Note: Granisol oral solution has been discontinued in the United States for more than 1 year.
Prevention of chemotherapy-associated nausea and vomiting: Manufacturer’s labeling:
Oral: 2 mg once daily up to 1 hour before chemotherapy or 1 mg twice daily; the first 1 mg dose should be administered up to 1 hour before chemotherapy (with the second 1 mg dose 12 hours later). Administer only on the day(s) chemotherapy is administered.
IV: 10 mcg/kg within 30 minutes prior to chemotherapy; only on the day(s) chemotherapy is administered.
SUBQ (ER injection): Moderately emetogenic chemotherapy or anthracycline/cyclophosphamide chemotherapy: 10 mg at least 30 minutes prior to chemotherapy on day 1 (in combination with IV dexamethasone on day 1 and [for anthracycline/cyclophosphamide chemotherapy] oral dexamethasone on days 2 to 4); do not administer more frequently than once every 7 days. May also be administered in combination with a neurokinin 1 (NK1) receptor antagonist antiemetic regimen.
Transdermal patch: Prophylaxis of chemotherapy-related emesis: Apply 1 patch at least 24 hours prior to chemotherapy; may be applied up to 48 hours before chemotherapy. Remove patch a minimum of 24 hours after chemotherapy completion. Maximum duration: Patch may be worn up to 7 days, depending on chemotherapy regimen duration.
Guideline recommendations:
Highly emetogenic chemotherapy (>90% risk of emesis [eg, cisplatin, breast cancer regimens that include an anthracycline combined with cyclophosphamide]) (ASCO [Hesketh 2020]; MASCC/ESMO [Roila 2016]):
Day of chemotherapy: Administer prior to chemotherapy and in combination with an NK1 receptor antagonist, dexamethasone, and olanzapine.
IV: 1 mg or 10 mcg/kg as a single dose.
Oral: 2 mg as a single dose.
SUBQ: 10 mg as a single dose.
Transdermal: Apply 1 patch.
Postchemotherapy days: 5-HT3 receptor antagonist use is not necessary (other components of the antiemetic regimen are administered) (ASCO [Hesketh 2020]).
Moderately emetogenic chemotherapy (30% to 90% risk of emesis): Carboplatin-based regimens (carboplatin AUC ≥4) (ASCO [Hesketh 2020]; MASCC/ESMO [Roila 2016]):
Day of chemotherapy: Administer prior to chemotherapy and in combination with an NK1 receptor antagonist and dexamethasone.
IV: 1 mg or 10 mcg/kg as a single dose.
Oral: 2 mg as a single dose.
SUBQ: 10 mg as a single dose.
Transdermal: Apply 1 patch.
Postchemotherapy days: 5-HT3 receptor antagonist use is not necessary (other components of the antiemetic regimen may be administered).
Moderately emetogenic chemotherapy (30% to 90% risk of emesis): Non–carboplatin-based regimens or carboplatin AUC <4) (alternative agent) (ASCO [Hesketh 2020]; MASCC/ESMO [Roila 2016]):
Note: Guidelines do not state a preference for which 5-HT3 receptor antagonist should be used in this setting; however, palonosetron may be preferred (Celio 2015; Popovic 2014).
Day of chemotherapy: Administer prior to chemotherapy and in combination with dexamethasone.
IV: 1 mg or 10 mcg/kg as a single dose.
Oral: 2 mg as a single dose.
SUBQ: 10 mg as a single dose.
Transdermal: Apply 1 patch.
Postchemotherapy days: 5-HT3 receptor antagonist use is not necessary (other components of the antiemetic regimen may be administered).
Low emetogenic risk (10% to 30% risk of emesis) (ASCO [Hesketh 2020]; MASCC/ESMO [Roila 2016]):
Note: Single-agent granisetron is an option for prophylaxis.
Day of chemotherapy:
IV: 1 mg or 10 mcg/kg as a single dose.
Oral: 2 mg as a single dose.
SUBQ: 10 mg as a single dose
Transdermal: Apply 1 patch.
Postchemotherapy days: Prophylaxis is not necessary on subsequent days.
Minimal emetogenic risk (<10% risk of emesis): Routine antiemetic prophylaxis is not generally necessary (ASCO [Hesketh 2020]).
Chemotherapy-induced nausea and vomiting, prevention: High-dose chemotherapy with stem or bone marrow transplant (ASCO [Hesketh 2020]):
Day of chemotherapy: Administer prior to chemotherapy and in combination with an NK1 receptor antagonist, dexamethasone, ± olanzapine.
IV: 1 mg or 10 mcg/kg as a single dose.
Oral: 2 mg as a single dose.
SUBQ: 10 mg as a single dose.
Transdermal: Apply 1 patch.
Prophylaxis of radiation therapy-associated emesis:
High-emetogenic risk radiation therapy (total body irradiation):
Radiation day(s):
IV (off label): 1 mg or 10 mcg/kg once daily prior to each fraction of radiation; administer in combination with dexamethasone (ASCO [Hesketh 2020]).
Oral: 2 mg once daily administered 1 to 2 hours prior to each fraction of radiation; administer in combination with dexamethasone (ASCO [Hesketh 2020]).
Postradiation days:
IV (off label), Oral: The appropriate duration of therapy following radiotherapy days is not well defined; ASCO guidelines recommend continuing granisetron once daily on the day after each day of radiation (ASCO [Hesketh 2020]).
Moderate-emetogenic risk radiation therapy (upper abdomen, craniospinal irradiation):
Radiation day(s):
IV (off label): 1 mg or 10 mcg/kg once daily prior to each fraction of radiation; may administer with or without dexamethasone before the first 5 fractions (ASCO [Hesketh 2020]).
Oral: 2 mg once daily administered 1 to 2 hours prior to each fraction of radiation; may administer with or without dexamethasone before the first 5 fractions (ASCO [Hesketh 2020]).
Low-emetogenic (brain, head and neck, thorax, pelvis) or minimal-emetogenic (extremities, breast) risk radiation therapy: Routine prophylaxis not recommended; however, for radiation therapy to the head and neck, thorax, or pelvis, or for minimal emetogenic risk radiation therapy, may use as rescue therapy (ASCO [Hesketh 2020]).
IV (off label): 1 mg or 10 mcg/kg (ASCO [Hesketh 2020]).
Oral: 2 mg (ASCO [Hesketh 2020]).
Prevention of postoperative nausea and vomiting (off-label use): IV: 0.35 to 3 mg (5 to 20 mcg/kg) administered at the end of surgery (SAA [Gan 2014]).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
IV, Oral, Transdermal: No dosage adjustment necessary.
SUBQ (ER injection):
CrCl ≥60 mL/minute: No dosage adjustment necessary.
CrCl 30 to 59 mL/minute: 10 mg on day 1 of chemotherapy; do not administer more frequently than once every 14 days.
CrCl <30 mL/minute: Avoid use.
Total clearance may be reduced by ~50% in patients with hepatic impairment. However, inter-subject variability limits interpretation of kinetic studies.
IV, Oral, Transdermal: No dose adjustment necessary (standard doses are well tolerated).
SubQ (ER injection): There is no dosage adjustment provided in the manufacturer’s labeling.
(For additional information see "Granisetron: Pediatric drug information")
Note: Granisol oral solution has been discontinued in the US for more than 1 year.
Chemotherapy-induced nausea and vomiting (CINV), prevention: Pediatric Oncology Group of Ontario (POGO) guidelines (POGO [Dupuis 2013]; POGO [Patel 2017]): Note: POGO guidelines do not recommend a maximum dose as most studies did not cap the dose (POGO [Dupuis 2013])
Highly-emetogenic chemotherapy:
Infants <6 months: IV: 40 mcg/kg as a single daily dose prior to chemotherapy; used in combination with dexamethasone
Infants ≥6 months, Children, and Adolescents: IV: 40 mcg/kg as a single daily dose prior to chemotherapy; used in combination with dexamethasone and aprepitant (if no known or suspected drug interactions)
Moderately-emetogenic chemotherapy: Infants, Children, and Adolescents:
IV: 40 mcg/kg as a single daily dose prior to chemotherapy; used in combination with dexamethasone. For patients ≥6 months of age who cannot receive dexamethasone, use granisetron in combination with aprepitant (if no known or suspected drug interactions).
Oral: 40 mcg/kg/dose every 12 hours; used in combination with dexamethasone on chemotherapy days. For patients ≥6 months of age who cannot receive dexamethasone, use granisetron in combination with aprepitant (if no known or suspected drug interactions).
Low-emetogenic chemotherapy: Infants, Children, and Adolescents:
IV: 40 mcg/kg as a single daily dose prior to chemotherapy
Oral: 40 mcg/kg/dose every 12 hours on chemotherapy days
Postoperative nausea and vomiting, prevention: Limited data available: Children and Adolescents: IV: 40 mcg/kg as a single dose; maximum dose: 0.6 mg/dose (Gan 2014); ideal administration time in pediatric patients is not defined; in adults, administration is recommended at the end of surgery; in a granisetron pediatric PONV trial, doses were administered before the surgical incision (Cieslak 1996; SAA [Gan 2014]). Note: QT prolongation has been observed at this dose in pediatric patients 2 to 16 years of age; monitor closely.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Children ≥2 years and Adolescents: No dosage adjustment necessary
Children ≥2 years and Adolescents: Pharmacokinetic studies in patients with hepatic impairment showed that total clearance was approximately halved; however, standard doses were very well tolerated, and dose adjustments are not necessary.
Refer to adult dosing.
Serotonin syndrome: If serotonin syndrome occurs, discontinue 5-HT3 receptor antagonist treatment and begin supportive management.
Transdermal patch: Skin reaction, severe or generalized (allergic rash, including erythematous, macular, or papular rash or pruritus): Remove patch.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Patch, Transdermal:
Sancuso: 3.1 mg/24 hr (1 ea)
Prefilled Syringe, Subcutaneous:
Sustol: 10 mg/0.4 mL (0.4 mL) [contains polyethylene glycol (macrogol)]
Solution, Intravenous:
Generic: 1 mg/mL (1 mL); 4 mg/4 mL (4 mL)
Solution, Intravenous [preservative free]:
Generic: 0.1 mg/mL (1 mL [DSC]); 1 mg/mL (1 mL)
Tablet, Oral:
Generic: 1 mg
May be product dependent
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Intravenous:
Generic: 1 mg/mL (1 mL, 4 mL)
Tablet, Oral:
Generic: 1 mg
Granisol oral solution has been discontinued in the US for more than 1 year.
An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:
Sustol: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022445s000lbl.pdf
Oral: Doses should be administered up to 1 hour prior to initiation of chemotherapy/radiation.
IV: Administer IV push over 30 seconds or as a 5-minute infusion.
SUBQ (ER injection): For SUBQ administration only. Administer as a single injection at the back of the upper arm or in abdomen (at least 1 inch away from the umbilicus). Avoid using areas where the skin is burned, hardened, inflamed, swollen, or otherwise compromised. Inject slowly; may take up to 20 to 30 seconds (product is viscous, pressing the syringe plunger will not result in faster expulsion). A topical anesthetic may be applied at injection site prior to administration. Do not administer if particulate matter or discoloration is observed, if the tip cap is missing or has been tampered with, or the luer fitting is missing or dislodged. Remove from refrigerator at least 60 minutes prior to administration; remove from pack and activate 1 syringe warming pouch and wrap syringe with warming pouch for 5 to 6 minutes to allow warming to body temperature. Injection site reactions may occur; if injection site reaction is not yet resolved prior to the next dose, rotate injection site with next administration.
Transdermal (Sancuso): Apply patch by pressing down firmly to clean, dry, nearly hairless, intact skin on upper outer arm; smooth down with fingers. Wash hands thoroughly after applying. Do not shave hair where applying; clip hair as close to the skin as possible. Do not use on red, irritated, or damaged skin. Do not apply to skin where creams, oils, lotions, powders, or other skin products have been applied; may prevent patch from adhering properly. Remove patch from pouch immediately before application. Do not cut patch. Cover patch application site with clothing to protect from natural or artificial sunlight exposure while patch is applied and for 10 days following removal; granisetron may potentially be affected by natural or artificial sunlight. Do not apply heat (eg, heating pad, heating lamp) over or in area of the transdermal patch; avoid prolonged exposure to heat (may increase plasma concentrations). Do not apply more than 1 patch at a time. Surgical or medical adhesive tape may be applied to lifted edges of patch to keep in place; do not completely cover patch or wrap tape around arm. Contact with water while bathing or showering will not affect patch; however, avoid swimming, saunas, hot tubs, and strenuous exercise. Dispose of any used or unused patches by folding adhesive ends together and discard properly in trash away from children and pets.
Oral: Given at least 1 hour prior to chemotherapy and repeated in 12 hours
Parenteral: IV: Infuse over 30 seconds undiluted or dilute in small volume NS or D5W and administer over 5 minutes; infusions administered over 30 to 60 minutes have also been reported (Komada 1999; Miyajima 1994; Wada 2001)
Chemotherapy-associated nausea and vomiting: Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic chemotherapy, including high-dose cisplatin (injection and tablets); prevention of nausea and vomiting associated with anthracycline/cyclophosphamide chemotherapy regimens; prevention of nausea and vomiting associated with moderately and/or highly emetogenic chemotherapy regimens of up to 5 consecutive days of duration (transdermal).
Radiation-associated nausea and vomiting: Prevention of nausea and vomiting associated with radiation therapy, including total body radiation and fractionated abdominal radiation (tablets).
Prevention of postoperative nausea and vomiting
Granisetron may be confused with dolasetron, ondansetron, palonosetron
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported incidences for adverse reactions are for the oral dosage form unless otherwise indicated.
>10%:
Gastrointestinal: Constipation (IV, oral, transdermal: 3% to 22%; including fecal impaction), nausea (20%), vomiting (12%)
Local: Injection site reaction (IV: 37% to 62%; including bleeding at injection site [2% to 4%], bruising at injection site [≤45%], erythema at injection site [11% to 17%], hematoma at injection site [≤45%], induration at injection site ≤10%], injection-site infection ≤1%], injection-site nodule [≤18%], injection-site pruritus [≤2%], injection-site scarring [≤2%], irritation at injection site [≤2%], lipohypertrophy at injection site [≤2%], localized vesiculation [≤2%], pain at injection site [3% to 20%], paresthesia [injection site: ≤2%], rash at injection site [≤2%], residual mass at injection site [≤18%], skin discoloration at injection site [≤2%], swelling at injection site [≤10%], tenderness at injection site [4% to 27%], warm sensation at injection site [≤2%])
Nervous system: Asthenia (IV: 2% to 5%; oral: 14% to 18%), fatigue (IV: 11% to 21%), headache (IV, oral: 9% to 21%; transdermal: 1%)
1% to 10%:
Cardiovascular: Atrial fibrillation (IV: <3%), flushing (IV: <3%), hypertension (IV, oral: 1% to 2%), prolonged QT interval on ECG (IV, oral, transdermal: 1% to 3%; >450 milliseconds), syncope (IV: <3%)
Dermatologic: Alopecia (3%), skin rash (IV: 1%)
Gastrointestinal: Abdominal pain (IV, oral: 4% to 7%), decreased appetite (6%), diarrhea (IV, oral: 4% to 9%), dysgeusia (IV: 2%), dyspepsia (IV, oral: 3% to 6%), gastroesophageal reflux disease (IV: 1% to 5%), pancreatitis (IV: <3%)
Hematologic & oncologic: Anemia (4%), leukopenia (9%), thrombocytopenia (2%)
Hepatic: Increased serum alanine aminotransferase (IV, oral: >2 x ULN: 3% to 6%), increased serum aspartate aminotransferase (IV, oral: >2 x ULN: 3% to 5%)
Hypersensitivity: Hypersensitivity reaction (including anaphylaxis; IV: <3%)
Nervous system: Agitation (IV: <2%), anxiety (IV, oral: ≤2%), central nervous system stimulation (IV: <2%), dizziness (IV, oral: 3% to 5%), drowsiness (IV, oral: ≤4%), insomnia (IV, oral: 4% to 5%)
Miscellaneous: Fever (IV, oral: 3% to 9%)
Frequency not defined (any route of administration): Cardiovascular: Angina pectoris, atrioventricular block, cardiac arrhythmia, ECG abnormality, hypotension, sinus bradycardia, ventricular ectopy (includes nonsustained ventricular tachycardia)
Postmarketing (any route of administration):
Cardiovascular: Asystole (Al Harbi 2016), bradycardia (Al Harbi 2016), chest pain, palpitations, sick sinus syndrome
Local: Application-site reaction (transdermal: application-site burning, application-site erythema, application-site irritation, application-site pain, application-site pruritus, application-site rash, application-site vesicles, skin discoloration [application-site], urticaria [application site])
Hypersensitivity to granisetron or any component of the formulation or to other 5-HT3 receptor antagonists.
Canadian labeling: Additional contraindications (not in the US labeling): Concomitant use with apomorphine.
Concerns related to adverse effects:
• ECG effects: Selective 5-HT3 antagonists, including granisetron, have been associated with dose-dependent increases in ECG intervals (eg, PR, QRS duration, QT/QTc, JT), usually occurring with IV formulations (compared to oral) and occurring 1 to 2 hours after IV administration. In general, these changes are not clinically relevant; however, when used in conjunction with other agents that prolong these intervals (eg, Class I and III antiarrhythmics), arrhythmia or clinically relevant QT interval prolongation may occur resulting in torsade de pointes. Use with caution in patients at risk of QT prolongation and/or ventricular arrhythmia; patients with cardiac disease, electrolyte abnormalities, or who are receiving concomitant cardiotoxic chemotherapy are at higher risk.
• GI effects: Constipation may occur with all formulations, although a higher incidence is observed with tablets and the ER SUBQ injection. Hospitalization due to constipation or fecal impaction has been reported with the ER SUBQ injection. Progressive ileus and/or gastric distention may be masked by the ER SUBQ injection and transdermal patch (assess risks/benefits in patients with recent abdominal surgery). Granisetron does not stimulate gastric or intestinal peristalsis; do not use it in place of nasogastric suction.
• Hypersensitivity: Hypersensitivity reactions (including anaphylaxis) have been reported with granisetron in patients who have experienced hypersensitivity to other 5-HT3 antagonists (cross-reactivity has been reported). Due to the ER properties of the SUBQ formulation, granisetron exposure may continue for 5 to 7 days following administration; hypersensitivity reactions may occur up to 7 days or longer following administration and may have an extended course.
• Injection site reactions: Injection site reactions are associated with the subcutaneous ER formulation. Injection site infections have been reported (median onset: 9 days); infections were managed with antibiotics and completely resolved. Bruising and/or hematomas occur in over one-third of patients (median onset: 2 days); may be delayed (~5 days or later following administration). Severe bruising has also been reported. Patients receiving anticoagulant or antiplatelet medications are at higher risk for severe bruising/hematoma at the injection site (consider risk/benefit in these patients). Injection site bleeding has also been observed, occasionally lasting >5 days. Injection site pain/tenderness was commonly reported, usually lasting 5 to 7 days. Pain/tenderness interfered with activity or caused significant discomfort at rest (rare); some patients required pain medications. Injection site nodules occurred in less than one-fifth of patients, usually persisting for 15 to 21 days. If injection site reaction is not yet resolved prior to the next dose, rotate injection site with next administration.
• Serotonin syndrome: Serotonin syndrome (SS) has been reported with 5-HT3 receptor antagonists, predominantly when used in combination with other serotonergic agents (eg, selective serotonin reuptake inhibitors, serotonin and norepinephrine reuptake inhibitors, monoamine oxidase inhibitors, mirtazapine, fentanyl, lithium, tramadol, methylene blue). Some of the cases have been fatal. The majority of SS reports due to 5-HT3 receptor antagonist have occurred in a postanesthesia setting or in an infusion center. SS has also been reported following overdose of another 5-HT3 receptor antagonist. Signs of SS include mental status changes (eg, agitation, hallucinations, delirium, coma); autonomic instability (eg, tachycardia, labile BP, diaphoresis, dizziness, flushing, hyperthermia); neuromuscular changes (eg, tremor, rigidity, myoclonus, hyperreflexia, incoordination); GI symptoms (eg, nausea, vomiting, diarrhea); and/or seizures.
Disease-related concerns:
• Long QT syndrome: Use with caution in patients with congenital long QT syndrome or other risk factors for QT prolongation (eg, medications known to prolong QT interval, electrolyte abnormalities [hypokalemia or hypomagnesemia], cumulative high-dose anthracycline therapy).
Dosage form specific issues:
• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggest that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.
• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer’s labeling.
• Transdermal patch: Application-site reactions have occurred with use; local reactions were generally mild and did not require discontinuation. Granisetron patch may potentially be affected by natural or artificial sunlight.
Other warnings/precautions:
• Chemotherapy-associated emesis: Antiemetics are most effective when used prophylactically (MASCC/ESMO [Roila 2016]). If emesis occurs despite optimal antiemetic prophylaxis, reevaluate emetic risk, disease status, concurrent morbidities and current medications to assure antiemetic regimen is optimized (ASCO [Hesketh 2020]).
Substrate of CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Apomorphine: Antiemetics (5HT3 Antagonists) may enhance the hypotensive effect of Apomorphine. Risk X: Avoid combination
Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy
Panobinostat: Granisetron may enhance the arrhythmogenic effect of Panobinostat. Risk C: Monitor therapy
QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy
Serotonergic Agents (High Risk): Antiemetics (5HT3 Antagonists) may enhance the serotonergic effect of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
TraMADol: Antiemetics (5HT3 Antagonists) may enhance the serotonergic effect of TraMADol. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
Adverse events have not been observed in animal reproduction studies. In an ex vivo placental perfusion study, granisetron was shown to cross the placenta in a concentration (dose) dependent manner (Julius 2014). Initial studies note the pharmacokinetics of the transdermal system may be different in pregnant women. A relationship between granisetron plasma concentrations and relief of symptoms of nausea and vomiting of pregnancy was also observed (Caritis 2016). Some dosage forms (injection) may contain benzyl alcohol.
It is not known if granisetron is excreted in breast milk. According to the manufacturer, the decision to continue or discontinue breast-feeding during therapy should take into account the risk of infant exposure, the benefits of breast-feeding to the infant, benefits of treatment to the mother, and the underlying maternal condition.
Monitor for development of constipation and for decreased bowel activity (particularly in patients at risk for GI obstruction). Monitor for signs/symptoms of hypersensitivity. Monitor for signs of serotonin syndrome.
ER SUBQ injection: Monitor for injection site reactions for at least 2 weeks after administration.
Selective 5-HT3-receptor antagonist, blocking serotonin, both peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone
Onset of action: IV: 1 to 3 minutes
Duration: Oral, IV: Generally up to 24 hours; SUBQ (extended release): Remains detectable in the plasma for 7 days
Absorption: Oral: Tablets and oral solution are bioequivalent; Transdermal patch: ~66% over 7 days
Distribution: Vd: 2 to 4 L/kg; widely throughout body
Protein binding: ~65%
Metabolism: Hepatic via CYP1A1 and CYP3A4 N-demethylation, oxidation, and conjugation; some metabolites may have 5-HT3 antagonist activity
Half-life elimination: Oral: 6 hours; IV: Mean range: 5 to 9 hours; SUBQ (extended release): ~24 hours
Time to peak, plasma: Transdermal patch: Maximum systemic concentrations: ~48 hours after application (range: 24 to 168 hours); SUBQ (extended release): ~24 hours
Excretion: Urine (11% to 12% as unchanged drug, 48% to 49% as metabolites); feces (34% to 38% as metabolites)
Hepatic function impairment: Total clearance is decreased by about 50% in patients with hepatic impairment (due to neoplastic disease) compared to patients with normal hepatic function.
Older adult: Mean values were lower for Cl and longer for half-life.
Sex: Men had a higher Cmax, but there was no difference in AUC.
Patch (Sancuso Transdermal)
3.1 mg/24 hrs (per each): $772.26
Prefilled Syringe (Sustol Subcutaneous)
10 mg/0.4 mL (per 0.4 mL): $838.80
Solution (Granisetron HCl Intravenous)
1 mg/mL (per mL): $10.80 - $24.00
4 mg/4 mL (per mL): $7.50 - $19.80
Tablets (Granisetron HCl Oral)
1 mg (per each): $59.01 - $59.05
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