2Antiemetics.txt

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HUSOP2014
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132153
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2Antiemetics.txt
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2012-02-10 11:47:15
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HUSOP DA EXAM1 Anti Emetic
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Questions from the Anti emetic lecture
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  1. Name the protective reflex that serves to rid the stomach and intestine of toxic substances and prevent their further ingestion.
    Emesis
  2. What are the three phases of Vomiting?
    Pre-ejection phase (gastric relaxation & retroperistalsis), Retching (rhythmic action of respiratory muscles preceding vomiting and consisting of contraction of abdominal and intercostal muscles and diaphragm against a closed glottis), Ejection (intense contraction of the abdominal muscles and relaxation of the upper esophageal sphincter
  3. The process of Emesis appears to be coordinated by what two areas of the Brain?
    Vomiting center (VC), Solitary tract nucleus (STN) of the vagus nerve
  4. Where does the VC receive signals from what (5) things?
    Chemoreceptor trigger zone (CTZ) in the area postrema (AP) at the bottom of the fourth ventricle., Gastric irritation, Solitary Tract Nucleus (STN), Higher Centers (pain, sight, other sensory inputs), Inner Ear Vestibular Apparatus
  5. The chemoreceptor trigger zone has high concentration of which (4) receptors in regards to emesis?
    5-HT3, D2, M1, and NK1
  6. Toxic substances, Ketoacidosis, and Uremia send signals to which Emetic Center?
    CTZ
  7. Gastric irritation stimulate_________ and _________afferents.
    vagal and sympathetic
  8. Which receptor predominates in gastric irritation?
    5-HT3
  9. The Solitary tract nucleus (STN) is rich with which (5) different receptors?
    enkephalin, histamine (H1), Ach (M1), 5-HT3 and D2
  10. STN can receive signals from which (5) different means?
    CTZ, vagal & sympathetic afferents, glossopharyngeal & trigeminal afferents
  11. What are some of the higher centers that can trigger emesis?
    Pain, sights, smells, texture of foods, and other sensory inputs
  12. Which (2) receptors are located within the inner ear vestibular apparatus that can trigger emesis?
    M1 and H1
  13. True or False: Motion can trigger emesis but vertigo cannot.
    FALSE
  14. Name the (6) classes of antiemetics.
    5-HT3 antagonists, DA antagonists, H1 antagonists, M3 antagonists, CB1 agonists, NK1 antagonists
  15. True/False: Each class of antiemetic drugs can affect many different classes of receptors.
    TRUE
  16. True/False: All of 5-HT3 antagonists can be administered effectively just once a day.
    TRUE
  17. Name the four 5-HT3 receptor antagonist on the market.
    Ondansetron, Granisetron, Dolasetron, Palonosetron
  18. Which 5-HT3 antagonist has the longest half-life?
    Palonosetron
  19. Which 5-HT3 antagonist is the primary choice for chemotherapeutic-induced N/V?
    Palonosetron
  20. How is Ondansetron extensively metabolized?
    CYP1A2, CYP2D6, and CYP3A4, followed by glucuronide or sulfate conjugation.
  21. How is Granisetron metabolized?
    by CYP3A family
  22. Ketoconazole inhibits which enzyme?
    CYP3A
  23. Which enzyme converts Dolasetron to its active metabolite? Name the metabolite.
    plasma carbonyl reductase, hydrodolasetron
  24. A portion of hydrodolasetron is metabolized by which CYPs?
    CYP2D6 and CYP3A4
  25. Palonosetron is metabolized by which CYP?
    CYP2D
  26. Therapeutic uses of 5-HT3-Receptor Antagonists are?
    Chemotherapy-induced nausea
  27. The 5-HT3 antagonists, Dolasetron, has a FDA black box warning for?
    Torsades de pointes
  28. T/F: 5-HT3-Receptor Antagonists are effective in treating motion sickness.
    FALSE
  29. Common adverse effects of 5-HT3 antagonists are:
    Constipation or diarrhea, Headache, Light-headedness
  30. What are the primary uses for H1-receptor antagonists?
    motion sickness and postoperative emesis
  31. Where are H1 receptors s found?
    on vestibular afferents and within the brainstem
  32. Examples of H1 antagonists (4) are:
    Cyclizine, hydroxyzine, promethazine, diphenhydramine
  33. Which H1 antagonist has additional anticholinergic effects that may be useful for patients with abdominal cancer?
    Cyclizine
  34. The most commonly used muscarinic receptor antagonist for emesis is?
    scopolamine (hyoscine)
  35. Anticholinergic agents are useful in the treatment of?
    Motion sickness, Some activity in postoperative N/V, and Can be used in chemotherapy-induced nausea
  36. The (proposed) MOA of Dronabinol for emesis is?
    stimulation of the CB1 receptors on neurons in and around the vomiting center
  37. T/F: Dronabinol is a highly lipid-soluble and is absorbed readily after oral administration.
    TRUE
  38. Dronabinol is metabolized by which CYP(s)? Name its active metabolite
    CYP2C19 and CYP3A4, 11-OH-delta-9-tetrahydrocannabinol
  39. Dronabinol stimulates appetite and is used in patients with?
    AIDS & anorexia
  40. Adverse effects of Dronabinol are?
    Central sympathomimetic activity: Palpitations, tachycardia, vasodilation, hypotension, Conjunctival injection, Euphoria, somnolence, detachment, dizziness, anxiety, nervousness, panic, paranoid reactions, etc.
  41. Abrupt withdrawal symptoms of Dronabinol include:
    Irritability, insomnia, restlessness
  42. Why can Dexamethasone or NSAIDS be useful adjuncts in the treatment of nausea in cancer patients?
    Possibly by suppressing peritumoral inflammation and prostaglandin production.
  43. Which effects of Lorazepam & alprazolam can be helpful in reducing the anticipatory component of nausea and vomiting?
    sedative, amnesic, and anti-anxiety effects
  44. Substance P is in vagal afferent fibers innervating which (4) areas?
    STN and area postrema
  45. Name the (2) NK1 receptors antagonists.
    aprepitant (EMEND), casopitant
  46. Where are NK1 receptors s found?
    STN and area posterma
  47. What are the effects of NK1 antagonists in patients receiving multiple cycles of chemotherapy?
    Delayed nausea and improve the efficacy of standard antiemetic regimens
  48. Aprepiant is metabolized by which CYP? Plasma protein bound %? T1/2 is?
    CYP3A4, 95%, 9-13 hrs.
  49. Indications for Aprepiant are?
    nausea & vomiting associated with cisplatin
  50. Adverse effects & Interactions of Aprepiant are?
    potential to interact with other substrates of CYP3A4, i.e. dexamethasone, methylprednisolone and warfarin
  51. Which drug is contraindicated with aprepiant? Why?
    cisapride, causes a prolonged QT interval
  52. What are the effects of Dopamine Receptor Antagonists that help with emesis?
    Increase GI motility, Increase lower esophageal sphincter and intragastric pressures, Increases Ach release from myenteric motor neurons (D2 mediated), and they are prokinetic drugs
  53. How do DA antagonists relieve N/V (MOA)?
    blocking D2 in CTZ
  54. Name the (2) DA antagonists from Lecture.
    Metoclopamide (Reglan), Domperidone
  55. MOA of Metoclopramide (Reglan)
    D2 receptor antagonist, 5-HT4 receptor agonist, 5-HT3 receptor antagonist (both vagal and central)
  56. what are the effects of Metoclopramide (Reglan)?
    confined largely to the upper digestive tract, Increases lower esophageal sphincter tone, Stimulates antral and small intestinal contractions, No effect on large-bowel motility
  57. Pharmacokinetics of Metoclopramide, T1/2, Onset, duration, metabolized, excreted.
    4-6 hours, 30 to 60 min, 1-2 hours, sufation and glucuroide conjugation, in the urine
  58. Therapeutic Uses of Metoclopramide (Reglan)
    Prevention of chemotherapy-induced emesis, Relief symptom associated with GERD, Treatment of gastroparesis (delayed gastric emptying), Adjunctive measure in medical or diagnostic procedures such as intestinal intubation or contrast radiography of the GI tract (as injection).
  59. Adverse effects & Interactions of Metoclopramide (Reglan)
    CNS side effects: Extrapyramidal effects, Parkinsonian-like symptoms, Tardive dyskinesia, Dystonia, Galactorrhea
  60. MOA of Domperidone (Motilium)
    D2 receptor antagonist
  61. T/F: both Metoclopramide and domperidone cross the BBB.
    False: domperidone does not
  62. side Effect of Domperidone (Molilim)
    elevates serum prolactin levels
  63. T/F: Metoclopramide has greater lower GI effects than Domperidone.
    True: Domperidone does not have significant Lower GI motility

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