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