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    Morphine - An Opioid Analgesic: Mechanism

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    Jesse Chusid
    Morphine is an opioid analgesic that acts on opiate receptors in the central nervous system, primarily the mu receptors, to inhibit neurotransmitter release. It is absorbed from the gastrointestinal tract but undergoes extensive first-pass metabolism, resulting in a bioavailability of around 25%. Morphine's major metabolite, morphine-6-glucuronide, has potent analgesic effects. Common indications for morphine include pain relief and decreasing gastrointestinal motility. Adverse reactions include nausea, vomiting, respiratory depression, and dependence. It is contraindicated in patients with gastrointestinal or pulmonary disorders due to the risks of obstruction and respiratory depression.

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    Morphine - An Opioid Analgesic: Mechanism

    Uploaded by

    Jesse Chusid
    14 views1 page
    Morphine is an opioid analgesic that acts on opiate receptors in the central nervous system, primarily the mu receptors, to inhibit neurotransmitter release. It is absorbed from the gastrointestinal tract but undergoes extensive first-pass metabolism, resulting in a bioavailability of around 25%. Morphine's major metabolite, morphine-6-glucuronide, has potent analgesic effects. Common indications for morphine include pain relief and decreasing gastrointestinal motility. Adverse reactions include nausea, vomiting, respiratory depression, and dependence. It is contraindicated in patients with gastrointestinal or pulmonary disorders due to the risks of obstruction and respiratory depression.

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    Notes on Pharmacology of Morphine

    Original Title

    Morphine

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    Morphine is an opioid analgesic that acts on opiate receptors in the central nervous system, primarily the mu receptors, to inhibit neurotransmitter release. It is absorbed from the gastrointestinal tract but undergoes extensive first-pass metabolism, resulting in a bioavailability of around 25%. Morphine's major metabolite, morphine-6-glucuronide, has potent analgesic effects. Common indications for morphine include pain relief and decreasing gastrointestinal motility. Adverse reactions include nausea, vomiting, respiratory depression, and dependence. It is contraindicated in patients with gastrointestinal or pulmonary disorders due to the risks of obstruction and respiratory depression.

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    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    14 views1 page

    Morphine - An Opioid Analgesic: Mechanism

    Uploaded by

    Jesse Chusid
    Morphine is an opioid analgesic that acts on opiate receptors in the central nervous system, primarily the mu receptors, to inhibit neurotransmitter release. It is absorbed from the gastrointestinal tract but undergoes extensive first-pass metabolism, resulting in a bioavailability of around 25%. Morphine's major metabolite, morphine-6-glucuronide, has potent analgesic effects. Common indications for morphine include pain relief and decreasing gastrointestinal motility. Adverse reactions include nausea, vomiting, respiratory depression, and dependence. It is contraindicated in patients with gastrointestinal or pulmonary disorders due to the risks of obstruction and respiratory depression.

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    of 1

    Morphine – an opioid analgesic

    Mechanism
    • acts as an agonist at opiate receptors within the CNS
    (primarily at µ receptors)
    • these receptors work to inhibit synaptic transmission in
    the CNS and the myenteric plexus
    • opens K channels to hyperpolarize cell, and interferes
    with Ca release, thus inhibiting neurotransmitter
    release

    Pharmacokinetics
    • morphine is absorbed well from the GI tract but is subject to extensive first-pass metabolism
    • oral bioavailability is approximately 25% - the duration of action of morphine is somewhat longer
    with the oral route
    • morphine-6-glucuronide is the major metabolite of morphine and has potent analgesic effects
    • morphine is eliminated by glomerular filtration primarily as morphine-3-glucuronide
    • 90% of the total excretion takes place the first day
    • the half life of morphine is about 2-4 hours

    Indications
    • pain
    • treatment of diarrhea – morphine decreases gastric motility and increases GI transit time (i.e.
    causes constipation)
    • treatment of cough – direct inhibition of tussive centers in brain

    Adverse Reactions
    • nausea and vomiting
    • respiratory depression
    • tolerance and physical dependence
    • opiate agonists can precipitate seizures
    • urinary retention

    Contraindications
    • patients with GI disorders (GI obstruction, ulcerative colitis etc.)
    • patients with pulmonary disease (due to respiratory depression)
    • asthmatics – morphine can precipitate the release of histamine

    Interactions
    • use of morphine with other CNS depressants can make respiratory depression extremely
    dangerous

    (see Clinical Pharm. Online for way too much detail)

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