Summary
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▴ Grepafloxadn (OPC-17116) is a new once-daily fluoroquinolone antimicrobial agent which appears to have high tissue penetration and the wide spectrum of antimicrobial activity typical of this class of agents, but with improved activity against Grampositive organisms, notably Streptococcus pneumoniae.
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▴ The in vitro activity of grepafloxacin was similar to or slightly lower than that of ciprofloxacin against Enterobacteriaceae but better than that of ciprofloxacin against most Gram-positive organisms. In particular, grepafloxacin showed good activity against pathogens implicated in community-acquired pneumonia, with 4-fold higher potency than ciprofloxacin against S. pneumoniae, including penicillinresistant strains.
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▴ In animal studies, grepafloxacin did not induce convulsions when administered at high doses in conjunction with nonsteroidal anti-inflammatory agents. A Grepafloxacin has a weak propensity for causing phototoxicity, similar to that of ciprofloxacin. ▴ In comparative clinical trials, grepafloxacin demonstrated similar efficacy to amoxicillin in community-acquired pneumonia, ofloxacin in pneumonia and chronic respiratory tract infection, and cefixime in uncomplicated gonococcal urethritis and gonococcal cervicitis.
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▴ Grepafloxacin has also shown clinical efficacy in preliminary studies in patients with chlamydial endocervical infection or bacillary dysentery.
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References
Sader HS, Jones RN, Allen SD, et al. In vitro comparison activity of OPC-17116, a new fluoroquinolone, against more than 5,000 recent clinical isolates from five medical centers. J Chemother 1993 Oct; 5: 283–8
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Sewell DL, Barry AL, Allen SD, et al. Tentative interpretive criteria and quality control parameters for in-vitro susceptibility testing of Neisseria gonorrhoeae to two fluoroquinolones (PD 131628 and grepafloxacin (OPC 17116)). J Antimicrob Chemother 1996 Jan; 37: 139–43
National Committee for Clinical Laboratory Standards. Performance standards for antimicrobial susceptibility testing. NCCLS Document M100-S5 1994 December; 14 (16): Tables 2, 2A, 2B
Marco F, Jones RN, Hoban DJ, et al. In-vitro activity of OPC-17116 against more than 6000 consecutive clinical isolates: a multicentre international study. J Antimicrob Chemother 1994 Mar; 33: 647–54
Spangler SK, Jacobs MR, Pankuch GA, et al. Susceptibility of 170 penicillin-susceptible and penicillin-resistant pneumococci to six oral cephalosporins, four quinolones, desacetylcefotaxime, Ro 23-9424 and RP 67829. J Antimicrob Chemother 1993 Feb; 31: 273–80
Wise R, Andrews JM, Brenwald N. The in-vitro activity of OPC-17116, a new 5-methyl substituted quinolone. J Antimicrob Chemother 1993 Apr; 31: 497–504
Tateyama M, Fukuhara H, Irabu Y, et al. In vitro antimicrobial activity of grepafloxacin and its therapeutic efficacy on respiratory infections [in Japanese]. Jpn J Chemother 1995 Jul; 43 Suppl. 1: 308–13
Sader HS, Erwin ME, Jones RN. In vitro activity of OPC-17116 compared to other broad-spectrum fluoroquinolones. Eur J Clin Microbiol Infect Dis 1992 Apr; 11: 372–81
Ohguro K, Wakebe H, Azuma A, et al. In vitro and in vivo antibacterial activity of grepafloxacin [in Japanese]. Jpn J Chemother 1995 Jul; 43 Suppl. 1: 74–90
Zenilman JM, Neumann T, Patton M, et al. Antibacterial activities of OPC-17116, ofloxacin, and ciprofloxacin against 200 isolates of Neisseria gonorrhoeae. Antimicrob Agents Chemother 1993 Oct; 37: 2244–6
Kenny GE, Cartwright FD. Susceptibilities of Mycoplasma hominis, Mycoplasma pneumoniae and Ureaplasma urealyticum to a new quinolone, OPC 17116. Antimicrob Agents Chemother 1993 Aug; 37: 1726–7
Kimura M, Kishimoto T, Niki Y, et al. In vitro and in vivo antichlamydial activities of newly developed quinolone antimicrobial agents. Antimicrob Agents Chemother 1993 Apr; 37: 801–3
Spangler SK, Jacobs MR, Appelbaum PC. Activity of CP 99,219 compared with those of ciprofloxacin, grepafloxacin, metronidazole, cefoxitin, piperacillin, and piperacillintazobactam against 489 anaerobes. Antimicrob Agents Chemother 1994 Oct; 38: 2471–6
Thomson KS, Sanders CC. Dissociated resistance among fluoroquinolones. Antimicrob Agents Chemother 1994 Sep; 38: 2095–100
Gu J-w, Fang W, Neu HC. Plasma bactericidal activity of a new C-5 methyl fluoroquinolone after oral doses of 400 and 800 mg. J Clin Pharmacol 1992 Sep; 32: 804–7
Forrest A, Amantea M, Collins DA, et al. Pharmacodynamics of oral OPC-17116 in patients with acute bacterial exacerbations of chronic bronchitis [abstract no. 81]. 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy 1993; New Orleans (LA): 17–20 Oct, 1993: 134
Ferguson J. Double blind placebo and ciprofloxacin controlled phototest study of the in vivo phototoxic potential of OPC-17116 in normal volunteers [abstract no. M57]. 34th Interscience Conference on Antimicrobial Agents and Chemotherapy 1994; Orlando (FL): 4–7 Oct, 1994: 246
Shintani S, Kusunoki A, Hosoki E, et al. Drug interaction of OPC-17116, a new quinolone antibacterial agent, with non-steroidal anti-inflammatory drugs in experimental animal [abstract no. 1479]. 31st Interscience Conference on Antimicrobial Agents and Chemotherapy 1991; Chicago (IL): 29 Sep–2Oct, 1991:345
Akiyama H, Koike M, Nii S, et al. OPC-17116, an excellently tissue-penetrative new quinolone: pharmacokinetic profiles in animals and antibacterial activities of metabolites [abstract no. 1477]. In: 31st Interscience Conference on Antimicrobial Agents and Chemotherapy 1991; Chicago (IL): 29 Sep–2 Oct, 1991: 345
Koike M, Nii S, Morita S, et al. OPC-17116, a new quinolone: pharmacokinetics and metabolism in healthy volunteers [abstract no. 1482]. 31st Interscience Conference on Antimicrobial Agents and Chemotherapy 1991; Chicago (IL): 29 Sep–Oct, 1991: 346
Nakashima M, Uematsu T, Nagashima S, et al. Phase I study of grepafloxacin [in Japanese]. Jpn J Chemother 1995 Jul; 43 Suppl. 1: 155–75
Child J, Andrews JM, Wise R. Pharmacokinetics and tissue penetration of the new fluoroquinolone grepafloxacin. Antimicrob Agents Chemother 1995 Feb; 39: 513–5
Matsuda S, Japanese Collaborative Study Group of OPC-17116 in Gynaecology. Clinical experience with OPC-17116 in the treatment of gynaecological infections and its penetration into gynaecological tissues. Drugs 1995; 49 Suppl 2: 395–8
Suzuki K, Horiba M, Ishikawa K, et al. Penetration of grepafloxacin in prostatic fluid and a clinical study in urinary tract infections [in Japanese]. Jpn J Chemother 1995 Jul; 43 Suppl. 1: 376–85
Shimizu T, Sato O. Studies on biliary excretion and clinical evaluation of a new oral antimicrobial agent, grepafloxacin [in Japanese]. Jpn J Chemother 1995 Jul; 43 Suppl. 1: 430–7
Cook PJ, Andrews JM, Wise R. Concentrations of OPC-17116, a new fluoroquinolone antibacterial, in serum and lung compartments. J Antimicrob Chemother 1995 Feb; 35: 317–26
Taira K, Koga H, Kohno S. Accumulation of a newly developed fluoroquinolone, OPC-17116, by human polymorphonuclear leukocytes. Antimicrob Agents Chemother 1993 Sep; 37: 1877–81
Niki Y, Hashiguchi K, Okimoto N. Quinolone antimicrobial agents and theophylline. Chest 1992 Mar; 101: 881
Goss TF, Forrest A, Amantea MA, et al. Multiple-dose pharmacokinetics (PKs) of oral OPC-17116 in elderly subjects (poster no. 408). 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy 1993; New Orleans (LA): 17–20 Oct, 1993
Kozawa O, Uematsu T, Matsuno H, et al. Comparative study of pharmacokinetics of two new fluoroquinolones, balofloxacin and grepafloxacin, in elderly subjects. Antimicrob Agents Chemother 1996 Dec; 40: 2824–8
Kawada Y, Itoh Y, Yamada S-i, et al. Pharmacokinetics of grepafloxacin in patients with impaired renal function [in Japanese]. Jpn J Chemother 1995 Jul; 43 Suppl. 1: 190–3
O’Doherty B, UK and Ireland OPC-17116 collaborative research team. Treatment of community-acquired pneumonia: a comparison of OPC-17116 and amoxicillin [abstract no. M55]. 34th Interscience Conference on Antimicrobial Agents and Chemotherapy 1994; Orlando (FL): 4–7 Oct, 1994: 245
Kobayashi H, Grepafloxacin Study Group. A multicentre double-blind comparative study of grepafloxacin (GPFX) versus ofloxacin in the treatment of pneumonia [poster no. LM18]. 36th Interscience Conference on Antimicrobial Agents and Chemotherapy 1996; New Orleans (LA): 15–18 Sep, 1996
Kobayashi H, Grepafloxacin Study Group. A multicenter, double-blind comparative study of grepafloxacin (GPFX) versus ofloxacin in the treatment of chronic respiratory tract infection [poster no. LM15]. 36th Interscience Conference on Antimicrobial Agents and Chemotherapy 1996; New Orleans (LA): 15–18 Sep, 1996
Hook EW, McCormack WM, Martin D, et al. Comparison of single-dose oral grepafloxacin with cefixime for treatment of uncomplicated gonorrhoea in men [poster no. LM19]. 36th Interscience Conference on Antimicrobial Agents and Chemotherapy 1996; New Orleans (LA): 15–18 Sep, 1996
Mroczkowski TF, Martin DH, Bean KA, et al. OPC-17116 in the treatment of gonococcal and chlamydial cervicitis [abstract no. 30]. J Eur Acad Dermatol Venereol 1995 Oct; 5 Suppl. 1: S77
Mroczkowski TF, Bean KA, Martin DH. A dose ranging study of a new quinolone, OPC-17116, for the treatment of Chlamydia trachomatis infection in women [abstract no. 17]. Sex Transm Dis 1994 Mar–Apr; 21 Suppl.: S106–7
Irimajiri S, Imagawa Y, Matsubara Y. Multi-center clinical trial of OPC-17116 in bacillary dysentery and cholera [abstract no. 1422]. 18th International Congress of Chemotherapy 1993; Stockholm, Sweden: 27 Jun–2 Jul, 1993: 359
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Wagstaff, A.J., Balfour, J.A. Grepafloxacin. Drugs 53, 817–824 (1997). https://doi.org/10.2165/00003495-199753050-00007
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DOI: https://doi.org/10.2165/00003495-199753050-00007