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Estrogen and Progesterone HRT
E & P for HRT
24
Medical
Undergraduate 4
03/22/2009
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Term

Estrogen Receptors

 Definition

• Nuclear hormone receptors

• ER-alpha and ER-beta; each with a different amt in different cells

• Estrogen receptor assumes different

conformations following binding of an agonist

or an antagonist:

       – Agonist-bound ER recruits co-activators resulting in increased transcription of genes with ERE

      – Antagonist-bound ER recruits co-repressors

resulting in decreased transcription of genes with

ERE
Term
Agonist Binds to Estrogen Receptor
 Definition

1. Agonist penetrates cell wall and enters nucleus

2. Agonist binds to ER bound to HSP

3. ER changes conformation and HSP dissociates from Agonist-ER

4. A-ER dimerizes and it recruits Co-Acivators

5. Co-A binds to A-ER

6. Co-A-A-ER binds to ERE in the promotor region of the gene

7. gene transcription is increased and the prodcution of proteins is increased.

Term
Antagonist binds to Estrogen Receptor
 Definition

1. Antagonist penetrates cell wall and enters nucleus

2. Antagonist binds to ER bound to HSP

3. ER changes conformation and HSP dissociates from Antagt-ER

4. Antag-ER dimerizes and it recruits Co-REPRESSORS

5. Co-R binds to Antag-ER

6. Co-R-Antag-ER binds to ERE in the promotor region of the gene

7. gene transcription is inhibited and the prodcution of proteins is stopped.

Term

Effects of Estrogen

Definition
  • ↓Vasomotor spasm: no hot flashes
  • ↓risk of osteoporosis
  • ↓choles., ↓LDL, ↑HDL
  • edometrial hyperplasia, ↑risk of uterine cancer
  • breast hyperplasia and tenderness, ↑risk of breast cancer
  • ↑ risk of thromboses (MI, Stroke, PE, DVT)
  • Others
    • ↑risk of cancer and genital abnormalities if used during pregnancy
    • worsening of glucose tolerance
    • Na & water retention, edema
    • headache, depression
    • ↓risk of colorectal cancer
Term
Estrogen as Hormone Replacement Therapy
 Definition

• Hormone replacement therapy to treat symptoms

   of menopause

  • Post-menopausal reduced ovarian function leads to lowered estrogen levels which can cause:
    • Vasomotor symptoms (“hot flashes”)
    • Flushed face/neck, sweating; 1-5 minutes
    • Osteoporosis
    • Vaginal atrophy and dryness
Term
Estradiol drugs
 Definition

*Used as HRT to Rx menopause Sx  

  • Estrace
  • Transdermals
    • Climara
    • Vivelle
Term

Ogen

 Definition

 

Estrogen HRT for menopausal Sx

 

estrone or estropiprate
Term

Premarin

Definition

Estrogen HRT Rx menopausal Sx

 

conjugated estrogen from horse urine

Term

Menest

Definition

Estrogen HRT for menopausal Sx

 

esterified estrogen

Term
Cenestin and Enjuvia
 Definition

Estrogen HRT for menopausal Sx

 

synthetic conjugated estrogen

Term
Regular Estrogen
 Definition

*estrogen HRT for Menopausal Sx  

  • Vagifem: vaginal tablets
  • Estring anf Femring: vaginal rings
Term

Selective Estrogen Receptor Modulators

"SERMs"

 

What are they and how to they wrk?

 Definition
  • Tissue-specific effects
    • Agonist in one cell, antagonist in another
  • Tissue-specific response depends on:
    • SERM-bound estrogen receptors assume conformations unique to each SERM
    • Different levels of certain co-activators and corepressors expressed in different cells, yield different effects
Term

SERMs Drug

Definition

– raloxifene (Evista)

– tamoxifen (Nolvadex)

– toremifene (Fareston)
Term
Raloxifene
Definition

Evista®     SERM

  • Rx for prevention of osteoporosis

  • Estrogenic effects on bone

  • Anti-estrogen effects in breast tissue

    • Recruitment of co-repressors by ER-raloxifene complex

  • NO BREAST CANCER

  • Decrease risk of thrombosis

  • No uterine cancer bc no effect on endometrium

  • ↑vasomotor Sx; increase hot flashes

Term
Tamoxifen and Toremifene (not used anymore)
 Definition

Nolvandex®    SERM 

  • Indicated for the treatment and prevention of breast cancer 

  • Anti-estrogen effects in breast tissue
    • Recruitment of co-repressors by ER-tamoxifen complex
  • ↑risk of thrombosis
  • ↑vasomotor Sx; more hot flashes

  • ↑uterine cancer

 
Term

Faslodex®

 

 Definition

Fluvestrant  

Selective Estrogen Receptor DownRegulator

"SERD"  

  • Rx for breast cancer  
  • Binds to ERα in a conformation that increases proteolytic degradation of ER-alpha
  • Results in down-regulation of ERα, decreased transcription of estrogen-responsive genes
  • IM INJ monthly

 
Term

Progestin receptors

 Definition
  • Nuclear hormone receptors
  • Very similar to estrogen receptors
    • a PRE (progesterone response element) found inthe promoter region of certain genes
  • Progestin agonists increase levels of various proteins
Term

Therapeutic uses of progestins

 Definition
  • Contraception
  • Hormone replacement therapy
    • As a supplement to estrogens
    • 7 to 10 days of progestin per month nullifies the increased risk of uterine cancer caused by estrogens alone
      • Progestins reduce estrogen-induced endometrial

    • proliferation
Term

Adverse effects of progestins

 Definition

*Progestin will reduce the benefits of Estrogen for a short while

 

  • Reduced bone density (opposite effect of estrogens)
  • Decreased HDL, increased LDL (opposite effect of estrogens)
  • Reduced glucose tolerance 
  • Nausea, vomiting, depression, fatigue
Term

Provera

 Definition

*Progestin receptor agonists used in HRT

 

Medroxyprogesterone acetate
Term

Aygestin

 Definition

*Progestin receptor agonists used in HRT

 

Norethindrone
Term

Progesterone Vaginal Suppositories

Definition

*Progestin receptor agonists used in HRT

 

– Prometrium capsules

– Crinone vaginal gel
Term
Tablet combination of Estrogen and Progestin
 Definition

Progestin receptor agonists and Estrogen receptor agonist used in HRT

 

• Prempro

• Femhrt
Term
Transdermal Patches of Combo estrogen and progestin
 Definition

Progestin receptor agonists and Estrogen receptor agonist used in HRT

 

*has less ADR than oral bc there is less drug being absorbed and so there is less first pass metabolism that yields the harmful metabolites

 

• Climara Pro

• Combipatch
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