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A Pharmacological Appraisal of Antimalarial Plant Species
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
Mahwahwatse J. Bapela, Precious B. Ramontja, Mcebisi J. Mabuza
Aryl-amino alcohols include quinine, mefloquine, halofantrine and lumefantrine, and their antimalarial activity seem to require the presence of an aromatic portion and an amino alcohol portion (Figure 18.2). Like the 4-aminoquinolines, aryl-amino alcohols are assumed to act primarily on the erythrocyte stage of the malaria parasite by inhibiting the formation of hemozoin (Anderson et al., 2006). 8-Aminoquinolines are derived quinoline molecules with an amine group at the 8-position of quinoline. Primaquine is the only 8-aminoquinoline used in malaria therapy, and studies have shown that it interferes with the parasite’s DNA structure and disrupts its mitochondrial membranes (Miller et al., 2013). It is also the only available drug that can prevent transmission of mature gametocytes, although it can cause intravascular hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency (Sinha et al., 2014). The precise mechanisms of action of the above-mentioned quinoline-based antimalarial drugs are not yet fully understood, and are still under investigation.
Anti-Infective Agents
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: Since the fetuses are considered relatively G6PD deficient, Primaquine should not be used during pregnancy because it is known to generate acute hemolysis in those who are G6PD deficient.
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
Primaquine is used for the radical cure of vivax and ovale malarias, as a community transmission-blocking (gametocytocidal) drug against P. falciparum and, to a very limited extent, for the prophylaxis of falciparum malaria.
Tafenoquine: a toxicity overview
Published in Expert Opinion on Drug Safety, 2021
The neuropsychiatric effects caused by mefloquine, a quinoline-methanol derivative, are well known though they are less commonly associated with 8-aminoquinolines. Data on symptoms most commonly reported (data collection may have been passive or active) with tafenoquine are headache, dizziness (vertigo), and lethargy (weakness, fatigue, somnolence) [38]. Supplement Figure 1–3. Overall, neurological symptoms did not occur more commonly after tafenoquine dosing. Primaquine compared to tafenoquine was associated with a significantly higher risk of any reported neurologic symptom; RR 2.35 (95% CI 1.15 to 4.80). Figure 2(a). Data on neuropsychiatric symptoms such as abnormal dreams, tremors, and effects on coordination, mood, and memory were less commonly collected; detailed psychiatric data were found in five published clinical trials [39–43]. Compared to placebo or chloroquine, primaquine, and mefloquine, tafenoquine was not associated with an increased risk of psychiatric symptoms; RR 0.66 (95% CI 0.27 to 1.60), RR 1.13 (95% CI 0.57 to 2.26), and RR 0.97 (95% CI 0.44 to 2.16), respectively. Figure 2(b). The US FDA Adverse Events Reporting System contains six psychiatric serious adverse events including two suicides associated with the post-market prophylaxis indication [44]. Other neuropsychiatric adverse events (e.g. headache, dizziness, and lethargy/weakness/fatigue) were similar between tafenoquine and placebo or the comparator drug group. Supplement Table 1A-C.
Doses of primaquine administered to children with Plasmodium vivax according to an age-based dose regimen
Published in Pathogens and Global Health, 2020
Michelle Valeria Dias Ferreira Vieira, Tamyris Regina Matos Lopes, Amanda Gabryelle Nunes Cardoso Mello, Luann Wendel Pereira de Sena, Robert J. Commons, José Luiz Fernandes Vieira
Children aged 2–3 years received the lowest mg/kg total doses and had the highest proportion of total doses below 3.5 mg/kg, suggesting that dosing patients in this age range according to their age was inappropriate. These data could explain the high vivax recurrence rate in children < 3 years recorded in the Brazilian Amazon basin [26]. On the other hand, doses as high as 0.80 mg/kg body weight/day was found in the study. High doses of primaquine can increase the rates of dose-dependent adverse reactions such as hemolysis, methemoglobinemia, and abdominal discomfort, which can decrease adherence to the treatment [3,6,21].
Antimalarial drugs for treating and preventing malaria in pregnant and lactating women
Published in Expert Opinion on Drug Safety, 2018
Makoto Saito, Mary Ellen Gilder, Rose McGready, François Nosten
Primaquine is an 8-aminoquinoline used in non-pregnant patients for radical cure of vivax and ovale infections, and as a gametocytocidal agent in falciparum malaria at a single low dose (0.25 mg/kg). Tafenoquine is an 8-aminoquinoline recently approved by FDA for the radical cure of vivax with a single-dose in non-pregnant patients.