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    Summary of Common Opioids: Opioid Morphine Oxycodone Fentanyl Alfentanil Remifentanil Pethidine

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    Sammuel1324
    This document summarizes common opioids including morphine, oxycodone, fentanyl, alfentanil, remifentanil, and pethidine. It provides information on their chemistry, dose equivalents, routes of administration, bioavailability, distribution, metabolism, elimination, half-life, and special pharmacological properties. The opioids listed are metabolized primarily in the liver by cytochrome P450 enzymes like CYP3A4 and CYP2D6 and undergo glucuronidation, demethylation, and hydrolysis. They are eliminated renally and have half-lives ranging from 1.5 hours for alfentanil to 4-5 hours for pethidine. Special

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    Summary of Common Opioids: Opioid Morphine Oxycodone Fentanyl Alfentanil Remifentanil Pethidine

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    Sammuel1324
    23 views2 pages
    This document summarizes common opioids including morphine, oxycodone, fentanyl, alfentanil, remifentanil, and pethidine. It provides information on their chemistry, dose equivalents, routes of administration, bioavailability, distribution, metabolism, elimination, half-life, and special pharmacological properties. The opioids listed are metabolized primarily in the liver by cytochrome P450 enzymes like CYP3A4 and CYP2D6 and undergo glucuronidation, demethylation, and hydrolysis. They are eliminated renally and have half-lives ranging from 1.5 hours for alfentanil to 4-5 hours for pethidine. Special

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    summary of opioids

    Original Title

    Opioid Summary

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    This document summarizes common opioids including morphine, oxycodone, fentanyl, alfentanil, remifentanil, and pethidine. It provides information on their chemistry, dose equivalents, routes of administration, bioavailability, distribution, metabolism, elimination, half-life, and special pharmacological properties. The opioids listed are metabolized primarily in the liver by cytochrome P450 enzymes like CYP3A4 and CYP2D6 and undergo glucuronidation, demethylation, and hydrolysis. They are eliminated renally and have half-lives ranging from 1.5 hours for alfentanil to 4-5 hours for pethidine. Special

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    23 views2 pages

    Summary of Common Opioids: Opioid Morphine Oxycodone Fentanyl Alfentanil Remifentanil Pethidine

    Uploaded by

    Sammuel1324
    This document summarizes common opioids including morphine, oxycodone, fentanyl, alfentanil, remifentanil, and pethidine. It provides information on their chemistry, dose equivalents, routes of administration, bioavailability, distribution, metabolism, elimination, half-life, and special pharmacological properties. The opioids listed are metabolized primarily in the liver by cytochrome P450 enzymes like CYP3A4 and CYP2D6 and undergo glucuronidation, demethylation, and hydrolysis. They are eliminated renally and have half-lives ranging from 1.5 hours for alfentanil to 4-5 hours for pethidine. Special

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    Summary of Common Opioids

    Opioid Morphine Oxycodone Fentanyl Alfentanil Remifentanil Pethidine


    Chemistry Phenanthrene Phenanthrene Phenylpiperidine Phenylpiperidine Phenylpiperidine Phenylpiperidine
    Dose equivalent (i.v.) 10 mg 15 mg 100 microg 1 mg 100 microg 100 mg
    Absorption
    Routes IV/IM/SC IV IV IV IV IV/IM
    IT/ED,PO,PR,TOP PO IT/ED,PO,IN,TOP PO
    Bioavailability (oral) 20 ~ 30% 60 ~ 80% 30% - - 50%
    Distribution
    Vd (steady state) ‡ 3.5 L/kg 2.5 L/kg 4 L/kg 0.4 L/kg 0.2 L/kg 4 L/kg
    pKa‡ 8.0 8.5 8.4 6.5 7.1 8.5
    %unionised (pH=7.4) 23% 7% 10% 90% 67% 5%
    §
    Relative lipid sol. 1 ~1 600 90 20 30
    Protein binding§ 35% 45% 83% 90% 70% 60%
    t(iv peak effect) 19 min 5 ~ 10 min (?) 4 min 2 min 1 ~ 2 min 6 min
    Metabolism
    Site hepatic + extra- CYP3A4 (major) CYP 3A4 CYP 3A4 plasma and tissue hepatic CYP
    hepatic (renal) CYP2D6 (minor) esterases
    Opioid Morphine Oxycodone Fentanyl Alfentanil Remifentanil Pethidine
    Metabolites glucuronidation: demethylation: demethylation: N-dealkylation: remifentanil acid demethylation:
    M3G (70%) - inactive noroxycodone (3A4) norfentanyl (inactive) noralfentanil (essentially inactive) norpethidine (90%,
    M6G (10%) - active oxymorphone (2D6) (inactive) active)
    demethylation: N-phenyl- ! norpethidinic acid
    nomorphine (5%) propionamide hydrolysis:
    codeine pethidinic acid
    Elimination
    Renal 1 ~ 2% parent 15% parent minimal < 0.5% parent∆ – pH dependent (acidic
    urine ! more parent)
    25% parent (@ pH 5)
    Clearance 16 mL/kg/min 7 mL/kg/min 13 mL/kg/min 6 mL/kg/min 40 mL/kg/min 12 mL/kg/min
    ∆
    t1/2 2 ~ 4 hrs 3 ~ 4 hrs 2 ~ 4 hrs 1.5 hrs 6 min 3 ~ 5 hrs
    CSHT (4 hr infusion) – – 4 hrs 60 min§ 4 min∆ –
    Pharmacodynamics
    Special properties histamine release muscle rigidity muscle rigidity muscle rigidity anticholinergic
    sphincter of Oddi LA effects
    spasm w/d start 2~6 hrs addictive +++
    w/d start 6~12 hrs w/d duration 4~5 d norpethidine !
    w/d duration 7~10 d induces seizures
    w/d same as fentanyl

    ‡ = Miller § = Peck and Hill ∆ = Stoelting 5th

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