Buprenorphine drug overdose

Naloxone is a pure competitive antagonist at all opioid receptors, notably the p- and K- receptors it has no agonist activity. Naloxone antagonises both agonist and partial agonist opioids (although it may not be sufficient to reverse the effects of buprenorphine in overdose, so tenaciously does the latter drug bind to receptors). It induces an acute withdrawal syndrome in opioid-dependent subjects. 

Buprenorphine is the most lipophilic compound in the oripavine series of compounds and therefore enters the brain very easily. Usually, such a drug would react quickly with its receptor. The fact that it does not is therefore a feature of its interaction with the receptor rather than the ease with which it can reach the receptor. It is 100 times more active than morphine as an agonist and four times more active than nalorphine as an antagonist. It is a particularly safe drug since it has very little effect on respiration and what little effect it does have actually decreases at high doses. Therefore, the risks of suffocation from a drug overdose are much smaller than with... 

Mortality related to the use and abuse of opioids is of public health concern. In an epidemiological study, mortality over 20 years among 42 676 clients in contact with opioid pharmacotherapy programs was reduced by 29% [24 "]. Mortality was higher when out of treatment, particularly in the first few weeks and during induction on to methadone, but not buprenorphine. The main causes of mortality were drug overdose and trauma. 

Drug overdose During November 2002 to December 2005 there were 96 reports of unintentional buprenorphine overdose in children under 6 years of age from US... 

Pain-relieving action is not superior to that of codeine Response to naloxone in overdose may be unreliable This drug, which does not activate opioid receptors, has been proposed as a maintenance drug in treatment programs for opioid addicts a single oral dose will block the effects of injected heroin for up to 48 hours (A) Amphetamine Buprenorphine Naloxone Naltrexone Propoxyphene... 

The total dose required to reverse the effects of the opioid is highly variable and is dependent on the concentration and receptor affinity of the opioid. Some drugs (eg, propoxyphene, diphenoxylate/atropine [Lomotil], buprenorphine, pentazocine, and the fentanyl derivatives) do not respond to usual doses of naloxone. However, if no response is achieved by a total dose of 10-15 mg, the diagnosis of opioid overdose should be questioned. 

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