II. Indications
- Chemotherapy associated Nausea
- Radiation Therapy associated Nausea
- Vomiting refractory to first-line Antiemetics
-
Theophylline
Overdose
- Used instead of Phenothiazines due to Seizure risk
III. Mechanism
- Blocks peripheral and central 5HT3 receptors
- Peripheral 5HT3 receptors at vagal nerve terminals
- Central 5HT3 receptors at ChemoreceptorTrigger Zone in Medulla (area postrema controls Vomiting)
IV. Contraindications
- QTc Prolongation
- First trimester pregnancy (Ondansetron)
- See Ondansetron
- Ondansetron has a relative contraindication based on preliminary data
- However it is also frequently used in Hyperemesis Gravidarum
V. Adverse Effects
- Mild Headache
- Dizziness
- Malaise or Fatigue
- Constipation
-
QTc Prolongation (Ondansetron, Dolasetron)
- See Ondansetron
- Higher risk in higher doses, preexisting QTc Prolongation, CHF, Bradycardia, Hypomagnesemia, Hypokalemia
- Serotonin Syndrome
VI. Dosing: Ondansetron (Zofran)
- See Ondansetron
- Adults
- Take 4 mg ODT tabs (typical acute care dosing)
- Children
- Exercise caution in age <6 months
- Weight 8-15 kg: Ondansetron 2 mg (half tab)
- Weight 15-30 kg: Ondansetron 4 mg (one tab)
- Weight >30 kg: Ondansetron 4 to 8 mg (one to two tabs)
- Freedman (2006) N Engl J Med 354:1698-705 [PubMed]
VII. Dosing: Dolasetron (Anzemet)
- See Dolasetron
-
General
- Pregnancy Category B
-
Nausea with Chemotherapy
- Adult 100 mg IV or orally given 60 minutes before Chemotherapy
- Child: 1.8 mg/kg for single dose up to 100 mg IV or orally given 60 minutes before Chemotherapy
- Prevention of Surgery Related Nausea
- Adult: 100 mg orally 2 hours before surgery
- Child: 1.2 mg/kg up to 100 mg orally 2 hours before surgery
- Surgery Related Nausea or Vomiting
- Given perioperatively for Nausea or Vomiting, or prophylactically 15 min before Anesthesia ends
- Adult: 12.5 mg IV for single dose
- Child: 0.35 mg/kg up to 12.5 mg IV for single dose
- Resources
VIII. Dosing: Granisetron (Kytril, Sustol, Sancuso)
- See Granisetron
-
General
- Pregnancy Category B
-
Nausea with Chemotherapy
- Intravenous: 10 mcg/kg IV over 5 minutes given 30 minutes before Chemotherapy
- SQ (Sustol): 10 mg SQ given 30 min prior to Chemotherapy
- Oral: 2 mg orally once daily OR 1 mg orally twice daily given 1 hour before Chemotherapy
- Transdermal (Sancuso, 34 mg patch delivers 3.1 mg per 24 hours)
- Apply 1 patch to upper outer arm 24 to 48 hours before Chemotherapy
- Remove 24 hours after Chemotherapy (may use 1 patch continuously for up to 7 days)
- Avoid exposing patch to heat or sunlight
-
Nausea with Radiation Therapy (adult)
- Dose: 2 mg orally 1 hour before each Radiation Therapy treatment
- Resources
IX. Dosing: Palonosetron (Aloxi)
- See Palonosetron
-
General
- Palonosetron is also available combined with the NK1 Antagonist Netupitant (Akynzeo)
- Pregnancy Category B
- Indications: Preventing Chemotherapy indiuced Nausea
- Not effective in treating Nausea after it occurs
- Most effective in preventing delayed Emesis
- Longer Half-Life (>40 hours) and higher 5-HT affinity than other 5HT3 Antagonists
- Precautions
- Do NOT repeat dose more than once weekly
-
Nausea with Chemotherapy
- Adult: 0.25 mg IV over 30 seconds, given 30 min before Chemotherapy
- Child: 20 mcg/kg up to 1.5 mg IV over 15 min, given 30 min before Chemotherapy
- Prevention of Surgery Related Nausea
- Give 0.075 mg IV over 10 seconds, before Anesthesia
- Resources
- References
X. References
- Johnson (1993) Harriet Lane, Mosby, p. 521
- (2002) Tarascon Pocket Pharmacopoeia, p. 67
- (1998) Med Lett Drugs Ther 40(1026): 53-4 [PubMed]
- (1991) Med Lett Drugs Ther 33(847): 63-4 [PubMed]
- Bell and Lovecchio (2016) Crit Dec Emerg Med 30(8): 28
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Definition (MSH) | Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS. |
Concepts | Pharmacologic Substance (T121) |
MSH | D058831 |
English | 5-HT3 Antagonist, Antagonist, 5-HT3, Antagonists, 5-HT3, Serotonin 5-HT3 Receptor Antagonists, Serotonin 5 HT3 Receptor Antagonists, 5-HT3 Antagonists, 5 HT3 Antagonists, 5 HT3 Antagonist |
French | Antagonistes des récepteurs 5-HT3 de la sérotonine, Antagonistes 5-HT3 |
German | 5-HT3-Antagonisten, 5-HT3-Antagonist, Serotonin-5-HT3-Rezeptorantagonisten |
Czech | serotoninové 5-HT3 receptory - antagonisté, serotoninové receptory 5-HT3 - antagonisté, 5-HT3 antagonisté |
Spanish | Antagonistas del Receptor de Serotonina 5-HT3 |
Russian | СЕРОТОНИНА 5-HT3 РЕЦЕПТОРОВ АНТАГОНИСТЫ, SEROTONINA 5-HT3 RETSEPTOROV ANTAGONISTY |
Portuguese | Antagonistas do Receptor 5-HT3 de Serotonina |
Polish | Antagoniści receptora serotoninowego 5-HT3 |
Italian | Antagonisti dei recettori della serotonina 5-HT3 |