From the Guidelines
Naloxone is included in buprenorphine (Suboxone) medication to reduce the risk of abuse and will block opioids if injected, serving as a deterrent against misuse. This formulation is preferred due to its safety feature, as the naloxone component is poorly absorbed via the sublingual route and is present only to prevent misuse of the medication by crushing and injecting the combined product 1. The presence of naloxone in Suboxone does not replace the need for a separate naloxone nasal spray at home, which is specifically designed as a rescue medication to reverse opioid overdose in emergency situations. Key points to consider include:
- The naloxone in Suboxone is not active when taken as prescribed sublingually, but becomes active if the medication is misused by injection.
- The primary purpose of naloxone in Suboxone is to deter misuse, not to treat an opioid overdose.
- The separate naloxone nasal spray serves as an emergency intervention tool for overdose situations, distinct from the preventative measure of naloxone in Suboxone.
- Both the naloxone in Suboxone and the separate naloxone nasal spray are important components in the comprehensive treatment of opioid use disorder, focusing on prevention and emergency response, respectively 1.
From the FDA Drug Label
CLINICAL PHARMACOLOGY Mechanism of Action Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. Pharmacodynamics Buprenorphine hydrochloride is a parenteral opioid analgesic with 0. 3 mg buprenorphine being approximately equivalent to 10 mg morphine sulfate in analgesic and respiratory depressant effects in adults.
The correct reason why naloxone is included in this formulation of buprenorphine is:
- C This medication includes naloxone to reduce the risk of abuse and will block opioids if injected 2.
Naloxone is included in the formulation to reduce the risk of abuse by blocking the effects of opioids if the medication is injected, rather than taken sublingually as intended.
From the Research
Rationale for Naloxone Inclusion in Buprenorphine Formulation
- The inclusion of naloxone in buprenorphine (Suboxone) medication is primarily to reduce the risk of abuse and will block opioids if injected 3, 4, 5.
- When buprenorphine/naloxone is taken sublingually as prescribed, the naloxone exerts no clinically significant effect, leaving the opioid agonist effects of buprenorphine to predominate 5.
- However, when buprenorphine/naloxone is parenterally administered in patients physically dependent on full agonist opioids, the opioid antagonism of naloxone causes withdrawal effects, thus reducing the abuse potential of the drug combination 4, 5.
- The addition of naloxone does not appear to affect the efficacy of buprenorphine as a maintenance drug, but it may create a barrier to care and increase the risk of overdose and death due to limited access to buprenorphine monoproduct 6.
Addressing the Patient's Concern
- The patient's question about why naloxone is included in the buprenorphine formulation when they already have naloxone nasal spray at home can be addressed by explaining the purpose of naloxone in the formulation, which is to reduce the risk of abuse and block opioids if injected 3, 4, 5.
- It is essential to note that the naloxone in the buprenorphine formulation serves a different purpose than the naloxone nasal spray, which is used to treat an opioid overdose 7.