Opioid partial agonist (buprenorphine) + opioid antagonist (naloxone)

Buprenorphine/Naloxone

Suboxone (sublingual film), Zubsolv (sublingual tablet), Sublocade (monthly injectable, buprenorphine extended-release)
FDA-Approved Indications
  • Opioid use disorder (OUD), maintenance treatment
Common Off-Label Uses
  • Opioid tapering
  • Bridge therapy in emergency departments with rapid linkage to outpatient MOUD
  • Chronic pain management (buprenorphine formulations: Belbuca, Butrans patch, not the focus of this page)

Side Effects Worth Knowing

Constipation: common

Mu-opioid-mediated reduction in GI motility. Present at maintenance doses. Manage with fiber, stool softeners, osmotic laxatives. Same mechanism as constipation from any opioid.

Headache: common

Often occurs early in treatment. Usually transient. May relate to opioid receptor adjustment.

Nausea/vomiting: common during induction

Often resolves as tolerance to this effect develops. Opioid receptor-mediated effect on the chemoreceptor trigger zone.

Insomnia: reported

Some patients experience sleep disruption, particularly during induction.

Sweating: common

Opioid-mediated effect on thermoregulation. May persist during maintenance. Patients may find this bothersome.

Precipitated withdrawal (induction): consequence of incorrect timing

Not a side effect of the medication per se, but a consequence of incorrect induction timing. Symptoms: severe cramping, diarrhea, vomiting, anxiety, agitation, diaphoresis, piloerection, mydriasis. Management: supportive care, adjunctive medications (clonidine, ondansetron, loperamide, benzodiazepines with respiratory monitoring), and in some cases additional buprenorphine once the acute phase passes. Prevention is far preferable to treatment.

Respiratory depression: substantially reduced risk compared to full agonists

The ceiling effect protects against buprenorphine-only respiratory depression at therapeutic and supratherapeutic doses in opioid-tolerant patients. Risk is NOT zero: respiratory depression can occur in opioid-naive individuals, with concurrent CNS depressants (benzodiazepines, alcohol, sedatives), or in patients with significant respiratory comorbidity.

Hepatic effects: rarely reported

Hepatitis and hepatic events have been reported, primarily in patients with pre-existing liver disease or concurrent hepatotoxic exposures. Monitor LFTs if clinically indicated.

Dental effects: FDA warning (2022)

An FDA drug safety communication noted reports of dental problems (cavities, tooth loss, oral infections) associated with buprenorphine sublingual formulations. Mechanism may involve the acidic pH of dissolving tablets/films in contact with teeth. Common counseling recommendations: after the sublingual dose has fully dissolved, take a sip of water, swish gently, and swallow; wait at least one hour before brushing teeth; maintain regular dental check-ups. Inform patients of this risk at initiation.

See This Medication in Action

These case studies show how buprenorphine/naloxone decisions play out in real clinical scenarios:

References & Further Reading

This page synthesizes information from standard clinical references. Consult primary sources for all prescribing decisions.

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For learning and board prep — not a prescribing reference. Dosing and safety information change. Always verify against current FDA labeling and your institution’s protocols before prescribing.