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Pharmacology > EXAM #5: ESTROGENS & PROGESTIN II > Flashcards

EXAM #5: ESTROGENS & PROGESTIN II Flashcards

1
Q

What adverse effects are associated with progestins?

A

1) Breakthrough bleeding (endometrial vasculature)
2) Impaired glucose tolerance
3) Changes in lipid metabolism
- Elevated LDL
- Lowered HDL

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2
Q

What are the key adverse effects associated with 19-nortestosterone compounds?

A

1) Acne
2) Hirsutism

Thus, 19-nor effects of BC cause acne vs. estrogen which is protective against acne

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3
Q

What is birth control?

A

Combined estrogen-progestin or progestin only drugs

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4
Q

What can birth control drugs never be composed of?

A

Estrogen alone

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5
Q

What is the most common type of injectable BC?

A

Progestin alone i.e. depo-provera, which is given:

  • Monthly
  • or Quarterly
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6
Q

What are implantable BC methods composed of?

A

Progestin only

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7
Q

How long can an implantable BC stay implanted?

A

3 years

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8
Q

What is the composition of IUD BC?

A

Progestins only

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9
Q

How long can an IUD stay in?

A

5 years

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10
Q

How often are vaginal rings and transdermal BC placed?

A

Monthly

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11
Q

What is the general MOA of BC?

A

1) Suppress LH and FSH surge for ovulation
2) Alter cervical mucus
3) Alter endometrium

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12
Q

Give an example of a progestin only BC.

A

Nor-QD

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13
Q

What hormone is in “Depo-provera?”

A

Medroxyprogesterone

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14
Q

What is the major difference between normal contraceptive therapy and emergency contraception?

A

Higher doses for emergency contraception

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15
Q

How long after intercourse can one take Plan-B?

A

72 hours

*Note that this is the drug of choice for emergency contraception

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16
Q

What is the failure rate of oral contraception with typical use?

A

8%

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17
Q

What are the mild adverse effects associated with contraceptives?

A
  • Nausea
  • Mastalgia (breast tenderness)
  • Breakthrough bleeding (Estrogen-mediated)
  • Edema
  • Headache
  • Withdrawal bleed failure
  • Serum protein changes
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18
Q

What are the moderate adverse effects of contraceptives?

A
  • Breakthrough bleeding (Progestin-mediated)
  • Weight gain
  • Increased skin pigmentation
  • Acne
  • Hirsutism
  • Vaginal infection
  • Amenorrhea
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19
Q

What are the severe adverse effects of contraceptives?

A
  • Thromboembolic disease
  • MI
  • CVA
  • GI disorders i.e. cholestasis
  • Depression
  • ?Cancer
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20
Q

What are the benefits of contraceptives?

A

1) Reduced risk of ovarian and endometrial cancer
2) Reduction in dysmenorrhea/ endometriosis
3) Decreased incidence of ectopic pregnancy
4) Decreased benign breast disease
5) Increased Hb concentrations
6) Suppress acne and hirsutism

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21
Q

What are the contraindications to estrogen containing contraceptives?

A

1) Known/ suspected breast cancer
2) Thromboembolic disorder
3) Liver disease
4) Cardiovascular disease
5) Smoker 35 y/o+

22
Q

What are the drugs that induce hormone metabolism?

A

1) HIV agents
2) Anti-convulsants
3) St. John’s wort

23
Q

What effect do antibiotics have on contraceptives?

A

Decreased efficacy

24
Q

What is the clinical indication for Clomiphene?

A

Fertility drug

25
Q

What is the MOA of Clomiphene?

A
  • PARTIAL AGONIST that blocks negative feedback on LH and FSH
  • Increase liklihood of ovulation
26
Q

What is a partial agonist?

A

Drug that produces a lower than maximal response compared to the agonist

27
Q

What adverse effects are associated with Clomiphene?

A

1) Hot flashes

2) Multiple births

28
Q

When in the menstrual cycle is Clomiphene given?

A
  • Follicular phase for 5x days

- Removed prior to day 14 (ovulation)

29
Q

What are SERMS?

A

Selective Estrogen Receptor Modulators

*Note that the same SERM can have different actions in different tissues i.e. agonist, partial agonist, antagonist

30
Q

What is the function of SERMS in bone?

A

Suppress bone resorption (agonist)

*I.e. estrogen receptor agonism will reduce osteoporosis

31
Q

What is the function of SERMS in the endometrium?

A

Proliferation (partial agonist)

This is an unintended adverse effect and can lead to development of endometrial hyperplasia and endometrial CA

32
Q

What is the function of SERMS in pituitary and breast?

A

Antagonist, which will

  • Hot flashes (pituitary)
  • Inhibited proliferation in breast (anti-ER+ cancer)
33
Q

List the two SERMS.

A

Tamoxifen

Raloxifene

34
Q

What is the clinical indication for Tamoxifen?

A

ER+ Breast Cancer

35
Q

What adverse effects are associated with Tamoxifen?

A

1) Hot flashes
2) Endometrial cancer
3) Nausea/vomiting

36
Q

How does Raloxifene differ from Tamoxifen?

A

NO partial agonist effects on endometrium

37
Q

What are the clinical indications for Raloxifene?

A

1) Breast cancer

2) Post-menopausal bone loss

38
Q

What key adverse effect is associated with Raloxifene?

A

Hot flashes

39
Q

What are the clinical indications for dananzol?

A

1) Endometriosis

2) Breast fibrocystic disease

40
Q

What is the MOA of dananzol?

A

Decreased estrogen concentration in blood by displacing estrogen from serum proteins and increasing estrogen clearance

41
Q

What adverse effects are associated with dananzol?

A

1) Hot flashes
2) Weight gain
3) Oily skin
4) Acne
5) Hirsutism

42
Q

What is the MOA of anaztrozole and letrozole?

A

Aromatase inhibitors that prevent conversion of Testosterone to Estrogen

43
Q

What are the indications for anaztrozole and letrozole?

A

ER+ breast cancer

44
Q

What adverse effects are associated with anaztrozole and letrozole?

A
  • GI disturbances
  • Hot flashes
  • Lethargy
45
Q

List the anti-progesterone drugs.

A

Mifepristone

Ulipristal

46
Q

What is the MOA of Mifepristone?

A

Progesterone receptor antagonist i.e. it will decrease the effects of progesterone

47
Q

What is the clinical use of Mifepristone?

A

Abortifacient (less than 7 weeks/ first trimester)

Followed by misoprostol (synthetic prostaglandin, which further increases uterine contractions) 48 hours later

48
Q

What is the clinical indication for Uliprastal?

A

Emergency contraception

49
Q

What is the MOA of Uliprastal?

A

Partial progesterone agonist

50
Q

What is the benefit of Uliprastal vs. Plan-B?

A

Can be used 5 days post-intercourse vs. 3 days for Plan-B

Pharmacology (64 decks)

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