5-HT3 Receptor Antagonist

Aka: 5-HT3 Receptor Antagonist, 5-HT3 Antagonist, Serotonin 5-HT3 Receptor Antagonist

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II. Indications

  1. Chemotherapy associated Nausea
  2. Radiation Therapy associated Nausea
  3. Vomiting refractory to first-line Antiemetics
  4. Theophylline Overdose
    1. Used instead of Phenothiazines due to Seizure risk

III. Mechanism

  1. Blocks peripheral and central 5HT3 receptors
    1. Peripheral 5HT3 receptors at vagal nerve terminals
    2. Central 5HT3 receptors at ChemoreceptorTrigger Zone in Medulla (area postrema controls Vomiting)

IV. Contraindications

  1. QTc Prolongation
  2. First trimester pregnancy (Ondansetron)
    1. See Ondansetron
    2. Ondansetron has a relative contraindication based on preliminary data
    3. However it is also frequently used in Hyperemesis Gravidarum

V. Adverse Effects

  1. Mild Headache
  2. Dizziness
  3. Malaise or Fatigue
  4. Constipation
  5. QTc Prolongation (Ondansetron, Dolasetron)
    1. See Ondansetron
    2. Higher risk in higher doses, preexisting QTc Prolongation, CHF, Bradycardia, Hypomagnesemia, Hypokalemia
  6. Serotonin Syndrome
    1. http://www.fda.gov/Drugs/GuidanceComplianceRegulatoryInformation/Surveillance/AdverseDrugEffects/ucm351864.htm

VI. Dosing: Ondansetron (Zofran)

  1. See Ondansetron
  2. Adults
    1. Take 4 mg ODT tabs (typical acute care dosing)
  3. Children
    1. Exercise caution in age <6 months
    2. Weight 8-15 kg: Ondansetron 2 mg (half tab)
    3. Weight 15-30 kg: Ondansetron 4 mg (one tab)
    4. Weight >30 kg: Ondansetron 4 to 8 mg (one to two tabs)
    5. Freedman (2006) N Engl J Med 354:1698-705 [PubMed]

VII. Dosing: Dolasetron (Anzemet)

  1. See Dolasetron
  2. General
    1. Pregnancy Category B
  3. Nausea with Chemotherapy
    1. Adult 100 mg IV or orally given 60 minutes before Chemotherapy
    2. Child: 1.8 mg/kg for single dose up to 100 mg IV or orally given 60 minutes before Chemotherapy
  4. Prevention of Surgery Related Nausea
    1. Adult: 100 mg orally 2 hours before surgery
    2. Child: 1.2 mg/kg up to 100 mg orally 2 hours before surgery
  5. Surgery Related Nausea or Vomiting
    1. Given perioperatively for Nausea or Vomiting, or prophylactically 15 min before Anesthesia ends
    2. Adult: 12.5 mg IV for single dose
    3. Child: 0.35 mg/kg up to 12.5 mg IV for single dose
  6. Resources
    1. Dolasetron (DailyMed)
      1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=201b0eb8-4a1e-4e22-ab4b-addb642710d6

VIII. Dosing: Granisetron (Kytril, Sustol, Sancuso)

  1. See Granisetron
  2. General
    1. Pregnancy Category B
  3. Nausea with Chemotherapy
    1. Intravenous: 10 mcg/kg IV over 5 minutes given 30 minutes before Chemotherapy
    2. SQ (Sustol): 10 mg SQ given 30 min prior to Chemotherapy
    3. Oral: 2 mg orally once daily OR 1 mg orally twice daily given 1 hour before Chemotherapy
    4. Transdermal (Sancuso, 34 mg patch delivers 3.1 mg per 24 hours)
      1. Apply 1 patch to upper outer arm 24 to 48 hours before Chemotherapy
      2. Remove 24 hours after Chemotherapy (may use 1 patch continuously for up to 7 days)
      3. Avoid exposing patch to heat or sunlight
  4. Nausea with Radiation Therapy (adult)
    1. Dose: 2 mg orally 1 hour before each Radiation Therapy treatment
  5. Resources
    1. Granisetron (DailyMed)
      1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=02f350c9-b7d2-4906-af28-70ed4461ff23

IX. Dosing: Palonosetron (Aloxi)

  1. See Palonosetron
  2. General
    1. Palonosetron is also available combined with the NK1 Antagonist Netupitant (Akynzeo)
    2. Pregnancy Category B
  3. Indications: Preventing Chemotherapy indiuced Nausea
    1. Not effective in treating Nausea after it occurs
    2. Most effective in preventing delayed Emesis
      1. Longer Half-Life (>40 hours) and higher 5-HT affinity than other 5HT3 Antagonists
  4. Precautions
    1. Do NOT repeat dose more than once weekly
  5. Nausea with Chemotherapy
    1. Adult: 0.25 mg IV over 30 seconds, given 30 min before Chemotherapy
    2. Child: 20 mcg/kg up to 1.5 mg IV over 15 min, given 30 min before Chemotherapy
  6. Prevention of Surgery Related Nausea
    1. Give 0.075 mg IV over 10 seconds, before Anesthesia
  7. Resources
    1. Palonosetron (DailyMed)
      1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=bb20ba9b-aa8c-4b24-8124-aff0cb6c956b
  8. References
    1. (2004) Med Lett Drugs Ther 46(1179): 27-8 [PubMed]

X. References

  1. Johnson (1993) Harriet Lane, Mosby, p. 521
  2. (2002) Tarascon Pocket Pharmacopoeia, p. 67
  3. (1998) Med Lett Drugs Ther 40(1026): 53-4 [PubMed]
  4. (1991) Med Lett Drugs Ther 33(847): 63-4 [PubMed]
  5. Bell and Lovecchio (2016) Crit Dec Emerg Med 30(8): 28

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