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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
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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.
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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)
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