Gonadal Hormones Flashcards
(34 cards)
Prolactin feed back inhibits the release of what? leading to what?
GnRH - leading to decreased spermatogenesis or ovulation
ACTH acts on what enzyme to increase synthesis of cortisol?
desmolase (cholesterol to pregnenolone)
Name 2-6 important physiological functions of estrogen that are NON-reproductive
prevent bone loss
lead to closure of epiphyseal plates in long bones
pro-coagulation state (+)
increase HDL and lower LDL
increase binding protein levels of some hormones (free levels are unaffected)
increase cholesterol in bile (form gallstones)
Which estrogen is a prodrug that gets converted to ethinyl estradiol and is present in some contraceptives?
Mestranol
How are oral contraceptives metabolized? What drugs can decrease their efficacy?
P450 system - CYP inducers decrease their efficacy by leading to more rapid breakdown
exposure to diethylstilbestrol in utero can lead to what complications in the fetus?
(DES) if female, fetus can have infertility and vaginal cancer
Name the 4 ABSOLUTE contraindications of estrogen use
- history of thromboembolism
- breast and endometrial cancer
- pregnancy
- liver disease
Which SERM has an increased risk of endometrial cancer due to agonist affects there?
Tamoxifen
Which SERM can be used as prophylaxis for breast cancer in high risk patients? What does it also help prevent?
Raloxifene
also agonistic on bone - prevents osteoporosis
Patient at high risk of breast cancer who has had endometrial cancer in the past can be treated with which SERM?
Raloxifene - antagonistic in breast with no effects on endometrium
Which drug can be given IM in the treatment of breast cancer that is resistant to Tamoxifen? What class of drug is this?
Fulvestrant - SERD (selective estrogen receptor downregulator)
What does the enzyme aromatase do? Name three drugs that inhibit it. Which is irreversible?
Converts androgens to estrogen
Letrozole, Anastrozole, and Exemestane (irreversible)
Which drug helps treat female infertility by acting as an estrogen antagonist in the hypothalamus and anterior pituitary? How does this work?
Clomiphene - prevents feedback inhibition of GnRH release in hypothalamus so anterior pituitary releases LH and FSH
Clomiphene - type of drug and side effects (4)
SERM in hypothal and ant pituitary
ovarian hyper-stimulation syndrome
ovarian enlargement
multiple pregnancy
visual disturbances
Which drug is a spironolactone derivative that is used in OC to treat acne in females? How does it work?
Drospirenone - antagonizes aldosterone effects
Name 4 of the new preparation progestins. What advantage do they have over the old?
Desogestrel, Norelgestromin, Etonogestrel, Norgestimate
fewer androgenic effects
Which drug is used as the “morning after” pill or as an abortifacient? what type of drug is it?
Mifepristone - antiprogestin
Which androgen is most potent in males that leads to male pattern baldness and BPH? What enzyme is responsible for its creation?
DHT
made from testosterone by 5-alpha-reductase
What are the two synthetic androgens that are more potent and have less andorgenic effects? What do they treat? How are they given?
Oxandrolone and Stanozolol
treats hypogonadism and increase bone density (osteoporosis)
transdermal, buccal, or subcutaneous implant
Excess use of androgens in males can lead to what adverse effects?
feminization (lolololol) - gynecomastia, testicular shrinkage, infertility (due to feedback inhibition)
Androgen receptor antagonist drugs have what ending? Name 3
- lutamide
Flutamide, Bicalutamide, Nilutamide
Name the 5-alpha-reductase inhibitor. What is it used for?
finasteride - treats BPH
Name the steroid synthesis inhibitor that is used to treat advanced prostate cancer that is resistant to first line drugs
Ketoconazole
What drugs can be used to produce reversible medical castration? (name and class) - what is important to remember about giving them?
Leuprolide and gonadorelin (antiandrogens - GnRH analogs)
must be given continuously (pulsatile has the opposite effect)
