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Pharmacokinetics of Centchroman in Nursing Women and Passage into Breast Milk

  • Clinical Pharmacokinetics
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Summary

The pharmacokinetics of centchroman (ormeloxifene), a nonsteroidal antifertility agent, was determined in 4 nursing mothers in the postpartum period after a single 30mg oral dose of the drug. The concentration-time profile of centchroman in serum and milk were not parallel. The milk/serum (M/S) area under the curve ratio of centchroman was 1.47 ± 0.56. Individual mean M/S concentration ratios of centchroman showed significant interindividual variation (range 0.38 to 1.94). A comparison of pharmacokinetic parameters in the nursing women with those reported previously in nonlactating women showed an insignificant difference; time to maximum concentration occurred later in milk than in maternal serum. The average infant dose of centchroman via breast milk, assuming a weekly milk intake of 1.05 L/kg and 100% absorption, would be 7.43 ± 3.18% per week of the maternal dose.

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References

  1. American Academy of Pediatrics, Committee on Drugs. Transfer of drugs and other chemicals in human milk. Paediatrics 1994; 93: 137–50

    Google Scholar 

  2. Kamboj VP, Kar AB, Ray S, et al. Antifertility activity of 3,4-trans-2,2-dimethyl-3-phenyl-4-(p-(3-pyrrolidinoethoxy)-phenyl)-7-methoxychroman. Indian J Exp Biol 1971; 9: 103–5

    CAS  Google Scholar 

  3. Kamboj VP, Ray S, Dhawan BN. New products: centchroman. Drugs Today 1992; 28: 227–32

    Google Scholar 

  4. Lal J, Asthana OP, Nityanand S, et al. Pharmacokinetics of centchroman in healthy female subjects after oral administration. Contraception 1995; 52: 297–300

    Article  PubMed  CAS  Google Scholar 

  5. Paliwal JK, Gupta RC, Grover PK, et al. High-performance liquid chromatography determination of centchroman in human serum and application to single-dose pharmacokinetics. Pharm Res 1989; 6: 1048–51

    Article  PubMed  CAS  Google Scholar 

  6. Paliwal JK, Grover PK, Asthana OP, et al. Excretion of centchroman in breast milk. Br J Clin Pharmacol 1994; 38: 485–6

    Article  PubMed  CAS  Google Scholar 

  7. Thomas J. Factors controlling drugs in human milk. East Pharm 1992; 416: 89–95

    Google Scholar 

  8. Wilson JT, Brown RD, Hinson JL, et al. Pharmacokinetic pitfalls in the estimation of the breast milk/plasma ratio for drugs. Ann Rev Pharmacol Toxicol 1985; 25: 667–89

    Article  CAS  Google Scholar 

  9. Lal J, Paliwal JK, Grover PK, et al. Simultaneous liquid chromatographic determination of centchroman and its 7-demethylated metabolite in serum and milk. J Chromatogr B 1994; 658: 197–9

    Google Scholar 

  10. Welling PG. In: Pharmacokinetics process & mathematics, ACS Monograph 185, American Chemical Society, Washington, DC, 1986; 229–37

    Google Scholar 

  11. Gibaldi M, Perrier D. Pharmacokinetics. In: Drugs and pharmaceutical sciences. New York: Marcel Dekker Inc, 1982; 409–17

    Google Scholar 

  12. Atkinson HC, Begg EJ, Darlow BA. Drugs in human milk: clinical pharmacokinetic considerations. Clin Pharmacokinet 1988; 14: 217–40

    Article  PubMed  CAS  Google Scholar 

  13. Atkinson HC, Begg EJ, Darlow BA. Guide to safety of drugs in human milk. Clinical pharmacokinetics drug data handbook. Sydney: Adis Press, 1990; 4: 125–64

    Google Scholar 

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Authors and Affiliations

  1. Pharmacokinetics and Metabolism Division, Central Drug Research Institute, Chattar Manzil, Post Box No. 173, Lucknow, 226 001, India

    Ram Chandra Gupta & Jawahar Lal

  2. Clinical and Experimental Medicine Division, Central Drug Research Institute, Lucknow, India

    Swaran Nityanand & Omkar P. Asthana

Authors
  1. Ram Chandra Gupta
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  2. Swaran Nityanand
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  3. Omkar P. Asthana
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  4. Jawahar Lal
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Gupta, R.C., Nityanand, S., Asthana, O.P. et al. Pharmacokinetics of Centchroman in Nursing Women and Passage into Breast Milk. Clin. Drug Invest. 11, 305–309 (1996). https://doi.org/10.2165/00044011-199611050-00007

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  • DOI: https://doi.org/10.2165/00044011-199611050-00007

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