Pharm

Antiemetic

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Antiemetic, Anti-emetic, Phenothiazine Antiemetic, Benzamide Antiemetic

  • Mechanism
  1. Nausea and Vomiting is mediated via the physiologic Vomiting center in the Medulla
  2. Stimulation of Vomiting center via three pathways
    1. Vestibular fibers (e.g. Vertigo)
    2. Afferent visceral fibers (e.g. gastrointestinal)
    3. Fourth Ventricle (Chemoreceptor Trigger Zone)
  1. Indications
    1. Preferred first-line Antiemetic in U.S. in most cases
    2. Severe Nausea and Vomiting
    3. Chemotherapy-Induced (See Nausea in Cancer)
  2. Agents
    1. Ondansetron (Zofran)
    2. Granisetron (Kytril)
    3. Dolasetron (Anzemet)
    4. Palonosetron (Aloxi)
  3. Adverse effects
    1. Asthenia
    2. Dizziness
    3. Constipation
    4. QT Prolongation (see Ondansetron)
    5. Serotonin Syndrome
    6. Use in pregnancy may be associated with increased risk of Congenital Heart Defect and Cleft Palate
      1. (2014) Presc Lett 21(1): 5
  • Preparations
  • Phenothiazines
  • Preparations
  • Substituted benzamides
  1. Indications
    1. Diabetic Gastroparesis
    2. Migraine Headaches
  2. Agents
    1. Metoclopramide (Reglan)
    2. Trimethobenzamide (Tigan)
  3. Adverse effects
    1. Extrapyramidal Side Effects
  • Preparations
  • Butyrophenones
  1. Agents
    1. Droperidol (Inapsine)
      1. Use limited due to potential for Prolonged QT
      2. Generally unavailable in U.S. since 2012
    2. Haloperidol (Haldol)
  2. Indications
    1. Chemotherapy-Induced (See Nausea in Cancer)
    2. Postoperative Nausea (See Nausea After Surgery)
  3. Adverse Effects
    1. Sedation
    2. Agitation or restlessness
  1. Agents
    1. Dimenhydrinate (Dramamine)
    2. Meclizine (Antivert)
    3. Scopolamine (Transdermal)
  2. Indications
    1. Vertigo
    2. Motion Sickness
  3. Adverse Effects (Anticholinergic effects)
    1. Sedation
    2. Constipation
    3. Dry Mouth
    4. Urinary Retention
  • Preparations
  • Adjunctive and atypical Antiemetics
  • Preparations
  • Brief list of some options for Adults
  1. Prochlorperazine (Compazine)
    1. Other Routes: 5-10 mg PO/IM/IV every 6-8 hours prn
    2. Rectal: 25 mg PR g12h
  2. Metoclopramide (Reglan)
    1. Dose: 10 mg PO/IM/IV every 6 hours prn or 1 hour before meals and qhs
  3. Promethazine (Phenergan)
    1. Dose: 12.5 mg IV or 25 mg PO/IM/PR q4-6h
  4. Ondansetron (Zofran)
    1. Dose: 4 mg (0.15mg/kg) IV (or PO) over 15 min q4h prn