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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
Structure of GRANISETRON HYDROCHLORIDE

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-;

HIDE SMILES / InChI

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C18H24N4O
Molecular Weight 312.4094
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 3 / 3
E/Z Centers 0
Optical Activity UNSPECIFIED

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
The efficacy and safety of once-daily Kytril (granisetron hydrochloride) tablets in the prophylaxis of nausea and emesis following fractionated upper abdominal radiotherapy.
2001
Double-blind comparative trial of oral ondansetron versus oral granisetron versus IV ondansetron in the prevention of nausea and vomiting associated with highly emetogenic preparative regimens prior to stem cell transplantation.
2001
[Study of neoadjuvant chemotherapy for invasive bladder cancer with MEC (methotrexate, epirubicin, cisplatin) therapy].
2001 Apr
5-HT1A and 5-HT2 receptors differentially regulate the excitability of 5-HT-containing neurones of the guinea pig dorsal raphe nucleus in vitro.
2001 Apr 27
[Does the addition of an anxiolytic drug improve the anti-emetic effectiveness of the steroid and granisetron combination in the prophylaxis of cisplatin-induced vomiting?].
2001 Aug 5
IgE-mediated allergy to granisetron and safe use of ondansetron.
2001 Dec
Randomised comparison of ondansetron plus dexamethasone with dexamethasone alone for the control of delayed cisplatin-induced emesis.
2001 Dec
The influence of a dominating centre on a quantitative systematic review of granisetron for preventing postoperative nausea and vomiting.
2001 Jul
A placebo-controlled, crossover trial of granisetron in SRI-induced sexual dysfunction.
2001 Jun
Efficacy of single-dose intravenous dolasetron versus ondansetron in the prevention of postoperative nausea and vomiting.
2001 Jun
Pegylated liposomal doxorubicin: tolerability and toxicity.
2001 Jun
Ramosetron compared with granisetron for the prevention of vomiting following strabismus surgery in children.
2001 Jun
Binding characteristics of GYKI-46 903, a non-competitive ligand at 5-HT3 receptors.
2001 Mar
Preoperative oral granisetron for the prevention of postoperative nausea and vomiting after breast surgery.
2001 Mar
5-Hydroxytryptamine (5-HT)-induced depolarization in isolated abdominal vagus nerves in the rat: involvement of 5-HT3 and 5-HT4 receptors.
2001 Mar-Apr
Diverging effects of 5-HT3 receptor antagonists ondansetron and granisetron on estramustine-inhibited cellular potassium transport.
2001 May
Implementing evidence based antiemetic guidelines in the oncology setting: results of a 4-month prospective intervention study.
2001 Nov
Barostat examination of proximal site of the anastomosis in patients with rectal cancer after low anterior resection.
2001 Nov
Characterization of the receptors involved in the 5-HT-induced excitation of canine antral longitudinal muscle.
2001 Nov
5-HT receptor subtypes involved in the spinal antinociceptive effect of acetaminophen in rats.
2001 Nov 30
Effective cross-over to granisetron after failure to ondansetron, a randomized double blind study in patients failing ondansetron plus dexamethasone during the first 24 hours following highly emetogenic chemotherapy.
2001 Oct 19
Effects of CP-99, 994, a tachykinin NK(1) receptor antagonist, on abdominal afferent vagal activity in ferrets: evidence for involvement of NK(1) and 5-HT(3) receptors.
2001 Oct 5
Comparison of tropisetron and granisetron in the control of nausea and vomiting in children receiving combined cancer chemotherapy.
2001 Sep
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
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
Phase II multicentre study of docetaxel plus cisplatin in patients with advanced urothelial cancer.
2002 Feb 1
Emerging treatments for irritable bowel syndrome.
2002 Jan
Antiemetic effects of granisetron, droperidol and dexamethasone in otologic surgery.
2002 Jul
Laxative and anti-diarrheal activity of polycarbophil in mice and rats.
2002 Jun
Effectiveness of serotonin-receptor antagonist antiemetic therapy over successive courses of carboplatin-based chemotherapy.
2002 Jun
Identification of critical residues in loop E in the 5-HT3ASR binding site.
2002 Jun 13
Preoperative oral granisetron for the prevention of vomiting following paediatric surgery.
2002 Mar
Clinical evaluation of granisetron as an inhibitor of nausea and vomiting induced by oral anticancer drugs.
2002 Mar-Apr
Ramosetron for the prevention of cisplatin-induced acute emesis: a prospective randomized comparison with granisetron.
2002 May-Jun
Oral granisetron revisited.
2002 Nov
Phase I study of docetaxel in combination with cyclophosphamide as first-line chemotherapy for metastatic breast cancer.
2002 Nov 4
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
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
Granisetron plus dexamethasone versus granisetron alone in the prevention of vomiting induced by conditioning for stem cell transplantation: a prospective randomized study.
2003 Jan
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.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:51:24 GMT 2023
Edited
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on Fri Dec 15 15:51:24 GMT 2023
Record UNII
318F6L70J8
Record Status Validated (UNII)
Record Version
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Name Type Language
GRANISETRON HYDROCHLORIDE
USP  
Official Name English
GRANISETRON HYDROCHLORIDE [MI]
Common Name English
NSC-759839
Code English
GRANISETRON HYDROCHLORIDE [JAN]
Common Name English
GRANISETRON HYDROCHLORIDE [USAN]
Common Name English
GRANISETRON HYDROCHLORIDE [EP MONOGRAPH]
Common Name English
GRANISETRON (AS HYDROCHLORIDE)
Common Name English
GRANISETRON HYDROCHLORIDE [MART.]
Common Name English
GRANISETRON HYDROCHLORIDE [USP-RS]
Common Name English
GRANISETRON HYDROCHLORIDE [VANDF]
Common Name English
BRL 43694A
Code English
GRANISETRON HYDROCHLORIDE [USP IMPURITY]
Common Name English
BEMA GRANISETRON
Brand Name English
1H-INDAZOLE-3-CARBOXAMIDE, 1-METHYL-N-(9-METHYL-9-AZABICYCLO(3.3.1)NON-3-YL)-, MONOHYDROCHLORIDE, ENDO-
Common Name English
Granisetron hydrochloride [WHO-DD]
Common Name English
1-METHYL-N-(9-METHYL-ENDO-9-AZABICYCLO(3.3.1)NON-3-YL)-1H-INDAZOLE-3-CARBOXAMIDE MONOHYDROCHLORIDE
Common Name English
GRANISETRON HYDROCHLORIDE [ORANGE BOOK]
Common Name English
GRANISETRON HCL
Common Name English
GRANISETRON HYDROCHLORIDE [EP IMPURITY]
Common Name English
GRANISETRON HYDROCHLORIDE [USP MONOGRAPH]
Common Name English
KYTRIL
Brand Name English
Classification Tree Code System Code
NCI_THESAURUS C267
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
NCI_THESAURUS C94726
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
Code System Code Type Description
FDA UNII
318F6L70J8
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
USAN
DD-90
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
ChEMBL
CHEMBL289469
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
NSC
759839
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
PUBCHEM
6918003
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
MERCK INDEX
m5842
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY Merck Index
DAILYMED
318F6L70J8
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
DRUG BANK
DBSALT000485
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
RS_ITEM_NUM
1298106
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
EVMPD
SUB02405MIG
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
RXCUI
142149
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY RxNorm
NCI_THESAURUS
C1353
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
CAS
107007-99-8
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
EPA CompTox
DTXSID7049057
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
SMS_ID
100000090454
Created by admin on Fri Dec 15 15:51:24 GMT 2023 , Edited by admin on Fri Dec 15 15:51:24 GMT 2023
PRIMARY
Related Record Type Details
PARENT->INNOVATOR
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY