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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
What is the effect of oral contraceptives on: incidence of benign breast disease?
Decreased
26
What is the effect of oral contraceptives on: Hb concentrations
Increased
27
What is the effect of oral contraceptives on: acne and hirsutism?
Generally reduces
28
What are the medications that reduce oral contraceptive effectiveness?
ABx HIV agents St. John's Wort
29
What are the contraindications to oral contraceptives?
``` Liver disease Thromboembolic disorders h/o MI Smokers h/o CA ```
30
What is the effect of St. John's Wort on oral contraceptives?
Increased metabolism
31
Why do some Abx decrease the efficacy of oral contraceptives?
reduced bacteria, which are responsible for helping re-uptaking estrogen
32
What is the MOA of clomiphene? Use? Side effects? (3)
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
How do partial agonists like clomiphene work to lower LH and FSH?
Decline in the response produced by estrogen (endogenous), of producing negative feedback
34
When is Clomiphene used to treat infertility? How?
Dose during the follicular phase, causing an increase in LH/FSH, and a surge in estrogen. The body can then response normally.
35
What are SERMS (selective estrogen receptor modulators)? MOA? Use? Side effects?
Drugs that modulate the expression of genes with estrogen. The effects vary depending on the tissue
36
What is the effect of SERMS on bone?
Suppress resorption
37
What is the effect of of SERMS on the endometrium?
Proliferation
38
What is the effect of SERMS on the pituitary?
Causes hot flashes
39
What is the effect of SERMS on breast tissue?
Inhibits the proliferation of breast tissue
40
What is the MOA and use of tamoxifen?
-ER in breast CA
41
What is the effect of tamoxifen on the bone?
Agonist
42
What is the effect of tamoxifen on the endometrium?
Partial agonist
43
What is the effect of tamoxifen on the the breast?
Antagonize proliferation in the breast
44
What are the side effects of tamoxifen?
Hot flashes Endometrial CA N/v
45
What is the use of raloxifene?
CA and postmenopausal bone loss
46
What is the effect of raloxifene on bone? Breast?
``` Bone = agonist Breast = antagonist ```
47
What are the side effects of raloxifene?
Hot flashes | n/v
48
Why could raloxifene be better than Tamoxifen in the treatment of breast CA?
It does not cause endometrial proliferation like tamoxifen does
49
What is the effect of estrogen on hot flashes? Tamoxifen?
``` Estrogen = Decreases significantly Tamoxifen = increases ```
50
What is the effect of estrogen and tamoxifen on uterine bleeding?
Estrogen increases significantly | Tamoxifen increases slightly
51
What is the effect of estrogen and tamoxifen on the risk of endometrial CA?
Both increase, but estrogen moreso
52
What is the effect of estrogen and tamoxifen on the prevention of bone loss?
Both prevent bone loss, but estrogen moreso
53
What is the effect of estrogen and tamoxifen on serum lipids?
Both Improve serum concentrations, but estrogen moreso
54
What is the effect of estrogen and tamoxifen on venous thrombosis?
Both increase by about the same amount
55
What is the use and MOA of Danazol? Side effect?
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
What is MOA, use, and side effects of Anastrozole?
Aromatase inhibitor Used to treat breast CA GI disturbances, hot flashes
57
What is MOA, use, and side effects of Letrozole?
Aromatase inhibitor Used to treat breast CA GI disturbances, hot flashes
58
What is MOA, use, and side effects of Mifepristone? What drugs is this followed up with?
Progesterone receptor antagonist, to block transcriptional activity Causes uterine contractions f/u with misoprostol
59
What type of drug is mifepristone?
Abortifacient via progesterone receptor antagonist
60
What is MOA, use, and side effects of Ulipristal?
Progesterone receptor partial agonist used for emergency contraception.
61
What type of drug is misoprostol?
Prostaglandin
62
What is the MOA of anti-progestins as abortifacients?
Inhibit progesterone = increase uterine contractions, sheds uterine lining, and opens cervix
63
What is the effect of progesterone on prostaglandin production in the uterus? What happens when you antagonize progesterone production?
Progesterone decreases prostaglandin production.

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