Flashcards in Estrogens, Progestrins, And Androgens Deck (55):
What is the main estrogen made by the ovary?
What 2 estrogens are made by conversion from androgens in the liver and adrenal glands?
Estrone and estriol
Which estrogen is high is high in pregnancy?
Where is estrogen made in the male?
Made by Sertoli cells in the testis
What is the enzyme used to convert testosterone to estrogen in the testis?
What are the physiological effects of estrogen?
1. Development of sex organs and secondary sex characteristics
2. Closure of the epiphyseal plates
3. Stimulate ductal development in breast
4. Pigmentation in the skin
5. Increase binding globulins
6. Increase HDL, decrease LDL
7. Reduce bone resorption
8. Enhance coaguability
9. Libido, mood
Where is progesterone produced in the female?
By the corpus luteum
During pregnancy: placenta
What are the physiological effects of progesterone?
1. Matures endometrium
2. Development of secretory apparatus of the breast
3. Increases body temp
4. Depressants effects, sedatives
How does progesterone or its metabolites make inhibitory effects?
Hits GABBA A receptor
How much testosterone is freely circulating?
What are the effects of testosterone?
1. Growth of pubic hair, axillary hair, beard
2. Growth of larynx, thickening of vocal chordsSebum secretion
3. Decrease binding globulin
4. Stimulate EPO secretion
5. Anabolic effects
What is oxymetholone?
17-alkyl deriv of testosterone
What oxymetholone used to treat?
Bone marrow hypoplasia, myelofibrosis
What are 17-alkyl derivatives associated with?
Hyperbilirubinemia, increased hepatic enzymes, cholestatic hepatitis,
What is the bioavailability of estradiol?
What may alter the efficacy of oral estrogens?
Broad spectrum antibiotics that alter intestinal flora
What drugs might estrogens alter the metabolism of?
Drugs metabolized by glucoronidases. Like acetaminophen
What is the MOA of oral contraceptives?
Exert negative feedback on the hypothalamus and pituitary --
1. Reduce GnRH
2. Reduce FSH secretion - incomplete follicular development
3. Reduce LH secretion - no ovulation
How do OCs affect sperm and endometrium?
It thickens the cervical mucous to reduce sperm.
It alters the endometrial structure makes the uterus unreceptive for implantation
What is the most commonly used estrogen in OCs?
What are th most commonly used progesterones?
What is the potency of the progesterones used?
3. Norgestimate, norethindrone
Which progesterone has an increased risk of thromboembolism?
Which estrogen has androgenicity that is similar to spironolactone?
Drospirenone in Yasmin
What are the advantages of triphasic OCs?
Less spotting, breakthrough bleeding and amenorrhea
Who do we use progestin only on?
Women at risk for certain estrogen-dependent cancers or who don't tolerate the estrogen portion in OCs or who are breast feeding
What is the disadvantage of using progestin only?
It is not as effective at inhibiting ovulation
What is injectable progestin for?
For long term contraception
Who is injectable progestin not good for?
Women who want to get pregnant soon after treatment
What are the disadvantages of implantable progestin?
Need for surgical implantation and removal
What can lower the efficacy of OCs?
What are the side effects of estrogen?
TE - increases clotting factors and decreases antithrombin III
Increase risk of MI
Nausea - heightened sense of smell
Headache or worsens migraines - converts tryptophan to nicotinic acid
Cancer of breast, cervix, liver
What are the side effects of progestin?
Increased appetite - increase in the amount of insulin
Increase acne and CV disease
What are the contraindications to OCs?
Women with history of estrogen-dependent neoplasm or breast cancer
What is plan b?
It is a high dose of levonorgestrel
What is RU486?
Mifepristone - has a luteolytic effect, usually combined with a prostaglandin which may trigger uterine contraction
What is DES?
May interfere with timing of uterine maturation
What are the post coital contraceptives?
What is hormone replacement used for?
Reducing menopause symptoms
Treating primary hypogonadism (ovarian failure, hypopituitarism)
What is the treatment for menopause?
Low dose estrogen and a progestin
What are the HRTs for menopause?
Conjugated equine estrogen
Metroxy-progesterone acetate (provera)
Prempro (CEE + MPA)
What are progestins given for in menopause?
For reducing endometrial and uterine cancer
What are the benefits of HRT?
Reduces heart attacks and strokes
Reduces hot flashes
Decreases bone loss
What are the problems with HRT?
Poor compliance because of bleeding and fear of cancer.
What are the side effects with estrogen in HRT.
What are the contraindications to HRT?
Hx of estrogen dependent cancers
What are the advantages of transdermal estradiol?
Reduced conversion of estradiol to estrone
Little risk for TE
No effect of SHBG
What is the disadvantage of transdermal estradiol?
May not cause increase in HDL or lower LDL
What is can androgen therapy be used for?
Reverse atrophy following trauma, surgery, disease
What are the side effects of androgen therapy?
Masculinizing effects or gynecomastia
What are the contraindications to androgens?
Hx of prostate or breast cancer
What are the disorders or androgen excess?
Prostatic hyperplasia - urinary retention
What drugs can be used for hirsutism?
AR antagonist - spironolactone, flutamide
DHT synthesis inhibitors - finasterides, dutasteride
Eflornithine cream - ornithine decarbox inhibitor
What is clomiphene?
A partial estrogen agonist - reduces negative feedback so increases gonadotropins and estrogens