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What is Rolapitant
Rolapitant is a substance P/neurokinin 1 (NK1) receptor antagonist that is used in adults in combination with dexamethasone and a 5-HT3 receptor antagonist for the prevention of chemotherapy-induced delayed nausea and vomiting.
Rolapitant inhibits the CYP2D6 enzyme, Breast-Cancer-Resistant Protein (BCRP), and P-gp.
Rolapitant is contraindicated with CYP2D6 substrates with a narrow therapeutic index, such as thioridazine and pimozide, due to an increased risk of QT prolongation.
Brand Name
Varubi
Indications
- chemotherapy-induced nausea/vomiting prophylaxis
For delayed chemotherapy-induced nausea/vomiting prophylaxis, in combination with other antiemetic agents
for delayed chemotherapy-induced nausea/vomiting prophylaxis associated with highly emetogenic chemotherapy
Side Effects
- abdominal pain
- anaphylactoid reactions
- anemia
- anorexia
- dizziness
- dyspepsia
- hiccups
- infection
- infusion-related reactions
- neutropenia
- stomatitis
Monitoring Parameters
- LFTs
Contraindications
- breast-feeding
- children
- infants
- infertility
- neonates
- pregnancy
- serious hypersensitivity reactions or anaphylaxis
- soya lecithin hypersensitivity
Interactions
- Acetaminophen; Butalbital; Caffeine; Codeine
- Acetaminophen; Caffeine; Dihydrocodeine
- Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
- Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
- Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
- Acetaminophen; Codeine
- Acetaminophen; Dextromethorphan
- Acetaminophen; Dextromethorphan; Doxylamine
- Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
- Acetaminophen; Dextromethorphan; Phenylephrine
- Acetaminophen; Dextromethorphan; Pseudoephedrine
- Acetaminophen; Diphenhydramine
- Acetaminophen; Hydrocodone
- Acetaminophen; Oxycodone
- Acetaminophen; Tramadol
- Afatinib
- Alpelisib
- Amitriptyline
- Amitriptyline; Chlordiazepoxide
- Apalutamide
- Aprepitant, Fosaprepitant
- Aripiprazole
- Asenapine
- Aspirin, ASA; Butalbital; Caffeine; Codeine
- Aspirin, ASA; Caffeine; Dihydrocodeine
- Aspirin, ASA; Carisoprodol; Codeine
- Aspirin, ASA; Oxycodone
- Atazanavir; Cobicistat
- Atomoxetine
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Betrixaban
- Brexpiprazole
- Brimonidine; Timolol
- Brompheniramine; Dextromethorphan; Guaifenesin
- Brompheniramine; Guaifenesin; Hydrocodone
- Brompheniramine; Hydrocodone; Pseudoephedrine
- Carbamazepine
- Carbetapentane; Chlorpheniramine
- Carbetapentane; Chlorpheniramine; Phenylephrine
- Carbetapentane; Diphenhydramine; Phenylephrine
- Carbinoxamine; Dextromethorphan; Pseudoephedrine
- Carbinoxamine; Hydrocodone; Phenylephrine
- Carbinoxamine; Hydrocodone; Pseudoephedrine
- Carvedilol
- Cevimeline
- Chlorpheniramine
- Chlorpheniramine; Codeine
- Chlorpheniramine; Dextromethorphan
- Chlorpheniramine; Dextromethorphan; Phenylephrine
- Chlorpheniramine; Dihydrocodeine; Phenylephrine
- Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
- Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
- Chlorpheniramine; Hydrocodone
- Chlorpheniramine; Hydrocodone; Phenylephrine
- Chlorpheniramine; Hydrocodone; Pseudoephedrine
- Chlorpheniramine; Phenylephrine
- Chlorpheniramine; Pseudoephedrine
- Chlorpromazine
- Cinacalcet
- Clomipramine
- Clozapine
- Cobicistat
- Cobimetinib
- Codeine
- Codeine; Guaifenesin
- Codeine; Phenylephrine; Promethazine
- Codeine; Promethazine
- Cyclosporine
- Dabigatran
- Darifenacin
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Delavirdine
- Desipramine
- Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
- Dextromethorphan
- Dextromethorphan; Diphenhydramine; Phenylephrine
- Dextromethorphan; Guaifenesin
- Dextromethorphan; Guaifenesin; Phenylephrine
- Dextromethorphan; Guaifenesin; Potassium Guaiacolsulfonate
- Dextromethorphan; Guaifenesin; Pseudoephedrine
- Dextromethorphan; Promethazine
- Dextromethorphan; Quinidine
- Digoxin
- Dihydrocodeine; Guaifenesin; Pseudoephedrine
- Diphenhydramine
- Diphenhydramine; Hydrocodone; Phenylephrine
- Diphenhydramine; Ibuprofen
- Diphenhydramine; Naproxen
- Diphenhydramine; Phenylephrine
- Docetaxel
- Donepezil
- Donepezil; Memantine
- Doravirine; Lamivudine; Tenofovir disoproxil fumarate
- Dorzolamide; Timolol
- Doxepin
- Doxorubicin
- Duloxetine
- Dutasteride; Tamsulosin
- 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 disoproxil fumarate
- Emtricitabine; Tenofovir disoproxil fumarate
- Encainide
- Enzalutamide
- Flecainide
- Fluoxetine
- Fluoxetine; Olanzapine
- Fluphenazine
- Fluticasone; Umeclidinium; Vilanterol
- Fluvoxamine
- Fosamprenavir
- Fosphenytoin
- Gefitinib
- Glyburide
- Glyburide; Metformin
- Guaifenesin; Hydrocodone
- Guaifenesin; Hydrocodone; Pseudoephedrine
- Haloperidol
- Homatropine; Hydrocodone
- Hydrochlorothiazide, HCTZ; Metoprolol
- Hydrochlorothiazide, HCTZ; Propranolol
- Hydrocodone
- Hydrocodone; Ibuprofen
- Hydrocodone; Phenylephrine
- Hydrocodone; Potassium Guaiacolsulfonate
- Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
- Hydrocodone; Pseudoephedrine
- Ibuprofen; Oxycodone
- Iloperidone
- Imatinib
- Imipramine
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Lamivudine; Tenofovir Disoproxil Fumarate
- Lapatinib
- Ledipasvir; Sofosbuvir
- Lesinurad
- Lesinurad; Allopurinol
- Lofexidine
- Loperamide
- Loperamide; Simethicone
- Maprotiline
- Maraviroc
- Meclizine
- Meperidine; Promethazine
- Mephobarbital
- Methadone
- Methotrexate
- Metoprolol
- Mexiletine
- Mirtazapine
- Mitotane
- Morphine
- Morphine; Naltrexone
- Nebivolol
- Nebivolol; Valsartan
- Nortriptyline
- Olanzapine
- Ondansetron
- Oxycodone
- Ozanimod
- Paclitaxel
- Paroxetine
- Pazopanib
- Pentamidine
- Perphenazine
- Perphenazine; Amitriptyline
- Phenobarbital
- Phenylephrine; Promethazine
- Phenytoin
- Pimozide
- Pirfenidone
- Primidone
- Promethazine
- Propafenone
- Propranolol
- Protriptyline
- Quinidine
- Ranolazine
- Rifampin
- Rimegepant
- Risperidone
- Rosuvastatin
- Sertraline
- Sirolimus
- Sofosbuvir
- Sofosbuvir; Velpatasvir
- Sofosbuvir; Velpatasvir; Voxilaprevir
- St. John’s Wort, Hypericum perforatum
- Sulfasalazine
- Talazoparib
- Tamsulosin
- Telotristat Ethyl
- Temsirolimus
- Tenofovir Alafenamide
- Tenofovir, PMPA
- Tetrabenazine
- Thioridazine
- Timolol
- Tolterodine
- Topotecan
- Tramadol
- Trimipramine
- Umeclidinium
- Umeclidinium; Vilanterol
- Vemurafenib
- Venetoclax
- Venlafaxine
- Vinblastine
- Vincristine
- Vincristine Liposomal
- Vortioxetine
- Warfarin
- Yohimbine