Abstract
This chapter provides details of studies that describe drug interactions in which antimalarial drugs affect the pharmacokinetics of various co-administered (non-antimalarial) drugs. These antimalarials include amodiaquine, artemether, artemisinin, artesunate, atovaquone, chloroquine, mefloquine, proguanil, and quinine.
Keywords
- Pharmacokinetic Parameter
- Single Oral Dose
- Pharmacokinetic Interaction
- Healthy Male Volunteer
- Open Label
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.
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Adedoyin A, Frye RF, Mauro K et al (1998a) Chloroquine modulation of specific metabolizing enzymes activities: investigation with selective five drug cocktail. Br J Clin Pharmacol 46(3):215–219
Adedoyin A, Stiff DD, Smith DC et al (1998b) All-trans-retinoic acid modulation of drug-metabolizing enzyme activities: investigation with selective metabolic drug probes. Cancer Chemother Pharmacol 41:133–139
Ali HM (1985) Reduced ampicillin bioavailability following oral coadministration with chloroquine. J Antimicrob Chemother 15(6):781–784
Amabeoku GJ, Chikuni O, Akino C et al (1993) Pharmacokinetic interaction of single doses of quinine and carbamazepine, phenobarbitone and phenytoin in healthy volunteers. East Afr Med J 70(2):90–93
Asimus S, Elsherbiny DA, Hai TN et al (2007) Artemisinin antimalarials moderately affect cytochrome P450 enzyme activity in healthy subjects. Fundam Clin Pharmacol 21(3):307–316
Asimus S, Hai TN, Van Huong N et al (2008) Artemisinin and CYP2A6 activity in healthy subjects. Eur J Clin Pharmacol 64(3):283–292
Babalola CP, Iwheye GB, Olaniyi AA et al (2002) Effect of proguanil interaction on bioavailability of cloxacillin. J Clin Pharm Ther 27(6):461–464
Back DJ, Purba HS, Park BK et al (1983) Effect of chloroquine and primaquine on antipyrine metabolism. Br J Clin Pharmacol 16(5):497–502
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
Bapiro TE, Sayi J, Hasler JA et al (2005) Artemisinin and thiabendazole are potent inhibitors of cytochrome P450 1A2 (CYP1A2) activity in humans. Eur J Clin Pharmacol 61(10):755–761
Boni J, Abbas R, Leister C et al (2009) Disposition of desipramine, a sensitive cytochrome P450 2D6 substrate, when coadministered with intravenous temsirolimus. Cancer Chemother Pharmacol 64(2):263–270
Cashman JR, Park SB, Yang ZC et al (1992) Metabolism of nicotine by human liver microsomes: stereoselective formation of trans-nicotine N′-oxide. Chem Res Toxicol 5(5):639–646
Cook JA, Randinitis EJ, Bramson CR et al (2006) Lack of a pharmacokinetic interaction between azithromycin and chloroquine. Am J Trop Med Hyg 74(3):407–412
Davis JD, Dixon R, Khan AZ et al (1996) Atovaquone has no effect on the pharmacokinetics of phenytoin in healthy male volunteers. Br J Clin Pharmacol 42(2):246–248
Doki K, Homma M, Kuga K, Aonuma K, Kohda Y (2009) Effects of CYP2D6 genotypes on age-related change of flecainide metabolism: involvement of CYP1A2-mediated metabolism. Br J Clin Pharmacol 68(1):89–96, PMID: 19660006
Engel G, Hofmann U, Heidemann H et al (1996) Antipyrine as a probe for human oxidative drug metabolism: identification of the cytochrome P450 enzymes catalyzing 4-hydroxyantipyrine, 3-hydroxymethylantipyrine, and norantipyrine formation. Clin Pharmacol Ther 59:613–623
Ereshefsky L, Riesenman C, Lam YW (1995) Antidepressant drug interactions and the cytochrome P450 system. The role of cytochrome P450 2D6. Clin Pharmacokinet 29(Suppl 1):10–18
Falloon J, Sargent S, Piscitelli SC et al (1999) Atovaquone suspension in HIV-infected volunteers: pharmacokinetics, pharmacodynamics, and TMP-SMX interaction study. Pharmacotherapy 19(9):1050–1056
Gu L, Gonzalez FJ, Kalow W et al (1992) Biotransformation of caffeine, paraxanthine, theobromine and theophylline by cDNA-expressed human CYP1A2 and CYP2E1. Pharmacogenetics 2:73–77
Ha HR, Chen J, Krahenbuhl S et al (1996) Biotransformation of caffeine by cDNA-expressed human cytochromes P-450. Eur J Clin Pharmacol 49(4):309–315
Hsu A, Granneman GR, Bertz RJ (1998) Ritonavir. Clinical pharmacokinetics and interactions with other anti-HIV agents. Clin Pharmacokinet 35:275–291
Ilo CE, Ilondu NA, Okwoli N et al (2006) Effect of chloroquine on the bioavailability of ciprofloxacin in humans. Am J Ther 13(5):432–435
Jacobson JM, Davidian M, Rainey PM et al (1996) Pyrimethamine pharmacokinetics in human immunodeficiency virus-positive patients seropositive for Toxoplasma gondii. Antimicrob Agents Chemother 40(6):1360–1365
Karam WG, Goldstein JA, Lasker JM et al (1996) Human CYP2C19 is a major omeprazole 5-hydroxylase, as demonstrated with recombinant cytochrome P450 enzymes. Drug Metab Dispos 24(10):1081–1087
Kerr BM, Thummel KE, Wurden CJ et al (1994) Human liver carbamazepine metabolism. Role of CYP3A4 and CYP2C8 in 10,11-epoxide formation. Biochem Pharmacol 47(11):1969–1979
Khaliq Y, Gallicano K, Tisdale C et al (2001) Pharmacokinetic interaction between mefloquine and ritonavir in healthy volunteers. Br J Clin Pharmacol 51(6):591–600
Kumar GN, Rodrigues AD, Buko AM et al (1996) Cytochrome P450-mediated metabolism of the HIV-1 protease inhibitor ritonavir (ABT-538) in human liver microsomes. J Pharmacol Exp Ther 277(1):423–431
Kusuhara H, Ito S, Kumagai Y et al (2011) Effects of a MATE protein inhibitor, pyrimethamine, on the renal elimination of metformin at oral microdose and at therapeutic dose in healthy subjects. Clin Pharmacol Ther 89(6):837–844
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
Makanjuola RO, Dixon PA, Oforah E (1988) Effects of antimalarial agents on plasma levels of chlorpromazine and its metabolites in schizophrenic patients. Trop Georgr Med 40(1):31–33
Masimirembwa CM, Hasler JA, Johansson I (1995) Inhibitory effects of antiparasitic drugs on cytochrome P450 2D6. Eur J Clin Pharmacol 48(1):35–38
Masimirembwa CM, Gusfafsson LL, Dahl ML et al (1996) Lack of effect of chloroquine on the debrisoquine (CYP2D6 and S-mephenytoin (CYP2C19) hydroxylation phenotypes. Br J Clin Pharmacol 41(4):344–346
Mihara K, Svensson US, Tybring G et al (1999) Stereospecific analysis of omeprazole supports artemisinin as a potent inducer of CYP2C19. Fundam Clin Pharmacol 13(6):671–675
Miller JL, Trepanier LA (2002) Inhibition by atovaquone of CYP2C9-mediated sulphamethoxazole hydroxylamine formation. Eur J Clin Pharmacol 58(1):69–72
Munafo A, Reymond-Michel G, Biollaz J (1990) Altered flecainide disposition in healthy volunteers taking quinine. Eur J Clin Pharmacol 38(3):269–273
Nyunt MM, Lu Y, El-Gasim M et al (2012) Effects of ritonavir-boosted lopinavir on the pharmacokinetics of quinine. Clin Pharmacol Ther 91(5):889–895
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
Onyeji CO, Toriola TA, Oqunbona FA (1993) Lack of pharmacokinetic interaction between chloroquine and imipramine. Ther Drug Monit 15(1):43–46
Pedersen KE, Lysgaard Madsen J, Klitgaard NA et al (1985) Effect of quinine on plasma digoxin concentration and renal digoxin clearance. Acta Med Scand 218(2):229–232
Pelkonen O, Rautio A, Raunio H et al (2000) CYP2A6: a human coumarin 7-hydroxylase. Toxicology 144:139–147
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
Riviere JH, Back DJ, Breckenridge AM (1985) The pharmacokinetics of mefloquine in man: lack of effect of mefloquine on antipyrine metabolism. Br J Clin Pharmacol 20(5):469–474
Simooya OO, Sijumbil G, Lennard MS et al (1998) Halofantrine and chloroquine inhibit CYP2D6 activity in healthy Zambians. Br J Clin Pharmacol 45(3):315–317
Soyinka JO, Onyeji CO, Omoruyi SI et al (2010) Pharmacokinetic interactions between ritonavir and quinine in healthy volunteers following concurrent administration. Br J Clin Pharmacol 69(3):262–270
Steiner E, Dumont E, Spina E et al (1988) Inhibition of desipramine 2-hydroxylation by quinidine and quinine. Clin Pharmacol Ther 43(5):577–581
Svensson US, Ashton M, Trinh NH et al (1998) Artemisinin induces omeprazole metabolism in human beings. Clin Pharmacol Ther 64(2):160–167
Trapnell CB, Klecker RW, Jamis-Dow C et al (1998) Glucuronidation of 3′-azido-3′-deoxythymidine (zidovudine) by human liver microsomes: relevance to clinical pharmacokinetic interactions with atovaquone, fluconazole, methadone, and valproic acid. Antimicrob Agents Chemother 42(7):1592–1596
von Bahr C, Spina E, Birgersson C et al (1985) Inhibition of desmethylimipramine 2-hydroxylation by drugs in human liver microsomes. Biochem Pharmacol 34(14):2501–2505
Wandell M, Powell JR, Hager MD et al (1980) Effect of quinine on digoxin kinetics. Clin Pharmacol Ther 28(4):425–430
Wennerholm A, Nordmark A, Pihlsgard M et al (2006) Amodiaquine, its desethylated metabolite, or both, inhibit the metabolism of debrisoquine (CYP2D6) and losartan (CYP2C9) in vivo. Eur J Clin Pharmacol 62(7):539–546
Yamazaki H, Inoue K, Shaw PM et al (1997) Different contributions of cytochrome P450 2C19 and 3A4 in the oxidation of omeprazole by human liver microsomes: effects of contents of these two forms in individual human samples. J Pharmacol Exp Ther 283(2):434–442
Yoshii K, Kobayashi K, Tsumuji M et al (2000) Identification of human cytochrome P450 isoforms involved in the 7-hydroxylation of chlorpromazine by human liver microsomes. Life Sci 67(2):175–184
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Kiang, T.K.L., Wilby, K.J., Ensom, M.H.H. (2015). Effects of Antimalarials on the Pharmacokinetics of Co-Administered Drugs. In: Clinical Pharmacokinetic and Pharmacodynamic Drug Interactions Associated with Antimalarials. Adis, Cham. https://doi.org/10.1007/978-3-319-10527-7_5
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DOI: https://doi.org/10.1007/978-3-319-10527-7_5
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