Buprenorphine, Suboxone®

Brand name

  • Suboxone®

Drug Class

  • Partial opioid agonist that blocks other opioids from attaching to receptors in the brain
  • A partial agonist produces less effect than a full agonist when it binds to opioid receptors

Preparations

  • Tablets: sublingual pills
    • Buprenorphine 2mg/naloxone 0.5mg;
    • Buprenorphine 8mg/naloxone 2mg
  • Film: Sublingual
  • Patch:

Indications

  • SUBOXONE is indicated for substitution treatment in opioid dependence.
  • SUBOXONE can decrease cravings and relieve withdrawal symptoms
  • Clinical researches have found Buprenorphine effective for:
    • Suppressing symptoms of opioid withdrawal
    • Reducing cravings for opioids
    • Reducing illicit opioid use

Pharmacology

Buprenorphine is a non-selective opioid receptor agonist–antagonist. Buprenorphine has been reported to possess the following pharmacological activity:

  • μ-Opioid receptor: Very strong partial agonist.
  • κ-Opioid receptor: Partial agonist or functional antagonist. Animal studies show antidepressive, anxiolytic, stress relieving, and anti-addictive properties.
  • δ-Opioid receptor: Antagonist. Possible attenuation of drug reward.
  • Nociceptin receptor: Weak affinity. Very weak partial agonist. May be involved in lack of respiratory depression with buprenorphine in overdose.

Naloxone is added to Suboxone to stop people from injecting it. If suboxone injected, hte naloxone blocks the effects of opioids like heroin, fentanyl, morphine and methadone and can cause withdrawal symptoms.

Metabolism

Buprenorphine is metabolized into norbuprenorphine  by the liver, via CYP3A4 isozymes of the cytochrome P450 enzyme system. individuals with liver cirrhosis or liver failure might need lower suboxone dose.

Drug Interactions

  • Using buprenorphine (Suboxone) is contraindicated with naltrexone and opioids such as methadone, morphine, oxycodone, tylenol3… and could result in precipitated withdrawal.
  • Medications that are metabolized in liver via P450 enzyme, could interact with suboxone metabolism.
  • Using buprenorphine together with following medications can lead to serious side effects such as respiratory distress, coma, or even death
    • Zolpiden
    • Benzodiazepines
    • Alcohol
  • Using buprenorphine together with sertraline may increase side effects such as dizziness, drowsiness, and difficulty concentrating.

Adverse Effects

Buprenorphine or buprenorphine and naloxone may cause side effects:

  1. headache
  2. difficulty falling asleep or staying asleep
  3. mouth numbness or redness
  4. tongue pain
  5. blurred vision
  6. stomach pain
  7. constipation
  8. vomiting
  9. back pain

 

What is Precipitated withdrawal?

  • Precipitated withdrawal can occur when buprenorphine is administered to a patient dependent on opioids
  • Due to Buprenorphine’s high affinity at the mu receptor it displaces opioids from the mu receptors, without activating the receptor to an equivalent degree, resulting in a net decrease in agonist effect, thus precipitating a withdrawal syndrome.
  • To avoid precipitated withdrawal you should start suboxone no earlier than 12 hours from the last use of short acting opioids (Heroin, Crushed OxyContin®, Percocet®, Vicodin®, Oxycodone®) and no earlier than 24 hours after the last use of long acting opioids (Methadone).

 

If you experience any of these symptoms call your doctor and 9-1-1 or go to emergency, immediately:

  1. hives
  2. skin rash
  3. itching
  4. difficulty breathing or swallowing
  5. swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
  6. slowed breathing
  7. upset stomach
  8. blurred vision
  9. slurred speech
  10. confusion
  11. unusual bleeding or bruising
  12. pain in the upper right part of the stomach
  13. yellowing of the skin or eyes
  14. dark-colored urine
  15. light-colored stools

Pregnancy and Breastfeeding

Suboxone has been used successfully during pregnancy and breastfeeding. Neonates born to mothers with opioid dependence who were started on suboxone during pregnancy experience less neonatal abstinent syndrome. Thomas et al (2014) found that buprenorphine maintenance during pregnancy was associated with improved maternal and fetal outcomes, compared with no medication-assisted treatment. Although, rates of neonatal abstinence syndrome were similar among infants born to methadone- vs. buprenorphine-maintained mothers, but symptoms were less severe for infants whose mothers were treated with buprenorphine replacement (Thomas et al. 2014).

Warning

Risk of overdose:

  • Suboxone, was involved in 30,135 emergency room visits in 2010, up from 3,161 visits in in 2005 (SAMHSA 2013).
  • Over half of the hospitalizations were for non-medical use of buprenorphine – with some users taking the drug to get high.

References

  • Elizabeth H. Crane, Ph.D, MPh Emergency Department Visits Involving Buprenorphine. The CBHSQ Report. 2013.

Special note

This document is prepared by the “Mental Health for All” team. This document is provided for information purposes only and does not necessarily represent endorsement by or an official position of the Essentials of Medicine. Advice on the treatment or care of an individual patient should be obtained through consultation with a physician who has examined that patient or is familiar with that patient’s medical history.

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