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    Antiemetik

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    ayu
    The document discusses various drugs used as antiemetics for different conditions causing nausea and vomiting. It describes the receptors and pathways involved and classifies antiemetic drugs. It provides details on specific drug classes including 5-HT3 antagonists, D2 receptor antagonists, NK1 antagonists, H1 receptor antagonists, and others. It summarizes that the choice of antiemetic depends on the underlying cause, such as motion sickness, vomiting during pregnancy, drug-induced vomiting, postoperative nausea, and vomiting due to cytotoxic drugs.

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    Antiemetik

    Uploaded by

    ayu
    42 views23 pages
    The document discusses various drugs used as antiemetics for different conditions causing nausea and vomiting. It describes the receptors and pathways involved and classifies antiemetic drugs. It provides details on specific drug classes including 5-HT3 antagonists, D2 receptor antagonists, NK1 antagonists, H1 receptor antagonists, and others. It summarizes that the choice of antiemetic depends on the underlying cause, such as motion sickness, vomiting during pregnancy, drug-induced vomiting, postoperative nausea, and vomiting due to cytotoxic drugs.

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    Antiemetik

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    The document discusses various drugs used as antiemetics for different conditions causing nausea and vomiting. It describes the receptors and pathways involved and classifies antiemetic drugs. It provides details on specific drug classes including 5-HT3 antagonists, D2 receptor antagonists, NK1 antagonists, H1 receptor antagonists, and others. It summarizes that the choice of antiemetic depends on the underlying cause, such as motion sickness, vomiting during pregnancy, drug-induced vomiting, postoperative nausea, and vomiting due to cytotoxic drugs.

    Copyright:

    © All Rights Reserved
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    42 views23 pages

    Antiemetik

    Uploaded by

    ayu
    The document discusses various drugs used as antiemetics for different conditions causing nausea and vomiting. It describes the receptors and pathways involved and classifies antiemetic drugs. It provides details on specific drug classes including 5-HT3 antagonists, D2 receptor antagonists, NK1 antagonists, H1 receptor antagonists, and others. It summarizes that the choice of antiemetic depends on the underlying cause, such as motion sickness, vomiting during pregnancy, drug-induced vomiting, postoperative nausea, and vomiting due to cytotoxic drugs.

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    © All Rights Reserved
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    of 23

    ANTIEMETICS DRUGS

    Bani Ayu Imaniah


    Receptors Associated with Nausea and
    Vomiting
    Pathophysiology of Emesis

    chemotherapy Cerebral cortex


    Opioids Smell
    Anesthetics Sight Anticipatory emesis
    Thought
    Chemoreceptor Vestibular
    Trigger Zone Vomiting Centre
    nuclei
    (medulla) Motion
    (CTZ) sickness Muscarinic
    Muscarinic, 5 HT3 Histaminic H1
    (Outside BBB)
    5 HT3
    Chemo & radio therapy
    Dopamine D2 Gastroenteritis
    Opioid receptors
    Substance p Pharynx & GIT
    5 HT3 receptors
    Chemical transmitters & receptors involved in vomiting
    include:

     Muscarinic receptors
     Dopamine (D2)
     Histamine (Histaminergic receptors H1)
     Serotonin (5 -HT3)
     Substance P (Neurokinin receptors, NK1)
     Opioid (Opioid receptors)
    Classification of Antiemetic Drugs

    1. 5-HT3 antagonists
    2. D2 receptor antagonists
    3. NK1 antagonists
    4. H1-receptor antagonists
    5. Muscarinic receptor antagonists
    6. Cannabinoids
    7. Glucocorticoids
    Serotonin (5-HT3) antagonists
     Drugs as
     Ondansetron
     Granisetron
     Orally or parenterally,
     have long duration of action, first pass effect
     The most potent antiemetic drugs
     Act by blocking 5-HT3 receptor centrally (in vomiting center,
    CTZ) and peripherally (5HT3 receptors on GI vagal afferents).
    Uses of 5-HT3 antagonists
     First choice for prevention of moderate to severe emesis:

     Chemotherapy-induced nausea and


    vomiting, especially cisplatin
     Post-radiation NV& Post-operative NV
     Their effects is augmented by combination
    with corticosteroids and NK1 antagonists.
    Side effects
    Headache, dizziness and constipation
    D2 receptor antagonists
     block D2 dopamine receptors in the CTZ
     Two types exist:

     Prokinetics drugs
     Neuroleptics (antipsychotics)
    D2 receptor antagonists
    Prokinetics drugs

     Domperidone: oral
     Metoclopramide: oral, i.v
     Are prokinetic agents ( increased GI
    motility & gastric emptying).
    Uses
     Antiemetics (blocking D2 receptors in CTZ)

     Effective against vomiting due to cytotoxic


    drugs, gastroenteritis, surgery, toxins,
    uremia, radiation

     Prokinetic (5 HT4 agonist activity )


     Gastroesophageal reflux disease (GERD)
     Gastroparesis (impaired gastric emptying
    after surgery).
    Metoclopramide crosses BBB but domperidone
    cannot (both have antiemetic effects as CTZ is
    outside BBB).

    Side effects (only for metoclopramide):


     Dyskinesia (extra-pyramidal side effects),
     menstrual disorders, impotence
     Sedation, drowsiness/mengantuk
    Other D2 receptor antagonists
    Neuroleptics (Antipsychotics)
     Chlorpromazine (CPZ), droperidol
     used for postoperative vomiting and chemotherapy-induced
    emesis.
    Side effects:
     Extra pyramidal symptoms
     Sedation
    Neurokinin1 (NK1) receptor antagonists
    Aprepitant
     Acts centrally as substance P antagonist by blocking
    neurokinin 1 receptors in vagal afferent fibers in STN.
     Orally
     Usually combined with 5-HT3 antagonists and corticosteroids
    in prevention of chemotherapy-induced nausea and vomiting
    and post- operative NV.
    H1-receptor antagonists
    • Include drugs as
    – diphenhydramine, promethazine
    – meclizine, cyclizine
    • Used for

    – Motion sickness
    – Morning sickness in pregnancy
    – Promethazine: severe morning sickness of
    pregnancy (if only essential).
    Muscarinic receptor antagonists
     Hyoscine (scopolamine)
     Orally, injection, patches
     Used as transdermal patches in motion sickness (applied
    behind the external ear).
     Reduce impulses from vestibular apparatus
     Not in chemotherapy-induced vomiting
    Cannabinoids
     Nabilone, dronabinol
     mechanism of action not understood.
     act at central cannabinoid receptors.
     Used in vomiting due to cytotoxic drugs
    (adjuvant therapy).
     Limited use due to side effects

    Side effects:
    sedation, hallucination.
    Glucocorticoids
     Dexamethasone - methylprednisolone
     Used in chemotherapy-induced vomiting
     combined with 5-HT3 antagonists or NK1 receptor
    antagonists.
    Glucocorticoids
    Side effects:
     Hyperglycemia
     Hypertension
     Cataract
     Osteoporosis
    Summary
    The choice of antiemetic depends on the etiology
    Motion sickness
    Muscarinic antagonists (scopolamine)
    Antihistaminics (diphenhydramine)

    Vomiting with pregnancy (morning sickness)


    avoid all drugs in the first trimester
    Pyridoxine (B6)
    Promethazine (late pregnancy).
    Drug- induced vomiting (CTZ), uremia, gastritis
    Dopamine antagonists (metoklopramide, domperidon)

    Post operative nausea & vomiting


    Dopamine antagonists (metoklopramide, domperidon)

    Vomiting due to cytotoxic drugs.


    5-HT3 antagonists (ondansentron)
    NK1 antagonists (aprepitant)
    D2- antagonists (metoklopramide, domperidon)
    Glucocorticoids (dexamthasone)
    Cannabinoids (nabilone)
    THANK YOU

    QUESTIONS ?

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