Gastroenterology Book

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5-HT3 Receptor AntagonistAka: 5-HT3 Antagonist, Ondansetron, Zofran, Granisetron, Kytril, Dolasetron, Anzemet, Palonosetron, Aloxi

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  1. See Also
    1. Nausea in Cancer
  2. 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
  3. Adverse Effects
    1. Mild Headache
    2. Dizziness
    3. Constipation
  4. Dosing: Ondansetron (Zofran)
    1. Nausea with Chemotherapy
      1. Intravenous dosing
        1. Timing
          1. First dose: 30 minutes before Chemotherapy
          2. Subsequent dosing: 4 and 8 hours after first dose
        2. Adult: 32 mg IV over 15 min
        3. Child: 0.15 mg/kg IV over 15 min
      2. Oral dosing
        1. Over age 12 years: 8 mg PO bid
        2. Age 4 to 11 years: 4 mg PO tid
    2. Nausea with Radiation therapy (adult)
      1. Dose: 8 mg PO qid
    3. Surgery related Nausea (adult)
      1. Prevention: 16 mg PO 1 hour before surgery
      2. Treatment: 4 mg IV or IM over 2-5 minutes
      3. Efficacy
        1. Meta-analysis of 7 randomized trials, n=1043
        2. Works in only 25% of patients
        3. No more effective than less expensive drugs
        4. Tramer (1997) BMJ 314:1088
  5. Dosing: Dolasetron (Anzemet)
    1. Nausea with Chemotherapy
      1. Dose: 1.8 mg/kg IV or PO for single dose to 100 mg
    2. Prevention of Surgery related Nausea
      1. Adult: 100 mg PO 2 hours before surgery
      2. Child: 1.2 mg/kg PO 2 hours before surgery
    3. Surgery related Nausea
      1. Adult: 12.5 mg IV for single dose
      2. Child: 0.35 mg/kg IV for single dose
  6. Dosing: Granisetron (Kytril)
    1. Nausea with Chemotherapy (administer 30 minutes before)
      1. Intravenous: 10 ug/kg IV over 5 minutes
      2. Oral: 1 mg PO bid for 1 day
    2. Nausea with Radiation therapy (adult)
      1. Dose: 2 mg PO 1 hour before each irradiation
  7. Preparations: Palonosetron (Aloxi)
    1. 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 and higher 5-HT affinity
    2. Dosing: 25 mg IV 30 minutes before Chemotherapy
      1. Do not repeat dose more than once weekly
  8. 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. (1991) Med Lett Drugs Ther 33(847):63

Ondansetron (C0061851)

Definition (MSH)A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.
Definition (CSP)competitive serotonin type 3 receptor antagonist used in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs; also has anxiolytic and neuroleptic properties.
Definition (NCI)A drug that prevents or reduces nausea and vomiting. It belongs to the family of drugs called antiemetics.
Definition (PDQ)A carbazole derivative with antiemetic activity. As a selective serotonin receptor antagonist, ondansetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=40693&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=40693&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1119" NCI Thesaurus)
Definition (NCI)A carbazole derivative with antiemetic activity. As a selective serotonin receptor antagonist, ondansetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting. (NCI04)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishOndansetron, ONDANSETRON PREPARATION
Spanishondansetrón, ondansetron, ondansetrona
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Granisetron (C0061863)

Definition (MSH)A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.
Definition (NCI)A drug that prevents or reduces nausea and vomiting. It belongs to the family of drugs called antiemetics.
Definition (NCI)An indazole derivative with antiemetic properties. As a selective serotonin receptor antagonist, granisetron competitively blocks the action of serotonin at 5-hydroxytryptamine3 (5-HT3) receptors, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishGRAN, Granisetron, GRANISETRON PREPARATION, Granisetron product
Spanishgranisetrón, granisetron, granisetrona
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Kytril (C0107189)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishKytril
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Zofran (C0206046)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishZofran
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Dolasetron (C0209210)

Definition (NCI)An indole derivative and a potent serotonin 5-HT3 receptor antagonist with anti-emetic property. Dolasetron blocks the activity of serotonin released from the enterochromaffin cells of the small intestine by selectively inhibiting and inactivating 5-HT3 receptors located on the nerve terminals of the vagus nerve in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. This results in suppression of signalling to trigger chemo- and radiotherapy induced nausea and vomiting.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishDolasetron, DOLASETRON PREPARATION
Spanishdolasetrón, dolasetron, dolasetrona
CreditsDerived from the NIH UMLS (Unified Medical Language System)


palonosetron (C0220578)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englishpalonosetron
Spanishpalonosetrón, palonosetron
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Anzemet (C0718607)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishAnzemet
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Aloxi (C1310735)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishAloxi
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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