Dr. Dawn-Elise Snipes is a Licensed Professional Counselor and Qualified Clinical Supervisor. She received her PhD in Mental Health Counseling from the University of Florida in 2002. In addition to being a practicing clinician, she has provided training to counselors, social workers, nurses and case managers internationally since 2006 through AllCEUs.com A direct link to the CEU course is in the podcast show notes. CEUs are available at https://www.allceus.com/member/cart/index/product/id/680/c/
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Pharmacology
~ 5 Topics
• Receptors
• Function of opioids at receptors
• Consequences of repeated administration and withdrawal of opioids
• The affinity, intrinsic activity and dissociation of opioids from receptors
• General characteristics of abused opioids
Receptors
~ Different types in the brain
~ Mu receptor is most relevant to opioid treatment
~ Activation of the mu receptor allows opioids to exert their analgesic, euphorigenic and addictive effects
Functions of Opioids at Receptors
~ Full Agonists
~ Activate receptors in the brain
~ Bind to receptors and turn them on
~ Increasing doses of full agonists produce increasing effects, until the receptor is fully activated
~ Opioids with the greatest abuse potential are full agonists
~ Examples of full agonists are morphine, heroin, methadone, oxycodone and hydromorphone
Functions of Opioids at Receptors cont…
~ Antagonists
~ Bind to opioid receptors, but instead of activating receptors, they effectively block them
~ Prevent receptors from being activated by agonist compounds
~ Like a key that fits in a lock but does not open it and prevents another key from being inserted
~ Examples of opioid antagonists are naltrexone and naloxone
Functions of Opioids at Receptors cont…
~ Partial Agonists
~ Bind to receptors and activate them but not to the same degree as full agonists
~ Increasing effects of partial agonists reach maximum levels and do not increase further, even if doses continue to rise—the ceiling effect
~ As higher doses are reached, partial agonists can act like antagonists by occupying receptors but not activating them and blocking full agonists from receptors
~ Buprenorphine is an example of a mu opioid partial agonist
Consequences of Repeated Administration and Withdrawal
~ Repeated administration of a mu opioid agonist results in tolerance and dose-dependent physical dependence
~ Spontaneous withdrawal
~ begins 6–12 hours after the last dose
~ peaks in intensity 36–72
~ lasts approximately 5 days
~ Precipitated withdrawal occurs when an individual physically dependent on opioids is administered an opioid antagonist or partial agonist
Characteristics of Abused Drugs
~ Rate of onset of the pharmacological effects of a drug, and its abuse potential, is determined by:
~ the drug's route of administration
~ its half-life
~ Abuse Potential is related to:
~ ease of administration
~ cost of the drug
~ how fast the user experiences the desired results
Naltrexone
~ Antagonist
~ Naltrexone may decrease the likelihood of relapse to drinking (vivtrol)
~ Can precipitate an opioid withdrawal syndrome in buprenorphine-maintained patients
~ Should not be prescribed for patients being treated with buprenorphine for opioid addiction
Buprenorphine
~ Because it is a partial agonist, higher doses of have fewer adverse effects
~ Slow dissociation rate (long half life)
~ Abuse of buprenorphine primarily via diverting sublingual tablets to the injection route
~ Buprenorphine's partial mu agonist properties make it mildly reinforcing thus encouraging patient compliance with regular administration