181lec8.key - Psych 181: Dr. Anagnostaras Lecture 8 OPIATES...

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OPIATES Psych 181: Dr. Anagnostaras Lecture 8 Opioids Opiates alkaloids found in the opium poppy (Papaver somniferum) [Gk. opion = “poppy juice”] Opioids compounds with opiate-like actions, including, but not conFned to opiates (e.g., synthetic, endogenous opioids) 1 2 3 Sunday, January 9, 2011
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Types of opioids 1. Naturally- occurring opium sap from opium poppy Two major active alkaloids morphine codeine 4 5 6 Sunday, January 9, 2011
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25 x more potent than paregoric Morphine Morpheus (god of Dreams) -son of Hypnos ~ 10% of opium by weight HO O OH N CH3 H Morphine Codeine methylmorphine ~ 0.5% of opium 7 8 9 Sunday, January 9, 2011
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2. Semi-synthetics 2. Semi-synthetics Heroin diacetylmorphine addition of two acetyl groups to morphine ~ 10x more potent than morphine pharmacological effect usually thought to be identical to morphine in brain: heroin > morphine (new data suggest morphine and heroin may have different actions; 1999) Semi-synthetic analgesics Hydromorphone (Dilaudid®) Hydrocodone (Hycodan®, Vicodin®) Oxycodone (Percodan®, Oxycontin®) 10 11 12 Sunday, January 9, 2011
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3. Synthetics Phenylpiperidines Fentanyl “china white” Carfentanil (Wildnil®) Meperidine (Demerol®) (MPPP) Methadone (Dolophine®) Propoxyphene (Darvon®) Benzomorphans Pentazocine (Talwin®) N CH3 CH2 C O O CH3 Pethidine (Meperidine) N H (CH3)2 Methadone CH2 C O CH3 H3C 13 14 15 Sunday, January 9, 2011
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Analgesic potency Analgesic potency Mild to moderate pain Moderately severe pain Severe pain codeine, propoxyphene (Darvon®) meperdine (Demerol®) heroin, hydromorphone (Dilaudid®) "Perc-a-pop" 4. Opioid antagonists naloxone (Narcan®) naltrexone Suboxone® (buprenorphine + naloxone) 16 17 18 Sunday, January 9, 2011
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5. Endogenous opioids Enkephalins, endorphins and dynorphins History of use - opium Since recorded history Ingredient in all sorts of medicinal preparations History of use - morphine “Soldiers disease” 19 20 21 Sunday, January 9, 2011
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History of use Ads for heroin Major effects Analgesia Relief of pain in absence of impairment in other sensory modalities Euphoria - Pleasure Produce sense of well being, reduce anxiety, positive feelings Other effects Respiratory depression Miosis (opposite of mydriasis) Gastrointestinal effects Cough Suppression Motor effects 22 23 24 Sunday, January 9, 2011
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Effects of repeated administration Tolerance, withdrawal & sensitization Tolerance and withdrawal 20 10 0 1 4 6 24 72 6 4 24 72 1 8 6 4 2 0 Naltrexone Morphine Control Time (hr) Behavioral withdrawal score LC unit activity 12.18 Sensitization Psychomotor stimulant effects Rewarding effects (conditioned place preference) 25 26 27 Sunday, January 9, 2011
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Mechanisms of action Primary action on opioid receptors located in CNS +/or periphery Different effects due to action at
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This note was uploaded on 04/01/2011 for the course PSYCH 181 taught by Professor Fick during the Spring '11 term at University of Tennessee.

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181lec8.key - Psych 181: Dr. Anagnostaras Lecture 8 OPIATES...

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