Lowest Oral Dosage of Buprenorphine Available
The lowest oral (sublingual) dosage of buprenorphine available is 0.4 mg in tablet form.
Available Buprenorphine Formulations
Buprenorphine is a partial mu-opioid receptor agonist that is available in several formulations for different indications:
Sublingual (Oral) Formulations:
- 0.4 mg tablets - lowest available oral dose 1
- 2 mg tablets
- 8 mg tablets
- Buprenorphine/naloxone combination tablets (2mg/0.5mg and 8mg/2mg)
Other Formulations:
- Transdermal patches (starting at 5 mcg/hour) 2
- Buccal film (starting at 150 μg) 3
- Injectable extended-release formulations 4
- Implantable formulations 4
Clinical Applications of Low-Dose Buprenorphine
The availability of low-dose formulations (0.4 mg) is particularly important in several clinical scenarios:
Pain Management: Lower doses are often used when treating chronic pain, with dosing ranges of 4-16 mg divided into 8-hour doses showing benefit 2
Buprenorphine Microdosing ("Low-Dosing"): Starting with very low doses (as low as 0.5 mg sublingual or even smaller doses using buccal or transdermal formulations) allows for initiation without requiring patients to endure withdrawal 3
Tapering: Low doses facilitate gradual dose reduction when discontinuing treatment 5
Renal Impairment: Based on its pharmacokinetics, buprenorphine may be especially appropriate for treating pain in patients with renal impairment, and lower doses may be preferred in these patients 2
Important Considerations
Buprenorphine exhibits a ceiling effect for respiratory depression, making it safer than full mu-opioid agonists at higher doses 2
When used for pain management, buprenorphine is often administered in divided doses (every 6-8 hours) rather than once daily as typically used for opioid use disorder 2
The FDA recommends limiting transdermal buprenorphine to a maximum of 20 mcg/hour due to concerns about QT prolongation 2
For patients transitioning between different formulations or from other opioids to buprenorphine, careful dose conversion is essential, and pain specialty consultation may be beneficial for complex cases 2
Caution
When prescribing low-dose buprenorphine, be aware that:
Due to its high binding affinity for the μ-opioid receptor, buprenorphine may block the effects of other opioids if they need to be used concurrently 2
Buprenorphine may precipitate withdrawal symptoms if administered to individuals currently taking high-dose opioids 2
Despite being a partial agonist, buprenorphine can still cause typical opioid side effects including nausea, constipation, and sedation, particularly in opioid-naïve patients