Estrogens, Progestrins, And Androgens Flashcards

1
Q

What is the main estrogen made by the ovary?

A

Estradiol

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2
Q

What 2 estrogens are made by conversion from androgens in the liver and adrenal glands?

A

Estrone and estriol

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3
Q

Which estrogen is high is high in pregnancy?

A

Estriol

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4
Q

Where is estrogen made in the male?

A

Made by Sertoli cells in the testis

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5
Q

What is the enzyme used to convert testosterone to estrogen in the testis?

A

Aromatase

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6
Q

What are the physiological effects of estrogen?

A
  1. Development of sex organs and secondary sex characteristics
  2. Closure of the epiphyseal plates
  3. Stimulate ductal development in breast
  4. Pigmentation in the skin
  5. Increase binding globulins
  6. Increase HDL, decrease LDL
  7. Reduce bone resorption
  8. Enhance coaguability
  9. Libido, mood
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7
Q

Where is progesterone produced in the female?

A

By the corpus luteum

During pregnancy: placenta

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8
Q

What are the physiological effects of progesterone?

A
  1. Matures endometrium
  2. Development of secretory apparatus of the breast
  3. Increases body temp
  4. Depressants effects, sedatives
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9
Q

How does progesterone or its metabolites make inhibitory effects?

A

Hits GABBA A receptor

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10
Q

How much testosterone is freely circulating?

A

2%

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11
Q

What are the effects of testosterone?

A
  1. Growth of pubic hair, axillary hair, beard
  2. Growth of larynx, thickening of vocal chordsSebum secretion
  3. Decrease binding globulin
  4. Stimulate EPO secretion
  5. Anabolic effects
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12
Q

What is oxymetholone?

A

17-alkyl deriv of testosterone

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13
Q

What oxymetholone used to treat?

A

Bone marrow hypoplasia, myelofibrosis

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14
Q

What are 17-alkyl derivatives associated with?

A

Hyperbilirubinemia, increased hepatic enzymes, cholestatic hepatitis,

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15
Q

What is the bioavailability of estradiol?

A

10%

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16
Q

What may alter the efficacy of oral estrogens?

A

Broad spectrum antibiotics that alter intestinal flora

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17
Q

What drugs might estrogens alter the metabolism of?

A

Drugs metabolized by glucoronidases. Like acetaminophen

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18
Q

What is the MOA of oral contraceptives?

A

Exert negative feedback on the hypothalamus and pituitary –

  1. Reduce GnRH
  2. Reduce FSH secretion - incomplete follicular development
  3. Reduce LH secretion - no ovulation
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19
Q

How do OCs affect sperm and endometrium?

A

It thickens the cervical mucous to reduce sperm.

It alters the endometrial structure makes the uterus unreceptive for implantation

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20
Q

What is the most commonly used estrogen in OCs?

A

Ethinyl estradiol

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21
Q

What are th most commonly used progesterones?

A

Norethindrone
Levonorgestrel
Norgestimate
Desogestrel

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22
Q

What is the potency of the progesterones used?

A
  1. Desogestrel
  2. Norgestrel
  3. Norgestimate, norethindrone
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23
Q

Which progesterone has an increased risk of thromboembolism?

A

Desogestrel

24
Q

Which estrogen has androgenicity that is similar to spironolactone?

A

Drospirenone in Yasmin

25
Q

What are the advantages of triphasic OCs?

A

Less spotting, breakthrough bleeding and amenorrhea

26
Q

Who do we use progestin only on?

A

Women at risk for certain estrogen-dependent cancers or who don’t tolerate the estrogen portion in OCs or who are breast feeding

27
Q

What is the disadvantage of using progestin only?

A

It is not as effective at inhibiting ovulation

28
Q

What is injectable progestin for?

A

For long term contraception

29
Q

Who is injectable progestin not good for?

A

Women who want to get pregnant soon after treatment

30
Q

What are the disadvantages of implantable progestin?

A

Need for surgical implantation and removal

Irregular bleeding

31
Q

What can lower the efficacy of OCs?

A

Phenytoin
Rifampin
Antibiotics

32
Q

What are the side effects of estrogen?

A

TE - increases clotting factors and decreases antithrombin III
Increase risk of MI
HTN
Nausea - heightened sense of smell
Edema
Headache or worsens migraines - converts tryptophan to nicotinic acid
Cancer of breast, cervix, liver

33
Q

What are the side effects of progestin?

A
Increased appetite - increase in the amount of insulin
Weight gain
Depression
Increased bp
Increase acne and CV disease
34
Q

What are the contraindications to OCs?

A
Pregnancy
Women with history of estrogen-dependent neoplasm or breast cancer
TE disorders 
Liver disease
Smokers
35
Q

What is plan b?

A

It is a high dose of levonorgestrel

36
Q

What is RU486?

A

Mifepristone - has a luteolytic effect, usually combined with a prostaglandin which may trigger uterine contraction

37
Q

What is DES?

A

May interfere with timing of uterine maturation

38
Q

What are the post coital contraceptives?

A

Plan B
Mifepristone
DES

39
Q

What is hormone replacement used for?

A

Reducing menopause symptoms
Reducing osteoporosis
Treating primary hypogonadism (ovarian failure, hypopituitarism)

40
Q

What is the treatment for menopause?

A

Low dose estrogen and a progestin

41
Q

What are the HRTs for menopause?

A

Conjugated equine estrogen
Metroxy-progesterone acetate (provera)
Estradiol
Prempro (CEE + MPA)

42
Q

What are progestins given for in menopause?

A

For reducing endometrial and uterine cancer

43
Q

What are the benefits of HRT?

A

Reduces heart attacks and strokes
Reduces hot flashes
Decreases bone loss

44
Q

What are the problems with HRT?

A

Poor compliance because of bleeding and fear of cancer.

Hypogonadism

45
Q

What are the side effects with estrogen in HRT.

A
Hyper pigmentation
Increased migraines
Breast tenderness
Nausea
Bleeding
Cancer
46
Q

What are the contraindications to HRT?

A

Hx of estrogen dependent cancers
TE
Liver disease
Smoking

47
Q

What are the advantages of transdermal estradiol?

A

Reduced conversion of estradiol to estrone
Little risk for TE
No effect of SHBG

48
Q

What is the disadvantage of transdermal estradiol?

A

May not cause increase in HDL or lower LDL

49
Q

What is can androgen therapy be used for?

A

Hypogonadal men
Reverse atrophy following trauma, surgery, disease
Anemia
Osteoporosis

50
Q

What are the side effects of androgen therapy?

A
Masculinizing effects or gynecomastia
Hirsutism
Acne
Hepatic dysfunction
Azospermia
Abuse
51
Q

What are the contraindications to androgens?

A

Hx of prostate or breast cancer

Pregnant women

52
Q

What are the disorders or androgen excess?

A
Hirsutism
Acne
Amenorrhea
Gynecomastia
Prostatic hyperplasia - urinary retention
PCOS
Cushing's
53
Q

What drugs can be used for hirsutism?

A

OCs
AR antagonist - spironolactone, flutamide
DHT synthesis inhibitors - finasterides, dutasteride
GnRh analogs
Eflornithine cream - ornithine decarbox inhibitor

54
Q

What is clomiphene?

A

A partial estrogen agonist - reduces negative feedback so increases gonadotropins and estrogens

55
Q

What is Faslodex?

A

Pure anti- estrogen