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Pharmacology - Winter > 12 - Estrogens & Progestins > Flashcards

12 - Estrogens & Progestins Flashcards

1
Q

What are estrogens?

A

Substances capable of inducing estrus or sexual receptivity in females

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2
Q

What is estradiol? Where is it produced?

A
  • Major natural estrogen

- Produced in ovaries

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3
Q

Where are estrone and estriol produced?

A

Liver and other tissues

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4
Q

How does the secretion rate of estradiol change during the menstrual cycle, pregnancy, and post menopause?

A
  • Menstrual cycle - low during first week of menstrual cycle, peaks during mid cycle and decreases during luteal phase
  • Pregnancy - very high
  • Post menopause - very low
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5
Q

What are the 2 types of estrogen receptors and where are they found?

A

1) Alpha receptors - uterus, ovaries, breast, testes, prostate heart, and brain
2) Beta receptors - more broadly expressed (brain, lungs, bones, blood vessels)

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6
Q

What is the function of alpha estrogen receptors?

A

Hormone production in testes and Leydig cells

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7
Q

What is the function of beta estrogen receptors?

A

Spermatogenesis in testes and Serotoli cells

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8
Q

What are the actions of estrogen?

A
  • Promotes synthesis of its own receptors and progesterone
  • During puberty, causes changes in reproductive organs, distribution of fat, and shape of body
  • Later required for skin texture, bone strength, gut motility, and low LDL/HDL ratio
  • Anabolic, weight gain, water and salt retention
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9
Q

What are the actions of progesterone in high concentrations?

A

Decrease synthesis, number, and responsiveness to estrogen and progesterone

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10
Q

How is estrogen metabolized?

A

Liver produces inactive sulfates and glucuronide derivatives for excretion

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11
Q

How is estrogen absorbed?

A
  • Through skin and mucous membranes

- Prompt and complete absorption from GI tract

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12
Q

What can prevent or slow down metabolism of estrogen?

A
  • Esters slow absorption and prolong action

- Micronization slows first pass metabolism

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13
Q

Example of a drug that is non-steroidal and estrogenic

A

Diethylstilbesterol

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14
Q

Example of a drug that is non-steroidal and anti-estrogenic

A

Clomiphen

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15
Q

Example of a drug that is non-steroidal and mixed

A
  • Tamoxifen and raloxifene
  • Anti-estrogenic or estrogenic depending on tissue
  • AKA SERMs (selective estrogen receptor modifiers)
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16
Q

What are the uses of estrogen?

A
  • Replacement therapy (ovarian failure, surgical removal, menopause)
  • Hirsutism, acne
  • Neoplastic diseases (anti-estrogen or estrogen)
  • Anti-estrogens as fertility drugs
  • Contraception
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17
Q

What does diane-35 contain? What is its function? How long is tx required?

A
  • A progestrogen w/ anti-androgenic properties
  • Reduces activity of sebaceous gland, excessive hair growth, and deepening of voice
  • Tx = 3-6 months
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18
Q

What benefits can estrogen have on menopause side effects?

A
  • Decreases post-menopausal sleep disturbances
  • Protective effect against CV disease
  • Decreases resorption of bone
  • Decreases frequency of hip fractures
  • Decreases frequency of hot flashes
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19
Q

Tx w/ estrogens must begin w/in ____ years of menopause, earlier if possible

A

2-3 years

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20
Q

What are some adverse reactions of estrogen use during menopause?

A
  • Most frequent = nausea; anorexia, vomiting, and mild diarrhea w/ larger doses
  • Bleeding
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21
Q

Where is tamoxifen an antagonist and where is it an agonist?

A
  • Competitive antagonist in brain and breast tissue

- Agonist in CV system, bone, and uterus

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22
Q

Where is raloxifene an antagonist and where is it an agonist?

A
  • Competitive antagonist in brain and breast tissue

- Agonist in CV system and bone (no effect in uterus)

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23
Q

Which SERM is preferred for osteoporosis?

A

Raloxifene

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24
Q

What is the action of clomiphene?

A
  • Increases pituitary secretion of gonadotropins (FSH and LH)
  • Interferes w/ estrogen “receptor sites” involved in feedback inhibition by estrogen on secretion of LH and FSH
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25
Q

What is the use of clomiphene?

A

Treating infertility and to induce ovulation

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26
Q

What are side effects of clomiphene?

A
  • Common = hot flashes

- Rare = skin rashes, gastric upset, and visual disturbances (reversible when drug stopped)

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27
Q

What are progestins?

A

Substances that prepare the uterus for reception of fertilized ovum

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28
Q

What is the function of progestins?

A

Increase secretions from endometrial tissue that has been primed w/ estrogen

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29
Q

When does withdrawal bleeding occur?

A
  • Aka menstruation

- When there is no progesterone and estrogen in the blood

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30
Q

What is breakthrough bleeding? What normally causes it?

A
  • Any bleeding that occurs despite the presence of steroids

- Usually due to high levels of progesterone relative to estrogen

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31
Q

What are characteristics of the ideal contraceptive method?

A
  • Few side effects
  • Full and easy reversibility
  • Absolute effectiveness
  • Ease of use
32
Q

How is efficacy of contraception assessed?

A

Measuring the number of pregnancies during use of a specified period

33
Q

What is the pearl index?

A
  • Number of failures per 100 women years of exposure (must follow at least 100 women for at least 12 cycles)
  • Pregnancies / total months of use (at least 12) * 1200
34
Q

Why are oral contraceptives considered the best amongst the various methods?

A
  • Easy reversibility
  • Ease of use
  • Few side effects
35
Q

What are the 3 groups of orally active contraceptive agents?

A

1) Estrogen/progestin (combination pills)
2) Progestin only (mini pills)
3) Interceptives or post-coital (morning after pill)

36
Q

What is the MOA of oral contraceptives?

A
  • Inhibit synthesis or release of pituitary gonadotropins w/ subsequent suppression of ovulation
  • Prevent sperm from entering uterus (progesterone secretes thick mucous)
  • Prevent implantation of fertilized ovum
37
Q

What are the predominant actions of estrogen and progesterone?

A
  • Estrogen = inhibit secretion of FSH

- Progesterone = inhibit release of LH

38
Q

How do large doses of estrogen prevent implantation of the fertilized ovum?

A
  • Alter motility of the oviduct

- Alter properties of endometrium

39
Q

Does estrogen or progesterone cause the majority of undesirable side effects?

A

Estrogen, so use a lower dose of estrogen

40
Q

What can very low estrogen cause? What should be done about this?

A
  • Can cause breakthrough bleeding

- If problem persists beyond 3 months, dose of estrogen should be increased

41
Q

When are progestin only pills recommended?

A
  • Breastfeeding

- Women w/ family or personal history of clots

42
Q

What is the mechanism of progestin only pills to prevent pregnancy?

A

Alteration of cervical mucous and endometrium w/o suppressing ovulation

43
Q

How long can subcutaneous implantations of progestin last?

A

Up to 5 years

44
Q

What is a warning w/ the progestin injection (Depo-provera)?

A

Possibility to cause permanent infertility

45
Q

What is a possible mechanism for breakthrough bleeding?

A
  • While estrogen promotes the synthesis of progesterone and its own receptors, progesterone inhibits the synthesis of estrogen and its own receptors
  • W/o receptors, hormones can’t have actions, so bleeding will occur despite the presence of steroids
46
Q

When is breakthrough bleeding likely to occur?

A
  • First 3 months of use

- More common in smokers

47
Q

What is the tx for breakthrough bleeding?

A

Short period of estrogen (either ethinyl estradiol or oral forms of estradiol) for 7 days when bleeding is present

48
Q

What is the Yuzpe method?

A

2 combination pills w/in 72 hours after sexual intercourse and 2 more 12 hours later

49
Q

What is the MOA of Mifeprix (mifepristone misoprostol)?

A
  • Competitive antagonist on progesterone receptor, causing detachment of blastocyst, decreasing hCG
  • Increases prostaglandins and uterine motility (misoprostol)
  • Causes cervical softening, facilitating expulsion
50
Q

What are side effects of Mifeprix?

A

Bleeding and abdominal cramps that may last 8-17 days

51
Q

When should oral contraceptives be discontinued?

A

Earliest sign of thrombo-embolic disorders, visual defects, or severe headache of unknown etiology

52
Q

What are some beneficial effects of oral contraceptives?

A
  • Less benign breast diseases
  • Less rheumatoid arthritis
  • Increased bone density
  • Dysfunctional bleeding
  • Less reports of ovarian cysts
53
Q

What are some side effects of oral contraceptives?

A
  • Common SE = N/V, headache, breast discomfort, weight gain
  • Depression (progestin)
  • Hypertension (related to age, duration of use, and concentration of estrogen)
  • Thromboembolism (risk decreased w/ low dose estrogen)
  • MI
  • Cerebrovascular diseases
  • Neoplastic diseases
  • Amenorrhea
  • Glucose intolerance (diabetes in women w/ family history)
  • Breakthrough bleeding
54
Q

What is the tx for hypertension caused by oral contraceptives?

A

Discontinue oral contraceptive and BP should return to normal

55
Q

Oral contraceptives should be discontinued _____ before and after major surgery to avoid risk of _____

A

4-6 weeks; thromboembolism

56
Q

Which drugs reduce the efficacy of oral contraceptives and increase incidence of breakthrough bleeding?

A
  • Barbiturates
  • Rifampicin
  • Phenylbutazone
  • Phenytoin
57
Q

What are some absolute contraindications for oral contraceptives?

A
  • Acute liver disease or impaired liver function
  • Carcinoma of breast
  • Known or suspected estrogen-dependent neoplasia
  • Undiagnosed genital bleeding
  • Suspected or known pregnancy
  • Past history of cerebrovascular disease, thromboembolic disease, or conditions predisposing to these disorders
58
Q

What are some relative contraindications for oral contraceptives?

A
  • Subjects over 40 y/o
  • Migraine headaches
  • Hypertension
  • Smoking
59
Q

____ is the major androgen

A

Testosterone

60
Q

What is testosterone responsible for in women?

A

Libido and growth

61
Q

What is the relationship between testosterone and LH?

A

Testosterone causes feedback inhibition of LH production

62
Q

What are androgens responsible for in males?

A

Development of male characteristics during puberty

63
Q

The active form of testosterone is _______

A

Dihydrotestosterone

64
Q

What are the therapeutic uses of testosterone?

A
  • Replacement therapy (hypogonadism in youth or andropause)
  • Endometriosis
  • Growth stimulation
  • Prevention of osteoporosis
65
Q

What is the tx for hypogonadism in youth?

A
  • Large doses of testosterone IM until maturation is complete
  • Long acting preparations given biweekly
66
Q

What is andropause/ADAM?

A
  • ADAM = androgen decline in aging male
  • Deficiency in serum androgen levels w/ or w/o genomic sensitivity
  • Causes significant alterations in QOL
67
Q

What is a contraindication for testosterone tx for andropause?

A

Men w/ severe bladder outlet obstruction due to benign prostate (b/c androgens stimulate prostate growth)

68
Q

What are the sx of andropause/ADAM?

A
  • Loss of sexual desire and erectile function
  • Decrease in bone mineral density leading to osteoporosis
  • Altered mood
  • Loss of muscle strength and body hair
69
Q

What is the criteria for diagnosis of andropause?

A

Testosterone level of less than 0.255 nM between 8-11 am

70
Q

What is the tx for andropause?

A
  • Oral (taken w/ meals in the morning)

- Transdermal preparations

71
Q

What are some adverse reactions from testosterone therapy for andropause?

A
  • Prostate cancer (must monitor prostate specific antigen levels)
  • Liver tumours and jaundice (rare w/ transdermal)
  • Mood changes
  • RBC mass and hemoglobin levels may increase
72
Q

What is the tx for endometriosis?

A

Mild androgen

73
Q

What are some adverse effects of anabolic steroids?

A
  • Masculinization of females, even w/ very low doses
  • Hepatic dysfunction, hepatocellular carcinoma
  • CNS effects (aggressiveness, anger)
  • Impotence and decreased sperm count w/ higher concentration
  • Increased LDL/HDL ratio
74
Q

Which drugs are androgen receptor blockers? What are they used for?

A
  • Cyproterone acetate
  • Flutamide
  • Used for prostatic cancer and hirsutism
75
Q

Which drug is a 5-alpha reductase blocker? What is its use?

A
  • Finasteride

- May be useful in prostatic cancer

Pharmacology - Winter (18 decks)

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