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Class: 5-HT3 Receptor Antagonists
Chemical Name: endo-1-Methyl-N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-1H-indazole-3-carboxamide monohydrochloride
Molecular Formula: C18H24N4O•ClH
CAS Number: 107007-99-8
Brands: Kytril

Medically reviewed by Last updated on Nov 25, 2020.


Antiemetic; selective inhibitor of type 3 serotonergic (5-HT3) receptors.1 2 3

Uses for Granisetron

Cancer Chemotherapy-induced Nausea and Vomiting

Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including high-dose cisplatin.1 33

For prevention of nausea and vomiting associated with highly emetogenic chemotherapy regimens (including an anthracycline plus cyclophosphamide), ASCO recommends a 3-drug antiemetic regimen consisting of an NK1 receptor antagonist (e.g., either oral aprepitant or IV fosaprepitant), a 5-HT3 receptor antagonist (e.g., dolasetron, granisetron, ondansetron, palonosetron), and dexamethasone.38 39 ASCO states that fixed-combination netupitant and palonosetron plus dexamethasone is an additional treatment option.39

For 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, use of any 5-HT3 receptor antagonist is appropriate.38

For chemotherapy regimens with a low emetogenic risk, ASCO recommends administration of a single dose of dexamethasone prior to chemotherapy.38

For chemotherapy regimens with minimal emetogenic risk, ASCO states that routine antiemetic administration is not necessary.38

Postoperative Nausea and Vomiting

Prevention and treatment of postoperative nausea and vomiting.1

Routine prophylaxis not recommended in patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively.1

Recommended for patients who, in the clinician’s judgment, must avoid nausea and/or vomiting postoperatively, even when anticipated incidence is low.1

Radiation-induced Nausea and Vomiting

Prevention of nausea and vomiting associated with radiation, including total body irradiation and daily fractionated abdominal radiation.33

Granisetron Dosage and Administration


Administer orally, by IV infusion, or by direct IV injection.1 33

Oral Administration

May use oral solution and tablets interchangeably.33

For prevention of nausea and vomiting associated with chemotherapy, administer once or twice daily.33 Administer only on days when emetogenic chemotherapy is administered.33

For prevention of radiation-induced nausea and vomiting, administer within 1 hour of radiation.33

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

For prevention of nausea and vomiting associated with chemotherapy, administer approximately 30 minutes before administration of emetogenic drug, only on days when emetogenic chemotherapy is administered.1

For prevention of postoperative nausea and vomiting, administer before induction of or immediately before reversal of anesthesia.1


IV infusion: Dilute in 5% dextrose or 0.9% sodium chloride injection1 to a total volume of 20–50 mL.HID

Rate of Administration

Direct IV injection: Administer undiluted over 30 seconds.1

IV infusion: Infuse over 5 minutes.1


Available as granisetron hydrochloride; dosage expressed in terms of granisetron.1 33

Pediatric Patients

Cancer Chemotherapy-induced Nausea and Vomiting

Children 2–16 years of age: 10 mcg/kg by IV infusion or direct IV injection within 30 minutes before administration of chemotherapy.1


Cancer Chemotherapy-induced Nausea and Vomiting

2 mg once daily up to 1 hour before administration of chemotherapy.33

Alternatively, 1 mg twice daily (first dose up to 1 hour before chemotherapy and second dose 12 hours after first dose).33


10 mcg/kg by IV infusion or direct IV injection within 30 minutes before administration of chemotherapy.1

Postoperative Nausea and Vomiting

1 mg as a single dose by direct IV injection before induction of or immediately before reversal of anesthesia.1


1 mg as a single dose by direct IV injection.1

Radiation-induced Nausea and Vomiting

2 mg once daily within 1 hour of radiation.33

Special Populations

Hepatic Impairment

No dosage adjustment required.1 33

Geriatric Patients

No dosage adjustment required.1 33

Cautions for Granisetron


  • Known hypersensitivity to granisetron or any ingredient in the formulation.1 33


Sensitivity Reactions

Hypersensitivity reactions, including anaphylactic reaction, shortness of breath, hypotension, and urticaria, reported rarely.1 33

Possible hypersensitivity reactions in patients who have exhibited hypersensitivity to other selective 5-HT3 receptor antagonists.1 33

General Precautions

GI Precautions

Does not stimulate gastric or intestinal peristalsis; do not use as a substitute for nasogastric suction.1

May mask progressive ileus and/or gastric distention when used in patients undergoing abdominal surgery or in those with chemotherapy-induced nausea and vomiting.1

Specific Populations


Category B.1 33


Not known whether granisetron is distributed into milk.1 33 Caution advised if used in nursing women.1 33

Pediatric Use

Safety and efficacy of IV granisetron for chemotherapy-induced nausea and vomiting not established in children <2 years of age; safety and efficacy of IV granisetron for prevention and treatment of postoperative nausea and vomiting not established in children of any age.1

Safety and efficacy of oral granisetron not established in children of any age.33

Geriatric Use

No substantial differences in safety and efficacy for chemotherapy-induced nausea and vomiting in geriatric patients relative to younger adults.1 33

Insufficient experience with IV granisetron for postoperative nausea and vomiting in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.1

Common Adverse Effects

Headache,1 33 constipation,1 33 pain,1 diarrhea,1 33 fever,1 abdominal pain,1 33 increased hepatic enzymes,1 33 asthenia,1 33 dyspepsia.33

Interactions for Granisetron

Apparently metabolized by CYP3A; does not induce or inhibit CYP isoenzymes.1 33

Drugs Affecting Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction (altered granisetron clearance and half-life) with inhibitors or inducers of CYP isoenzymes.1 33

Specific Drugs



Antineoplastic agents

No apparent interaction with emetogenic cancer chemotherapies1 33


Inhibition of granisetron metabolism in vitro33

Granisetron Pharmacokinetics



Dose of oral solution is bioequivalent to corresponding dose of oral tablets.33


Food has minimal effect on extent of absorption; may increase peak plasma concentration by 30%.33



Distributes freely between plasma and red blood cells.1 33 Not known whether granisetron distributed into milk.1 33

Plasma Protein Binding

Approximately 65%.1 33



Metabolized via N-demethylation and aromatic ring oxidation followed by conjugation; metabolism appears to be mediated by CYP3A subfamily.1 33

Elimination Route

Excreted in urine as unchanged drug (11–12%) and metabolites (48–49%) and in feces as metabolites (34–38%).1 33


IV administration: Terminal half-life is approximately 9 hours in adult cancer patients or adults undergoing surgery.1

Oral administration: Terminal half-life is approximately 6.2 hours in healthy adults.1

Special Populations

In pediatric cancer patients, pharmacokinetic profile is similar to that in adult cancer patients.1

In geriatric patients, mean clearance may be decreased and half-life increased compared with younger adults.1

In patients with hepatic impairment due to neoplastic liver involvement, total clearance following a single IV dose is reduced by approximately 50% compared with patients without hepatic impairment.1

In patients with severe renal impairment, total clearance following a single 40-mcg/kg IV dose is not altered.1





Tight container at 15–30°C; protect from light.33


Tight container at 25°C (may be exposed to 15–30°C).33 Store in upright position; protect from light.33



25°C (may be exposed to 15–30°C).1 Do not freeze; protect from light.1 Once multiple-dose vial is penetrated, use contents within 30 days.1

Following dilution with sodium chloride 0.9% or dextrose 5% injection, stable for at least 24 hours at room temperature under normal lighting conditions.1


For information on systemic interactions resulting from concomitant use, see Interactions.


Solution Compatibility


Dextrose 5% in sodium chloride 0.45 or 0.9%HID

Dextrose 5% in waterHID

Sodium chloride 0.9%HID

Drug Compatibility
Admixture CompatibilityHID


Dexamethasone sodium phosphate

Methylprednisolone sodium succinate

Y-Site CompatibilityHID


Allopurinol sodium


Amikacin sulfate


Amphotericin B cholesteryl sulfate complex

Ampicillin sodium

Ampicillin sodium–sulbactam sodium


Bleomycin sulfate


Buprenorphine HCl

Butorphanol tartrate

Calcium gluconate



Cefazolin sodium

Cefepime HCl

Cefotaxime sodium

Cefotetan disodium

Cefoxitin sodium

Ceftaroline fosamil


Ceftriaxone sodium

Cefuroxime sodium

Chlorpromazine HCl




Clindamycin phosphate






Daunorubicin HCl

Dexamethasone sodium phosphate

Dexmedetomidine HCl

Diphenhydramine HCl

Dobutamine HCl


Dopamine HCl


Doxorubicin HCl

Doxorubicin HCl liposome injection

Doxycycline hyclate




Etoposide phosphate


Fenoldopam mesylate




Fludarabine phosphate



Gallium nitrate

Ganciclovir sodium

Gemcitabine HCl

Gentamicin sulfate

Haloperidol lactate

Heparin sodium

Hetastarch in lactated electrolyte injection (Hextend)

Hydrocortisone sodium succinate

Hydromorphone HCl

Hydroxyzine HCl

Idarubicin HCl


Imipenem–cilastatin sodium

Leucovorin calcium



Magnesium sulfate

Mechlorethamine HCl

Melphalan HCl

Meperidine HCl


Methotrexate sodium

Methylprednisolone sodium succinate

Metoclopramide HCl



Mitoxantrone HCl

Morphine sulfate

Nalbuphine HCl



Pemetrexed disodium

Piperacillin sodium–tazobactam sodium

Potassium chloride

Prochlorperazine edisylate

Promethazine HCl


Ranitidine HCl


Sodium bicarbonate




Ticarcillin disodium–clavulanate potassium

Tobramycin sulfate

Topotecan HCl

Vancomycin HCl

Vinblastine sulfate

Vincristine sulfate

Vinorelbine tartrate



Amphotericin B


Acyclovir sodium


  • Antiemetic activity appears to be mediated both centrally (in medullary chemoreceptor trigger zone) and peripherally (in GI tract) via inhibition of 5-HT3 receptors.4 5 6 8 11 12 13 29 30

Advice to Patients

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1

  • Importance of advising patients of other important precautionary information.1 (See Cautions.)


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.

Granisetron Hydrochloride


Dosage Forms


Brand Names




1 mg (of granisetron) per 5 mL



Tablets, film-coated

1 mg (of granisetron)




Injection, for IV use

0.1 mg (of granisetron) per mL (0.1 mg)



1 mg (of granisetron) per mL (1 and 4 mg)



AHFS DI Essentials™. © Copyright 2021, Selected Revisions December 5, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.


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34. Spitzer TR, Friedman CJ, Bushnell W et al. Oral granisetron (Kytril) and ondansetron (Zofran) in the prevention of hyperfractionated total body irradiation induced emesis: the results of a double-blind, randomized parallel group study. Blood. 1998; 92(Suppl 1):278a.

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