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ACUTE EXPOSURE INFORMATION

  1. USES: Schedule III prescription medication used for opioid addiction maintenance therapy.
  1. PHARMACOLOGY: Partial agonist at the mu-opioid receptor, antagonist at the kappa opioid receptor.
  1. TOXICOLOGY: The toxicity is an extension of the pharmacology. Effects include CNS depression, respiratory depression, constipation, and euphoria. Hypotension can occur from mast cell G protein activation and subsequent degranulation of histamine-containing vesicles.
  1. EPIDEMIOLOGY: Buprenorphine exposures are common. In adults, severe toxicity may occur from crushing and injecting tablets, but is not common after ingesting buprenorphine alone. Children are at risk for toxicity following ingestion of less than a single tablet. While most deaths are due to overdose, deaths following inadvertent ingestion have occurred.
  1. WITH THERAPEUTIC USE
    1. Sedation, headache, nausea, vomiting, abdominal pain, constipation, and withdrawal syndrome. At high doses, buprenorphine's agonist effects plateau ("ceiling effect"), limiting the maximum analgesic and respiratory depressant effects. Due to this "ceiling effect," patients who are chronic users/abusers of opioids can experience withdrawal after ingestion of buprenorphine.
  1. WITH POISONING/EXPOSURE
    1. MILD TO MODERATE POISONING: Miosis, sedation, and relative bradycardia. Hepatitis is reported rarely.
    1. SEVERE POISONING: CNS depression, coma, respiratory depression, and hypotension. Children, in particular, may develop profound, recurrent, or delayed CNS and respiratory depression. In adults, severe effects are generally only seen after crushing and injecting tablets, or after very large ingestions. Acute renal failure is reported rarely.
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