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2. Outline of Chapter  Terminology  Mechanism of action  Pharmacokinetics  Pharmacologic effects  Adverse Rxns  Classification  Dental considerations

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4.  Opioids  Analgesic that is a natural or synthetic morphine-like substance used for reducing moderate-severe pain that cannot be controlled with other types of analgesics  Narcotics  Act exclusively on CNS  Morphine is the protype  Standard by which all other opioids are measured  Produces analgesia, drowsiness, change in mood, mental clouding without loss of consciousness  Heroin is 3x more potent than morphine & more rapidly addicting (can never be legally prescribed)

5. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.  Just like nicotine, patients develop tolerance and dependence to opioids (they are narcotics)  Federally restricted as potential for abuse (controlled substances)  DEA number on the Rx is required  Most are Schedule II  Weaker opioids (codeine, hydrocodone, dextromethorphan for cough) are Schedule III-V according to their strength

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7.  Act on specific receptors in CNS – esp limbic system  Opioids do NOT bind to receptors in peripheral nerves like CH5 drugs  Drugs cause the release of natural endogenous substances (peptides, enkephalins, endorphins, dynorphins) that activate opioid receptors – thereby blocking transmission of pain impulses  Ex: endorphins release when work out – why working out makes you feel better!

8. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.  3 opioid receptors 1) mu (μ): endorphine produced from hypothalamus & pituitary gland 2) kappa (κ): dynorphins found around pain nerve endings 3) delta (δ) : enkephlins produced in CNS/PNS  Naloxone is an antagonist & blocks all 3 receptors  Different opioids block varying receptors = explains why they have differing effects in different people

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10.  Absorption: oral (not morphine), parental  Distribution: bound to plasma PRO in varying degrees (35-65%)  Metabolism: Must go through Phase I & II  Excretion: kidney **Generally all have 1 hr onset, 4-6hr duration**

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12. EFFECTS OF OPIOIDSACTION AnalgesiaRaise pain threshold Sedation & Euphoria Cough SuppressionDepress the cough center in the medulla (antitussive) GIIncreased smooth-muscle tone of intestinal tract to ↓ propulsive contractions and motility

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14.  Severity of side effects is proportional to the potency  Opioid allergy is uncommon  Can be allergic to specific opioids & not others  Ex: allergy to codeine, can take hydrocodone ADVERSE RXNACTION Respiratory depressionCause of death in OD Nausea & EmesisStimulate chemoreceptor trigger zone (medulla) Constipation & Urinary retention See last slide MiosisIn OD Skin itchingHistamine released by opioids

15. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. CLASSIFICATIONACTION Full agonistStrong-mod analgesic Mixed opioidAnalgesia Some antagonist activity Pure antagonistsNo analgesic effects Used in opioid OD

16. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. STRONG POTENCY OPIOID AGONIST Morphine Methadone & Buprenorphine Meperidine(Demerol) Oxycodone Hydrocodone Fentanyl(Duragesic patch) MODERATE POTENCY OPIOID AGONIST Codeine Propoxyphene Dextromethorphan(Robitussin,Sucrets,Vicks,Delsm,Benylin) Loperamide(Imodium) Diphenoxylate(Lomotil) Tramadol(Ultram)

17. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. STRONG POTENCY OPIOID AGONIST Morphine Methadone & Buprenorphine Meperidine(Demerol) Oxycodone(OxyCotin) Hydrocodone Fentanyl(Duragesic patch)

18. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Morphine: prototype p.64  All other opioids compared to 10mg of morphine  Body recognizes painful stimulus but not perceived by brain as pain  Not commonly used in dentistry  Parental only Methadone(Dolophine) p.67  Used to treat opioid addiction  Used to “wean” people off narcotics Buprenorphine not in book but need to know for boards  Newest drug on market to tx withdrawal  Used for heroin addiction, OxyCotin, Percocet  Used in combo with Naloxone

19. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Mereridine(Demerol) p.67  Less effective than morphine  Half duration of action  75mg demerol = 10mg morphine (book correction P.67  Sometimes used in dentistry

20. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Which narcotic is not used in dentistry? a. Morphine b. Hydrocodone c. Oxycodone d. Meperidine e. Codeine f. Fentanyl

21. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Which narcotic is not used in dentistry? a. Morphine b. Hydrocodone c. Oxycodone d. Meperidine e. Codeine f. Fentanyl

22. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Oxycodone(OxyCotin) & Hydrocodone  Can combo with NSAIDs, aspirin, acetaminophen Drug NameHydrocodone + Vicodin, Lortab, Lorcet, Percocet, Tylox Acetaminophen VicoprofenIbuprofen Aspirin Drug NameOxycodone + Acetaminophen CombunoxIbuprofen PercodanAspirin

23. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. A patient who has taken Vicoprofen (hydrocodone with ibuprofen) for the first time could likely complain of all the following adverse rxns EXPECT which one? a) Nausea b) Diarrhea c) Queasy stomach d) Dizziness e) Drowsiness

24. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. A patient who has taken Vicoprofen (hydrocodone with ibuprofen) for the first time could likely complain of all the following adverse rxns EXPECT which one? a) Nausea b) Diarrhea c) Queasy stomach d) Dizziness e) Drowsiness

25. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Fentanyl(Duragesic)  Used during general anesthesia  Useful for SEVERE CHRONIC pain  Patch, parental

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27. Codeine p.67  120mg codeine = 10mg morphine  Prodrug with P450 metabolism  Uses Combined w/ acetaminophen for mild-moderate pain Amt codeine designated by # Ex: #2 (15 mg), #3 (30 mg), #4 (60 mg) Added to cough syrups as an antitussive

28. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Propoxyphene  November 2010: FDA banned Darvon & Darvocet from containing propoxyphene  Cardio issues in otherwise healthy people Dextromethorphan(Robitussin,Sucrets,Vicks,Delsm,Benylin)  ANTITUSSIVE  No analgesia Loperamide(Imodium)  No analgesia  Smooth muscle tone in GI tract = antidiarrheal Diphenoxylate(Lomotil)  Antidiarrheal (combo with atropine) Tramadol(Ultram) p.68  CNS & opioid activity  Not a controlled substance  Can cause serious neurotoxicity – do NOT use as first line drug

29. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Which of the following drugs is the standard to which all opiates are compared? a) Codeine b) Oxycodone c) Hydrocodone d) Morphine e) Fentanyl f) Meperidine

30. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Which of the following drugs is the standard to which all opiates are compared? a) Codeine b) Oxycodone c) Hydrocodone d) Morphine e) Fentanyl f) Meperidine

31. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Your patient has a hx of neuropathic pain. They are currently taking oxycodone (Oxycontin), which is an opiate analgesic. Which 2 of the following are adverse effects of oxycodone? a. Nausea b. Constipation c. Peptic ulcers d. Insomnia

32. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Your patient has a hx of neuropathic pain. They are currently taking oxycodone (Oxycontin), which is an opiate analgesic. Which 2 of the following are adverse effects of oxycodone? a. Nausea b. Constipation c. Peptic ulcers d. Insomnia

33. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Which of the following drugs is a synthetic opioid analgesic used as an intravenous sedative and is more potent than morphine? a. Meperidine b. Pentazocine(Talwin) c. Percocet d. Fentanyl

34. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Which of the following drugs is a synthetic opioid analgesic used as an intravenous sedative and is more potent than morphine? a. Meperidine b. Pentazocine(Talwin) c. Percocet d. Fentanyl

35. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. CLASSIFICATIONACTION Full agonistStrong-mod analgesic Mixed opioidAnalgesia Some antagonist activity Pure antagonistsNo analgesic effects Used in opioid OD

36. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.  Combinations of agonists, antagonists, partial agonists  Uses  Pre & post-op surgery analgesia  During labor & delivery (L&D)

37. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. DrugNotations Pentazocine(Talwin)Only mixed for oral use Agonist-Antagonist Butorphanol(Stadol)Nasal spray for migraines Buprenorphine(Buprenex, SubutexNarcotics withdrawal drug

38. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. CLASSIFICATIONACTION Full agonistStrong-mod analgesic Mixed opioidAnalgesia Some antagonist activity Pure antagonistsNo analgesic effects Used in opioid OD

39. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.  Used for OD = reverse opioid effects  All dental emerg kits should contain!! (NBQ) OPIOID ANTAGONIST Naloxone(Narcan) Naltrexone(ReVia, Vivitrol, Relistor) Embeda (Naltrexone+Morphine) Not in book but been in boards in recent years BOOK CORRECTION: Nalmefene on p.68 is a discontinued drug – not need to know! p.68

40. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Which of the following drugs is the protype opioid antagonist? a) Morphine b) Naloxone c) Propanolol d) Ibuprofen

41. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Which of the following drugs is the protype opioid antagonist? a) Morphine b) Naloxone c) Propanolol d) Ibuprofen

42. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.  WHO has a stepladder for treating dental pain  Dental pain is a nociceptive pain  Mild-Mod pain = NSAIDs (ceiling effect: ↑ dose does not ↑ effects)  Mod pain = Short-acting narcotic combination containing either oxycodone or codeine (NO ceiling effect)  Chronic pain (TMD, trigeminal, neuropathy) = difficult to tx & BEST option is tricyclic antidepressant, muscle relaxers, anticonvulsant

43. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Your hygiene patient has a hx of opioid dependence. Which of the drugs below has been approved by the FDA as maintenance treatment of opioid dependency and which the patient may be taking? a. Suboxone b. Sudafed c. Sufentanyl d. Fentanyl

44. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Your hygiene patient has a hx of opioid dependence. Which of the drugs below has been approved by the FDA as maintenance treatment of opioid dependency and which the patient may be taking? a. Suboxone b. Sudafed c. Sufentanyl d. Fentanyl

45. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Your patient has a history of drug abuse. Which agent could be given if needed in the treatment plan with no liability to cause an addiction? a. Phenobarbital b. Ibuprofen c. Hydrocodone d. Meperidine e. Codeine

46. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Your patient has a history of drug abuse. Which agent could be given if needed in the treatment plan with no liability to cause an addiction? a. Phenobarbital b. Ibuprofen c. Hydrocodone d. Meperidine e. Codeine

47. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Opioid drugs are used as all of the following EXCEPT which one? a) Analgesics b) Antiinflammatories c) Antitussives d) Antidiarrheals e) Preanesthetic medications

48. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Opioid drugs are used as all of the following EXCEPT which one? a) Analgesics b) Antiinflammatories c) Antitussives d) Antidiarrheals e) Preanesthetic medications

49. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Which of the following analgesics can produce drug dependence and addiction? a) Aspirin b) Ibuprofen c) Codeine d) Morphine e) Meperidine

50. Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved. Which of the following analgesics can produce drug dependence and addiction? a) Aspirin b) Ibuprofen c) Codeine d) Morphine e) Meperidine