Granisetron

Indications

Granisetron is used for: Nausea and vomiting, Chemotherapy-induced nausea and vomiting, Post-operative nausea and vomiting

Adult Dose

Chemotherapy Induced Nausea & Vomiting Oral 1 mg PO 1 hr before chemotherapy, then 1 mg 12 hr after 1st dose; OR 2 mg 1 hr before chemotherapy IV 0.01 mg/kg/dose infused over 5 min or direct injected over 30 sec, 30 min before chemotherapy Radiation-Induced Nausea & Vomiting 2 mg PO, 1 hr before radiation treatment Postoperative Nausea & Vomiting Prevention: 1 mg (undiluted) IV push over 30 seconds; administer before anesthetic induction or immediately before reversal of anesthesia Treatment: 1 mg (undiluted) IV push over 30 seconds Elderly: Chemotherapy Induced Nausea & Vomiting Oral: 2 mg 1 hr before chemotherapy, then 1 mg 12 hr after 1st dose; OR 2 mg 1 hr before chemo IV: 0.01 mg/kg/dose infused over 5 min or direct injected over 30 sec, 30 min before chemotherapy Radiation-Induced Nausea & Vomiting 2 mg PO, 1 hr before radiation treatment Postoperative Nausea & Vomiting Prevention: 1 mg (undiluted) IV push over 30 seconds; administer before anesthetic induction or immediately before reversal of anesthesia Treatment: 1 mg (undiluted) IV push over 30 seconds Hepatic impairment No dosage adjustment required

Child Dose

Chemotherapy Induced Nausea & Vomiting <2 years: Safey and efficacy not established 2-16 years: As adults; 0.01 mg/kg infused over 5 min or direct inj over 30 sec, 30 min before chemotherapy Oral administration: Currently FDA-approved for IV administration in children; safety and efficacy of oral administration is not established Postoperative Nausea & Vomiting Safety and efficacy not established Not approved for postoperative N/V in pediatric patients because of lack of efficacy and QT prolongation observed in clinical trials

Renal Dose

Renal impairment IV Severe (CrCl <30 mL/min): Total clearance was not affected in patients with severe renal failure who received a single 40 mcg/kg IV dose PO No dosage adjustment required

Administration

May be taken with or without food. Take up to 1 hr before chemotherapy.

Contra Indications

Hypersensitivity.

Precautions

Subacute intestinal obstruction or ileus. Moderate to severe hepatic impairment. Congenital long QT syndrome or other risk factors for QT prolongation (e.g. electrolyte abnormalities and cumulative high-dose anthracycline therapy). Pregnancy, lactation. Lactation: excretion in milk unknown; use with caution

Pregnancy-Lactation

Pregnancy Category: B Lactation: excretion in milk unknown; use with caution

Interactions

Phenobarbital may induce metabolism of granisetron.

Adverse Effects

Side effects of Granisetron : >10% Headache (10-21%) 1-10% Diarrhea (1-9%), Constipation (3-18%), Asthenia (5%), Somnolence (10%), Sedation (10%), Drowsiness (10%) Frequency Not Defined Anxiety, Fatigue, Malaise, Increased LFTs

Mechanism of Action

Granisetron is a selective 5-HT3-receptor antagonist with little or no affinity for other serotonin receptors. It blocks serotonin in the chemoreceptor zone.