What
are designer drugs ?? The drug
designers idea was to find out such designers (say in case of exogenous
estrogens) which in vivo will preserve the beneficial effects of
oestrogens but will impede the ill effects of oesrogens. The idea was novel but
till date this motto have not been fully
successful in thr mission till date.
SERM: SERM are structurally diverse compounds which act a
both as a agonists and antagonists in the same woman :- Designer Oestrogens (SERMs ie.
selective oestrgen recpror modulators) :-The SERMs cause agonist effects (stimulant effect) in some tissues
while depresses or suppresses some in other parts of tissues in a same person.
A)
First
SERM: is clomiphene citrates (CC ) B)
Second SERM to come in the market is :-Tamoxifen(preventive measure as barest
cancer) 3) Third SERM:-Raloxifene.(This structure looks like tamoxifen).
B)
How many kinds of oestrogen receptors are there ? 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 specific receptors and either exerts stimulatory action or inhibitory action.
Menopausal Replacement made easy(only
for PGs):- 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,-Estrogen
will be a better choice as either COC or Patch.
C)
Phase II of treatment (HRT):- as prophylaxis as long term health
maintenance. Raloxifene is an important member of this therapy.Additinally high
calcium, Yoga and life style modifications, Invovemenyt with NGOs, will make
you life meaningful if husband cant afford time and most of the family members are well placed
and too busy to talk with you.
Drugs for Hot flushes : Made easy for house officers working at OPD :-My choice of drugs for menopausal hot
flushes are as fllows A) Clonidine(trade
name are Arkamin or catapress B) If not relieved
by 15 days switch over to next agent oestrogens for short period only say 6 months. One can use oestrgen as monotherapy
if hysterctomy was done earlier. Or else Oestrgen and progesterone for about 6 months . Third choice will be costlier
Tibolone.
What is the presumable risk factor with Oestrgen replacement therapy?? Problem
with oestrgen is that about 20% of menopausal
women (a guess estimate) are medically unfit for oetsrogen therapy . Such
medical contraindications are uncontrolled DM, HTN, Chr. Liver disorders etc. I also apprehend that client once satisfied of relief of her hot
flushes like magic, she may not t come back for follow up and may
presumably continue to ingest such prescribed HRT (E 2 alone or Estrogen & Prog) for 2-3 yrs without the knowledge of prescriber concerned. Poor follow up is the chief concern for search
for alternative, less effective but relatively safe agent for”at risk women”
agents.
Tibolone (second drug
of choice in hot flush) may be considered only when the prescriber considers
that the concerned woman is “at risk
woman for VTE” and he also feels
that she may be lost to follow up:-
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