A 60-year-old man with a history of moderate chronic obstructive pulmonary disease presents in the emergency department with a broken hip suffered in an automobile accident. He complains of severe pain. What is the most appropriate immediate treatment for his pain? Are any special precautions needed?
Morphine, the prototypical opioid agonist, has long been known to relieve severe pain with remarkable efficacy. The opium poppy is the source of crude opium from which Sertürner in 1803 isolated morphine, the pure alkaloid, naming it after Morpheus, the Greek god of dreams. It remains the standard against which all drugs that have strong analgesic action are compared. These drugs are collectively known as opioid analgesics and include not only the natural and semisynthetic alkaloid derivatives from opium but also synthetic surrogates, other opioid-like drugs whose actions are blocked by the nonselective antagonist naloxone, plus several endogenous peptides that interact with the different subtypes of opioid receptors.
Opium, the source of morphine, is obtained from the poppy, Papaver somniferum and P album. After incision, the poppy seed pod exudes a white substance that turns into a brown gum that is crude opium. Opium contains many alkaloids, the principal one being morphine, which is present in a concentration of about 10%. Codeine is synthesized commercially from morphine.
Classification & Chemistry
Opioid drugs include full agonists, partial agonists, and antagonists. Morphine is a full agonist at the μ (mu)-opioid receptor, the major analgesic opioid receptor (Table 31–1). In contrast, codeine functions as a partial (or "weak") μ-receptor agonist. Other opioid receptor subtypes include δ (delta) and κ (kappa) receptors. Simple substitution of an allyl group on the nitrogen of the full agonist morphine plus addition of a single hydroxyl group results in naloxone, a strong μ-receptor antagonist. The structures of some of these compounds are shown later in this chapter. Some opioids, eg, nalbuphine, are capable of producing an agonist (or partial agonist) effect at one opioid receptor subtype and an antagonist effect at another. The receptor activating properties and affinities of opioid analgesics can be manipulated by pharmaceutical chemistry; in addition, certain opioid analgesics are modified in the liver, resulting in compounds with greater analgesic action. Chemically, the opioids derived from opium are phenanthrene derivatives and include four or more fused rings, while most of the synthetic opioids are simpler molecules.
Table 31–1 Opioid Receptor Subtypes, Their Functions, and Their Endogenous Peptide Affinities. |Favorite Table|Download (.pdf)
Table 31–1 Opioid Receptor Subtypes, Their Functions, and Their Endogenous Peptide Affinities.
|Receptor Subtype||Functions||Endogenous Opioid Peptide Affinity|
|μ (mu)||Supraspinal and spinal analgesia; sedation; inhibition of respiration; slowed gastrointestinal transit; modulation of hormone and neurotransmitter release||Endorphins > enkephalins > dynorphins|
|δ (delta)||Supraspinal and spinal analgesia; modulation of hormone and neurotransmitter release||Enkephalins > endorphins and dynorphins|
|κ (kappa)||Supraspinal and spinal ...|
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