SERM: SERM are structurally diverse compounds which act a
both as a agonists and antagonists in the same woman and such
agents are also called “Designer Oestrogens”:-
Because the SERMs cause agonist effects on oestrogen
receptors in some tissues of women , while
depresses or suppresses some other oestrogen receptors in other parts of
tissues in a same individual .
.
Classification / Evolution of
SERM:- A) First SERM is :CC ( 1982/ 1968)
B) Second SERM:-Tamoxifen
(still used as an effective agent or preventive measure as barest cancer after
surgery –antagonist effect at Breast).
C) Third
SERM:-Raloxifene.(This structure looks more like tamoxifen).
Basics of Designer oestrogens? There
are 3 types of E2 receptors 1) Alpha α homo-dimer2) β beta homodimer 3) hetero-dimer α
& β receptor heterodimers. They by virtue of their structural stereochemical
composition they (designer) affect some spenic receptors and either exerts
stimulatory action or inhibitory action.
The idea of designers was to find out such
designers which when consumed in vivo
will preserve the beneficial effects of oestrogens but will impede the ill
effects of oesrogens.
Limitations of designer oestrogens :--They
have not been fully successful in their mission till date.
Q.7: How we can use such designer oestrogens
in menopausal women / post menopause??
Ans: There are two phases of Ry for menopausal
women. A) Phase I treatment:- it spans from first
few months or years when there are acute menopausal symptoms like hot flashes,
mood changes, sleep disturbance,
vaginal dryness . In such acute
phase estrogen will be a better choice either COC or Patch.
Phase II of treatment (HRT):-As we
know such phase two Tr is aimed at prevention
of some diseases like Osteopenia, Breast Ca . This phase II tr in established menopause
is purely prophylaxis as a measure to achieve long term health maintenance.
Raloxifene is an important member of this therapy.
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