Gonadal Hormones and Inhibitors Flashcards by Jamaira Belmes

MOA of Estrogens

activation of estrogen receptor leads to changes in rates of transcription of estrogen regulated changes

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Estrogens

Ethinyl estradiol
Mestranol
Estrogen esters

hypogonadism in girls
HRT

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A prodrug that is converted to ethinyl estradiol contained in some contraceptives

Mestranol

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Long acting estrogens administered IM and used for hypogonadism in young females

Estrogen esters

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MOA of Progestins

activation of progesterone receptors leads to changes in rates of transcription of progesterone regulated genes

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Progestins

Norgestrel
Megestrol acetate
Norethindrone
Ethynodiol
Desogestrel
Norelgestromin
Noregestimate
Etonogestrel
Drospirenone

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Progesterone derivatives

Medroxyprogesterone acetate

Megestrol acetate

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Older 19-nortestosterone derivatives

Norethindrone

Ethynodiol

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Newer 19-nortestosterone derivatives

Desogestrel
Norelgestromin
Noregestimate
Etonogestrel

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Spironolactone derivatives

Drospirenone

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Hormone Replacement Therapy

ESTROGEN: Conjugated estrogens, Estradiol, Estrone, Estriol

PROGESTIN: Progesterone, Medroxyprogesterone acetate

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Oral Hormonal Contraceptive

COMBINED: Ethinyl estradiol or Mestranol PLUS Progestin

PROGESTIN ONLY: Norethindrone or Norgestrel

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Estrogen ANTAGONIST actions in breast tissue and CNS

Estrogen AGONIST effects in liver and bone

for prevention and adjuvant treatment of hormone-responsive breast cancer

ANTIESTROGENS

Selective Estrogen Receptor Modulators (SERMS)

Tamoxifen
Bazedoxifene
Clomiphene

SE:
hot flushes
DVT
Endometrial hyperplasia
Endometrial cancer

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Approved for osteoporosis and prevention of breast cancer in selected patients

ANTAGONIST effects in breast, CNS and endometrium

AGONIST effects in liver

Preferred in patients with HISTORY OF BREAST CANCER in the management of hot flushes

Raloxifene

SE:
hot flushes
DVT

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Approved for the treatment of MENOPAUSAL SYMPTOMS and PROPHYLAXIS OF POSTMENOPAUSAL OSTEOPOROSIS in combination w/ conjugated estrogens

Bazedoxifene

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Partial agonist at estrogen receptor

antagonist effect in pituitary increases gonadotropin secretion

used for ovulation induction

Clomiphene

SE:
multiple pregnancies
ovarian enlargement
headache
constipation

increased risk of low grade ovarian cancer with long term use

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Used for INFERTILITY

Clomiphene
hMG and hCG
GnRH analogs
Progesterone
Bromocriptine

Estrogen receptor antagonist in all tissues

Adjuvant treatment of hormone-responsive breast cancer that is resistant to 1st line anti-estrogen therapy

RECEPTOR ANTAGONIST

Fulvestrant

Reduces estrogen synthesis by inhibiting aromatase enzyme

adjuvant treatment of hormone-responsive breast cancer

precocious puberty

AROMATASE INHIBITORS

Anastrozole
Letrozole
Exemastane

Weak cytochrome P450 inhibitor and partial agonist of progestin and androgen receptors

Danazol

for endometriosis, fibrocystic breast disease

Progestin and glucocorticoid receptor antagonist

ANTIPROGESTIN

Mifepristone

Androgen receptor agonist

for male hypogonadism
weight gain in patients w/ wasting syndrome

ANDROGEN RECEPTOR AGONIST

Testosterone
Fluoxymesterone, Methyltestosterone
Testosterone esters

Inhibition of 5-alpha reductase enzyme that converts testosterone to dihydrotestosterone

for BPH, male pattern hair loss

5 ALPHA REDUCTASE INHIBITORS

Finasteride
Dutasteride

Competitive Inhibition of Androgen Receptor

for advanced prostate cancer

RECEPTOR ANTAGONISTS

Flutamide
Bicalutamide
Nilutamide

Mineralocorticoid receptor antagonist used mainly as a potassium-sparing diuretic Also has androgen receptor antagonistic activity

Spironolactone hirsutism

Inhibition of cytochrome P450 enzymes involved in androgen synthesis

SYNTHESIS INHIBITOR Ketoconazole advanced prostate cancer that is resistant to 1st line antiandrogen drugs

NATURAL ANDROGENS

Testosterones Androstenedione senile osteoporosis HRT (males) hypogonadism

SYNTHETIC ANDROGENS (Androgenic)

Methyltestosterone | Fluoxymeterone

SYNTHETIC ANDROGENS (Anabolic)

Danazol Nandrolone Oxandrolone Stanozolol

A teenager seeks postcoital contraception. Which of the following preparations will be effective for this purpose? (A) Clomiphene (B) Tamoxifen (C) Diethylstilbestrol (DES) (D) Mifepristone

(D) Mifepristone Mifepristone, an antagonist at progesterone and glucocorticoid receptors, has a luteolytic effect and is effective as a postcoital contraceptive. When combined with a prostaglandin, it is also an effective abortifacient

A 23-year-old woman desires a combined oral contraceptive for pregnancy protection. Which of the following patient factors would lead a health professional to recommend an alternative form of contraception? (A) Evidence of hirsutism (B) History of gastroesophageal reflux disease and is currently taking omeprazole (C) History of pelvic inflammatory disease (D) History of migraine headache that is well controlled by sumatriptan (E) She plans to use this contraceptive for about 1 year and will then attempt to become pregnant

(D) History of migraine headache that is well controlled by sumatriptan

Men who use large doses of anabolic steroids are at increased risk of which of the following? ``` (A) Anemia (B) Cholestatic jaundice and elevation of aspartate transaminase levels in the blood (C) Hirsutism (D) Hyperprolactinemia (E) Testicular enlargement ```

(B) Cholestatic jaundice and elevation of aspartate transaminase levels in the blood In men, large doses of anabolic steroids are associated with liver impairment, including cholestasis and elevation of serum concentrations of transaminases

A 50-year-old woman with a positive mammogram undergoes lumpectomy and a small carcinoma is removed. Biochemical analysis of the cancer reveals the presence of estrogen and progesterone receptors. After this procedure, she will probably receive which of the following drugs? ``` (A) Danazol (B) Flutamide (C) Leuprolide (D) Mifepristone (E) Tamoxifen ```

(E) Tamoxifen

A 60-year-old man is found to have a prostate lump and an elevated prostate-specific antigen (PSA) blood test. Magnetic resonance imaging suggests several enlarged lymph nodes in the lower abdomen, and an x-ray reveals 2 radiolucent lesions in the bony pelvis. This patient is likely to be treated with which of the following drugs? ``` (A) Anastrozole (B) Desogestrel (C) Leuprolide (D) Methyltestosterone (E) Oxandrolone ```

(C) Leuprolide Leuprolide is a GnRH agonist used in the treatment of men with prostate cancer. Continuous use leads to downregulation of testosterone production. Initially, the agonist action increases testosterone, causing a tumor flare. To prevent this, flutamide, a competitive antagonist of the androgen receptor, is added until downregulation of testosterone is complete

A young woman complains of abdominal pain at the time of menstruation. Careful evaluation indicates the presence of significant endometrial deposits on the pelvic peritoneum. Which of the following is the most appropriate medical therapy for this patient? (A) Flutamide, orally (B) Medroxyprogesterone acetate by intramuscular injection (C) Norgestrel as an IUD (D) Oxandrolone by intramuscular injection (E) Raloxifene orally

(B) Medroxyprogesterone acetate by intramuscular injection In endometriosis, suppression of ovarian function and production of gonadal steroids are useful. Intramuscular injection of relatively large doses of medroxyprogesterone provides 3 months of an ovarian suppressive effect because of inhibition of pituitary production of gonadotropins

Diethylstilbestrol (DES) should never be used in pregnant women because it is associated with which of the following? (A) Deep vein thrombosis (B) Feminization of the external genitalia of male offspring (C) Infertility and development of vaginal cancer in female offspring (D) Miscarriages (E) Virilization of the external genitalia of female offspring

(C) Infertility and development of vaginal cancer in female offspring Diethylstilbestrol (DES) is a nonsteroidal estrogen agonist. Several decades ago, misguided use of the drug in pregnant women appears to have resulted in fetal damage that predisposed female offspring to infertility and a rare form of vaginal cancer.

Which of the following is a unique property of SERMs? (A) Act as agonists in some tissues and antagonists in other tissues (B) Activate a unique plasma membrane-bound receptor (C) Have both estrogenic and progestational agonist activity (D) Inhibit the aromatase enzyme required for estrogen synthesis (E) Produce estrogenic effects without binding to estrogen receptors

(A) Act as agonists in some tissues and antagonists in other tissues

Finasteride has efficacy in the prevention of male-pattern baldness by virtue of its ability to do which of the following? (A) Competitively antagonize androgen receptors (B) Decrease the release of gonadotropins (C) Increase the serum concentration of sex hormone-binding globulin (D) Inhibit the synthesis of testosterone (E) Reduce the production of dihydrotestosterone

(E) Reduce the production of dihydrotestosterone

A 52-year-old postmenopausal patient has evidence of low bone mineral density. She and her physician are considering therapy with raloxifene or a combination of conjugated estrogens and medroxyprogesterone acetate. Which of the following patient characteristics is most likely to lead them to select raloxifene? ``` (A) Previous hysterectomy (B) Recurrent vaginitis (C) Rheumatoid arthritis (D) Strong family history of breast cancer (E) Troublesome hot flushes ```

(D) Strong family history of breast cancer Conjugated estrogens and raloxifene both improve bone mineral density and protect against osteoporosis. The 2 advantages of raloxifene over full estrogen receptor agonists are that raloxifene has antagonist effects in breast tissue and lacks an agonistic effect in endometrium. If a patient’s uterus was removed by surgery, the difference in the endometrial effect is moot. In patients with a strong family history of breast cancer, raloxifene may be a better choice than a full estrogen agonist because it will not further increase the woman’s risk of breast cancer and may even lower her risk.

Synthetic Estrogen associated with INFERTILITY, ECTOPIC PREGNANCY SE: CLEAR CELL CARCINOMA ADENOCARCINOMA

Diethylstilbestrol (DES)

ANDROGEN RECEPTOR AGONIST Marked progestational effect that suppresses the feedback enhancement of LH and FSH for hirsutism, component of OCP

Cyproterone, Cyproterone Acetate ``` SE: hepatotoxicity adrenal suppression depression gynecomastia ```