Sex hormones Flashcards
T/F: Oral route of estradiol should be avoided in patients with CVD risk factors
True, this is because it could cause greater toxicity
What are contraindications of HRT?
- Breast cancer
- Liver disease
- Stroke
- DVT
- CVD
- High CVD risk
T/F: If you have a uterus estrogen by itself is fine
False, this will increase risk of endometrial cancer and should be given with progestin. It should only be used alone if uterus is absent
What are side effects seen with progestins?
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
How does progestin help to act as a contraceptive?
- Decreases transit of sperm
- Suppresses ovulation
- Matures endometrial lining
T/F: Withdrawal of progestins can trigger menstruation
True, if deficient in this it would occur in the late cycle phase and would cause heavier bleeding compared to a lack in estrogen
Dosage forms for estrogen/progestin tablets
- Monophasic (traditional pills)
- Multiphasic aka bi or tri (mimic natural hormones and may have lower AEs)
- Extended interval (less periods bc placebo every 3 mon)
- Continuous (prevents periods w no placebo)
Norethindrone
1st gen progestin that is derived from testosterone and is moderately androgenic
Norgestrel or levonorgestrel
2nd gen progestin that is derived from testosterone and is most androgenic
Norgestimate
3rd gen progestin that is derived from desogestrel (and test?) and is the least androgenic
Drospirenone
4th gen progestin that is anti-androgenic and derived from spironolactone
Testosterone
Primary systemic androgen that is available in parenteral forms (patch, gel, implant, inj) and is not orally bioavailable
T/F: Dihydrotestosterone or DHT is less potent than testosterone
False, it is more potent but is not a drug
Methyltestosterone
Modified androgen used for hypogonadism
Oxandrolone
Modified androgen used for weight gain
Danazol
Modified androgen used for endometriosis
What are negative adverse effects seen with too much testosterone?
Aggression, CVD, liver injury, prostate cancer, BPH, acne
What drug would I give if there is pulsatile release of GnRH that is increasing the levels of sex hormones (estrogen, progesterone, testosterone)?
GnRH antagonist–> degarelix
Note- these are used for hormone dependent cancers
What drug would I give if there is continuous release of GnRH that is increasing the levels of sex hormones (estrogen, progesterone, testosterone)?
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
What drug would you initiate with an androgen receptor antagonist?
Goserelin
What is the important synthesis pathway of hormones that are derived from progesterone?
- 17-hydroxylase makes testosterone from progesterone
- Aromatase makes estradiol (E2) from testosterone
- 5a-reductase makes DHT from testosterone
What drugs are 17-hydroxylase inhibitors (inhibit testosterone) and what are they used for?
- Abiraterone is a strong inhibitor and is used for prostate cancer
- Spironolactone is a weak inhibitor and is used for hirsutism
What drugs are 5a-reductase inhibitors (inhibit formation of DHT) and what are they used for?
Finasteride and dutasteride and are used for BPH and baldness
- Note: can cause sexual dysfunction
What drug is an aromatase inhibitor (inhibit estrogen) and what is it used for?
Anastrozole and its used for breast cancer
- Note: predicted adverse effects would be mood swings, depression, hot flashes, and decreased bone density
T/F: abiraterone should always be given with steroids like prednisone
True, if not then the patient could have hypertension and hypokalemia d/t decreased cortisol that would stimulate production of aldosterone
Tamoxifen
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
Raloxifene
MOA: acts as agonist at bone and cholesterol but antagonist in breast and uterus
Indications: breast cancer and osteoporosis
What are examples of other SERMs (idk how important these rlly are lol)
- Clomiphene blocks hypothalamus negative feedback and is used for infertility to help stimulate ovulation
- Ospemifene stimulates uterus/vagina and used in dysparenuia or painful sex
- Toremifene blocks breast tissue and used for ER+ breast cancer
- Bazedoxifene blocks bone and used for menopause HRT and prophylaxis of osteoporosis
What is ulipristal?
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
What drug blocks the estrogen receptor?
Fulvestrant and this is used in treatment for breast cancer
What drug blocks the progestin receptor?
Mifepristone and this is used in medical abortion (combined w misoprostol)
What two drugs block the androgen receptor?
- Bicalutamide which is used for prostate cancer
- Spironolactone which is used for hirsutism
T/F: Fulvestrant can prevent tumor flare when starting goserelin
False, bicalutamide is an androgen blocker and can be used to prevent tumor flare because it decreases levels of hormones responsible for the cancer
