Bicalutamide

Bicalutamide Brand Name– Casodex

What is Bicalutamide

Bicalutamide is an oral nonsteroidal antiandrogen structurally related to flutamide (Eulexin(R)).

Bicalutamide is used as an antihormonal agent in the treatment of metastatic prostatic carcinoma.

Unlike flutamide, bicalutamide has a long plasma half-life that allows once-daily dosing compared with three times daily for flutamide.

In addition, bicalutamide is more selective for the peripheral androgen receptor and has less activity at the central androgen receptor on the hypothalamic-pituitary axis.

Bicalutamide is most effective when combined with LHRH agonists such as leuprolide acetate. The FDA approved bicalutamide on October 4, 1995, for the treatment of advanced prostatic carcinoma.

While a 150 mg dosage form was once under investigation as monotherapy or in combination with other drugs for select stages of prostate cancer, this dosage is not FDA-approved and select clinical trials have found significant trends in terms of increased mortality/decreased survival in the bicalutamide-treated group at the 150 mg-dosage versus patients undergoing castration or other treatments.

Indications

  • prostate cancer
  • stuttering priapism

For the treatment of stage D-2 metastatic prostate cancer in combination with a luteinizing hormone-releasing hormone (LHRH) analog

Side Effects

  1. abdominal pain
  2. alopecia
  3. anemia
  4. angina
  5. angioedema
  6. anorexia
  7. anxiety
  8. arthralgia
  9. asthenia
  10. back pain
  11. bone fractures
  12. bone pain
  13. cardiac arrest
  14. cataracts
  15. chest pain (unspecified)
  16. chills
  17. confusion
  18. constipation
  19. cough
  20. dehydration
  21. depression
  22. diabetes mellitus
  23. diaphoresis
  24. diarrhea
  25. dizziness
  26. drowsiness
  27. dyspepsia
  28. dysphagia
  29. dyspnea
  30. dysuria
  31. edema
  32. elevated hepatic enzymes
  33. epistaxis
  34. fever
  35. flatulence
  36. GI bleeding
  37. gout
  38. gynecomastia
  39. headache
  40. heart failure
  41. hematuria
  42. hepatic failure
  43. hepatitis
  44. hot flashes
  45. hyperbilirubinemia
  46. hypercholesterolemia
  47. hyperglycemia
  48. hypertension
  49. hypertonia
  50. impotence (erectile dysfunction)
  51. increased urinary frequency
  52. infection
  53. insomnia
  54. libido decrease
  55. melena
  56. muscle cramps
  57. myalgia
  58. myasthenia
  59. myocardial infarction
  60. nausea
  61. neutropenia
  62. new primary malignancy
  63. nocturia
  64. paresthesias
  65. peripheral edema
  66. pharyngitis
  67. photosensitivity
  68. pneumonitis
  69. pruritus
  70. pulmonary fibrosis
  71. rash
  72. rhinitis
  73. sinusitis
  74. syncope
  75. urinary incontinence
  76. urinary retention
  77. urinary urgency
  78. urticaria
  79. vomiting
  80. weight gain
  81. weight loss
  82. xerosis
  83. xerostomia

Monitoring Parameters

  • LFTs
  • prostate-specific antigen (PSA)

Contraindications

  • breast-feeding
  • children
  • contraception requirements
  • diabetes mellitus
  • females
  • hepatic disease
  • hepatitis
  • infertility
  • jaundice
  • male-mediated teratogenicity
  • pregnancy
  • reproductive risk

Interactions

  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Oxycodone
  • Amiodarone
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Oxycodone
  • Barbiturates
  • Benzhydrocodone; Acetaminophen
  • Bosentan
  • Carbamazepine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Clarithromycin
  • Delavirdine
  • Dexamethasone
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Eliglustat
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Fluconazole
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fosphenytoin
  • grapefruit juice
  • Ibuprofen; Oxycodone
  • Imatinib
  • Itraconazole
  • Ketoconazole
  • Lomitapide
  • Mifepristone
  • Nefazodone
  • Nevirapine
  • Nisoldipine
  • Oxycodone
  • Phenytoin
  • Protease inhibitors
  • Rifamycins
  • St. John’s Wort, Hypericum perforatum
  • Sufentanil
  • Ubrogepant
  • Vinorelbine
  • Voriconazole
  • Warfarin
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