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-;
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 |
---|---|---|
Randomized open-label trial of dolasetron for the control of nausea and vomiting associated with high-dose chemotherapy with hematopoietic stem cell transplantation. | 2001 |
|
Randomised comparison of ondansetron plus dexamethasone with dexamethasone alone for the control of delayed cisplatin-induced emesis. | 2001 Dec |
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Effects of nutrients and serotonin 5-HT3 antagonism on symptoms evoked by distal gastric distension in humans. | 2001 Feb |
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Intestinal serotonin acts as a paracrine substance to mediate vagal signal transmission evoked by luminal factors in the rat. | 2001 Feb 1 |
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Prophylaxis with oral granisetron for the prevention of nausea and vomiting after laparoscopic cholecystectomy: a prospective randomized study. | 2001 Jan |
|
Manifest Anxiety Scale for evaluation of effects of granisetron in chemotherapy with CDDP and 5FU for head and neck cancer. | 2001 Jul |
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A placebo-controlled, crossover trial of granisetron in SRI-induced sexual dysfunction. | 2001 Jun |
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Preoperative oral granisetron for the prevention of postoperative nausea and vomiting after breast surgery. | 2001 Mar |
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Prevention of cisplatin-induced emesis by the oral neurokinin-1 antagonist, MK-869, in combination with granisetron and dexamethasone or with dexamethasone alone. | 2001 Mar 15 |
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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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Phase I and pharmacological study of a new camptothecin derivative, exatecan mesylate (DX-8951f), infused over 30 minutes every three weeks. | 2001 Oct |
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Effects of lerisetron, a new 5-HT3 receptor antagonist, on ipecacuanha-induced emesis in healthy volunteers. | 2002 |
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Effects of ondansetron, granisetron, ramosetron, and azasetron on human neutrophil functions. | 2002 |
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Sensitization of enteric reflexes in the rat colon in vitro. | 2002 Apr 18 |
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Emerging treatments for irritable bowel syndrome. | 2002 Jan |
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ATP and 5-HT are the principal neurotransmitters in the descending excitatory reflex pathway of the guinea-pig ileum. | 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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Functional group interactions of a 5-HT3R antagonist. | 2002 Jun 13 |
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Preoperative oral granisetron for the prevention of vomiting following paediatric surgery. | 2002 Mar |
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Gateways to clinical trials. | 2002 May |
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Comparison of granisetron and ramosetron for the prevention of nausea and vomiting after thyroidectomy. | 2002 May |
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A dose-finding study of carboplatin-epirubicin-docetaxel in advanced epithelial ovarian cancer. | 2002 May 6 |
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Oral granisetron revisited. | 2002 Nov |
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Motilin regulates interdigestive gastric blood flow in dogs. | 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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Compatibility and stability of 5-HT3 receptor antagonists: a pharmacology review. | 2002 Nov-Dec |
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Prophylactic antiemetic efficacy of granisetron or ramosetron in patients undergoing thyroidectomy. | 2002 Oct |
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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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Treatment of vomiting after paediatric strabismus surgery with granisetron, droperidol, and metoclopramide. | 2002 Sep-Oct |
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5-HT3-receptor antagonists and the cytochrome P450 system: clinical implications. | 2002 Sep-Oct |
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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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Survival with dacarbazine and fotemustine in newly diagnosed glioblastoma multiforme. | 2003 Feb 24 |
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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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Comparison of granisetron and granisetron plus dexamethasone for the prevention of postoperative nausea and vomiting after laparoscopic cholecystectomy. | 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.
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ACTIVE MOIETY
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