clomiphene

Q. 15:-CONTRAINDICATIONS of  Clomiphene citrate

1)Hypersensitivity 2) a known hypersensitivity or allergy to clomiphene citrate or to any of its ingredients. 3)

3)Pregnancy .  But point is if she has consumes CC unknowingly will it cause harm ? Ans: research has shown  that 4.5 mg/kg/day for various periods during pregnancy did not have any abnormal offspring. 4) hepatic diseases :-

Clomiphene citrate therapy is contraindicated in patients with liver disease or a history of

liver dysfunction 6)Abnormal Uterine Bleeding. Clomiphene citrate is contraindicated in patients with abnormal uterine bleeding of undetermined origin

7) Ovarian Cysts. CC is contraindicated in patients with ovarian cysts or enlargement not due to polycystic ovarian syndrome .

8) CC is contraindicated in patients with uncontrolled thyroid or adrenal dysfunction

or in the presence of an organic intracranial lesion such as pituitary tumor

q 12: What near life threartening compl may occur ?? Visual Symptoms

Patients should be advised that blurring or other visual symptoms such as spots or flashes

(scintillating  scotomata) may occasionally occur during therapy with CC. These visual

symptoms increase in incidence with increasing total dose or therapy duration and generally

disappear within a few days or weeks after CC is discontinued. Patients should be warned

that these visual symptoms may render such activities as driving a car or operating machinery

more hazardous than usual, particularly under conditions of variable lighting.

These visual symptoms appear to be due to intensification and prolongation of afterimages.

Symptoms often first appear or are accentuated with exposure to a brightly lit environment.

While measured visual acuity usually has not been affected, a study patient taking 200 mg CC

daily developed visual blurring on the 7th day of treatment, which progressed to

severe diminution of visual acuity by the 10th day. No other abnormality was found, and the

visual acuity returned to normal on the 3rd day after treatment was stopped.

Ophthalmologic ally definable scotomata and retinal cell function (electroretinographic) changes

have also been reported. A patient treated during clinical studies developed phosphates and

scotomata during prolonged CC administration, which disappeared by the 32nd day after

stopping therapy. Post marketing surveillance of adverse events has also revealed other visual signs and symptoms during CC While the etiology of these visual symptoms is not yet understood, patients with any visual symptoms should discontinue treatment and have a complete ophthalmological evaluation

carried out promptly.

Ovarian Hyperstimulation Syndrome  by Clomiphen Citrate.

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Part II ,      

1)What it is? Pharmacokinetics

It is a SERM, Blocks Hypothalamus Clomiphene (Nagori):- Zuclomiphene (cis form) is only 38% in ordinary clomiphene. but zu-CLOM(TRANS FORM 0 IS  62% AND VIRTUALLY .

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 stereoisomer’s. CLOMID (clomiphene citrate tablets USP) is an orally administered, nonsteroidal, ovulatory stimulant designated chemically as 2-[p-(2-chloro-1,2-diphenylvinyl)phenoxy] triethylamine Citrate (1:1). It has the molecular formula of C26H28ClNO • C6H8O7 and a molecular weight of  598.09. It is represented structurally as: .

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. a 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 CC therapy.