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INTRODUCTION

This chapter will be most useful after having a basic understanding of the material in Chapter 18, Opioids, Analgesia, and Pain Management in Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 12th Edition. In addition to the material presented here, the 12th Edition includes:

  • A history of analgesic use

  • A detailed description of the endogenous opioid systems: ligands and receptors

  • A discussion of opioid receptor classes, distribution, binding/coupling requirements for opiate ligands, and the functional consequences of acute and chronic opiate receptor activation

  • Figure 18-8 Structures of morphine-related opiate agonists and antagonists

  • Figure 18-9 Chemical structures of piperidine and phenylpiperidine analgesics

  • Details of the cellular and molecular mechanisms of opioid tolerance, dependence, and withdrawal

  • Nonanalgesic therapeutic uses of opioids

  • Table 18-4 Resources for Pain Management

  • Table 18-5 World Health Organization Analgesic Ladder

LEARNING OBJECTIVES

  • Understand the mechanisms of action, adverse effects, and therapeutic uses of opiate receptor agonists.

  • Know the mechanisms of action and therapeutic uses of opiate receptor antagonists.

  • Know the role of opiate receptor agonists in the management of acute and chronic pain.

  • Know the different methods of administration of opiate receptor agonists that improve analgesic efficacy while reducing side effects.

DRUGS INCLUDED IN THIS CHAPTER

  • Alfentanil (ALFENTA)

  • Benzonatate (TESSALON, others)

  • Buprenorphine; injection (BUPRENEX); oral (SUBUTEX); in combination with naloxone (SUBOXONE)

  • Butorphanol (STADOL, others)

  • Codeine

  • Dextromethorphan marketed for over-the-counter sales

  • Difenoxin (MOTOFEN) available only in combination with atropine

  • Diphenoxylate (LOMOTIL, others) available only in combination with atropine

  • Fentanyl citrate (SUBLIMAZE, others); transdermal patch (DURAGESIC, others); fentanyl buccal tablets, buccal film, lollipop-like lozenges (FENTORA, ONSOLIS, ACTIQ, others)

  • Hydrocodone (LORTAB, VICODIN, others)

  • Hydromorphone (DILAUDID, others)

  • Levorphanol (LEVO-DROMORAN)

  • Loperamide (IMODIUM, others)

  • Meperidine (pethidine, DEMEROL, others)

  • Methadone (DOLOPHINE, others)

  • Methylnaltrexone (RELISTOR)

  • Morphine sulfate; liposomal formulation (DEPODUR); preservative-free for spinal delivery (DURAMORPH, DEPODUR, others)

  • Nalbuphine (NUBAIN, others)

  • Nalmefene—no longer marketed in the United States

  • Nalorphine (NALLINE, others)

  • Naloxone (NARCAN, others)

  • Naltrexone (REVIA, VIVITROL, others)

  • Naltrindole (δ receptor antagonist used only for biomedical research)

  • Oxycodone (PERCODAN); in combination with acetaminophen (PERCOCET); extended release (OXYCONTIN)

  • Oxymorphone (NUMORPHAN, others)

  • Pentazocine (TALWIN); in combination with acetaminophen (TALCEN); in combination with naloxone (TALWIN NX)

  • Propoxyphene (DARVON, others)

  • Propoxyphene napsylate (DARVON-N)

  • Remifentanil (ULTIVA)

  • Sufentanil (SUFENTA, others)

  • Tapentadol (NUCYNTA)

  • Tramadol (ULTRAM)

ACTIONS AND SELECTIVITIES OF SOME OPIOIDS AT μ, δ, κ RECEPTORS

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