Pharm Chapter 40- Gonadal Hormones And Inhibitors

Front 1

MOA of both estrogen and progesterone in ovulatory/menstrual cycle

Back 1

enters cells, binds to cytosolic receptors, and translocates the receptor-hormone complex into the nucleus where it modulates gene expression

Front 2

Major ovarian estrogen in women

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estradiol

Front 3

Administration of estradiol pharmacologically

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transdermal patch, vaginal cream, or intramuscular injection
long acting esters of estradiol that get converted are administered IM

Front 4

Synthetic estrogens with high bioavailability

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ethinyl estradiol, mestranol; used for oral contraceptives

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metabolic effects of estrogen

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modifies serum protein levels and reduces bone resorption; enhances coagulability of blood and increases plasma triglyceride levels while reducing LDL cholesterol and increasing HDL

Front 6

effect of continuous administration of estrogen, especially in combination with progestin

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inhibition of gonadotrophins from anterior pituitary

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Clinical use of estrogens?

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treatment of hypogonadism in young females; HRT in women with estrogen deficiency from premature ovarian failure, menopause, or ovariectomy

Front 8

Estrogen toxicity when used in hypogonadal girls?

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careful adjustment needed to prevent premature closure of the epiphyses of the long bones and short stature

Front 9

Estrogen tox when use in HRT?

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increases the risk of endometrial cancer; prevented with simultaneous administration of progestin

Front 10

Dose dependent tox of estrogens?

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mausea, breast tenderness, migraines, thromboembolic events, gallbladder disease, hypertriglyceridemia, and hypertension

Front 11

DES

Back 11

diethylstilbestrol; nonsteroidal estrogenic compound associated with infertility, ectopic pregnancy, and vaginal adenocarcinoma in the daughters of women who were treated with the drug during pregnancy

Front 12

Effects of progesterone

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induces secretory changes in the endometrium and is required for the maintenance of pregnancy

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Other effects of progesterone

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affect carbohydrate metabolism and stimulate the deposition of fat

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Long term use of high doses of progestins in premenopausal women is associated with?

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reversible decerase in bone density (2ndary to ovarian suppression and decreased ovarian production of estrogen)

Front 15

three types of oral contraceptives available for women in the US

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-combination estrogen-progestin tablets taken constant dosage throughout the menstrual cycle (monophasic preparations)
-combination preparations (biphasic/triphasic) in which progestin or estrogen dosage changes during the month
-progestin only preparations

Front 16

postcoital contraceptives: use and combination

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prevent pregnancy when administered within 72 hours after unprotected intercourse
-preparations containing a progestin alone, estrogen alone, or combination of the two

Front 17

MOA of combination contraceptives

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combo contraceptives: inhibit ovulation and exert effects on the cervical mucus glands, uterine tubes, and endometrium that decrease the likelihood of fertilization and implantation

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MOA of progestin-only contraceptives

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effect the cervical mucus glands, uterine tubes, and endometrium so that they decrease the likelihood of fertilization and implantation

Front 19

MOA of postcoital contraceptives

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inhibit ovulation when administered before the LH surge, affect cervical mucus, tubal function and endometrial lining

Front 20

Other clinical uses of contraceptives

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treatment of acne, hirsutism, dysmenorrhea, endometriosis

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Beneficial effects of contraceptive use

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reduced risk of ovarian cysts, ovarian and endometrial cancer, benign breast disease, and PID; also lower incidence of ectopic pregnancy, iron deficiency anemia, and RA

Front 22

major toxic effects of the combined hormonal contraceptives

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**increase in the risk of thromboembolic events in older women, smokers, women with a FH of this, and women with fenetic defects that affect the production of clotting factors; risk is less than that imposed by pregnancy

Front 23

Selective estrogen receptor modulators

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mixed estrogen agonists that have estrogen agonist effects in some tissues and act as partial agonists or antagonists of estrogens in other tissues

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Tamoxifen

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SERM effective in treatment of hormone-responsive breast cancer, acts as an antagonist to prevent receptor activation by endogenous estrogens

Front 25

Tamoxifen as an agonist?

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acts on endometrial receptors and promotes endometrial hyperplasia and increases the risk of endometrial cancer

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increased risk for antagonist and agonist activity of tamoxifen

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antagonist: hot flushes
agonist: venous thrombosis

Front 27

benefit of agonist>antagonist activity of tamoxifen on bone?

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prevents osteoporosis (estrogen reduces bone resorption)

Front 28

drug related to tamoxifen

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toremifene

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use of raloxifene

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prevention and treatment of osteoporosis in postmenopausal women (partial agonist on bone)

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alternative use of raloxifene

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reduces the incidence of breast cancer in women who are at very high risk because of antagonist effect in breast tissue; no estrogenic effects on endometrial tissue

Front 31

clomiphene

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nonsteroidal compound with tissue-selective actions

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use of clomiphene

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to induce ovulation in anovulatory women

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MOA of clomiphene

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selectively blocks estrogen receptors in the pituitary, reducing negative feedback and increasing FSH and LH output

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fulvestrant

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pure estrogen receptor antagonist in all tissues

Front 35

use of fulvestrant

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treatment of women with breast cancer that has developed resistance to tamoxifen

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aromatase inhibitors

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anastrazole, letrozole, exemestane

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anastrazole (letrozole)

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nonsteroidal competitive inhibitors of aromatase (enzyme in last step in estrogen synthesis)

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exemestane

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irreversible aromatase inhibitor; treatment of breast cancer

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use of GnRH agonists

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in combination with other agents in controlled ovarian hyperstimulation and treatment of precocious puberty

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GnRH agonists and short term treatment?

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endometriosis and uterine fibroids (<6 mo)

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GnRH receptor antagonists used for controlled ovarian hyperstimulation

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ganirelix and cetrorelix

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Mifepristone (RU 486)

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orally active steroid antagonist of progestrone and glucocorticoids

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use of mifepristone

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abortifacient up to 49 days after the last menstrual period; combination of mifeprisone and misoprostol achieves a complete abortion in over 95% of early pregnancies

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side effects of abortion pill (mostly due to misoprostol)

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nausea, vomiting, and diarrhea, plus vaginal cramping and bleeding assd with passing the pregnancy

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testosterone is synthesized from?

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progesterone and dehydroepiandrosterone (DHEA)

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testosterone converted to?

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dihydrotestosterone; active hormone in appropriate tissues

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drugs that have increased ratio of anabolic-androgenic action

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oxandrolone and stanozolol

Front 48

MOA of androgens

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enter cells and bind to cytosolic receptors; hormone-receptor complex enters the nucleus and modulates the expression of target genes

Front 49

effect of testosterone after puberty

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maintain secondary sex characteristics, fertility, and libido; also acts on hair cells to cause male-pattern baldness

Front 50

clinical use of androgens

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replacement therapy in hypogonadism; stimulate red blood cell production in certain anemias and to promote weight gain in patients with wasting syndromes

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androgen toxicity

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females- virilization and menstrual irregularity; virilization of fetus
excessive dose in men- feminization (gynecomastia, testicular shrinkage, infertility)--> feedback inhibition of the pituitary and conversion of exogenous androgens to estrogens

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systemic androgen toxicity

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cholestatic jaundice, elevation of liver enzymes, HCC

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flutamide

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nonsteroidal competitve antagonists of androgen receptors; decrease action of endogenous androgens in patients with prostate carcinoma

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spironolactone hormone effects

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inhibits androgen receptors and is used in treatment of hirsutism in women

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finasteride

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inhibits 5a-reductase to treat BPH; lower doses for baldness

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use of leuprolide in prostatic carcinoma

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GnRH agonist that suppresses LH and reduces production of testosterone

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GnRH receptor antagonists approved for advanced prostate cancer

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abarelix and degarelix

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MOA of combined hormonal contraceptives in treatment of androgen-induced hirsutism

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estrogen in the contraceptive acts in the liver to increase production of sex hormone-binding globulin, which reduces the concentration of free androgen that causes male pattern hair growth

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ketoconazole

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antifungal drug that inhibits gonadal and adrenal steroid synthesis; used to suppress adrenal steroid synthesis in patients with steroid-responsive metastatic prostate cancer