Estrogen preps
Natural- estradiol
Semisynthetic (steroidal)
Synthetic (non steroidal) - DES
Oral but first pass with low bioavailability
Estradiol
Fat soluble so stored in adipose with high bioavailability
Ethinylstradiol orally
From mestranol
Also effective orally but not a steroid
DES
Enhances the coagulability of blood
Estrogen- increasing levels of factors 2 7 9 and 10
Added to estrogen to decrease the risk of endometrial cancer
Progesterone
Main use of progesterone
Oral contraception alone or with estrogen
Dysmenorrhoea and amenorrhoea
Progesterone in amenorrhea
On the 15th to 25th day (take estrogen for 25 days)
Progesterone preps
Natural - Hydroxyprogesterone caproate
Synthetic -
Rapidly metabolised so given as oily IM injection (or pellets or microcrystal implants)
Hydroxyprogesteron caproate
Synthetic progesterone prep
Medroxy progesterone (orally/ IM)- progesterone derivative
Norethindrone and norgestrel (orally/ SC)- nortestosterone derivatives
Weal androgenic effect progesterone
Because nortestosterone derivatives some of them
Anti estrogen (SERM)
Chlomiphene citrate - ovulation inducing
Tamoxifen
Raloxifene
Estrogen synthesis inhibitors
Aromatase inhibitors for extra adrenaline sources of estrogen in breast, liver, fat, skin, muscle :
Steroidal (suicidal) exemestane
Non steroidal (binds reversibly) letrozole
Ovulation inducing agents
Chlomiphene citrate - blocks hypothalamic ER so no usual negative feedback increasing FSH and all the estrogen
Human menopausal gonadotropins
Metforming in PCOs 50 percent
Letrozole (NS aromatase inhibitor)
Must be followed by HCG with LH activity only
Human Menopausal Gonadotropins
Antiprogestrones
Mifepristone
Danazol
Used as postcoital contraceptive with prostaglandin analogue misoprostol either orally or intravaginally
Mifrepristone
Danazol
Weak androgen, anti estrogen, anti progesterone
Used in ttt of endometriosis and fibrocystic breast disease
Danazol
Androgen prep
Natural - androsterone and testosterone
Synthetic- test. propionate and methyl test.
Doesn’t require active form of test.
Muscle
Anti androgens
Finasteride
Flutamide and cyproterone
Spironolactone
Androgens themselves not given orally but…
Their anti androgens (eg Fiansteride) can