granisetron (Kytril, Sancuso)

Introduction

Tradename: Kytril.

Indications

• prophylaxis & treatment of chemotherapy-related emesis
  • patients refractory to standard anti-emetic regimens
  • young persons (< 45 years of age) who are more likely to develop extrapyramidal reactions to high-dose metoclopramide
• nausea/vomiting

Contraindications

Caution: use wiuth caution in patients with liver disease

pregnancy category = b

safety in lactation = ?

Dosage

• 10 ug/kg IV over 5 min, 30 min prior to chemotherapy
• 1 mg PO BID

Tabs: 1 mg.

Injection: 1 mg/mL (1 mL)

Transdermal patch: (Sancuso)

Adverse effects

• common (> 10%)
  • headache
• less common (1-10%)
  • hypertension, hypotension, dizziness, insomnia, anxiety, constipation, abdominal pain, diarrhea, weakness
• uncommon (< 1%)
  • arrhythmias, somnolence, agitation, hot flashes, abnormal liver function tests

Mechanism of action

• acts to prevent nausea, not in the rescue of nausea
• 5-hydroxytryptamine-3 (5HT-3) receptor antagonist

More general terms

• serotonin antagonist
• anti-emetic

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3510
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5284566
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=65264