hormonal therapy and cancer tx

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Created by:

monty1313  on May 13, 2011

Subjects:

reproductive pharmacology

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hormonal therapy and cancer tx

Control of female hormones
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Control of female hormones
-pic
control of androgen secretions
-pic
Leuprolide
-mechanism
-use
-toxicity
Mechanism: GnRH analog w/ antagonist properties

Special:
1)Agonist properties when used pulsatile
2)Antagonist properties when used continuous

Use:
1)Infertility (pulsatile)
2)Prostate cancer(continuous)
3)Uterine fibroids

Toxicity:
-Anti-androgen
-nausea
-vomiting
Testosterone (methyltestosterone)
-mechanism
-use
-toxicity
Mechanism: Androgen receptor agonist

Use:
1)hypogonadism
2)stimulate anabolism to promote burn recovery
3)treat ER-positive breast cancer

Toxicity:
Females--> masculinization

Males-->Gonadal atrophy
*inhibiting release of LH which results in reduced intra-testicular testosterone
Antiandrogens1)Finasteride
2)Flutamide
3)Ketoconazole
4)Spironalactone
Finastaride5α-reductase inhibitor (↓ conversion of testosterone to dihydrotestosterone)

Use: BPH, male pattern baldness

Toxicity: promotes female breast growth
Flutamidenonsteroidal competitive inhibitor of androgens at the testosterone receptor

Use: prostate carcinoma
Ketoconazole and Spironolactone
-mech
-use
-toxicity
Ketoconazole: inhibits steroid synthesis (desmolase)
Spironolactone: inhibits steroid binding

Use: used in polycystic ovarian syndrome to prevent hirsutism

Toxicity:
-Gynecomastia
-Amenorrhea
Estrogens
-drugs
-mechanism
-clinical use
-toxicity
-contraindications
Drugs: ethinyl estradiol, diethylstilbestrol (DES), mestranol

Mechanism: bind estrogen receptors

Use:
1)Hypogonadism or ovary failure
2)menstrual abnormality
3)HRT in postmenopausal women

MEN: men with androgen dependent prostate cancer

Toxicity:
1)increase risk of endometrial cancer
2)bleeding in postmenopausal women
3)increased risk of thrombi

Contra:
1)ER-positive breast cancer
2)history of DVTs
Selective estrogen receptor modulators
-what
-who
What: estrogen partial agonists

Who:
1)Clomiphene
2)Tamoxifen
3)Raloxifene
Clomiphene
-what
-use
-toxicity
What: partial agonist at estrogen receptors in hypothalamus

Use: prevents normal feedback inhibitions and ↑ release of LH and FSH from pituitary which stimulates ovulation
**used for infertility and PCOS

Toxicity:
-hot flashes
-ovarian enlargement
-multiple pregnancies
-visual disturbances
Tamoxifen
-what
-use
What: Antagonist on breast tissue

Use: treat and prevent recurrence of ER-positive breast cancer
Raloxifene
-what
-use
What: Agonist on bone

Use: tx osteoporosis by ↓ bone resorption
Hormone Replacement Therapy
-use
-dangers
Use: to relive or prevent menopausal symptoms and osteoporosis (↑estrogen = ↓osteoclast activity)

Danger: unopposed estrogen replacement ↑ risk of endometrial cancer
Anastrozole/exemestaneAromatase inhibitors used in postmenopausal women with breast cancer
Progestins
-mechanism
-use
Mechanism: bind progesterone receptors
-reduces growth and ↑ vascularization of endometrium

Use:
1)oral contraceptive
2)tx of endometrial cancer
3)tx for abnormal uterine bleeding

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