• Register
  • Login

Iranian Journal of Pharmaceutical Sciences

  • Home
  • Journal Info
    • About the Journal
    • Aims and Scope
    • Editorial Team
    • Indexing & Abstracting
    • Privacy Statement
    • Contact us
  • Issues
    • Current
    • Archives
  • New Submissions
  • Author Guidelines
  • Policies & Process
    • Peer Review
    • Publication Ethics
    • Open Access Policy
    • Plagiarism
    • Retraction Policies
    • Archiving
  • Ethical Considration
Advanced Search
  1. Home
  2. Archives
  3. Vol. 1 No. 2 (2005): IJPS_Volume 1_Issue 2
  4. Research/Original Articles

Vol. 1 No. 2 (2005)

April 2005

An Ex-Vivo Study on the Stereoselective Accumulation of Mefloquine Enantiomers in Human Blood Fractions Accumulation of mefloquine in blood

  • Effat Souri
  • Hassan Farsam
  • Hamid Reza Akbarpo

Iranian Journal of Pharmaceutical Sciences, Vol. 1 No. 2 (2005), 1 April 2005 , Page 101-106
https://doi.org/10.22037/ijps.v1.39452 Published: 2005-06-30

  • View Article
  • Download
  • Cite
  • References
  • Statastics
  • Share

Abstract

Mefloquine (MFQ), as a racemic mixture is used for the prophylaxis and treatment of malaria. Stereoselective pharmacodynamic and pharmacokinetic differences have been observed for MFQ. In the present study, the human blood was spiked with racemic MFQ. The concentration of MFQ enantiomers in various blood fractions including packed erythrocyte layer, platelet rich plasma and platelet poor plasma was determined. The results showed that the ratio of (+)-MFQ was about 1.5 time higher than (-)-MFQ in packed erythrocyte layer. Results obtained from the separated erythrocytes spiked with racemic MFQ showed no significant
difference between the enantiomer concentrations. It can be concluded that the stereoselective accumulation of MFQ enantiomers in erythrocytes might be in relation to protein binding or the presence of other blood cells.

Keywords:
  • Mefloquine
  • Enantiomer
  • Stereoselective
  • Blood fractions
  • IJPS_Volume 1_Issue 2_Pages 101-106

How to Cite

Souri, E. ., Farsam, H. ., & Akbarpo, H. R. . (2005). An Ex-Vivo Study on the Stereoselective Accumulation of Mefloquine Enantiomers in Human Blood Fractions: Accumulation of mefloquine in blood. Iranian Journal of Pharmaceutical Sciences, 1(2), 101–106. https://doi.org/10.22037/ijps.v1.39452
  • ACM
  • ACS
  • APA
  • ABNT
  • Chicago
  • Harvard
  • IEEE
  • MLA
  • Turabian
  • Vancouver
  • Endnote/Zotero/Mendeley (RIS)
  • BibTeX

References

[1] Palmer KJ, Holliday SM, Brogden RN. Mefloquine: a review of its antimalarial activity, pharmacokinetic properties and therapeutic efficacy. Drugs 1993; 45: 430-75.
[2] Gimenez F, Farinotti R, Thuillier A, Hazebroucq G, Wainer IW. Determination of the enantiomers of mefloquine in plasma and whole blood using a coupled achiral-chiral HPLC system. J Chromatogr 1990; 529: 339-46.
[3] Martin C, Gimenez F, Bangchang KN, Karbwang J, Wainer IW, Farinotti R. Whole blood concentrations of mefloquine enantiomers in healthy Thai volunteers. Eur J Clin Pharmacol 1994; 47: 85-7.
[4] Gimenez F, Pennie RA, Koren G. Stereoselective pharmacokinetics of mefloquine in healthy Caucasians after multiple doses. J Pharm Sci 1994; 83: 824-7.
[5] Souri E, Farsam H, Jamali F. Apreliminary study of stereoselectivty of mefloquine enantiomers in rat. Acta Med Iranica 1998; 36: 133-7.
[6] Baudry S, Pham YT, Baune B, Vidrequin S, Crevoisier C, Gimenez F, Farinotti R. Stereoselective passage of mefloquine through the blood-brain barrier in the rat. J Pharm Pharmacol 1997; 49: 1086-90.
[7] Karle JM, Olmeda R, Gerena L, Milhous WK. Plasmodium falciparum, role of absolute stereochemistry in the antimalarial activity of synthetic amino alcohol antimalarial agents. Exp Parasitol 1993; 76: 345-51.
[8] Souri E, Nateghpour M, Farsam H, Kaji Z, Hamedi Y, Amanlou M. in vitro activity of mefloquine and its enantiomers against Plasmodium falciparum. Iranian J Pharmacol Res 2002, 1: 17-9.
[9] San George RC, Nagel RL, Fabry ME. On the mechanism for the red cell accumulation of mefloquine, an antimalarial drug. Biochim Biophys Acta 1984; 803: 174-81.
[10] Adovelande J, Boulard Y, Berry JP, Galle P, Slodzian G, Schrevel J. Detection and cartography of the fluorinated antimalarial drug mefloquine in normal and Plasmodium falciparum infected red blood cells by scanning ion microscopy and mass spectrometry. Biol Cell 1994; 81: 185-92.
[11] Pham YT, Regina A, Farinotti R, Couraud P, Wainer IW, Roux F, Gimenez F. Interactions of racemic mefloquine and its enantiomers with Pglycoprotein
in an immortalized rat brain capillary endothelial cell line, GPNT. Biochim Biophys Acta 2000; 1524: 212-9.
[12] Bergqvist Y, Doverskog M, Al Kabbani J. HPLC determination of (SR)- and (RS)-enantiomers of mefloquine in plasma and capillary blood sampled on paper after derivatization with (-)-1-(9- fluorenyl) ethyl chloroformate. J Chromatogr B 1994; 652: 73-81.
[13] Brocks DR, Skeith KJ, Johnston C, Emamibafrani J, Davis P, Russell AS, Jamali F. Hematologic disposition of hydroxychloroquine enantiomers. J Clin Pharmacol 1994; 34: 1088-97.
  • Abstract Viewed: 279 times
  • IJPS_Volume 1_Issue 2_Pages 101-106 Downloaded: 166 times

Download Statastics

  • Linkedin
  • Twitter
  • Facebook
  • Google Plus
  • Telegram

Developed By

Open Journal Systems

Information

  • For Readers
  • For Authors
  • For Librarians
  • Home
  • Archives
  • Submissions
  • About the Journal
  • Editorial Team
  • Contact

Creative Commons License
This journal (and its contents) is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.

Print ISSN: 1735-2444

Online ISSN: 2252-0457

Powered by OJSPlus