Opioids Pain Management

Chapter 12:  Pain Management:  Opioids

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Table of Contents: Opioids

Organ Systems

Clinical Use: Opioid Analgesics

Specific Drugs

Opioids

Morphine

 

Codeine and Oxycodone (methylated at C3)

Pharmacokinetics

Way, W.L., Fields, H.L. and Way, E. L. Opioid Analgesics and Antagonists, in Basic and Clinical Pharmacology, (Katzung, B. G., ed) Appleton-Lange, 1998, pp 496-515.

Coda, B.A. Opioids, In Clinical Anesthesia, 3rd Edition (Barash, P.G., Cullen, B.F. and Stoelting, R.K.,eds) Lippincott-Ravin Publishers, Philadelphia, New York, 1997, pp 329-358.

Schuckit, M.A. and Segal D.S., Opioid Drug Abuse and Dependence, In Harrison's Principles of Internal Medicine 14th edition, (Isselbacher, K.J., Braunwald, E., Wilson, J.D., Martin, J.B., Fauci, A.S. and Kasper, D.L., eds) McGraw-Hill, Inc (Health Professions Division), 1998, pp 2508-2512.

Pharmacodynamics

Opioid Receptor Subtype

Drug

Mu (m)

Delta (d)

Kappa (k)

Opioid Peptides

Enkephalins

Antagonist

Agonist

beta-endorphin

Agonist

Agonist

Dynorphin

Weak Agonist

Agonist

Agonists

Codeine

Weak Agonist

Weak Agonist

etorphine

Agonist

Agonist

Agonist

fentanyl (Sublimaze)

Agonist

meperidine (Demerol)

Agonist

methadone (Dolophine)

Agonist

morphine

Agonist

Weak Agonist

Agonist-antagonists

Buprenorphine

Partial Agonist

dezocine (Dalgan)

Partial Agonist

Agonist

nalbuphine (Nubain)

Antagonist

Agonist

pentazocine (Talwan)

Antagonist or Partial Agonist

Agonist

Antagonist: naloxone (Narcan)

Antagonist

Antagonist

Antagonist

Spinal Cord Sites of Opioid Action

 

courtesy of Roxane Pain Institute used with permission http://pain.roxane.com/sitemap.html

Way, W.L., Fields, H.L. and Way, E. L. Opioid Analgesics and Antagonists, in Basic and Clinical Pharmacology, (Katzung, B. G., ed) Appleton-Lange, 1998, pp 496-515.

Schuckit, M.A. and Segal D.S., Opioid Drug Abuse and Dependence, In Harrison's Principles of Internal Medicine 14th edition, (Isselbacher, K.J., Braunwald, E., Wilson, J.D., Martin, J.B., Fauci, A.S. and Kasper, D.L., eds) McGraw-Hill, Inc (Health Professions Division), 1998, pp 2508-2512.

Coda, B.A. Opioids, In Clinical Anesthesia, 3rd Edition (Barash, P.G., Cullen, B.F. and Stoelting, R.K.,eds) Lippincott-Ravin Publishers, Philadelphia, New York, 1997, pp 329-358.

Reticular formation (RF), vestibular nuclei (V), cerebellar roof nuclei (R), periaquiductal gray (PG).  Posterior hypothalamic nuclei (P), paraventricular hypothalamic nucleus (PV), substantia nigra (SN),  Thalamic nuclei (T), preoptic hypothalamic nuclei (PO), locus ceruleus (LC), median raphe nuclei (MR) . 

Opioid Effects: Degree of Tolerance Developed
High Intermediate Limited/None
analgesia bradycardia miosis
euphoria, dysphoria   constipation
mental clouding   convulsions
 sedation   antagonist actions
respiratory depression    
antidiuresis    
nausea/vomiting    
cough suppression    

adapted from Figure 31-4: Way, W.L., Fields, H.L. and Way, E. L. Opioid Analgesics and Antagonists, in Basic and Clinical Pharmacology, (Katzung, B. G., ed) Appleton-Lange, 1998, p. 505.

 

Some Symptoms of Opioid Withdrawal
rhinorrhea lacrimation chills hyperventilation muscular aches vomiting
anxiety diarrhea hostility piloerection yawning hyperventilation

 

Opioid Drug Listing
  • alfentanil (Alfenta)
  • butorphanol (Stadol)
  • codeine
  • dezocine (Dalgan)
  • fentanyl (Sublimaze)
  • hydromorphone (Dilaudid)
  • levorphanol (Levo-dromoran)
  • meperidine (Demerol)
  • methadone (Dolophine)
  • morphine
  • nalbuphine
  • oxycodone (Roxicodone)
  • oxymorphone (Numorphan)
  • pentazocine (Talwain)
  • propoxyphene (Darvon)
  • sufentanil (Sufenta)
 

Combinations

  • Codeine/acetaminophen
  • Codeine/aspirin
  • Propoxyphene/aspirin
  • Codone/acetaminophen
  • Oxycodone/aspirin
 

Antitussives

  • Codeine
  • Dextromethorphan
  • Delsym

 

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