bicalutamide B, Casodex

 Indications

Treatment of metastatic prostate carcinoma in conjunction

with luteinizing hormone–releasing hormone

(LHRH) analogs (goserelin, leuprolide).

Action

Antagonizes the effects of androgen at the cellular level.

Therapeutic Effects: Decreased spread of prostate

carcinoma.

Pharmacokinetics

Absorption: Well absorbed after oral administration.

Distribution: Unknown.

Protein Binding: 96%.

Metabolism and Excretion: Mostly metabolized

by the liver.

Half-life: 5.8 days.

TIME/ACTION PROFILE (blood levels)

ROUTE ONSET PEAK DURATION

PO unknown 31.3 hr unknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Women.

Use Cautiously in: Moderate to severe liver impairment;

Rep: Men with female partners of reproductive

potential; Pedi: Safety not established.

Adverse Reactions/Side Effects

CNS: weakness, dizziness, headache, insomnia. Resp:

dyspnea. CV: chest pain, hypertension, peripheral

edema. GI: HEPATOTOXICITY, constipation, diarrhea,

nausea, abdominal pain,qliver enzymes, vomiting.

GU: erectile dysfunction,pfertility, hematuria, incontinence,

nocturia, urinary tract infections. Derm: alopecia,

photosensitivity, rash, sweating. Endo: breast

pain, gynecomastia. Hemat: anemia.Metab: hyperglycemia,

weight loss. MS: back pain, pelvic pain, bone

pain. Neuro: paresthesia. Misc: generalized pain,

hot flashes, flu-like syndrome, infection.

Interactions

Drug-Drug: Mayqthe effect of warfarin.

Route/Dosage

PO (Adults): 50 mg once daily (must be given concurrently

with LHRH analog).

Availability (generic available)

Tablets: 50 mg.