pharmacopeia
GET
/api/v1/drug/granisetron
2D structure
1-methyl-N-[(1R,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide
SMILES CN1[C@@H]2CCC[C@H]1CC(C2)NC(=O)C3=NN(C4=CC=CC=C43)C
InChIKey MFWNKCLOYSRHCJ-AGUYFDCRSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Serotonin 3 Receptor Antagonists; Serotonin 5HT-3 Antagonists.

Serotonin 3 ReceptorSerotonin 5HT-3

Indications

Sourced from openFDA
  • Granisetron is indicated for the prevention of: Nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin. Nausea and vomiting associated with radiation, including total body irradiation and fractionated abdominal radiation.ICD-10: R11.2

Contraindications

Sourced from openFDA
  • Granisetron is contraindicated in patients with known hypersensitivity to the drug or any of its components.contraindicated

Dosage & administration

Sourced from openFDA

Emetogenic Chemotherapy The recommended adult dosage of oral granisetron hydrochloride is 2 mg once daily or 1 mg twice daily. In the 2 mg once-daily regimen, 10 mL of GRANISOL oral solution (2 teaspoonfuls, equivalent to 2 mg of granisetron) are given up to 1 hour before chemotherapy. In the 1 mg twice-daily regimen, the first teaspoonful (5 mL) of GRANISOL oral solution is given up to 1 hour before chemotherapy, and the second teaspoonful (5 mL) of GRANISOL oral solution, 12 hours after the first. Either regimen is administered only on the day(s) chemotherapy is given. Continued treatment, while not on chemotherapy, has not been found to be useful. Use in the Elderly, Renal Failure Patients or Hepatically Impaired Patients No dosage adjustment is recommended (see CLINICAL PHARMACOLOGY: Pharmacokinetics ). Pediatric Use Safety and effectiveness in pediatric patients have not been established. Radiation (Either Total Body Irradiation or Fractionated Abdominal Radiation) The recommended adult dosage of oral granisetron hydrochloride is 2 mg once daily. Ten milliliters of GRANISOL oral solution (2 teaspoonfuls, equivalent to 2 mg of granisetron) are taken within 1 hour of radiation. Pediatric Use Safety and effectiveness in pediatric patients have not been established. Use in the Elderly No dosage adjustment is recommended.

Warnings & precautions

Sourced from openFDA

Serotonin Syndrome The development of serotonin syndrome has been reported with 5-HT3 receptor antagonists alone but particularly with concomitant use of serotonergic drugs (e.g., selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors, mirtazapine, fentanyl, lithium, tramadol, and intravenous methylene blue). Some of the reported cases were fatal. Serotonin syndrome occurring with overdose of another 5-HT3 receptor antagonist alone has also been reported. The majority of reports of serotonin syndrome related to 5-HT3 receptor antagonist use occurred in a post-anesthesia care unit or an infusion center. Symptoms associated with serotonin syndrome may include mental status changes (e.g., agitation, hallucinations, delirium, and coma), autonomic instability (e.g., tachycardia, labile blood pressure, dizziness, diaphoresis, flushing, hyperthermia), neuromuscular symptoms (e.g., tremor, rigidity, myoclonus, hyperreflexia, incoordination), seizures, and/or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea). Patients should be monitored for the emergence of serotonin syndrome, especially with concomitant use of granisetron and other serotonergic drugs. If symptoms of serotonin syndrome occur, discontinue granisetron and initiate supportive treatment. Patients should be informed of the increased risk of serotonin syndrome, especially if granisetron is used concomitantly with other serotonergic drugs [see Drug Interactions ].

Adverse reactions

Sourced from openFDA

QT prolongation has been reported with granisetron (see PRECAUTIONS and Drug Interactions ). Chemotherapy-Induced Nausea and Vomiting Over 3700 patients have received Kytril tablets in clinical trials with emetogenic cancer therapies consisting primarily of cyclophosphamide or cisplatin regimens. In patients receiving Kytril tablets 1 mg bid for 1, 7 or 14 days, or 2 mg daily for 1 day, adverse experiences reported in more than 5% of the patients with comparator and placebo incidences are listed in Table 4 . Table 4 Principal Adverse Events in Clinical Trials Percent of Patients With Event Kytril 1 Tablets 1 mg twice a day (n=978) Kytril 1 Tablets 2 mg once a day N=1450) Comparator 2 (n=599) Placebo (n=185) Headache 3 21% 20% 13% 12% Constipation 18% 14% 16% 8% Asthenia 14% 18% 10% 45 Diarrhea 8% 9% 10% 4% Abdominal Pain 6% 4% 6% 3% Dyspepsia 4% 6% 5% 4% 1 Adverse events were recorded for 7 days when Kytril tablets were given on a single day and for up to 28 days when Kytril tablets were administered for 7 or 14 days. 2 Metoclopramide/dexamethasone; phenothiazines/dexamethasone; dexamethasone alone; prochlorperazine. 3 Usually mild to moderate in severity. Other adverse events reported in clinical trials were: Gastrointestinal : In single-day dosing studies in which adverse events were collected for 7 days, nausea (20%) and vomiting (12%) were recorded as adverse events after the 24-hour efficacy assessment period.

Use in specific populations

Sourced from openFDA

Pregnancy Teratogenic Effects Pregnancy Category B Reproduction studies have been performed in pregnant rats at oral doses up to 125 mg/kg/day (750 mg/m 2 /day, 507 times the recommended human dose based on body surface area) and pregnant rabbits at oral doses up to 32 mg/kg/day (378 mg/m 2 /day, 255 times the recommended human dose based on body surface area) and have revealed no evidence of impaired fertility or harm to the fetus due to granisetron. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Pharmacokinetics

Sourced from openFDA
Metabolism
In healthy volunteers and adult cancer patients undergoing chemotherapy, administration of Kytril tablets produced mean pharmacokinetic data shown in Table 1 . Table 1 Pharmacokinetic Parameters (Median [range]) Following Kytril Tablets 1 Not determined after oral administration; following a single intravenous dose of 40 mcg/kg, terminal phase half-life was determined to be 8.95 hours.

Overdosage

Sourced from openFDA

There is no specific treatment for granisetron hydrochloride overdosage. In case of overdosage, symptomatic treatment should be given. Overdosage of up to 38.5 mg of granisetron hydrochloride injection has been reported without symptoms or only the occurrence of a slight headache.

Approval history

Sourced from openFDA
  • Feb 13, 2008ANDAANDA078678Orbion Pharms
  • Jun 30, 2008ANDAANDA078096Fresenius Kabi Usa
  • Sep 12, 2008NDANDA022198Cumberland
  • Jun 22, 2009ANDAANDA078969Natco Pharma
  • Dec 23, 2009ANDAANDA078629Hikma Farmaceutica
  • Apr 9, 2010ANDAANDA091136Mylan Asi
  • Apr 9, 2010ANDAANDA091137Mylan Asi
  • Aug 9, 2016NDANDA022445Heron Theraps Inc

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
11,923 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Nausea1,46412%
  2. 2Febrile Neutropenia8687.3%
  3. 3Vomiting8667.3%
  4. 4Diarrhoea8457.1%
  5. 5Pyrexia7896.6%
  6. 6Dyspnoea6715.6%
  7. 7Death6645.6%
  8. 8Fatigue6165.2%
  9. 9Neutropenia5604.7%
  10. 10Anaemia5524.6%
  11. 11Off Label Use5304.4%
  12. 12Decreased Appetite4573.8%
  13. 13Constipation4493.8%
  14. 14Pneumonia4363.7%
  15. 15Product Adhesion Issue3993.3%

Literature

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Recent PubMed references pinned to Granisetron as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 138 ClinicalTrials.gov registrations naming Granisetron as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Granisetron work?
Mechanism-of-action classes: Serotonin 3 Receptor Antagonists; Serotonin 5HT-3 Antagonists.
What is Granisetron used for?
According to FDA labeling, Granisetron carries indications including: Granisetron is indicated for the prevention of: Nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin. Nausea and vomiting associated with radiation, including total body irradiation and fractionated abdominal radiation.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Granisetron?
Granisetron is classified as Serotonin (5HT3) antagonists, Serotonin-3 Receptor Antagonist, Serotonin 3 Receptor Antagonists, Serotonin 5HT-3 Antagonists, Decreased Serotonin Activity, Emesis Suppression.
What are the brand names for Granisetron?
Granisetron is marketed under brand names including Granisol, Sancuso, Sustol.
What are the contraindications for Granisetron?
Granisetron labeling lists contraindications including: Granisetron is contraindicated in patients with known hypersensitivity to the drug or any of its components.. Always consult the full prescribing information and a clinician.
Note. Data for granisetron is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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