Buprenorphine/naloxone

Buprenorphine/naloxone
Combination of
Buprenorphine Opioid modulator
Naloxone Opioid antagonist
Clinical data
Trade names Suboxone, Bunavail, Zubsolv
AHFS/Drugs.com suboxone
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration		 Sublingual
ATC code
Legal status
Legal status
Identifiers
PubChem CID
KEGG

Buprenorphine/naloxone (trade name Suboxone) is a combination drug formulation of buprenorphine, a μ-opioid receptor (MOR) weak partial agonist and κ-opioid receptor antagonist, and naloxone, a MOR silent antagonist, in a 4:1 ratio.[1][2] It is used in the treatment of opioid dependence.[1][2] The purpose of naloxone is to deter intravenous abuse; parenteral administration rapidly induces opioid withdrawal symptoms, while regular, intended use does not (as naloxone is minimally bioavailable with sublingual ingestion).[1][2][3][4]

This combination is available as sublingual tablets or film.[5]

Medical uses

Buprenorphine/naloxone is used for the treatment of opioid dependence in combination with psychosocial support and counseling for the patient.[5][6] It has been found to be effective for treating opioid dependence, as is the first line medication according to U.S. National Institute on Drug Abuse.[7] Due to the high binding affinity and low activation for the opioid receptor, cravings and withdrawal for opioids are decreased while preventing a patient from getting high and relapsing from using another opioid.

Contraindications

Contraindications are severe respiratory or liver impairment and acute alcoholism.[6]

Adverse effects

Side effects are basically the same as those of buprenorphine and other opioids.[6] In addition, naloxone can induce withdrawal symptoms in people who are addicted to opioids.[6] Buprenorphine/naloxone has a milder side effect profile than methadone, and has limited respiratory effects, due to both agonist/antagonist effects. However, buprenorpine/naloxone is less safe than methadone in patients with stable liver disease.[8]

Dependence and withdrawal

Suboxone sublingual tablets
Suboxone film (package)

Buprenorphin/naloxone in a 4:1 combination, when taken parenterally, produces dysphoric symptoms due to the naloxone, which acts to deter abuse. However when taken orally or sublingually as directed, the naloxone is not absorbed, allowing buprenorphine to act.[7] The Suboxone formulation still has potential to produce an opioid agonist "high" if injected by non-dependent persons, which may provide some explanation to street reports indicating that the naloxone is an insufficient deterrent to injection of Suboxone.[9][10] The addition of naloxone and the reasons for it are conflicting. Published data show that the μ-opioid receptor binding affinity of buprenorphine is higher than naloxone's (K(i) = 0.2157 nM for buprenorphine, K(i) = 1.1518 nM for naloxone; smaller K(i) mean higher affinity).[11] Furthermore, the IC50 or the half maximal inhibitory concentration for buprenorphine to displace naloxone is 0.52 nM, while the IC50s of other opiates in displacing buprenorphine, is 100 to 1,000 times greater.[12] These studies help explain the ineffectiveness of naloxone in preventing Suboxone abuse, as well as the potential dangers of overdosing on buprenorphine, since a continuous infusion of naloxone can be necessary in order to reverse its respiratory effects.[13]

Interactions

The sedating/narcotic effect of buprenorphine is increased by other sedating drugs such as other opioids, benzodiazepines, older antihistamines, alcohol, and antipsychotics. In addition, opioids and especially benzodiazepines increase the risk for potentially lethal respiratory depression.[6]

Strong inhibitors of the liver enzyme CYP3A4, such as ketoconazole, moderately increase buprenorphine concentrations; CYP3A4 inducers can theoretically decrease concentrations of buprenorphine.[5][6]

See also

In the show Mr.Robot, the protagonist hacker Elliot uses Suboxone to counteract addiction to the morphine he takes for social anxiety and clinical depression.

References

  1. 1 2 3 Diane S. Aschenbrenner; Samantha J. Venable (2009). Drug Therapy in Nursing. Lippincott Williams & Wilkins. pp. 396–. ISBN 978-0-7817-6587-9.
  2. 1 2 3 Gary L. Fisher; Nancy A. Roget (11 November 2008). Encyclopedia of Substance Abuse Prevention, Treatment, and Recovery. SAGE Publications. pp. 570–. ISBN 978-1-4129-5084-8.
  3. ↑ Atta-ur Rahman; M. Iqbal Choudhary (1 January 2010). Frontiers in CNS Drug Discovery. Bentham Science Publishers. pp. 631–. ISBN 978-1-60805-159-5.
  4. ↑ Linda E. McCuistion; Joyce LeFever Kee; Evelyn R. Hayes (25 March 2014). Pharmacology: A Patient-Centered Nursing Process Approach. Elsevier Health Sciences. pp. 56–. ISBN 978-0-323-29348-8.
  5. 1 2 3 Drugs.com: FDA Professional Drug Information for Suboxone Film.
  6. 1 2 3 4 5 6 Haberfeld, H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag.
  7. 1 2 Yokell, Michael A.; Zaller, Nickolas D.; Green, Traci C.; Rich, Josiah D. (1 March 2011). "Buprenorphine and Buprenorphine/Naloxone Diversion, Misuse, and Illicit Use: An International Review". Current drug abuse reviews. 4 (1): 28–41. ISSN 1874-4737. PMC 3154701 Freely accessible.
  8. ↑ Bonhomme, Jean; Shim, Ruth S.; Gooden, Richard; Tyus, Dawn; Rust, George (1 January 2012). "Opioid Addiction and Abuse in Primary Care Practice: A Comparison ofMethadone and Buprenorphine as Treatment Options". Journal of the National Medical Association. 104 (0): 342–350. ISSN 0027-9684. PMC 4039205 Freely accessible.
  9. ↑ Strain EC, Stoller K, Walsh SL, Bigelow GE (2000). "Effects of buprenorphine versus buprenorphine/naloxone tablets in non-dependent opioid abusers". Psychopharmacology. 148 (4): 374–383. PMID 10928310. doi:10.1007/s002130050066.
  10. ↑ Clinical Guidelines for the Use of Buprenorphine in the Treatment of Opioid Addiction. Treatment Improvement Protocol (TIP) 40. Laura McNicholas. US Department of Health and Human Services.
  11. ↑ Volpe DA, McMahon Tobin GA, Mellon RD, Katki AG, Parker RJ, Colatsky T, Kropp TJ, Verbois SL (2011). "Uniform assessment and ranking of opioid Mu receptor binding constants for selected opioid drugs". Regulatory Toxicology and Pharmacology. 59 (3): 385–390. PMID 21215785. doi:10.1016/j.yrtph.2010.12.007.
  12. ↑ Villiger JW, Taylor KM (1981). "Buprenorphine : Characteristics of binding sites in the rat central nervous system". Life Sciences. 29 (26): 2699–2708. PMID 6276633. doi:10.1016/0024-3205(81)90529-4.
  13. ↑ Dahan A. (2006). "Opioid-induced respiratory effects: new data on buprenorphine.". Palliative medicine. 20 Suppl 1: s3–8. PMID 16764215.
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