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  • Pharmacology Opioids

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    Jireh Mejino
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    This document discusses opioids and their mechanisms and effects. It describes three main opioid receptor types (MOP, KOP, DOP) that are involved in analgesia and can cause different side effects like respiratory depression, dysphoria, or decreased gastrointestinal motility. It outlines how opioids are absorbed, distributed, metabolized and excreted in the body. The major pharmacological effects of opioids on the central nervous system, cardiovascular, respiratory, gastrointestinal and other systems are summarized. Finally, it discusses clinical uses of opioids as well as topics like opioid tolerance, dependence and addiction.

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    Review material for Opioid Drugs

    Original Title

    Pharmacology_Opioids

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    This document discusses opioids and their mechanisms and effects. It describes three main opioid receptor types (MOP, KOP, DOP) that are involved in analgesia and can cause different side effects like respiratory depression, dysphoria, or decreased gastrointestinal motility. It outlines how opioids are absorbed, distributed, metabolized and excreted in the body. The major pharmacological effects of opioids on the central nervous system, cardiovascular, respiratory, gastrointestinal and other systems are summarized. Finally, it discusses clinical uses of opioids as well as topics like opioid tolerance, dependence and addiction.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Flag for inappropriate content
    19 views5 pages

    Pharmacology Opioids

    Uploaded by

    Jireh Mejino
    This document discusses opioids and their mechanisms and effects. It describes three main opioid receptor types (MOP, KOP, DOP) that are involved in analgesia and can cause different side effects like respiratory depression, dysphoria, or decreased gastrointestinal motility. It outlines how opioids are absorbed, distributed, metabolized and excreted in the body. The major pharmacological effects of opioids on the central nervous system, cardiovascular, respiratory, gastrointestinal and other systems are summarized. Finally, it discusses clinical uses of opioids as well as topics like opioid tolerance, dependence and addiction.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
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    of 5

    OPIOIDS

    I. Different types of pain and their mechanisms


    ● Nociceptive
    ● Neuropathic

    ● Opium
    ● Opiate
    ● Opioid
    ● Narcotic

    II. Pharmacological effects associated with opioid receptors

    MOP supraspinal/spinal analgesia smooth muscle spasm, physical dependence, release of


    prolactin and growth hormone, nausea and vomiting

    KOP supraspinal/spinal analgesia less physical dependence, dysphoria, psychotomimetic effects,


    diuresis

    DOP supraspinal/spinal analgesia less respiratory depression, decreased gastrointestinal motility,


    release of Growth Hormone

    Absorption Distribution Metabolism Excretion

    SQ, IM, Oral Bind to plasma proteins w/ Converted to polar metabolites Polar metabolites are excreted in
    varying affinity the urine
    Oral = higher dose due to first HEPATIC P450 METABOLISM
    pass effect Rapidly leave the blood and > Primary route of degradation of In patients with renal impairment,
    localize in highly perfused tissues: the phenylpiperidine opioids caution should be observed in
    Other routes: Oral mucosa Brain, lungs, liver, kidneys, spleen (fentanyl, meperidine, alfentanil, giving morphine or any potent
    (Lozenges), Transdermal (patch) sufentanil) opioids due to the risk of sedation
    Accumulates in fatty tissues and respiratory depression (when
    (highly lipophilic opioids) given in higher doses).
    PHARMACOLOGICAL EFFECTS
    CNS Cardiovascular Respiratory Gastrointestinal Genitourinary
    Ocular Effects –
    Analgesia Bradycardia (mild) Respiratory Nausea and vomiting Depressed renal Miosis
    Sedation Peripheral depression Delayed absorption function: increased
    Euphoria/Dysphoria vasodilation Cough suppression Spasm of sphincter of bladder & ureteral Histamine release –
    Hallucinations oddi tone anaphylaxis
    Tolerance & Constipation Uterus: prolonged
    Dependence labor Truncal rigidity
    Immunity
    Effects on pregnancy
    and neonates

    CLINICAL USES OPIOID TOLERANCE OPIOID DEPENDENCE


    ● Analgesia ● Lesser susceptibility to the effects of Physical Dependence
    ● Obstetrical Labor opioids or decrease in drug effect ● Sweating, lacrimation, dehydration
    ● Renal / Biliary colic ● Can be due to down regulation of opioid ● Fear, anxiety, restlessness
    ● Acute Pulmonary Edema receptors ● Mydriasis, tremor, colic
    ● Cough ● May also be caused by decrease in ● Hypertension, tachycardia, weight
    ● Diarrhea production of endogenous opioids loss
    ● Can be a result of opioid addiction Psychological Dependence
    ● Associated with cravings (lasting for
    months or years)
    III. Opioid agonists and antagonists

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