Antiemetic

Aka: Antiemetic, Anti-emetic, Phenothiazine Antiemetic, Benzamide Antiemetic

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II. 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)

III. Preparations: 5-HT3 Receptor Antagonist

  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

IV. Preparations: Phenothiazines

  1. Indications
    1. Migraine Headaches
    2. Motion Sickness or Vertigo
    3. Chemotherapy-Induced (See Nausea in Cancer)
    4. Postoperative Nausea (See Nausea After Surgery)
    5. Severe Nausea and Vomiting
  2. Agents
    1. Prochlorperazine (Compazine)
    2. Promethazine (Phenergan)
  3. Adverse effects
    1. Extrapyramidal Side Effects (e.g. Dystonic Reaction)

V. 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

VI. 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

VII. Preparations: Antihistamines

  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

VIII. Preparations: Adjunctive and atypical Antiemetics

  1. Dexamethasone
    1. Chemotherapy-Induced (See Nausea in Cancer)
  2. Cannabinoids (Dronabinol)
    1. Chemotherapy-Induced (See Nausea in Cancer)
  3. Benzodiazepines (Lorazepam, Diazepam, Clonazepam)
    1. Chemotherapy-Induced (See Nausea in Cancer)
    2. Not generally recommended

IX. 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

X. References

  1. Flake (2015) Am Fam Physician 91(5): 293-6 [PubMed]

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Ontology: Antiemetics (C0003297)

Definition (MSH) Drugs used to prevent NAUSEA or VOMITING.
Definition (NCI_NCI-GLOSS) A drug that prevents or reduces nausea and vomiting.
Definition (NCI) Drugs used to prevent nausea or vomiting. Antiemetics act by a wide range of mechanisms. Some act on the medullary control centers (the vomiting center and the chemoreceptive trigger zone) while others affect the peripheral receptors. (MeSH)
Definition (CSP) drugs used to prevent nausea or vomiting; act by a wide range of mechanisms; some act on the medullary control centers while others effect the peripheral receptors.
Concepts Pharmacologic Substance (T121)
MSH D000932
SnomedCT 372764000, 52017007
English Antiemetic Drugs, Drugs, Antiemetic, Agents, Antiemetic, Antiemetic Agents, ANTIEMETICS, [GA605] ANTIEMETICS, Anti-emetic, Anti-emetic Agent, Anti-emetic Agent [TC], Antiemetic Agent, anti-emetic agents, antiemetic drugs, antiemetic agents, antiemetics, antiemetic drug, antiemetic, antinauseant drugs, Antiemetic, Antiemetic (product), Antiemetic (substance), Antiemetic, NOS, Anti emetics, Anti-emetics, Antinauseant Drugs, Antiemetics
French Agents antiémétiques, Anti-émétiques, Médicaments antiémétiques, Médicaments antivomitifs, Antiémétisants, Agents antivomitifs, Anti-vomitifs, Antiémétiques, Antivomitifs
Swedish Antiemetika
Czech antiemetika
Finnish Antiemeetit
Italian Sostanze antiemetiche, Farmaci antiemetici, Antiemetici
Russian PROTIVORVOTNYE SREDSTVA, ПРОТИВОРВОТНЫЕ СРЕДСТВА
Japanese 制吐剤, 制吐薬, 鎮吐剤, 鎮吐薬
Polish Leki przeciwwymiotne
Spanish Efecto Antiemético, Antiemético, antiemético (producto), antiemético (sustancia), antiemético, Antieméticos
Portuguese Efeito Antiemético, Antiemético, Antieméticos
German Antiemetika
Derived from the NIH UMLS (Unified Medical Language System)

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