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BuprenorphineAka: Subutex

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  1. Indications
    1. Pain management (intravenous Buprenorphine)
    2. Opioid Addiction (e.g. Heroin addiction)
      1. Alternative to low dose Methadone
      2. Prescribing requires FDA waiver
  2. Contraindications
    1. Use caution and liver function monitoring in hepatitis
  3. Mechanism
    1. Partial mu-Opioid receptor agonist
    2. Mu-receptor activation increases with dose to ceiling
      1. No further activation once max dose effect is reached
      2. Hence, unlike heroin or Methadone, low risk of abuse
    3. Slowly dissociates from mu-receptors
      1. May block other Narcotic binding
      2. May displace recently taken Opioids
        1. May result in Opioid withdrawal symptoms
  4. Pharmacokinetics
    1. Metabolism: Liver via P450
    2. Plasma half-life: 37 hours
    3. Routes
      1. Oral bioavailability is too low to be useful
      2. Intravenous route used for pain management
      3. Sublingual is preferred route
        1. Bioavailability: Up to 50% of IV dose
        2. Peak concentration reached 1 hour post-dose
  5. Drug Interactions
    1. P450 Inducers may decrease Buprenorphine effect
      1. Carbamazepine
      2. Phenytoin
      3. Phenobarbital
      4. Reverse Transcriptase Inhibitors
      5. Rifampin
    2. P450 Inhibitors may increase Buprenorphine effect
      1. Azole Antifungals (e.g. Ketoconazole, Fluconazole)
      2. Macrolides (e.g. Erythromycin, Azithromycin)
  6. Efficacy: Buprenorphine compared with Methadone
    1. Low dose Methadone (<40 mg): Buprenorphine as effective
    2. High dose Methadone (>60 mg): Not as effective
    3. References
      1. Barnett (2001) Addiction 96:683
  7. Pregnancy
    1. FDA Category C
  8. Adverse Effects
    1. Constipation
    2. Urinary Retention
    3. Sedation
    4. Mild respiratory depression
    5. Opioid Withdrawal
  9. Toxicity
    1. Overdose has occured when taken with Benzodiazepines
  10. Formulations
    1. Pain management
      1. Buprenorphine intravenous
    2. Opioid addiction
      1. Buprenorphine sublingual
      2. Buprenorphine with Naloxone sublingual
  11. Dosing: Prescriber must have FDA waiver
    1. Induction Phase (3-7 days)
      1. Started >12 hours after last short acting Narcotic
      2. Started >24 hours after last long acting Narcotic
      3. Adjusted based on physician evaluation, withdrawal
        1. Day 1: 2 mg every 1-2 hours to max 8-12 mg/day
        2. By day 7: Maximum of 32 mg/day
    2. Stabilization Phase (1-2 months)
      1. Identify minimum effective dose
      2. Typical: Buprenorphine 12-24 mg/day divided
    3. Maintenance Phase (indefinite)
      1. Dosing based on stabilization phase
  12. References
    1. Donaher (2006) Am Fam Physician 73(9):1573
    2. Fudala (2003) N Engl J Med 349:949

Subutex (C0006404)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD002047
EnglishBuprex, Essex Brand of Buprenorphine Hydrochloride, Reckitt & Colman Brand 2 of Buprenorphine Hydrochloride, Reckitt Benckiser Brand of Buprenorphine Hydrochloride, Reckitt Brand of Buprenorphine Hydrochloride, Schering Plough Brand of Buprenorphine Hydrochloride, Schering-Plough Brand of Buprenorphine Hydrochloride, Subutex, Temgesic
SourcesMSH, MTH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Buprenorphine (C0006405)

Definition (MSH)A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.
Definition (CSP)21-cyclopropyl-7-alpha-(2-hydroxy-3, 3-dimethyl-2-butyl)-6,14-endo-ethano -6,7,8,14-tetrahydro oripavine, a narcotic analgesic with mixed agonist-antagonist opiate properties; potential efficacy in heroin withdrawal.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD002047
EnglishBuprenorphine, BUPRENORPHINE PREPARATION, Buprenorphine product
Spanishbuprenorfina, producto con buprenorfina
Parent Conceptsoripavine derivative opioids (C0682979), Morphinans (C0026548), Narcotic Antagonists (C0027410), Opioids (C0242402), Opioid Receptor Agonist (C1883695), Analgesics, Opioid (C0002772), Opiate partial agonist (C0304353), Morphinan opioid (C0360445), Duplicate concept (C1274013), Opiate agonist-antagonist (C1299972), Drug allergen (C1320237), Opioid Analgesics, Short-acting (C1579331)
SourcesAOD, CSP, LCH, LNC, MSH, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)



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