Granisetron

Granisetron Brand Names

Granisol | Kytril | Sancuso | Sustol

What is Granisetron

Granisetron is an oral, parenteral, and transdermal serotonin-3 (5HT3) receptor antagonist.

It is commonly used to offset nausea and vomiting from highly emetogenic chemotherapy (HEC); its efficacy has been demonstrated alone and in combination with dexamethasone.

Granisetron is similar to ondansetron in activity, efficacy, and adverse effects. Despite its effectiveness, granisetron is not recommended for the routine treatment of nausea due to its significant cost relative to other anti-nauseants.

Granisetron injection was approved by the FDA in 1993 for the prevention of chemotherapy-induced nausea and/or vomiting (CINV). The oral dosage form was subsequently approved 1995 and has been shown to be as effective as IV ondansetron.

The FDA approved oral granisetron (1999) for the prevention of radiation-induced nausea and vomiting and IV granisetron (2002) for the prevention of post-operative nausea and vomiting.

In 2008, the FDA approved granisetron transdermal system (Sancuso) for the prevention of CINV in patients receiving moderately emetogenic chemotherapy (MEC) and/or HEC regimens of up to 5 days duration.

An extended-release injection for subcutaneous administration (Sustol) that is non-inferior to palonosetron was FDA approved in 2016 for the prevention of acute CINV prior to both MEC and HEC; it is also approved for the prevention of delayed CINV prior to MEC only.

Indications

  1. chemotherapy-induced nausea/vomiting
  2. chemotherapy-induced nausea/vomiting prophylaxis
  3. post-operative nausea/vomiting (PONV)
  4. post-operative nausea/vomiting (PONV) prophylaxis
  5. radiation-induced nausea/vomiting prophylaxis

For chemotherapy-induced nausea/vomiting (CINV) and chemotherapy-induced nausea/vomiting prophylaxis

for chemotherapy-induced nausea/vomiting (CINV) prophylaxis, including for high-dose cisplatin

Side Effects

  1. abdominal pain
  2. agitation
  3. alopecia
  4. anaphylactoid reactions
  5. anemia
  6. angina
  7. anorexia
  8. anxiety
  9. asthenia
  10. atrial fibrillation
  11. AV block
  12. bleeding
  13. bleeding
  14. bradycardia
  15. burns
  16. chest pain (unspecified)
  17. coma
  18. constipation
  19. diaphoresis
  20. diarrhea
  21. dizziness
  22. drowsiness
  23. dysgeusia
  24. dyspepsia
  25. dyspnea
  26. elevated hepatic enzymes
  27. erythema
  28. fatigue
  29. fever
  30. flushing
  31. gastroesophageal reflux
  32. GI obstruction
  33. hallucinations
  34. headache
  35. hematoma
  36. hematoma
  37. hyperreflexia
  38. hypertension
  39. hyperthermia
  40. hypotension
  41. ileus
  42. infection
  43. injection site reaction
  44. injection site reaction
  45. insomnia
  46. leukopenia
  47. nausea
  48. palpitations
  49. pancreatitis
  50. paresthesias
  51. photosensitivity
  52. pruritus
  53. QT prolongation
  54. rash
  55. seizures
  56. serotonin syndrome
  57. sinus tachycardia
  58. skin discoloration
  59. skin irritation
  60. syncope
  61. thrombocytopenia
  62. tremor
  63. urticaria
  64. vesicular rash
  65. vomiting

Contraindications

  • ambient temperature increase
  • anticoagulant therapy
  • apheresis
  • AV block
  • benzyl alcohol hypersensitivity
  • bipolar disorder
  • bleeding
  • bradycardia
  • breast-feeding
  • cardiac arrhythmias
  • cardiac disease
  • cardiomyopathy
  • celiac disease
  • constipation
  • depression
  • dolasetron hypersensitivity
  • females
  • fever
  • geriatric
  • GI obstruction
  • granisetron hypersensitivity
  • heart failure
  • heating pad
  • human immunodeficiency virus (HIV) infection
  • hyperparathyroidism
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • hypothermia
  • hypothyroidism
  • ileus
  • long QT syndrome
  • myocardial infarction
  • neonates
  • ondansetron hypersensitivity
  • pain
  • palonosetron hypersensitivity
  • pheochromocytoma
  • pregnancy
  • QT prolongation
  • rheumatoid arthritis
  • sickle cell disease
  • sleep deprivation
  • stroke
  • sunlight (UV) exposure
  • surgery
  • systemic lupus erythematosus (SLE)

Interactions

  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Codeine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Tramadol
  • Aclidinium; Formoterol
  • Albuterol
  • Albuterol; Ipratropium
  • Alfentanil
  • Alfuzosin
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Aliskiren; Hydrochlorothiazide, HCTZ
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Amiodarone
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Anagrelide
  • Apalutamide
  • Apomorphine
  • Aprepitant, Fosaprepitant
  • Arformoterol
  • Aripiprazole
  • Arsenic Trioxide
  • Artemether; Lumefantrine
  • Asenapine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atenolol; Chlorthalidone
  • Atomoxetine
  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Azilsartan; Chlorthalidone
  • Azithromycin
  • Bedaquiline
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Benazepril; Hydrochlorothiazide, HCTZ
  • Bendroflumethiazide; Nadolol
  • Benzhydrocodone; Acetaminophen
  • Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Bepridil
  • Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Bisoprolol; Hydrochlorothiazide, HCTZ
  • Boceprevir
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Budesonide; Formoterol
  • Bumetanide
  • Buprenorphine
  • Buprenorphine; Naloxone
  • Candesartan; Hydrochlorothiazide, HCTZ
  • Captopril; Hydrochlorothiazide, HCTZ
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Ceritinib
  • Chloroquine
  • Chlorothiazide
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpromazine
  • Chlorthalidone
  • Chlorthalidone; Clonidine
  • Ciprofloxacin
  • Cisapride
  • Citalopram
  • Clarithromycin
  • Class IA Antiarrhythmics
  • Clofazimine
  • Clozapine
  • Cobicistat
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Crizotinib
  • Cyclobenzaprine
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Dasatinib
  • Degarelix
  • Desvenlafaxine
  • Deutetrabenazine
  • Dextromethorphan; Promethazine
  • Dextromethorphan; Quinidine
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Disopyramide
  • Dofetilide
  • Dolasetron
  • Dolutegravir; Rilpivirine
  • Donepezil
  • Donepezil; Memantine
  • Dronedarone
  • Droperidol
  • Duloxetine
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elbasvir; Grazoprevir
  • Eliglustat
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Emtricitabine; Rilpivirine; Tenofovir alafenamide
  • Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
  • Enalapril; Hydrochlorothiazide, HCTZ
  • Encorafenib
  • Entrectinib
  • Enzalutamide
  • Eprosartan; Hydrochlorothiazide, HCTZ
  • Eribulin
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Escitalopram
  • Ethacrynic Acid
  • Ezogabine
  • Fenfluramine
  • Fentanyl
  • Fingolimod
  • Flecainide
  • Fluconazole
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluphenazine
  • Fluticasone; Salmeterol
  • Fluticasone; Umeclidinium; Vilanterol
  • Fluticasone; Vilanterol
  • Fluvoxamine
  • Formoterol
  • Formoterol; Mometasone
  • Foscarnet
  • Fosinopril; Hydrochlorothiazide, HCTZ
  • Furosemide
  • Gemifloxacin
  • Gemtuzumab Ozogamicin
  • Gilteritinib
  • Glasdegib
  • Glycopyrrolate; Formoterol
  • Goserelin
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Halogenated Anesthetics
  • Haloperidol
  • Histrelin
  • Homatropine; Hydrocodone
  • Hydralazine; Hydrochlorothiazide, HCTZ
  • Hydrochlorothiazide, HCTZ
  • Hydrochlorothiazide, HCTZ; Irbesartan
  • Hydrochlorothiazide, HCTZ; Lisinopril
  • Hydrochlorothiazide, HCTZ; Losartan
  • Hydrochlorothiazide, HCTZ; Methyldopa
  • Hydrochlorothiazide, HCTZ; Metoprolol
  • Hydrochlorothiazide, HCTZ; Moexipril
  • Hydrochlorothiazide, HCTZ; Olmesartan
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Hydrochlorothiazide, HCTZ; Quinapril
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Telmisartan
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrochlorothiazide, HCTZ; Valsartan
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Hydroxychloroquine
  • Hydroxyzine
  • Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate
  • Ibuprofen; Oxycodone
  • Ibutilide
  • Idelalisib
  • Iloperidone
  • Indacaterol
  • Indacaterol; Glycopyrrolate
  • Inotuzumab Ozogamicin
  • Ipecac
  • Isavuconazonium
  • Isocarboxazid
  • Itraconazole
  • Ivosidenib
  • Ketoconazole
  • Lapatinib
  • Lasmiditan
  • Lefamulin
  • Lenvatinib
  • Lesinurad
  • Lesinurad; Allopurinol
  • Letermovir
  • Leuprolide
  • Leuprolide; Norethindrone
  • Levalbuterol
  • Levofloxacin
  • Levomilnacipran
  • Levorphanol
  • Linezolid
  • Lithium
  • Lofexidine
  • Long-acting beta-agonists
  • Loop diuretics
  • Loperamide
  • Loperamide; Simethicone
  • Lopinavir; Ritonavir
  • Macimorelin
  • Maprotiline
  • Mefloquine
  • Meperidine
  • Meperidine; Promethazine
  • Mesoridazine
  • Metaproterenol
  • Methadone
  • Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine
  • Methyclothiazide
  • Methylene Blue
  • Metolazone
  • Metronidazole
  • Midostaurin
  • Mifepristone
  • Milnacipran
  • Mirtazapine
  • Mitotane
  • Morphine
  • Morphine; Naltrexone
  • Moxifloxacin
  • Nalbuphine
  • Nilotinib
  • Norfloxacin
  • Octreotide
  • Ofloxacin
  • Olanzapine
  • Olodaterol
  • Ombitasvir; Paritaprevir; Ritonavir
  • Ondansetron
  • Oritavancin
  • Osilodrostat
  • Osimertinib
  • Oxaliplatin
  • Oxycodone
  • Oxymorphone
  • Ozanimod
  • Paliperidone
  • Panobinostat
  • Paroxetine
  • Pasireotide
  • Pazopanib
  • Pentamidine
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenelzine
  • Phenobarbital
  • Phenylephrine; Promethazine
  • Pimavanserin
  • Pimozide
  • Pirbuterol
  • Pitolisant
  • Posaconazole
  • Primaquine
  • Primidone
  • Procainamide
  • Prochlorperazine
  • Promethazine
  • Propafenone
  • Quetiapine
  • Quinidine
  • Quinine
  • Ranolazine
  • Rasagiline
  • Remifentanil
  • Ribociclib
  • Ribociclib; Letrozole
  • Rilpivirine
  • Risperidone
  • Ritonavir
  • Romidepsin
  • Salmeterol
  • Saquinavir
  • Selegiline
  • Selpercatinib
  • Sertraline
  • Short-acting beta-agonists
  • Siponimod
  • Solifenacin
  • Sorafenib
  • Sotalol
  • Sparfloxacin
  • Sufentanil
  • Sunitinib
  • Tacrolimus
  • Tamoxifen
  • Tapentadol
  • Telaprevir
  • Telavancin
  • Telithromycin
  • Telotristat Ethyl
  • Terbutaline
  • Tetrabenazine
  • Thiazide diuretics
  • Thioridazine
  • Tiotropium; Olodaterol
  • Tolterodine
  • Toremifene
  • Torsemide
  • Tramadol
  • Tranylcypromine
  • Trazodone
  • Triclabendazole
  • Tricyclic antidepressants
  • Trifluoperazine
  • Triptorelin
  • Tucatinib
  • Umeclidinium; Vilanterol
  • Vandetanib
  • Vardenafil
  • Vemurafenib
  • Venlafaxine
  • Vilazodone
  • Voriconazole
  • Vorinostat
  • Vortioxetine
  • Ziprasidone
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