FEMALE SEX HORMONES Flashcards by Qúophy Calbert

What are the female sex hormones

Estrogens
Progestogens

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Which enzyme synthesizes estrogens

Aromatase

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The four natural estrogens

Estrone E1
Estradiol E2
Estriol. E3
Estetrol E4

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Estrogens receptors

Estrogen receptor alpha
Estrogen receptor beta

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Potency of estrogens

Estradiol > Estrone > Estriol

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Potency of estrogens

Estradiol > Estrone > Estriol

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Major Source of natural estrogens

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

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Function of 17B- hydroxysteroid dehydrogenase type 1

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

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Function of 17B- hydroxysteroid dehydrogenase type 2

Conversion of estradiol to estrone in the liver

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Precursors for estrogens

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

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Which estrogen is synthesized solely in pregnancy

Estetrol from the fetal liver

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Developmental effects of estrogen in women

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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Effects of estrogen on reproductive tract

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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Effect of estrogen on bones

Increase bone mass

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Effect of estrogen on lipids

Elevate serum triglycerides
Reduce total serum cholesterol
Increase HDL
Reduce LDL

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Effect of estrogen on glucose

Slightly reduces fasting plasma glucose and insulin

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Effect of estrogen on bile

Increase cholesterol secretion
Decrease bile acid secretion

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Effect of estrogen on serum proteins

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

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Effect of estrogen on coagulation

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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Therapeutic estrogens

Estradiol
Ethinyl-estradiol
Estrone

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Therapeutic indications of estrogens

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

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Formulations containing estradiol

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

Side effects of therapeutic estrogens

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

Drug interactions of therapeutic estrogens

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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

Contraindications to therapeutic estrogens

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

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

endometrial hyperplasia

Oral HRT formulations

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)

Benefits of vaginal creams and rings over oral HRT formulations

Reduces vaginal dryness Yeast infections Urinary tract infections

Tamoxifen MOA

Estrogen antagonist in breast Estrogen agonist in endometrium and bones

Raloxifene MOA

Estrogen agonist in bones Estrogen antagonist in breasts and endometrium

Examples pf selective estrogen receptor modulators

Tamoxifen Raloxifene

Examples of antiestrogens

Clomiphene Fulvestrant

Aromatase inhibitors

Steroidal: Exemestane and Formestane Nonsteroidal: Anastrozole and Letrozole

Clomiphene MOA

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

MOA of fulvestrant

Pure estrogen antagonist

Source of progestogens

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

Natural progesterone preparations

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

Metabolic effects of progestins

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

Therapeutic uses of progestins

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

What is a selective progestin

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

Two main classification of progestins

17-a-hydroxy-progesterone derivatives 19-nor testosterone derivatives

Selectivity index of progestins

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

Second generation progestins

Gonanes from testosterone: Levonorgestrel Norgestrel

Fist generation progestins

Estranes from testosterone: Norethindrone/ Norethisterone Norethynodrel Lynestrenol Ethynodiol diacetate Pregnanes from progesterone Medroxyprogesterone acetate Megestrol Chlormadinone Cyproterone acetate

How many generations of progestins are there

Four

Third generation progestins

Gonanes from levonorgestrel: Desogestrel Gestodene Norgestimate Etonorgestrel

Fourth generation progestins

Non ethylated estranes: Dienogest Drospirenone Pregnanes from 19-nor progesterone: Nestorone Nomegestrel Trimegestone Promegestone

Antiandrogenic progestins

Cyprotenone acetate Chlormadinone acetate Dienogest Drospirenone

Androgenic activity of progestins

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

API of nestorone

Segesterone

Andogenic side effects of progestins

Increase LDL Hyperglycemia Oily skin Acne Hirsutism Android obesity Androgenic alopecia

Benefits of newer progestins

Reduced androgenic side effects More potent progestational effects

Examples of progesterone antagonists

Mifepristone

Danazol MOA

weak progestational, androgenic and glucocorticoid activities

FEMALE SEX HORMONES Flashcards

(54 cards)