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MEDICAL TOXICOLOGYANDOPIOID ABUSE
Fred Harchelroad, MD FACEP, FAAEM, FACMT
Westmoreland Emergency Medicine Specialists
Excela Health System
DISCLOSURE
I am an emergency medicine physician working
for more than three decades. My reality is biased
by all those patients with whom I have interacted.
OBJECTIVES
• Better understanding of the history of opioids.
• Compare and contrast an opiate and an opioid.
• Discuss the utility of commonly used urine drug screens.
• Critique the efforts to manage opioid abuse in your area.
• Differentiate the different opioid detox/rehab options.
OPIOIDS THROUGH-OUT HISTORY
• Sumarians (4000 B.C.) “hul gil” = joy plant = poppy
• Ebers papyrus (1500 B.C.) milk of poppy helped infants sleep
• Theophrastus (300 B.C.) written reference of opium.
• Paracelsus (1493–1541) compounded laudanum (tincture of opium; alcohol-based 10% opium by weight).
• 1600 – 1700: gradual increase in opium use until tobacco smoking concept exported from North America to China.
OPIOIDS THROUGH-OUT HISTORY
• 1729 : China - 28,000 lbs. imported; edict prohibited opium use.
• 1800 : China - 630,000 lbs. imported.
• 1803 : Morphine isolated from opium.
• 1832 : Codeine isolated from opium.
• 1838 : China - 5,600,000 lbs. imported.
• 1839 – 1842 : First Opium War
OPIOIDS THROUGH-OUT HISTORY
• California Gold Rush/Hypodermic needle/Civil War/Continental RR
• 1874 : Charles Wright synthesized heroin from morphine
• 1898 : Bayer marketed heroin as anti-tussive.
• 1908 : Pres. T. Roosevelt appoints Dr. Hamilton Wright as the first Opium Commissioner of the U.S.
• 1914 : Harrison Narcotic Act
• 1925 : International Opium Convention
OPIOIDS THROUGH-OUT HISTORY
• 1960’s: Designer drugs
• 1970 : Comprehensive Drug Abuse Prevention & Control Act
• 1973 : Identification of opioid binding sites/DEA established
• 1978 : Psychotropic Substances Act
• 1979 : China White in California
• 1986 : Controlled Substances Analogue Enforcement Act
• 1988 : China White in Pittsburgh
EPIDEMICS/PANDEMICS IN HISTORY
• Black Death : 1345 – 1355; 75,000,000 deaths
• Cholera : 1832 – 1849; 150,000 in U.S.
• Influenza : 1918 – 1920; 50,000,000 worldwide/500,000 in U.S.
• SARS : 800 deaths worldwide
• HIV : 14,000 deaths per year in U.S.
• Opioids : 40,000 deaths per year in U.S.
MULTIFACTORIAL ETIOLOGY
• New drugs.
• More drugs.
• More media.
• Different labeling.
• More regulations.
JCAHO AND THE MILLENNIALS
• Generation Me
• Pain is the 5th vital sign.
• Speak-up about your pain.
• Your pain deserves to be treated.
• No one should have to suffer any pain.
THE MEDIA
• 22 May 2016 : Pittsburgh Post-Gazette “Overdosed: How doctors wrote the script for an epidemic.”
• 14 September 2016 : Pittsburgh Post-Gazette “Emergency room narcotics prescribing would be reined in under legislation endorsed this week by Governor Tom Wolfe.”
• 20 September 2016 : Tribune-Review “Obama opens blitz on addiction crisis…..proclaiming…Prescription Opioid and Heroin Epidemic Awareness Week.”
• 27 October 2016 : Pittsburgh Post-Gazette “Four bills restricting prescribing and improving doctor education won final passage…”
DESIGNER DRUGS
• Psychedelics
• Dissociatives
• Piperazines
• Empathogens
• Stimulants
• Sedatives
• Synthetic Cannabinoids
• Androgens
• Peptides
• PDE-5 Inhibitors
• Nootropics
EMCDDA
• European Monitoring Centre for Drugs and Drug Addiction
• 2009…………………………..24 new drugs
• 2010…………………………..41 new drugs
• 2012…………………………..73 new drugs
• 2013…………………………..81 new drugs
DEFINITIONS
• An opiate is : any of the alkaloids naturally derived from the opium poppy (morphine, codeine, thebaine, and noscapine).
• An opioid is : any zenobiotic that is capable either of producing an opium-like effect or of binding to opioid receptors.
• Semisynthetic opioids (heroin or oxycodone) : created by chemical modification of an opiate.
• Synthetic opioids ( methadone or fentanyl) : a chemical, not derived from an opiate, that binds to an opioid receptor.
FENTANYL
• N-(1-(2-phenylethyl)-4- piperidinyl-N-phenylpropanamide.
• CAS #437-38-7
• 100 x more potent than morphine
• Duration of action 45 minutes.
• Developed 1960 (Paul Janssen)
FURANYL FENTANYL
• N-phenyl-N-[1-(2-phenylethyl)-4-piperidinyl]-2-furamide
• PubChem CID #13653606
• 5 x less potent than morphine.
• Duration of action 45 minutes.
CARFENTANIL
• Methyl-1-(2-phenylethyl)-4-(N-propanoylanilino)piperidine-4-carboxylate
• CAS #59708-52-0
• 10,000 x more potent than morphine.
• Developed 1974 by Janssen Pharmaceuticals.
• 2002 Moscow hostage rescue.
U47700
• 3,4-dichloro-N-[(1R,2R)-2-dimethylamino)cyclohexyl]-N-methylbenzamide
• CAS #82657-23-6
• 7.5 x more potent than morphine.
• Selective Kappa receptor agonist
• Developed by Upjohn in 1970’s
• Pink
URINE DRUG SCREENS
• Opiate assay is based on chemical structure of morphine.
• Heroin (diacetyl morphine) is metabolized to morphine.
• Methadone is not metabolized to anything that resembles morphine.
• Buprenorphine is not metabolized to anything that resembles morphine.
• Fentanyl is not metabolized to anything that resembles morphine.
OPIOID OUTCOMES IN CLINICAL PRACTICE
DEAD
• Cardiac
• Brain• ? Organ Donation
ALIVE
• Vegetative from anoxic brain
• Recurrent sedation
• ARDS
• HIV/Hep C/Endocarditis
• Adulterants
• Movement disorders
• Endocrine effects
OPIOID PRESCRIBING
Do
• Treat acute pain as needed.
• Advise patient that some pain is expected.
• Check PA PDMP
Do Not
• Use combination opioid with acetaminophen.
• Provide opioid because patient will complain to administration or State Medical Board.
• Prescribe in dose not exceeding 50 MME per day (10mg oxycodone every 4 hours while awake.
THE PENDULUM SWINGS
• God’s own medicine
• Ethical duty to treat pain
• Medicine for the individual
• No government intervention
• Life must be without physical pain
• Opiophobia
• No pain no gain
• Medicine for the public welfare
• Government regulation
• Life without physical pain is not a full life