Clinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives.

Reliable and reproducible methods for the measurements of artemisinin and its derivatives in body fluids have proved difficult to develop. The available evidence suggests that all compounds are hydrolysed to a biologically active metabolite, dihydroartemisinin, which is eliminated rapidly. The role...

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Auteur principal: White, N
Format: Conference item
Publié: 1994
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author White, N
author_facet White, N
author_sort White, N
collection OXFORD
description Reliable and reproducible methods for the measurements of artemisinin and its derivatives in body fluids have proved difficult to develop. The available evidence suggests that all compounds are hydrolysed to a biologically active metabolite, dihydroartemisinin, which is eliminated rapidly. The role of other (hydroxylated) metabolites in humans requires further study. The hydrolysis of artesunate is so rapid that it may be considered a pro-drug for dihydroartemisinin. All the artemisinin compounds induce more rapid reduction of parasitaemia than other antimalarial drugs, indicating a direct effect on ring forms. This pharmacodynamic measure can be used in drug comparisons, and allows estimations of the number of parasites removed before sequestration.
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spelling oxford-uuid:6f38ebca-f8f1-433e-a91c-34e425b15f152022-03-26T19:29:18ZClinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives.Conference itemhttp://purl.org/coar/resource_type/c_5794uuid:6f38ebca-f8f1-433e-a91c-34e425b15f15Symplectic Elements at Oxford1994White, NReliable and reproducible methods for the measurements of artemisinin and its derivatives in body fluids have proved difficult to develop. The available evidence suggests that all compounds are hydrolysed to a biologically active metabolite, dihydroartemisinin, which is eliminated rapidly. The role of other (hydroxylated) metabolites in humans requires further study. The hydrolysis of artesunate is so rapid that it may be considered a pro-drug for dihydroartemisinin. All the artemisinin compounds induce more rapid reduction of parasitaemia than other antimalarial drugs, indicating a direct effect on ring forms. This pharmacodynamic measure can be used in drug comparisons, and allows estimations of the number of parasites removed before sequestration.
spellingShingle White, N
Clinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives.
title Clinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives.
title_full Clinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives.
title_fullStr Clinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives.
title_full_unstemmed Clinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives.
title_short Clinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives.
title_sort clinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives
work_keys_str_mv AT whiten clinicalpharmacokineticsandpharmacodynamicsofartemisininandderivatives