Week 9 Module 6 Group 1
Group 1: Describe the differences between Naloxone, Naltrexone, and Buprenorphine/Naloxone. Include the properties of each, their classification, mechanism of actions, onset, half-life, and formulations (routes of delivery). Please discuss the implications of differences in the clinical setting (including pre-hospital)
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Naloxone, Naltrexone, and Buprenorphine/Naloxone are prescribed to patients who suffer from substance use disorders.
Naloxone, or commonly known as Narcan, is an agent for opioid antagonist. It is administered to patients who have overdosed on an opioid and can fully reverse the effects. Naloxone has little to no effect on patients who have not ingested an opioid. It works by binding to opioid receptors, including mu, kappa, and delta. Based on the route of delivery, the onset can be from 2 minutes to 15 minutes. The average half-life is from 30 minutes to 2 hours. Routes of delivery include intravenously, intramuscularly, intraosseously, subcutaneously, or intranasally (Prescribers Digital Reference, 2022). Naloxone is given in emergency situations in patients who are suspected of overdose. It can be given in the field or hospital setting (FDA, 2015).
Naltrexone is classified as an opioid antagonist. It is given to patients who suffer from alcohol and opioid dependence. The molecular formula of this medication is C20H23NO4(FDA, 2009). Naltrexone has a high affinity for the mu opioid receptor and will prevent withdraw symptoms in patients who are opioid dependent. Absorption is rapid and levels peak in about 1 hour. The half-life on average is about 4 hours. Naltrexone can be given by intramuscular injection or in tablet form by mouth. Patients who suffer from alcohol dependence or opioid dependence can be prescribed this medication in the outpatient setting (Prescribers Digital Reference, 2022).
Buprenorphine/Naloxone (Suboxone) is a mixed opioid agonist-antagonist (buprenorphine) combined with an opioid antagonist (naloxone). This medication is prescribed to patients who are dependent on short-acting opioids, such as heroin, who are in withdrawal and for maintenance treatment. Buprenorphine partials acts as an agonist at the mu receptor and an antagonist as the kappa receptors. Naloxone is a mu receptor antagonist. The onset is up to 2 hours and the half-life of buprenorphine is 24-48 hours and of naloxone is 2-12 hours. Buprenorphine/naloxone is given sublingually. This medication can be prescribed and taken in the outpatient setting (Prescribers Digital Reference, 2022).
n/a. (2009). Vivitrol. FDA. https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021897s005s010lbl.pdf
n/a. (2015). NARCAN (naloxone hydrochloride) nasal spray. FDA. https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208411lbl.pdf
n/a. (2022). Buprenorphine/naloxone-Drug Summary. Prescriber’s Digital Reference. https://www.pdr.net/drug-summary/Suboxone-buprenorphine-naloxone-1292.8207
n/a. (2022). Naloxone hydrochloride- Drug Summary. Prescriber’s Digital Reference. https://www.pdr.net/drug-summary/Narcan-naloxone-hydrochloride-3837.6202
n/a. (2022). Naltrexone hydrochloride- Drug Summary. Prescriber’s Digital Reference. https://www.pdr.net/drug-summary/Revia-naltrexone-hydrochloride-1753.2479
Naloxone is used to block or reverse the effect of opioid overdoses, such as loss of consciousness, drowsiness, and slowed breathing. The drug is appropriate for patients who are on long-term opioid medications, those taking extended-release opioid medication, and those recovering from abuse of opioid drugs. It can also be used as an adjunctive to raise blood pressure. Naloxone possesses a higher affinity for the μ-opioid receptors. Therefore, it antagonizes the effects of opioids by binding to these receptors, causing the removal of other drugs the opioid attached to these receptors, hence the reverse of the opioid effects. Due to its high affinity for opioid receptors, the drug only works when an individual has taken opioid medications or substances. Naloxone is only effective for 30-90 minutes, and therefore multiple doses might be required; in such cases, the individual should seek medical care for further interventions (National Institute on Drug Abuse, 2022).
Naltrexone is a narcotic antagonist more potent than naloxone. The drug is commonly used in behavioral modification programs, including alcohol and opiate cessation programs. It is administered together with drugs such as morphine to prevent dependence among patients in healthcare. In the CNS, the drug binds to the mc, κ, μ, and δ receptors, where it prevents the effects of endogenous opioids. The dosage is usually dependent on the symptoms and is adjusted to meet the individual needs (Drug Bank, 2022).
Buprenorphine/Naloxone is a mixed medication combining two drugs. The active drug in this combination is buprenorphine, a partial opioid agonist. It works as an opioid, but the effect is milder than other full agonists. It, therefore, lowers the effects of withdrawal symptoms associated with the use of opioid substances without causing full opioid effects. The naloxone part of this drug combination is only absorbed and activated in the body when injected instead of dissolved. However, when injected into the bloodstream, it causes severe side effects and discourages individuals from using intravenous opioids (National Alliance on Mental Illness, 2022).
Drug Bank, (2022) Naltrexone Retrieved from: https://go.drugbank.com/drugs/DB00704
National Alliance on Mental Illness, (2022) Buprenorphine/Naloxone (Suboxone) Retrieved from: https://www.nami.org/About-Mental-Illness/Treatments/Mental-Health-Medications/Types-of-Medication/Buprenorphine/Buprenorphine-Naloxone-(Suboxone)
National Institute on Drug Abuse, (2022) What is naloxone? Retrieved from: https://nida.nih.gov/publications/drugfacts/naloxone