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    Pharmacology L1, Antiemetics & Prokinetic Drugs 2024

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    Pharmacology L1, Antiemetics & Prokinetic Drugs 2024

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    7 views28 pages

    Pharmacology L1, Antiemetics & Prokinetic Drugs 2024

    Uploaded by

    mido.ali.01148515771

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    of 28

    Anti-emetics & Prokinetic drugs

    Dr/Amira Eladl
    Lecturer of Clinical Pharmacology
    Faculty of medicine
    Mansoura - Horus University
    Part 1: Drugs for vomiting
    How vomiting occur?
    Antiemetic Drugs
    1. Muscarinic blockers:
    Atropine Hyoscine

    2. H1-blockers

    3. 5-HT3 blockers: Ondansetron Granisetron


    They block 5HT3 receptors in the GIT, solitary tract nucleus and CTZ.

    4. Dopamine blockers
    Metoclopramide Domperidone
    They block D2 receptors in the CTZ.

    5. Cannabinoid derivatives:
    Nabilone and Dronabinol
    1. Muscarinic blockers
    2. H1-blockers
    H1-blockers are mainly useful for the
    prevention of motion sickness. They are
    also effective in morning sickness,
    postoperative and other types of
    vomiting .

    Dimenhydrinate, diphenhydramine,
    doxylamine, promethazine, cyclizine and
    meclizine are some of the H1-blockers
    that have antiemetic properties.
    Their antiemetic effect is due to
    sedative, H1 blockade and central
    anticholinergic actions.
    3-5-HT3 blockers
    (Ondansetron)
    4. Dopamine blockers

    They block D2 receptors


    in the CRTZ.

    Metoclopromide : pass
    BBB
    Domperidone :not pass
    BBB
    4. Dopamine blockers
    Other antiemetics
    5.Neurokinin (NK1)-Receptor Antagonists.
    Aprepitant (orally) and fosaprepitant (infused intravenously)
    They block action of substance P in CTZ and NTS. They are highly effective in
    prevention of delayed emesis following moderately or highly emetogenic
    chemotherapy and increase the efficacy of standard antiemetic regimens (e.g.
    5-HT3 antagonist. They are well tolerated; flatulence can occur.

    6. Cannabinoids
    Dronabinol. It is either obtained from marijuana plant or synthesized and is
    used to prevent cancer chemotherapy–induced vomiting not responding to
    other antiemetics.
    It is effective orally. It produces serious side effects such as sedation, central
    sympathomimetic effects (tachycardia, palpitations and hypotension),
    hallucinations, disorientation and drug dependence – hence kept as a reserve
    antiemetic.
    Drugs affecting GIT motility
    Drugs affecting GIT motility
    • Drugs increase GIT
    motility
    • Upper GIT: prokinetic
    drugs
    • Lower GIT: laxatives

    • Drugs decrease GIT


    motility
    • Antispasmodics
    • Antidiarrheal drugs
    Part 2: PROKINETIC AGENTS

    Drugs that enhance gastroduodenal motility and hasten


    gastric emptying

    1. D2 antagonists
    • Metoclopramide, domperidone

    2. Others
    • 5HT4 receptors agonists : Cisapride, mosapride, itopride
    • Cholinomimetics:
    Direct :bethanechol
    Indirect :neostigmine
    • Motilin receptor agonist: erythromycin
    PROKINETIC AGENTS
    Dopamine antagonists
    Dopamine antagonists
    Dopamine antagonists
    Metoclopromide effects

    ➢ GIT: Metoclopramide promotes forward movement of contents of the


    upper GI tract—increases oesophageal and gastric peristalsis.

    ➢ It raises lower oesophageal sphincter pressure, speeds up gastric


    emptying and prevents the reflux of stomach contents into the
    oesophagus. It thus prevents reflux oesophagitis.

    ➢ CNS: Metoclopramide acts as an antiemetic by blocking the D2


    dopamine receptors on the CTZ. The effect on the gut, i.e. speeding up
    gastric emptying

    • But, Drug Insight: from disturbed motility to disordered


    movement
    Uses of metoclopromide
    1. As an antiemetic: Metoclopramide is effective for prevention and
    treatment of:
    (a) Disease-associated vomiting.
    (b) Drug-induced vomiting (not used to control levodopa-induced vomiting).
    (c) Postoperative vomiting.
    (d) Cancer chemotherapy-induced vomiting. It is used in combination with 5-
    HT antagonists/dexamethasone/promethazine/diazepam.
    3

    2. Gastroesophageal reflux disease (GERD): Metoclopramide produces


    symptomatic relief in patients with reflux oesophagitis by increasing the tone
    of LES. It is less effective than proton-pump inhibitors (PPIs) and H -blockers.
    2

    3. To alleviate symptoms associated with gastric stasis in patients with


    diabetes, postoperative or idiopathic gastroparesis

    4. To stimulate gastric emptying before general anaesthesia in emergency


    surgeries.
    Dopamine antagonists
    Domperidone
    • It blocks peripheral D2 receptors leading to ↓
    the inhibitory action of dopamine on GIT
    motility. is a preferred antiemetic in children,
    as it rarely produces EPS.

    • Is used to counteract nausea and vomiting


    caused by levodopa and during treatment of
    Parkinson’s disease??
    Dopamine antagonists
    Domperidone

    • It increases prolactin
    levels.

    • The important side


    effects are dryness of
    mouth, diarrhoea,
    headache, skin rashes,
    galactorrhoea and
    menstrual irregularities.
    Other prokinetic agents
    Cisapride, prokinetic agent, was banned because of its dangerous side effect
    ventricular fibrillation (torsades de pointes).

    Mosapride
    • The prokinetic effect is due to 5-HT4-agonism; also has weak 5-HT3
    antagonistic effect
    • Does not cause EPS, hyperprolactinaemia (no D2-blocking action)
    • May be useful in dyspepsia, diabetic gastroparesis, GERD
    • Side effects are dizziness, diarrhoea, headache, etc.; QT prolongation has
    been reported
    Other prokinetic agents

    Itopride
    • Prokinetic effect is due to
    D2-antagonism and
    anticholinesterase activity

    • Drug interactions are rare


    and does not cause EPS
    MCQ
    You want to prescribe a prokinetic drug to a 59-year-old
    woman who is having chronic indigestion due to
    diabetic gastroparesis.

    Which one of the following medications is most likely


    to precipitate extrapyramidal side-effects?
    A - Bethanechol
    B - Erythromycin
    C - Domperidone
    D - Cisapride
    E – Metoclopramide
    MCQ
    A 74-year-old man went on a cruise to celebrate his 50th
    wedding anniversary. Concerned about a history of motion
    sickness, the patient saw his primary care physician about a
    medication to take. He is now seen by the onboard physician
    with complaints of blurred vision, confusion, constipation, and
    urinary retention.
    Which of the following did the primary care physician
    likely prescribe?
    a. Scopolamine
    b. Metoclopramide
    c. Haloperidol
    d. Dronabinol
    e. Ondansetron

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