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PMID: 3292209 Published · ppublish English Journal Article Review

Ciprofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.

Drugs ·Vol. 35 ·No. 4 ·1988-04-00 ·Pages 373-447

Campoli-Richards DM, Monk JP, Price A, Benfield P, Todd PA, Ward A

Abstract

Ciprofloxacin is one of a new generation of fluorinated quinolones structurally related to nalidixic acid. The primary mechanism of action of ciprofloxacin is inhibition of bacterial DNA gyrase. It is a broad spectrum antibacterial drug to which most Gram-negative bacteria are highly susceptible in vitro and many Gram-positive bacteria are susceptible or moderately susceptible. Unlike most broad spectrum antibacterial drugs, ciprofloxacin is effective after oral or intravenous administration. Ciprofloxacin has been most extensively studied following oral administration. It attains concentrations in most tissues and body fluids which are at least equivalent to the minimum inhibitory concentration designated as the breakpoint for bacterial susceptibility in vitro. The results of clinical trials with orally and intravenously administered ciprofloxacin have confirmed the potential for its use in a wide range of infections, which was suggested by its in vitro antibacterial and pharmacokinetic profiles. It has proven an effective treatment for many types of systemic infections as well as for both acute and chronic infections of the urinary tract. Ciprofloxacin generally appeared to be at least as effective as alternative orally administered antibacterial drugs in the indications in which they were compared, and in some indications, to parenterally administered antibacterial therapy. However, further studies are needed to fully clarify the comparative efficacy of ciprofloxacin and standard antibacterial therapies. Bacterial resistance to ciprofloxacin develops infrequently, both in vitro and clinically, except in the setting of pseudomonal respiratory tract infections in cystic fibrosis patients. The drug is also well tolerated. Thus, as an orally active, broad spectrum and potent antibacterial drug, ciprofloxacin offers a valuable alternative to broad spectrum parenterally administered antibacterial drugs for use in a wide range of clinical infections, including difficult infections due to multiresistant pathogens.

MeSH Terms
Animals Bacteria/drug effects Bacterial Infections/drug therapy Ciprofloxacin/pharmacokinetics,pharmacology,therapeutic use Humans
Chemicals
Ciprofloxacin
Authors & Affiliations
6 authors, click to expand affiliations / ORCID
Campoli-Richards D M
ADIS Drug Information Services, Auckland.
Monk J P
Price A
Benfield P
Todd P A
Ward A
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    Antimicrob Agents Chemother. 1986 Feb;29(2):337-8 PMID: 2940967
  148. Penetration of ciprofloxacin into gynecological tissues following oral and intravenous administration.
    Chemotherapy. 1986;32(1):7-17 PMID: 2936582
  149. Treatment of Staphylococcus aureus endocarditis in rats with coumermycin A1 and ciprofloxacin, alone or in combination.
    Antimicrob Agents Chemother. 1987 Apr;31(4):539-43 PMID: 3606060
  150. Systemic treatment of cutaneous infections. A comparative study of ciprofloxacin and cefotaxime.
    Am J Med. 1987 Apr 27;82(4A):227-9 PMID: 3555041
  151. Studies on ciprofloxacin therapy of experimental Legionnaires' disease.
    J Infect. 1985 May;10(3):194-203 PMID: 3161954
  152. Ciprofloxacin therapy for Mediterranean spotted fever.
    Antimicrob Agents Chemother. 1986 Oct;30(4):606-7 PMID: 3789693
  153. Ciprofloxacin for cholangitis.
    Lancet. 1987 Jul 25;2(8552):212 PMID: 2885658
  154. Treatment of chronic bacterial prostatitis with ciprofloxacin. Results of a one-year follow-up study.
    Am J Med. 1987 Apr 27;82(4A):280-3 PMID: 3555048
  155. Comparative activity of ciprofloxacin against anaerobic bacteria.
    Antimicrob Agents Chemother. 1985 Mar;27(3):427-8 PMID: 3158278
  156. Efficacy and safety of oral ciprofloxacin for treatment of serious urinary tract infections.
    Antimicrob Agents Chemother. 1987 Feb;31(2):148-50 PMID: 3566244
  157. Pharmacokinetics of intravenously administered ciprofloxacin.
    Antimicrob Agents Chemother. 1984 Aug;26(2):208-10 PMID: 6486762
  158. Ciprofloxacin for eradication of methicillin-resistant Staphylococcus aureus colonization.
    Am J Med. 1987 Apr 27;82(4A):215-9 PMID: 3555039
  159. Comparative evaluation of recently developed quinolone compounds--with a note on the frequency of resistant mutants.
    Chemotherapy. 1985;31(1):19-28 PMID: 3156025
  160. Comparative in vitro activity of seven quinolones against 100 clinical isolates of Clostridium difficile.
    Antimicrob Agents Chemother. 1986 Feb;29(2):374-5 PMID: 2940968
  161. Quinolones and colonization resistance in human volunteers.
    Pharm Weekbl Sci. 1986 Feb 21;8(1):67-71 PMID: 2938072
  162. Antibiotic-induced endotoxin release.
    Lancet. 1985 Nov 9;2(8463):1069-70 PMID: 2865548
  163. In vitro susceptibility of nosocomial Pseudomonas aeruginosa, enterobacteriaceae, and staphylococci to ciprofloxacin and ten other broad-spectrum antibiotics.
    Chemioterapia. 1987 Oct;6(5):315-8 PMID: 3123078
  164. Frequent antibiotic therapy improves survival of cystic fibrosis patients with chronic Pseudomonas aeruginosa infection.
    Acta Paediatr Scand. 1983 Sep;72(5):651-7 PMID: 6637463
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  167. Randomized trial of ciprofloxacin compared with other antimicrobial therapy in the treatment of osteomyelitis.
    Am J Med. 1987 Apr 27;82(4A):266-9 PMID: 3555046
  168. Sub-MICs of cefuroxime and ciprofloxacin influence interaction of complement and immunoglobulins with Klebsiella pneumoniae.
    Antimicrob Agents Chemother. 1987 May;31(5):758-62 PMID: 3300538
  169. Isolation and structural elucidation of urinary metabolites of ciprofloxacin.
    Arzneimittelforschung. 1986 Oct;36(10):1545-9 PMID: 3814216
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    Lancet. 1987 Jun 13;1(8546):1367 PMID: 2884467
  171. Efficacy of ciprofloxacin in experimental aortic valve endocarditis caused by a multiply beta-lactam-resistant variant of Pseudomonas aeruginosa stably derepressed for beta-lactamase production.
    Antimicrob Agents Chemother. 1986 Oct;30(4):528-31 PMID: 3539007
  172. Comparative trial of single-dose ciprofloxacin and ampicillin plus probenecid for treatment of gonococcal urethritis in men.
    Antimicrob Agents Chemother. 1986 Aug;30(2):267-9 PMID: 3094439
  173. The influence of quinolone derivatives on theophylline clearance.
    Br J Clin Pharmacol. 1986 Dec;22(6):677-83 PMID: 3567014
  174. Comparative efficacy of pefloxacin and six other antimicrobial agents on Staphylococcus aureus experimental abscesses.
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  175. Ciprofloxacin (4-quinolone) and Mycobacterium leprae.
    Lepr Rev. 1986 Jun;57(2):159-62 PMID: 2943954
  176. Single dose ciprofloxacin for treating gonococcal infections in men.
    Genitourin Med. 1985 Oct;61(5):302-5 PMID: 2931345
  177. Ciprofloxacin versus vancomycin in the therapy of experimental methicillin-resistant Staphylococcus aureus endocarditis.
    Antimicrob Agents Chemother. 1987 Apr;31(4):527-30 PMID: 3649202
  178. An overview of the pharmacology of intravenously administered ciprofloxacin.
    Am J Med. 1987 Apr 27;82(4A):339-45 PMID: 3578325
  179. Treatment of chancroid with ciprofloxacin. A prospective, randomized clinical trial.
    Am J Med. 1987 Apr 27;82(4A):317-20 PMID: 3555055
  180. Pharmacokinetics of ciprofloxacin in the elderly.
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  181. Evaluation of ciprofloxacin 500 mg twice daily for one week in treating uncomplicated gonococcal chlamydial, and non-specific urethritis in men.
    Genitourin Med. 1986 Jun;62(3):170-4 PMID: 2942454
  182. Effect of tetracycline on the phagocytic function of human leukocytes.
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  183. Ciprofloxacin therapy in cystic fibrosis.
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  184. Comparative activities of ciprofloxacin, ticarcillin, and tobramycin against experimental Pseudomonas aeruginosa pneumonia.
    Antimicrob Agents Chemother. 1984 Jul;26(1):1-4 PMID: 6433786
  185. Ofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.
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  186. Efficacy of ciprofloxacin in experimental arthritis caused by Escherichia coli--in vitro-in vivo correlations.
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  188. Comprehensive evaluation of ciprofloxacin-aminoglycoside combinations against Enterobacteriaceae and Pseudomonas aeruginosa strains.
    Antimicrob Agents Chemother. 1985 Nov;28(5):663-6 PMID: 2936301
  189. Treatment of Salmonella typhimurium infection in a renal transplant patient with ciprofloxacin.
    N Z Med J. 1987 Mar 25;100(820):190-1 PMID: 3330583
  190. Comparative in vitro activities of selected antimicrobial agents against Aeromonas species and Plesiomonas shigelloides.
    Antimicrob Agents Chemother. 1985 Apr;27(4):643-5 PMID: 4004196
  191. Susceptibility of clinical isolates of Campylobacter pyloridis to 11 antimicrobial agents.
    Antimicrob Agents Chemother. 1985 Dec;28(6):837-8 PMID: 2935076
  192. Pharmacokinetics of oral ciprofloxacin, 100 mg single dose, in volunteers and elderly patients.
    J Antimicrob Chemother. 1986 May;17(5):629-35 PMID: 2941402
  193. The mode of action of 4-quinolones and possible mechanisms of resistance.
    J Antimicrob Chemother. 1986 Nov;18 Suppl D:21-9 PMID: 3542946
  194. Oral ciprofloxacin therapy of infections due to Pseudomonas aeruginosa.
    Lancet. 1986 Apr 12;1(8485):819-22 PMID: 2870313
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    Am J Med. 1987 Apr 27;82(4A):12-20 PMID: 3034057
  197. The pharmacokinetics of ciprofloxacin in patients with impaired renal function.
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  198. Randomized study of two dosage regimens of ciprofloxacin for treating chronic bronchopulmonary infection in patients with cystic fibrosis.
    Am J Med. 1987 Apr 27;82(4A):189-95 PMID: 3555035
  199. Pharmacokinetics of ciprofloxacin after oral and intravenous administration in healthy volunteers.
    Eur J Clin Microbiol. 1984 Aug;3(4):355-9 PMID: 6489326
  200. In-vitro susceptibility of mycobacteria to ciprofloxacin.
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  201. In vitro antibacterial activities of antibiotics against Pseudomonas aeruginosa in peritoneal dialysis fluid.
    Antimicrob Agents Chemother. 1985 Jun;27(6):908-11 PMID: 3927837
  202. Penetration of ciprofloxacin into cerebrospinal fluid.
    Eur J Clin Microbiol. 1986 Apr;5(2):206-7 PMID: 2941282
  203. In-vitro sensitivity of Bacteroidaceae, clostridia and propionibacteria to newer antimicrobial agents.
    J Antimicrob Chemother. 1986 Dec;18 Suppl E:41-6 PMID: 3469196
  204. Antibacterial activity of the metabolites of ciprofloxacin and its significance in the bioassay.
    Arzneimittelforschung. 1987 Feb;37(2):131-4 PMID: 3555512
  205. Gyrase-inhibitors impair caffeine elimination in man.
    Methods Find Exp Clin Pharmacol. 1987 Mar;9(3):193-8 PMID: 3037212
  206. Penetration of ciprofloxacin into cerebrospinal fluid of patients with bacterial meningitis.
    Antimicrob Agents Chemother. 1987 Jun;31(6):899-902 PMID: 3619422
  207. Absolute oral bioavailability of ciprofloxacin.
    Antimicrob Agents Chemother. 1986 Sep;30(3):444-6 PMID: 3777908
  208. Chemoprophylaxis of bacterial infections in granulocytopenic patients with ciprofloxacin.
    Onkologie. 1987 Feb;10(1):57-8 PMID: 3295628
  209. Pharmacokinetics of two dosage regimens of ciprofloxacin during a two-week therapeutic trial in patients with cystic fibrosis.
    Am J Med. 1987 Apr 27;82(4A):142-5 PMID: 3555028
  210. Treatment of Salmonella typhi carrier state with ciprofloxacin.
    Lancet. 1985 May 4;1(8436):1047 PMID: 2859498
  211. Ciprofloxacin-resistant Staphylococcus aureus.
    Lancet. 1985 Aug 17;2(8451):383 PMID: 2862526
  212. Pharmacokinetics of ciprofloxacin after oral and parenteral administration.
    Antimicrob Agents Chemother. 1985 Mar;27(3):375-9 PMID: 3158275
  213. Controlled, comparative study of ciprofloxacin versus ampicillin in treatment of bacterial respiratory tract infections.
    Am J Med. 1987 Apr 27;82(4A):164-8 PMID: 3555030
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    Eur J Clin Microbiol. 1986 Apr;5(2):236-40 PMID: 2941289
  215. Ciprofloxacin resistance.
    Lancet. 1987 Mar 28;1(8535):749-50 PMID: 2882167
  216. Ciprofloxacin versus ampicillin and probenecid in the treatment of uncomplicated gonorrhoea in men.
    J Antimicrob Chemother. 1987 Jul;20(1):117-21 PMID: 3624110
  217. In vitro activity of antimicrobial agents against Acinetobacter calcoaceticus.
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  218. In vitro activity of ciprofloxacin against aerobic bacteria isolated in a southern European hospital.
    Antimicrob Agents Chemother. 1987 Oct;31(10):1651-5 PMID: 3435111
  219. In vitro activity of ciprofloxacin compared with those of other new fluorinated piperazinyl-substituted quinoline derivatives.
    Antimicrob Agents Chemother. 1984 Apr;25(4):518-21 PMID: 6732221
  220. Release of endotoxin from Escherichia coli by quinolones.
    J Antimicrob Chemother. 1986 Dec;18(6):765-6 PMID: 3546245
  221. Preliminary evaluation of ciprofloxacin, a new 4-quinolone antibiotic, in the treatment of febrile neutropenic patients.
    J Antimicrob Chemother. 1986 Nov;18 Suppl D:165-74 PMID: 3468101
  222. The post-antimicrobial suppressive effect of quinolone agents.
    Drugs Exp Clin Res. 1987;13(2):63-7 PMID: 3107958
  223. Ciprofloxacin in oral treatment of ear infections.
    Pharm Weekbl Sci. 1986 Feb 21;8(1):63-6 PMID: 2938071
  224. Infection prophylaxis in acute leukemia: a comparison of ciprofloxacin with trimethoprim-sulfamethoxazole and colistin.
    Ann Intern Med. 1987 Jan;106(1):7-11 PMID: 3466563
  225. Penetration of ciprofloxacin into human lung tissue following intravenous injection.
    Infection. 1986 Nov-Dec;14(6):299-300 PMID: 3818107
  226. Activities of pefloxacin and ciprofloxacin against Mycobacterium leprae in the mouse.
    Int J Lepr Other Mycobact Dis. 1987 Mar;55(1):70-7 PMID: 3549940
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    Dtsch Med Wochenschr. 1986 Oct 17;111(42):1599-602 PMID: 3769803
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  229. Ciprofloxacin pharmacokinetics in patients with normal and impaired renal function.
    Antimicrob Agents Chemother. 1987 May;31(5):709-12 PMID: 3300537
  230. Bactericidal activity of ciprofloxacin against amikacin- and cefotaxime-resistant gram-negative bacilli and methicillin-resistant staphylococci.
    Antimicrob Agents Chemother. 1986 Jun;29(6):1098-100 PMID: 2942105
  231. Renal elimination of sulfo-ciprofloxacin, a new metabolite of ciprofloxacin.
    Eur J Clin Microbiol. 1986 Aug;5(4):476 PMID: 3758059
  232. The use of fluoroquinolones in chronic otitis suppurativa.
    Pharm Weekbl Sci. 1987 Dec 11;9 Suppl:S87-9 PMID: 3325935
  233. Activity of ciprofloxacin against methicillin-resistant Staphylococcus aureus.
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  234. Effect of ciprofloxacin on intracellular organisms: in-vitro and in-vivo studies.
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  235. Clinical resistance to long-term oral ciprofloxacin.
    Lancet. 1985 Jun 1;1(8440):1275 PMID: 2860471
  236. Efficacy of ciprofloxacin in patients with cystic fibrosis.
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    Antimicrob Agents Chemother. 1987 Nov;31(11):1782-6 PMID: 3435125
  238. Effect of inoculum, pH, and medium on the activity of ciprofloxacin against anaerobic bacteria.
    Antimicrob Agents Chemother. 1984 Mar;25(3):342-3 PMID: 6721466
  239. Ciprofloxacin treatment of systemic salmonella infection in sensitive and resistance mice.
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  240. Treatment of uncomplicated gonococcal urethritis in men with two dosages of ciprofloxacin.
    Eur J Clin Microbiol. 1986 Apr;5(2):244-6 PMID: 2941291
  241. Clinical uses of nalidixic acid analogues: the fluoroquinolones.
    Eur J Clin Microbiol. 1986 Apr;5(2):138-40 PMID: 3013628
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  243. Resistance occurring after fluoroquinolone therapy of experimental Pseudomonas aeruginosa peritonitis.
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    J Antimicrob Chemother. 1986 Nov;18 Suppl D:175-8 PMID: 3804905
  245. Post-antibiotic suppressive effect of ciprofloxacin against gram-positive and gram-negative bacteria.
    Am J Med. 1987 Apr 27;82(4A):58-62 PMID: 3578330
  246. Pharmacokinetics and pharmacodynamics of ciprofloxacin in cystic fibrosis patients.
    Antimicrob Agents Chemother. 1986 Aug;30(2):260-6 PMID: 3094438
  247. Comparative activities of ciprofloxacin and ceftazidime against Klebsiella pneumoniae in vitro and in experimental pneumonia in leukopenic rats.
    Antimicrob Agents Chemother. 1987 Nov;31(11):1809-15 PMID: 3324962
  248. Comparative pharmacokinetics of ciprofloxacin and ofloxacin in cystic fibrosis patients.
    J Antimicrob Chemother. 1987 Oct;20(4):575-83 PMID: 3479419
  249. Clinical efficacy of ciprofloxacin therapy for gram-negative bacillary osteomyelitis.
    Am J Med. 1987 Apr 27;82(4A):262-5 PMID: 3555045
  250. Efficacy of ciprofloxacin in the treatment of nasopharyngeal carriers of Neisseria meningitidis.
    J Infect Dis. 1987 Jul;156(1):211-3 PMID: 3110305
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    Antimicrob Agents Chemother. 1984 Nov;26(5):785-6 PMID: 6517561
  252. Influence of quinolones on throat- and faecal flora of healthy volunteers.
    Pharm Weekbl Sci. 1987 Dec 11;9 Suppl:S41-4 PMID: 3438150
  253. Comparative in vitro activity of five quinoline derivatives and five other antimicrobial agents used in oral therapy.
    Eur J Clin Microbiol. 1984 Aug;3(4):333-8 PMID: 6237901
  254. In vitro susceptibility of Clostridium difficile to new beta-lactam and quinolone antibiotics.
    Antimicrob Agents Chemother. 1985 Dec;28(6):842-4 PMID: 4083868
  255. Antibacterial activities of ciprofloxacin, norfloxacin, oxolinic acid, cinoxacin, and nalidixic acid.
    Antimicrob Agents Chemother. 1984 May;25(5):633-7 PMID: 6233935
  256. In vitro synergy of ciprofloxacin and three other antibiotics against Bacteroides fragilis.
    Drugs Exp Clin Res. 1987;13(8):489-92 PMID: 3428131
  257. New approaches to the treatment of urinary tract infection.
    Am J Med. 1987 Apr 27;82(4A):270-7 PMID: 3555047
  258. Comparative activities of five antimicrobial agents in experimental Proteus pyelonephritis in mice.
    Pharm Weekbl Sci. 1987 Dec 11;9 Suppl:S30-2 PMID: 3325927
  259. Ciprofloxacin increases serum levels of theophylline.
    Am J Med. 1987 Apr 27;82(4A):115-8 PMID: 3578320
  260. Treatment of multiresistant Salmonella typhi with oral ciprofloxacin.
    Lancet. 1987 Dec 12;2(8572):1407-8 PMID: 2891000
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    Lancet. 1986 May 10;1(8489):1103 PMID: 2871373
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    Am J Med. 1987 Apr 27;82(4A):103-7 PMID: 3578319
  264. Fluorinated quinolones. A review of their mode of action, antimicrobial activity, pharmacokinetics and clinical efficacy.
    Pharm Weekbl Sci. 1986 Feb 21;8(1):1-21 PMID: 3515312
  265. Effects of ciprofloxacin on eucaryotic pyrimidine nucleotide biosynthesis and cell growth.
    Antimicrob Agents Chemother. 1987 May;31(5):774-9 PMID: 3606077
  266. Effects of a new quinoline derivative, ciprofloxacin, on some professional phagocytic cell functions.
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  267. Pharmacokinetics of ciprofloxacin in acutely ill and convalescent elderly patients.
    Am J Med. 1987 Apr 27;82(4A):124-9 PMID: 3578321
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    Trans Ophthalmol Soc U K. 1986;105 ( Pt 6):650-2 PMID: 3477893
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  276. Emergence of ciprofloxacin-resistant Pseudomonas aeruginosa after combined therapy with ciprofloxacin and amikacin.
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    Eur J Clin Pharmacol. 1987;32(2):217-8 PMID: 3582488
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    Eur J Clin Microbiol. 1986 Apr;5(2):193-6 PMID: 2941279
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  286. Dual individualization of intravenous ciprofloxacin in patients with nosocomial lower respiratory tract infections.
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    Chemotherapy. 1987;33(3):183-8 PMID: 3109815
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    Eur J Clin Microbiol. 1986 Feb;5(1):23-8 PMID: 2938945
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  298. Effect of oral ciprofloxacin on the faecal flora of healthy volunteers.
    Eur J Clin Microbiol. 1986 Apr;5(2):201-5 PMID: 2941281
  299. Ciprofloxacin monotherapy for acute pulmonary exacerbations of cystic fibrosis.
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  300. Norfloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.
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  302. Oral ciprofloxacin therapy for chronic contiguous osteomyelitis caused by aerobic gram-negative bacilli.
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  304. Ciprofloxacin or trimethoprim-sulfamethoxazole as initial therapy for travelers' diarrhea. A placebo-controlled, randomized trial.
    Ann Intern Med. 1987 Feb;106(2):216-20 PMID: 3541724
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  306. Serum bactericidal activity of two newer quinolones against Salmonella typhi compared with standard therapeutic regimens.
    Eur J Clin Microbiol. 1986 Jun;5(3):297-302 PMID: 2943588
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    Eur J Clin Microbiol. 1986 Apr;5(2):220-5 PMID: 2941286
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Article Info
Journal
Drugs
Abbr.
Drugs
ISSN
0012-6667
DOI
10.2165/00003495-198835040-00003
Published
1988-04-00
Pages
373-447
Language
English
Region
New Zealand
NLM ID
7600076
Subset
IM
External Links
PubMed source DOI: 10.2165/00003495-198835040-00003 View journal details
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