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66 Cards in this Set
- Front
- Back
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Describe the effects of GnRH on the pituitary in both pulsatile and constant secretion patterns
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GnRH is released from the hypothalamus and causes the pituitary to release both FSH and LH.
When release in a pulsatile manner, it causes the pituitary to release the hormones, but a constant release will inhibit pituitary hormone release |
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What is the function of FSH?
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It stimulates follicular development and estrogen secretion and induces LH receptor formation
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What is the function of LH?
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To maintain the corpus luteum and to stimulate ovulation (mid-cycle surge)
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What are the main effects of estrogens?
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1) primary and secondary sexual characteristics
2) proliferation of the endometrium 3) increased uterine and tubal motility 4) watery cervical secretions |
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What are the "side effects" of estrogens (either exogenous or endogenous)?
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Bloating, edema, and thrombosis develop due to:
1) Na+ and water retention 2) Increase in clotting factors 3) Lipid alterations (increased HDL decreased LDL) |
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What are the main effects of progestins?
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1) development of the secretory endometrium
2) viscous cervical secretions 3) decreased uterine motility 4) increased temp 5) maintenance of pregnancy 6) suppression of LH release |
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Conditions in the female reproductive tract are optimized for implantation or maintenance of pregnancy when under the effects of what hormones?
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progestins
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Conditions in the female reproductive tract are optimized for fertilization when under the effects of what hormones?
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estrogens
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What causes the surge in LH which leads to ovulation?
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A rapid rise in estrogen concentration in late follicular phase
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What happens if pregnancy does not occur?
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The decline in LH leads to the loss of function of the corpus luteum and menses ensues
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What maintains the corpus luteum if fertilization-implantation occurs?
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human chorionic gonadotropin
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What is the ultimate precursor for both estradiol and progesterone?
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cholesterol
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From what molecules are estrogens derived and what is the enzyme that makes the conversion?
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Estrogens are derived from androgens (androstenedione, testosterone, DHEA) and are converted by the enzyme aromatase
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Where is the majority of estrogen made in the premenopausal female? Postmenopausal?
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In premenopausal females, most of the estrogen comes from the ovary
In postmenopausal females, most of the estrogen comes from other tissues such as the adrenal and fat |
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What kind of molecule are GnRH and it's analogs and how does this affect pharmacokinetics?
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They are small peptides which cannot be given p.o. but can be used nasally
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What kind of molecules are FSH, LH and hCG ?
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Large glycoproteins
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What kind of molecules are estrogens, progestins, and similar analogs and what effect does this have on pharmacokinetics?
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They are steroids which are very lipophilic and absorbed well from the gut, skin, but undergo extensive first pass metabolism
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Describe the two cell model
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LH binds to receptors on theca cells, and cholesterol is converted into testosterone which diffuses into the granulosa cells, which convert it into estradiol/estrone via aromatase (which is stimulated by FSH)
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What are the estrogen receptor agonists?
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1) estradiol and its esters
2) estrone 3) conjugated estrogens |
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How is first pass metabolism of estrogens blunted?
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By the addition of ethinyl groups on the 17 carbon (17-ethinylation)
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What maintains the corpus luteum if fertilization-implantation occurs?
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human chorionic gonadotropin
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What is the ultimate precursor for both estradiol and progesterone?
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cholesterol
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From what molecules are estrogens derived and what is the enzyme that makes the conversion?
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Estrogens are derived from androgens (androstenedione, testosterone, DHEA) and are converted by the enzyme aromatase
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Where is the majority of estrogen made in the premenopausal female? Postmenopausal?
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In premenopausal females, most of the estrogen comes from the ovary
In postmenopausal females, most of the estrogen comes from other tissues such as the adrenal and fat |
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What kind of molecule are GnRH and it's analogs and how does this affect pharmacokinetics?
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They are small peptides which cannot be given p.o. but can be used nasally
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What kind of molecules are FSH, LH and hCG ?
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Large glycoproteins
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What kind of molecules are estrogens, progestins, and similar analogs and what effect does this have on pharmacokinetics?
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They are steroids which are very lipophilic and absorbed well from the gut, skin, but undergo extensive first pass metabolism
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Describe the two cell model
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LH binds to receptors on theca cells, and cholesterol is converted into testosterone which diffuses into the granulosa cells, which convert it into estradiol/estrone via aromatase (which is stimulated by FSH)
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What are the natural estrogen receptor agonists and why are they poor drugs?
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1) estradiol and its esters
2) estrone 3) conjugated estrogens They have extensive first pass metabolism in the liver which limits oral utility |
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How is first pass metabolism of estrogens blunted?
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By the addition of ethinyl groups on the 17 carbon (17-ethinylation)
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Which synthetic estrogen is teratogenic and what does it cause?
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diethylstilbesterol; it causes vaginal adencarcinoma to develop in the offspring of women who took the drug during pregnancy
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What are the semi-synthetic estrogen receptor agonists?
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1) 17- ethinylestradiol
2) mestranol |
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Why do natural estrogens have limited oral utility and what is done to overcome this?
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They have extensive first-pass metabolism, this is overcome with 17 ethinylation
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What are the xenoestrogens?
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These are ubiquitous estrogen compound
1) phytoestrogens (from plants) 2) environmental estrogens (DDT) 3) endocrine disruptors - genistein |
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What are the three major ways to inhibit estrogen action?
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1) interfere with gonadotropin release and subsequent ovarian estrogen production
2) inhibit synthesis (aromatase inhibitors) 3) block the estrogen receptor |
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What are two examples of estrogen receptor antagonists and for what are they commonly used?
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1) clomiphene - anovulatory infertility treatment
2) tamoxifen - estrogen dependant cancer |
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What are two examples of aromatase inhibitors?
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1) anastrazole
2) exemestane They do not cause an interference with the H-P-O axis |
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What is a SERM and what is an example?
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Selective estrogen receptor modulators - drugs that have a selectivity for subclasses of estrogen receptors - an e
xample is raloxifene |
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What is the therapeutic use of raloxifene?
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It maintains bone mass in post-menopausal women without extreme stimulation of breast or uterine tissue
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What are examples of progesterone receptor agonists?
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1) progesterone
2) medroxyprogesterone 3) 19-Nortestosterones (norethindrone, norethyndrel, norgestrel, ethynodiol) |
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Which synthetic estrogen is teratogenic and what does it cause?
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diethylstilbesterol; it causes vaginal adencarcinoma to develop in the offspring of women who took the drug during pregnancy
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What are the semi-synthetic estrogen receptor agonists?
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1) 17- ethinylestradiol
2) mestranol |
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Why do natural estrogens have limited oral utility and what is done to overcome this?
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They have extensive first-pass metabolism, this is overcome with 17 ethinylation
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What are the xenoestrogens?
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These are ubiquitous estrogen compound
1) phytoestrogens (from plants) 2) environmental estrogens (DDT) 3) endocrine disruptors - genistein |
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What are the three major ways to inhibit estrogen action?
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1) interfere with gonadotropin release and subsequent ovarian estrogen production
2) inhibit synthesis (aromatase inhibitors) 3) block the estrogen receptor |
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What are two examples of estrogen receptor antagonists and for what are they commonly used?
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1) clomiphene - anovulatory infertility treatment
2) tamoxifen - estrogen dependant cancer |
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What are two examples of aromatase inhibitors?
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1) anastrazole
2) exemestane They do not cause an interference with the H-P-O axis |
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What is a SERM and what is an example?
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Selective estrogen receptor modulators - drugs that have a selectivity for subclasses of estrogen receptors - an e
xample is raloxifene |
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What is the therapeutic use of raloxifene?
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It maintains bone mass in post-menopausal women without extreme stimulation of breast or uterine tissue
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What are examples of progesterone receptor agonists?
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1) progesterone
2) medroxyprogesterone 3) norethindrone 4) norethynodrel |
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What is norethindrone?
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This is the prototype of the 19-nortestosterone family of progestins
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What happens if you remove the C-19 of an androgen?
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It changes it to a progestin
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Name the members of the 19-Nortestosterone class; what function do they have?
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They are progesterone receptor agonists
1) norethynodrel 2) norgestrel 3) norethindrone 4) ethynodiol |
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Name the progesterone receptor antagonist and for what is it used?
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Mefipristone is used as an abortifactant; promotes uterine contractility
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What can be used to mimic pituitary function and stimulate the ovary in fertility therapy?
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1) FSH (urofolliculin)
2) FSH + LH (menotropins) 3) hCG |
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What are the uses of exogenous GnRH analogs and gonadotropins?
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To mimic pituitary function and stimulate the ovary in fertility therapy
and to inhibit pituitary gonadotropin secretion and decrease ovarian function |
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What exogenous GnRH analogs and gonadotropins are used to inhibit pituitary gonadotropin secretion and decrease ovarian function?
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1)Danazol - anti-gonadotropin
2) leuprolide 3) gonadorelin 4) nafarelin 5) goserelin |
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What is danazol and how does it work?
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It is an anti-gonadotropin that exerts negative feedback on the pituitary without estrogenic effects; useful in endometriosis
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How should the sustained release GnRH analogs be given?
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Constant administration in the form of a depot injection or nasal spray
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How can pituitary gonadotropin secretion be stimulated?
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Pulsatile administration of GnRH analogs
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What are some common uses of estrogenic agents besides oral contraception?
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Dysmenorrhea
Hirsutism post-menopausal osteporosis menopause |
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What is the most likely possible benefit of hormone replacement therapy in post-menopausal women?
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decreased risk of osteoporosis
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What are the major uses for anti-estrogens?
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1) hormone responsive tumors
2) endometriosis |
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What drugs are used to treat cancers that are derived from estrogen hormone dependent tissues (such as breast, prostate, uterus)?
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estrogen receptor inhibitors and aromatase inhibitors
Breast cancers that express estrogen receptors respond well to anti-estrogen drugs |
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What pharmacotherapy is used for endometriosis?
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GnRH analogs and danazol
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What are the major uses of progestins?
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1) dysfunctional uterine bleeding
2) contraception 3) abortion |
