Dosing & Uses
Dosage Forms & Strengths
injectable solution: Schedule III (Buprenex)
- 0.3mg/mL
tablet, sublingual: Schedule III (generic)
- 2mg
- 8mg
Moderate-to-Severe Pain
0.3 mg IV/IM q6hr; may be repeated once (up to 0.3 mg) if required 30-60 minutes after initial dose
Also see Administration
Opioid Dependence
Induction (sublingual tablet)
- 8 mg SL on day 1, then 16 mg SL on day 2; continued over 3-4 days
Maintenance (buprenorphine-naloxone combination)
- Switch to buprenorphine/naloxone combination for unsupervised maintenance
- For dosing, see drug monograph for buprenorphine/naloxone
Dosage Modifications
Renal impairment
- No differences in pharmacokinetics observed between 9 dialysis-dependent and 6 normal patients following IV administration of 0.3 mg buprenorphine
- Renal failure: Pharmacokinetics are unknown
Hepatic impairment
-
SL use
- Mild: No dose adjustment is needed
- Moderate: No dose adjustment is necessary, closely monitor for signs and symptoms of toxicity or overdose
- Severe: Reducing starting and titration incremental dose by half, and monitor for signs and symptoms of toxicity or overdose
-
IV/IM use
- Mild-to-moderate: No dosage adjustments provided
- Severe: No dosage adjustment provided; use with caution
Dosing Considerations
For prescriber qualifications, see prescribing information
Also given in combination with naloxone
Induction with SL tablets
-
Patients dependent on heroin or other short-acting opioids
- At initiation, administer first dose of buprenorphine SL tablets only when signs/symptoms of moderate opioid withdrawal appear, and ≥4 hr after patient last used an opioid
- Titrate to clinical effectiveness achieved as rapidly as possible; dosing on the initial day of treatment may be given in 2-4 mg increments if preferred
-
Patients dependent on methadone or other long-acting opioids
- Administer first dose of buprenorphine sublingual tablets should when clear signs/symptoms of moderate opioid withdrawal appear, and generally ≥24 hr after the patient last used a long-acting opioids
Access to naloxone for opioid overdose
- Assess need for naloxone upon initiating and renewing treatment
-
Consider prescribing naloxone
- Based on patient’s risk factors for overdose (eg, concomitant use of CNS depressants, a history of opioid use disorder, prior opioid overdose); presence of risk factors should not prevent proper pain management
- Household members (including children) or other close contacts at risk for accidental ingestion or overdose
-
Consult patients and caregivers on the following:
- Availability of naloxone for emergency treatment of opioid overdose
- Ways differ on how to obtain naloxone as permitted by individual state dispensing and prescribing requirements or guidelines (eg, by prescription, directly from a pharmacist, as part of a community-based program)
Dosage Forms & Strengths
injectable solution: Schedule III (Buprenex)
- 0.3mg/mL
Moderate-to-Severe Pain
<2 years: Safety and efficacy not established
2-12 years: 2-6 mcg/kg IV/IM q4-6hr PRN
>12 years: 0.3 mg IV/IM q6hr; may be repeated once (up to 0.3 mg) if required 30-60 minutes after initial dose
Also see Administration
Moderate-to-Severe Pain
0.15 mg IV/IM q6hr; titrate slowly due to increase risk of respiratory depression
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (2)
- alvimopan
alvimopan, buprenorphine. receptor binding competition. Contraindicated. Alvimopan is contraindicated in opioid tolerant patients (ie, those who have taken therapeutic doses of opioids for >7 consecutive days immediately prior to taking alvimopan). Patients recently exposed to opioids are expected to be more sensitive to the effects of alvimopan and therefore may experience abdominal pain, nausea and vomiting, and diarrhea. No significant interaction is expected with concurrent use of opioid analgesics and alvimopan in patients who received opioid analgesics for 7 or fewer consecutive days prior to alvimopan.
- lefamulin
lefamulin will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lefamulin is contraindicated with CYP3A substrates know to prolong the QT interval.
Serious - Use Alternative (67)
- abametapir
abametapir will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use is warranted, carefully monitor, particularly during treatment initiation and dose adjustment. Discontinue oliceridine if serotonin syndrome is suspected.
- alfentanil
buprenorphine, alfentanil. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- apalutamide
apalutamide will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
- belladonna and opium
buprenorphine, belladonna and opium. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- benzhydrocodone/acetaminophen
benzhydrocodone/acetaminophen, buprenorphine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.
buprenorphine decreases effects of benzhydrocodone/acetaminophen by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Mixed opioid agonists/antagonists and partial opioid agonists may reduce the analgesic effect of hydrocodone (benzhydrocodone prodrug of hydrocodone) and/or precipitate withdrawal symptoms in opioid tolerant patients. - bremelanotide
bremelanotide will decrease the level or effect of buprenorphine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- butorphanol
buprenorphine, butorphanol. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- calcium/magnesium/potassium/sodium oxybates
buprenorphine, calcium/magnesium/potassium/sodium oxybates. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.
- chloramphenicol
chloramphenicol will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- cimetidine
cimetidine increases effects of buprenorphine by decreasing metabolism. Avoid or Use Alternate Drug.
- clarithromycin
clarithromycin will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- clonidine
clonidine, buprenorphine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- codeine
buprenorphine, codeine. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- conivaptan
conivaptan will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- dextromoramide
buprenorphine, dextromoramide. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- diamorphine
buprenorphine, diamorphine. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- diazepam intranasal
diazepam intranasal, buprenorphine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.
- difenoxin hcl
buprenorphine, difenoxin hcl. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- diphenoxylate hcl
buprenorphine, diphenoxylate hcl. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- dipipanone
buprenorphine, dipipanone. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- eluxadoline
buprenorphine, eluxadoline. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that cause constipation. Increases risk for constipation related serious adverse reactions. .
- fentanyl
fentanyl, buprenorphine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.
buprenorphine decreases effects of fentanyl by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Coadministration of mixed agonist/antagonist and partial agonist opioid analgesics may reduce fentanyl's analgesic effect and possibly precipitate withdrawal symptoms. - fentanyl intranasal
fentanyl intranasal, buprenorphine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.
buprenorphine decreases effects of fentanyl intranasal by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Coadministration of mixed agonist/antagonist and partial agonist opioid analgesics may reduce fentanyl's analgesic effect and possibly precipitate withdrawal symptoms. - fentanyl transdermal
fentanyl transdermal, buprenorphine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.
buprenorphine decreases effects of fentanyl transdermal by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Coadministration of mixed agonist/antagonist and partial agonist opioid analgesics may reduce fentanyl's analgesic effect and possibly precipitate withdrawal symptoms. - fentanyl transmucosal
fentanyl transmucosal, buprenorphine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.
buprenorphine decreases effects of fentanyl transmucosal by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Coadministration of mixed agonist/antagonist and partial agonist opioid analgesics may reduce fentanyl's analgesic effect and possibly precipitate withdrawal symptoms. - fexinidazole
fexinidazole and buprenorphine both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels and/or prolong QT interval.
fexinidazole will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates. - hydrocodone
buprenorphine decreases effects of hydrocodone by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Mixed opioid agonists/antagonists and partial opioid agonists may reduce the analgesic effect of hydrocodone and/or precipitate withdrawal symptoms in opioid tolerant patients. .
hydrocodone, buprenorphine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation. - hydromorphone
buprenorphine, hydromorphone. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- idelalisib
idelalisib will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates
- isocarboxazid
isocarboxazid increases toxicity of buprenorphine by unknown mechanism. Avoid or Use Alternate Drug. Risk of hypotension, hyperpyrexia, somnolence, or death; separate by 14 d.
- itraconazole
itraconazole will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ivosidenib
ivosidenib will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
- ketoconazole
ketoconazole will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- levorphanol
buprenorphine, levorphanol. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- linezolid
linezolid increases toxicity of buprenorphine by unknown mechanism. Avoid or Use Alternate Drug. Risk of hypotension, hyperpyrexia, somnolence, or death; separate by 14 d.
- lonafarnib
lonafarnib will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.
- meperidine
buprenorphine, meperidine. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- methadone
buprenorphine, methadone. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- methylene blue
methylene blue and buprenorphine both increase serotonin levels. Avoid or Use Alternate Drug. If drug combination must be administered, monitor for evidence of serotonergic or opioid-related toxicities
- metoclopramide intranasal
buprenorphine, metoclopramide intranasal. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient.
- mifepristone
mifepristone will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- morphine
buprenorphine, morphine. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- nalbuphine
buprenorphine, nalbuphine. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- nefazodone
nefazodone will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- oliceridine
buprenorphine, oliceridine. Other (see comment). Avoid or Use Alternate Drug. Comment: Concomitant use may reduce analgesic effect of oliceridine and/or precipitate withdrawal symptoms.
- opium tincture
buprenorphine, opium tincture. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- oxycodone
buprenorphine, oxycodone. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- oxymorphone
buprenorphine, oxymorphone. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- ozanimod
ozanimod and buprenorphine both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Avoid or Use Alternate Drug. Because the active metabolite of ozanimod inhibits MAO-B in vitro, there is a potential for serious adverse reactions, including hypertensive crisis. Therefore, coadministration of ozanimod with drugs that can increase norepinephrine or serotonin is not recommended. Monitor for hypertension with concomitant use.
- papaveretum
buprenorphine, papaveretum. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- pentazocine
buprenorphine, pentazocine. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- phenelzine
phenelzine increases toxicity of buprenorphine by unknown mechanism. Avoid or Use Alternate Drug. Risk of hypotension, hyperpyrexia, somnolence, or death; separate by 14 d.
- posaconazole
posaconazole will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- procarbazine
procarbazine increases toxicity of buprenorphine by unknown mechanism. Avoid or Use Alternate Drug. Do not use within 14 days of MAOI use. .
- selegiline
selegiline increases toxicity of buprenorphine by unknown mechanism. Avoid or Use Alternate Drug. Buprenorphine transdermal is not recommended for in patients who have received MAOI within 14 days, because severe and unpredictable potentiation by MAO inhibitors has been reported with opioid analgesics.
- selegiline transdermal
selegiline transdermal increases toxicity of buprenorphine by unknown mechanism. Avoid or Use Alternate Drug. Risk of hypotension, hyperpyrexia, somnolence, or death.
- selinexor
selinexor, buprenorphine. unspecified interaction mechanism. Avoid or Use Alternate Drug. Patients treated with selinexor may experience neurological toxicities. Avoid taking selinexor with other medications that may cause dizziness or confusion.
- sodium oxybate
buprenorphine, sodium oxybate. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.
- sufentanil
buprenorphine, sufentanil. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- sufentanil SL
buprenorphine decreases effects of sufentanil SL by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Coadministration of opioid mixed agonist/antagonist or partial agonist may reduce sufentail SL analgesic effect and/or precipitate withdrawal symptoms.
sufentanil SL, buprenorphine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may result in hypotension, profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation. - tapentadol
buprenorphine, tapentadol. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx.
- tramadol
tramadol, buprenorphine. Other (see comment). Avoid or Use Alternate Drug. Comment: Tramadol may reinitiate opiate dependence in pts. previously addicted to other opiates; it may also provoke withdrawal Sx. in pts. who are currently opiate dependent.
buprenorphine, tramadol. Other (see comment). Avoid or Use Alternate Drug. Comment: Mixed opiate agonist/antagonists usually produce additive sedation with narcotics; however, in narcotic addicted pts., the antagonist activity may provoke withdrawal Sx. - tranylcypromine
tranylcypromine increases toxicity of buprenorphine by unknown mechanism. Avoid or Use Alternate Drug. Risk of hypotension, hyperpyrexia, somnolence, or death; separate by 14 d.
- tucatinib
tucatinib will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.
- valerian
valerian and buprenorphine both increase sedation. Avoid or Use Alternate Drug.
- voriconazole
voriconazole will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- voxelotor
voxelotor will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.
Monitor Closely (207)
- albuterol
buprenorphine increases and albuterol decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- alfentanil
alfentanil and buprenorphine both increase sedation. Use Caution/Monitor.
- alprazolam
alprazolam and buprenorphine both increase sedation. Use Caution/Monitor.
- amitriptyline
buprenorphine and amitriptyline both increase sedation. Use Caution/Monitor.
- amobarbital
amobarbital and buprenorphine both increase sedation. Use Caution/Monitor.
amobarbital will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - amoxapine
buprenorphine and amoxapine both increase sedation. Use Caution/Monitor.
- apalutamide
apalutamide will decrease the level or effect of buprenorphine by increasing elimination. Use Caution/Monitor. Apalutamide induces UGT and may decrease systemic exposure of drugs that are UGT substrates.
- apomorphine
buprenorphine and apomorphine both increase sedation. Use Caution/Monitor.
- aripiprazole
buprenorphine and aripiprazole both increase sedation. Use Caution/Monitor.
- armodafinil
buprenorphine increases and armodafinil decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- atazanavir
atazanavir increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Potential for increased toxicity.
- azelastine
azelastine and buprenorphine both increase sedation. Use Caution/Monitor.
- baclofen
baclofen and buprenorphine both increase sedation. Use Caution/Monitor.
- belladonna and opium
buprenorphine and belladonna and opium both increase sedation. Use Caution/Monitor.
- benperidol
buprenorphine and benperidol both increase sedation. Use Caution/Monitor.
- benzphetamine
buprenorphine increases and benzphetamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- bosentan
bosentan will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- brexanolone
brexanolone, buprenorphine. Either increases toxicity of the other by sedation. Use Caution/Monitor.
- brompheniramine
brompheniramine and buprenorphine both increase sedation. Use Caution/Monitor.
- buprenorphine, long-acting injection
buprenorphine increases toxicity of buprenorphine, long-acting injection by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of buprenorphine and benzodiazepines or other CNS depressants increases risk of adverse reactions including overdose, respiratory depression, and death. Cessation of benzodiazepines or other CNS depressants is preferred in most cases. In some cases, monitoring at a higher level of care for tapering CNS depressants may be appropriate. In others, gradually tapering a patient off of a prescribed benzodiazepine or other CNS depressant or decreasing to the lowest effective dose may be appropriate.
- butabarbital
butabarbital and buprenorphine both increase sedation. Use Caution/Monitor.
- butalbital
butalbital and buprenorphine both increase sedation. Use Caution/Monitor.
- butorphanol
buprenorphine and butorphanol both increase sedation. Use Caution/Monitor.
- carbamazepine
carbamazepine decreases levels of buprenorphine by increasing metabolism. Use Caution/Monitor. Carbamazepine increases metabolism of buprenorphine; monitor for decreased efficacy.
carbamazepine will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - carbinoxamine
carbinoxamine and buprenorphine both increase sedation. Use Caution/Monitor.
- carisoprodol
carisoprodol and buprenorphine both increase sedation. Use Caution/Monitor.
- cenobamate
cenobamate will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
cenobamate, buprenorphine. Either increases effects of the other by sedation. Use Caution/Monitor. - chloral hydrate
chloral hydrate and buprenorphine both increase sedation. Use Caution/Monitor.
- chlordiazepoxide
chlordiazepoxide and buprenorphine both increase sedation. Use Caution/Monitor.
- chlorpheniramine
chlorpheniramine and buprenorphine both increase sedation. Use Caution/Monitor.
- chlorpromazine
buprenorphine and chlorpromazine both increase sedation. Use Caution/Monitor.
- chlorzoxazone
chlorzoxazone and buprenorphine both increase sedation. Use Caution/Monitor.
- cinnarizine
cinnarizine and buprenorphine both increase sedation. Use Caution/Monitor.
- clemastine
clemastine and buprenorphine both increase sedation. Use Caution/Monitor.
- clobazam
buprenorphine, clobazam. Other (see comment). Use Caution/Monitor. Comment: Concomitant administration can increase the potential for CNS effects (e.g., increased sedation or respiratory depression).
- clomipramine
buprenorphine and clomipramine both increase sedation. Use Caution/Monitor.
- clonazepam
clonazepam and buprenorphine both increase sedation. Use Caution/Monitor.
- clorazepate
clorazepate and buprenorphine both increase sedation. Use Caution/Monitor.
- clozapine
buprenorphine and clozapine both increase sedation. Use Caution/Monitor.
- cobicistat
cobicistat will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- codeine
buprenorphine and codeine both increase sedation. Use Caution/Monitor.
- crizotinib
crizotinib increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Dose reduction may be needed for coadministered drugs that are predominantly metabolized by CYP3A.
- crofelemer
crofelemer increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.
- cyclizine
cyclizine and buprenorphine both increase sedation. Use Caution/Monitor.
- cyclobenzaprine
cyclobenzaprine and buprenorphine both increase sedation. Use Caution/Monitor.
- cyproheptadine
cyproheptadine and buprenorphine both increase sedation. Use Caution/Monitor.
- dabrafenib
dabrafenib will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dantrolene
dantrolene and buprenorphine both increase sedation. Use Caution/Monitor.
- darunavir
darunavir increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Carefully titrate dose when initiating buprenorphine, buprenorphine/naloxone, or methadone with patients taking darunavir/cobicstat. When initiating cobicistat in patients taking buprenorphine, buprenorphine/naloxone, or methadone, adjust dose for buprenorphine, buprenorphine/naloxone, or methadone and monitor clinical signs and symptoms.
- desflurane
desflurane and buprenorphine both increase sedation. Use Caution/Monitor. Opioids may decrease MAC requirements, less inhalation anesthetic may be required.
- desipramine
buprenorphine and desipramine both increase sedation. Use Caution/Monitor.
- deutetrabenazine
buprenorphine and deutetrabenazine both increase sedation. Use Caution/Monitor.
- dexamethasone
dexamethasone will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dexchlorpheniramine
dexchlorpheniramine and buprenorphine both increase sedation. Use Caution/Monitor.
- dexfenfluramine
buprenorphine increases and dexfenfluramine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- dexmedetomidine
dexmedetomidine and buprenorphine both increase sedation. Use Caution/Monitor.
- dextromoramide
buprenorphine and dextromoramide both increase sedation. Use Caution/Monitor.
- diamorphine
buprenorphine and diamorphine both increase sedation. Use Caution/Monitor.
- diazepam
diazepam and buprenorphine both increase sedation. Use Caution/Monitor.
- difenoxin hcl
buprenorphine and difenoxin hcl both increase sedation. Use Caution/Monitor.
- dimenhydrinate
dimenhydrinate and buprenorphine both increase sedation. Use Caution/Monitor.
- diphenhydramine
diphenhydramine and buprenorphine both increase sedation. Use Caution/Monitor.
- diphenoxylate hcl
buprenorphine and diphenoxylate hcl both increase sedation. Use Caution/Monitor.
- dipipanone
buprenorphine and dipipanone both increase sedation. Use Caution/Monitor.
- dopexamine
buprenorphine increases and dopexamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- dosulepin
buprenorphine and dosulepin both increase sedation. Use Caution/Monitor.
- doxepin
buprenorphine and doxepin both increase sedation. Use Caution/Monitor.
- doxylamine
doxylamine and buprenorphine both increase sedation. Use Caution/Monitor.
- droperidol
buprenorphine and droperidol both increase sedation. Use Caution/Monitor.
- efavirenz
efavirenz will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- elagolix
elagolix will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.
- encorafenib
encorafenib, buprenorphine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
- enzalutamide
enzalutamide will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- esketamine intranasal
esketamine intranasal, buprenorphine. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- estazolam
estazolam and buprenorphine both increase sedation. Use Caution/Monitor.
- ethanol
buprenorphine and ethanol both increase sedation. Use Caution/Monitor.
- etomidate
etomidate and buprenorphine both increase sedation. Use Caution/Monitor.
- etravirine
etravirine will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fedratinib
fedratinib will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- fenfluramine
buprenorphine increases and fenfluramine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- flibanserin
buprenorphine and flibanserin both increase sedation. Modify Therapy/Monitor Closely. Risk for sedation increased if flibanserin is coadministration with other CNS depressants.
- fluphenazine
buprenorphine and fluphenazine both increase sedation. Use Caution/Monitor.
- flurazepam
flurazepam and buprenorphine both increase sedation. Use Caution/Monitor.
- fosamprenavir
fosamprenavir increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Potential for increased toxicity. .
- fosphenytoin
fosphenytoin will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- gabapentin
gabapentin, buprenorphine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.
- gabapentin enacarbil
gabapentin enacarbil, buprenorphine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.
- haloperidol
buprenorphine and haloperidol both increase sedation. Use Caution/Monitor.
- hydromorphone
buprenorphine and hydromorphone both increase sedation. Use Caution/Monitor.
- hydroxyzine
hydroxyzine and buprenorphine both increase sedation. Use Caution/Monitor.
- iloperidone
buprenorphine and iloperidone both increase sedation. Use Caution/Monitor.
iloperidone increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4. - imipramine
buprenorphine and imipramine both increase sedation. Use Caution/Monitor.
- indinavir
indinavir increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Potential for increased toxicity. .
- istradefylline
istradefylline will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.
- ketamine
ketamine and buprenorphine both increase sedation. Use Caution/Monitor.
- ketotifen, ophthalmic
buprenorphine and ketotifen, ophthalmic both increase sedation. Use Caution/Monitor.
- lasmiditan
lasmiditan, buprenorphine. Either increases effects of the other by sedation. Use Caution/Monitor. Coadministration of lasmiditan and other CNS depressant drugs, including alcohol have not been evaluated in clinical studies. Lasmiditan may cause sedation, as well as other cognitive and/or neuropsychiatric adverse reactions.
- lemborexant
lemborexant, buprenorphine. Either increases effects of the other by sedation. Modify Therapy/Monitor Closely. Dosage adjustment may be necessary if lemborexant is coadministered with other CNS depressants because of potentially additive effects.
- letermovir
letermovir increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- levorphanol
buprenorphine and levorphanol both increase sedation. Use Caution/Monitor.
- lofepramine
buprenorphine and lofepramine both increase sedation. Use Caution/Monitor.
- lofexidine
buprenorphine and lofexidine both increase sedation. Use Caution/Monitor.
- lopinavir
lopinavir increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Potential for increased toxicity.
- loprazolam
loprazolam and buprenorphine both increase sedation. Use Caution/Monitor.
- lorazepam
lorazepam and buprenorphine both increase sedation. Use Caution/Monitor.
- lorlatinib
lorlatinib will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lormetazepam
lormetazepam and buprenorphine both increase sedation. Use Caution/Monitor.
- loxapine
buprenorphine and loxapine both increase sedation. Use Caution/Monitor.
- loxapine inhaled
buprenorphine and loxapine inhaled both increase sedation. Use Caution/Monitor.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lurasidone
lurasidone, buprenorphine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Potential for increased CNS depressant effects when used concurrently; monitor for increased adverse effects and toxicity.
- maprotiline
buprenorphine and maprotiline both increase sedation. Use Caution/Monitor.
- marijuana
buprenorphine and marijuana both increase sedation. Use Caution/Monitor.
- melatonin
buprenorphine and melatonin both increase sedation. Use Caution/Monitor.
- meperidine
buprenorphine and meperidine both increase sedation. Use Caution/Monitor.
- meprobamate
buprenorphine and meprobamate both increase sedation. Use Caution/Monitor.
- metaxalone
metaxalone and buprenorphine both increase sedation. Use Caution/Monitor.
- methadone
buprenorphine and methadone both increase sedation. Use Caution/Monitor.
- methocarbamol
methocarbamol and buprenorphine both increase sedation. Use Caution/Monitor.
- methylenedioxymethamphetamine
buprenorphine increases and methylenedioxymethamphetamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- midazolam
midazolam and buprenorphine both increase sedation. Use Caution/Monitor.
- midazolam intranasal
midazolam intranasal, buprenorphine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Concomitant use of barbiturates, alcohol, or other CNS depressants may increase the risk of hypoventilation, airway obstruction, desaturation, or apnea and may contribute to profound and/or prolonged drug effect.
- mirtazapine
buprenorphine and mirtazapine both increase sedation. Use Caution/Monitor.
- mitotane
mitotane will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- morphine
buprenorphine and morphine both increase sedation. Use Caution/Monitor.
- motherwort
buprenorphine and motherwort both increase sedation. Use Caution/Monitor.
- moxonidine
buprenorphine and moxonidine both increase sedation. Use Caution/Monitor.
- nabilone
buprenorphine and nabilone both increase sedation. Use Caution/Monitor.
- nafcillin
nafcillin will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nalbuphine
buprenorphine and nalbuphine both increase sedation. Use Caution/Monitor.
- nelfinavir
nelfinavir increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Potential for increased toxicity. .
- nevirapine
nevirapine will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nortriptyline
buprenorphine and nortriptyline both increase sedation. Use Caution/Monitor.
- olanzapine
buprenorphine and olanzapine both increase sedation. Use Caution/Monitor.
- oliceridine
oliceridine, buprenorphine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.
- ombitasvir/paritaprevir/ritonavir & dasabuvir
ombitasvir/paritaprevir/ritonavir & dasabuvir will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increases levels of buprenorphine and active metabolite norbuprenorphine; no dose adjustment of buprenorphine is required, but closely monitor for sedation and cognitive effects
- opium tincture
buprenorphine and opium tincture both increase sedation. Use Caution/Monitor.
- orphenadrine
orphenadrine and buprenorphine both increase sedation. Use Caution/Monitor.
- osilodrostat
osilodrostat and buprenorphine both increase QTc interval. Use Caution/Monitor.
- oxazepam
oxazepam and buprenorphine both increase sedation. Use Caution/Monitor.
- oxcarbazepine
oxcarbazepine will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- oxycodone
buprenorphine and oxycodone both increase sedation. Use Caution/Monitor.
- oxymorphone
buprenorphine and oxymorphone both increase sedation. Use Caution/Monitor.
- paliperidone
buprenorphine and paliperidone both increase sedation. Use Caution/Monitor.
- papaveretum
buprenorphine and papaveretum both increase sedation. Use Caution/Monitor.
- papaverine
buprenorphine and papaverine both increase sedation. Use Caution/Monitor.
- pegvisomant
buprenorphine decreases effects of pegvisomant by unknown mechanism. Use Caution/Monitor.
- pentazocine
buprenorphine and pentazocine both increase sedation. Use Caution/Monitor.
- pentobarbital
pentobarbital and buprenorphine both increase sedation. Use Caution/Monitor.
pentobarbital will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - perampanel
perampanel and buprenorphine both increase sedation. Use Caution/Monitor.
- perphenazine
buprenorphine and perphenazine both increase sedation. Use Caution/Monitor.
- phenobarbital
phenobarbital and buprenorphine both increase sedation. Use Caution/Monitor.
phenobarbital will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - phenylephrine PO
buprenorphine increases and phenylephrine PO decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor. .
- phenytoin
phenytoin will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- pholcodine
buprenorphine and pholcodine both increase sedation. Use Caution/Monitor.
- pimozide
buprenorphine and pimozide both increase sedation. Use Caution/Monitor.
- pregabalin
pregabalin, buprenorphine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.
- primidone
primidone and buprenorphine both increase sedation. Use Caution/Monitor.
primidone will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - prochlorperazine
buprenorphine and prochlorperazine both increase sedation. Use Caution/Monitor.
- promethazine
promethazine and buprenorphine both increase sedation. Use Caution/Monitor.
- propofol
propofol and buprenorphine both increase sedation. Use Caution/Monitor.
- propylhexedrine
buprenorphine increases and propylhexedrine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- protriptyline
buprenorphine and protriptyline both increase sedation. Use Caution/Monitor.
- quazepam
quazepam and buprenorphine both increase sedation. Use Caution/Monitor.
- quetiapine
buprenorphine and quetiapine both increase sedation. Use Caution/Monitor.
- ramelteon
buprenorphine and ramelteon both increase sedation. Use Caution/Monitor.
- remimazolam
remimazolam, buprenorphine. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely. Coadministration may result in profound sedation, respiratory depression, coma, and/or death. Continuously monitor vital signs during sedation and recovery period if coadministered. Carefully titrate remimazolam dose if administered with opioid analgesics and/or sedative/hypnotics.
- ribociclib
ribociclib will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rifabutin
rifabutin will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rifampin
rifampin will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rifapentine
rifapentine will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- risperidone
buprenorphine and risperidone both increase sedation. Use Caution/Monitor.
- ritonavir
ritonavir increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Potential for increased toxicity.
- rolapitant
rolapitant will increase the level or effect of buprenorphine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Rolapitant may increase plasma concentrations of CYP2D6 substrates for at least 28 days following rolapitant administration.
- rucaparib
rucaparib will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- saquinavir
saquinavir increases levels of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Potential for increased toxicity. .
- scullcap
buprenorphine and scullcap both increase sedation. Use Caution/Monitor.
- secobarbital
secobarbital and buprenorphine both increase sedation. Use Caution/Monitor.
secobarbital will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. May also enhance CNS depressant effect of buprenorphine - sevoflurane
sevoflurane and buprenorphine both increase sedation. Use Caution/Monitor.
- shepherd's purse
buprenorphine and shepherd's purse both increase sedation. Use Caution/Monitor.
- sodium sulfate/?magnesium sulfate/potassium chloride
sodium sulfate/?magnesium sulfate/potassium chloride increases toxicity of buprenorphine by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias.
- sodium sulfate/potassium sulfate/magnesium sulfate
sodium sulfate/potassium sulfate/magnesium sulfate increases toxicity of buprenorphine by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias.
- St John's Wort
St John's Wort will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- stiripentol
stiripentol, buprenorphine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
stiripentol, buprenorphine. Either increases effects of the other by sedation. Use Caution/Monitor. Concomitant use stiripentol with other CNS depressants, including alcohol, may increase the risk of sedation and somnolence. - sufentanil
buprenorphine and sufentanil both increase sedation. Use Caution/Monitor.
- suvorexant
suvorexant and buprenorphine both increase sedation. Modify Therapy/Monitor Closely. Dosage adjustments of suvorexant and concomitant CNS depressants may be necessary
- tapentadol
buprenorphine and tapentadol both increase sedation. Use Caution/Monitor.
- tazemetostat
tazemetostat will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- temazepam
temazepam and buprenorphine both increase sedation. Use Caution/Monitor.
- thioridazine
buprenorphine and thioridazine both increase sedation. Use Caution/Monitor.
- thiothixene
buprenorphine and thiothixene both increase sedation. Use Caution/Monitor.
- tipranavir
tipranavir will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- topiramate
buprenorphine and topiramate both increase sedation. Modify Therapy/Monitor Closely.
- tramadol
buprenorphine and tramadol both increase sedation. Use Caution/Monitor.
- trazodone
buprenorphine and trazodone both increase sedation. Use Caution/Monitor.
- triazolam
triazolam and buprenorphine both increase sedation. Use Caution/Monitor.
- triclofos
triclofos and buprenorphine both increase sedation. Use Caution/Monitor.
- trifluoperazine
buprenorphine and trifluoperazine both increase sedation. Use Caution/Monitor.
- trimipramine
buprenorphine and trimipramine both increase sedation. Use Caution/Monitor.
- triprolidine
triprolidine and buprenorphine both increase sedation. Use Caution/Monitor.
- xylometazoline
buprenorphine increases and xylometazoline decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- ziconotide
buprenorphine and ziconotide both increase sedation. Use Caution/Monitor.
- ziprasidone
buprenorphine and ziprasidone both increase sedation. Use Caution/Monitor.
- zotepine
buprenorphine and zotepine both increase sedation. Use Caution/Monitor.
Minor (7)
- brimonidine
brimonidine increases effects of buprenorphine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- dextroamphetamine
dextroamphetamine increases effects of buprenorphine by unspecified interaction mechanism. Minor/Significance Unknown.
- elvitegravir
elvitegravir increases levels of buprenorphine by unknown mechanism. Minor/Significance Unknown. No dose adjustment of buprenorphine/naloxone is required upon coadministration with VITEKTA. Patients should be closely monitored for sedation and cognitive effects.
- eucalyptus
buprenorphine and eucalyptus both increase sedation. Minor/Significance Unknown.
- lidocaine
lidocaine increases toxicity of buprenorphine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- sage
buprenorphine and sage both increase sedation. Minor/Significance Unknown.
- ziconotide
ziconotide, buprenorphine. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Additive decreased GI motility. Additive analgesia. Ziconotide does NOT potentiate opioid induced respiratory depression.
Adverse Effects
>10% (SL)
Headache (29.1-30%)
Pain (18.4-24%)
Withdrawal syndrome (18.4-22%)
Insomnia (21.4%)
Infection (20%)
Asthenia (14%)
Back pain (7.8-14%)
Nausea (10-13.6%)
Sweating (12-12.6%)
Abdominal pain (11.7%)
Infection (11.7%)
Constipation (7.8-11%)
1-10% (IV/IM)
5-10%
- Nausea
- Dizziness/vertigo
1-5%
- Sweating
- Headache
- Hypotension
- Nausea/vomiting
- Hypoventilation
- Miosis
1-10% (SL)
Rhinitis (9.7%)
Chills (6-7.8%)
Vomiting (5-7.8%)
Flu syndrome (6%)
Nervousness (6%)
Runny eyes (5%)
Diarrhea (4.9-5%)
Asthenia (4.9%)
Vasodilation (3.9%)
Fever (3%)
Dyspepsia (3%)
Accidental injury (2-3%)
Abscess (2%)
<1%
Confusion, blurred vision, euphoria, weakness/fatigue, dry mouth, nervousness, depression, slurred speech, paresthesia
Hypertension, tachycardia, bradycardia
Constipation
Dyspnea, cyanosis
Pruritus
Diplopia, visual abnormalities
Injection site reaction, urinary retention, dreaming, flushing/warmth, chills/cold, tinnitus, conjunctivitis, Wenckebach block, and psychosis
Other effects observed infrequently include malaise, hallucinations, depersonalization, coma, dyspepsia, flatulence, apnea, rash, amblyopia, tremor, and pallor
Postmarketing Reports
Serotonin syndrome
Adrenal insufficiency
Anaphylaxis
Androgen deficiency
Glossodynia, glossitis, oral mucosal erythema, oral hypoesthesia, and stomatitis
Warnings
Black Box Warnings
Opioid analgesic risk evaluation and mitigation strategy (REMS)
- To ensure that benefits of opioid analgesics outweigh risks of addiction, abuse, and misuse, the Food and Drug Administration (FDA) has required a REMS for these products; under requirements of the REMS, drug companies with approved opioid analgesic products must make REMS-compliant education programs available to healthcare providers
Healthcare providers are strongly encouraged to:
- Complete a REMS-compliant education program
- Counsel patients and/or their caregivers, with every prescription, on safe use, serious risks, storage, and disposal of these products
- Emphasize to patients and their caregivers the importance of reading the Medication Guide every time it is provided by their pharmacist
- Consider other tools to improve patient, household, and community safety
- To obtain further information on opioid analgesic REMS and for a list of accredited REMS CME/CE, call 1-800-503-0784, or log on to www.opioidanalgesicrems.com; the FDA Blueprint can be found at www.fda.gov/OpioidAnalgesicREMSBlueprint
Addiction, abuse, and misuse
- Risk of opioid addiction, abuse, and misuse, which can lead to overdose and death
- Assess each patient’s risk prior to prescribing and monitor all patients regularly for the development of these behaviors or conditions
Life-threatening respiratory depression
- Serious, life-threatening, or fatal respiratory depression may occur
- Monitor for respiratory depression, especially during initiation or following a dose increase
Accidental exposure
- Accidental exposure of even 1 dose, especially by children, can result in a fatal overdose
Neonatal opioid withdrawal syndrome
- Prolonged use during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated, and requires management according to protocols developed by neonatology experts
- Syndrome presents as irritability, hyperactivity and abnormal sleep pattern, high-pitched cry, tremor, vomiting, diarrhea, and failure to gain weight
- Onset, duration, and severity of neonatal opioid withdrawal syndrome vary based on the specific opioid used, duration of use, timing and amount of last maternal use, and rate of elimination of the drug by the newborn
- If opioid use is required for a prolonged period in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available
Risks from concomitant use with benzodiazepines or other CNS depressants
- Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death; reserve concomitant use in patients for whom alternative treatment options are inadequate; limit dosages and durations to minimum required; and monitor for signs and symptoms of respiratory depression and sedation
Contraindications
Hypersensitivity
Significant respiratory depression
Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment
Known or suspected gastrointestinal obstruction, including paralytic ileus
Cautions
Partial agonist at the mu opioid receptor and a schedule III controlled opioid exposes users to the risks of addiction, abuse, and misuse; there is a greater risk for overdose and death with extended-release opioids owing to the larger amount of active opioid present (see Black Box Warnings)
Serious, life-threatening, or fatal respiratory depression reported; may occur more frequently in elderly or debilitated patients, or in conditions associated with hypoxia or hypercapnia (even moderate therapeutic doses) (see Black Box Warnings)
Neonatal opioid withdrawal syndrome reported with long-term use during pregnancy (see Black Box Warnings)
Do not abruptly discontinue buprenorphine in a patient physically dependent on opioids; when discontinuing therapy, in a physically dependent patient, gradually taper the dosage; rapid tapering in a patient physically dependent on opioids may lead to a withdrawal syndrome and return of pain
Accidental exposure reported, including fatalities (see Black Box Warnings)
May impair mental or physical abilities needed to perform potentially hazardous activities (eg, driving a car, operating machinery)
Risk of apnea in patients with chronic pulmonary disease; closely monitor these patients, when initiating and titrating therapy; alternatively, consider the use of alternative non-opioid analgesics in these patients (see Black Box Warnings and Contraindications)
QTc prolongation observed in healthy individuals at 40 mcg/hr; avoid in patients with history of long QT syndrome or coadministration with class IA (eg, quinidine, procainamide, disopyramide) or class III (eg, sotalol, amiodarone, dofetilide) antiarrhythmics
Respiratory depressant effects of opioids may include carbon dioxide retention and lead to elevated CSF pressure
Opioids can cause sleep-related breathing disorders including central sleep apnea (CSA) and sleep-related hypoxemia; opioid use increases risk of CSA in a dose-dependent fashion; in patients who present with CSA, consider decreasing opioid dosage using best practices for opioid taper
Can cause severe hypotension; caution with depleted blood volume or coadministration of drugs that that affect vasomotor tone (eg, phenothiazines), vasodilators, or antihypertensives
Hypothyroidism, myxedema, adrenocortical insufficiency, alcohol intoxication, alcohol withdrawal syndrome, coma, geriatric or debilitated patients, delirium tremens, toxic psychoses, kyphoscoliosis, prostatic hypertrophy, urethral stricture, central nervous system (CNS) depression, biliary tract dysfunction, head injury, intracranial lesions, intracranial hypertension or conditions in which intracranial pressure may be increased
Cases of cytolytic hepatitis and hepatitis with jaundice observed in individuals receiving buprenorphine SL for opioid dependence treatment; increased risk for overdose with moderate or severe hepatic impairment (see Dosage Modifications)
Anaphylactic reactions reported
May cause sphincter of Oddi spasm and aggravate abdominal conditions, including ileus (see Contraindications)
Similar to other opioids, may aggravate seizure disorders by lowering seizure threshold
Special risk groups may experience increased adverse reactions; caution with alcoholism, delirium tremens, adrenocortical insufficiency, CNS depression, debilitation, kyphoscoliosis associated with respiratory compromise, myxedema or hypothyroidism, prostatic hypertrophy or urethral stricture, severe impairment of hepatic, pulmonary or renal function, and toxic psychosis
Prescribers should discuss with patients importance and benefits of management of opioid addiction throughout pregnancy
Cases of adrenal insufficiency reported with opioid use, more often following greater than one month of use; symptoms may include nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure; if adrenal insufficiency is diagnosed, treat with physiologic replacement doses of corticosteroids; wean patient off of opioid to allow adrenal function to recover and continue corticosteroid treatment until adrenal function recovers; other opioids may be tried as some cases reported use of a different opioid without recurrence of adrenal insufficiency
Consider discontinuing therapy 24-36 hr prior anticipated need for surgical anesthesia to undergo elective surgery; may administer short-acting opioids during and/or after surgery; in patients unable to abruptly discontinue therapy may add full opioid to buprenorphine to maintain proper anesthesia; increased doses may be required to overcome buprenorphine receptor blockade; continuously monitor if opioid therapy required as part of anesthesia in an anesthesia care setting
Abrupt discontinuation following prolonged therapy may lead to withdrawal symptoms; not recommended; taper gradually
Use caution in patients who are morbidly obese
Avoid use in patients with impaired consciousness or coma; patients are susceptible to intracranial effects of CO2 retention
Use caution in patients with a history of ileus or bowel obstruction; contraindicated in patients with known or suspected GI obstruction including paralytic ileus
Chronic use of opioids may cause reduced fertility in females and males of reproductive potential; unknown whether effects on fertility are reversible (see Pregnancy)
Patient access to naloxone for emergency treatment of opioid overdose
- Assess potential need for naloxone; consider prescribing for emergency treatment of opioid overdose
- Consult on availability and ways to obtain naloxone as permitted by individual state naloxone dispensing and prescribing requirements or guidelines
- Educate patients regarding the signs and symptoms of respiratory depression and to call 911 or seek immediate emergency medical help in the event of a known or suspected overdose
Drug interactions overview
- Concomitant use of buprenorphine and benzodiazepines, a muscle relaxant, or other CNS depressants increases risk of adverse reactions including overdose and death; if an opioid analgesic is initiated in a patient already taking a benzodiazepine or other CNS depressant, prescribe a lower initial dose of the opioid analgesic, and titrate based on clinical response; follow patients closely for signs and symptoms of respiratory depression and sedation; if concomitant use with benzodiazepine ior muscle relaxant s warranted, consider prescribing naloxone for the emergency treatment of opioid overdose (See Black Box Warnings)
- Opioids may reduce efficacy of diuretics by inducing release of antidiuretic hormone
- Anticholinergic drugs may increase risk of urinary retention and/or severe constipation, which may lead to paralytic ileus; monitor for signs of urinary retention or reduced gastric motility when buprenorphine is concomitantly used with anticholinergics
-
Serotonergic drugs
- Opioids may enhance serotonergic effect of drugs (eg, selective serotonin reuptake inhibitors, monoamine oxidase inhibitors) that affect the serotonergic neurotransmitter system; which increases the risk of serotonin syndrome; if concomitant use is warranted, monitor; discontinue if serotonin syndrome is suspected
- Use of MAOIs with buprenorphine is not recommended during or within 14 days of discontinuing treatment
-
CYP3A4 inhibitors
- Concomitant use of buprenorphine and CYP3A4 inhibitor may increase the plasma concentration of buprenorphine, resulting increased or prolonged opioid effects; specifically when adding a CYP3A4 inhibitor after achieving a stable buprenorphine dose
-
CYP3A4 inducers
- Concomitant use of buprenorphine and CYP3A4 inducers may decrease plasma concentration of buprenorphine, potentially resulting in decreased efficacy or onset of a withdrawal syndrome in patients who have developed physical dependence to buprenorphine
Pregnancy & Lactation
Pregnancy
Data in pregnancy are limited; however, these data do not indicate an increased risk of major malformations specifically due to buprenorphine exposure; observational studies reported on congenital malformations among exposed pregnancies, but were also not designed appropriately to assess risk of congenital malformations specifically due to drug exposure
Dosage adjustments of buprenorphine may be required during pregnancy, even if patient was maintained on stable dose prior to pregnancy; withdrawal signs and symptoms should be monitored closely and the dose adjusted as necessary
Fetal/neonatal adverse reactions
- Neonatal opioid withdrawal syndrome may occur in newborn infants of mothers who are receiving treatment
Lactation
Data on two studies in 13 lactating women receiving therapy where the drug and it metabolite were present in low levels in human milk did not show adverse reactions in breastfed infants; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition
Advise breastfeeding women taking buprenorphine products to monitor infant for increased drowsiness and breathing difficulties
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Semisynthetic narcotic mixed agonist-antagonist analgesic; exerts agonistic effects at mu and delta opioid receptors in CNS and antagonistic effects at kappa opioid receptor
Absorption
Onset: 15 min (IM); ~1 hr (IV)
Duration: >6 hr (IM)
Peak plasma time: 1.84 hr (2-mg SL dose); 1.28 hr (8-mg SL dose); 1.42 hr (16-mg SL dose)
Peak plasma concentration: 1.25 ng/mL (2-mg SL dose); 2.88 ng/mL (8-mg SL dose); 4.7 ng/mL (16-mg SL dose)
AUC: 10.93 hr·ng/mL (2-mg SL dose); 28.39 hr·ng/mL (8-mg SL dose); 47.09 hr·ng/mL (16-mg SL dose)
Distribution
Protein bound: 96%, primarily to alpha and beta globulin
Metabolism
Buprenorphine undergoes both N-dealkylation to norbuprenorphine and glucuronidation
N-dealkylation pathway is mediated primarily by CYP3A4
Metabolites: Norbuprenorphine (N-dealkylbuprenorphine)
Elimination
Mean half-life: 2.2 hr (IV); 31-35 hr (SL)
Excretion: Urine (30%), feces (69%)
Administration
IV Incompatibilities
Additive: Floxacillin, furosemide
Y-site: Amphotericin B cholesteryl sulfate, doxorubicin liposomal
IV Compatibilities
Additive: Bupivacaine
Syringe: Heparin, midazolam
Y-site: Allopurinol, amifostine, aztreonam, cefepime, cisatracurium, cladribine, docetaxel, etoposide phosphate, filgrastim, gatifloxacin, gemcitabine, granisetron, linezolid, melphalan, piperacillin-tazobactam, propofol, remifentanil, teniposide, thiotepa, vinorelbine
IV Preparation
Solution: Dilute to final concentration of 15 mcg/mL in D5W, D5/NS, NS, or LR
Administer via controlled infusion device
IV/IM Administration
Administer by deep IM injection or by slow IV injection over ≥2 minutes
Storage
Injection: Store at 20-25°C (68-77°F)
SL tablets: Store at 20-25°C (68-77°F); excursions permitted between 15-30°C (59-86°F)
Protect from prolonged exposure to light
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Butrans transdermal - | 20 mcg/hour transdermal system |  | |
| Butrans transdermal - | 5 mcg/hour transdermal system |  | |
| Butrans transdermal - | 15 mcg/hour transdermal system |  | |
| Butrans transdermal - | 7.5 mcg/hour transdermal system |  | |
| Butrans transdermal - | 10 mcg/hour transdermal system |  | |
| Sublocade subcutaneous - | 300 mg/1.5 mL solution |  | |
| Sublocade subcutaneous - | 100 mg/0.5 mL solution |  | |
| buprenorphine transdermal - | 5 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 10 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 10 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 5 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 20 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 5 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 15 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 10 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 15 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 20 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 15 mcg/hour transdermal system |  | |
| buprenorphine transdermal - | 20 mcg/hour transdermal system |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
buprenorphine transdermal
BUPRENORPHINE - TRANSDERMAL
(BUE-pre-NOR-feen)
COMMON BRAND NAME(S): Butrans
WARNING: Buprenorphine has a risk for abuse and addiction, which can lead to overdose and death. Buprenorphine may also cause severe, possibly fatal, breathing problems. To lower your risk, your doctor should have you use the smallest dose of buprenorphine that works, and use it for the shortest possible time. See also How to Use section for more information about addiction.The risk for severe breathing problems is higher when you start this medication and after a dose increase, or if you use the wrong dose/strength or misuse the medication (such as chewing or swallowing the patch). Using this medication with alcohol or other drugs that can cause drowsiness or breathing problems may cause very serious side effects, including death. Be sure you know how to use buprenorphine and what other drugs you should avoid taking with it. See also Drug Interactions section. Get medical help right away if any of these very serious side effects occur: slow/shallow breathing, unusual lightheadedness, severe drowsiness/dizziness, difficulty waking up.Keep this medicine in a safe place to prevent theft, misuse, or abuse. If someone accidentally swallows or uses this drug, get medical help right away because fatal breathing problems may occur.Before using this medication, women of childbearing age should talk with their doctor(s) about the risks and benefits. Tell your doctor if you are pregnant or if you plan to become pregnant. During pregnancy, this medication should be used only when clearly needed. It may slightly increase the risk of birth defects if used during the first two months of pregnancy. Also, using it for a long time or in high doses near the expected delivery date may harm the unborn baby. To lessen the risk, use the smallest effective dose for the shortest possible time. Babies born to mothers who use this drug for a long time may develop severe (possibly fatal) withdrawal symptoms. Tell the doctor right away if you notice any symptoms in your newborn baby such as crying that doesn't stop, slow/shallow breathing, irritability, shaking, vomiting, diarrhea, poor feeding, or difficulty gaining weight.
USES: This medication is used to help relieve severe ongoing pain (such as due to arthritis, chronic back pain). Buprenorphine belongs to a class of drugs known as opioid analgesics. It works in the brain to change how your body feels and responds to pain.The higher strengths of this drug (7.5, 10, 15, or 20 micrograms per hour patches) should be used only if you have been regularly taking moderate amounts of opioid pain medication. These strengths may cause overdose (even death) if used by a person who has not been regularly taking opioids.Do not use this medication to relieve pain that is mild or that will go away in a few days. This medication is not for occasional ("as needed") use.
HOW TO USE: See also Warning section.Read the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start using this medication and each time you get a refill. Learn how to properly use, store, and discard the patches. If you have any questions, ask your doctor or pharmacist.Use this medication on a regular schedule as directed by your doctor, not as needed for sudden (breakthrough) pain. If you are already using an opioid medication, ask your doctor or pharmacist if you should stop or change how you use your other opioid medication. It may take 24 hours or longer before you have pain relief from buprenorphine patches. Other pain relievers (such as acetaminophen, ibuprofen) may also be prescribed. Ask your doctor or pharmacist about using buprenorphine safely with other drugs.Apply this medication to the skin as directed by your doctor. Do not apply on burns, cuts, irritated skin, or skin that has been exposed to radiation (x-ray treatment). Select a dry, non-hairy area on a flat part of your body, such as the upper chest, sides of the chest, upper back, or upper outer arms. In people unable to think clearly (such as due to dementia), apply the patch on the upper back to lessen the chance it might be removed or placed in the mouth. If there is hair on the skin, use scissors to clip the hair as close as possible to the skin. Do not shave hair since this might cause skin irritation. If needed, use water to clean the area. Do not use soap, oils, lotions, or alcohol on the application site. Dry the skin well before applying the patch.The patch is usually changed every 7 days. To avoid irritation, apply to a different area each time and do not apply to the same site within 3 weeks. Be sure to remove the old patch before applying a new patch. The used patch should be folded in half with the sticky sides together and properly discarded. If your manufacturer has supplied a patch disposal unit, follow directions for its use.Do not use the patch if it appears to be broken, cut, or damaged. Remove from the sealed pouch, peel off the protective liner, and apply right away to the skin. Press firmly in place with the palm of the hand for about 15 to 30 seconds, making sure the contact is complete (especially around the edges). If your prescribed dose is for more than one patch, apply them right next to each other but make sure the edges of the patches do not touch or overlap. After applying the patch, wash your hands with water only.You may bathe, shower, or swim while wearing the patch. If you have problems with the patch not sticking at the application site, you may tape the edges in place with certain kinds of first aid tape. Ask your doctor or pharmacist about which type of tape should be used. If this problem persists, ask your doctor for advice. If the patch falls off before 7 days, a new patch may be applied to a different skin site. Be sure to let your doctor know if this happens.If you accidentally touch the sticky layer to your skin or handle a cut or damaged patch, wash the area well with clear water. If the patch comes off and accidentally sticks to the skin of another person, immediately remove the patch, wash the area with water, and get medical help for them right away. Do not use soap, alcohol, or other products to wash the area.The dosage is based on your medical condition and response to treatment. Do not apply more patches than directed, change them more frequently, or use them for a longer time than prescribed. Your risk for side effects will increase.Suddenly stopping this medication may cause withdrawal, especially if you have used it for a long time or in high doses. To prevent withdrawal, your doctor may lower your dose slowly. Tell your doctor or pharmacist right away if you have any withdrawal symptoms such as restlessness, mental/mood changes (including anxiety, trouble sleeping, thoughts of suicide), watering eyes, runny nose, nausea, diarrhea, sweating, muscle aches, or sudden changes in behavior.When this medication is used for a long time, it may not work as well. Talk with your doctor if this medication stops working well.Though it helps many people, this medication may sometimes cause addiction. This risk may be higher if you have a substance use disorder (such as overuse of or addiction to drugs/alcohol). Use this medication exactly as prescribed to lower the risk of addiction. Ask your doctor or pharmacist for more details.Tell your doctor if your pain does not get better or if it gets worse.
SIDE EFFECTS: See also Warning section.Nausea, vomiting, constipation, lightheadedness, dizziness, drowsiness, dry mouth, or headache may occur. Irritation, itching, or redness at the application site may also occur. Some of these side effects may decrease after you have been using this medication for a while. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.To prevent constipation, eat dietary fiber, drink enough water, and exercise. You may also need to take a laxative. Ask your pharmacist which type of laxative is right for you.To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: interrupted breathing during sleep (sleep apnea), mental/mood changes (such as agitation, confusion, hallucinations), difficulty urinating, swelling/blistering at the patch application site, signs of your adrenal glands not working well (such as unusual tiredness, weight loss).Get medical help right away if you have any very serious side effects, including: fainting, seizure, slow/shallow breathing, severe drowsiness/difficulty waking up, fast/irregular heartbeat, severe dizziness.This drug may rarely cause serious liver disease. Get medical help right away if you have any symptoms of liver damage, including: dark urine, persistent nausea/vomiting, loss of appetite, yellowing eyes/skin, severe stomach/abdominal pain.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before using buprenorphine, tell your doctor or pharmacist if you are allergic to it; or to adhesives; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: brain disorders (such as head injury, tumor, seizures), breathing problems (such as asthma, sleep apnea, chronic obstructive pulmonary disease-COPD), kidney disease, liver disease, mental/mood disorders (such as confusion, depression), personal or family history of a substance use disorder (such as overuse of or addiction to drugs/alcohol), stomach/intestinal problems (such as blockage, constipation, diarrhea due to infection, paralytic ileus), difficulty urinating (such as due to enlarged prostate), disease of the pancreas (pancreatitis), gallbladder disease.Buprenorphine may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using buprenorphine, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using buprenorphine safely.This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Raising your skin/body temperature may cause overdose. Avoid increasing your skin temperature at or near the application site (for example, using products such as heating pads, electric blankets, hot tubs, heat or tanning lamps). Avoid taking hot baths and sunbathing. Tell your doctor promptly if you develop a fever.If you are going to have an MRI test, tell testing personnel that you are using this patch. Some patches may contain metals that can cause serious burns during an MRI. Ask your doctor whether you will need to remove your patch before the test and apply a new patch afterward, and how to do so properly.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the effects of this drug, especially confusion, dizziness, drowsiness, slow/shallow breathing, and QT prolongation (see above).During pregnancy, this medication should be used only when clearly needed. It may harm an unborn baby. Discuss the risks and benefits with your doctor. (See also Warning section.)This drug passes into breast milk and may have undesirable effects on a nursing infant. Tell the doctor right away if your baby develops unusual sleepiness, difficulty feeding, or trouble breathing. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: See also Warning section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: certain pain medications (mixed opioid agonist-antagonists such as pentazocine, nalbuphine, butorphanol), naltrexone.Many drugs besides buprenorphine may affect the heart rhythm (QT prolongation), including amiodarone, dofetilide, disopyramide, quinidine, procainamide, sotalol, among others.The risk of serious side effects (such as slow/shallow breathing, severe drowsiness/dizziness) may be increased if this medication is used with other products that may also cause drowsiness or breathing problems. Tell your doctor or pharmacist if you are taking other products such as other opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana (cannabis), drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine).Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.This medication may interfere with certain laboratory tests (including amylase/lipase levels), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.
OVERDOSE: This medication patch may be harmful if chewed or swallowed. If someone has overdosed, remove the patch if possible. For serious symptoms such as passing out or trouble breathing, give them naloxone if available, then call 911. If the person is awake and has no symptoms, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: slow/shallow breathing, slow heartbeat, coma.
NOTES: Do not share this medication with others. Sharing it is against the law.This medication has been prescribed for your current condition only. Do not use it later for another condition unless told to do so by your doctor. A different medication may be necessary in that case.Ask your doctor or pharmacist if you should have naloxone available to treat opioid overdose. Teach your family or household members about the signs of an opioid overdose and how to treat it.
MISSED DOSE: If you leave a patch on for more than 7 days, remove the patch and apply a new patch as soon as you remember. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not freeze. Keep all medications away from children and pets. See also Warning section.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed (see also How to Use section). For more details, read the Medication Guide, or consult your pharmacist or local waste disposal company.
Information last revised April 2020. Copyright(c) 2021 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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- View the formulary and any restrictions for each plan.
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