Clomiphene Citrate.
,
1)What it is? It is a SERM(selective oestrogen receptor Blockers)
,In fact there are two types of oestrogen receptors e,g,., Blocks Hypothalamus
Clomiphene: - Zuclomiphene (cis form) is only 38% in ordinary clomiphene. but zu-clomiphene (trans is 62%.
Q.2. Which isomer to use? En
is more potent and responsible for OI. Besides life time is also short.
It is a raceme mixture of
two stereoisomers. clomiphene citrate tablets is an orally administered, nonsteroidal , ovulatory
stimulant designated chemically as 2-[p-(2-chloro-1,2-diphenylvinyl)peony]
triethylamine Citrate (1:1). It has the molecular formula of C26H28ClNO •
C6H8O7 and a molecular weight of 598.09.
It is represented structurally as: .
Clomiphene citrate(CC) is a mixture of two geometric isomers [cis
(zuclomiphene) and trans
(enclomiphene)]
Containing between 30% and
50% of the cis-isomer.
Each white scored tablet
contains 50 mg clomiphene citrate USP. The tablet also contains the following
inactive ingredients: corn starch, lactose, magnesium stearate, pregelatinized
Cornstarch, and sucrose. at
present in the feces 6 weeks after administration.
Subsequent single-dose studies in normal
volunteers showed that zuclomiphene (cis) has a longer half-life than enclomiphene
(trans). Detectable levels of zuclomiphene persisted for longer than a month in
these subjects. This may be suggestive of stereo-specific enterohepatic
recycling or sequestering of
the zuclomiphene. Thus, it is possible that
some active drug may remain in the body during early pregnancy in women who
conceive in the menstrual cycle during Clomiphene citrate(CC) therapy.
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