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Chemical Compound Review

ST 155     (6-chloro-17-ethanoyl-10,13- dimethyl-3-oxo...

Synonyms: Verton, C-Quens, SureCN40360, AC1L1EAT, AC1Q6OGT, ...
 
 
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Disease relevance of Chlormadinone

 

High impact information on Chlormadinone

 

Chemical compound and disease context of Chlormadinone

  • Effects on ventilatory responses to progressive isocapnic hypoxia of a synthetic potent progestin, chlormadinone acetate (CMA), were determined in the halothane-anesthetized male rat [5].
  • The slopes of hypoxic ventilatory and occlusion pressure response lines remained unchanged in hypocapnia after CMA or MPA ingestion, but they increased when entidal PCO2 was adjusted to the predrug level [10].
  • Doses of zero, one, 10 and 25 times the expected human dose of megestrol acetate and 25 times the expected human dose of chlormadinone acetate (on a milligram per kilogram body weight basis) are being given daily [11].
  • In one study, combined androgen blockade (CAB) with leuprorelin plus chlormadinone appeared to prolong time to disease progression when compared with leuprorelin monotherapy, but there was no difference in survival between these treatment groups [12].
  • Endometrial morphology and peripheral steroid levels in women with and without intermenstrual bleeding during contraception with the 300 microgram norethisterone (NET) minipill [13].
 

Biological context of Chlormadinone

  • The extent of apoptosis observed in the prostate was significantly higher in the chlormadinone acetate group compared to that of the control and finasteride groups [9].
  • The high effectiveness of the DSG minipill is attributable to an almost constant inhibition of ovulation, as shown by the absence of elevated progesterone circulating levels and inhibition of follicular growth in the vast majority of cycles studied [14].
  • Pharmacokinetics of norethindrone (NET) was evaluated in eleven women belonging to a low socio-economic group and in five womem belonging to the high socio-economic group after the administration of an oral dose of 0.35 mg NET minipill on an empty stomach [15].
  • No significant differences (P greater than 0.05) were found between geometric means of the total area under curve at weekly intervals for FSH, LH and T hormones between the male infants from control group (n=10) when compared with oral minipill or Norplant(R)-2 users [16].
  • Histopathological studies of subcutaneous implantation of chlormadinone acetate (CMA) for preventing estrus in queens [17].
 

Anatomical context of Chlormadinone

  • Some doubts on this conviction are raised by the results of recent studies providing evidence that cyproterone acetate and two structural analogues, chlormadinone acetate and megestrol acetate, are genotoxic in female rats but only for the liver, and in primary human hepatocytes from donors of both genders [18].
  • Ventilation during the breathing of hyperoxic gas was largely unaffected by treatment with CMA when carotid chemoreceptor afferents were kept intact [5].
  • The precise reason for the higher transfer ratio of LNG from breast milk to infant's serum in Minipill users cannot be explained [19].
  • The results suggests a genotoxic and cytotoxic effect of chlormadinone acetate in mouse bone marrow cells [20].
  • Morphometric studies of the endometrium, the fallopian tube and the corpus luteum during contraception with the 300 micrograms norethisterone (NET) minipill [21].
 

Associations of Chlormadinone with other chemical compounds

 

Gene context of Chlormadinone

  • Effects of a new steroidal aromatase inhibitor, TZA-2237, and/or chlormadinone acetate on hormone-induced and spontaneous canine benign prostatic hyperplasia [26].
  • Treatment with 0.5 mg/kg/day of TZP-4238 decreased 5 alpha-reductase activity, DHT content, and nuclear androgen receptor (AR) content in the prostate, and treatment with 0.1 mg/kg/day of TZP-4238 or 2.5 mg/kg/day of CMA also decreased or tended to decrease these parameters [27].
  • Serum prolactin concentrations in women treated with chlormadinone acetate [23].
  • RESULTS: Of 28 patients who had been treated with chlormadinone acetate, 12 (42.9%) revealed 50% or more decline in PSA level following withdrawal of the agent [4].
  • The study revealed a lower LNG percentage transfer from maternal sera to breast milk--11.8 +/- 2, 7 +/- 2 and 8 +/- 1 and relatively higher percentage LNG transfer from breast milk to infant's sera--75 +/- 17, 68 +/- 20 and 32 +/- 3, in LNG-IUD, Norplant (R)-2 and minipill users, respectively [28].
 

Analytical, diagnostic and therapeutic context of Chlormadinone

References

  1. Pure red cell aplasia caused by chlormadinone. Tsuda, H., Kuniyasu, W., Fukuda, K., Shirono, K. Lancet (1994) [Pubmed]
  2. Oral contraceptives containing chlormadinone acetate and cancer incidence at selected sites in the German Democratic Republic--a correlation analysis. Nischan, P., Ebeling, K. Int. J. Cancer (1984) [Pubmed]
  3. Histological evaluation of benign prostatic hyperplasia treated by long-term administration of chlormadinone acetate (CMA). Harada, M., Kinoshita, Y., Moriyama, M., Kondo, I., Nakahashi, M., Kumagai, H., Sasaki, K., Hosaka, M. Prostate (1994) [Pubmed]
  4. Incidence and characteristics of antiandrogen withdrawal syndrome in prostate cancer after treatment with chlormadinone acetate. Akakura, K., Akimoto, S., Furuya, Y., Ito, H. Eur. Urol. (1998) [Pubmed]
  5. Effect of a synthetic progestin on ventilatory response to hypoxia in anesthetized rats. Kimura, H., Mikami, M., Kuriyama, T., Fukuda, Y. J. Appl. Physiol. (1989) [Pubmed]
  6. Interaction of chlormadinone acetate with the ouabain binding site of Na+,K+-ATPase. Wehling, M., Schwartz, A., Whitmer, K., Grupp, G., Grupp, I.L., Wallick, E.T. Mol. Pharmacol. (1981) [Pubmed]
  7. Estrogen and progestin regulation of the progesterone receptor concentration in human endometrium. Kreitmann, B., Bugat, R., Bayard, F. J. Clin. Endocrinol. Metab. (1979) [Pubmed]
  8. Measurement of serum clogestone acetate (AY-11,440) by a radioreceptor assay: a practical approach to the quantitative determination of synthetic progestins. Stern, M.D., Givner, M.L. J. Clin. Endocrinol. Metab. (1975) [Pubmed]
  9. Comparison of histological compositions and apoptosis in canine spontaneous benign prostatic hyperplasia treated with androgen suppressive agents chlormadinone acetate and finasteride. Shibata, Y., Fukabori, Y., Ito, K., Suzuki, K., Yamanaka, H. J. Urol. (2001) [Pubmed]
  10. Comparison of two synthetic progesterones on ventilation in normal males: CMA vs. MPA. Morikawa, T., Tanaka, Y., Maruyama, R., Nishibayashi, Y., Honda, Y. J. Appl. Physiol. (1987) [Pubmed]
  11. Progestogen-related gross and microscopic changes in female Beagles. Nelson, L.W., Kelly, W.A. Vet. Pathol. (1976) [Pubmed]
  12. Global update on defining and treating high-risk localized prostate cancer with leuprorelin: a Japanese perspective - the effect of primary androgen deprivation therapy on stage C prostate cancer. Akaza, H. BJU Int. (2007) [Pubmed]
  13. Endometrial morphology and peripheral steroid levels in women with and without intermenstrual bleeding during contraception with the 300 microgram norethisterone (NET) minipill. Johannisson, E., Landgren, B.M., Diczfalusy, E. Contraception. (1982) [Pubmed]
  14. Seventy-five microgram desogestrel minipill, a new perspective in estrogen-free contraception. Benagiano, G., Primiero, F.M. Ann. N. Y. Acad. Sci. (2003) [Pubmed]
  15. Pharmacokinetics of norethindrone in Indian Women. Prasad, K.V., Rao, B.S., Sivakumar, B., Prema, K. Contraception. (1979) [Pubmed]
  16. Pharmacodynamic effects of levonorgestrel (LNG) administered either orally or subdermally to early postpartum lactating mothers on the urinary levels of follicle stimulating hormone (FSH), luteinizing hormone (LH) and testosterone (T) in their breast-fed male infants. Shikary, Z.K., Betrabet, S.S., Toddywala, W.S., Patel, D.M., Datey, S., Saxena, B.N. Contraception. (1986) [Pubmed]
  17. Histopathological studies of subcutaneous implantation of chlormadinone acetate (CMA) for preventing estrus in queens. Murakoshi, M., Tagawa, M., Ikeda, R. Tokai J. Exp. Clin. Med. (2000) [Pubmed]
  18. Species, sex and inter-individual differences in DNA repair induced by nine sex steroids in primary cultures of rat and human hepatocytes. Martelli, A., Mattioli, F., Angiola, M., Reimann, R., Brambilla, G. Mutat. Res. (2003) [Pubmed]
  19. ICMR Task Force Study on hormonal contraception. Transfer of norethisterone (NET) and levonorgestrel (LNG) from a single tablet into the infant's circulation through the mother's milk. Betrabet, S.S., Shikary, Z.K., Toddywalla, V.S., Toddywalla, S.P., Patel, D., Saxena, B.N. Contraception. (1987) [Pubmed]
  20. Evaluation of genotoxic potential of synthetic progestin chlormadinone acetate. Siddique, Y.H., Afzal, M. Toxicol. Lett. (2004) [Pubmed]
  21. Morphometric studies of the endometrium, the fallopian tube and the corpus luteum during contraception with the 300 micrograms norethisterone (NET) minipill. Kim-Björklund, T., Landgren, B.M., Johannisson, E. Contraception. (1991) [Pubmed]
  22. Endogenous digitalis-like factors: in vitro comparison of biological and immunological activities of peptide and steroid candidates. Hnatowich, M., Labella, F. Eur. J. Pharmacol. (1984) [Pubmed]
  23. Serum prolactin concentrations in women treated with chlormadinone acetate. Beck, P., Malarkey, W.B. Am. J. Obstet. Gynecol. (1976) [Pubmed]
  24. Changes in the binding of oestradiol to uterine oestrogen receptors induced by some progesterone and 19-nor-testosterone derivatives. Di Carlo, F., Gallo, E., Conti, G., Racca, S. J. Endocrinol. (1983) [Pubmed]
  25. Multiple actions of synthetic 'progestins' on the growth of ZR-75-1 human breast cancer cells: an in vitro model for the simultaneous assay of androgen, progestin, estrogen, and glucocorticoid agonistic and antagonistic activities of steroids. Poulin, R., Baker, D., Poirier, D., Labrie, F. Breast Cancer Res. Treat. (1991) [Pubmed]
  26. Effects of a new steroidal aromatase inhibitor, TZA-2237, and/or chlormadinone acetate on hormone-induced and spontaneous canine benign prostatic hyperplasia. Ito, K., Fukabori, Y., Shibata, Y., Suzuki, K., Mieda, M., Gotanda, K., Honma, S., Yamanaka, H. Eur. J. Endocrinol. (2000) [Pubmed]
  27. Effects of the new steroidal antiandrogen TZP-4238 on hormone-induced canine prostatic hyperplasia. Takezawa, Y., Fukabori, Y., Yamanaka, H., Mieda, M., Honma, S., Kushitani, M., Hamataki, N. Prostate (1992) [Pubmed]
  28. ICMR task force study on hormonal contraception. Transfer of levonorgestrel (LNG) administered through different drug delivery systems from the maternal circulation into the newborn infant's circulation via breast milk. Shikary, Z.K., Betrabet, S.S., Patel, Z.M., Patel, S., Joshi, J.V., Toddywala, V.S., Toddywala, S.P., Patel, D.M., Jhaveri, K., Saxena, B.N. Contraception. (1987) [Pubmed]
  29. Effect of antiandrogen treatment on chemical hepatocarcinogenesis in rats. Matsuura, B., Taniguchi, Y., Ohta, Y. J. Hepatol. (1994) [Pubmed]
  30. Combined oral contraceptives containing chlormadinone acetate and breast cancer: results of a case-control study. Ebeling, K., Ray, R., Nischan, P., Thomas, D.B., Kunde, D., Stalsberg, H. Br. J. Cancer (1991) [Pubmed]
  31. Development of a new sensitive and specific time-resolved fluoroimmunoassay (TR-FIA) of chlormadinone acetate in the serum of treated menopausal women. Fiet, J., Giton, F., Auzerie, J., Galons, H. Steroids (2002) [Pubmed]
 
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