Primaquine

Publication Title: 
Antimicrobial Agents and Chemotherapy

The in vitro effect of the following antimicrobial agents on Toxoplasma gondii tachyzoites were studied: artemisinin ether (arteether), cycloguanil hydrochloride (cycloguanil), mefloquine, primaquine phosphate, and quinine sulfate, as well as the calcium channel blocker verapamil and the calmodulin inhibitor trifluoperazine hydrochloride. Arteether at > or = 0.5 micrograms/ml and cycloguanil at > or = 1.0 micrograms/ml inhibited T. gondii in vitro. Cycloguanil (2.5 micrograms/ml) combined with a noninhibitory concentration of sulfadiazine (25 micrograms/ml) inhibited T.

Author(s): 
Holfels, E.
McAuley, J.
Mack, D.
Milhous, W. K.
McLeod, R.
Publication Title: 
FEBS letters

We recently demonstrated that 2,3,4,5,6-pentahydroxyxanthone (X5) inhibits the in vitro growth of both chloroquine-sensitive and multidrug-resistant strains of P. falciparum. To study the molecular basis of its antimalarial action, we tested X5 and selected hydroxyxanthone analogs as inhibitors of in vitro heme polymerization in a low ionic strength phosphate solution at mildly acidic pH. We found that addition of 1 Eq. of X5 resulted in complete inhibition of polymerization in this system whereas addition of up to 40 Eqs.

Author(s): 
Ignatushchenko, M. V.
Winter, R. W.
Bächinger, H. P.
Hinrichs, D. J.
Riscoe, M. K.
Publication Title: 
Memórias Do Instituto Oswaldo Cruz

An assay was developed measuring the disruption of rosettes between Plasmodium falciparuminfected (trophozoites) and uninfected erythrocytes by the antimalarial drugs quinine, artemisinin mefloquine, primaquine, pyrimethamine, chloroquine and proguanil. At 4 hr incubation rosettes were disrupted by all the drugs in a dose dependent manner. Artemisinin and quinine were the most effective anti-malarials at disrupting rosettes at their therapeutic concentrations with South African RSA 14, 15, 17 and The Gambian FCR-3 P. falciparum strains.

Author(s): 
Goldring, J. D.
Padayachee, T.
Ismail, I.
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

To define the current efficacy of Fansidar (F. Hoffmann-La Roche Ltd., Basel Switzerland) (pyrimethamine and sulfadoxine), primaquine in a high dose, and artesunate for treating acute Plasmodium vivax malaria, we conducted a comparative clinical trial of these 3 drugs in an open-label study. Patients (15-65 years old) were assigned to 1 of 4 treatments regimens in a serial order. Ninety percent of the patients were infected at Thailand-Myanmar border.

Author(s): 
Wilairatana, P.
Silachamroon, U.
Krudsood, S.
Singhasivanon, P.
Treeprasertsuk, S.
Bussaratid, V.
Phumratanaprapin, W.
Srivilirit, S.
Looareesuwan, S.
Publication Title: 
Memórias Do Instituto Oswaldo Cruz

A cell-free system from Plasmodium falciparum able to translate endogenous mRNA was used to determine the effect of artemisinin, chloroquine and primaquine on the protein synthesis mechanism of the parasite. The antimalarial drugs did not inhibit the incorporation of [3H] methionine into parasite proteins even at concentrations higher than the ones found to strongly inhibit the parasite growth. Results clearly indicate that these compounds do not have a direct effect on protein synthesis activity of P. falciparum coded by endogenous mRNA.

Author(s): 
Ferreras, Ana
Triana, Ledia
Sánchez, Erlinda
Herrera, Flor
Publication Title: 
Revista Da Sociedade Brasileira De Medicina Tropical

with the objective of evaluating shortened therapeutic outlines effective in vivax malaria treatment, we accomplished an open, prospective study allocating 234 patients with vivax malaria distributed at random into eight therapeutic groups. Six groups used oral arthemisin as blood esquizonticide at different doses for one day and the other two groups received chloroquine in a single dose. The primaquine was used as a hypnozoiticide in all groups. They received a daily dose of 30mg in the course of five or seven days in all groups.

Author(s): 
da Silva, Rita do Socorro Uchôa
Pinto, Ana Yecê das Neves
Calvosa, Vanja Suely Pachiano
de Souza, José Maria
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

An open randomized controlled study of mefloquine-artesunate and mefloquine-primaquine for the treatment of uncomplicated Plasmodium falciparum malaria was carried out in Kanchanaburi in the Saiyok District in western Thailand. Weekly parasite counts from thick and thin blood films were done for six weeks. The gametocyte carriage rate was calculated and compared between the two treatment groups. Gametocytes on presentation, recrudescent infection, and reinfection were the significant factors associated with subsequent development of gametocytemia.

Author(s): 
Suputtamongkol, Yupin
Chindarat, Supat
Silpasakorn, Saowalak
Chaikachonpatd, Suchada
Lim, Kimheng
Chanthapakajee, Kittiporn
Kaewkaukul, Naparat
Thamlikitkul, Visanu
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

We studied prospectively 801 Thai patients admitted to the Bangkok Hospital for Tropical Diseases with acute, symptomatic Plasmodium vivax malaria to determine the optimum duration of treatment with oral artesunate and the safety, tolerability, and effectiveness of a high dose of primaquine in prevention of relapse.

Author(s): 
Silachamroon, Udomsak
Krudsood, Srivicha
Treeprasertsuk, Sombat
Wilairatana, Polrat
Chalearmrult, Kobsiri
Mint, Hla Yin
Maneekan, Pannamas
White, Nicholas J.
Gourdeuk, Victor R.
Brittenham, Gary M.
Looareesuwan, Sornchai
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

The sporontocidal activity of tafenoquine (WR-238605) and artelinic acid was determined against naturally circulating isolates of Plasmodium vivax in western Thailand. Primaquine was used as a negative control and a dihydroacridine-dione (WR-250547) was used as a positive control. Laboratory-reared Anopheles dirus mosquitoes were infected with P. vivax by allowing mosquitoes to feed on blood (placed in an artificial-membrane feeding apparatus) collected from gametocytemic volunteers reporting to local malaria clinics in Tak province, Thailand.

Author(s): 
Ponsa, Narong
Sattabongkot, Jetsumon
Kittayapong, Pattamaporn
Eikarat, Nantana
Coleman, Russell E.
Publication Title: 
Antimicrobial Agents and Chemotherapy

The activities of primaquine in combination with quinine or artesunate against asexual- and sexual-stage parasites were assessed in 176 adult Thai patients with uncomplicated Plasmodium falciparum malaria. Patients were randomized to one of the six following 7-day oral treatment regimens: (i) quinine alone, (ii) quinine with tetracycline, (iii) quinine with primaquine at 15 mg/day, (iv) quinine with primaquine at 30 mg/day, (v) artesunate alone, or (vi) artesunate with primaquine. Clinical recovery occurred in all patients.

Author(s): 
Pukrittayakamee, Sasithon
Chotivanich, Kesinee
Chantra, Arun
Clemens, Ralf
Looareesuwan, Sornchai
White, Nicholas J.

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