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Details

Stereochemistry ACHIRAL
Molecular Formula C18H24N4O
Molecular Weight 312.4094
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GRANISETRON

SMILES

CN1N=C(C(=O)N[C@@H]2C[C@@H]3CCC[C@H](C2)N3C)C4=CC=CC=C14

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

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

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

1992
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
The development of a protocol for the use of 5-HT3 antagonists in chemotherapy-induced nausea and vomiting.
2001
Randomized open-label trial of dolasetron for the control of nausea and vomiting associated with high-dose chemotherapy with hematopoietic stem cell transplantation.
2001
Involvement of nerves and calcium channels in the intestinal response to Clostridium difficile toxin A: an experimental study in rats in vivo.
2001 Jul
A placebo-controlled, crossover trial of granisetron in SRI-induced sexual dysfunction.
2001 Jun
Binding characteristics of GYKI-46 903, a non-competitive ligand at 5-HT3 receptors.
2001 Mar
Effect of paroxetine on extracellular serotonin and dopamine levels in the prefrontal cortex.
2002 Feb
Preoperative oral granisetron for the prevention of vomiting following paediatric surgery.
2002 Mar
Novel potent 5-HT(3) receptor ligands based on the pyrrolidone structure: synthesis, biological evaluation, and computational rationalization of the ligand-receptor interaction modalities.
2002 Mar
Clinical evaluation of granisetron as an inhibitor of nausea and vomiting induced by oral anticancer drugs.
2002 Mar-Apr
Granisetron vs ondansetron: is it a question of duration of 5-HT3 receptor blockade?
2002 May 20
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
Phase I study of docetaxel in combination with cyclophosphamide as first-line chemotherapy for metastatic breast cancer.
2002 Nov 4
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
Granisetron: relating pharmacology to clinical efficacy.
2003 Feb
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.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:55:10 GMT 2023
Edited
by admin
on Fri Dec 15 15:55:10 GMT 2023
Record UNII
WZG3J2MCOL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GRANISETRON
INN   JAN   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official 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
Granisetron [WHO-DD]
Common Name 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 Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
NCI_THESAURUS C267
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
NDF-RT N0000175817
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
WHO-VATC QA04AA02
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
LIVERTOX 467
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
WHO-ATC A04AA02
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
NDF-RT N0000175818
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
EMA ASSESSMENT REPORTS SANCUSO (AUTHORIZED: VOMITTING)
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
Code System Code Type Description
INN
6230
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
DRUG BANK
DB00889
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
MERCK INDEX
m5842
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY Merck Index
CAS
109889-09-0
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
EPA CompTox
DTXSID0023111
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
DAILYMED
WZG3J2MCOL
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
ChEMBL
CHEMBL289469
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
USAN
DD-30
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
IUPHAR
2300
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
SMS_ID
100000084258
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
MESH
D017829
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
NCI_THESAURUS
C62031
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
CAS
124998-65-8
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
NON-SPECIFIC STEREOCHEMISTRY
WIKIPEDIA
GRANISETRON
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
FDA UNII
WZG3J2MCOL
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
RS_ITEM_NUM
1298092
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
EVMPD
SUB07964MIG
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
CHEBI
5537
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
DRUG CENTRAL
1329
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY
RXCUI
26237
Created by admin on Fri Dec 15 15:55:10 GMT 2023 , Edited by admin on Fri Dec 15 15:55:10 GMT 2023
PRIMARY RxNorm
Related Record Type Details
SALT/SOLVATE -> PARENT
LABELED -> NON-LABELED
BINDER->LIGAND
BINDING
EXCRETED UNCHANGED
Based on a study with intravenous injection, approximately 12% of the dose is excreted unchanged in the urine of healthy subjects in 48 hours.
AMOUNT EXCRETED
URINE
TARGET -> INHIBITOR
IC50
Related Record Type Details
METABOLITE ACTIVE -> PARENT
After both oral and intravenous administration, the metabolite is present at about 10% of that of the parent (Clarke et al., 1994; Boppana, 1995). Assuming similar free fractions, it can be estimated that the metabolite would contribute about 20% of the activity of the parent.
Related Record Type Details
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC following patch application