Literature DB >> 21219551

Effect of artesunate and mefloquine in combination on the Fridericia corrected QT intervals in Plasmodium falciparum infected adults from Thailand.

S Krudsood1, S Looareesuwan, P Wilairatama, W Leowattana, N Tangpukdee, K Chalermrut, S Ramanathan, V Navaratnam, P Olliaro, M Vaillant, J R Kiechel, W R J Taylor.   

Abstract

OBJECTIVE: To ascertain whether mefloquine (MQ) produces electrocardiogram (ECG) changes that could be a risk for Torsades de Pointe (TdP), a potentially malignant, ventricular tachyarrhythmia.
METHODS: We measured the Fridericia corrected QT (QTcF) intervals on 12 lead ECGs on days (D) 0, 3, 7 in Plasmodium falciparum infected adults, treated with oral artesunate (AS) and MQ as a new fixed dose (n = 25) combination or loose tablets (n = 25) over 3 days. Target total doses were 12 mg/kg of AS and 24-25 mg/kg of MQ. MQ concentrations ([MQ]) were measured by HPLC.
RESULTS: All ECG intervals were similar between drug arms and were combined for analysis. Mean QTcF values were 389 (D0), 407 (D3) and 399 (D7) ms (Ps < 0.003 vs. D0); corresponding heart rates and [MQ]s were 83, 67 and 73 beats/minute (Ps ≤ 0.0003 vs. D0) and 0, 3095 and 1721 ng/ml. One male patient (loose arm) had a D3 QTcF 504 ms (D0 406 ms, D7 433 ms). In the modelling of QTcF and JTcF from D0 to D7, significant effects were observed individually for [MQ], temperature and heart rate (HR). The MQ AUC(0-∞) was not a significant factor. Using a manual descending, model building approach to select variables, the HR was the only significant variable (P = 0.001) over time in the model that best explained the changes in the QTcF and JTcF intervals.
CONCLUSIONS: In this small group of patients, slowing heart rates due to malaria resolution best explained the observed increases in the QTcF intervals.
© 2011 Blackwell Publishing Ltd.

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Year:  2011        PMID: 21219551     DOI: 10.1111/j.1365-3156.2010.02714.x

Source DB:  PubMed          Journal:  Trop Med Int Health        ISSN: 1360-2276            Impact factor:   2.622


  10 in total

1.  The story of artesunate-mefloquine (ASMQ), innovative partnerships in drug development: case study.

Authors:  Susan Wells; Graciela Diap; Jean-René Kiechel
Journal:  Malar J       Date:  2013-02-21       Impact factor: 2.979

2.  Fixed dose artesunate amodiaquine - a phase IIb, randomized comparative trial with non-fixed artesunate amodiaquine.

Authors:  Bernhards Ogutu; Elizabeth Juma; Charles Obonyo; Vincent Jullien; Gwenaelle Carn; Michel Vaillant; Walter Robert John Taylor; Jean-René Kiechel
Journal:  Malar J       Date:  2014-12-16       Impact factor: 2.979

Review 3.  Drug-drug interactions and QT prolongation as a commonly assessed cardiac effect - comprehensive overview of clinical trials.

Authors:  Barbara Wiśniowska; Zofia Tylutki; Gabriela Wyszogrodzka; Sebastian Polak
Journal:  BMC Pharmacol Toxicol       Date:  2016-03-10       Impact factor: 2.483

4.  Pooled Multicenter Analysis of Cardiovascular Safety and Population Pharmacokinetic Properties of Piperaquine in African Patients with Uncomplicated Falciparum Malaria.

Authors:  Thanaporn Wattanakul; Bernhards Ogutu; Abdunoor M Kabanywanyi; Kwaku-Poku Asante; Abraham Oduro; Alex Adjei; Ali Sie; Esperanca Sevene; Eusebio Macete; Guillaume Compaore; Innocent Valea; Isaac Osei; Markus Winterberg; Margaret Gyapong; Martin Adjuik; Salim Abdulla; Seth Owusu-Agyei; Nicholas J White; Nicholas P J Day; Halidou Tinto; Rita Baiden; Fred Binka; Joel Tarning
Journal:  Antimicrob Agents Chemother       Date:  2020-06-23       Impact factor: 5.191

5.  The arrhythmogenic cardiotoxicity of the quinoline and structurally related antimalarial drugs: a systematic review.

Authors:  Ilsa L Haeusler; Xin Hui S Chan; Philippe J Guérin; Nicholas J White
Journal:  BMC Med       Date:  2018-11-07       Impact factor: 8.775

6.  Effects of Dihydroartemisinin-Piperaquine Phosphate and Artemether-Lumefantrine on QTc Interval Prolongation.

Authors:  Christian Funck-Brentano; Antonella Bacchieri; Giovanni Valentini; Silvia Pace; Silva Tommasini; Pascal Voiriot; David Ubben; Stephan Duparc; Eric Evene; Mathieu Felices; Marco Corsi
Journal:  Sci Rep       Date:  2019-01-28       Impact factor: 4.379

7.  Sequential Open-Label Study of the Safety, Tolerability, and Pharmacokinetic Interactions between Dihydroartemisinin-Piperaquine and Mefloquine in Healthy Thai Adults.

Authors:  Borimas Hanboonkunupakarn; Rob W van der Pluijm; Richard Hoglund; Sasithon Pukrittayakamee; Markus Winterberg; Mavuto Mukaka; Naomi Waithira; Kesinee Chotivanich; Pratap Singhasivanon; Nicholas J White; Arjen M Dondorp; Joel Tarning; Podjanee Jittamala
Journal:  Antimicrob Agents Chemother       Date:  2019-07-25       Impact factor: 5.191

8.  Mefloquine induces cell death in prostate cancer cells and provides a potential novel treatment strategy in vivo.

Authors:  Kun-Huang Yan; Yung-Wei Lin; Chi-Hao Hsiao; Yu-Ching Wen; Ke-Hsun Lin; Chung-Chi Liu; Mao-Chih Hsieh; Chih-Jung Yao; Ming-DE Yan; Gi-Ming Lai; Shuang-En Chuang; Liang-Ming Lee
Journal:  Oncol Lett       Date:  2013-03-15       Impact factor: 2.967

9.  Electrocardiographic study in Ghanaian children with uncomplicated malaria, treated with artesunate-amodiaquine or artemether-lumefantrine.

Authors:  George O Adjei; Collins Oduro-Boatey; Onike P Rodrigues; Lotte C Hoegberg; Michael Alifrangis; Jorgen A Kurtzhals; Bamenla Q Goka
Journal:  Malar J       Date:  2012-12-17       Impact factor: 2.979

10.  Mefloquine exerts anticancer activity in prostate cancer cells via ROS-mediated modulation of Akt, ERK, JNK and AMPK signaling.

Authors:  Kun-Huang Yan; Chih-Jung Yao; Chi-Hao Hsiao; Ke-Hsun Lin; Yung-Wei Lin; Yu-Ching Wen; Chung-Chi Liu; Ming-DE Yan; Shuang-En Chuang; Gi-Ming Lai; Liang-Ming Lee
Journal:  Oncol Lett       Date:  2013-02-22       Impact factor: 2.967

  10 in total

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