Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C18H24N4O.ClH |
Molecular Weight | 348.87 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN1N=C(C(=O)N[C@@H]2C[C@@H]3CCC[C@H](C2)N3C)C4=CC=CC=C14
InChI
InChIKey=QYZRTBKYBJRGJB-WQTKJZBYSA-N
InChI=1S/C18H24N4O.ClH/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17;/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23);1H/t12-,13+,14-;
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C18H24N4O |
Molecular Weight | 312.4094 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.drugbank.ca/drugs/DB00889Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022445s000lbl.pdf
Sources: http://www.drugbank.ca/drugs/DB00889
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022445s000lbl.pdf
Granisetron is a selective inhibitor of type 3 serotonergic (5-HT3) receptors. The drug is structurally and pharmacologically related to ondansetron, another selective inhibitor of 5-HT3 receptors. The serontonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. The temporal relationship between the emetogenic action of emetogenic drugs and the release of serotonin, as well as the efficacy of antiemetic agents suggest that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting. Granisetron is a potent, selective antagonist of 5-HT3 receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. Granisetron is used for the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy (including high dose cisplatin), postoperation, and radiation (including total body irradiation and daily fractionated abdominal radiation).
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9824238
Curator's Comment: The increasing brain/blood concentration ratio of granisetron suggests that granisetron penetrates the blood-brain barrier in rats.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1899 Sources: http://www.drugbank.ca/drugs/DB00889 |
1.45 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Secondary | SUSTOL Approved UseSUSTOL is a serotonin-3 (5-HT3) receptor antagonist indicated in combination with other antiemetics in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic chemotherapy (MEC) or anthracycline and cyclophosphamide (AC) combination chemotherapy regimens. Launch Date1992 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4.948 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22452942 |
10 μg/kg bw single, intravenous dose: 10 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
GRANISETRON plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
36.87 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22452942 |
10 μg/kg bw single, intravenous dose: 10 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
GRANISETRON plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22452942 |
10 μg/kg bw single, intravenous dose: 10 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
GRANISETRON plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Other AEs: Constipation, Headache... Other AEs: Constipation (27.5%) Sources: Headache (17.6%) Leukopenia (15%) Asthenia (6.9%) Abdominal pain (9%) Decreased appetite (5.6%) Anemia (1.3%) Diarrhea (4.3%) Abnormal liver function tests (2.6%) Alopecia (3%) Pain (0.4%) |
160 ug/kg single, intravenous Highest studied dose Dose: 160 ug/kg Route: intravenous Route: single Dose: 160 ug/kg Co-administed with:: cisplatin(>50 mg/m^2) Sources: |
unhealthy, 54 n = 165 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 54 Sex: M+F Population Size: 165 Sources: |
Other AEs: Headache, Constipation... Other AEs: Headache (13.9%) Sources: Constipation (4.2%) Somnolence (2.4%) Dizziness (1.2%) Dyspepsia (1.8%) Back pain (3%) |
15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Other AEs: Constipation, Diarrhea... Other AEs: Constipation (23.1%) Sources: Diarrhea (15.4%) Headache (30.8%) Fatigue (15.4%) Anorexia (15.4%) Weight loss (7.7%) Dizziness (7.7%) Neutropenia (15.4%) Mucosal inflammation (15.4%) Dyspnea (7.7%) Insomnia (7.7%) Thrombocytopenia (7.7%) Injection site bruising (7.7%) Pain injection site (2.2%) |
1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Other AEs: Pain, Constipation... Other AEs: Pain (10.1%) Sources: Constipation (9.4%) Anemia (9.4%) Headache (8.6%) Fever (7.9%) Abdominal pain (6%) Hepatic enzymes increased (5.6%) Insomnia (4.9%) Bradycardia (4.5%) Dizziness (4.1%) Leukocytosis (3.7%) Anxiety (3.4%) Hypotension (3.4%) Diarrhea (3.4%) Flatulence (3%) Infection (3%) Dyspepsia (3%) Hypertension (2.6%) Urinary tract infection (2.6%) Oliguria (2.2%) Coughing (2.2%) |
40 ug/kg single, intravenous Recommended Dose: 40 ug/kg Route: intravenous Route: single Dose: 40 ug/kg Sources: |
unhealthy n = 1268 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Population Size: 1268 Sources: |
Other AEs: Headache, Asthenia... Other AEs: Headache (14%) Sources: Asthenia (5%) Somnolence (4%) Diarrhea (4%) Constipation (3%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Pain | 0.4% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Anemia | 1.3% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Leukopenia | 15% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Headache | 17.6% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Abnormal liver function tests | 2.6% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Constipation | 27.5% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Alopecia | 3% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Diarrhea | 4.3% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Decreased appetite | 5.6% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Asthenia | 6.9% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Abdominal pain | 9% | 2 mg 2 times / day multiple, oral Highest studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, 50.6 years (range: 23-76 years) n = 233 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 50.6 years (range: 23-76 years) Sex: M+F Population Size: 233 Sources: |
Dizziness | 1.2% | 160 ug/kg single, intravenous Highest studied dose Dose: 160 ug/kg Route: intravenous Route: single Dose: 160 ug/kg Co-administed with:: cisplatin(>50 mg/m^2) Sources: |
unhealthy, 54 n = 165 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 54 Sex: M+F Population Size: 165 Sources: |
Dyspepsia | 1.8% | 160 ug/kg single, intravenous Highest studied dose Dose: 160 ug/kg Route: intravenous Route: single Dose: 160 ug/kg Co-administed with:: cisplatin(>50 mg/m^2) Sources: |
unhealthy, 54 n = 165 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 54 Sex: M+F Population Size: 165 Sources: |
Headache | 13.9% | 160 ug/kg single, intravenous Highest studied dose Dose: 160 ug/kg Route: intravenous Route: single Dose: 160 ug/kg Co-administed with:: cisplatin(>50 mg/m^2) Sources: |
unhealthy, 54 n = 165 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 54 Sex: M+F Population Size: 165 Sources: |
Somnolence | 2.4% | 160 ug/kg single, intravenous Highest studied dose Dose: 160 ug/kg Route: intravenous Route: single Dose: 160 ug/kg Co-administed with:: cisplatin(>50 mg/m^2) Sources: |
unhealthy, 54 n = 165 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 54 Sex: M+F Population Size: 165 Sources: |
Back pain | 3% | 160 ug/kg single, intravenous Highest studied dose Dose: 160 ug/kg Route: intravenous Route: single Dose: 160 ug/kg Co-administed with:: cisplatin(>50 mg/m^2) Sources: |
unhealthy, 54 n = 165 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 54 Sex: M+F Population Size: 165 Sources: |
Constipation | 4.2% | 160 ug/kg single, intravenous Highest studied dose Dose: 160 ug/kg Route: intravenous Route: single Dose: 160 ug/kg Co-administed with:: cisplatin(>50 mg/m^2) Sources: |
unhealthy, 54 n = 165 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 54 Sex: M+F Population Size: 165 Sources: |
Anorexia | 15.4% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Diarrhea | 15.4% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Fatigue | 15.4% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Mucosal inflammation | 15.4% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Neutropenia | 15.4% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Pain injection site | 2.2% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Constipation | 23.1% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Headache | 30.8% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Dizziness | 7.7% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Dyspnea | 7.7% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Injection site bruising | 7.7% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Insomnia | 7.7% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Thrombocytopenia | 7.7% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Weight loss | 7.7% | 15 mg single, subcutaneous Highest studied dose Dose: 15 mg Route: subcutaneous Route: single Dose: 15 mg Sources: |
unhealthy, 64.3 n = 13 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Age Group: 64.3 Sex: M+F Population Size: 13 Sources: |
Pain | 10.1% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Coughing | 2.2% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Oliguria | 2.2% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Hypertension | 2.6% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Urinary tract infection | 2.6% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Dyspepsia | 3% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Flatulence | 3% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Infection | 3% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Anxiety | 3.4% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Diarrhea | 3.4% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Hypotension | 3.4% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Leukocytosis | 3.7% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Dizziness | 4.1% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Bradycardia | 4.5% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Insomnia | 4.9% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Hepatic enzymes increased | 5.6% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Abdominal pain | 6% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Fever | 7.9% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Headache | 8.6% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Anemia | 9.4% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Constipation | 9.4% | 1 mg single, intravenous Recommended Dose: 1 mg Route: intravenous Route: single Dose: 1 mg Sources: |
unhealthy n = 267 Health Status: unhealthy Condition: nausea and vomiting, postoperative Population Size: 267 Sources: |
Headache | 14% | 40 ug/kg single, intravenous Recommended Dose: 40 ug/kg Route: intravenous Route: single Dose: 40 ug/kg Sources: |
unhealthy n = 1268 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Population Size: 1268 Sources: |
Constipation | 3% | 40 ug/kg single, intravenous Recommended Dose: 40 ug/kg Route: intravenous Route: single Dose: 40 ug/kg Sources: |
unhealthy n = 1268 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Population Size: 1268 Sources: |
Diarrhea | 4% | 40 ug/kg single, intravenous Recommended Dose: 40 ug/kg Route: intravenous Route: single Dose: 40 ug/kg Sources: |
unhealthy n = 1268 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Population Size: 1268 Sources: |
Somnolence | 4% | 40 ug/kg single, intravenous Recommended Dose: 40 ug/kg Route: intravenous Route: single Dose: 40 ug/kg Sources: |
unhealthy n = 1268 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Population Size: 1268 Sources: |
Asthenia | 5% | 40 ug/kg single, intravenous Recommended Dose: 40 ug/kg Route: intravenous Route: single Dose: 40 ug/kg Sources: |
unhealthy n = 1268 Health Status: unhealthy Condition: nausea and vomiting, chemotherapy-Induced Population Size: 1268 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as victim
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
The development of a protocol for the use of 5-HT3 antagonists in chemotherapy-induced nausea and vomiting. | 2001 |
|
The efficacy and safety of once-daily Kytril (granisetron hydrochloride) tablets in the prophylaxis of nausea and emesis following fractionated upper abdominal radiotherapy. | 2001 |
|
Double-blind comparative trial of oral ondansetron versus oral granisetron versus IV ondansetron in the prevention of nausea and vomiting associated with highly emetogenic preparative regimens prior to stem cell transplantation. | 2001 |
|
[Study of neoadjuvant chemotherapy for invasive bladder cancer with MEC (methotrexate, epirubicin, cisplatin) therapy]. | 2001 Apr |
|
5-HT1A and 5-HT2 receptors differentially regulate the excitability of 5-HT-containing neurones of the guinea pig dorsal raphe nucleus in vitro. | 2001 Apr 27 |
|
[Does the addition of an anxiolytic drug improve the anti-emetic effectiveness of the steroid and granisetron combination in the prophylaxis of cisplatin-induced vomiting?]. | 2001 Aug 5 |
|
IgE-mediated allergy to granisetron and safe use of ondansetron. | 2001 Dec |
|
Randomised comparison of ondansetron plus dexamethasone with dexamethasone alone for the control of delayed cisplatin-induced emesis. | 2001 Dec |
|
The influence of a dominating centre on a quantitative systematic review of granisetron for preventing postoperative nausea and vomiting. | 2001 Jul |
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A placebo-controlled, crossover trial of granisetron in SRI-induced sexual dysfunction. | 2001 Jun |
|
Efficacy of single-dose intravenous dolasetron versus ondansetron in the prevention of postoperative nausea and vomiting. | 2001 Jun |
|
Pegylated liposomal doxorubicin: tolerability and toxicity. | 2001 Jun |
|
Ramosetron compared with granisetron for the prevention of vomiting following strabismus surgery in children. | 2001 Jun |
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Binding characteristics of GYKI-46 903, a non-competitive ligand at 5-HT3 receptors. | 2001 Mar |
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Preoperative oral granisetron for the prevention of postoperative nausea and vomiting after breast surgery. | 2001 Mar |
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5-Hydroxytryptamine (5-HT)-induced depolarization in isolated abdominal vagus nerves in the rat: involvement of 5-HT3 and 5-HT4 receptors. | 2001 Mar-Apr |
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Diverging effects of 5-HT3 receptor antagonists ondansetron and granisetron on estramustine-inhibited cellular potassium transport. | 2001 May |
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Implementing evidence based antiemetic guidelines in the oncology setting: results of a 4-month prospective intervention study. | 2001 Nov |
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Barostat examination of proximal site of the anastomosis in patients with rectal cancer after low anterior resection. | 2001 Nov |
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Characterization of the receptors involved in the 5-HT-induced excitation of canine antral longitudinal muscle. | 2001 Nov |
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5-HT receptor subtypes involved in the spinal antinociceptive effect of acetaminophen in rats. | 2001 Nov 30 |
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Effective cross-over to granisetron after failure to ondansetron, a randomized double blind study in patients failing ondansetron plus dexamethasone during the first 24 hours following highly emetogenic chemotherapy. | 2001 Oct 19 |
|
Effects of CP-99, 994, a tachykinin NK(1) receptor antagonist, on abdominal afferent vagal activity in ferrets: evidence for involvement of NK(1) and 5-HT(3) receptors. | 2001 Oct 5 |
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Comparison of tropisetron and granisetron in the control of nausea and vomiting in children receiving combined cancer chemotherapy. | 2001 Sep |
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The cardiotoxic potential of the 5-HT(3) receptor antagonist antiemetics: is there cause for concern? | 2002 |
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5-Hydroxytryptamine receptors, especially the 5-HT4 receptor, in guinea pig urinary bladder. | 2002 Aug |
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Progress in preventing chemotherapy-induced nausea and vomiting. | 2002 Aug |
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Impaired gastrocolonic response and peristaltic reflex in slow-transit constipation: role of 5-HT(3) pathways. | 2002 Aug |
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A 'modified de Gramont' regimen of fluorouracil, alone and with oxaliplatin, for advanced colorectal cancer. | 2002 Aug 12 |
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Phase II multicentre study of docetaxel plus cisplatin in patients with advanced urothelial cancer. | 2002 Feb 1 |
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Emerging treatments for irritable bowel syndrome. | 2002 Jan |
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Antiemetic effects of granisetron, droperidol and dexamethasone in otologic surgery. | 2002 Jul |
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Laxative and anti-diarrheal activity of polycarbophil in mice and rats. | 2002 Jun |
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Effectiveness of serotonin-receptor antagonist antiemetic therapy over successive courses of carboplatin-based chemotherapy. | 2002 Jun |
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Identification of critical residues in loop E in the 5-HT3ASR binding site. | 2002 Jun 13 |
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Preoperative oral granisetron for the prevention of vomiting following paediatric surgery. | 2002 Mar |
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Clinical evaluation of granisetron as an inhibitor of nausea and vomiting induced by oral anticancer drugs. | 2002 Mar-Apr |
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Ramosetron for the prevention of cisplatin-induced acute emesis: a prospective randomized comparison with granisetron. | 2002 May-Jun |
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Oral granisetron revisited. | 2002 Nov |
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Phase I study of docetaxel in combination with cyclophosphamide as first-line chemotherapy for metastatic breast cancer. | 2002 Nov 4 |
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Irinotecan, cisplatin and mitomycin in inoperable gastro-oesophageal and pancreatic cancers - a new active regimen. | 2002 Oct 7 |
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[Nausea disintegrating buccal tablet in the prevention of gastrointestinal reaction induced by anticancer drugs]. | 2002 Sep |
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In vivo assessment of acceleration of motor activity associated with acetylcholine release via 5-hydroxytryptamine4 receptor in dog intestine. | 2002 Sep |
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Combination therapy with granisetron, methylprednisolone and droperidol as an antiemetic prophylaxis in CDDP-induced delayed emesis for gynecologic cancer. | 2003 |
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Severe pruritus in a haemodialysed patient: dramatic improvement with granisetron. | 2003 Feb |
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Effects on muscle pain by intramuscular injection of granisetron in patients with fibromyalgia. | 2003 Feb |
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A randomized double-blind trial to compare the clinical efficacy of granisetron with metoclopramide, both combined with dexamethasone in the prophylaxis of chemotherapy-induced delayed emesis. | 2003 Feb |
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Granisetron: relating pharmacology to clinical efficacy. | 2003 Feb |
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Granisetron plus dexamethasone versus granisetron alone in the prevention of vomiting induced by conditioning for stem cell transplantation: a prospective randomized study. | 2003 Jan |
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Pharmacological characterization of the 5-HT1A, 5-HT2 and 5-HT3 receptors in the bovine ciliary muscle. | 2003 Mar 7 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/granisetron.html
IV: 10 mcg/kg over 5 minutes, beginning 30 minutes before initiation of chemotherapy.
Orally: 2 mg, given up to 1 hour before chemotherapy, or 1 mg twice a day (the first dose is given up to 1 hour before chemotherapy, and the second dose is given 12 hours later).
Granisetron transdermal system: Apply a single patch to the upper outer arm a minimum of 24 hours before chemotherapy. The patch may be applied up to a maximum of 48 hours before chemotherapy as appropriate. Remove the patch a minimum of 24 hours after completion of chemotherapy. The patch can be worn for up to 7 days depending on the duration of the chemotherapy regimen. Granisetron transdermal system is a 52 cm2 patch containing 34.3 mg of granisetron. The patch releases 3.1 mg of granisetron per 24 hours for up to 7 days.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9401783
Granisetron (1 uM) shifted the response curves to mucosally applied 5-HT to the right in a parallel and surmountable manner in the guinea pig isolated ileum.
Substance Class |
Chemical
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