Naloxone treatment in opioid addiction: the risks and benefits

Abstract

Naloxone is a non-selective, short-acting opioid receptor antagonist that has a long clinical history of successful use and is presently considered a safe drug over a wide dose range (up to 10 mg). In opioid-dependent patients, naloxone is used in the treatment of opioid-overdose-induced respiratory depression, in (ultra)rapid detoxification and in combination with buprenorphine for maintenance therapy (to prevent intravenous abuse). Risks related to naloxone use in opioid-dependent patients are: i) the induction of an acute withdrawal syndrome (the occurrence of vomiting and aspiration is potentially life threatening); ii) the effect of naloxone may wear off prematurely when used for treatment of opioid-induced respiratory depression; and iii) in patients treated for severe pain with an opioid, high-dose naloxone and/or rapidly infused naloxone may cause catecholamine release and consequently pulmonary edema and cardiac arrhythmias. These risks warrant the cautious use of naloxone and adequate monitoring of the cardiorespiratory status of the patient after naloxone administration where indicated.

Combined oral prolonged-release oxycodone and naloxone in chronic pain management

“…Unlike other opioid antagonists, which do not completely inhibit the analgesic properties of opioids, N is devoid of any intrinsic agonist activity and antagonizes all actions of morphine. When administered intravenously, it acts centrally as a specific antidote in the management and reversal of overdoses caused by opioid agents, with a proven long-term safety profile and a safety over a wide dose range [11].…”

The Relative Potency of Inverse Opioid Agonists and a Neutral Opioid Antagonist in Precipitated Withdrawal and Antagonism of Analgesia and Toxicity

“…Opioid antagonists (e.g., naltrexone and naloxone) have a long clinical history in the management of opioid overdose (Ling and Wesson, 1990;Gutstein and Akil, 2001;Clarke et al, 2005). However, in opioid overdose situations, administration of an opioid antagonist can induce an acute withdrawal syndrome that could be life-threatening (e.g., van Dorp et al, 2007). Consequently, precipitated withdrawal by opioid antagonists may be a concern in the management of opioid overdose and treatment of opioid dependence (Ling and Wesson, 1990;van Dorp et al, 2007).…”

“…However, in opioid overdose situations, administration of an opioid antagonist can induce an acute withdrawal syndrome that could be life-threatening (e.g., van Dorp et al, 2007). Consequently, precipitated withdrawal by opioid antagonists may be a concern in the management of opioid overdose and treatment of opioid dependence (Ling and Wesson, 1990;van Dorp et al, 2007). In light of these issues, recent data on inverse agonists and neutral antagonists in opioid dependence may be of pragmatic importance.…”

Buprenorphine Use and Risk of Abuse and Diversion

“…Two forms of buprenorphine are available: A tablet containing only buprenorphine, and one that combines buprenorphine with the opioid antagonist naloxone in a 4:1 ratio. Naloxone has poor oral bioavailability, which means that after sublingual administration the concentration is too low to cause severe and protracted withdrawal symptoms [34]. However, it has good parenteral bioavailability, with an elimination half-life in plasma of about 30 min [35].…”