Progestins, Estrogens, and Androgens

Question 1

What are the main actions of Estrogen/Estradiol?

Answer 1

• Promote endometrial proliferation during the follicular phase (1st half) of the menstrual cycle
• Negative feedback on GnRH and FSH/LH secretion
• Decrease bone resorption (Osteoclast activity)
• Increase clotting factors and risk for thromboembolism
• Increase endometrial and breast CA

Question 2

What are the main actions of Progesterone?

Answer 2

• Promote endometrial development during the luteal phase (2nd half) of the menstrual cycle
• Decrease amount of cervical mucus and increase viscosity of cervical mucus
• Negative feedback on GnRH and FSH/LH secretion
• Important in placenta for maintenance of pregnancy

Question 3

What types of drugs can be used for contraception?

Answer 3

Progesterone, Estrogen, Combinations, and Selective Progesterone Receptor Modulators (SPRMs)

Question 4

What types of drugs can be used for suppression of the Hypothalamic-Pituitary-Gonadal (HPG) axis?

Answer 4

Progesterone and Estrogen

Question 5

What types of drugs can be used for replacement therapy?

Answer 5

Progesterone, Estrogen, and Selective Estrogen Receptor Modulators (SERMs)

Question 6

What types of drugs can be used for breast CA therapy?

Answer 6

SERMs and Aromatase Inhibitors

Question 7

What types of drugs can be used for ovulation induction?

Answer 7

Estrogen Antagonists and Aromatase Inhibitors

Question 8

What types of drugs can be used for Abortions?

Answer 8

Progesterone Antagonists

Question 9

Estradiol or Ethinyl estradiol

1) Use
2) Mechanism of Action
3) Adverse Effects

Answer 9

1)Combination-type Contraceptive Agent w/Progestin
2)Prevent ovulation by inhibiting the hypothalamus and pituitary
Progestin decreases amount and increases viscosity of cervical mucus
3)Thromboembolism-mostly in smokers over 35 years old

Question 10

Norethindrone or Norgestrel

1) Use
2) Mechanism of Action
3) Adverse Effect

Answer 10

1) Progestin-ONLY Contraception
2) Prevent fertilization by decreasing the amount and increasing the viscosity of cervical mucus
3) Abnormal menstrual bleeding

Question 11

Medroxyprogesterone acetate (Depo-Provera)

1) Use
2) Mechanism of Action
3) Adverse Effect

Answer 11

1) Progestin-ONLY Contraception (IM injection)
2) Prevent fertilization by decreasing the amount and increasing the viscosity of cervical mucus
3) Decreased bone density

Question 12

What drugs can decrease the efficacy of combination-type contraceptives?

Answer 12

• Rifampin

- Anticonvulsants (via CYP3A4)

Question 13

What is another use of norgestrel when given in VERY high dose? What is the mechanism of action in high doses? What is the most common adverse effect?

Answer 13

• Emergency Contraceptive
• Suppression of the hypothalamic-pituitary-gonadal axis therefore inhibiting ovulation
• Nausea and Vomiting

Question 14

Ulipristal

1) Use
2) Mechanism of Action

Answer 14

1)Emergency Contraceptive
2)Selective Progesterone Receptor Modulator (SPRM)-inhibits ovulation by antagonizing the actions of progesterone on the granulosa cell progesterone receptor
Also a Progesterone agonist in the pituitary/hypothalamus and therefore delays the LH surge

Question 15

Estrone Sulfate

1)Use

Answer 15

1) Treatment of postmenopausal symptoms and postmenopausal osteoporosis
* Use lowest effective dose and shortest duration possible

Question 16

Raloxifene

1) Use
2) Mechanism of Action

Answer 16

1) Relief of Postmenopausal symptoms, Osteoporosis, Estrogen-dependent breast CA in Postmenopausal women
2) Selective Estrogen Receptor Modulator (SERM) and Estrogen Receptor Antagonist

Question 17

Tamoxifen

1) Use
2) Mechanism of Action

Answer 17

1) Relief of Postmenopausal symptoms, Osteoporosis, Estrogen-dependent breast CA
2) Selective Estrogen Receptor Modulator (SERM) and Estrogen Receptor Antagonist

Question 18

Bazedoxifene

1) Use
2) Mechanism of Action

Answer 18

1)Postmenopausal symptoms
2)Selective Estrogen Receptor Modulator (SERM) and Estrogen Receptor Antagonist
Also has Agonist effects on bone

Question 19

Clomiphene

1) Use
2) Mechanism of Action

Answer 19

1) Induction of ovulation
2) Estrogen Receptor Antagonist-Antagonizes the inhibitory effects of estrogen on the pituitary and hypothalamus
* Do NOT use long-term!

Question 20

Exemestane

1) Use
2) Mechanism of Action

Answer 20

1) Breast CA in Postmenopausal women, Induce ovulation

2) Steroidal Aromatase Inhibitor-inhibits the conversion of androgens to estrogens

Question 21

Letrozole

1) Use
2) Mechanism of Action

Answer 21

1) Breast CA in Postmenopausal women, Induce ovulation

2) Non-steroidal Aromatase Inhibitor-inhibits the conversion of androgens to estrogens

Question 22

RU486/mifepristone

1) Use
2) Mechanism of Action

Answer 22

1) Abortions
2) Progesterone Receptor Antagonist-antagonizes progesterone actions everywhere including the endometrium
* Also has a glucocorticoid antagonist activity so can be used for Cushing syndrome and Type 2 DM

Question 23

What are the main actions of Androgens?

Answer 23

• Puberty in males
• Maintenance of secondary sexual characteristics and accessory organs in males
• Promote anabolic reactions throughout the body

Question 24

What are the uses of Androgen therapy?

Answer 24

• Replacement therapy in male hypogonadism (low androgen levels)
• Treatment of catabolic states such as muscle wasting associated w/AIDS

Question 25

Finasteride

1) Use
2) Mechanism of Action

Answer 25

1) Syndromes of androgen excess like BPH, prostate CA, hirsutism, congenital androgen hyperplasia, male precocious puberty
2) 5-alpha Reductase Inhibitor-inhibit 5-alpha reductase enzyme to prevent conversion of testosterone to dihydrotestosterone

Question 26

Flutamide

1) Use
2) Mechanism of Action

Answer 26

1) Syndromes of androgen excess like BPH, prostate CA, hirsutism, congenital androgen hyperplasia, male precocious puberty
2) Androgen Receptor Antagonists-directly bind to the androgen receptor and block all activity at the receptor

Question 27

Bicalutamide

1) Use
2) Mechanism of Action

Answer 27

1) Syndromes of androgen excess like BPH, prostate CA, hirsutism, congenital androgen hyperplasia, male precocious puberty
2) Androgen Receptor Antagonists-directly bind to the androgen receptor and block all activity at the receptor

Question 28

FSH

1)Use

Answer 28

1)Induce follicular growth prior to in vitro fertilization

Question 29

CG

1) Use
2) Mechanism of Action

Answer 29

1) Induce ovulation (release of mature eggs) prior to in vitro fertilization
2) Acts on the LH receptor

Question 30

Gonadorelin

1) Use
2) Mechanism of Action

Answer 30

1) Delayed puberty, Anovulatory disorders
2) Synthetic GnRH-stimulates gonadotropin secretion
* Administered in pulsatile fashion

Question 31

Cetrorelix

1) Use
2) Mechanism of Action

Answer 31

1) Precocious puberty in boys, Endometriosis, Dysmenorrhea

2) GnRH Antagonist-shuts down hypothalamic-pituitary axis by blocking the GnRH receptor to reduce gonadotropin secretion

Question 32

Luprolide

1) Use
2) Mechanism of Action

Answer 32

1) Precocious puberty in boys, Endometriosis, Dysmenorrhea
2) Long-acting Synthetic GnRH Agonist-initially stimulates gonadotropin secretion then suppresses it d/t long-acting desensitization

Question 33

Methyltestosterone

1) Mechanism of Action
2) Adverse Effects

Answer 33

1) 17-alpha-Alkylated Androgen
2) Hepatic Toxicity
* Can be given orally unlike testosterone

Question 34

Danazol

1) Mechanism of Action
2) Adverse Effects

Answer 34

1) 17-alpha-Alkylated Androgen
2) Hepatic Toxicity
* Can be given orally unlike testosterone

Question 35

Testosterone

1)Route of Administration

Answer 35

1)Transdermal, Buccal tablets