Abiraterone

Abiraterone Brand Names – Yonsa and ZYTIGA

What is Abiraterone

Abiraterone acetate inhibits 17 a-hydroxylase/C17,20-lyase (CYP17), which is an enzyme that is required for androgen biosynthesis and is expressed in testicular, adrenal, and prostatic tumor tissues.

Abiraterone is used in combination with a corticosteroid for the treatment of metastatic castration-resistant prostate cancer (CRPC) either as first-line therapy, or after progression with docetaxel.

There are 2 formulations of abiraterone acetate (Zytiga and Yonsa), which have different dosing recommendations and different food effects; one formulation should not be substituted for the other.

Abiraterone should be used with caution in patients with a history of cardiovascular disease, as it may cause hypertension, hypokalemia, and fluid retention and its safety in patients with heart failure was not established in clinical trials.

Indications

  • prostate cancer

For the treatment of metastatic prostate cancer

for the treatment of metastatic high risk hormone-sensitive prostate cancer, in combination with prednisone and androgen-deprivation therapy

Side Effects

  1. adrenocortical insufficiency
  2. anemia
  3. angina
  4. arthralgia
  5. arthralgia
  6. atrial fibrillation
  7. atrial flutter
  8. atrial tachycardia
  9. AV block
  10. bone fractures
  11. bradycardia
  12. cardiac arrest
  13. cardiomyopathy
  14. chest pain (unspecified)
  15. chest pain (unspecified)
  16. constipation
  17. constipation
  18. cough
  19. diarrhea
  20. diarrhea
  21. dyspepsia
  22. dyspnea
  23. dyspnea
  24. edema
  25. edema
  26. elevated hepatic enzymes
  27. elevated hepatic enzymes
  28. fatigue
  29. fatigue
  30. fever
  31. fever
  32. fluid retention
  33. headache
  34. headache
  35. heart failure
  36. heart failure
  37. hematuria
  38. hematuria
  39. hepatic failure
  40. hepatitis
  41. hepatotoxicity
  42. hot flashes
  43. hot flashes
  44. hyperbilirubinemia
  45. hyperbilirubinemia
  46. hypercholesterolemia
  47. hyperglycemia
  48. hyperglycemia
  49. hypernatremia
  50. hypernatremia
  51. hypertension
  52. hypertension
  53. hypertriglyceridemia
  54. hypertriglyceridemia
  55. hypokalemia
  56. hypokalemia
  57. hypophosphatemia
  58. hypophosphatemia
  59. increased urinary frequency
  60. increased urinary frequency
  61. infection
  62. infection
  63. insomnia
  64. insomnia
  65. lymphopenia
  66. lymphopenia
  67. musculoskeletal pain
  68. musculoskeletal pain
  69. myalgia
  70. myalgia
  71. myopathy
  72. nocturia
  73. peripheral edema
  74. pharyngitis
  75. pneumonitis
  76. QT prolongation
  77. rash
  78. respiratory arrest
  79. rhabdomyolysis
  80. sinus tachycardia
  81. supraventricular tachycardia (SVT)
  82. torsade de pointes
  83. ventricular tachycardia
  84. vomiting

Monitoring Parameters

  • blood pressure
  • LFTs
  • serum potassium

Contraindications

  • adrenal insufficiency
  • breast-feeding
  • cardiac disease
  • contraception requirements
  • females
  • heart failure
  • hepatic disease
  • hepatitis
  • hepatotoxicity
  • hypertension
  • hypokalemia
  • infection
  • infertility
  • male-mediated teratogenicity
  • myocardial infarction
  • pregnancy
  • reproductive risk
  • surgery
  • treatment outside of a clinical trial
  • ventricular arrhythmias

Interactions

  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Codeine
  • Acetaminophen; Dextromethorphan
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
  • Acetaminophen; Dextromethorphan; Phenylephrine
  • Acetaminophen; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Tramadol
  • Alogliptin; Pioglitazone
  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amoxapine
  • Apalutamide
  • Aripiprazole
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Brexpiprazole
  • Brompheniramine; Dextromethorphan; Guaifenesin
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Carbamazepine
  • Carbinoxamine; Dextromethorphan; Pseudoephedrine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Cevimeline
  • 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
  • Clomipramine
  • Clozapine
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Desipramine
  • Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Dextromethorphan
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Guaifenesin
  • Dextromethorphan; Guaifenesin; Phenylephrine
  • Dextromethorphan; Guaifenesin; Potassium Guaiacolsulfonate
  • Dextromethorphan; Guaifenesin; Pseudoephedrine
  • Dextromethorphan; Promethazine
  • Dextromethorphan; Quinidine
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Doxepin
  • Doxorubicin
  • Dutasteride; Tamsulosin
  • Elbasvir; Grazoprevir
  • Eliglustat
  • Enzalutamide
  • Flecainide
  • Fluvoxamine
  • Fosphenytoin
  • Gefitinib
  • Glimepiride; Pioglitazone
  • Glimepiride; Rosiglitazone
  • 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
  • Imipramine
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Lesinurad
  • Lesinurad; Allopurinol
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • Maprotiline
  • Mephobarbital
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Methadone
  • Metoprolol
  • Mitotane
  • Nanoparticle Albumin-Bound Paclitaxel
  • Nebivolol
  • Nebivolol; Valsartan
  • Nortriptyline
  • Omeprazole; Amoxicillin; Rifabutin
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenobarbital
  • Phenytoin
  • Pimozide
  • Pioglitazone
  • Pitavastatin
  • Primidone
  • Propranolol
  • Protriptyline
  • Quinine
  • Radium-223 Dichloride
  • Repaglinide
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Rosiglitazone
  • St. John’s Wort, Hypericum perforatum
  • Tamsulosin
  • Telotristat Ethyl
  • Thioridazine
  • Tramadol
  • Trimipramine
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