8-Aminoquinolines

Carson, Paul E.

doi:10.1007/978-3-642-69254-3_3

Cited by 19 publications

(9 citation statements)

References 70 publications

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“…None had greater than 13% methaemoglobin (up to 25% methaemoglobin is said to be tolerated well and without cyanosis'O). A long-lived primaquine metabolite may be responsible for the mild methaemoglobinaemia that occurs with a standard 14-day regimen.21 However, after 50 weeks of daily primaquine use, the concentration of methaemoglobin in our primaquine group resembled (p=0'23) that reported by Fletcher et a122 (respectively, mean 8-5 g/L, range 2-19 vs mean 7-5 g/L, range [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16] g/L) after a standard 14-day course of 0-25 mg primaquine base per day. We conclude that primaquine provides well-tolerated and effective prophylaxis against P falciparum and P vivax in males who have had little exposure to malaria.…”

Section: Discussionmentioning

confidence: 57%

Randomised placebo-controlled trial of primaquine for prophylaxis of falciparum and vivax malaria

Fryauff¹,

Baird²,

Basri³

et al. 1995

The Lancet

129

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Drug resistance has made malaria prevention difficult and the new agents are too expensive for widespread use. Primaquine, an established drug for treatment, is potentially useful for prevention. Malaria prophylaxis with primaquine was evaluated in Irian Jaya during one year in Javanese men who were not deficient in glucose-6-phosphate dehydrogenase (G-6-PD). 126 volunteers were randomised to receive 0.5 mg/kg primaquine base or placebo daily (double-blinded), or 300 mg chloroquine base weekly (open). The protective efficacy of primaquine relative to placebo was 94.5% (95% confidence interval 57-99) for Plasmodium falciparum and 90.4% (95% CI 58-98) for P vivax. Attack rates for either parasite did not differ significantly between the chloroquine and placebo groups. Incidence density of physical complaints not associated with parasitaemia was low (17-18 complaints/person-year) and was about the same in all groups except for cough, which was increased in the primaquine group. Complete blood counts were normal and no evidence of hepatic or renal dysfunction was found with primaquine. However, at 50 weeks the primaquine group had a mean methaemoglobin of 5.8% (range 1.4-13%), which declined by half within 7 days of ending prophylaxis. When used daily for one year by men with normal G-6-PD activity, primaquine was well tolerated and effective for prevention of malaria.

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Section: Discussionmentioning

confidence: 57%

Randomised placebo-controlled trial of primaquine for prophylaxis of falciparum and vivax malaria

Fryauff¹,

Baird²,

Basri³

et al. 1995

The Lancet

129

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“…To give two examples, sitamaquine ( Fig. 1), an 8-aminoquinoline is well distributed to the liver (29) and is being considered for treatment of VL, whereas the antifungal itraconazole (a triazole) is well distributed to the skin (95) and has been on trial for the treatment of CL. Two other aspects of pharmacokinetics, metabolism and excretion, also require consideration.…”

Section: Pharmacokineticsmentioning

confidence: 99%

Drug Resistance in Leishmaniasis

Sundar¹,

Chakravarty²

2017

Antimicrobial Drug Resistance

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“…The clinical trials post the second worldwar, which was focused upon the 8-aminoquinolines, led to the development of primaquine. Primaquine became available for commercial use during the Korean war (Carson, 1984).It interrupts the disease transmission from host to mosquitoes. It is believed that primaquine can cause an interference with the functioning of ubiquinone in the respiratory chain, thus leading to an impairment of the mitochondrial activity in the parasites.…”

Section: Primaquinementioning

confidence: 99%

Drug Resistance in Malaria-in a nutshell

Bhattacharjee¹,

Shivaprakash²

2016

J App Pharm Sci

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One peek into the history of malaria, shows us that despite many attempts by mankind to counter the development and propagation of malaria, it has always risen back like a 'phoenix from its ashes'. This has been possible by virtue of the singular ability of the malarial parasite to mutate and evade the actions of various anti-malarial drugs. The emergence of drug resistant malarial parasites by virtue of the various molecular mechanisms, has put the authorities under the cosh and forced the scientists to start generating newer and better anti-malarial drugs. In this review, we have dwelt upon the various molecular mechanisms which have allowed the malaria parasite to develop resistance, as it can serve to educate the scientists in their effort to generate newer anti-malarials.

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8-Aminoquinolines

Cited by 19 publications

References 70 publications

Randomised placebo-controlled trial of primaquine for prophylaxis of falciparum and vivax malaria

Randomised placebo-controlled trial of primaquine for prophylaxis of falciparum and vivax malaria

Drug Resistance in Leishmaniasis

Drug Resistance in Malaria-in a nutshell

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