Opioid Receptor Agonist

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Contents 1 More Specific Terms 2 Introduction 3 Dosage 4 Pharmacokinetics 5 Adverse-effects 6 More General Terms 7 Additional Terms 8 References

More Specific Terms

• 6-monoacetylmorphine
• alfentanil (Alfenta)
• butorphanol (Stadol, Stadol NS)
• codeine
• diacetylmorphine (heroin)
• difenoxin
• dihydrocodeine
• fentanyl (Sublimaze, Duragesic, Fentanyl Oralet, Actiq, Fentora, Ionsys, Onsolis, Abstral, Lazanda)
• hydromorphone; dihydromorphinone (Dilaudid, Palladone)
• levorphanol (Levo-Dromoran)
• meperidine (Demerol, Isonipecaine, Chlorbycyclen, Centralgin)
• methadone (Dolophine, Methadose, Physeptone, Algolysin)
• mixed opioid agonist-antagonist (analgesic narcotic partial-mixed agonist)
• morphine (morphine sulfate [MS], MS Contin, Roxanol, Oramorph SR, Kadian, Avinza, DepoDur, Duromorph)
• narcotic combination
• normeperidine (Norpethidine)
• opiate
• opioid partial agonist
• oxycodone (Roxicodone, OxyContin, OxyIR, OxyFast, Oxecta)
• oxymorphone (Numorphan, Opana, Opana ER)
• propoxyphene (Darvon, Dolene, Proxagesic, Novopropoxyn)
• sufentanil (Sufenta)
• tapentadol (Nucynta)

Introduction

• Any morphine-like compound, natural or synthetic, that stimulates opioid receptors producing bodily effects including pain relief, sedation, constipation, & respiratory depression.

Dosage

• rescue dose for breakthrough pain should be 10% of daily dose [5]

• Relative opioid receptor potency: (mg for equipotent effects) (also see reference [5])

*                                   route      dose (mg) 
* morphine                         IM, SC       10 
*                                      PO       30 
* hydromorphone (Dilaudid)         IM, SC        1.5 
*                                      PO        7.5 
* oxymorphone (Numorphan)          IM, SC        1 
*                                      PR        5 
* levorphanol (Levo-Dromoran)      IM, SC        2 
*                                      PO        4 
* methadone (Dolophine)                IM        5 
*                                      PO       10 
* meperidine                       IM, SC       75 
*                                      PO      300 
* fentanyl* (Sublimaze)                IM        0.1 
* hydrocodone (Hycodan)                PO       30 
* oxycodone (OxyContin)                PO       20 
* propoxyphene                         PO       65 
* pentazocine (Talwin)             IM, SC       60 
*                                      PO      180 
* nalbuphine (Nubain)                  IM       10 
* butorphanol (Stadol)                 IM       10 
* 
* Antitussive/antidiarrheal doses: 
* diphenoxlate                         PO       5 
* loperamide                           PO       2 
* codeine                              IM      60 
*                                      PO     180 
*

• * see fentanyl for patch equivalent to oral morphine
  
• Combination drugs containing opiate
  
• Percodan, Percocet, Endocet: see oxycodone
• Darvon, Darvocet: see propoxyphene

Pharmacokinetics

• metabolized by cyt P450
• duration of action:

• generally 4-6 hours
• exceptions:

• meperidine 3-5 hours
• fentanyl 1-2 hours

• 1/2 lives more variable than duration of action

Adverse-effects

• sedation

• level of arousal dose-dependent
• tolerance develops within a few days

• hypogonadism (both genders), erectile dysfunction [12]
• nausea/vomiting (tolerance develops within a few days)
• constipation (use docusate & senna)

• tolerance does NOT develop to constipating effects [13]

• urinary retention [13]
• respiratory depression (tolerance develops)
• hypotension
• hypothermia
• hyporeflexia
• pruritis, hives, flushing due to release of histamine from mast cells [6]
• miosis (usually)
• true allergy uncommon, generally adverse effect [6]
• myoclonus ?
  

• also see opioid overdose
  

• drug adverse effects of sedatives
• drug adverse effects of opiates

More General Terms

• receptor agonist
• analgesic (antalgic)
• sedative/hypnotic (tranquilizer)

Additional Terms

• opioid maintenance therapy
• Opioid Overdose
• opioid receptor antagonist or narcotic antagonist

References

1. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
2. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996 pg 535
3. Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 682-683
4. VA Greater Los Angeles Healthcare System
5. Prescriber's Letter 11(9): 2004 Equianalgesic Dosing of Opioids for Pain Management Detail-Document#: [1] (subscription needed) [2]
6. Prescriber's Letter 13(2): 2006 Opioid Intolerance Decision Algorithm Detail-Document#: [3] (subscription needed) [4]
7. Prescriber's Letter 15(3): 2008 Detail-Document#: [5] Dosing frequency of long-acting opioids (subscription needed) [6]
8. Medical Knowledge Self Assessment Program (MKSAP) 15, American College of Physicians, Philadelphia 2009
9. Prescriber's Letter 17(7): 2010 Equianalgesic Dosing of Opioids for Pain Management Detail-Document#: [7] (subscription needed) [8]
   - Prescriber's Letter 17(12): 2010 CHART: Equianalgesic Dosing of Opioids for Pain Management Detail-Document#: [9] (subscription needed) [10]
10. Bohnert ASB et al. Association between opioid prescribing patterns and opioid overdose-related deaths. JAMA 2011 Apr 6; 305:1315. PMID: [11]
11. Prescriber's Letter 18(6): 2011 COMMENTARY: REMS for Long-Acting and Extended-Release Opioids CHART: Prescription Drug Monitoring Programs Detail-Document#: [12] (subscription needed) [13]
12. Prescriber's Letter 19(2): 2012 Hormonal Effects of Opioids Detail-Document#: [14] (subscription needed) [15]
13. Geriatric Review Syllabus, 7th edition Parada JT et al (eds) American Geriatrics Society, 2010
14. National Guideline Clearinghouse Methadone and buprenorphine for the management of opioid dependence. (National Institute for Health and Clinical Excellence) ngc-guideline: [16]
    - Naltrexone for the management of opioid dependence. (National Institute for Health and Clinical Excellence) ngc-guideline: [17]

opioid receptor agonist (narcotic)