Drug reference

Buprenorphine

Opioid Analgesic · Opioid

Opioid AnalgesicOpioid

CDSCO approvedSchedule X

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Use lowest dose; neonatal withdrawal symptoms

FDA category + note

Top interactionssee all 12 →

AcetaminophenSevereTextbookHarrison 22e · p98-99
BarbituratesSevereTextbookKDT 7e · p401
BenzodiazepinesSevereTextbookKDT 7e · p383
Chlordiazepoxide HydrochlorideSevereTextbookG&G 14e

Mechanism

Buprenorphine functions as a partial agonist at μ-opioid receptors. It binds to these receptors, including those in ventilatory pacemaker neurons of the brainstem, to produce a submaximal agonistic effect. This results in analgesia with a reduced risk of severe respiratory depression compared to full agonists. However, its mixed agonist-antagonist properties can also precipitate withdrawal in opioid-dependent individuals or diminish the effect of more efficacious opioids.

Indications

opioid abuse and withdrawalmild-to-moderate painmanagement of opioid use disorderOpioid use disorder maintenance treatmentOpioid use disorder induction of treatmentAnalgesiclong-lasting painful conditions requiring an opioid analgesic (e.g. cancer pain)premedicationpostoperative painmyocardial infarctiontreatment of morphine dependence

Dosing

Adult: Pain (sublingual): 200-400 mcg every 6-8h. Transdermal (Butrans): initially 5 mcg/h patch every 7 days. Opioid dependence (sublingual): initially 0.8-4 mg day 1, adjusted by 2-4 mg daily; usual 12-24 mg daily.
Pediatric: Parenteral: 0.004 mg/kg/6–8 h
Max dose: 32 mg/day (dependence)

Pharmacokinetics

Peak effect

Intramuscular: 5 min (blood peak); Oral/Sublingual: 1-2 h (blood peak)

Duration

Onset of action is slower and duration longer. After a single dose, analgesia lasts for 6–8 hours. With repeated dosing, duration of action increases to ~24 hours due to accumulation in tissues. Remains in tissues for several days.

Half-life

3 h (plasma); ~170 min (dissociation from mu receptor)

Bioavailability

SL: 51 ± 13%; BC: 28 ± 9%

Protein binding

96%

Metabolism

Metabolized to norbuprenorphine by CYP3A4

Excretion

Negligible

Contraindications

Concomitant use with CNS depressants
use during labour (neonatal respiratory depression cannot be effectively reversed by naloxone)

Side effects

Common

Respiratory depressionSomnolencesedationvomitingmiosissubjective effects (similar to morphine)cardiovascular effects (similar to morphine)constipation (less marked than morphine)postural hypotension (prominent)respiratory depression (exhibits ceiling effect)

Serious

Potentially fatal respiratory depression
respiratory depression (less than full agonists, has ceiling effect)
precipitation of withdrawal (in opioid-dependent patients taking full agonists)
adverse effects in breastfed infants (if given with CYP3A4 inhibitors)
Precipitate withdrawal (if other opioids are present)

Pregnancy & lactation

Pregnancy

Use lowest dose; neonatal withdrawal symptoms

Drug interactions

Acetaminophen

Severe

Textbook

Acetaminophen-related hepatotoxicity, a significant cause for liver failure.

Many practitioners have moved away from opioid-acetaminophen combination analgesics to avoid the risk of excessive acetaminophen exposure.

Source: Harrison 22e · p98-99

Barbiturates

Severe

Textbook

Exaggerated CNS depression.

Source: KDT 7e · p401

Benzodiazepines

Severe

Textbook

Marked depression of respiration, cardiac contractility, and blood pressure.

Carefully monitor respiratory and cardiovascular functions when co-administering benzodiazepines with opioids due to increased risk of severe depression of vital signs.

Source: KDT 7e · p383

Chlordiazepoxide Hydrochloride

Severe

Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: G&G 14e

Clomethiazole

Severe

Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.