Drug Interactions with Quinolone Antibacterials

Brouwers, Jacobus

doi:10.2165/00002018-199207040-00003

Cited by 55 publications

(15 citation statements)

References 57 publications

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“…Several quinolones have been reported to alter the phar-macokinetic profile of theophylline and induce increased steady-state theophylline concentrations to a clinically significant extent (3). In this study, patients who had chronic obstructive airway disease and who received concomitant rufloxacin and theophylline did not experience more adverse events than patients who received rufloxacin alone.…”

Section: Resultsmentioning

confidence: 65%

Double-blind, comparative study of rufloxacin once daily versus amoxicillin three times a day in treatment of outpatients with exacerbations of chronic bronchitis

Klietmann¹,

Cesana²,

Rondel³

et al. 1993

Antimicrob Agents Chemother

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In a double-blind, randomized, multicenter study, the efficacy and safety of two dosage schedules of rufloxacin once daily were compared with those of amoxicillin three times a day in the treatment of 192 outpatients with exacerbations of chronic bronchitis. Rufloxacin was given as a single oral dose of 400 mg on day 1 and single daily doses of 200 mg on the subsequent 9 days (n = 64) or as 300 mg on day 1 and then 150 mg daily for 9 days (n = 63); amoxicillin was given as 500 mg orally three times a day for 10 days (n = 65).Clinical and bacteriological assessments were carried out before treatment, between study days 3 and 5, and at days 1 and 8 after treatment. Pretreatment cultures were positive for 139 patients, the most frequently isolated pathogens being Streptococcus pneumoniae, Moraxella catarrhalis, and Haemophilus influenzae.Clinical success rates were comparable in the three groups (94, 95, and 98%, respectively), as were bacteriological success rates at the end of treatment (93, 95, and 91%, respectively) and at follow-up (88, 95, and 98%, respectively). The power to detect a significant 15% difference in cure rates was 74.9%k. Follow-up bacteriological failures from pneumococcal infection were 18% in both rufloxacin groups combined and 5% in the amoxicillin group. The 200-mg dose regimen achieved average steady-state concentrations in plasma higher than did the 150-mg dose regimen (3.75 versus 2.72 ag/ml). Adverse events occurred in 11 and 13 patients, respectively, on rufloxacin and 8 on amoxicillin. This study shows that rufloxacin once daily may be a possible option for the treatment of acute exacerbations of chronic bronchitis. The 200-mg daily oral dose preceeded by a loading dose of 400 mg displays a better pharmacokinetic profile than the lower dose.Amoxicillin, a broad-spectrum antibiotic, is currently often used to treat patients with acute exacerbations of chronic bronchitis. Amoxicillin is effective against the most common potential pathogens causing this condition and has a convenient dosage and a satisfactory degree of safety. Because of the recent increase in the number ofHaemophilus influenzae and Moraxella catarrhalis ,-lactamase-producing strains (10, 28) and of penicillin-resistant Streptococcus pneumoniae strains in the etiology of these infections (21), the new-broad spectrum fluoroquinolones may be a good alternative (30).Rufloxacin is a new fluoroquinolone antibacterial agent (4) with broad bactericidal activity (24, 31) and a long elimination half-life (35 h), which allows once-daily oral administration (15, 23). It is more active than amoxicillin against the major respiratory pathogens, H. influenzae and M. catarrhalis, and other gram-negative organisms but less active against S. pneumoniae (31). This finding has been observed with other quinolones (7).Rufloxacin concentrates for a long time in respiratory sites, reaching respective concentrations in the epithelial lining fluid of the distal airways and in alveolar macrophages of 10 and 20 times those in serum, with levels l...

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Section: Resultsmentioning

confidence: 65%

Double-blind, comparative study of rufloxacin once daily versus amoxicillin three times a day in treatment of outpatients with exacerbations of chronic bronchitis

Klietmann¹,

Cesana²,

Rondel³

et al. 1993

Antimicrob Agents Chemother

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“…13,14 Many interactions between ciprofloxacin and other drugs, metabolised by hepatic cytochrome P450 isoenzymes, have been identified. [15][16][17]20,21,32 Thus, it has been established that ciprofloxacin is an inhibitor of cytochrome P450 3A2 activity in vitro and in vivo. [16][17][18][19][20] Since CYP3A2 is involved in both pathways, that is, activation and deactivation of CY, a decreased clearance and subsequently a decreased metabolic ratio (AUC 4ÀOHÀCY /AUC CY ) caused by ciprofloxacin would be expected.…”

Section: Discussionmentioning

confidence: 99%

“…Particularly, interactions between ciprofloxacin and drugs metabolised by the hepatic cytochrome P450 (CYP) system have attracted attention. 15 Studies with hepatic microsomes demonstrated that ciprofloxacin can decrease CYP3A-mediated biotransformation in man and rat by competitive inhibition. 16 Pharmacokinetic interaction between cyclosporine and ciprofloxacin has been established in vivo and in vitro.…”

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confidence: 99%

Alteration of pharmacokinetics of cyclophosphamide and suppression of the cytochrome P450 genes by ciprofloxacin

Xie

Griškevičius

Broberg

et al. 2003

Bone Marrow Transplant

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Summary:Recently, it has been reported that prophylactic administration of ciprofloxacin during cyclophosphamide (CY) conditioning was a high-risk factor for relapse in patients undergoing allogeneic BMT. In the present study, we investigated the possible mechanisms of this interaction in male Sprague-Dawley rats. The kinetics of CY and its active 4-OH-CY metabolite were determined, after 3 days pretreatment with ciprofloxacin (200 mg/kg) and compared to control rats without treatment. CY was administered as a high or low single intravenous dose (150 and 90 mg/kg, respectively). The expression of the CYP2B1, CYP2B2, CYP2C11, CYP3A1 and CYP3A2 genes was evaluated by SYBR Green I Dye real-time PCR for quantification of mRNA. The administration of ciprofloxacin resulted in a significant increase in the AUC (P ¼ 0.007) and a significant decrease in clearance (P ¼ 0.007) when CY was given as a high dose. In accordance, the metabolic ratio (AUC4-OH-CY/ AUCCY) was significantly lower (P ¼ 0.007) compared to that found in the control group. Ciprofloxacin significantly suppressed gene expression of CYP2C11 (P ¼ 0.01) and CYP3A1 (P ¼ 0.04); however, no effect was observed on the gene expression of CYP3A2, CYP2B1 and CYP2B2. Our study revealed that ciprofloxacin interacts with CY and suppressed relevant cytochromes P450 at the transcriptional level. This study may have a great clinical impact when ciprofloxacin is used in therapy. Bone Marrow Transplantation (2003Transplantation ( ) 31, 197-203. doi:10.1038 Keywords: cyclophosphamide; ciprofloxacin; interaction; cytochrome P450; gene expression; bone marrow transplantation Cyclophosphamide (CY) is a prodrug, which requires hepatic biotransformation to exert its cytotoxic effect. 1 An alternative but minor pathway is the inactivation of CY and both pathways are dependent on cytochrome P450 enzymes. [2][3][4][5] In humans, CYP2B6 is the main catalyst of CY activation, along with the contribution from CYP2C, CYP3A4, and CYP2A6 isoenzymes. 5-7 CY inactivation is mostly catalysed by CYP3A4. 5 In noninduced male rats, the constitutively expressed CYP2C11 and CYP3A2 are the major enzymes involved in CY bioactivation, while the inducible CYP2B1 was shown to be a major catalyst of CY activation in induced rats. 2,4 Thus, in vivo or in vitro alteration of hepatic CYPs could change the rate and pattern of CY metabolism. 8 Concomitant use of CY with other drugs that are inhibitors or inducers of CYP2B, CYP2C, or CYP3A enzymes could cause interactions. [9][10][11][12] Ciprofloxacin is a DNA gyrase inhibitor used as an antibacterial drug. 13 This fluoroquinolone agent has gained widespread use in the treatment of a broad range of infections. 14 Investigations focused on drug interactions between ciprofloxacin and other drugs have been reported in recent years. Particularly, interactions between ciprofloxacin and drugs metabolised by the hepatic cytochrome P450 (CYP) system have attracted attention. 15 Studies with hepatic microsomes demonstrated that ciprofloxacin can decrease CYP3A-me...

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“…Usually fluoroquinolones are prescribed for many diseases including respiratory and urinary tract infections. Historical background reveals that parallel administration of NSAIDs and new quinolones (NQ) can induce a synergistic interaction that results in convulsions and NQinduced neurotoxic effect synergistically increased in the presence of NSAIDs [29][30][31]. For the same purpose, to determine the effect of simultaneous administration of sparfloxacin (quinolones) and NSAIDs, a new RP-HPLC method has been developed which is simple, fast, cheap and easy to perform.…”

Section: Introductionmentioning

confidence: 99%

New Method for Optimization and Simultaneous Determination of Sparfloxacin and Non Steroidal Anti-Inflammatory Drugs: Its <i>In-Vitro</i> Application

Gul¹,

Sultana²,

Arayne³

et al. 2012

AJAC

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A simple reversed phase HPLC method was developed and validated for the simultaneous determination of sparfloxacin (SPFX), diclofenac sodium, meloxicam, ibuprofen, flurbiprofen, naproxen and mefenemic acid in a relatively short time with high linearity in bulk material, pharmaceutical formulations and human serum. Purospher STAR C 18 (250 × 4.6 mm, 5 μm) column was utilized with mobile phase, methanol and water (90:10, v/v pH 2.70 adjusted by phosphoric acid), was delivered at a flow rate of 1.5 mL·min -1 . Eluent was monitored using UV detector at 240 nm. The proposed method is specific, accurate (98.42% -102.75%), precise (intra-day and inter-day variation 0.011% -1.85%) and linear (R 2 > 0.999) with in the desired range 0.15 -40 µg·mL -1 and the detection and quantification limit was 1.19E+08 -0.150 µg·mL -1 and 3.62E+08 -0.4574 µg·mL -1 respectively for SPFX and NSAIDs. The analysis of variance (ANOVA) and student's t-test were applied to verify the results. The anticipated method is applicable to routine analysis of SPFX and NSAIDs in pharmaceutical formulations as well as in human serum samples. It has also applied on interaction of SPFX with NSAIDs.

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Drug Interactions with Quinolone Antibacterials

Cited by 55 publications

References 57 publications

Double-blind, comparative study of rufloxacin once daily versus amoxicillin three times a day in treatment of outpatients with exacerbations of chronic bronchitis

Double-blind, comparative study of rufloxacin once daily versus amoxicillin three times a day in treatment of outpatients with exacerbations of chronic bronchitis

Alteration of pharmacokinetics of cyclophosphamide and suppression of the cytochrome P450 genes by ciprofloxacin

New Method for Optimization and Simultaneous Determination of Sparfloxacin and Non Steroidal Anti-Inflammatory Drugs: Its <i>In-Vitro</i> Application

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Drug Interactions with Quinolone Antibacterials

Cited by 55 publications

References 57 publications

Double-blind, comparative study of rufloxacin once daily versus amoxicillin three times a day in treatment of outpatients with exacerbations of chronic bronchitis

Double-blind, comparative study of rufloxacin once daily versus amoxicillin three times a day in treatment of outpatients with exacerbations of chronic bronchitis

Alteration of pharmacokinetics of cyclophosphamide and suppression of the cytochrome P450 genes by ciprofloxacin

New Method for Optimization and Simultaneous Determination of Sparfloxacin and Non Steroidal Anti-Inflammatory Drugs: Its &lt;i&gt;In-Vitro&lt;/i&gt; Application

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New Method for Optimization and Simultaneous Determination of Sparfloxacin and Non Steroidal Anti-Inflammatory Drugs: Its <i>In-Vitro</i> Application