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granisetron (Kytril, Sancuso)

Tradename: Kytril. Indications: 1) prophylaxis & treatment of chemotherapy-related emesis a) patients refractory to standard anti-emetic regimens b) young persons (< 45 years of age) who are more likely to develop extrapyramidal reactions to high-dose metoclopramide 2) nausea/vomiting Contraindications: Caution: use wiuth caution in patients with liver disease Dosage: 1) 10 ug/kg IV over 5 min, 30 min prior to chemotherapy 2) 1 mg PO BID Tabs: 1 mg. Injection: 1 mg/mL (1 mL) Transdermal patch: (Sancuso) Adverse effects: 1) common (> 10%) - headache 2) less common (1-10%) - hypertension, hypotension, dizziness, insomnia, anxiety, constipation, abdominal pain, diarrhea, weakness 3) uncommon (< 1%) - arrhythmias, somnolence, agitation, hot flashes, abnormal liver function tests Mechanism of action: 1) acts to prevent nausea, not in the rescue of nausea 2) 5-hydroxytryptamine-3 (5HT-3) receptor antagonist [3]

General

anti-emetic serotonin antagonist

Properties

INHIBITS: serotonin [5HT]-3 receptor MISC-INFO: elimination route LIVER pregnancy-category B safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Bruera & Neumann Canadian Medical Assoc. J (CAMJ):158:1717 1998