Disease relevance of Clomifene

• Developing rats were injected intraperitoneally twice weekly with a combination of three hypocholesterolemic agents: Zuclomiphene (formerly called trans-clomiphene; dosage, 30 mg/kg body weight), Triparanol (30 mg/kg body weight) and AY-9944 (3 mg/kg body weight) [1].

High impact information on Clomifene

• Similarly the relative potency of estrogens to stimulate prolactin synthesis was diethylstilbestrol identical to estradiol greater than ICI 77,949 greater than ICI 47,699 identical to zuclomiphene, consistent with their RBAs [2].
• Effect of hypocholesterolemic agents on central nervous system cholesterol biosynthesis. I. Zuclomiphene [3].
• CONCLUSIONS: Prospective studies of clomiphene citrate should be performed to confirm the hypothesis that the monitoring of plasma zuclomiphene concentrations can significantly accelerate dose individualization and improve the therapeutic outcome with this "orphan" drug [4].
• The appropriateness of starting with these low and intermediate intensity treatments is supported by evidence that CC/IUI increases cycle fecundity two- to three-fold, and FSH/IUI, three- to five-fold over the baseline chance of pregnancy in this patient group [5].
• The combined maximum concentration of enclomiphene and zuclomiphene attained in practice approximates 100 nmol/L and is generally well below levels previously demonstrated to have adverse effects in vitro [6].

Biological context of Clomifene

• Zuclomiphene levels increased rapidly between 14 and 8 days before the surge (53.9 +/- 2.8 ng/ml, mean +/- SE, n = 5) and then decreased gradually but remained elevated throughout the luteal phase (29.0 +/- 1.2 ng/ml, mean +/- SE, n = 33) [7].
• The effectiveness of 'Fertivet' (180 mg. Cisclomiphene Citrate and 120 mg. Transclomiphene citrate mixture) in the induction of estrus and fertility was tested on sixteen anestrous cows [8].
• The incidence of abortion in the 131 pregnancies obtained was 14.68% with Clomiphene; none with Cisclomiphene; 11.11% with Cyclophenil, and 35.10% with Tamoxifen [9].

Anatomical context of Clomifene

• Alteration of developing and adult rat muscle membranes by zuclomiphene and other hypocholesterolemic agents [10].
• Isolated large and small luteal cells derived from intact, enucleated ovine corpora lutea were incubated for 48-120 h with or without 22R-hydroxycholesterol or pregnenolone (2.5 microM) and a range of enclomiphene, zuclomiphene, and/or oestradiol concentrations (3-100 microM), both with and without ovine luteinizing hormone (100 ng/ml) [11].
• A chemical antiestrogen, cis-clomiphene, inhibited FSH-induced ovarian follicle growth [12].
• Tx caused much greater damage to the ovary and uterus than did Clm and Naf [13].

Associations of Clomifene with other chemical compounds

• Five daily injections of 0.1 microgram 17 beta-estradiol (E2) beginning at 30 days of age increased uterine weight and ADL occupancy extent in Tx (2-200 micrograms), Clm and Naf mice [14].
• Ovariectomy performed at 10 days resulted in a reduction in the weight of uteri and the extent of ADL occupancy in Tx, Clm and Naf mice [14].

Analytical, diagnostic and therapeutic context of Clomifene

• Positive electromyography findings were observed in the developing and adult animals receiving 20, 25-diazacholesterol and zuclomiphene [10].

References