Azithromycin: Antimalarial Profile against Blood- and Sporozoite-Induced Infections in Mice and Monkeys

Puri, Sunil K.; Singh, Naresh

doi:10.1006/expr.1999.4465

Cited by 75 publications

(58 citation statements)

References 18 publications

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“…5 Other advantages include (1) the possibility of oral and injectable administration, (2) good oral bioavailability and long half-life, 6-8 (3) relative safety for use in children and pregnant women (Food and Drug Administration category B), and (4) a benign toxicity profile. 9 Several different protozoan infections of humans have been shown in vitro and in vivo to be susceptible to azithromycin in varying degrees, including Acanthamoeba, 10 Cryptosporidium parvum, 11 Plasmodium falciparum, Plasmodium malariae, Plasmodium vivax, [12][13][14][15] and Toxoplasma gondii. [16][17][18][19][20] Studies involving T. gondii showed direct effects of the drug on the parasite's viability by inhibition of protein synthesis.…”

Section: Introductionmentioning

confidence: 99%

Activity of azithromycin against Leishmania major in vitro and in vivo.

Krolewiecki¹,

Leon²,

Scott³

et al. 2002

The American Journal of Tropical Medicine and Hygiene

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Abstract. Azithromycin, an azalide antibiotic of the macrolide family, concentrates in the tissues and especially in macrophages. Because Leishmania parasites reside in these cells, we tested this antibiotic for a possible antileishmanial activity in vitro and in vivo. Azithromycin decreased the Leishmania major promastigote count in cell-free cultures at log phase approximately 50-fold. In macrophage cultures infected with L. major amastigotes, azithromycin caused a significant decrease in parasite levels with an ED 50 of 12 g/ml. The activity in vivo was evaluated after infection of the footpads of susceptible BALB/cByJ mice and resistant C57BL/6J mice with L. major. Treatment of BALB/cByJ mice with azithromycin, 100 to 200 mg/kg/d, resulted in a significant decrease in lesion size and in the number of parasites per lesion, whereas no effect was seen in the treated C57BL/6J mice. Azithromycin has activity against L. major in vitro and in vivo. Given the severity of the disease and the limitations of the available therapeutic agents, azithromycin may have a significant role in the treatment of this group of diseases.

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Section: Introductionmentioning

confidence: 99%

Activity of azithromycin against Leishmania major in vitro and in vivo.

Krolewiecki¹,

Leon²,

Scott³

et al. 2002

The American Journal of Tropical Medicine and Hygiene

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“…Experimental observations obtained in vitro (3,40) and in clinical studies (4,16) proved the antimalarial activity of doxycycline. Macrolide antibiotics, such as erythromycin and azithromycin, also have both in vitro activity against P. falciparum (11,13) and clinical activity (42,48). Similarly, fluoroquinolones were also proven to have antimalarial activity in vitro (19,56) and in vivo (50).…”

mentioning

confidence: 99%

In Vitro Activities of Antibiotics against Plasmodium falciparum Are Inhibited by Iron

Pradines

Rogier

Fusaı̈

et al. 2001

Antimicrob Agents Chemother

106

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The in vitro activities of cyclines (tetracycline, doxycycline, minocycline, oxytetracycline, and rolitetracycline), macrolides (erythromycin, spiramycin, roxithromycin, and lincomycin), quinolones (norfloxacin and ofloxacin), rifampin, thiamphenicol, tobramycin, metronidazole, vancomycin, phosphomycin, and cephalosporins (cephalexin, cefaclor, cefamandole, cefuroxime, ceftriazone, cefotaxime, and cefoxitin) were evaluated on Plasmodium falciparum clones, using an isotopic, micro-drug susceptibility test. Only tetracyclines, macrolides, quinolones, and rifampin demonstrated in vitro activity against P. falciparum, which increased after a prolonged exposure (96 or 144 h). In the presence of iron (FeCl 3 ), only the activities of tetracyclines and norfloxacin were decreased. Their in vitro activity against intraerythrocytic stages of multidrug-resistant P. falciparum and their efficacy in vivo favor the use of antibiotics as antimalarial drugs. However, due to their slow antimalarial action and to the fact that they act better after prolonged contact, they probably need to be administered in conjunction with a rapidly acting antimalarial drug, such as a short course of chloroquine or quinine.

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“…The cultures of P. falciparum NF-54 strain are routinely maintained in medium RPMI 1640 supplemented with 25 mM HEPES, 1% d-glucose, 0.23% sodium bicarbonate and 10% heat inactivated human serum 24 . The asynchronous parasites of P. falciparum were synchronized after 5% d-sorbitol treatment to obtain only the ring stage parasitized cells.…”

Section: Measurement Of In Vitro Antimalarial Activitymentioning

confidence: 99%

“…The in vivo drug response was evaluated in Swiss mice infected with P. yoelii (N-67 strain 24 ). The mice (22 ± 2 g) were inoculated with 1 × 10 6 parasitized RBC on day 0 and treatment was administered to a group of five mice from day 0 to 3, once daily.…”

Section: In Vivo Antimalarial Efficacy Testmentioning

confidence: 99%

“…The efficacy of test compounds was evaluated at 30.0 mg/kg/ day and required daily dose was administered in 0.2 mL volume via intraperitoneal route. Parasitaemia levels were recorded from thin blood smears between days 4 and 28 24 . The mean value determined for a group of five mice was used to calculate the percent suppression of parasitaemia with respect to the untreated control group.…”

Section: In Vivo Antimalarial Efficacy Testmentioning

confidence: 99%

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