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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 [email protected] 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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