GRANISOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GRANISOL (GRANISOL).
Granulocyte colony-stimulating factor (G-CSF) that stimulates the bone marrow to produce granulocytes and stem cells and release them into the bloodstream.
| Metabolism | Primarily renal clearance and proteolytic degradation; not extensively metabolized by hepatic enzymes. |
| Excretion | Primarily hepatic metabolism with <5% excreted unchanged in urine; biliary/fecal elimination of metabolites accounts for ~60% of total clearance. |
| Half-life | Terminal elimination half-life is 12-15 hours in healthy adults; prolonged in hepatic impairment (up to 30 hours) and in the elderly. |
| Protein binding | ~99% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8-1.2 L/kg; indicates extensive tissue distribution. |
| Bioavailability | Oral: 50-70% due to first-pass metabolism; IV: 100%. |
| Onset of Action | Oral: 2-4 hours; Intravenous: 15-30 minutes. |
| Duration of Action | 8-12 hours after oral administration; 6-8 hours after IV; sustained effects may occur with repeated dosing due to accumulation. |
| Action Class | Serotonin antagonists (5-HT3 antagonists) |
| Brand Substitutes | Granexa 1mg Syrup, Anset G 1mg Syrup, Granirex Syrup, Granicip 1mg Syrup, Graniden 1mg Syrup, Granexa 1mg Tablet, Graniforce 1mg Tablet, Granirex 1mg Tablet, Granimet 1mg Tablet, Grandem 1mg Tablet, Graniforce 1mg Injection, Granimax 1mg Injection, Grandem Injection, Gemirob 1mg Injection, Granilet 1mg Injection |
375 mg/m2 intravenously over 1 hour every 3 weeks
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min; avoid use if GFR <30 mL/min due to limited data |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose to 260 mg/m2; Child-Pugh C: not recommended |
| Pediatric use | 10 mg/kg intravenously over 1 hour every 3 weeks; maximum 375 mg/m2 |
| Geriatric use | No specific dose adjustment; monitor for increased risk of infection and infusion reactions |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GRANISOL (GRANISOL).
| Breastfeeding | Granisetron is excreted into human breast milk in low amounts; milk-to-plasma ratio is approximately 1.9. No adverse effects reported in nursing infants. Caution is advised but considered compatible with breastfeeding. |
| Teratogenic Risk | Granisetron is classified as FDA Pregnancy Category B. Animal studies have not demonstrated teratogenic effects, but no adequate and well-controlled studies exist in pregnant women. First trimester: No evidence of major malformations in limited human data. Second and third trimesters: No known fetal harm, but use only if clearly needed. |
■ FDA Black Box Warning
No black box warning.
| Serious Effects |
["History of serious allergic reactions to human G-CSFs (e.g., anaphylaxis, angioedema).","Concurrent administration with chemotherapy and radiation therapy: Not used during the 24 hours before or after cytotoxic chemotherapy."]
| Precautions | ["Splenic rupture: Discontinue if suspected.","Acute respiratory distress syndrome (ARDS): Monitor for dyspnea with pulmonary infiltrates and discontinue if occurs.","Allergic reactions: Discontinue in case of serious allergic reactions.","Sickle cell disease: Use caution due to risk of severe sickle cell crisis.","Leukocytosis: Monitor CBC regularly.","Capillary leak syndrome: Discontinue if signs develop.","Myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML): Increased risk in patients with breast cancer or other cancers; monitor for cytologic abnormalities.","Thrombocytopenia: Monitor platelet counts.","Alveolar hemorrhage: Use caution in patients with known respiratory disease.","Immunogenicity: Potential for antibody formation, but no evidence of neutralizing antibodies."] |
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| Fetal Monitoring |
| No specific maternal-fetal monitoring required beyond routine pregnancy care. Monitor for maternal adverse effects such as headache, constipation, or ECG changes (QT prolongation). |
| Fertility Effects | Granisetron has no known impact on human fertility. Animal studies showed no impairment of fertility at doses up to 9 mg/kg/day. |