ATC Class:A04AA02
Granisetron hydrochloride, a selective, first-generation inhibitor of type 3 serotonergic (5-HT3) receptors, is an antiemetic.1, 36, 38
Granisetron hydrochloride is used orally or IV for the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy.1, 33, 36 The drug also is used orally for the prevention of radiation-induced nausea and vomiting.33 In addition, granisetron hydrochloride is used IV for the prevention and treatment of postoperative nausea and vomiting.1
Cancer Chemotherapy-induced Nausea and Vomiting
Granisetron is used IV for the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including high-dose cisplatin therapy, in adults and children 2-16 years of age.1, 36 Granisetron is used orally in adults for the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including high-dose cisplatin therapy.33 The drug has been used effectively for the prevention of chemotherapy-induced emesis in patients receiving cisplatin alone or in combination with other antineoplastic agents.1, 6, 8, 9, 10, 18, 19, 20, 21, 22
To prevent chemotherapy-induced nausea and vomiting associated with highly emetogenic chemotherapy regimens (including an anthracycline plus cyclophosphamide), the American Society of Clinical Oncology (ASCO) currently recommends a 3-drug antiemetic regimen consisting of a neurokinin-1 (NK1) receptor antagonist (e.g., either oral aprepitant or IV fosaprepitant dimeglumine), a type 3 serotonin (5-HT3) receptor antagonist (e.g., dolasetron, granisetron, ondansetron, palonosetron, ramosetron [not commercially available in the US], tropisetron [not commercially available in the US]), and dexamethasone.38, 39 ASCO states that the oral, fixed-combination of netupitant and palonosetron plus dexamethasone is an additional antiemetic treatment option in this setting.39
For patients receiving moderately emetogenic chemotherapy regimens, ASCO recommends a 2-drug antiemetic regimen preferably consisting of palonosetron and dexamethasone.38, 39 If palonosetron is not available, a first-generation 5-HT3 receptor antagonist (preferably granisetron or ondansetron) may be substituted.38 Limited evidence suggests that aprepitant may be added to this regimen; in such cases, ASCO states that any of the 5-HT3 receptor antagonists is appropriate.38
For patients receiving chemotherapy regimens with a low emetogenic risk , ASCO recommends administration of a single dose of dexamethasone prior to chemotherapy.38
In patients receiving chemotherapy regimens with a minimal emetogenic risk , antiemetics should not be routinely administered prior to or following chemotherapy.38
Radiation-induced Nausea and Vomiting
Granisetron is used orally for the prevention of radiation-induced nausea and vomiting in adults.33, 34, 35 The drug has been used effectively to prevent nausea and vomiting in patients receiving total body irradiation or daily fractionated radiation to the abdomen.33, 34, 35
Postoperative Nausea and Vomiting
Granisetron is used IV for the prevention and treatment of postoperative nausea and vomiting.1 The drug has been used effectively to prevent nausea and vomiting in surgical patients in whom nausea and vomiting must be avoided postoperatively and to treat patients who have developed postoperative nausea and/or vomiting.1 The manufacturer states that as with other antiemetics, routine prophylaxis with granisetron is not recommended in patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively.1 However, use of the drug is recommended for patients in whom nausea and/or vomiting must be avoided postoperatively, even when the anticipated incidence of such nausea and/or vomiting is low.1
Reconstitution and Administration
Granisetron hydrochloride is administered orally, by IV infusion, or by direct IV injection.1, 33 For IV infusion, the drug should be diluted in 5% dextrose or 0.9% sodium chloride injection to a total volume of 20-50 mL and infused IV over 5 minutes.1 For direct IV injection, the drug is administered undiluted over 30 seconds.1
The manufacturer states that safety and efficacy of IV granisetron for cancer chemotherapy-induced nausea and vomiting in children younger than 2 years of age have not been established.1 Safety and efficacy of IV granisetron for the prevention and treatment of postoperative nausea and vomiting, and safety and efficacy of oral granisetron have not been established in children of any age.1, 33
Dosage of granisetron, which is available for oral or IV use as the hydrochloride, is expressed in terms of granisetron.1, 33
The manufacturer states that a dose of granisetron oral solution is bioequivalent to the corresponding dose of the oral tablets, and the dosage forms may be used interchangeably.33
The manufacturer states that dosage modification in geriatric patients is not necessary.37
Cancer Chemotherapy-induced Nausea and Vomiting
For the prevention of cancer chemotherapy-induced emesis in adults and children 2-16 years of age, 10 mcg/kg of granisetron is given as a 5-minute IV infusion or direct IV injection within 30 minutes before administration of an emetogenic drug.1 If the drug is administered orally, the usual adult dosage is 1 mg twice daily, or, alternatively, 2 mg once daily.33 When the twice-daily dosing regimen is used, the first dose (1 mg) is given up to 1 hour before chemotherapy and the second dose (1 mg) is given 12 hours after the first dose.33 When the once-daily dosing regimen is used, 2 mg is given up to 1 hour before chemotherapy.33 Oral or IV granisetron is administered only on the days when emetogenic chemotherapy is administered.1, 33 The manufacturer states that continued granisetron therapy while patients are not receiving emetogenic chemotherapy has not been found to be useful.33
Radiation-induced Nausea and Vomiting
For the prevention of radiation-induced nausea and vomiting in adults undergoing total body irradiation or daily fractionated radiation to the abdomen, the usual oral dosage of granisetron is 2 mg once daily.33 Patients should receive oral granisetron within 1 hour of radiation.33 The manufacturer states that there is no experience with use of oral granisetron for the prevention of radiation-induced nausea and vomiting in children.33
Postoperative Nausea and Vomiting
For the prevention of postoperative nausea and vomiting in adults, a single granisetron IV dose of 1 mg is given undiluted over 30 seconds before induction of anesthesia or immediately before reversal of anesthesia.1 For the treatment of postoperative nausea and vomiting in adults, 1 mg of undiluted granisetron injection is administered IV over 30 seconds.1 The manufacturer states that clinical studies of granisetron for postoperative nausea and vomiting did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger patients;1 however, other clinical experience has not revealed age-related differences in response.1
Dosage in Renal and Hepatic Impairment
The manufacturer states that dosage modification is not necessary when granisetron is used in patients with renal or hepatic impairment.1, 33
Granisetron hydrochloride, a selective inhibitor of type 3 serotonergic (5-HT3) receptors, is an antiemetic.1, 36 The drug is structurally and pharmacologically related to ondansetron.2, 3 The antiemetic activity of granisetron appears to be mediated both centrally and peripherally via inhibition of 5-HT3 receptors.4, 5, 6, 8, 11, 12, 13, 29, 30 Current evidence indicates that 5-HT3 receptors play a major role in acute emesis, but only a minor role in delayed nausea and vomiting.4, 5, 6, 8, 11, 12, 13, 29, 30
The role of serotonin as a mediator of acute chemotherapy (e.g., cisplatin)-induced emesis has been strongly suggested by the temporal relationship between the emetogenic action of such drugs and the release (e.g., from GI enterochromaffin cells) of serotonin (e.g., as reflected by increases in plasma and urine concentrations of the serotonin metabolite 5-hydroxyindoleacetic acid [5-HIAA]) as well as by the clinical efficacy of antiemetic agents that act as inhibitors of 5-HT3 receptors (e.g., granisetron, metoclopramide, ondansetron).4, 5, 6, 7, 8, 9, 10, 11, 29 Studies in animals have shown that such chemotherapy-induced emesis can be prevented completely by ablation of the area postrema (the locus of the chemoreceptor trigger zone [CTZ]) or depletion of serotonin from this area; in addition, high levels of 5-HT3 receptors have been demonstrated in this area, and direct injection of 5-HT3 receptor antagonists into the area postrema also can prevent such chemotherapy-induced emesis.6, 29 Therefore, current evidence suggests that the emetogenic action of such chemotherapy may be initiated by degenerative changes in the GI tract (e.g., small intestine) induced by these drugs and associated increases in endogenous serotonin release; serotonin then stimulates vagal and splanchnic nerve receptors that project to the medullary vomiting (emetic) center of the brain and also appears to stimulate 5-HT3 receptors in the area postrema.4, 5, 6, 11, 29 Thus, 5-HT3 receptor antagonists appear to prevent or ameliorate acute chemotherapy-induced emesis by inhibiting visceral (from the GI tract) afferent stimulation of the emetic center probably indirectly at the level of the area postrema and by directly inhibiting serotonin activity within the area postrema and CTZ.4, 5, 6, 11, 29
Alternative mechanisms appear to be principally responsible for delayed nausea and vomiting induced by such chemotherapy (e.g., cisplatin), since similar temporal relationships between serotonin and emesis beyond the first day after a dose have not been established, and inhibitors of 5-HT3 receptors do not appear to be effective alone in preventing or ameliorating delayed effects.4, 5, 8, 11, 12, 13
Additional Information
SumMon® (see Users Guide). For additional information on this drug until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the labeling be consulted for detailed information on the usual cautions, precautions, and contraindications.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions December 5, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
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