Drug information of Bicalutamide

Mechanism of effect

Androgen receptor inhibitor; pure nonsteroidal antiandrogen that binds to androgen receptors; specifically a competitive inhibitor for the binding of dihydrotestosterone and testosterone; prevents testosterone stimulation of cell growth in prostate cancer

Pharmacodynamic

Bicalutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer.

Pharmacokinetics

Absorption:Well absorbed; unaffected by food
Metabolism:Extensively hepatic; glucuronidation and oxidation of the R (active) enantiomer to inactive metabolites; the S enantiomer is inactive.
Excretion:Urine and feces
Time to Peak:Active enantiomer: ~31 hours
Protein Binding:96%
Half-Life Elimination:Active enantiomer: ~6 days.

Drug indications

Prostate Cancer

Dosage

Prostate cancer, metastatic: Adults: Oral: 50 mg once daily (in combination with an LHRH analogue)
Prostate cancer, locally advanced, high recurrence risk (off-label use): Adults: Oral: 150 mg once daily (as monotherapy) (McLeod, 2006). Additional trials may be necessary to further define the role of bicalutamide in this condition.

Drug contraindications

Pregnancy , hypersensitivity to drug or its components. , use in women

Side effects

nausea , Headache , insomnia , chest pain , constipation , Hematuria , abdominal pain , dizziness , vomiting , rash , flushing , Depression , Diarrhea , Dyspnea , Chills , pruritus , Hypertension , anemia , paresthesia , neuropathy , dyspepsia , Urinary tract infection , edema , Peripheral edema , impotence , weight decrease , Hypertonia , anxiety , confusion , Alopecia , Infections , anorexia , Gynecomastia , dehydration , back pain , Pain , Hyperglycemia , syncope , dysphagia , urinary retention , coronary artery disease, , Angina pectoris , Cataracts , flatulence , Weight increase , MI , decreased libido , mastalgia , cardiac failure , weakness

Interactions

Aripiprazole , Pimozide , Nimodipine , Warfarin , fentanyl , Mipomersen , Axitinib , Dolasetron , vandetanib , Dofetilide , triparanol , Halofantrine , Grepafloxacin , aminolevulinic acid oral , Aminolevulinic acid topical , Terfenadine , Flibanserin , Entrectinib , Nilutamide , Methyl aminolevulinate , Bepridil , bedaquiline , Gefitinib , Remdesivir , Cannabidiol , Avapritinib

Alerts

1-Use with caution in patients with moderate-to-severe hepatic impairment
2-Treatment for metastatic cancer should be started concomitantly with an LHRH analogue.
3-May cause gynecomastia or breast pain at higher (off-label) doses.
4- Anemia may occur with testosterone suppression; monitor CBC periodically as indicated.
5-May lead to spermatogenesis inhibition.

Points of recommendation

1-Dose should be taken at the same time each day, either in the morning or in the evening.
2-May be administered with or without food.

Pregnancy level

X

Related drugs

Apalutamide