U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C18H24N4O
Molecular Weight 312.41
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GRANISETRON

SMILES

CN1[C@]2([H])CCC[C@@]1([H])C[C@]([H])(C2)NC(=O)c3c4ccccc4n(C)n3

InChI

InChIKey=MFWNKCLOYSRHCJ-BTTYYORXSA-N
InChI=1S/C18H24N4O/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)/t12-,13+,14-

HIDE SMILES / InChI

Description
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

Curator's Comment:: The increasing brain/blood concentration ratio of granisetron suggests that granisetron penetrates the blood-brain barrier in rats.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1.45 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
SUSTOL

Approved Use

SUSTOL 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 Date

7.2576002E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
4.948 ng/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
36.87 ng × h/mL
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

T1/2

ValueDoseCo-administeredAnalytePopulation
5 h
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

Doses

DosePopulationAdverse 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%)
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%)
Sources:
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%)
Constipation (4.2%)
Somnolence (2.4%)
Dizziness (1.2%)
Dyspepsia (1.8%)
Back pain (3%)
Sources:
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%)
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%)
Sources:
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Other AEs: Pain, Constipation...
Other AEs:
Pain (10.1%)
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%)
Sources:
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%)
Asthenia (5%)
Somnolence (4%)
Diarrhea (4%)
Constipation (3%)
Sources:
AEs

AEs

AESignificanceDosePopulation
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
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Coughing 2.2%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Oliguria 2.2%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Hypertension 2.6%
1 mg single, intravenous
Recommended
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
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Dyspepsia 3%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Flatulence 3%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Infection 3%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Anxiety 3.4%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Diarrhea 3.4%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Hypotension 3.4%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Leukocytosis 3.7%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Dizziness 4.1%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Bradycardia 4.5%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Insomnia 4.9%
1 mg single, intravenous
Recommended
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
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Abdominal pain 6%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Fever 7.9%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Headache 8.6%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Anemia 9.4%
1 mg single, intravenous
Recommended
unhealthy
n = 267
Health Status: unhealthy
Condition: nausea and vomiting, postoperative
Population Size: 267
Sources:
Constipation 9.4%
1 mg single, intravenous
Recommended
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

Overview

Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
likely
likely
likely
likely
likely
likely
likely
likely
likely
major
unknown (co-administration study)
Comment: Administration of intravenous granisetron hydrochloride with phenobarbital, an enzyme inducer, resulted in a 25% increase in total plasma clearance of granisetron. The clinical significance of this interaction is not known.
Page: 113.0
minor
unknown (co-administration study)
Comment: the potential for an in vivo pharmacokinetic interaction with ketoconazole is not known; Administration of intravenous granisetron hydrochloride with phenobarbital, an enzyme inducer, resulted in a 25% increase in total plasma clearance of granisetron. The clinical significance of this interaction is not known.
Page: 113.0
no
no
no
no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Gastroprokinetic effect and mechanism of SK-896, a new motilin analogue, during the interdigestive period in conscious dogs.
2001
Manifest Anxiety Scale for evaluation of effects of granisetron in chemotherapy with CDDP and 5FU for head and neck cancer.
2001 Jul
A placebo-controlled, crossover trial of granisetron in SRI-induced sexual dysfunction.
2001 Jun
[5-HT3 receptors in amygdala mediate neuroimmunomodulation in rats].
2001 Oct
Comparison of tropisetron and granisetron in the control of nausea and vomiting in children receiving combined cancer chemotherapy.
2001 Sep
Effects of lerisetron, a new 5-HT3 receptor antagonist, on ipecacuanha-induced emesis in healthy volunteers.
2002
The cardiotoxic potential of the 5-HT(3) receptor antagonist antiemetics: is there cause for concern?
2002
5-Hydroxytryptamine receptors, especially the 5-HT4 receptor, in guinea pig urinary bladder.
2002 Aug
Ondansetron but not granisetron affect cell volume regulation and potassium ion transport of glioma cells treated with estramustine phosphate.
2002 Aug
Progress in preventing chemotherapy-induced nausea and vomiting.
2002 Aug
Impaired gastrocolonic response and peristaltic reflex in slow-transit constipation: role of 5-HT(3) pathways.
2002 Aug
A 'modified de Gramont' regimen of fluorouracil, alone and with oxaliplatin, for advanced colorectal cancer.
2002 Aug 12
Triplet chemotherapy with vinorelbine, gemcitabine, and cisplatin for advanced non-small cell lung cancer: a phase II study.
2002 Dec 2
Ramosetron, a 5-HT3 receptor antagonist for the control of nausea and vomiting.
2002 Feb
Preoperative induction chemotherapy with cisplatin and irinotecan for pathological N(2) non-small cell lung cancer.
2002 Feb 12
Antiemetic effects of granisetron, droperidol and dexamethasone in otologic surgery.
2002 Jul
Irinotecan pharmacokinetics-pharmacodynamics: the clinical relevance of prolonged exposure to SN-38.
2002 Jul 15
Laxative and anti-diarrheal activity of polycarbophil in mice and rats.
2002 Jun
Involvement of serotonin and nitric oxide in endotoxin-induced gastric motility changes in conscious rats.
2002 Jun
ATP and 5-HT are the principal neurotransmitters in the descending excitatory reflex pathway of the guinea-pig ileum.
2002 Jun
Identification of critical residues in loop E in the 5-HT3ASR binding site.
2002 Jun 13
Clinical evaluation of granisetron as an inhibitor of nausea and vomiting induced by oral anticancer drugs.
2002 Mar-Apr
Gateways to clinical trials.
2002 May
Granisetron vs ondansetron: is it a question of duration of 5-HT3 receptor blockade?
2002 May 20
A phase I trial of weekly gemcitabine and concurrent radiotherapy in patients with locally advanced pancreatic cancer.
2002 May 20
Ramosetron for the prevention of cisplatin-induced acute emesis: a prospective randomized comparison with granisetron.
2002 May-Jun
Comparative study of low-dose oral granisetron plus dexamethasone and high-dose metoclopramide plus dexamethasone in prevention of nausea and vomiting induced by CHOP-therapy in young patients with non-Hodgkin's lymphoma.
2002 Nov
Oral granisetron revisited.
2002 Nov
Motilin regulates interdigestive gastric blood flow in dogs.
2002 Nov
The effect of serotonin and serotonin receptor antagonists on motion sickness in Suncus murinus.
2002 Nov
Phase I study of docetaxel in combination with cyclophosphamide as first-line chemotherapy for metastatic breast cancer.
2002 Nov 4
Compatibility and stability of 5-HT3 receptor antagonists: a pharmacology review.
2002 Nov-Dec
Prophylactic antiemetic efficacy of granisetron or ramosetron in patients undergoing thyroidectomy.
2002 Oct
Irinotecan, cisplatin and mitomycin in inoperable gastro-oesophageal and pancreatic cancers - a new active regimen.
2002 Oct 7
[Nausea disintegrating buccal tablet in the prevention of gastrointestinal reaction induced by anticancer drugs].
2002 Sep
In vivo assessment of acceleration of motor activity associated with acetylcholine release via 5-hydroxytryptamine4 receptor in dog intestine.
2002 Sep
Comparison of granisetron with granisetron plus droperidol combination prophylaxis in post-operative nausea and vomiting after laparoscopic cholecystectomy.
2002 Sep-Oct
Treatment of vomiting after paediatric strabismus surgery with granisetron, droperidol, and metoclopramide.
2002 Sep-Oct
5-HT3-receptor antagonists and the cytochrome P450 system: clinical implications.
2002 Sep-Oct
Analysis of purinergic and cholinergic fast synaptic transmission to identified myenteric neurons.
2003
Combination therapy with granisetron, methylprednisolone and droperidol as an antiemetic prophylaxis in CDDP-induced delayed emesis for gynecologic cancer.
2003
Severe pruritus in a haemodialysed patient: dramatic improvement with granisetron.
2003 Feb
Effects on muscle pain by intramuscular injection of granisetron in patients with fibromyalgia.
2003 Feb
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
Granisetron: relating pharmacology to clinical efficacy.
2003 Feb
Survival with dacarbazine and fotemustine in newly diagnosed glioblastoma multiforme.
2003 Feb 24
Granisetron plus dexamethasone versus granisetron alone in the prevention of vomiting induced by conditioning for stem cell transplantation: a prospective randomized study.
2003 Jan
Comparison of granisetron and granisetron plus dexamethasone for the prevention of postoperative nausea and vomiting after laparoscopic cholecystectomy.
2003 Jan
Feasibility of combination chemotherapy with cisplatin and etoposide for haemodialysis patients with lung cancer.
2003 Jan 13
Pharmacological characterization of the 5-HT1A, 5-HT2 and 5-HT3 receptors in the bovine ciliary muscle.
2003 Mar 7
Patents

Sample Use Guides

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
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.
Name Type Language
GRANISETRON
INN   JAN   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
GRANISETRON [WHO-DD]
Common Name English
GRANISETRON [USAN]
Common Name English
GRANISETRON [JAN]
Common Name English
APF530
Code English
LY-278584
Code English
GRANISETRON [VANDF]
Common Name English
GRANISETRON [USP MONOGRAPH]
Common Name English
GRANISETRON [USP-RS]
Common Name English
APF-530
Code English
1H-INDAZOLE-3-CARBOXAMIDE, 1-METHYL-N-(9-METHYL-9-AZABICYCLO(3.3.1)NON-3-YL)-, ENDO-
Common Name English
GRANISETRON [MI]
Common Name English
BRL-43694
Code English
GRANISETRON [ORANGE BOOK]
Common Name English
BRL 43694
Code English
GRANISETRON [INN]
Common Name English
SANCUSO
Brand Name English
1-METHYL-N-(9-METHYL-ENDO-9-AZABICYCLO(3.3.1)NON-3-YL)-1H-INDAZOLE-3-CARBOXAMIDE
Common Name English
SUSTOL
Brand Name English
Classification Tree Code System Code
NCI_THESAURUS C94726
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
NCI_THESAURUS C267
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
NDF-RT N0000175817
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
WHO-VATC QA04AA02
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
LIVERTOX 467
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
WHO-ATC A04AA02
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
NDF-RT N0000175818
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
EMA ASSESSMENT REPORTS SANCUSO (AUTHORIZED: VOMITTING)
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
Code System Code Type Description
INN
6230
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
DRUG BANK
DB00889
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
MERCK INDEX
M5842
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY Merck Index
CAS
109889-09-0
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
EPA CompTox
109889-09-0
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
ChEMBL
CHEMBL289469
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
IUPHAR
2300
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
MESH
D017829
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
NCI_THESAURUS
C62031
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
CAS
124998-65-8
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
NON-SPECIFIC STEREOCHEMISTRY
WIKIPEDIA
GRANISETRON
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
FDA UNII
WZG3J2MCOL
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
EVMPD
SUB07964MIG
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
DRUG CENTRAL
1329
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY
RXCUI
26237
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY RxNorm
USP_CATALOG
1298092
Created by admin on Sat Jun 26 08:16:20 UTC 2021 , Edited by admin on Sat Jun 26 08:16:20 UTC 2021
PRIMARY USP-RS