Mefloquine for preventing malaria in non-immune adult travellers

Croft, Ashley M.; Garner, Paul

doi:10.1002/14651858.cd000138.pub2

Cited by 17 publications

(35 citation statements)

References 89 publications

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“…Mefloquine is effective against chloroquine resistant Plasmodium species, however there are some areas in SE Asia with known mefloquine resistance. Of note, mefloquine has been found to have serious neuropsychiatric adverse events, which limit its usefulness in certain populations (Castelli et al, 2010;Croft & Garner, 2008). Mefloquine efficacy has been shown to be greater than 90% in multiple clinical trials , the longest of which was in Peace-Corps volunteers in Africa during the early 1990's.…”

Section: Mefloquinementioning

confidence: 99%

“…Mefloquine efficacy has been shown to be greater than 90% in multiple clinical trials , the longest of which was in Peace-Corps volunteers in Africa during the early 1990's. In addition, a review of mefloquine trials found that it did prevent malaria in chloroquine resistant areas (Croft & Garner, 2000). Although an effective medication, the endemic risk of malaria, current resistance patterns, the drug's side effect profile and the patient's medical and psychiatric history should be carefully considered before prescribing mefloquine (Croft & Garner, 2000).…”

Section: Mefloquinementioning

confidence: 99%

“…In addition, a review of mefloquine trials found that it did prevent malaria in chloroquine resistant areas (Croft & Garner, 2000). Although an effective medication, the endemic risk of malaria, current resistance patterns, the drug's side effect profile and the patient's medical and psychiatric history should be carefully considered before prescribing mefloquine (Croft & Garner, 2000). The mefloquine label lists many side effects, the most common of which are nausea, vomiting, diarrhea, and abdominal pain.…”

Section: Mefloquinementioning

confidence: 99%

See 2 more Smart Citations

Malaria Chemoprophylaxis for the International Traveler, Current Options and Future Possibilities

Parker¹,

Leary²

2012

Current Topics in Tropical Medicine

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Section: Mefloquinementioning

confidence: 99%

Section: Mefloquinementioning

confidence: 99%

Section: Mefloquinementioning

confidence: 99%

See 1 more Smart Citation

Malaria Chemoprophylaxis for the International Traveler, Current Options and Future Possibilities

Parker¹,

Leary²

2012

Current Topics in Tropical Medicine

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“…Mefloquine has been used for the chemoprophylaxis and treatment of malaria [1,2,3,4,5,6,7,8], schistosomes and other helminthes [9]. The use is limited by various side effects [4] including neuropsychiatric disorders [10,11,12,13,14], skin reactions [15] as well as risk of miscarriage and stillbirth [16].…”

Section: Introductionmentioning

confidence: 99%

Stimulation of Suicidal Erythrocyte Death by the Antimalarial Drug Mefloquine

Bissinger

Barking

Alzoubi

et al. 2015

Cell Physiol Biochem

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Background: The antimalarial drug mefloquine has previously been shown to stimulate apoptosis of nucleated cells. Similar to apoptosis, erythrocytes may enter suicidal death or eryptosis, which is characterized by cell shrinkage and phospholipid scrambling of the erythrocyte cell membrane with phosphatidylserine translocation to the erythrocyte surface. Stimulators of eryptosis include oxidative stress, increase of cytosolic Ca²⁺-activity ([Ca²⁺]_i), and ceramide. Methods: Phosphatidylserine abundance at the cell surface was estimated from annexin V binding, cell volume from forward scatter, reactive oxidant species (ROS) from 2′,7′-dichlorodihydrofluorescein diacetate (DCFDA) fluorescence, [Ca²⁺]_i from Fluo3-fluorescence, and ceramide abundance from specific antibody binding. Results: A 48 h treatment of human erythrocytes with mefloquine significantly increased the percentage of annexin-V-binding cells (≥5 µg/ml), significantly decreased forward scatter (≥5 µg/ml), significantly increased ROS abundance (5 µg/ml), significantly increased [Ca²⁺]_i (7.5 µg/ml) and significantly increased ceramide abundance (10 µg/ml). The up-regulation of annexin-V-binding following mefloquine treatment was significantly blunted but not abolished by removal of extracellular Ca²⁺. Even in the absence of extracellular Ca²⁺, mefloquine significantly increased annexin-V-binding. Conclusions: Mefloquine treatment leads to erythrocyte shrinkage and erythrocyte membrane scrambling, effects at least partially due to induction of oxidative stress, increase of [Ca²⁺]_i and up-regulation of ceramide abundance.

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“…[1][2][3] This drug is a chiral compound with two asymmetric carbon centers that result in potentially four stereoisomers. The marketed anti-malarial drug mefloquine consist of two of these isomers, the RS and SR pair (referred hereafter as (+) and (−)).…”

Section: Introductionmentioning

confidence: 99%

A Randomized, Double-Blind, Placebo-Controlled Study to Investigate the Safety, Tolerability, and Pharmacokinetics of Single Enantiomer (+)-Mefloquine Compared with Racemic Mefloquine in Healthy Persons

Tansley¹,

Lotharius²,

Priestley³

et al. 2010

The American Society of Tropical Medicine and Hygiene

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Racemic mefloquine is a highly effective antimalarial whose clinical utility has been compromised by its association with neuropsychiatric and gastrointestinal side effects. It is hypothesized that the cause of the side effects may reside in the (−) enantiomer. We sought to compare the safety, tolerability and pharmacokinetic profile of (+)-mefloquine with racemic mefloquine in a randomized, ascending-dose, double-blind, active and placebo-controlled, parallel cohort study in healthy male and female adult volunteers. Although differing in its manifestations, both study drugs displayed a substantially worse tolerability profile compared with placebo. The systemic clearance was slower for (−)-mefloquine than (+)-mefloquine. Thus, (+)-mefloquine has a different safety and tolerability profile compared with racemic mefloquine but its global safety profile is not superior and replacement of the currently used antimalarial drug with (+)-mefloquine is not warranted.

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Mefloquine for preventing malaria in non-immune adult travellers

Abstract: BackgroundMefloquine is commonly prescribed to prevent malaria in travellers, and has replaced other drugs because Plasmodium falciparum is commonly resistant to them. However, mefloquine may be associated with neuropsychiatric harmful effects.

Cited by 17 publications

References 89 publications

Malaria Chemoprophylaxis for the International Traveler, Current Options and Future Possibilities

Malaria Chemoprophylaxis for the International Traveler, Current Options and Future Possibilities

Stimulation of Suicidal Erythrocyte Death by the Antimalarial Drug Mefloquine

A Randomized, Double-Blind, Placebo-Controlled Study to Investigate the Safety, Tolerability, and Pharmacokinetics of Single Enantiomer (+)-Mefloquine Compared with Racemic Mefloquine in Healthy Persons

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