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Pharm > Inhibitors of progestins and estrogen > Flashcards

Inhibitors of progestins and estrogen Flashcards

1
Q

What are the three major adverse effects of progestins?

A
  1. Breakthrough bleeding
  2. Impaired glucose tolerance
  3. Changes in lipid metabolism
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2
Q

What causes the breakthrough bleeding with progestins?

A

Neovascularization of the endometrium, causing fragile vessels

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3
Q

What component of birth control causes acne? Hirsutism?

A

19-nortestosterone

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4
Q

When referring to the “type” of birth control, we primarily mean what?

A

Administration

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5
Q

Are most contraceptives lipophilic, or hydrophilic?

A

Lipophilic

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6
Q

What are the types of birth control that are given orally?

A

Estrogens and progestins or progestins alone

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7
Q

What are the contraceptives that are given as an injection?

A

Estrogen and progestins or progestins alone

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8
Q

What type of contraceptives are given as an implant? HOw long do these last?

A

Progestins alone

3 years

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9
Q

What type of contraceptives are given as an IUD? How long do these usually last?

A

Progestins alone
Cu
5 years

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10
Q

What type of contraceptives are given transdermally?

A

Estrogens and progestins

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11
Q

What type of contraceptives are given as a vaginal ring?

A

Estrogens and progestins

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12
Q

Can you give estrogens or progestins alone?

A

Progestins yes, estrogens no no no!

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13
Q

What are the three major MOAs of hormonal birth controls?

A

Suppress LH and FSH
Alter cervical mucus
Alter endometrium

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14
Q

What type of hormone is levonorgestrel?

A

Progesterone

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15
Q

What is the hormone that is found in Depo-provera?

A

Medroxyprogesterone

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16
Q

What is the main difference between regular oral contraceptives, and emergency (“plan-b”) pills? What types of hormones are used in this?

A

Higher dose

Either progesterone or estrogens + progesterone

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17
Q

What is the hormone that is in Plan B? What is the failure rate?

A

Progestin (levonorgestrel)

12% failure rate (better than the 25% with combo therapy)

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18
Q

What is the failure rate of oral contraceptives? How does the efficacy change with changing the administration route to injectable/implant?

A

8%, getting lower with less user control

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19
Q

Why does breakthrough bleeding occur with estrogen? What can be done to alleviate this?

A

Increased proliferation with not enough progesterone to support the continued growth

Administration of progesterone

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20
Q

What are the severe side effects of hormone contraceptives?

A

Thromboembolism
MI
cerebrovascular disease

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21
Q

Breakthrough bleeding in more severe if it is estrogen or progesterone mediated?

A

Progesterone

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22
Q

What is the effect of oral birth control on the risk of ovarian and endometrial CA?

A

Reduced

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23
Q

What is the effect of oral birth control on dysmenorrhea and endometriosis?

A

Reduced

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24
Q

What is the effect of oral contraceptives on: the incidence of ectopic pregnancy?

A

Lowers

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25
Q

What is the effect of oral contraceptives on: incidence of benign breast disease?

A

Decreased

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26
Q

What is the effect of oral contraceptives on: Hb concentrations

A

Increased

27
Q

What is the effect of oral contraceptives on: acne and hirsutism?

A

Generally reduces

28
Q

What are the medications that reduce oral contraceptive effectiveness?

A

ABx
HIV agents
St. John’s Wort

29
Q

What are the contraindications to oral contraceptives?

A 
Liver disease
Thromboembolic disorders
h/o MI
Smokers
h/o CA
30
Q

What is the effect of St. John’s Wort on oral contraceptives?

A

Increased metabolism

31
Q

Why do some Abx decrease the efficacy of oral contraceptives?

A

reduced bacteria, which are responsible for helping re-uptaking estrogen

32
Q

What is the MOA of clomiphene? Use? Side effects? (3)

A

partial agonist of estrogen receptor in the pituitary, to block the negative feedback of FSH and LH.

This increases likelihood of ovulation

Multiple births, hot flashes, ovary enlargement

33
Q

How do partial agonists like clomiphene work to lower LH and FSH?

A

Decline in the response produced by estrogen (endogenous), of producing negative feedback

34
Q

When is Clomiphene used to treat infertility? How?

A

Dose during the follicular phase, causing an increase in LH/FSH, and a surge in estrogen. The body can then response normally.

35
Q

What are SERMS (selective estrogen receptor modulators)? MOA? Use? Side effects?

A

Drugs that modulate the expression of genes with estrogen. The effects vary depending on the tissue

36
Q

What is the effect of SERMS on bone?

A

Suppress resorption

37
Q

What is the effect of of SERMS on the endometrium?

A

Proliferation

38
Q

What is the effect of SERMS on the pituitary?

A

Causes hot flashes

39
Q

What is the effect of SERMS on breast tissue?

A

Inhibits the proliferation of breast tissue

40
Q

What is the MOA and use of tamoxifen?

A

-ER in breast CA

41
Q

What is the effect of tamoxifen on the bone?

A

Agonist

42
Q

What is the effect of tamoxifen on the endometrium?

A

Partial agonist

43
Q

What is the effect of tamoxifen on the the breast?

A

Antagonize proliferation in the breast

44
Q

What are the side effects of tamoxifen?

A

Hot flashes
Endometrial CA
N/v

45
Q

What is the use of raloxifene?

A

CA and postmenopausal bone loss

46
Q

What is the effect of raloxifene on bone? Breast?

A 
Bone = agonist
Breast = antagonist
47
Q

What are the side effects of raloxifene?

A

Hot flashes

n/v

48
Q

Why could raloxifene be better than Tamoxifen in the treatment of breast CA?

A

It does not cause endometrial proliferation like tamoxifen does

49
Q

What is the effect of estrogen on hot flashes? Tamoxifen?

A 
Estrogen = Decreases significantly
Tamoxifen = increases
50
Q

What is the effect of estrogen and tamoxifen on uterine bleeding?

A

Estrogen increases significantly

Tamoxifen increases slightly

51
Q

What is the effect of estrogen and tamoxifen on the risk of endometrial CA?

A

Both increase, but estrogen moreso

52
Q

What is the effect of estrogen and tamoxifen on the prevention of bone loss?

A

Both prevent bone loss, but estrogen moreso

53
Q

What is the effect of estrogen and tamoxifen on serum lipids?

A

Both Improve serum concentrations, but estrogen moreso

54
Q

What is the effect of estrogen and tamoxifen on venous thrombosis?

A

Both increase by about the same amount

55
Q

What is the use and MOA of Danazol? Side effect?

A

Inhibits gonadal function by competing for steroid binding to serum proteins, causing an increased clearance of

Used to treat endometriosis

Weight gain, oily skin, hot flashes

56
Q

What is MOA, use, and side effects of Anastrozole?

A

Aromatase inhibitor
Used to treat breast CA

GI disturbances, hot flashes

57
Q

What is MOA, use, and side effects of Letrozole?

A

Aromatase inhibitor
Used to treat breast CA

GI disturbances, hot flashes

58
Q

What is MOA, use, and side effects of Mifepristone? What drugs is this followed up with?

A

Progesterone receptor antagonist, to block transcriptional activity

Causes uterine contractions

f/u with misoprostol

59
Q

What type of drug is mifepristone?

A

Abortifacient via progesterone receptor antagonist

60
Q

What is MOA, use, and side effects of Ulipristal?

A

Progesterone receptor partial agonist used for emergency contraception.

61
Q

What type of drug is misoprostol?

A

Prostaglandin

62
Q

What is the MOA of anti-progestins as abortifacients?

A

Inhibit progesterone = increase uterine contractions, sheds uterine lining, and opens cervix

63
Q

What is the effect of progesterone on prostaglandin production in the uterus? What happens when you antagonize progesterone production?

A

Progesterone decreases prostaglandin production.

Pharm (73 decks)

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