Sex Hormones Flashcards
Which drugs are GnRH agonists? How are they different from antagonists?
Leuprolide and Goserelin
They have a longer lasting effect
Which drugs are GnRH antagonists?
Cetrorelix and Ganirelix
What are GnRH drugs used for?
precocious puberty, endometriosis, etc.
How do you treat metastatic prostate cancer?
With an antiandrogen, avoid using an agonist because of initial surge of Testosterone
What two drugs are used to mimic LH and FSH? Which one is FSH only?
hMG and Urofollitropin; Uro is FSH only
What does LH do? Which drug is used to replace LH?
causes ovulation and increases progesterone; hCG is used to stimulate ovulation and for steroid production (controls when LH surge happens)
What are LH and FSH used for?
REVERSING INFERTILITY
What are the SE of gonadotropins?
Mostly trophic effects except for OHS: EMERGENT SITUATION! vascular perm increases, fluid builds up everywhere, hypovolemic, will go into shock! If you start feeling really bad, get to ER immediately
What is the MOA for estrogens?
binds to a nuclear receptor because they are lipophilic, but that means they take time
How are estrogens metabolized?
by the liver, they enter enterohepatic circ which increases T1/2
What are major adverse effects of estrogen?
- Endometrial hyperplasia
- Nausea and breast tenderness
- MIGRAINES– leads to OHS
- Gallbladder disease
- HYPERTENSION
- Thromboembolism, thrombophlebitis; increased platelet aggregation; accelerated blood clotting
What are contraindications for estrogen use?
Estrogen-dependent neoplasms (e.g. breast cancer) •Undiagnosed genital bleeding •Uncontrolled hypertension •Liver disease •Thromboembolic disorders •Smoking & over 35 •Pregnancy
What are the estrogens?
Ethinyl estradiol (Not available individually)
Estradiol (Estraderm®)
Conjugated estrogens (Premarin®)
Estropipate (Ogen®)
What are the SERMs (can be agonist or antagonist)?
Tamoxifen, Toremifene, Raloxifene, Clomiphene
What are indications for tamoxifen or toremifene use as an antagonist?
for palliative tx of PREMENOPAUSAL breast CA
What are effects of tamoxifen and toremifene as an agonist
LIMITS BONE LOSS but may increase risk of uterine CA
Which SERM is better to use for a person with already low HDL?
Toremifine
Which of the antiestrogens is not a SERM but a complete antagonist? What sx does it cause?
Fulvestrant; menopausal type sx
not used due to use of aromatase inhibitors
Which SERM antagonizes negative feedback of estrogen in hypothalamus to increase LH and FSH thereby inducing multiple pregnancies as a side effect of medication?
CLOMIPHENE
What drugs are aromatase inhibitors?
Anastrozole, letrozole, exemestrane
What drugs are used as the DOC for breast cancer treatment in postmenopausal women as well as for advanced breast cancer after tamoxifen failure in postmenopausal women?
Aromatase inhibs
What are absolute CI of aromatase inhibs?
PGN, premenopause
What are AR of aromatse inhibs?
Post menopausal, abd pain, N/V/D
Which progestins have both progestin and androgenic activity? What are their names?
19-nortestosterones: Levonorgestrel (Plan B®) Norethindrone (Aygestin®) Norgestrel (Ovrette®) Norgestimate
What are some SE of progestins?
Possible increased blood pressure
High doses may reduce plasma HDL levels
(19-nortestosterones esp)
Depression and drowsiness
Which antiprogestin acts as both a porgesterone and glucocoricoid receptor antagonist and is used for abortions? Who is it CI in?
Mifepristone; PGN
Which antiprogestin is a weak progestin and androgen used to treat endometriosis?
danazol
What are the two progesterone derivatives?
Medroxyprogesterone (Provera®)
Megestrol (Megace®)
What drug has the ability to reduce water retention, thus it is the only combination pill that is FDA approved for reducing PMDD symptoms?
Drospirenone/ethinyl estradiol (Yasmin, Yaz); Estrogen and spiro derivative with progesterone agonist effects!!!
What are main adverse effects of combination oral contraceptives?
–Increased breakthrough bleeding, especially during first year
–Hard to tell if you are pregnant and should have discontinued pill
What are the combination oral contraceptives?
Norethindrone/ ethyinyl estradiol (Brevicon®, Modicon®, Ovcon®)
Levonorgestrel/ ethinyl estradiol (Triphasil®, Tri-Levlen®)
Norethindrone acetate/ ethinyl estradiol (Loestrin®)
Norgestrel/ ethinyl estradiol (Ovral®)
Norethindrone/mestranol (Norinyl®, Ortho-Novum®)
Norgestimate/ethinyl estradiol (Ortho Tri-Cyclen®)
Drospirenone/ethinyl estradiol (Yasmin®, Yaz®)
Dienogest/estradiol valerate (Natazia®)
What three drugs are used for post-coital contraception?
Mifepristone, Levonorgesterel (P only), Preven (E&P)
What are major adverse effects of combined oral contraceptives?
- Cardiovascular problems, esp clotting in smoking women over 35, Mild hypertension, Migraine, MI/Stroke
- Cholestatic jaundice and gallbladder disease
- Teratogenesis
- Fertility – can be suppressed for 3+ months
What are some major benefits form combined oral contraceptives?
Ovarian & Endometrial cancer
50% reduction in endometrial and ovarian cancer, even after 2 years of treatment, lasts 15 years following d/c
What are absolute contraindications for combined oral contraceptives (not progesterone based)?
- Thrombophlebitis
- Thromboembolic phenomena
- Cerebrovascular disorders
- Estrogen-dependent neoplasms
- Pregnancy
What are RELATIVE contraindications for combined oral contraceptives?
LIVER DISEASE •Adolescents prior to epiphyseal closure •Asthma; eczema •Migraine; hypertension DIABETES •Optic neuritis; retrobulbar neuritis •Seizure disorders SMOKING OVER 35
What do oral contraceptives decrease the effectiveness of?
–Anticoagulants –Anticonvulsants –Tricyclic antidepressants –Guanethidine –Oral hypoglycemics
What drugs will reduce the effectiveness of oral contraceptives?
•P450 inducers reduce effectiveness
–phenytoin, rifampin, carbamazepine, etc.
•Antibiotics can reduce effectiveness
–Stop enterohepatic circulation
What should you give a woman for HRT who has had a hyster?
Estrogen only because they have no endometrium for the progesterone to inhibit hyperplasia of
What are adverse effects of HRT?
–Endometrial cancer – progestins reduce –Breast cancer – small risk (1.25 fold) •8 cases per 10,000 women/year –Gallbladder disease (2.5 fold) –Cardiovascular
In what age group could estrogen be the most effective for cardioprotection and breast cancer protection?
age 50-59
What is the general guideline for HRT?
10 Years after menopause = HRT is not so great
What is an option Dr. Call would recommend for using HRT?
Put a woman on ERT for 10 years, then 10 years with raloxifene, then switch something else, if anything because at this point we have protected bones for long enough that we are out of the woods and might not even need estrogen
What are androgens used for in men? Women? Both?
Men: Testicular deficiency Female hypopituitarism (estrogens and androgens) Both: to treat hypoproteinemia of nephrosis and negative nitrogen balance patients (burns, etc)
What two drugs are found in the androgen category?
testosterone and methyl-testosterone
What drugs are considered anti-androgens?
Flutamide, bicalutamide, nilutamide, spironolactone
What drug works as an androgen receptor antagonist to treat prostate cancer in combo with a long acting GnRH agonist?
Flutamide, just given until GnRH agonist kicks in
What drugs are considered 5a-reductase inhibitors?
Finasteride and Dutasteride
What some indications for use of finasteride and dutasteride?
BPH, male pattern baldness: suppressess male sex accessory organs without affecting libido
What are some side effects of 5-alpha reductase inhibitors?
POTENT TERATOGEN!
Which SERM is used to treat breast cancer with a decreased risk of uterine CA?
Raloxifene
