Gastroenterology Book

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5-HT3 Receptor Antagonist

Aka: 5-HT3 Receptor Antagonist, 5-HT3 Antagonist, Ondansetron, Zofran, Granisetron, Kytril, Dolasetron, Anzemet, Palonosetron, Aloxi
  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 (ODT)
        1. Over age 12 years: 8 mg PO twice daily
        2. Age 4 to 11 years: 4 mg PO three times daily
        3. Age under 4 years: 0.15 mg/kg/dose
    2. Nausea with Radiation Therapy (adult)
      1. Dose: 8 mg PO four times daily
    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 314:1088-93
  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
    4. (1991) Med Lett Drugs Ther 33(847): 63-4

Ondansetron (C0061851)

Definition (NCI) The active ingredient in a drug used to treat nausea and vomiting caused by cancer treatment. Ondansetron is a type of serotonin receptor antagonist and a type of antiemetic.
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 (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)
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 (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)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D017294
SnomedCT 108418007, 372487007
English 4H-Carbazol-4-one, 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)methyl)-, ondansetron, ondansetron (medication), ONDANSETRON, Ondansetron [Chemical/Ingredient], Ondansetron, Ondansetron (product), Ondansetron (substance)
Swedish Ondansetron
Czech ondansetron
Finnish Ondansetroni
Russian ONDANSETRON, ОНДАНСЕТРОН
Japanese オンダンセトロン
Croatian ONDANSETRON
Spanish ondansetrona, ondansetrón (producto), ondansetrona (producto), ondansetrona (sustancia), ondansetrón (sustancia), ondansetrón, Ondansetron, Ondansetrón
Polish Ondansetron
French Ondansétron
German Ondansetron
Italian Ondansetrone
Portuguese Ondansetron
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Granisetron (C0061863)

Definition (NCI) The active ingredient in a drug used to treat nausea and vomiting caused by cancer treatment. Granisetron is a type of serotonin receptor antagonist and a type of antiemetic.
Definition (MSH) A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.
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.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D017829
SnomedCT 108424001, 372489005
English 1H-Indazole-3-carboxamide, 1-methyl-N-(9-methyl-9-azabicyclo(3.3.1)non-3-yl)-, endo-, GRANISETRON, granisetron, 1-Methyl-N-(9-methyl-endo-9-azabicyclo(3.3.1)non-3-yl)-1H-indazole-3-carboxamide, Granisetron [Chemical/Ingredient], Granisetron Transdermal System, 1-Methyl-N-(endo-9-Methyl-9-Azabicyclo(3.3.1)non-3-yl)-1H-Indazole-3-Carboxamide, Granisetron product, Granisetron (product), Granisetron (substance), GRAN, Granisetron
Swedish Granisetron
Czech granisetron
Finnish Granisetroni
Russian GRANISETRON, ГРАНИСЕТРОН
Japanese グラニセトロン
Spanish granisetrón (producto), granisetrona (producto), granisetrona, granisetrona (sustancia), granisetrón (sustancia), granisetrón, Granisetron, Granisetrón
Polish Granisetron
French Granisétron
German Granisetron
Italian Granisetrone
Portuguese Granisetron
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Zofran (C0206046)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D017294
English zofran, Zofran
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Kytril (C0107189)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D017829
English kytril, Kytril
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Anzemet (C0718607)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C060344
English Anzemet, anzemet
Sources
Derived from the NIH UMLS (Unified Medical Language System)


palonosetron (C0220578)

Definition (NCI) The active ingredient in a drug used to treat nausea and vomiting caused by cancer treatment. Palonosetron is a type of serotonin receptor antagonist and a type of antiemetic.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C083418
SnomedCT 404851001, 404852008
English 2-QHBIQO, 2-(1-azabicyclo(2.2.2)oct-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benz(de)isoquinolin-1-one, palonosetron [Chemical/Ingredient], palonosetron, Palonosetron (product), Palonosetron (substance), Palonosetron, PALONOSETRON
Spanish palonosetrón (sustancia), palonosetron (sustancia), palonosetron, palonosetrón (producto), palonosetrón
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Dolasetron (C0209210)

Definition (NCI) The active ingredient in a drug used to treat nausea and vomiting caused by cancer treatment. Dolasetron is a type of serotonin receptor antagonist and a type of antiemetic.
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.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C060344
SnomedCT 108421009, 372488002
English octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl 1H-indole-3-carboxylate, DOLASETRON, Dolasetron, Dolasetron (product), Dolasetron (substance), dolasetron
Spanish dolasetrón (producto), dolasetrona, dolasetrona (producto), dolasetrona (sustancia), dolasetrón (sustancia), dolasetrón
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Aloxi (C1310735)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C083418
English Aloxi, aloxy, aloxi
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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