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    Trimebutine: Drug Delivery Systems Ii

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    merve yaman
    Trimebutine is a spasmolytic agent used to treat irritable bowel syndrome and other gastrointestinal motility disorders. It exists as both a white to off-white powder and as the maleate salt trimebutine maleate. Trimebutine regulates intestinal and colonic motility by targeting ion conductance involved in gastrointestinal motility through various mechanisms including inhibiting calcium and potassium currents. It can both stimulate and inhibit spontaneous contractions in the gastrointestinal tract depending on its concentration. Common side effects include dry mouth and gastrointestinal issues like diarrhea, while overdosage is treated with gastric lavage.

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    © All Rights Reserved
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    Trimebutine: Drug Delivery Systems Ii

    Uploaded by

    merve yaman
    95 views12 pages
    Trimebutine is a spasmolytic agent used to treat irritable bowel syndrome and other gastrointestinal motility disorders. It exists as both a white to off-white powder and as the maleate salt trimebutine maleate. Trimebutine regulates intestinal and colonic motility by targeting ion conductance involved in gastrointestinal motility through various mechanisms including inhibiting calcium and potassium currents. It can both stimulate and inhibit spontaneous contractions in the gastrointestinal tract depending on its concentration. Common side effects include dry mouth and gastrointestinal issues like diarrhea, while overdosage is treated with gastric lavage.

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    Trimebutin

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    trimebutine

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    Trimebutine is a spasmolytic agent used to treat irritable bowel syndrome and other gastrointestinal motility disorders. It exists as both a white to off-white powder and as the maleate salt trimebutine maleate. Trimebutine regulates intestinal and colonic motility by targeting ion conductance involved in gastrointestinal motility through various mechanisms including inhibiting calcium and potassium currents. It can both stimulate and inhibit spontaneous contractions in the gastrointestinal tract depending on its concentration. Common side effects include dry mouth and gastrointestinal issues like diarrhea, while overdosage is treated with gastric lavage.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    95 views12 pages

    Trimebutine: Drug Delivery Systems Ii

    Uploaded by

    merve yaman
    Trimebutine is a spasmolytic agent used to treat irritable bowel syndrome and other gastrointestinal motility disorders. It exists as both a white to off-white powder and as the maleate salt trimebutine maleate. Trimebutine regulates intestinal and colonic motility by targeting ion conductance involved in gastrointestinal motility through various mechanisms including inhibiting calcium and potassium currents. It can both stimulate and inhibit spontaneous contractions in the gastrointestinal tract depending on its concentration. Common side effects include dry mouth and gastrointestinal issues like diarrhea, while overdosage is treated with gastric lavage.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 12

    Trimebutine 

    DRUG DELIVERY SYSTEMS II 


    M E RV E YA M A N
    524517016
    Trimebutine
    Proper Name: Trimebutine
    Chemical Name: 2-dimethyl amino-2-phenyl-butyl 3,4,5-trimethoxybenzoate
    Molecular Formula: C22H29NO5
    Structural Formula:

    Molecular Weight: 387.5


    Description: Trimebutine is a white to off-white powder practically insoluble in water, sparingly soluble in ethanol, ether, n-
    hexane, and methanol and freely soluble in acetone and chloroform.
    Melting Point: 78 to 82 °C
    Trimebutine Maleate
    The maleate salt of trimebutine (C22 H29 NO5 C4 H4 O4; M.W.: 503.6) is a white to off-white powder
    (M.P. 128- 134°C ) very slightly soluble in ether and n-hexane, sparingly soluble in water, soluble
    in acetone, ethanol and methanol and freely soluble in chloroform.
    Description
    Trimebutine is a spasmolytic agent that regulates intestinal and colonic motility and relieves
    abdominal pain with antimuscarinic and weak opioid agonist effects.
    It is marketed for the treatment of irritable bowel syndrome (IBS) and lower gastrointestinal(GI)
    tract motility disorders, with IBS being one of the most common multifactorial GI disorders.

    IBS and GI SYMPTOMS


    Description
    It is used to restore normal bowel function and is commonly present in pharmaceutical mixtures
    as trimebutine maleate salt form.
    Trimebutine is not a FDA-approved drug, but it is available in Canada and several other
    international countries
    Pharmacodynamics
    Trimebutine is a spasmolytic agent that acts directly on smooth muscle to modulate gastric
    motility.
    It shows a "dual function" that stimulates or inhibits spontaneous contractions depending on
    the concentration and prior contractile activity in the preparation.
    Pharmacodynamics
    •Targeting ion conductance that regulates GI(gastroinstestinal) motility, trimebutine inhibits the
    inward calcium currents and calcium-dependent potassium currents in a concentration-
    dependent manner.
    •At lower concentrations (1-10uM), trimebutine depolarizes the resting membrane potential
    without affecting the amplitude of contractions, which is thought to be mediated by inhibition of
    outward potassium currents. It is also shown to activate T-type Ca2+ channel and increase gastric
    emptying, intestinal and colonic contractility.
    •At higher concentrations (100-300uM), reduced amplitude of spontaneous contractions and
    action potentials is thought to be mediated by inhibition of L-type Ca2+ channels and inward
    calcium current. Trimebutine mediates a local anesthetic action by acting as a weak agonist at mu
    opioid receptors.
    Mechanism of action
    At high concentrations, trimebutine is shown to inhibit the
    extracellular Ca2+ influx in the smooth muscle cells through
    voltage dependent L-type Ca2+ channels and further Ca2+
    release from intracellular Ca2+ stores.
    Trimebutine is suggested to bind to the inactivated state of the
    calcium channel with high affinity. Reduced calcium influx
    attenuates membrane depolarization and decrease colon
    peristalsis. It also inhibits outward K+ currents in response to
    membrane depolarization of the GI smooth muscle cells at
    resting conditions through inhibition of delayed rectifier K+
    channels and Ca2+ dependent K+ channels, which results in
    induced muscle contractions.
    Trimebutine binds to opioid receptors with more selectivity
    compared to delta or kappa opioid receptors but with lower
    affinity than their natural ligands. Its metabolites (N-
    monodesmethyl-trimebutine or nor-trimebutine), are also
    shown to bind to opoid receptors on brain membranes and
    myenteric synaptosomes.
    Toxicity
    Common gastrointestinal adverse effects include;
    dry mouth,
    foul taste,
    diarrhea,
     dyspepsia,
    epigastric pain,
    nausea and
    constipation.
    Some CNS effects include drowsiness, fatigue, dizziness, hot/cold sensations and headaches.
    Toxicity
    In case of overdosage, gastric lavage is recommended.
    Trimebutine is not reported to display teratogenic, mutagenic or carcinogenic potential.
    Dosage Forms

    FORM ROUTE STRENGTH


    Tablet Oral 200 mg
    Liquid Intramuscular; Intravenous 10 mg
    Tablet Oral 100 mg
    THANK YOU...

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