scholarly journals Activity of Picolinic Acid in Combination with the Antiprotozoal Drug Quinacrine against Mycobacterium avium Complex

2006 ◽  
Vol 50 (9) ◽  
pp. 3186-3188 ◽  
Author(s):  
Toshiaki Shimizu ◽  
Haruaki Tomioka

ABSTRACT We studied the in vitro and in vivo antimicrobial activities of picolinic acid (PA) in combination with the antiprotozoal drug quinacrine against intramacrophage Mycobacterium avium complex (MAC). Quinacrine significantly potentiated the anti-MAC activity of PA, suggesting the usefulness of this combination in the clinical control of MAC infection.

Tubercle ◽  
1988 ◽  
Vol 69 (3) ◽  
pp. 187-192 ◽  
Author(s):  
Hajime Saito ◽  
Katsumasa Sato ◽  
Haruaki Tomioka

1994 ◽  
Vol 28 (11) ◽  
pp. 1250-1254 ◽  
Author(s):  
Daniel S. Maddix ◽  
Kimberly B. Tallian ◽  
Paul S. Mead

OBJECTIVE: To discuss the mechanism of action, in vitro and in vivo activity, pharmacokinetics, clinical trials, adverse effects, drug interactions, and dosage guidelines of rifabutin. DATA SOURCES: Pertinent literature published between 1982 and 1993 was identified via a MEDLINE search. Published proceedings of selected conferences were also reviewed. STUDY SELECTION: Selected basic science, microbiologic, and pharmacokinetic articles were evaluated. Because only limited data regarding rifabutin were available in the literature, all clinical trials involving the use of rifabutin in the prevention of Mycobacterium avium complex (MAC) infection in AIDS patients were reviewed. DATA SYNTHESIS: Rifabutin is a rifamycin derivative that was approved recently for the prevention of disseminated MAC disease in patients with advanced HIV infection. The drug has in vitro and in vivo activity against gram-positive bacteria, gram-negative bacteria, and mycobacteria. Two prospective, randomized, double-blind, placebo-controlled, multicenter trials demonstrated that rifabutin decreased the progression to MAC bacteremia in AIDS patients by about 50 percent. Adverse effects that resulted in the discontinuation of rifabutin prophylaxis occurred in 16 percent of patients. Rifabutin induces hepatic enzymes to a lesser extent than does rifampin, but dosage adjustment of drugs that are known to interact with rifampin may be required. CONCLUSIONS: Rifabutin is the only drug shown to be effective in the prevention of MAC bacteremia in AIDS patients; therefore, it should be made available as a formulary agent. It may be reasonable to delay initiation of rifabutin prophylaxis until CD4 lymphocyte counts are less than 75–50/mm3.


1999 ◽  
Vol 43 (12) ◽  
pp. 3001-3004 ◽  
Author(s):  
Haruaki Tomioka ◽  
Katsumasa Sato ◽  
Tatsuya Akaki ◽  
Hiroko Kajitani ◽  
Shin Kawahara ◽  
...  

ABSTRACT We compared the in vitro antimycobacterial activity of a new fluoroquinolone, HSR-903, with strong activity against gram-positive cocci with those of levofloxacin (LVFX), sitafloxacin (STFX), and gatifloxacin (GFLX). The MICs of the quinolones for Mycobacterium tuberculosis and Mycobacterium avium complex were in the order STFX ≈ GFLX < LVFX ≦ HSR-903 and STFX ≦ GFLX ≦ HSR-903 ≦ LVFX, respectively. HSR-903 effectively eliminated intramacrophagial M. tuberculosis, as did LVFX, and exhibited bacteriostatic effects against M. tuberculosis replicating in type II alveolar cells.


1994 ◽  
Vol 4 (3) ◽  
pp. 175-181 ◽  
Author(s):  
Hajime Saito ◽  
Haruaki Tomioka ◽  
Katsumasa Sato ◽  
Satoshi Dekio

2011 ◽  
Vol 37 (4) ◽  
pp. 296-301 ◽  
Author(s):  
Chiaki Sano ◽  
Yutaka Tatano ◽  
Toshiaki Shimizu ◽  
Seiko Yamabe ◽  
Katsumasa Sato ◽  
...  

1996 ◽  
Vol 40 (3) ◽  
pp. 546-551 ◽  
Author(s):  
L E Bermudez ◽  
C B Inderlied ◽  
P Kolonoski ◽  
M Wu ◽  
L Barbara-Burnham ◽  
...  

Levofloxacin, ofloxacin, and Bay Y 3118 are new fluoroquinolones with variable in vitro bacteriostatic and bactericidal activities against the Mycobacterium avium complex (MAC). The potential therapeutic activities of these agents both alone and combined with ethambutol were evaluated in a human macrophage test system and in the beige mouse animal test system with MAC strain 101. Bay Y 3118 at a human-equivalent dose of 30 mg/kg/day for 4 weeks caused a significant reduction in mortality compared with that in untreated controls (P = 0.02). Bay Y 3118 also caused significant reductions in the number of MAC organisms in the blood, liver tissue, and spleen tissue compared with those in untreated controls. Levofloxacin at a human-equivalent dose of 200 mg/kg/day was associated with a significant reduction in mortality (10 versus 39%); however, treatment with either levofloxacin or ofloxacin (200 mg/kg/day) did not result in significant reductions in the numbers of MAC organisms in blood, liver, and spleen compared with those in untreated controls. When Bay Y 3118 was combined with ethambutol, there was no enhancement in therapeutic activity except in the spleen in terms of CFU per gram (reductions of 89% compared with the untreated control, 63% compared with Bay Y 3118 alone, and 72.5% compared with ethambutol alone). Levofloxacin in combination with ethambutol was more active than either drug alone in the reduction of organisms in blood, liver, and spleen. Bay Y 3118 was the most active fluoroquinolone for monotherapy of MAC infection in beige mice, and the combination of ethambutol plus either levofloxacin or ofloxacin was at least additive. In summary, this study demonstrates that quinolones, although active, are inhibitory against MAC in vivo and that there is little correlation between the activity of quinolones in vitro and the activity in mice.


1989 ◽  
Vol 159 (5) ◽  
pp. 994-997 ◽  
Author(s):  
C. B. Inderlied ◽  
P. T. Kownoski ◽  
M. Wu ◽  
L. S. Young

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