Clinical pharmacology and therapeutic potential of artemisinin and its derivatives in the treatment of malaria.

Drugs
P J de Vries, T K Dien

Abstract

Artemisinin and its derivatives are renowned for their potent antimalarial activity. They have found their way into clinical use in many areas where malaria is endemic. The in vitro concentration at which artemisinin can inhibit 50% of the growth of Plasmodium falciparum ranges from 3 to 30 micrograms/L. The fat-soluble derivatives artemether and arteether are approximately twice as active. The water-soluble dihydro-artemisinin and artesunate are 4 to 5 times more active in vitro. Artemisinin is available only for oral and rectal administration. Absorption is incomplete and elimination is fast, with and elimination half-life of 2 to 5 hours. Plasma concentrations after a single 500 mg oral dose most often exceed 200 micrograms/L. Artesunate and artemether can be considered as prodrugs. Biotransformation into the active metabolite dihydro-artemisinin occurs rapidly--almost immediately for artesunate. The reported elimination half-life of artesunate is less than 1 hour, and for artemether the figure is 3 to 11 hours. The pharmacokinetics of dihydro-artemisinin are not yet completely clear. Elimination is probably also rapid, with an elimination half-life of a few hours. Arteether, dissolved in oil for intramuscular administration...Continue Reading

Citations

Feb 26, 2004·Indian Journal of Pediatrics·Tanu Singhal
Feb 3, 2009·Archives of Pharmacal Research·Muhammad Tayyab AnsariVivian Bruce Sunderland
Jun 10, 2011·Archives of Pharmacal Research·Muhammad Tayyab AnsariVivian Bruce Sunderland
Nov 1, 2003·Bioorganic & Medicinal Chemistry Letters·Luigi MessoriFranco Francesco Vincieri
Mar 4, 2014·Materials Science & Engineering. C, Materials for Biological Applications·Pinkee PhukonRaju Khan
Apr 28, 2004·Transactions of the Royal Society of Tropical Medicine and Hygiene·Markus S MuellerLutz Heide
Dec 4, 2001·International Journal for Parasitology·J UtzingerM Tanner
Dec 29, 2000·Transactions of the Royal Society of Tropical Medicine and Hygiene·R BakshiE Alteri
Dec 16, 1998·Transactions of the Royal Society of Tropical Medicine and Hygiene·R KoopmansC J van Boxtel
Feb 19, 2002·British Journal of Clinical Pharmacology·Kenneth F IlettTimothy M E Davis
Jun 26, 2001·British Journal of Clinical Pharmacology·T Q BinhV D Phuong
Oct 30, 1999·Tropical Medicine & International Health : TM & IH·K Na-BangchangJ Karbwang
Jan 13, 2000·Tropical Medicine & International Health : TM & IH·N TingaP J Vries
Sep 11, 1997·The New England Journal of Medicine·T M DavisJ S McCarthy
Aug 30, 2005·International Journal of Toxicology·Qigui LiPeter J Weina
Mar 30, 2011·The Journal of Alternative and Complementary Medicine : Research on Paradigm, Practice, and Policy·Maurizio BonatiRoberto Fanelli
Feb 27, 2003·Journal of Cardiovascular Pharmacology·Michelle P McIntoshSusan J Coker
Jul 28, 2006·Antimicrobial Agents and Chemotherapy·Timothy M E DavisP Hugh R Barrett
Jul 7, 2011·Antimicrobial Agents and Chemotherapy·Nguyen Trong ChinhMichael D Edstein
Feb 15, 2012·Antimicrobial Agents and Chemotherapy·Kevin T BattyTimothy M E Davis
Apr 19, 2000·Antimicrobial Agents and Chemotherapy·P J de VriesS H Heisterkamp
Dec 20, 2000·Antimicrobial Agents and Chemotherapy·T M DavisT Q Binh
Dec 26, 2001·Antimicrobial Agents and Chemotherapy·Nehal VyasChristy M Wyandt
Sep 8, 2007·Canadian Journal of Physiology and Pharmacology·Janet I EjioforJoseph A Anuka
Dec 17, 2011·Journal of Biomedicine & Biotechnology·Maria P Crespo-Ortiz, Ming Q Wei
Mar 10, 2011·Malaria Journal·Andrea CoddMichelle L Gatton
Nov 9, 2000·Clinical Pharmacokinetics·V NavaratnamP Olliaro
Jul 4, 2001·Clinical Pharmacokinetics·P T Giao, P J de Vries
Mar 18, 2009·Pharmacogenomics·Rajeev K MehlotraPeter A Zimmerman
Jul 19, 2006·Biomedical Research·Athip NilkaeoSeuptrakool Wisessombat

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