Aminoquinolines

Publication Title: 
The Cochrane Database of Systematic Reviews

BACKGROUND: Molluscum contagiosum is a common skin infection that is caused by a pox virus and occurs mainly in children. The infection usually resolves within months in people without immune deficiency, but treatment may be preferred for social and cosmetic reasons or to avoid spreading the infection. A clear evidence base supporting the various treatments is lacking.This is an update of a Cochrane Review first published in 2006, and updated previously in 2009.

Author(s): 
van der Wouden, Johannes C.
van der Sande, Renske
Kruithof, Emma J.
Sollie, Annet
van Suijlekom-Smit, Lisette Wa
Koning, Sander
Publication Title: 
Antimicrobial Agents and Chemotherapy

The antimicrobial activities of chloroquine (CQ) and several 4-aminoquinoline drugs were tested against Penicillium marneffei, an opportunistic fungus that invades and grows inside macrophages and causes disseminated infection in AIDS patients. Human THP1 and mouse J774 macrophages were infected in vitro with P. marneffei conidia and treated with different doses of drugs for 24 to 48 h followed by cell lysis and the counting of P. marneffei CFU. CQ and amodiaquine exerted a dose-dependent inhibition of fungal growth, whereas quinine and artemisinin were fungistatic and not fungicidal.

Author(s): 
Taramelli, D.
Tognazioli, C.
Ravagnani, F.
Leopardi, O.
Giannulis, G.
Boelaert, J. R.
Publication Title: 
British Journal of Clinical Pharmacology

AIMS: To describe the population pharmacokinetics of tafenoquine in healthy volunteers after receiving tafenoquine for malaria prophylaxis. METHODS: The population consisted of 135 male Thai soldiers (mean age 28.9 years; weight 60.3 kg). All soldiers were presumptively treated with artesunate for 3 days plus doxycycline for 7 days to remove any pre-existing malaria infections. After the treatment regime, 104 soldiers (drug group) received a loading dose of 400 mg tafenoquine base daily for 3 days followed by 400 mg tafenoquine monthly for 5 consecutive months.

Author(s): 
Edstein, M. D.
Kocisko, D. A.
Brewer, T. G.
Walsh, D. S.
Eamsila, C.
Charles, B. G.
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

Emergence and spread of drug-resistant falciparum malaria has created an urgent demand for alternative therapeutic agents. This study was conducted to assess the in vitro blood schizontocidal activity of tafenoquine, the most advanced candidate drug of the 8-aminoquinolines, and of its 1:1 combination with artemisinin in fresh isolates of Plasmodium falciparum in an area with multi-drug resistance, measuring the inhibition of schizont maturation.

Author(s): 
Ramharter, Michael
Noedl, Harald
Thimasarn, Krongthong
Wiedermann, Gerhard
Wernsdorfer, Gunther
Wernsdorfer, Walther H.
Publication Title: 
Antimicrobial Agents and Chemotherapy

Three antimalarial drugs, artesunate, pyrimethamine, and pamaquine, were evaluated for their growth-inhibitory effects against Babesia equi and Babesia caballi in in vitro culture. B. equi was more resistant to pyrimethamine than B. caballi. B. equi was also found to be more sensitive to artesunate and pamaquine than B. caballi. Of the three compounds, pyrimethamine gave the most promise for in vivo effectiveness.

Author(s): 
Nagai, Akiko
Yokoyama, Naoaki
Matsuo, Tomohide
Bork, Sabine
Hirata, Haruyuki
Xuan, Xuenan
Zhu, Yinchang
Claveria, Florencia G.
Fujisaki, Kozo
Igarashi, Ikuo
Publication Title: 
Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America

We measured plasma tafenoquine concentrations in Thai soldiers given a monthly regimen of tafenoquine to determine whether these concentrations adequately suppressed malarial infections on the Thai-Cambodian border. After receiving a treatment course of artesunate and doxycycline, 104 male soldiers were administered a loading dose of tafenoquine (400 mg daily for 3 days), followed by tafenoquine monthly (400 mg every 4 weeks) for 5 months.

Author(s): 
Edstein, Michael D.
Kocisko, David A.
Walsh, Douglas S.
Eamsila, Chirapa
Charles, Bruce G.
Rieckmann, Karl H.
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

Malaria is the third most significant cause of infectious disease in the world. The search for new antimalarial chemotherapy has become increasingly urgent due to parasite resistance to classical drugs. Trioxaquines are synthetic hybrid molecules containing a trioxane motif (which is responsible for the antimalarial activity of artemisinin) linked to an aminoquinoline entity (which is responsible for the antiplasmodial properties of chloroquine).

Author(s): 
Benoit-Vical, Françoise
Lelièvre, Joel
Berry, Antoine
Deymier, Caroline
Dechy-Cabaret, Odile
Cazelles, Jérôme
Loup, Christophe
Robert, Anne
Magnaval, Jean-François
Meunier, Bernard
Publication Title: 
Antimicrobial Agents and Chemotherapy

In an attempt to augment the efficacy of 7-chloro 4-aminoquinoline analogs and also to overcome resistance to antimalarial agents, we synthesized three cyclen (1,4,7,10-tetraazacyclododecane) analogs of chloroquine [a bisquinoline derivative, 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline HBr, and a 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline-Zn(2+) complex]. The bisquinoline displays the most potent in vitro and in vivo antimalarial activities.

Author(s): 
Khan, M. O. Faruk
Levi, Mark S.
Tekwani, Babu L.
Khan, Shabana I.
Kimura, Eiichi
Borne, Ronald F.
Publication Title: 
Malaria Journal

Effective anti-malarial drug treatment reduces malaria transmission. This alone can reduce the incidence and prevalence of malaria, although the effects are greater in areas of low transmission where a greater proportion of the infectious reservoir is symptomatic and receives anti-malarial treatment. Effective treatment has greater effects on the transmission of falciparum malaria, where gametocytogenesis is delayed, compared with the other human malarias in which peak gametocytaemia and transmissibility coincides with peak asexual parasite densities.

Author(s): 
White, Nicholas J.

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