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Estrogen
Hormon replacement therapy
Post menoupousal hormon therapy
Indication : menopausal symptoms ( for
examples hot flashesor hot flushes and
vaginal atrophy
Combining with progesteron would reduces
the risk of endometrial carcinoma for woman
who have intact uterus
For women who have undergo histerektomi
estrogen is more recommended than progestin
in beneficial effect of lipid parameter
Stimulated
development of
secondary sex characteristics in
young women ( 11-13 years of age
with primary hipogonadism ,usually
in combination with a progesteron.
Used for women who have
premature menoupouse or
premature ovarian failure
Farmakokinetik
Naturally occuring estrogens: Readily absorbed
Metabolism:
transported in the blood by binding to
Adverse
effects
infarktion
Breast & endometrial cancer ( the
incraesed risk of endometrial cancer can
be offset by including a progesteron
along with estrogen therapy)
Selective
estrogen- receptor
madulators(SERMs)
Agonism
Antagonism
According to the tissue type
Include : tamoxifen, raloxifene(orphan
Mechanism
of action
tamoxifen >< estrogen
Some
Raloxifene
Therapeutic
uses
Pharmacokinetik
The SERMs are rapidly absorbed after oral
administration.
Tamoxifen is extensively metabolized by
cytochrome P 450 enzymes
Raloxifene is rapidly converted to glucuronide
conjugates through first-pass metabolism.
More 95% of raloxifene is bound to plasma protein.
All three agent undergo enterohepatic cycling and
the primary route of excretion is through the bile
into feces.
Advers
event
tamoxifene
raloxifene
clomiphene
Headache , nausea,
vasomotor flushes,
visual disturbance
Menstrual
irregularities,
vaginal bleeding
Deep vein
trombosis
Pulmonary
embolism, retinal
vein trombosis
Ovarian enlargment
Hyperplasia ,
malignancy
endometrium
Drug interaction:
amiodarone,
haloperidol,
Drug interaction :
colestiramin
60% adminitration
of raloxifene
risk of multiple
birds
Progestogens
Mechanism
of action
3.
4.
5.
bleeding
Tretment of dismenore
Management of endometriosis and
infertility
micronized preparation of
progesterone is rapidly absorbed
after oral administration
It has a short half-life in plasma
Almost completely metabolized by
the liver.
Headache
Mifepristone
is a progesterone
antagonist with partial agonist activity
Administration of this drug to females
early in pregnancy usually result in
abortion of the fetus
Mifepristone is often combine with
prostaglandin analog misoprostol
( administered orally or intravginally),
to induce uterine contraction