Abstract
This chapter provides details of studies that describe drug interactions in which antimalarial drugs affect the pharmacokinetics of various co-administered antimalarial drugs. These antimalarials include amodiaquine, artemether, artemisinin, artesunate, atovaquone, chloroquine, dapsone, mefloquine, primaquine, proguanil, pyrimethamine, quinidine, quinine, sulfadoxine/pyrimethamine, and tafenoquine.
Keywords
- Pharmacokinetic Parameter
- Single Oral Dose
- Falciparum Malaria
- Negative Finding
- Pharmacokinetic Interaction
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
This is a preview of subscription content, log in via an institution.
Buying options
Tax calculation will be finalised at checkout
Purchases are for personal use only
Learn about institutional subscriptionsReferences
Adedoyin A, Frye RF, Mauro K et al (1998) Chloroquine modulation of specific metabolizing enzymes activities: investigation with selective five drug cocktail. Br J Clin Pharmacol 46(3):215–219
Ahmad RA, Rogers HJ (1980) Pharmacokinetics and protein binding interactions of dapsone and pyrimethamine. Br J Clin Pharmacol 10(5):519–524
Alin MH, Ashton M, Kihamia CM et al (1996) Clinical efficacy and pharmacokinetics of artemisinin monotherapy and in combination with mefloquine in patients with falciparum malaria. Br J Clin Pharmacol 41(6):587–592
Bapiro TE, Egnell AC, Hasler JA et al (2001) Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos 29(1):30–35
Baune B, Flinois JP, Furlan V et al (1999) Halofantrine metabolism in microsomes in man: major role of CYP 3A4 and CYP 3A5. J Pharm Pharmacol 51(4):419–426
Birkett DJ, Rees D, Andersson T et al (1994) In vitro proguanil activation to cycloguanil by human liver microsomes is mediated by CYP3A isoforms as well as by S-mephenytoin hydroxylase. Br J Clin Pharmacol 37(5):413–420
Coller JK, Somogyi AA, Bochner F (1999) Comparison of (S)-mephenytoin and proguanil oxidation in vitro: contribution of several CYP isoforms. Br J Clin Pharmacol 48(2):158–167
Davis TM, England M, Dunlop AM et al (2007) Assessment of the effect of mefloquine on artesunate pharmacokinetics in healthy male volunteers. Antimicrob Agents Chemother 51(3):1099–1101
Edstein MD, Looareesuwan S, Viravan C et al (1996) Pharmacokinetics of proguanil in malaria patients treated with proguanil plus atovaquone. Southeast Asian J Trop Med Public Health 27(2):216–220
Edwards G, McGrath CS, Ward SA et al (1993) Interactions among primaquine, malaria infection and other antimalarials in Thai subjects. Br J Clin Pharmacol 35(2):193–198
Fontaine F, de Sousa G, Burcham PC et al (2000) Role of cytochrome P450 3A in the metabolism of mefloquine in human and animal hepatocytes. Life Sci 66(22):2193–2212
Funck-Brentano C, Becquemont L, Lenevu A et al (1997) Inhibition by omeprazole of proguanil metabolism: mechanism of the interaction in vitro and prediction of in vivo results from the in vitro experiments. J Pharmacol Exp Ther 280(2):730–738
German PI, Aweeka FT (2008) Clinical pharmacology of artemisinin-based combination therapies. Clin Pharmacokinet 47(2):91–102
Gillotin C, Mamet JP, Veronese L (1999) Lack of a pharmacokinetic interaction between atovaquone and proguanil. Eur J Clin Pharmacol 55(4):311–315
Ilett KF, Ethell BT, Maggs JL et al (2002) Glucuronidation of dihydroartemisinin in vivo and by human liver microsomes and expressed UDP-glucuronosyltransferases. Drug Metab Dispos 30(9):1005–1012
Karbwang J, Bunnag D, Breckenridge AM et al (1987) The pharmacokinetics of mefloquine when given alone or in combination with sulphadoxine and pyrimethamine in Thai male and female subjects. Eur J Clin Pharmacol 32(2):173–177
Karbwang J, Back DJ, Bunnag D et al (1990) Pharmacokinetics of mefloquine in combination with sulfadoxine-pyrimethamine and primaquine in male Thai patients with falciparum malaria. Bull World Health Organ 68(5):633–638
Karbwang J, Na-Bangchang K, Thanavibul A et al (1992) Pharmacokinetics of mefloquine in the presence of primaquine. Eur J Clin Pharmacol 42(5):559–560
Karbwang J, Na-Bangchang K, Thanavibul A et al (1994) Pharmacokinetics of mefloquine alone or in combination with artesunate. Bull World Health Organ 72(1):83–87
Kim KA, Park JY, Lee JS et al (2003) Cytochrome P450 2C8 and CYP3A4/5 are involved in chloroquine metabolism in human liver microsomes. Arch Pharm Res 26(8):631–637
Lefevre G, Bindschedler M, Ezzet F, Schaeffer N, Meyer I, Thomsen MS (2000) Pharmacokinetic interaction trial between co-artemether and mefloquine. Eur J Pharm Sci 10(2):141–151, PMID: 10727880
Lefevre G, Carpenter P, Souppart C et al (2002) Interaction trial between artemether-lumefantrine (Riamet) and quinine in healthy subjects. J Clin Pharmacol 42(10):1147–1158
Li XQ, Bjorkman A, Andersson TB et al (2002) Amodiaquine clearance and its metabolism to N-desethyamodiaquine is mediated by CYP2C8: a new high affinity and turnover enzyme-specific probe substrate. J Pharmacol Exp Ther 300:399–407
Li XQ, Bjorkman A, Andersson TB et al (2003) Identification of human cytochrome P(450)s that metabolise anti-parasitic drugs and predictions of in vivo drug hepatic clearance from in vitro data. Eur J Clin Pharmacol 59:429–442
Miller AK, Harrell E, Ye L et al (2013) Pharmacokinetic interactions and safety evaluations of coadministered tafenoquine and chloroquine in healthy subjects. Br J Clin Pharmacol 76(6):858–867
Na-Bangchang K, Karbwang J, Molunto P et al (1995) Pharmacokinetics of mefloquine, when given alone and in combination with artemether, in patients with uncomplicated falciparum malaria. Fundam Clin Pharmacol 9(6):576–582
Na-Bangchang K, Tan-ariya P, Thanavibul A et al (1999) Pharmacokinetic and pharmacodynamic interactions of mefloquine and quinine. Int J Clin Pharmacol Res 19(3):73–82
Na-Bangchang K, Karbwang J, Ubalee R et al (2000) Absence of significant pharmacokinetic and pharmacodynamic interactions between artemether and quinoline antimalarials. Eur J Drug Metab Pharmacokinet 25:171–178
Obua C, Ntale M, Lundblad MS et al (2006) Pharmacokinetic interactions between chloroquine, sulfadoxine and pyrimethamine and their bioequivalence in a generic fixed-dose combination in healthy volunteers in Uganda. Afr Health Sci 6(2):86–92
Omoruyi SI, Onyeji CO, Daniyan MO (2007) Effects of prior administration of amodiaquine on the disposition of halofantrine in healthy volunteers. Ther Drug Monit 29(2):203–206
Orrell C, Little F, Smith P et al (2008) Pharmacokinetics and tolerability of artesunate and amodiaquine alone and in combination in healthy volunteers. Eur J Clin Pharmacol 64(7):683–690
Projean D, Baune B, Farinotti R et al (2003) In vitro metabolism of chloroquine: identification of CYP2C8, CYP3A4, and CYP2D6 as the main isoforms catalyzing N-desethylchloroquine formation. Drug Metab Dispos 31(6):748–754
Tan-ariya P, Na-Bangchang K, Ubalee R et al (1998) Pharmacokinetic interactions of artemether and pyrimethamine in healthy male Thais. Southeast Asian J Trop Med Public Health 29(1):18–23
van Agtmael MA, Van Der Graaf CA, Dien TK et al (1998) The contribution of the enzymes CYP2D6 and CYP2C19 in the demethylation of artemether in healthy subjects. Eur J Drug Metab Pharmacokinet 23(3):429–436
van Agtmael MA, Cheng-Qi S, Qing JX et al (1999) Multiple dose pharmacokinetics of artemether in Chinese patients with uncomplicated falciparum malaria. Int J Antimicrob Agents 12(2):151–158
van Vugt M, Edstein MD, Proux S et al (1999) Absence of an interaction between artesunate and atovaquone–proguanil. Eur J Clin Pharmacol 55(6):469–474
Zhang SQ, Hai TN, Ilett KF et al (2001) Multiple dose study of interactions between artesunate and artemisinin in healthy volunteers. Br J Clin Pharmacol 52(4):377–385
Author information
Authors and Affiliations
Rights and permissions
Copyright information
© 2015 Springer International Publishing Switzerland
About this chapter
Cite this chapter
Kiang, T.K.L., Wilby, K.J., Ensom, M.H.H. (2015). Effects of Antimalarials on the Pharmacokinetics of Co-Administered Antimalarials. In: Clinical Pharmacokinetic and Pharmacodynamic Drug Interactions Associated with Antimalarials. Adis, Cham. https://doi.org/10.1007/978-3-319-10527-7_6
Download citation
DOI: https://doi.org/10.1007/978-3-319-10527-7_6
Published:
Publisher Name: Adis, Cham
Print ISBN: 978-3-319-10526-0
Online ISBN: 978-3-319-10527-7
eBook Packages: MedicineMedicine (R0)