, deaths associated with overdoses of bupropion alone have been reported rarely in patients ingesting massive doses of bupropion. Multiple uncontrolled seizures, bradycardia, cardiac failure,
and cardiac arrest prior to death were reported in these patients.
Management of Overdose:
Following suspected overdose, hospitalization is advised. If the patient is conscious, vomiting should be induced by syrup of ipecac. Activated charcoal also may be administered every 6 hours during the first 12 hours after ingestion. Baseline
laboratory values should be obtained. Electrocardiogram and EEG monitoring also are recommended for the next 48 hours. Adequate fluid intake should be provided.
If the patient is stuporous, comatose, or convulsing, airway intubation is recommended prior to undertaking gastric lavage. Although there is little clinical experience with lavage following an overdose of bupropion, it is likely to be of benefit
within the first 12 hours after ingestion since absorption of the drug may not yet be complete.
While diuresis, dialysis, or hemoperfusion are sometimes used to treat drug overdosage, there is no experience with their use in the management of overdoses of bupropion. Because diffusion of bupropion from tissue to plasma may be slow, dialysis
may be of minimal benefit several hours after overdose.
Based on studies in animals, it is recommended that seizures be treated with an intravenous benzodiazepine preparation and other supportive measures, as appropriate.
Further information about the treatment of overdoses may be available from a poison control center.
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