Women's Health Pharmacology

What are some steroid receptors?

Estrogen receptor, androgen receptor, progesterone receptor

What steroid receptors dimerise before translocating to the nucleus?

Estrogen and androgen receptors

What from the receptors of steroids does the nucleus recognise?

Response elements e.g., estrogen response element, ARE, PRE that regulate gene transcription

How do steroids act on the cell?

Binds to the cell using binding protein, binds to corresponding receptor e.g., estrogen receptor which translocates to the nucleus and response elements are acted upon

How does estrogen act as a signalling molecule?

Interacts with specific target cells e.g., in bone, breast and uterus tissue, as well as brain, heart, liver

How is ER modulation used in contraception?

Used to treat peri/post menopause problems

What other disease state is ER modulation used for?

Treating/preventing breast cancer

How many types of estrogen receptor are there?

2 - alpha and beta

How are estrogen receptors characterised?

Homo or heterodimer e.g., 1a1b, 2a or 2b

How does estrogen have a higher affinity for the estrogen response elements?

Dimerisation

What are estrogen-receptor agonists?

Natural and synthetic estrogens used for HRT and contraception

What are SERMs?

Specific estrogen receptor modulator - different selectivity for different tissues

What is an example of a SERM?

Tamoxifen

Where does tamoxifen act as an agonist?

Bone and uterus

Where does tamoxifen work as an antagonist?

Breast

What is tamoxifen used to treat?

Breast cancer

What do progestins do?

Interact with PR to mimic the stimulatory affects of progesterone

What is the physiological target of progestins?

Reproductive tract - decrease estrogen-driven endometrial proliferation, establish and maintain pregnancy

What are the common uses of progestins?

Oral contraceptives, HRT to limit estrogens effects on endometrium, uterine bleeding disorders, premature labour to decrease uterine contractions

What is mifepristone?

PR antagonist used to terminate pregnancy

What is mifepristone used alongside?

Prostaglandins to increase uterine contractions and induce labour after fetal death

What do all oral contraceptives rely on?

Role of sex-steroids in normal regulation of female reproductive cycle

Got to structure of ovary slide 12