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Infections
Published in Anne Lee, Sally Inch, David Finnigan, Therapeutics in Pregnancy and Lactation, 2019
Breastfeeding is not contraindicated in mothers taking standard prophylactic doses of chloroquine or proguanil.46,47 Small amounts of mefloquine pass into breast milk and although breastfeeding is not recommended it is unlikely to cause harm.46 Pyrimethamine is safe to use, but enough dapsone may pass into breast milk to cause toxicity; use of Maloprim is therefore not advised while breastfeeding.47,68
Information on level of drugs into breastmilk
Published in Wendy Jones, Breastfeeding and Medication, 2018
Mefloquine has a long elimination half-life; adverse effects may occur or persist up to several weeks after the last dose. The most frequent adverse effects of mefloquine are nausea, diarrhoea, vomiting, abdominal pain, anorexia, headache, dizziness, loss of balance, somnolence and sleep disorders, notably insomnia and abnormal dreams. Neurological or psychiatric disturbances have also been reported and there have been rare reports of suicidal thoughts. Treatment should begin two and a half weeks before entering the endemic area. Pregnancy should be avoided during and for three months after prophylactic use.
Treatment and prevention of malaria
Published in David A Warrell, Herbert M Gilles, Essential Malariology, 2017
David A Warrell, William M Watkins, Peter A Winstanley
Mefloquine is used for the prophylaxis and treatment of uncomplicated multiresistant falciparum malaria. In combination with artesunate, it has proved effective against uncomplicated falciparum malaria in areas, such as the Thai-Burmese border, where there is a high level of resistance to mefloquine alone.
Antimalarial treatment in infants
Published in Expert Opinion on Pharmacotherapy, 2022
Laura C. Kalkman, Thomas Hanscheid, Sanjeev Krishna, Peter G. Kremsner, Martin P. Grobusch
Mefloquine pharmacokinetics is primarily impacted by body weight, justifying weight-based dosing [94]. However, studies including infants over six months revealed a negative correlation between mefloquine concentration and body weight, resulting in higher concentrations of mefloquine in infants and young children. This likely because of decreased mefloquine elimination due to incomplete organ maturation [63,95,96]. Guidi et al. also found increased absorption of mefloquine in younger age groups and speculated this to be the result of breast milk being the more appropriate nutrition to be co-administered with mefloquine as compared to food given to older children [63]. High plasma mefloquine levels may be problematic, as increased mefloquine dosing is associated with risk of vomiting, and vomiting is linked to treatment failure [96–98].
Review of the mechanism underlying mefloquine-induced neurotoxicity
Published in Critical Reviews in Toxicology, 2021
Airton C. Martins, Monica M. B. Paoliello, Anca O. Docea, Abel Santamaria, Alexey A. Tinkov, Anatoly V. Skalny, Michael Aschner
At present, there are no effective antimalarial vaccines. Mefloquine (a 4-quinolinemethanol synthetic quinoline) is commonly prescribed as an antimalarial drug, with long retention in the human body and high efficacy (Tinckel-Painter et al. 2017a), commonly recommended as a prophylactic for malaria endemic areas (CDC 2020). Given the widespread resistance of Plasmodium to chloroquine, the use of mefloquine has grown due to its efficacy; resistance to mefloquine has been observed only in clearly defined areas in Thailand, Northern Cameroon and West Africa, due to cross-resistance with quinine (Schlagenhauf et al. 2010). Several mechanisms have been ascribed to the antimalarial efficacy of mefloquine, such as binding to heme molecules of erythrocyte damaging the parasite vacuoles or generating excess reactive oxygen species in the parasite (Kumar et al. 2020). The chemical structure of mefloquine and several of its analogs is shown in Figure 1.
Fluorinated scaffolds for antimalarial drug discovery
Published in Expert Opinion on Drug Discovery, 2020
Charu Upadhyay, Monika Chaudhary, Ronaldo N. De Oliveira, Aniko Borbas, Prakasha Kempaiah, Poonam S, Brijesh Rathi
Mefloquine 41 is an antimalarial drug that is used to treat mild Pf malaria in the regions where parasites have not developed resistance [65]. A combination of artesunate and mefloquine is now used to treat severe malarial infection to deal with the drug resistance [66]. For the first time, Wipf et al. reported the synthesis of two novel analogues 44 and 45 (Figure 5), pentafluorosulfanyl derivatives of mefloquine [35]. The regioisomers 44 and 45 have improved activity and selectivity against the malaria parasite compared to the parent drug 41 and the trifluoromethylated quinoline methanols 42 and 43.