Assignment:
Question: Describe the differences between Naloxone, Naltrexone, and Buprenorphine/Naloxone (Suboxone). Need Assignment Help?
Include the properties of each, their classification, and mechanism of actions, onset, half-life, and formulations (routes of delivery).
Please discuss the implications of differences in the clinical setting (including pre-hospital)
Discussion Rubric
Posts are a minimum of 250 words, scholarly written, APA formatted (with some exceptions due to limitations in the D2L editor), and a minimum of 2 references (which may include the course textbook).
Student's Post: Naloxone (Narcan) is a pure opioid antagonist known for its lifesaving abilities in opioid overdose emergencies (Bennett & Elliott, 2022). It is a synthetic opioid antagonist which rapidly transfers opioids from the μ-opioid receptors, reversing opioid induced respiratory depression (OIRD) (Moss et al., 2020). It is vital for naloxone to replace the opioids on at least 50% of the receptors in order to successfully reverse OIRD, so the concentration of the naloxone must be sufficient (Dahan et al., 2024). With the increase of fentanyl related deaths, there has been a lot of research into the correct dosing of naloxone, since fentanyl is about 50 times stronger than heroin we now have 8mg intranasal (IN) spray (as opposed to the formerly effective 2-4mg before fentanyl made its way into the street drug market) and intramuscular routes available to the public to intervene with an opioid overdose; in the hospital setting, naloxone is used intravenously (Dahan et al., 2024). Naloxone is so effective partly because of its very quick onset of 2-5 minutes (Dahan et al., 2024). Naloxone has a short half-life of about 1.5-2.5 hours, so patients often require monitoring and immediate medical attention because the opioid may outlast the naloxone; this is especially true with the synthetic opioids such as fentanyl (Dahan et al., 2024). Many efforts have been made over the years for naloxone to be easily obtainable by the public, making it much easier for family members or a stranger on the street to administer IN naloxone, increasing the chances of survival and recovery (Bennett & Elliott, 2022).
Naltrexone is a non-selective opioid receptor antagonist, but unlike naloxone, it is used for relapse prevention rather than overdose reversal (Spencer et al., 2023). It has been used for decades, and it is still not fully understood how it reduces addictive behavior, specifically alcohol and opioid cravings (Spencer et al., 2023). Some research has shown that naltrexone reduces the rewarding and euphoric effects of alcohol and opioids because it works with the brain's endogenous opioid system and the way it regulates dopamine (Spencer et al., 2023). It is available as an oral tablet, which has a half-life of 13 hours, or a monthly intramuscular injection (Vivitrol) (Srivastava & Gold, 2018). One thing to consider with oral tablets, is that if a patient chooses to be non-compliant they are at a high risk of relapse once the half-life passes and this can lead to an overdose if the patient uses more opioids than usual to "bypass" the naltrexone's effects, which is why vivitrol is often preferred (Srivastava & Gold, 2018). Because it can precipitate severe opioid withdrawal, patients must be opioid-free for at least 3-5 days (for an average user) before starting treatment (Srivastava & Gold, 2018).
Buprenorphine/naloxone (Suboxone) is used for maintenance treatment of opioid use disorder, as well as pain management in some cases (Paul et al., 2024; Infantino et al., 2021). Buprenorphine is a partial mu-opioid agonist with a ceiling effect, making it much safer than full opioid agonists because it lowers the risk of respiratory depression due to its lessened ability to cross the blood-brain barrier (Infantino et al., 2021). Naloxone is added primarily to discourage intravenous misuse causing withdrawal and diminished euphoria, since naloxone has minimal bioavailability when taken sublingually as prescribed, it has no effect when taken this way (Infantino et al., 2021). Buprenorphine has a long half-life of approximately 24-42 hours (Infantino et al., 2021).
I remember when Vivitrol first was making its way into the market, I was working at a substance abuse treatment center, and it was talked about as a miracle drug for patients who were chronically relapsing. These medications are truly game changers for those who struggle with addiction, offering them a second chance at life, and hope for a future in recovery.
References:
- Bennett, A. S., & Elliott, L. (2021). Naloxone's role in the national opioid crisis-past struggles, current efforts, and future opportunities. Translational Research : The Journal of Laboratory and Clinical Medicine, 234, 43-57.
- Dahan, A., Franko, T. S, Carroll, J. W., Craig, D. S., Crow, C., Galinkin, J. L., Garrity, J. C., Peterson, J., & Rausch, D. B. (2024). Fact vs. fiction: Naloxone in the treatment of opioid-induced respiratory depression in the current era of synthetic opioids. Frontiers in Public Health, 12:1346109.
- Infantino, R., Mattia, C., Locarini, P., Pastore, A. L., Maione, S., & Luongo, L. (2021). Buprenorphine: Far beyond the "ceiling". Biomolecules, 11(6), 816.
- Moss, R. B., Pryor, M. M., Baillie, R., Kudrycki, K., Friedrich, C., Reed, M., & Carlo, D. J. (2020). Higher naloxone dosing in a quantitative systems pharmacology model that predicts naloxone-fentanyl competition at the opioid mu receptor level. PloS One, 15(6), e0234683.
- Paul, K. K., Frey, C. G., Troung, S., Paglicawan, L. V. Q., Cunningham, K. A., Preston Hill, T., Bothwell, L. G., Golovko, G., Pillay, Y., & Jehle, D. (2024). Buprenorphine-Naloxone for opioid use disorder: Reduction in mortality and increased remission. The Western Journal of Emergency Medicine, 25(6), 869-874.
- Spencer, C. N., Elton, A., Dove, S., Faulkner, M. L., Robinson, D. L., & Boettiger, C. A. (2023). Naltrexone engages a brain reward network in the presence of reward-predictive distractor stimuli in males. Addiction Neuroscience, 7, 100085.
- Srivastava, A. B., & Gold, M. S. (2018). Naltrexone: A history and future directions. Cerebrum: The Dana forum on brain science, 2018, cer-13-18.