ANALGESIA2011-01.key

ANALGESIA2011-01.key - Pharmacology of Opioid Analgesics...

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Pharmacology of Opioid Analgesics Spring 2011 Harvey Alan Berman, PhD, MPH Department of Pharmacology and Toxicology [email protected] 829-2658
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Pain • “An unpleasant sensory and emotional experience associated with actual or potential tissue damage” • Distinguish: –Pain as a specific sensation –Pain as suffering
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Pain is transmitted through Thin (1-5 μ m), myelinated A δ fibers v = 12-30 m/sec – Fast, 1 st pain Very thin (< 1 μ m), nonmyelinated C fibers v = 0.5-2 m/sec – Slow, 2 nd pain • Duller, aching, diffuse pain • These fibers also carry sensation of itching
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Conduction of pain impulses from the periphery to the brain occurs through a multineuron pathway
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Types of Pain • Nociceptive pain results from injury to tissues – Somatic pain – Visceral pain • Neuropathic pain results from injury to peripheral nerves. • Both types respond differently to analgesic drugs.
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Nociceptive pain • Somatic pain – Results from injury to tissues • Bones, joints, muscles – Localized and sharp in quality • Visceral pain – Results from injury to visceral organs • E.g., small intestine – Vaguely localized with a diffuse aching quality
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Papaver somniferum Opium poppy • Resin from the poppy is collected and processed into opium
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Opium alkaloids Morphine (9-17 % by weight opium) – Chiefly responsible for pharmacological actions of opium Codeine (0.3-4 %) – Methylmorphine, has similar but weaker actions Thebaine (0.2 %) – Practically devoid of analgesic activity – No medicinal use, but it provides a synthetic route fo hydroxylated opioids
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Morphine N O HO OH CH 3 3 6 17
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Structural relationships among some opiates N O HO OH CH 3 N O H 3 CO OH CH 3 N O O CH 3 CCH 3 O O O H 3 CC N O H 3 CO OCH 3 CH 3 N O HO O CH 2 CH CH 2 OH N O H 3 CO O CH 3 OH MORPHINE CODEINE HEROIN THEBAINE NALOXONE OXYCODONE 3 6 17
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A-D-M-E • In general: – Opioids are absorbed well IM, SC, and oral and nasal mucosa – Rapid distribution from blood into highly perfused tissues (lung, liver, kidney, spleen)
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This note was uploaded on 03/06/2011 for the course PMY 406 taught by Professor Berman during the Spring '11 term at SUNY Buffalo.

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ANALGESIA2011-01.key - Pharmacology of Opioid Analgesics...

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