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MATERNAL HEALTH > FEMALE SEX HORMONES > Flashcards

FEMALE SEX HORMONES Flashcards

1
Q

What are the female sex hormones

A

Estrogens
Progestogens

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2
Q

Which enzyme synthesizes estrogens

A

Aromatase

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3
Q

The four natural estrogens

A

Estrone E1
Estradiol E2
Estriol. E3
Estetrol E4

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4
Q

Estrogens receptors

A

Estrogen receptor alpha
Estrogen receptor beta

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5
Q

Potency of estrogens

A

Estradiol > Estrone > Estriol

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6
Q

Potency of estrogens

A

Estradiol > Estrone > Estriol

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7
Q

Major Source of natural estrogens

A

Ovaries in premenopausal women
Adipose tissue in post menopausal women
Placenta in pregnancy

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8
Q

Function of 17B- hydroxysteroid dehydrogenase type 1

A

Production of testosterone from androstenedione
and estradiol from estrone in the ovaries

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9
Q

Function of 17B- hydroxysteroid dehydrogenase type 2

A

Conversion of estradiol to estrone in the liver

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10
Q

Precursors for estrogens

A

Estetrol from estriol
Estriol from estradiol and estrone
Estradiol from testosterone
Estrone from androstenedione

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11
Q

Which estrogen is synthesized solely in pregnancy

A

Estetrol from the fetal liver

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12
Q

Developmental effects of estrogen in women

A

Pubertal growth spurt of long bones
Breast enlargement
Epiphyseal closure
Secondary sexual characteristics
Growth and development of vagina, uterus and fallopian tube
Molding of body contours
Growth of axillary and pubic hair
Pigmentation of genital region
Regional pigmentation of nipples and areolae in pregnancy

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13
Q

Effects of estrogen on reproductive tract

A

Development of vaginal mucosa and lubrication
Increase in amount and water content of cervical mucus
Uterine contractions
Proliferation and differentiation of fallopian tube
Increases tubal muscular contractility

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13
Q

Effect of estrogen on bones

A

Increase bone mass

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14
Q

Effect of estrogen on lipids

A

Elevate serum triglycerides
Reduce total serum cholesterol
Increase HDL
Reduce LDL

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14
Q

Effect of estrogen on glucose

A

Slightly reduces fasting plasma glucose and insulin

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14
Q

Effect of estrogen on bile

A

Increase cholesterol secretion
Decrease bile acid secretion

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15
Q

Effect of estrogen on serum proteins

A

Increase plasma levels of:
Cortisol-binding globulin
Thyroxine-binding globulin
Sex hormone-binding globulin (SHBG)

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16
Q

Effect of estrogen on coagulation

A

Increase in coagulation factors II, VII, IX, X, and XII,
Decrease the anticoagulation factors protein C, protein S, and antithrombin III

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17
Q

Therapeutic estrogens

A

Estradiol
Ethinyl-estradiol
Estrone

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18
Q

Therapeutic indications of estrogens

A

Primary Hypogonadism
Postmenopausal Hormonal Therapy
Oral Contraceptives
Suppress ovulation in patients with intractable dysmenorrhea or hirsutism
Fertility treatments

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19
Q

Formulations containing estradiol

A

Patch- estraderm, estrogel
Depot inj.- Depo Estradiol
Vaginal cream- Estring

19
Q

Side effects of therapeutic estrogens

A

Nausea
Fluid retention
Breakthrough bleeding
Breast tenderness
Thrombolytic complications
Breast cancer
Ovarian cancer
Hypertension

20
Q

Drug interactions of therapeutic estrogens

A

Reduce efficacy of oral anticoagulants and hypoglycemic agents
Increase adverse effects of TCA
Increase effects of oxytocin on uterus
St. John’s wort reduces their efficacy

20
Q

Contraindications to therapeutic estrogens

A

Pregnancy
Incomplete bone growth
Undiagnosed genital bleeding
Stroke
Thromboembolic disease
Heart disease
Family history of breast or uterine cancer

21
Q

Addition of progestins to estrogen for Hormone Replacement Therapy (HRT) is now used to limit ……………

A

endometrial hyperplasia

21
Q

Oral HRT formulations

A

PREMPRO (PREMARIN plus MPA) as fixed daily dose

PREMPHASE (PREMARIN for 28 days and MPA for days 14-28)

FEM HRT (estradiol plus norethindrone acetate)

ORTH PREFEST (estradiol plus norgestimate)

21
Q

Benefits of vaginal creams and rings over oral HRT formulations

A

Reduces vaginal dryness Yeast infections
Urinary tract infections

22
Q

Tamoxifen MOA

A

Estrogen antagonist in breast
Estrogen agonist in endometrium and bones

22
Q

Raloxifene MOA

A

Estrogen agonist in bones
Estrogen antagonist in breasts and endometrium

22
Q

Examples pf selective estrogen receptor modulators

A

Tamoxifen
Raloxifene

23
Q

Examples of antiestrogens

A

Clomiphene
Fulvestrant

23
Q

Aromatase inhibitors

A

Steroidal: Exemestane and Formestane

Nonsteroidal: Anastrozole and Letrozole

23
Q

Clomiphene MOA

A

Weak agonist and strong antagonist estrogen receptors
Oppose the negative feedback effects of endogenous estrogen.
Increase amplitude of the LH and FSH pulses

23
Q

MOA of fulvestrant

A

Pure estrogen antagonist

24
Q

Source of progestogens

A

Corpus luteum during menstrual cycle and 1st tmonth of pregnancy
Placenta and fetal adrenal glands from 2nd or 3rd month of pregnancy

24
Q

Natural progesterone preparations

A

Micronized natural progesterone (PROMETRIUM)
Vaginal gel (CRINONE)
Slow-release IUD (PROGESTASERT)

24
Q

Metabolic effects of progestins

A

Increase basal insulin levels
Long term use decreases glucose tolerance
Enhance fat deposition
Increase LDL

24
Q

Therapeutic uses of progestins

A

Oral contraceptives
HRT to limit estrogen’s effects on the endometrium
Uterine Bleeding disorders
Premature labor
Stimulate Appetite in AIDS or cancer patients

24
Q

What is a selective progestin

A

A selective progestin has progestational effects at low concentrations and androgenic effects at high concentrations

25
Q

Two main classification of progestins

A

17-a-hydroxy-progesterone derivatives

19-nor testosterone derivatives

25
Q

Selectivity index of progestins

A

The ratio of desired agonistic progestational binding to undesired secondary agonistic androgenic bind-ing

25
Q

Second generation progestins

A

Gonanes from testosterone:
Levonorgestrel
Norgestrel

25
Q

Fist generation progestins

A

Estranes from testosterone:
Norethindrone/ Norethisterone
Norethynodrel
Lynestrenol
Ethynodiol diacetate

Pregnanes from progesterone
Medroxyprogesterone acetate
Megestrol
Chlormadinone
Cyproterone acetate

26
Q

How many generations of progestins are there

A

Four

26
Q

Third generation progestins

A

Gonanes from levonorgestrel:
Desogestrel
Gestodene
Norgestimate
Etonorgestrel

26
Q

Fourth generation progestins

A

Non ethylated estranes:
Dienogest
Drospirenone

Pregnanes from 19-nor progesterone:
Nestorone
Nomegestrel
Trimegestone
Promegestone

26
Q

Antiandrogenic progestins

A

Cyprotenone acetate
Chlormadinone acetate
Dienogest
Drospirenone

26
Q

Androgenic activity of progestins

A

1st gen > 2nd gen > 3rd gen > 4th gen

26
Q

API of nestorone

A

Segesterone

26
Q

Andogenic side effects of progestins

A

Increase LDL
Hyperglycemia
Oily skin
Acne
Hirsutism
Android obesity
Androgenic alopecia

26
Q

Benefits of newer progestins

A

Reduced androgenic side effects
More potent progestational effects

27
Q

Examples of progesterone antagonists

A

Mifepristone

28
Q

Danazol MOA

A

weak progestational, androgenic and glucocorticoid activities

MATERNAL HEALTH (25 decks)

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