Classifications: antiemetic; 5-ht3 antagonist; Therapeutic: antiemetic; 5-ht3 antagonist
Pregnancy Category: B
1 mg tablets; 1 mg/mL injection
Granisetron is a selective serotonin (5-HT3) receptor antagonist. Serotonin receptors of the 5-HT3 type are located centrally in the chemoreceptor trigger zone, and peripherally on the vagal nerve terminals. Serotonin
released from the wall of the small intestine stimulates the vagal afferent neurons through the serotonin (5-HT3) receptors, and initiates the vomiting reflex.
This selective serotonin (5-HT3) receptor antagonist is used for the prevention of nausea and vomiting associated with cancer chemotherapy.
Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose
cisplatin, postoperative nausea and vomiting.
Hypersensitivity to granisetron, or benzyl alcohol; GI obstruction; neonates; children less than 2 y.
Hypersensitivity to ondansetron or similar drugs; liver disease, pregnancy (category B), lactation.
Route & Dosage
|Chemotherapy-Related Nausea and Vomiting
Adult/Child: IV >2 y, 10 mcg/kg, beginning at least 30 min before initiation of chemotherapy (up to 40 mcg/kg per dose has been used) PO 1 mg b.i.d., start 1 mg up to 1 h prior to chemotherapy, then second tab 12 h later OR 2 mg q.d.
Postoperative Nausea and Vomiting
Adult: IV 1 mg before anesthesia induction or before reversal of anesthesia
PREPARE: Direct: Give undiluted. IV Infusion: Dilute in NS or D5W to a total volume of 2050 mL. Prepare infusion at time of administration; do not mix in solution
with other drugs.
ADMINISTER: Direct: Give a single dose over 30 sec. IV Infusion: Infuse diluted drug over 5 min or longer; complete infusion 2030 min prior to initiation of chemotherapy.
INCOMPATIBILITIES Y-site: Amphotericin B, doxorubicin.
- Store at 15°30° C (59°86° F) for 24 h after dilution under normal lighting conditions.
Adverse Effects (≥1%)CNS: Headache,
dizziness, somnolence, insomnia
, labile mood, anxiety, fatigue
. GI: Constipation
, elevated liver function tests.
may inhibit metabolism
Several minutes. Duration:
Approximately 24 h. Distribution:
Widely distributed in body tissues. Metabolism:
Appears to be metabolized in liver. Elimination:
Excreted in urine as metabolites. Half-Life:
1011 h in cancer
patients, 45 h in healthy volunteers.
Assessment & Drug Effects
- Monitor the frequency and severity of nausea and vomiting.
- Lab tests: Monitor liver function; elevated AST and ALT values usually normalize within 2 wk of last dose.
- Assess for headache, which usually responds to nonnarcotic analgesics.
Patient & Family Education
- Note: Headache requiring an analgesic for relief is a common adverse effect.
- Learn ways to manage constipation.