OPIATES AND ADDICTION MEDICATIONS. Dr. Carroll W. Thornburg, D.O Chief Medical Officer in Primary Care and Addiction Services

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1 OPIATES AND ADDICTION MEDICATIONS Dr. Carroll W. Thornburg, D.O Chief Medical Officer in Primary Care and Addiction Services

2 Dr. Carroll W. Thornburg, D.O Chief Medical Officer in Primary Care and Addiction Services

3 Titles Chief Medical Officer of Primary Care and Addiction Services for Emergence Health Network Program Physician at MedMark Treatment Center of El Paso (Methadone Clinic) Consultant/Speaker for Alkermes Pharmaceutical Consultant/Speaker for Indivior Pharmaceutical Registered Nurse

4 Certifications Board Certified in Family Practice and Osteopathic Manipulative Treatment Board Certified in Addiction Medicine. The American Society of Addiction Medicine Certified by The American Osteopathic Association in the subspecialty of addiction medicine. Legal consultant for Hinkle Law Firm in New Mexico

5 Disclosure to Participants Requirements for Successful Completion of Continuing Education Activity Requires You to: Complete registration and sign in sheet Attend entire educational activity Participate in education activities Complete participant evaluation Commercial Support: This educational activity received no commercial support. Disclosure of Conflict of Interest: The speakers and planning committee for this event have disclosed no financial interests.

6 Disclosure to Participants. Non-Endorsement Statement: Accredited status does not imply endorsement by the Department of State Health Services, Continuing Education Service; Texas Medical Association ; or American Nurse Credentialing Center. Off-Label Use of Drugs: The speakers did not disclose the use of products for a purpose other than what it had been approved for by the Food and Drug Administration. Expiration Date for Awarding Contact Hours: Complete the attendance sheet and evaluation by the end of the session.

7 Objectives What are Opiates History of Opiate Use, Abuse and Legal Control Impact of Opiate Use Mechanism of Action Treatment options through MAT programs

8 Papaver Somniferum Incisions are made in the pods and the milky fluid that oozes out is air dried. This must be done while the pods are still green.

9 Opiates Are Derived From The Poppy Plant CONTENTS OF THE POPPY POD FLUID: Morphine 4-21 % Codeine 1-25% *There are at least 20 other alkaloids, such as Thebaine, in the fluid.*

10 Wizard Of Oz

11 Opium History BC: Opium believed to be discovered in the Mediterranean area BC: Egyptian papyri list opium as one of 7000 remedies thousands of Chinese laborers immigrated to the US and brought the habit of opium smoking with them

12 Opium History Civil war soldiers became opioid dependent through medical treatment referred to as army disease or soldier s disease It was estimated that the total number of opium users in the U.S. In 1886 the use was 100,000 Heroin was first synthesized in 1874 by the chemist, C.R. Alder Wright

13 Historical Opiate Products This bottle of Stickney and Poor's paregoric was distributed much like the spices for which the company is better known. McCormick also manufactured and sold paregoric, which is a mixture of opium and alcohol. Doses for infants, children, and adults are given on the bottle. At 46% alcohol, this product is 92 proof which is pretty potent in itself.

14 Historical Opiate Products Many products, marketed for adults and children, were sold for pain and cough relief. They all contained opium.

15 Historical Opiate Products There were ads in papers and journals for Bayer s many products, including aspirin and heroin.

16

17 Morphine - Effects

18 Federal Laws Associated With The Control Of Narcotics 1914 HARRISON ACT First federal legislation to regulate and control the production, importation, sale, purchase and free distribution of opium and drugs derived from opium 1924 HEROIN ACT Made it illegal to manufacture heroin 1942 OPIUM POPPY CONTROL ACT Prohibited growing opium poppies in the US, except under license

19 Federal Laws Associated With The Control Of Narcotics 1973 METHADONE CONTROL ACT Placed controls on methadone licensing 1986 EXECUTIVE ORDER Mandated a drug-free workplace program 2000 CHILDREN S HEALTH ACT A section of this act dealt with drug addiction treatment (DATA) Allowed qualified physicians to prescribe medications classified as schedule III, IV and V narcotics for treatment of addiction. This is the law that allows and regulates buprenorphine use in addiction treatment.

20 The Present 40-60% of addiction vulnerability is genetic and environment. 80% of Heroin users previously misused prescription pain relievers (data from ) Adults with Anxiety or Mood Disorders are 4.6x as likely to have Opioid Use Disorder In million adults used prescription pain relievers for nonmedical purposes.

21 The Present In 2015: 2 million Americans had a Substance Abuse Disorder using prescription 591,000 Americans had a Substance Abuse Disorder involving Heroin 20,000 Overdose deaths were related to prescription pain relievers 276,000 Adolescents between ages 12 and 17 years of age were current nonmedical users of pain medication and hundred and 22,000 experiencing addiction to prescription pain relievers

22 The Present 810,000-1,000,000* heroin addicted individuals in the United States (2004) 25% are involved in some type of treatment 2016 overdose deaths was 60,000 *These are estimates; the incidence of heroin addiction may be under reported.

23 Drugs Involved in U.S. Overdose Deaths

24 Understanding The Brain

25 The Brain & Pleasure

26 Functions of Endogenous Opioids Modulation of pain perception Modulation of Motor activity for sustained periods runners high Autonomic regulation

27 Classifications Natural: Morphine Codeine thebaine Esters of morphine: diacetylmorphine(morphine diacetate; heroin) nicomorphine (morphine dinicotinate) dipropanoylmorphine (morphine dipropionate) desomorphine acetylpropionylmorphine dibe nzoylmorphine diacetyldihydromorphine

28 Classifications Semi-synthetic: hydromorphone hydrocodone oxycodone oxymorphone eth ylmorphine buprenorphine Endogenous: endorphins enkephalins dynorphins endomorphins. Fully synthetic : fentanyl Pethidine levorphanol methadone tramadol tapent adol Dextropropoxyphene

29 Opiates Morphine and/or codeine use may be found on evaluation if a urine specimen if the patient: Used heroin Ingested poppy seeds In some studies, only 2-3 poppy-seed bagels or Poppy-seed bread need to be eaten. If depends on the amount of poppy seeds in the cooked item. Used codine containing product (i.e. Tylenol #3) Used a morphine-containing product

30 OPIATE PHARMACOLOGY

31 Opiates What are the opiate user s desired effects? Sedation Euphoria Analgesia

32 Opiate Effects After IV injection Warm skin rush Pruritis (severe itchiness), especially with morphine use which releases histamines Pleasure, relaxation and satisfaction in 45 seconds

33 Side Effects The principle side effects of the opioid narcotics, besides their abuse potential, include: Drowsiness Respiratory depression Nausea, vomiting, and constipation Inability to urinate Drop in blood pressure

34 The Brain & Chronic Opioid Use

35 Intoxication or Withdrawal? Withdrawal Intoxication Always look at the pupils; the pupil size can give very good clinical information.

36 Opiate Withdrawal Late Phase Increase in heart rate Increase in blood pressure Nausea and vomiting Diarrhea Abdominal cramps Labile mood Depression Muscle spasm Weakness Bone pain

37 Opiate Withdrawal Treatment Treatment can be done inpatient or ambulatory Involves the use of medication to damper the increased signs of opiate withdrawal Clonidine, an antihypertensive medication, has been used in many older protocols Buprenorphine has recently been approved for use by authorized physicians Methadone can be used if a detoxification program has the proper approvals

38 Needs for Treatment Patients need to want treatment to be successful Contracts for treatment need to be in place for use of medication in the MAT format to discourage diversion PMP (Prescription Monitoring Program) should be generated to validate patient history and prescription use

39 Needs for Treatment Urine drug screens should be performed to confirm compliance of current therapy in the MAT program Psychosocial treatment needs to be implemented to supplement treatment outcome success

40 Opioid Use Disorder Key Summary Points OUD has many medical complications including high lethality Medication treatment is essential to safe and successful management of OUD Naltrexone (antagonist) Methadone (full agonist) Buprenorphine (partial agonist)

41 The Brain & Agonist Therapy

42 The Brain & Partial Agonist Therapy

43 The Brain & Antagonist Therapy

44 Methadone (agonist) Federal/State regulated programs require special requirements for the implementation Patients are long term users of opiates and stabilized on the current dose Patients are assessed for dependence and tolerance prior to induction 30mg is the typical induction does but this is determined by tolerance. Steady state is reached in 5-8 days.

45 Methadone Maintenance Adjustments in the dose are made based on daily COW scores Patients must be dosed at the clinic daily and can progress the take-home bottles based on compliance Concurrent counseling/therapy is required to fulfill program guidelines for social integration Maintenance lasts for months but can last a lifetime for some

46 Buprenorphine (partial agonist) Note: opiate detox is not required prior to use but patients need to stop the use of the current opiate Patients last use of opiates should be at least 12 hours prior to induction Patient should be in moderate withdrawal prior to administration due to the affinity of the receptor site A certificate of waiver and training is required prior to use of the scheduled III medication

47 Buprenorphine Types of administration are: transdermal, sublingual, buccal, and long acting injectable Ceiling effect of euphoria and respiratory depression to decrease the risk of overdose Dosing is usually between 2-24mg with the average dose of 8 16mg Diversion can occur except with injectable

48 Buprenorphine Injectable version of administration lasts 30 days with extra long half life Medication is effectively reversed with naloxone tablets/injectable/nasal administration Psychosocial treatment and intervention increases successful outcomes Synthetic thebaine congener and highly lipid soluble

49 Buprenorphine Given Sublingually or parenterally but not oral high 1st pass metabolism Selective μ-agonist analgesic times more potent than Morphine Slow but longer duration of action up to 24 hrs

50 Buprenorphine Pharmacological effects are similar to Morphine Has ceiling effect in analgesic and respiratory depression Good analgesic for naive patients but addicts precipitates withdrawal syndrome Lower tolerance and physical dependence than Morphine and abuse liability Withdrawal syndromes are similar to Morphine

51 Naltrexone (antagonist) Patients must be detoxed from the current use of opiates 5-7 days for short acting heroin or 10 days to 2 weeks for long-acting opiates (Buprenorphine or Methadone) A naloxone challenge can be performed to determine with drawal risk if last dose of use of opiated is in question

52 Naltrexone Naltrexone 25mg can be used on day one to verify tolera nce and prevention of withdrawal, thereafter 50mg orally can be used daily Patient compliance is a major limiting factor and risk of decreased tolerance may possibly precipitate overdose through re-exposure of opiates

53 Naltrexone Dosing (For opiate-dependent patients) Must wait 5 7 days after last use of a short-acting opiate (heroin) or 7 10 days after a long-acting opiate to prevent withdrawal. Can perform a narcan challenge test* to see if withdrawal can be induced, thus not safe to start naltrexone yet Should always have a negative urine drug screen for opiates before starting Start with 25 mg first day, then 50 mg per day thereafter. Can dose for 3 times a week (100mg 100mg 150 mg on Monday, Wednesday and Friday)

54 Naltrexone Narcan Challenge Test Do not do test if patient is showing symptoms of o piate withdrawal Do not do test is patient is suspected of recent opia te use Do not do test if urine drug screen is still positive f or opiates Why? Will precipitate withdrawal

55 Naltrexone For opiate-dependent patients Poor compliance appears to be a major limiting factor Use of this medication is not addictive; by itself, it will not cause opiate withdrawal

56 Depot Naltrexone to Block Heroin Effect

57 Long acting Naltrexone It is an opiate Antagonist It should not be administered to anyone on opiates and a negative urine drug screen should be obtained to confirm lack of current use. It is a monthly injection lasting 30 days Detox required from opiates for 5 to 7 days for short acting opiates and up to 2 weeks for long-acting opiates

58 Long acting Naltrexone A naloxone challenge test can be done to ensure that withdrawal will not be precipitated 5 to 7 days of naltrexone is recommended prior to the administration of the long-acting version to ensure no precipitation of withdrawal Risk of overdose if possible if opiates are resumed after the duration of the injected medication. The is due to low tolerance developed through the course of treatment.

59 Long acting Naltrexone Nonaddictive Must be administered by a healthcare provider No reasonable risk for diversion No special license or training is required for administration Non-scheduled medication Any provider can administer

60 Use of XR-Naltrexone 380 mg is given as a gluteal intramuscular (IM) in jection every 4 weeks or once a month Upper outer quadrant of alternating buttocks eac h month Side effects similar to oral Injection site reactions possible

61 Conclusion There is an opiate crisis in America The crisis of opiate abuse and death is increasing at a rapid rate Anyone is a risk to the crisis or to knowing someone affiliated by Opiate use Disorder Genetic predisposition and environment plays a role of risk in Opiate use Disorder

62 Conclusion There are effective MAT treatments for Opiate use Disorder Treatment options may be limited to socioeconomic status and availability of service Psychosocial treatment is a critical component that should be utilized in MAT treatments to improve patient stability and successful outcomes

63

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