ESTROGENS & PROGESTERONS (progestins)

Question 1

NATURAL estrogens: (drug names)

Answer 1

1. estradiol (estradiol-17 beta, E2)
   
   • PRE-menopausal
   • most potent
   • produced & secreted by the ovaries
2. estrone (E1)
   
   • POST-menopausal
   • from conversion of androstenedione in peripheral tissues
3. estriol (E3)
   
   • ass. with PREGNANCY
   • produced by the placenta

Question 2

SYNTHETIC estrogens: (drug names)

Answer 2

steroidal:

1. ethinyl estradiol (EE)
2. mestranol
3. quinestrol (a prodrug of ethinyl estradiol)
4. estradiol valerate

non-steroidal:

1. diethylstilbestrol
2. chlorotrianisene
3. methallenestril
4. genistein

Question 3

NATURAL & SYNTHETIC estrogens → pharmacokinetics:

Answer 3

NATURAL estrogens:

1. absorbed trough GIT, skin, mucous
2. rapidly metabolized when taken ORALLY
3. micronized estradiol → better bioavailability

SYNTHETIC estrogens:

1. well absorbed when taken ORALLY
2. metabolized more slowly
3. prolonged action & higher potency than natural estrogens

Question 4

NATURAL & SYNTHETIC estrogens → indications:

Answer 4

1. postmenopausal hormone therapy
2. primary hypogonadism
3. contraception (together with progestogen)
4. osteoporosis
5. suppression of ovulation in patients with intractable dysmenorrhea
6. atrophic vaginitis
7. premature menopause
8. premature ovarian failure

Question 5

NATURAL & SYNTHETIC estrogens → CONTRAindications:

Answer 5

1. estrogen-dependent neoplasms (= endometrial)
2. high risk of breast cancer
3. undiagnosed genital bleeding
4. liver disease
5. thromboembolic disorders

Question 6

NATURAL & SYNTHETIC estrogens → side effects:

Answer 6

1. nausea
2. breast tenderness
3. hyperpigmentation
4. migraine headaches
5. peripheral edema
6. breast cancer
7. endometrial cancer
8. thromboembolism
9. hypertension
10. MI
11. gall bladder disease

Question 7

NATURAL progestogens: (drug names)

Answer 7

1. progesterone
2. hydroxyprogesterone hexanoate
3. medroxyprogesterone

Question 8

SYNTHETIC progestogens = PROGESTINS: (drug names)

Answer 8

1. desogestrel
2. dienogest
3. drospirenone
4. levonorgestrel
5. norethindrone
6. norethindrone acetate
7. norgestimate
8. norgestrel
9. medroxyprogesterone acetate
10. gestodene
11. norethisterone

Question 9

NATURAL & SYNTHETIC progesterons → indications:

Answer 9

1. contraception (together with estrogen)
2. hormone deficiency
3. dysmenorrhea
4. endometriosis
5. bleeding disorders
6. management of infertility
7. prevention of threatened miscarriage

Question 10

NATURAL & SYNTHETIC progesterons → side effects:

Answer 10

1. headache
2. depression
3. weight gain
4. change in libido
5. acne & hirsutism (norethindrone, norethindrone acetate, norgestrel, levonorgestrel & other testosterone derivatives)
6. increased risk of hyperkalemia (drospirenone)
7. increase LDL, decrease HDL
8. increase body temp 0,5-1,0°C
9. some have mild mineralocorticoid activity

Question 11

gestodene & desogestrel VS. older testosterone derivatives:

Answer 11

1. less effect on lipids
2. less acne, depression & breakthrough bleeding
3. higher risk of venous thromboembolism