ANALGESIA2011-02.key

ANALGESIA2011-02.key - Pharmacology of Selected Opiods...

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Pharmacology of Selected Opiods Spring 2011 Harvey Alan Berman, PhD, MPH Department of Pharmacology and Toxicology hberman@buffalo.edu 829-2658
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Opioid classification Agonist –Strong –Mild-to-moderate Opioids with mixed actions –Agonist-antagonist (Ag-Antag) –Partial agonist Antagonist
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Strong Agonists • Morphine • Heroin • Hydromorphone ( D ILAUDID ) • Oxymorphone ( N UMORPHAN ) • Methadone ( D OLOPHINE ) • Meperidine ( D EMEROL ) • Fentanyl ( S UBLIMAZE ) • Levorphanol ( L EVO -D ROMORAN )
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Metabolism of Heroin • Heroin is biologically inactive • In the body it is converted to MAM and then into morphine • MAM and morphine are responsible for the effects elicited upon injection of heroin N O HO OH CH 3 N O OH CH 3 O O H 3 CC MORPHINE HEROIN N O O CH 3 CCH 3 O O O H 3 CC MONOACETYLMORPHINE
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Methadone (Dolophine) μ -Agonist • Similar to morphine • Prolonged use give rise to tolerance • Uses: – Relief of pain – Treatment of opioid abstinence – Treatment of opioid dependence • Oral efficacy ! C CH 2 C HC CH 2 O CH 3 CH 3 N CH 3 CH 3 CH 3 N CH 3 CH 3 CH 3 O
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Opioid Withdrawal Syndrome W/i hours of missing first dose of morphine – sense of intense fear (this can be alleviated by a placebo) 8-16 hrs : lacrimation, rhinorrhea (as in a severe head cold), yawning, sweating, mydriasis, anorexia, nervousness, irritability, tremors, increased anxiety and fear, restless sleep
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W/i 36 hrs : – skeletal muscle fasciculation and twitch – severe/painful cramps develop in legs and stomach – intense/uncontrolled vomiting, salivation, diarrhea, and urination – weakness, depression, chilliness/sweating, gooseflesh ( " cold turkey " ), muscle spasms, kicking movements ( " kicking the habit " ). – patient is unable to sleep; respiratory rate, blood pressure, temperature, blood sugar, basal metabolic rate Withdrawal syndrome reaches its peak within 48-72 hours, and subsides over the next 10 days. Withdrawal reaction is evidence for physical dependence .
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• Intensity of withdrawal reaction depends Half-life of drug being used Degree of physical dependence • Withdrawal syndrome of methadone and codeine qualitatively the same but less intense than for morphine. For morphine, with a short half-life, symptoms of abstinence are intense but brief. For methadone, with a long-half-life, symptoms are less intense but more prolonged.
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• It is to be emphasized that, although withdrawal from opioids is unpleasant, the opioid withdrawal syndrome is rarely dangerous to the patient.
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ANALGESIA2011-02.key - Pharmacology of Selected Opiods...

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