Summary: <div>Treating Opiate Addiction<br> Presented by: Dr. Dawn-Elise Snipes<br> Executive Director, AllCEUs<br> California Drug and Alcohol Treatment Assessment's Findings<br> ~ Treatment was cost beneficial averaging $7 returned for every dollar invested<br> ~ Patients in MAT showed the greatest reduction in intensity of heroin use<br> ~ Decreased healthcare use<br> ~ Number of days of hospitalization, down more than half during MAT<br> Pharmacology<br> ~ 5 Topics<br> • Receptors<br> • Function of opioids at receptors<br> • Consequences of repeated administration and withdrawal of opioids<br> • The affinity, intrinsic activity and dissociation of opioids from receptors<br> • General characteristics of abused opioids<br> Receptors<br> ~ Different types in the brain<br> ~ Mu receptor is most relevant to opioid treatment<br> ~ Activation of the mu receptor allows opioids to exert their analgesic, euphorigenic and addictive effects</div> <div>Functions of Opioids at Receptors<br> ~ Full Agonists<br> ~ Activate receptors in the brain<br> ~ Bind to receptors and turn them on<br> ~ Increasing doses of full agonists produce increasing effects, until the receptor is fully activated<br> ~ Opioids with the greatest abuse potential are full agonists<br> ~ Examples of full agonists are morphine, heroin, methadone, oxycodone and hydromorphone</div> <div>Functions of Opioids at Receptors cont…<br> ~ Antagonists<br> ~ Bind to opioid receptors, but instead of activating receptors, they effectively block them<br> ~ Prevent receptors from being activated by agonist compounds<br> ~ Like a key that fits in a lock but does not open it and prevents another key from being inserted<br> ~ Examples of opioid antagonists are naltrexone and naloxone</div> <div>Functions of Opioids at Receptors cont…<br> ~ Partial Agonists<br> ~ Bind to receptors and activate them but not to the same degree as full agonists<br> ~ Increasing effects of partial agonists reach maximum levels and do not increase further, even if doses continue to rise—the ceiling effect<br> ~ As higher doses are reached, partial agonists can act like antagonists by occupying receptors but not activating them and blocking full agonists from receptors<br> ~ Buprenorphine is an example of a mu opioid partial agonist</div> <div>Consequences of Repeated Administration and Withdrawal<br> ~ Repeated administration of a mu opioid agonist results in tolerance and dose-dependent physical dependence<br> ~ Spontaneous withdrawal<br> ~ begins 6–12 hours after the last dose<br> ~ peaks in intensity 36–72<br> ~ lasts approximately 5 days<br> ~ Precipitated withdrawal occurs when an individual physically dependent on opioids is administered an opioid antagonist or partial agonist</div> <div>Characteristics of Abused Drugs<br> ~ Rate of onset of the pharmacological effects of a drug, and its abuse potential, is determined by:<br> ~ the drug's route of administration<br> ~ its half-life<br> ~ Abuse Potential is related to:<br> ~ ease of administration<br> ~ cost of the drug<br> ~ how fast the user experiences the desired results<br> Naltrexone<br> ~ Antagonist<br> ~ Naltrexone may decrease the likelihood of relapse to drinking (vivtrol)<br> ~ Can precipitate an opioid withdrawal syndrome in buprenorphine-maintained patients<br> ~ Should not be prescribed for patients being treated with buprenorphine for opioid addiction<br> Buprenorphine<br> ~ Because it is a partial agonist, higher doses of have fewer adverse effects<br> ~ Slow dissociation rate (long half life)<br> ~ Abuse of buprenorphine primarily via diverting sublingual tablets to the injection route<br> ~ Buprenorphine's partial mu agonist properties make it mildly reinforcing thus encouraging patient compliance with regular administration<br> ~ Suboxone is buprenorphine plus naloxone<br> ~ Naloxone exerts antagonist properties when inject</div>
