SANCUSO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SANCUSO (SANCUSO).
Granisetron is a selective 5-HT3 receptor antagonist. It blocks serotonin binding at 5-HT3 receptors in the chemoreceptor trigger zone (CTZ) of the area postrema and on peripheral vagal nerve terminals, thereby inhibiting the vomiting reflex.
| Metabolism | Primarily hepatic via CYP3A4 (major), also CYP1A2 and CYP2D6 (minor). |
| Excretion | Approximately 95% of the dose is metabolized, with <5% excreted unchanged in urine. Metabolites are eliminated primarily via feces (about 70%) and urine (about 25%). |
| Half-life | Terminal elimination half-life is approximately 25 hours following transdermal application. This long half-life supports the 72-hour dosing interval of the transdermal patch. |
| Protein binding | Granisetron is approximately 65% bound to plasma proteins, primarily albumin and α1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 3 L/kg. This high Vd indicates extensive tissue distribution, consistent with its lipophilic nature and ability to cross the blood-brain barrier. |
| Bioavailability | Following transdermal administration, absolute bioavailability is approximately 65% compared to intravenous administration. The transdermal system provides continuous drug delivery over 72 hours. |
| Onset of Action | Following transdermal application, therapeutic plasma concentrations are achieved within 6–8 hours. Maximum concentration is reached at approximately 48 hours. |
| Duration of Action | The transdermal patch provides continuous controlled release for up to 72 hours (3 days). Clinical efficacy is maintained for the 3-day wear period. |
3.1 mg patch applied to upper outer arm every 24 hours; applied 24-48 hours before chemotherapy and left on for 24 hours after chemotherapy completion.
| Dosage form | FILM, EXTENDED RELEASE |
| Renal impairment | No dosage adjustment required for GFR ≥30 mL/min. For GFR <30 mL/min or on hemodialysis: use alternative therapy due to limited data. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: consider alternative; Child-Pugh C: avoid use (no data). |
| Pediatric use | 1.24 mg patch (1/2 of adult dose) for weight 40-60 kg; 3.1 mg patch for weight >60 kg. Applied to upper outer arm per standard schedule for chemotherapy-induced nausea and vomiting. |
| Geriatric use | No specific adjustment recommended; monitor for electrolyte disturbances, QT prolongation, and skin irritation due to potential age-related changes in skin barrier and renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SANCUSO (SANCUSO).
| Breastfeeding | Granisetron is excreted into human breast milk in low amounts. The milk-to-plasma ratio is not established. While it is generally considered compatible with breastfeeding due to low oral bioavailability, caution is advised. Use only if clearly needed. |
| Teratogenic Risk | Granisetron is classified as FDA Pregnancy Category B. Animal studies have not demonstrated fetal harm, but adequate and well-controlled studies in pregnant women are lacking. No specific fetal risks have been identified across trimesters; however, use during the first trimester should be avoided unless clearly needed due to theoretical risks. During the second and third trimesters, no specific risks are documented. |
■ FDA Black Box Warning
No black box warning.
| Serious Effects |
["Hypersensitivity to granisetron or any component of the formulation."]
| Precautions | ["Hypersensitivity reactions including anaphylaxis and urticaria have been reported.","Serotonin syndrome has been reported with 5-HT3 receptor antagonists alone, but particularly with concomitant use of serotonergic drugs.","Granisetron may mask progressive ileus and/or gastric distension caused by the underlying condition (e.g., bowel obstruction)."] |
Loading safety data…
| Fetal Monitoring | No specific monitoring is required. Standard obstetrical monitoring is recommended. In cases of severe nausea and vomiting, assess maternal hydration and electrolyte status. |
| Fertility Effects | Granisetron has no known adverse effects on fertility based on animal studies. No human data are available. |