Prostate Cancer - Medications

bicalutamide - Casodex ® flutamide - Eulexin ®
goserelin - Zoladex ® leuprolide - Lupron ®
nilutamide - Nilandron ®  

bicalutamide - Casodex ® top of page icon

Drug Category:  Antineoplastic Agent, Antiandrogen.

Dosing (Adults):  Metastatic prostate cancer: Oral: 50 mg once daily (in combination with an LHRH analogue).  Locally-advanced prostate cancer (unlabeled use): Oral: 150 mg once daily (as monotherapy).
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Use
In combination therapy with LHRH agonist analogues in treatment of advanced prostatic carcinoma

Mechanism of Action
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

Dosing:
Adults: Oral: 50 to 150 mg/day
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Dosage adjustment in liver impairment: Limited data in subjects with severe hepatic impairment suggest that excretion of bicalutamide may be delayed and could lead to further accumulation. Use with caution in patients with moderate to severe hepatic impairment.
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Supplied:  50 mg tablet.

flutamide  - Eulexin ®  top of page icon

Use
Treatment of metastatic prostatic carcinoma in combination therapy with LHRH agonist analogues

Mechanism of Action
Nonsteroidal antiandrogen that inhibits androgen uptake or inhibits binding of androgen in target tissues
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Dosing (Adults)
Oral: Adults:
Prostatic carcinoma: 250 mg 3 times/day

Female hirsutism (unlabeled use): 250 mg daily
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Supplied
Capsule: 125 mg

goserelin - Zoladex ® top of page icon

Use
Palliative treatment of advanced breast cancer and carcinoma of the prostate; treatment of endometriosis, including pain relief and reduction of endometriotic lesions; endometrial thinning agent as part of treatment for dysfunctional uterine bleeding

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Mechanism of Action
Goserelin is a synthetic analog of luteinizing-hormone-releasing hormone (LHRH). Following an initial increase in luteinizing hormone (LH) and follicle stimulating hormone (FSH), chronic administration of goserelin results in a sustained suppression of pituitary gonadotropins. Serum testosterone falls to levels comparable to surgical castration. The exact mechanism of this effect is unknown, but may be related to changes in the control of LH or down-regulation of LH receptors.

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Dosing (Adults)
SubQ: Adults:
Prostate cancer:
Monthly implant: 3.6 mg injected into upper abdomen every 28 days

3-month implant: 10.8 mg injected into the upper abdominal wall every 12 weeks

Note: Treatment should begin 8 weeks prior to radiotherapy in Stage B2-C prostate cancer; treatment may continue indefinitely

Breast cancer, endometriosis, endometrial thinning: Monthly implant: 3.6 mg injected into upper abdomen every 28 days

Note: For breast cancer, treatment may continue indefinitely; for endometriosis, it is recommended that duration of treatment not exceed 6 months. Only 1-2 doses are recommended for endometrial thinning.
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Supplied
Injection, solution, 1-month implant [disposable syringe; single-dose]: 3.6 mg [with 16-gauge hypodermic needle]

Injection, solution, 3-month implant [disposable syringe; single-dose]: 10.8 mg [with 14-gauge hypodermic needle]

leuprolide  - Lupron ®  top of page icon

Use
Palliative treatment of advanced prostate carcinoma; management of endometriosis as initial treatment and/or treatment of recurrent symptoms; preoperative treatment of anemia caused by uterine leiomyomata (fibroids); central precocious puberty

Mechanism of Action
Potent inhibitor of gonadotropin secretion; continuous daily administration results in suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH with subsequent decrease in testosterone (male) and estrogen (female) levels. Leuprolide may also have a direct inhibitory effect on the testes, and act by a different mechanism not directly related to reduction in serum testosterone.
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Dosing (Adults)
Advanced prostatic carcinoma:
SubQ:
Eligard®: 7.5 mg monthly or 22.5 mg every 3 months or 30 mg every 4 months
Lupron®: 1 mg/day
Viadur®: 65 mg implanted subcutaneously every 12 months

I.M.:
Lupron Depot®: 7.5 mg/dose given monthly (every 28-33 days) or
Lupron Depot-3®: 22.5 mg every 3 months or
Lupron Depot-4®: 30 mg every 4 months

Endometriosis: I.M.: Initial therapy may be with leuprolide alone or in combination with norethindrone; if retreatment for an additional 6 months is necessary, norethindrone should be used. Retreatment is not recommended for longer than one additional 6-month course.

Lupron Depot®: 3.75 mg/month for up to 6 months or
Lupron Depot-3®: 11.25 mg every 3 months for up to 2 doses (6 months total duration of treatment)

Uterine leiomyomata (fibroids): I.M. (in combination with iron):
Lupron Depot®: 3.75 mg/month for up to 3 months or
Lupron Depot-3®: 11.25 mg as a single injection

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Supplied
Implant (Viadur®): 65 mg [released over 12 months; packaged with administration kit]

Injection, solution, as acetate (Lupron®): 5 mg/mL (2.8 mL) [contains benzyl alcohol; packaged with syringes and alcohol swabs]

Injection, powder for reconstitution, as acetate [depot formulation; prefilled syringe]:

Eligard®:
7.5 mg [released over 1 month]
22.5 mg [released over 3 months]
30 mg [released over 4 months]

Lupron Depot®: 3.75 mg, 7.5 mg [released over 1 month; contains polysorbate 80]
Lupron Depot®-3 Month: 11.25 mg, 22.5 mg [released over 3 months; contains polysorbate 80]
Lupron Depot®-4 Month: 30 mg [released over 4 months; contains polysorbate 80]
Lupron Depot-Ped®: 7.5 mg, 11.25 mg, 15 mg [released over 1 month; contains polysorbate 80]

nilutamide -  Nilandron ®  top of page icon

Mechanism of Action
Nonsteroidal antiandrogen that inhibits androgen uptake or inhibits binding of androgen in target tissues. It specifically blocks the action of androgens by interacting with cytosolic androgen receptor F sites in target tissue
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Dosing (Adults):
Refer to individual protocols.
Adults: Oral: 300 mg daily for 30 days starting the same day or day after surgical castration, then 150 mg/day
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Supplied
Tablet: 150 mg
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Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.