Lobby Question What are the specific challenges you are experiencing with opioid use in your communities? 1
CAPT WEBINAR September 6, 2017 Opioids Prevalence, Effects, and Pharmacology Hayden D. Center, Jr., Ph.D., L.P.C. CAPT Associate
This training was developed under the Substance Abuse and Mental Health Services Administration s Center for the Application of Prevention Technologies task order. Reference #HHSS283201200024I/HHSS28342002T. The views expressed in this webinar do not necessarily represent the views, policies, and positions of the Substance Abuse and Mental Health Services Administration or the U.S. Department of Health and Human Services. This webinar is being recorded and archived, and will be available to all webinar participants. Please contact the webinar facilitator if you have any concerns or questions. 3
Agenda/Roadmap Opioids: Overview Description of Opioids and their Actions Effects of Opioids on the Brain & Body Pharmacology Medication Treatment 4
Presenter Hayden Center CAPT Associate Hayden provides technical assistance and training to community-based and governmental agencies. He also has taught Psychopharmacology in multiple higher education settings. 5
Opioids 6
Overdose Deaths Involving Opioids 7
Prevalence of the Problem Of the 20.5 million Americans 12 or older that had a substance use disorder in 2015, 2 million had a substance use disorder involving prescription pain relievers and 591,000 had a substance use disorder involving heroin 1 8
Prevalence of the Problem Drug overdose is the leading cause of accidental death in the United States, with 52,404 lethal drug overdoses in 2015 Opioid addiction is driving this epidemic with: 20,101 overdose deaths related to prescription pain relievers 12,990 overdose deaths related to heroin in 2015 2 9
Prevalence of the Problem From 1999 to 2008, overdose death rates, sales, and substance use disorder treatment admissions related to prescription pain relievers increased in parallel The overdose death rate in 2008 was nearly four times the 1999 rate The sales of prescription pain relievers in 2010 were four times those in 1999 The substance use disorder treatment admission rate in 2009 was six times the 1999 rate 3 10
Prevalence of the Problem In 2012, 259 million prescriptions were written for opioids, which is more than enough to give every American adult their own bottle of pills 4 Four in five new heroin users started out misusing prescription painkillers 94% of respondents in a 2014 survey of people in treatment for opioid addiction said they chose to use heroin because prescription opioids were far more expensive and harder to obtain 5 11
What are Opioids? Opioids are natural or synthetic substances that act on the brain s opiate receptors Opioids dull pain and relieve anxiety that comes from thinking about pain 12
Opioid Actions 13
Opioid Pathways to Spinal Cord and Brain 14
Localization of Opioid Bonding Sites 15
Physical Effects of Opioids Constricted pupils Flushing of the skin Heavy feeling in the limbs The rush is followed by a confused, drowsy feeling that lasts several hours Breathing and heart rate slow during this period 16
Opioids & Tolerance Higher and higher doses are required to achieve the opioid s effects. This is called tolerance. Eventually, the drug is taken mainly to prevent withdrawal, not to get high. 17
Opioids & Withdrawal Withdrawal occurs when someone who is dependent or addicted stops taking opioids suddenly Withdrawal symptoms: Severe muscle and bone pain Trouble sleeping Diarrhea Vomiting Cold flashes 18
Risks with Opioid Analgesics There are longstanding beliefs in some parts of the medical community that the risks associated with opioid medications are too great to justify their use outside a limited subset of patients, such as those in the context of palliative care 6 19
Mu Opioid Receptor 7 Activation of the mu receptor results in: Analgesia Euphoria Miosis Decreased respiratory rate Decreased muscle tone Decreased gastric motility and hormonal changes 20
Opioids Opioids have been used for centuries to treat pain, cough, and diarrhea The most common modern use of opioids is to treat acute pain 21
Pharmacology Endogenous Opioid Peptides Sensory role: Prominent in inhibiting response to painful stimuli Modulatory role: Gastrointestinal, endocrine, and autonomic functions Emotional role: Indicated by the highly rewarding and addicting qualities Cognitive role: Memory and learning 8 22
Opioid Receptors Three major receptor sites: o Mu o Kappa o Delta These receptor sites spread throughout the central and peripheral nervous systems Opioid receptors are also found in the central respiratory centers 9 23
Absorption, Distribution, Metabolism, and Elimination Opioids are absorbed: gastrointestinal tract nasal or buccal mucosa transdermally Most opioids act quickly when given intravenously 8 24
Clinical Effects Analgesia Mood and Reward Neuroendocrine System Respiration Gastrointestinal Tract Cardiovascular System Other Effects o Reflexes o Pupillary dialation 10 25
Poll What is the most common type of opioid being misused in your communities? 26
Endogenous Opioids Endogenous opioids include: Endorphins 8 Enkephalins Dynorphins 27
Common Types of Opioids 28
Opium 29
Morphine 30
Morphine Is most abundant opiate found in opium, the dried latex extracted by shallowly scoring the unripe seedpods of the Papaver somniferum poppy Is produced most predominantly early in the life cycle of the plant The human body produces endorphins, which are chemically related endogenous opioid peptides that function as neuropeptides and have similar effects as morphine 8 31
Morphine: Delivery Methods Oral (liquid) morphine solution or tablets Injection Intravenously or subcutaneously Rectal suppositories o Effects may last 3-7 hours o Administered intravenously: Maximum effect ~ 20 minutes o Administered orally: Maximum effect ~ 60 minutes o Duration of effect is between three and seven hours 11 32
Morphine Morphine is the prototypical opioid and is the standard against which other opioids are tested The μ-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, caudate nucleus, putamen, and certain cortical areas They are also found on the terminal axons of primary afferents (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve 12 33
Opioid Agonist: Heroin Semi-synthetic analgesic synthesized in the body to morphine Considered a prodrug that facilitates the brain entry of morphine Euphorigenic action: o 30 minutes after intranasal ingestion o 15 minutes after subcutaneous injection o Almost instantaneously after IV injection 8 34
Heroin 35
Heroin & Opioid Effects 36
Opioid Agonist: Codeine 13 Approximately 10% of ingested codeine is O- demethylated to morphine Tramadol Levorphanol Meperidine Diphenoxylate Loperamide 37
Opioid Agonist: Fentanyl 14 Synthetic opioid Actions similar to those of other mu-receptor agonists Popular in anesthesia practice 100 times more potent than morphine Can be delivered transdermally through a patch Fentanyl may be extracted from the patch 38
Opioid Agonist: Hydrocodone 15 Hydrocodone is a semi-synthetic codeine derivative 10-milligrams(mg) oral dose results in maximum serum level in a little over an hour Hydrocodone has a complex pattern of metabolism and is considered a prodrug 39
Opioid Agonist: Oxycodone 13 Potent analgesic and not a prodrug Similar in potency to morphine Side effects are similar to morphine, except less likely to experience hallucination 40
Common Brand Name Drug Containing Oxycodone 8 OxyContin Immediate and controlled-release versions Can be in combination with aspirin and acetaminophen When taken orally the controlled-release version will last up to 12 hours When the controlled-release mechanism is destroyed by crushing the tablet, then the oxycodone can be snorted, ingested, or injected for a powerful effect 41
Antagonist Opioid: Naltrexone 16 Naltrexone is an antagonist medication that prevents other opioids from binding to and activating opioid receptors Used to treat overdose and addiction An injectable, long-acting form of naltrexone (Vivitrol) can be a useful treatment choice for patients who do not have ready access to health care or who struggle with taking their medications regularly 42
Opioid Agonist/N-methyl-D-aspartate (NMDA) Receptor Antagonist: Methadone 17 Methadone is usually taken by mouth and rarely by injection into a muscle or vein Used to treat pain Used as maintenance therapy or to help with tapering in people with opioid dependence o Single dose has rapid effect o Maximum effect can take 5 days of use o Effects last about 6 hours after a single dose 43
Mixed Opioid Agonist/Antagonist: Buprenorphine 18 Buprenorphine is a partial opioid agonist it binds to the opioid receptor but only partially activates it that can be prescribed by certified physicians in an office setting Like methadone, it can reduce cravings and is well tolerated by patients In May 2016, the U.S. Food and Drug Administration (FDA) approved the National Institute on Drug Abuse (NIDA)- supported development of an implantable formulation of buprenorphine 44
Reversing an Opioid Overdose with Naloxone 19 The opioid overdose-reversal drug naloxone is an opioid antagonist that can rapidly restore normal respiration to a person who has stopped breathing as a result of overdose on prescription opioids or heroin Naloxone can be administered by: o Emergency medical personnel o First responders o Bystanders 45
Questions and Discussion 46 46
CAPT Resources Tools are available on the CAPT area of the SAMHSA website: https://www.samhsa.gov/c apt/capt/ Downloadable Resources: CAPT Decision-Support Tools Preventing Prescription Drug Misuse CAPT Resources to Prevent the Non- Medical Use of Prescription Drugs, Opioid Misuse, and Opioid Overdose 47
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If you have questions or comments, please don t hesitate to contact: Janet Porter Training and Technical Assistance Specialist CAPT West Resource Team jporter@casat.org 49
References 1 Center for Behavioral Health Statistics and Quality. (2016). Key substance use and mental health indicators in the United States: Results from the 2015 national survey on drug use and health (HHS Publication No. SMA 16-4984, NSDUH Series H-51). Retrieved from http://www.samhsa.gov/data/. 2 Rudd, R. A., Seth, P., David, F., & Scholl, L. (2016). Increases in drug and opioid-involved overdose deaths United States, 2010 2015. Morbidity and Mortality Weekly Report, 65, 1445 1452. 3 Paulozzi, L. J., M. D., Jones, C. M., Pharm, D., Mack, K., & Rudd, R. A. (2011). Vital signs: overdoses of prescription opioid pain relievers United States, 1999-2008. Morbidity and Mortality Weekly Report, 60(43), 1487-1492. Retrieved from https://www.cdc.gov/mmwr. 4 Centers for Disease Control and Prevention. (2014). Opioid painkiller prescribing, where you live makes a difference. Atlanta, GA: Centers for Disease Control and Prevention. Retrieved from http://www.cdc.gov/vitalsigns/opioid-prescribing/. 5 Jones, C. M. (2013). Heroin use and heroin use risk behaviors among nonmedical users of prescription opioid pain relievers -United States, 2002-2004 and 2008-2010. Drug and Alcohol Dependence, 132(1-2), 95-100. 50
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References 14 Cone, E. J., Heit, H. A., Caplan, Y. H., & Gourlay, D. (2006). Evidence of morphine metabolism to hydromorphone in pain patients chronically treated with morphine. Journal of Annals of Toxicology, 30(1), 1-5. 15 Ling, W., Wesson, D. R., & Smith, D. E. (2005). In J. H. Lowinson, P. Ruiz, R. B. Millman, & J. G. Langrod (Eds). Substance abuse: A comprehensive textbook (4th ed.), 459-468. Philadelphia, PA: Lippincott Williams and Wilkins. 16 Mattick, R. P., Breen, C., Kimber, J., & Davoli, M. (2009). Methadone maintenance therapy versus no opioid replacement therapy for opioid dependence. Cochrane Database Systematic Reviews, (3), CD002209. 17 Benyamin, R., Trescot, A. M., Datta S., Buenaventura, R. M., Adlaka, R, & Vallejo, R. (2008). Opiod complications and side effects. Pain Physician, 11, S105-S120. 18 Mattick, R. P., Breen, C., Kimber, J., & Davoli, M. (2014). Buprenorphine maintenance versus placebo or methadone maintenance for opioid dependence. Cochrane Database Systematic Reviews, (2), CD002207. 19 Wheeler, E., Jones, T. S., Gilbert, M. K., & Davidson, P. J. (2014). Opioid overdose prevention programs providing naloxone to laypersons - United States, 2014. Morbidity and Mortality Weekly Report, 64(23), 631-635. 52