Top

Clinical Drug Investigation

Published in:

01-06-2006 | Original Research Article

Ciprofloxacin Bioavailability is Enhanced by Oral Co-Administration with Phenazopyridine

A Pharmacokinetic Study in a Mexican Population

Authors: Dr Gabriel Marcelín-Jiménez, Alionka P. Ángeles, Luis Martínez-Rossier, Adolfo S. Fernández

Published in: Clinical Drug Investigation | Issue 6/2006

Abstract

Background and objective: In Mexico, urinary tract infections (UTIs) constitute the second most frequent type of infections treated at primary-care clinics. Ciprofloxacin has played a major role in the treatment of UTIs because it has a broad spectrum of antibacterial activity. In addition to antimicrobial agents, phenazopyridine has been used to alleviate symptoms that occur during episodes of UTI. Thus, the present study was designed to compare the pharmacokinetic behaviour of ciprofloxacin administered alone versus ciprofloxacin combined with phenazopyridine.

Patients and methods: Twenty-four healthy male Mexican volunteers participated in this project. The study was carried out with a single oral dose of ciprofloxacin 500mg. The double-blind, crossover, randomised, balanced trial design comprised two treatments, two periods and two sequences. After administration of the study medication, serial blood samples were collected for a period of 12 hours. The harvested plasma was analysed for ciprofloxacin by high-performance liquid chromatography. The area under the concentration-time curve to last measurable concentration (AUCt), area under the concentration-time curve extrapolated to infinity (AUC_∞), peak plasma concentration (C_max), time to reach C_max (t_max), mean residence time (MRT), elimination constant (k_e) and elimination half-life (t_½) were determined from plasma concentrations of both treatments and considered as primary variables for statistical analysis.

Results: While there were no differences between the two treatments in terms of C_max and k_e, AUC_t and AUC_∞ were 35% and 29% higher, respectively, in the combined treatment arm. Moreover, a significant delay in t_max (from 1 to 1.5 hours) and a statistical increase of 29% in MRT were also observed with phenazopyridine co-administration.

Conclusion: Oral co-administration of phenazopyridine increases ciprofloxacin bioavailability with regard to the amount absorbed (AUC) and permanence in the body (MRT), which could be useful during treatment.

The use of trade names is for product identification purposes only and does not imply endorsement.

Distribución de los casos nuevos de enfermedades en los Estados Unidos Mexicanos. Directión General de Epidemiología, SSA. Anuario 2004 [online]. Available from URL: http://www.dgepi.salud.gob.mx [Accessed 2005 Jul]

Mehnert-Kay SA. Diagnosis and management of uncomplicated urinary infections. Am Fam Physician 2005; 72: 451–546PubMed

Mascellino MT, Farinelli S, Legri F, et al. Antimicrobial activity of fluoroquinolones and other antibiotics on 1,116 clinical Gram-positive and Gram-negative isolates. Drug Exp Clin Res 1998; 24: 139–51

Goldstein EJC, Citron DM, Hunt GS, et al. Comparative in vitro activities of DU-6859a, levofloxacin, ofloxacin, sparfloxacin and ciprofloxacin against 387 aerobic and anaerobic bite wound isolates. Antimicrob Agents Chemother 1997; 41: 1193–5PubMed

Grude N, Tveten Y, Jenkins A, et al. Uncomplicated urinary tract infections: bacterial findings and efficacy of empirical antibacterial treatment. Scand J Prim Health Care 2005; 2: 115–9CrossRef

Wise R, Andrews JM, Edwards LJ. In vitro activity of Bay 09867, a new quinolone derivative, compared with those of other antimicrobial agents. Antimicrob Agents Chemother 1983; 23: 559–64PubMedCrossRef

Sörgel F, Jaehde U, Naber K, et al. Pharmacokinetic disposition of quinolones in human body fluids and tissues. Clin Pharmacokinet 1989; 16Suppl. 1: 5–24PubMedCrossRef

Mandel GJ, Petri Jr WA. Sulfonamides, trimethoprim-sulfamethoxazole, quinolones and agents for urinary tract infections. In: Hardman JG, Limbird LE, editors. Goodman & Gilman’s The pharmacological basis of therapeutics, 9th edition. New York: McGraw Hill International, 1996: 1057–72

Gaines KK. Phenazopyridine hydrochloride: the use and abuse of an old standby for UTI. Urol Nurs 2004; 24: 207–9PubMed

10.

Samanidou VF, Demetriou CE, Papadoyannis IN. Direct determination of four fluoroquinolones enoxacin, norfloxacin, ofloxacin and ciprofloxacin in Pharmaceuticals and blood serum by HPLC. Anal Bioanal Chem 2003; 375: 623–9PubMed

11.

Weber A, Chaffin D, Smith A, et al. Quantitation of ciprofloxacin in body fluids by HPLC. Antimicrob Agents Chemother 1985; 27: 531–4PubMedCrossRef

12.

Morton SJ, Shull VH, Dick JD. Determination of norfloxacin and ciprofloxacin concentrations in serum and urine by HPLC. Antimicrob Agents Chemother 1986; 30: 325–7PubMedCrossRef

13.

Du Preez JL, Botha SA, Lôtter AP. HPLC determination of phenazopyridine HC1, tetracycline HC1 and sulfametizole in combination. J Chromatogr 1985; 333: 249–52PubMedCrossRef

14.

Lin CE, Deng Jr Y, Liao WS, et al. Electrophoretic behaviour and pKa determination of quinolones with a piperazinyl substituent by capillary zone electrophoresis. J Chromatogr A 2004; 1051(1–2): 283–90PubMed

15.

Gaspari R, Bosker G. Urinary tract infections: risk stratification, clinical evaluation and evidence-based antibiotic therapy. Primary Care Consensus Reports. American Health Consultants; 2003 Update

16.

Naber KG, Landen H. Rapid resolution of symptoms with ciprofloxacin therapy in 3859 hospitalized patients with urinary tract infections. Int J Antimicrob Agents 2004; 23Suppl. 1: S35–40PubMedCrossRef

Title: Ciprofloxacin Bioavailability is Enhanced by Oral Co-Administration with Phenazopyridine
A Pharmacokinetic Study in a Mexican Population
Authors: Dr Gabriel Marcelín-Jiménez
Alionka P. Ángeles
Luis Martínez-Rossier
Adolfo S. Fernández
Publication date: 01-06-2006
Publisher: Springer International Publishing
Published in: Clinical Drug Investigation / Issue 6/2006
Print ISSN: 1173-2563
Electronic ISSN: 1179-1918
DOI: https://doi.org/10.2165/00044011-200626060-00003

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Ciprofloxacin Bioavailability is Enhanced by Oral Co-Administration with Phenazopyridine

A Pharmacokinetic Study in a Mexican Population

Abstract

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

Please log in to get access to this content

Other articles of this Issue 6/2006

Impact of Influenza Treatment with Oseltamivir on Health, Sleep and Daily Activities of Otherwise Healthy Adults and Adolescents

Use of Unfractionated Heparin and a Low-Molecular-Weight Heparin following Thrombolytic Therapy for Acute ST-Segment Elevation Myocardial Infarction

Levetiracetam in Idiopathic Generalised Epilepsy and Porphyria Cutanea Tarda

Cholelithiasis and Thrombosis of the Central Retinal Vein in a Renal Transplant Recipient Treated with Cyclosporin

Long-Term Safety of Intravenous Ibandronic Acid for Up to 4 Years in Metastatic Breast Cancer

Montelukast Decreases Plasma Endothelin-1 and Serum Eosinophil Cationic Protein Levels in Paediatric Atopic Asthma