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