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Pharmacology II > Estrogens > Flashcards

Estrogens Flashcards

1
Q

Female Sex Hormones

A 
Progestins
Estrogens
Human Chorionic Gonadotropin
Oxytocin
Prolactin
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2
Q

Human Chorionic Gonadotropin

A

hCG
Produced by the placenta after implantation that maintains the corpus luteum
Keeps the progesterone levels up and maintains caloric intake

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3
Q

Oxytocin

A

Secreted by posterior pituitary

Facilitates labour

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4
Q

Prolactin

A

Secreted by anterior pituitary gland

Breast milk production

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5
Q

What causes ovulation?

A

Initially the secretion of estradiol inhibits LH and FSH secretion, but with the peak of estradiol you get a FSH and LH peak that causes ovulation

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6
Q

3 physiologic effects of progestins

A

Increases lipoprotein lipase activity
Increase insulin levels
Increase insulin response to glucose (promotes glycogen storage)

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7
Q

Physiologic effects of estrogen (liver, CV, CNS, bone, uterus, ovary, breast)

A

Liver (lowers cholesterol)
Cardiovascular (clotting factors and cardioprotection)
CNS (neuroprotection)
Bone (maintain bone density)
Uterus (proliferation of the endometrium)
Ovary (mitotic effects on granulosa cells)
Breast (growth and differentiation of the ductal epithelium)

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8
Q

How can you modulate the effects of estrogen at the hypothalamic level?

A

Disrupt the pulsate release of GnRH
Will act as an antagonist and decrease the amount of FSH and LH produced
Ex: Leuprolin

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9
Q

General way hormonal contraceptives work

A

Strengthen negative feedback to prevent ovulation

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10
Q

SERMs

A

Selective estrogen receptor modulators
Agonists or antagonist actions, depending on the tissue
Occupy estrogen binding site on ER
Ex: tamoxifen, raloxifene, clomiphene
Main side effects are hot flashes and increased risk of DVT

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11
Q

Clomiphene

A

SERM
Used for infertility due to lack of ovulation
Moderate estrogen antagonist
Blocks ER in hypothalamus and pituitary
Prevents estrogen negative feedback
Increases LH and FSH leading to ovulation
Treatment for 5 days at beginning of menstrual cycle
Slight increase for the risk of multiple pregnancies

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12
Q

Tamoxifen

A

SERM
Antagonistic activity at ERs in breast tissue
Used to reduce tumor size in ER positive breast cancer
Non-steroid taken orally
Partial agonist in endometrium tissue and has been linked to endometrial cancer after prolonged use

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13
Q

Raloxifene

A

SERM
Agonist activity at ERs in bone tissue
Used in primary prevention of osteoporosis and bone fracture
Antagonist activity at ERs in breast tissue (alternative to tamoxifen)

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14
Q

How can SERMs be agonists in one tissue while being an antagonist somewhere else?

A

SERMs bind to and change the conformation of the ER
The ER conformation dictates interaction with cofactors
Tissues require different active cofactors to activate specific gene transcription
Thus, changing the conformation of the ER in the presence of SERM may: enhance, not change, or prevent transcription

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15
Q

Fulvestrant

A 
Anti-estrogen
Antagonist at ERs
Inhibits the dimerization of ER
Used in tamoxifen resistant, ER positive breast cancers
Adverse effects: hot flashes, headache
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16
Q

Thecal cells

A

Surround the follicle within the ovary

17
Q

Granulosa cells

A

Somatic follicle cells

18
Q

2 important enzymes for estrogen biosynthesis

A

P450 17 alpha (hydroxylase) - from cholesterol to testosterone
Aromatase - from testosterone to estrogen

19
Q

3 P450c17 inhibitors

A

Ketoconazole
Danazol
Anastrozole

20
Q

Ketoconazole

A

P450c17 inhibitor
Antifungal
Not typically used due to other systemic effects

21
Q

Danazol

A 
P450c17 inhibitor
Partial agonist of several sex hormone receptors
Can inhibit synthesis of androstenedione
Used to treat endometriosis
Several masculinizing side effects
22
Q

Anastrozole

A

P450c17 inhibitor
Inhibits aromatase (lower estrogen)
Used to treat ER+ breast cancer

23
Q

Leuprorelin

A

Agonist/antagonist of GnRH receptor
Same as male system
Disrupt the pulsate release of GnRH to reduce estrogen

24
Q

FSH stimulates ____ to secrete ____

A

Developing follicle

Estrogen

25
Q

How does progestin alone prevent ovulation?

A

Higher levels of progestin early in the cycle has negative feedback on FSH and LH
This results in no follicle estrogen secretion, no LH surge, and no ovulation

26
Q

Micronor

A

Progestin only pill

Pill needs to be taken at the same time every day to maintain adequate hormone levels

27
Q

2 side effects of progestin only contraceptives

A

Breakthrough (mid-cycle) bleeding

May increase weight and acne

28
Q

Side effects of combination estrogen/progestin contraceptives

A 
Nausea, edema, migraines (typically subside after prolonged use or lowered dose)
CV disorders (MI, stroke, blood clots) - smoking and being older than 35 increase these risks
29
Q

Monophasic combined oral contraceptives

A

Same levels of hormones for entire cycle

Ex: Alesse, Yasmin

30
Q

Biphasic and triphasic combined oral contraceptives

A

Levels of hormones change throughout the cycle

Ex: Triphasil, Natazia

31
Q

Alesse

A

Combined monophasic oral contraceptive
Estrogen: ethinyl estradiol (0.02 mg/pill)
Progestin: L-norgestrel (levelnorestrel - 0.1 mg/pill)

32
Q

Yasmin

A

Combined monophasic oral contraceptive
Estrogen: ethinyl estradiol (0.02 mg/pill)
Progestin: drospirenone (3 mg/pill)

33
Q

Triphasil

A

Combined triphasic oral contraceptive
Estrogen: ethinyl estradiol (stays pretty constant, slight increase for days 7-11)
Progestin: levonorgestrel (increases throughout cycle, highest level days 12-21)
Changing hormone levels more closely mimic physiologic cycles (reduces side effects)

34
Q

Emergency contraception

A

Same hormones found in oral contraceptives, much higher doses and more concentrated form
Plan B is levonorgestrel (2 x 0.75 mg tablets in one day, or 1.5 mg single dose)
Adverse effects: nausea, vomiting, cramping

35
Q

How does Phenytoin influence hormone metabolism

A

It is an anti-seizure medication
Increases liver metabolism (CYP 3A4)
Have to adjust dosage to compensate, or use alternative methods

36
Q

2 mechanisms how antibiotics can have an effect on combined oral contraceptives

A

Increase liver metabolism of the contraceptives due to induction of enzymes by antibiotics
Decreased enterohepatic circulation of contraceptive

37
Q

Bothersome symptoms in menopause related to fluctuations in estrogen levels

A

Vasomotor symptoms (hot flashes)
Vaginal dryness
Reduced bone mass density/osteoporosis
Increased risk for CV events

38
Q

Why do you not give estrogen alone?

A

Can potentiate hormone sensitive cancers and endometriosis

Always administered with progestins to reduce these effects

Pharmacology II (24 decks)

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