Sex hormones Flashcards

1
Q

T/F: Oral route of estradiol should be avoided in patients with CVD risk factors

A

True, this is because it could cause greater toxicity

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2
Q

What are contraindications of HRT?

A
  1. Breast cancer
  2. Liver disease
  3. Stroke
  4. DVT
  5. CVD
  6. High CVD risk
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3
Q

T/F: If you have a uterus estrogen by itself is fine

A

False, this will increase risk of endometrial cancer and should be given with progestin. It should only be used alone if uterus is absent

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4
Q

What are side effects seen with progestins?

A

Drowsiness, increased body temp, increased appetite
Note- it is safest to give this alone in patient with hypertension or cardiovascular risk factors
Note- progestin requires perfect adherence because of shorter half-life if PO

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5
Q

How does progestin help to act as a contraceptive?

A
  1. Decreases transit of sperm
  2. Suppresses ovulation
  3. Matures endometrial lining
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6
Q

T/F: Withdrawal of progestins can trigger menstruation

A

True, if deficient in this it would occur in the late cycle phase and would cause heavier bleeding compared to a lack in estrogen

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7
Q

Dosage forms for estrogen/progestin tablets

A
  1. Monophasic (traditional pills)
  2. Multiphasic aka bi or tri (mimic natural hormones and may have lower AEs)
  3. Extended interval (less periods bc placebo every 3 mon)
  4. Continuous (prevents periods w no placebo)
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8
Q

Norethindrone

A

1st gen progestin that is derived from testosterone and is moderately androgenic

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9
Q

Norgestrel or levonorgestrel

A

2nd gen progestin that is derived from testosterone and is most androgenic

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10
Q

Norgestimate

A

3rd gen progestin that is derived from desogestrel (and test?) and is the least androgenic

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11
Q

Drospirenone

A

4th gen progestin that is anti-androgenic and derived from spironolactone

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12
Q

Testosterone

A

Primary systemic androgen that is available in parenteral forms (patch, gel, implant, inj) and is not orally bioavailable

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13
Q

T/F: Dihydrotestosterone or DHT is less potent than testosterone

A

False, it is more potent but is not a drug

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14
Q

Methyltestosterone

A

Modified androgen used for hypogonadism

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15
Q

Oxandrolone

A

Modified androgen used for weight gain

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16
Q

Danazol

A

Modified androgen used for endometriosis

17
Q

What are negative adverse effects seen with too much testosterone?

A

Aggression, CVD, liver injury, prostate cancer, BPH, acne

18
Q

What drug would I give if there is pulsatile release of GnRH that is increasing the levels of sex hormones (estrogen, progesterone, testosterone)?

A

GnRH antagonist–> degarelix
Note- these are used for hormone dependent cancers

19
Q

What drug would I give if there is continuous release of GnRH that is increasing the levels of sex hormones (estrogen, progesterone, testosterone)?

A

GnRH agonists –> goserelin
Note- these are used for hormone dependent cancers (could cause tumor flare so do not use alone) and off-label for transgender therapy

20
Q

What drug would you initiate with an androgen receptor antagonist?

A

Goserelin

21
Q

What is the important synthesis pathway of hormones that are derived from progesterone?

A
  1. 17-hydroxylase makes testosterone from progesterone
  2. Aromatase makes estradiol (E2) from testosterone
  3. 5a-reductase makes DHT from testosterone
22
Q

What drugs are 17-hydroxylase inhibitors (inhibit testosterone) and what are they used for?

A
  • Abiraterone is a strong inhibitor and is used for prostate cancer
  • Spironolactone is a weak inhibitor and is used for hirsutism
23
Q

What drugs are 5a-reductase inhibitors (inhibit formation of DHT) and what are they used for?

A

Finasteride and dutasteride and are used for BPH and baldness
- Note: can cause sexual dysfunction

24
Q

What drug is an aromatase inhibitor (inhibit estrogen) and what is it used for?

A

Anastrozole and its used for breast cancer
- Note: predicted adverse effects would be mood swings, depression, hot flashes, and decreased bone density

25
Q

T/F: abiraterone should always be given with steroids like prednisone

A

True, if not then the patient could have hypertension and hypokalemia d/t decreased cortisol that would stimulate production of aldosterone

26
Q

Tamoxifen

A

MOA: acts as agonist at bone, cholesterol, and uterus and as an antagonist in the breast
Indications: breast cancer
Note- more likely to cause endometrial cancer

27
Q

Raloxifene

A

MOA: acts as agonist at bone and cholesterol but antagonist in breast and uterus
Indications: breast cancer and osteoporosis

28
Q

What are examples of other SERMs (idk how important these rlly are lol)

A
  1. Clomiphene blocks hypothalamus negative feedback and is used for infertility to help stimulate ovulation
  2. Ospemifene stimulates uterus/vagina and used in dysparenuia or painful sex
  3. Toremifene blocks breast tissue and used for ER+ breast cancer
  4. Bazedoxifene blocks bone and used for menopause HRT and prophylaxis of osteoporosis
29
Q

What is ulipristal?

A

MOA: selective progesterone receptor modulator or SPRM that is an agonist of the HPA axis that works by suppressing ovulation and altering the endometrium
Indications: emergency contraception

30
Q

What drug blocks the estrogen receptor?

A

Fulvestrant and this is used in treatment for breast cancer

31
Q

What drug blocks the progestin receptor?

A

Mifepristone and this is used in medical abortion (combined w misoprostol)

32
Q

What two drugs block the androgen receptor?

A
  1. Bicalutamide which is used for prostate cancer
  2. Spironolactone which is used for hirsutism
33
Q

T/F: Fulvestrant can prevent tumor flare when starting goserelin

A

False, bicalutamide is an androgen blocker and can be used to prevent tumor flare because it decreases levels of hormones responsible for the cancer