Sunday, 17 May 2020

Hot flush how to treat ??


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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