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Pharm > Estrogens & progestins > Flashcards

Estrogens & progestins Flashcards

1
Q

What are the indications for estrogen therapy?

A

HRT for postmenopausal women
Component of oral contraceptive
Primary hypogonadism (eg Turner)
Primary ovarian insufficiency

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2
Q

When would you add a progestin to estrogen therapy? Why?

A
  • If uterus present

- Add a progestin to reduce risk of endometrial cancer

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3
Q

Adverse effects of estrogen therapy?

A 
Increased risk of:
Endometrial cancer
Thromboembolic disease
GB disease
Postmenopausal bleeding
Dementia (older pts)
Breast tenderness
Severe migraines
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4
Q

What are the contraindications for estrogen therapy?

A 
High risk for or h/o breast cancer
H/o endometrial cancer
H/o thromboembolic disease
H/o genital bleeding
Liver disease
Heavy smoking (stroke risk)
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5
Q

Which CYP450 enzyme does estrogen interact w/, and how?

A

Estrogen metabolized by CYP3A4

- Decreased clinical efficacy in presence of CYP3A4 inducers

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6
Q

List the 3 SERMs.

What does SERM stand for?

A

Tamoxifen, Raloxifen, Clomiphene

Selective estrogen receptor modulator

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7
Q

Tamoxifen’s MoA?

Raloxifen’s MoA?

Clomiphene’s MoA?

A

Tamoxifen: ER antagonist in breast
ER partial agonist–endometrium & bone

Raloxifen: Partial agonist bone (induces ER-dependent bone promoting genes)
ER antagonist in endometrium & breast

Clomiphene: ER antagonist hypothalamus/pituitary: inhibits ER negative feedback and maintains gonadotropin release
ER partial agonist in ovary

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8
Q

Indications for tamoxifen, raloxifen, and clomiphene, respectively?

A

Tamoxifen: Primary prevention of high risk breast cancer
Treatment of advanced breast cancer
Treatment male gynecomastia

Raloxifen: Treatment of osteoporosis in post menopausal women
Alternative to tamoxifen in breast cancer primary prevention (not approved for tx)

Clomiphene: Female infertility due to anovulation (e.g. PCOS)

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9
Q

What are the adverse effects of tamoxifen, raloxifen, and clomiphene, respectively.

A

Tamoxifen: Hot flashes
Increased risk of thromboembolic events
Increased risk of endometrial cancer

Raloxifen: Hot flashes
Increased risk of thromboembolic events
Leg cramps

Clomiphene: Hot flashes
Multiple pregnancies

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10
Q

What are the contraindications for tamoxifen, raloxifen, and clomiphene, respectively?

A

Tamoxifen: H/o thromboembolic events
H/o endometrial cancer

Raloxifen: H/o thromboembolic events
Pregnancy (birth defects)

Clomiphene: none listed

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11
Q

What is the name of the drug that is a selective estrogen receptor degrader (SERD)?

What is the MoA?

A

Fulvestrant

Binds the estrogen receptor and promotes its degradation via the proteosome- inhibits ER signaling

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12
Q

When would you use fulvestrant?

A

Treatment of advanced ER+ metastatic breast cancer, typically following failure of tamoxifen therapy

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13
Q

What are the adverse effects of fulvestrant?

A

Hot flashes
Increased risk of thromboembolic events
Elevated liver enzymes

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14
Q

When is fulvestrant contraindicated?

A

Pregnancy/lactation

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15
Q

What are the names of 3 drugs that are aromatase inhibitors?

What is the MoA?

A

Anastrozole, Letrozole, Exemestane
“Let Ana’s Ex” inhibit Aram

Inhibit aromatase -> Prevent the conversion of androgens into estrogens

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16
Q

When are the aromatase inhibitors indicated?

A

Adjuvant therapy of ER+ breast cancer in post menopausal women

17
Q

What are the adverse effects of anastrozole, letrozole, and exemestane?

How are they advantageous compared to tamoxifen?

A

Symptoms of estrogen deficiency
Increased bone fractures
Unlike tamoxifen does not increase endometrial cancer

18
Q

What are aromatase inhibitors contraindicated?

A

Premonopausal women (since there is little effect due to increased homeostatic expression of aromatase)

19
Q

Try to name the progestins. (6 we have to know)

A 
Norgestrel
Levongestrel
Norethindrone (only 1 w/o gest in the name)
Desogestrel
Gestodene
Norgestimate
20
Q

What is the MoA of progestins?

A

Agonists of the PR (some also weakly activate AR). Results in:
(A) Decrease in frequency of GnRH pulses
-> Decreased gonadotropins
-> Decreased ovulation
(B) Thickens cervical mucus
-> impairs sperm penetration
(C ) Reduces endometrial growth and impairs blastocyst implantation

21
Q

When are progestins indicated?

A

Hormone replacement

Hormone contraception

22
Q

What are the adverse effects of progestins?

A

Menstrual irregularities
Breast tenderness
Ovarian cysts
Acne

23
Q

What is the MoA of combined oral contraceptive estrogen + progestin?

A

Estrogen + progestin

  • > inhibit GnRH release
  • > Inhibit LH + FSH
  • > Inhibit follicular development and ovulation

Progestin also:
Promotes thickening of cervical mucus
Reduces endometrial growth

24
Q

What are the indications for combined oral contraceptive estrogen + progestin besides contraception? (4)

What diseases does it decrease risk of?

A
  • Tx of menstrual cycle disorders
  • Hyperandrogenism (e.g. acne)
  • Bleeding due to fibroids
  • Tx of endometriosis
  • Decrease risk of endometrial and ovarian cancer
25
Q

What are the adverse effects a/w combined oral contraceptive estrogen + progestin?

A 
Bloating, nausea
Breast tenderness
Breakthrough bleeding
Risk of venous thrombosis
Risk of MI
Increased risk hepatic adenoma
26
Q

When is combined oral contraceptive estrogen + progestin contraindicated?

A 
Age > 35 y & smoking
CAD
H/o venous thrombosis
H/o stroke
Systemic lupus (clotting)

H/o breast cancer
H/o liver disease

27
Q

What are the names of the 2 emergency contraceptives? (which is given at high dose?)

A

Levonorgestrel (high dose)

Ulipristal

28
Q

What is the MoA for levonorgestrel?

For ulipristal?

A

Levonorgestrel: Activates PR; Inhibits or delays ovulation by inhibiting the LH surge

Ulipristal: partial agonist of PR- acts as an antagonist in presence of progesterone; Inhibits or delays ovulation by antagonizing PR-dependent genes involved in follicular rupture.
Effective even if given at time of LH surge”

29
Q

What are the indications for levonorgestrel?

For ulipristal?

A

Levonorgestrel: Prevention of pregnancy
Following unprotected sex or failure of barrier contraception”

Ulipristal: same, but also tx of uterine fibroids

30
Q

What are the adverse effects a/w levonorgestrel?

For ulipristal?

A

Nausea
Delay of menses
(for both)

31
Q

Which is containdicated during pregnancy: levonorgestrel, ulipristal, both, or neither?

A

Ulipristal

32
Q

When must you give levonorgestrel for it to be effective as an emergency contraceptive?

Ulipristal?

A

Levonorgestrel: Only effective if given 1-2 days prior to LH surge.

  • Must be given within 72 hrs of intercourse
  • Taken once daily for 5 days

Ulipristal: effective when given up to 5 days after sex

33
Q

What types of drugs are mifepristone + misprostol (given together), and what is each of their MoA?

A

Abortifacient

  • PR antagonist, impairs development of endometrium and promotes menses.
  • Also Glucocorticoid R and androgen R antagonist
  • Misprostol (PGE1 analog) promotes uterine contraction and expulsion of blastocyst
34
Q

When must mifepristone + misprostol be given by?

A

Before 70 days gestation

35
Q

What are the adverse effects of mifepristone + misprostol?

A

Excessive vaginal bleeding

Abdominal cramps

36
Q

When are mifepristone + misprostol contraindicated?

A

Chronic adrenal insufficiency as can precipitate an adrenal crisis
Bleeding disorder or anticoagulants

37
Q

Name the progestin that doesn’t have “gest” in it’s name.

A

Norethindrone (AKA norethisterone)

Pharm (32 decks)

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