Buprenorphine

FDA label

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Renal Undefined

Hepatic Severe impairment: consider halving starting and titration incremental doses; monitor for toxicity/overdose

NOT for use as an analgesic — deaths reported in opioid-naïve individuals given a 2 mg SL dose.

Instructions

• Administer sublingually as a single daily dose; tablets must be taken whole — do not cut, chew, or swallow.
• Place under the tongue until dissolved; no food or drink until fully dissolved; then sip water, swish gently, swallow; wait ≥1 hour before brushing teeth.
• Induct only when objective, clear signs of moderate opioid withdrawal are evident — ≥4 h after last short-acting opioid; generally ≥24 h after methadone/long-acting opioids.
• Adjust maintenance dose in 2 mg or 4 mg increments/decrements to suppress withdrawal and hold patient in treatment.
• Taper gradually when discontinuing to avoid withdrawal.
• Strongly consider prescribing an opioid overdose reversal agent (naloxone/nalmefene) at initiation and renewal.

Cautions

• Addiction, abuse, and misuse (Schedule III) — monitor for diversion; limit early refills.
• Life-threatening respiratory and CNS depression, especially with benzodiazepines, other CNS depressants, or alcohol.
• Unintentional pediatric exposure can be fatal — store out of sight and reach of children.
• Neonatal opioid withdrawal syndrome with prolonged use in pregnancy.
• Adrenal insufficiency — treat with physiologic corticosteroids and wean off opioid if diagnosed.
• Opioid withdrawal with abrupt discontinuation.
• Hepatitis/hepatic events — monitor LFTs before and during treatment.
• Precipitated opioid withdrawal if taken before agonist effects of other opioids have subsided (or with parenteral misuse).
• Overdose risk in opioid-naïve patients; orthostatic hypotension; elevated CSF and intracholedochal pressure; dental problems with sublingual route.

Adverse reactions

• Oral hypoesthesia, glossodynia, oral mucosal erythema
• Headache
• Nausea, vomiting
• Hyperhidrosis
• Constipation
• Withdrawal signs and symptoms, insomnia, pain, peripheral edema

Pregnancy Limited data do not indicate increased risk of major malformations; neonatal opioid withdrawal syndrome expected with prolonged use; dose adjustment (often higher) may be needed during pregnancy.

Lactation Present in low levels in human milk (<1% of maternal dose); no adverse reactions shown in breastfed infants — monitor infant for drowsiness and breathing difficulty.