Efetividade e segurança do regime de tratamento contendo gemifloxacino no tratamento de primeira linha para Helicobacter pylori / Efficacy and safety of gemifloxacin containing treatment regimen in first-line treatment of helicobacter pylori

ABSTRACT Background: After eradication of Helicobacter pylori (H. pylori) chronic gastritis will resolve, complications due to H. pylori infection and recurrence of infection will be prevented. Objective: To determine efficacy and safety of gemifloxacin containing treatment regimen in first line treatment of H. pylori with comparison to bismuth containing quadruple therapy. Methods: This retrospective study was conducted in a tertiary care university hospital between January 2018 and January 2021 with 410 participants who were diagnosed to have H. pylori infection with biopsies obtained during upper gastrointestinal system endoscopy. Patients were distributed into two groups according to their first-line treatment regimens. First group patients were treated with amoxicillin, gemifloxacin and pantoprazole and second group patients were treated with amoxicillin, metronidazole, bismuth subcitrate and pantoprazole for seven days. Results: Intention to treat and per protocol ratios for gemifloxacin containing regimen were 90.0% and 91.2%, while quadruple treatment has these ratios as 91.7% and 93.8% respectively. Treatment success rate in both regimens were similar. But adverse effects were lower and patient compliance were better in patients who had gemifloxacin containing treatment (P<0.001). Conclusion: Gemifloxacin containing treatment regimen is as effective as bismuth containing quadruple treatment regimen for H. pylori infection and patient compliance is better in this group. Gemifloxacin containing treatment regimens may be novel and effective alternatives for eradication of H. pylori infection.

RESUMO Contexto: Após a erradicação do Helicobacter pylori (HP), a gastrite crônica será resolvida, as complicações devido à infecção por HP e a recorrência da infecção serão prevenidas. Objetivo: Determinar a eficácia e segurança do regime de tratamento contendo gemifloxacino no tratamento de primeira linha do HP, em comparação com a terapia quádrupla contendo bismuto. Métodos: Este estudo prospectivo foi conduzido em um hospital universitário de atendimento terciário entre janeiro de 2018 e janeiro de 2021, com 410 participantes diagnosticados com infecção por HP, obtidos por meio de biópsias durante a endoscopia do sistema gastrointestinal superior. Os pacientes foram divididos em dois grupos de acordo com seus regimes de tratamento de primeira linha. Os pacientes do primeiro grupo foram tratados com amoxicilina, gemifloxacino e pantoprazol, e os pacientes do segundo grupo foram tratados com amoxicilina, metronidazol, subcitrato de bismuto e pantoprazol por 7 dias. Resultados: As taxas de intenção de tratar e por protocolo para o regime contendo gemifloxacino foram de 90,0% e 91,2%, enquanto o tratamento quádruplo apresentou essas taxas como 91,7% e 93,8%, respectivamente. A taxa de sucesso do tratamento em ambos os regimes foi similar. No entanto, os efeitos adversos foram menores e a adesão dos pacientes foi melhor nos que receberam o tratamento contendo gemifloxacino (P<0,001). Conclusão: O regime de tratamento contendo gemifloxacino é tão eficaz quanto o regime de tratamento quádruplo contendo bismuto para a infecção por HP, e a adesão dos pacientes é melhor neste grupo. Os regimes de tratamento contendo gemifloxacino podem ser alternativas novas e eficazes para a erradicação da infecção por HP.

Determination of Gemifloxacin in human plasma by high performance liquid chromatography using Ultra Violet detector and its application to a bioequivalence study

A liquid chromatography method was developed and validated for the determination of gemifloxacin in human plasma using chloramphenicol as internal standard to achieve lower quantification limit. Acetonitrile was used to precipitated and extracted analyte and internal standard from plasma by Protein Precipitation. Analysis was performed isocratically on C18 column using 25% acetonitrile and 75% 0.02 M phosphate buffer as mobile phase. The method was demonstrated to be linear from 0.003 µg/mL to 5 µg/mL with the lower limit of quantitation of 0.003 µg/mL. The method was successfully applied for the bioequivalence study of gemifloxacin after a single oral administration of 320 mg gemifloxacin mesylate tablets to 12 healthy volunteers.

Clinical Efficacy of Gemifloxacin-containing Triple Therapy for First-line Treatment of Helicobacter pylori Infection: A Pilot Study

BACKGROUND/AIMS: Levofloxacin resistance is increasing rapidly, and widely limits its application in Helicobacter pylori eradication. This study aimed to evaluate the efficacy of a clarithromycin- versus gemifloxacin-containing triple therapy regimen in first-line eradication of H. pylori infection. MATERIALS AND METHODS: This was an open-label, prospective, non-randomized two-armed pilot study in which treatment-naïve subjects with active H. pylori infection received a seven-day triple therapy with rabeprazole 20 mg bid (twice daily), gemifloxacin 320 mg qd (once daily), and amoxicillin 500 mg bid (n=70) or seven-day triple therapy with rabeprazole 20 mg bid (twice daily), clarithromycin 500 mg bid (twice daily), and amoxicillin 500 mg bid (n=83). H. pylori infection status was checked in all patients at enrollment and at least 8 weeks after the end of therapy by the urea breath test. RESULTS: Intention-to-treat eradication rates were 71.1% and 74.3% for clarithromycin-containing triple therapy and gemifloxacin- containing triple therapy, respectively (P=0.398). The corresponding per-protocol eradication rates were 76.6% and 76.1% (P=0.624). The gemifloxacin-containing triple therapy was associated with a lower incidence of adverse events (2.9% vs. 18.5%, P=0.003). CONCLUSIONS: Although the seven-day gemifloxacin-containing triple therapy regimen showed a more favorable safety profile, there was no significant difference in eradication rates between the gemifloxacin-containing and clarithromycin-containing triple regimens, and both regimens had eradication rates slightly lower than acceptable efficacy for the Korean population. Therefore, the gemifloxacin-containing regimen might be useful as an alternative regimen for patients showing severe side effects of clarithromycin due to poor tolerance. Further studies on the efficacy of gemifloxacin in the Korean population are warranted.

HPTLC Methods for Determination of Gemifloxacin Mesylate in Rabbit Plasma.

Aim: A new, simple, rapid, very sensitive and accurate high performance thin-layer chromatographic (HPTLC) method has been developed and validated for estimation of Gemifloxacin in rabbit plasma. Study Design: Validation study. Methodology: HPTLC was performed on silica gel 60F254 plates with ethanol: ethyl acetate: hexane, 2:7:1 (v/v), as mobile phase. Densitometry scanning was performed in absorbance mode at λ=254 nm. Result: The RF value was 0.21. The response was a linear function of concentration over the range 0.1–0.7μg mL−1 (r2=0.996). A maximum recovery of drug from plasma was obtained by using chloroform and glacial acetic acid. Mean extraction recovery was 80%. Intra-day and inter-day precision (% RSD) of the assay were in the range 1.19–2.85% and accuracy was 1.7-5.66% Conclusion: This method can be applied to pharmacokinetic studies in rabbit plasma.

Biphasic anaphylaxis to gemifloxacin

Anaphylaxis have been documented as adverse effects of ciprofloxacin, ofloxacin, norfloxacin, levofloxacin, and moxifloxacin. However resistant and biphasic anaphlylactic reactions to gemifloxacin have not been reported to date. Management of severe anaphylaxis in the elderly can be complicated by concurrent medications such as beta (β) adrenergic, alpha (α) adrenergic blockers and angiotensin-converting enzyme (ACE) inhibitors. We report here in the case of a 60-year-old male who was taking on ACE inhibitor, α and β blockers and experienced a severe, resistant and biphasic anaphlylactic reaction to gemifloxacin mesylate.

A probable association of acute dystonia with gemifloxacin administration.

Gemifloxacin is a recently introduced fluoroquinolone antibiotic frequently used for its broad spectrum and once-daily dosing. Fluoroquinolones are associated with various neuropsychiatric side effects, such as seizures, insomnia, confusion, lightheadedness, psychosis, paranoia and hallucinations. We report a case of a 36-year-old woman given gemifloxacin for an upper respiratory tract infection who developed acute dystonia on the third day following therapy initiation. The clinical implications are discussed.

A Randomized, Double-Blind Study to Assess the Efficacy and Safety of Oral LB20304 (Gemifloxacin) at Doses of 160mg or 320mg (Equivalent to 200mg or 400mg of the Mesylate Salt) Once Daily for 7 Days for the Treatment of Acute Exacerbations of Chronic Bron / 결핵

BACKGROUND: LB20304(gemifloxacin) is a new fluoroquinolone antibacterial agent with excellent activity against both Gram-negative and Gram-positive organisms. In vitro studies using clinical isolates have shown gemifloxacin to be highly active against penicillin-resistant strains of S. pneumoniae and in contrast to other reference quinolones, gemifloxacin retained good activity against clinical isolates of S. pneumoniae that were resistant to other members of the quinolone class. Therefore, gemifloxacin is thought to be effective in treating acute bacterial exacerbation of chronic bronchitis(AECB). The objective of this study was to evaluate the efficacy and safety of oral gemifloxacin at doses of 160mg or 320mg once daily for 7 days for the treatment of AECB in Korean adult population. METHODS: This was a randomized, multicenter, double-blind, parallel group Phase II study to assess the clinical and antibacterial efficacy and safety of oral gemifloxacin for the treatment of AECB. Treatment Group A (67 patients) took oral gemifloxacin 160mg once daily for seven days and treatment Group B (70 patients) took oral gemifloxacin 320mg once daily for seven days. RESULTS: The demographic profiles of the two treatment groups were similar. The clinical response at follow-up was 84.2% in the gemifloxacin 160-mg group, and 88.7% in the gemifloxacin-320 mg group, showing no statistically significant difference between two treatment groups(p=0.49). The clinical response at the end of therapy was 96.5% in the 160-mg group, and 96.4% in the 320-mg group. The bacteriological response at the end of therapy and follow-up were 81.8% and 78.9%, respectively, in the 160-mg group, and 86.4% and 84.2%, respectively, in the 320-mg group, showing no statistically significant difference between two treatment groups(p=0.68 and 0.68, respectively). S. pneumoniae(12 isolates) and H. influenzae(10 isolates) were the most prevalent pathogens. The MICs were lower for gemifloxacin than other quinolones against these key pathogens, and for S. pneumoniae, the MICs for gemifloxacin were considerably lower(< or = 0.03 ug/mL) than those for other quinolones, beta-lactams and acrolides. In the period on-therapy plus 30 days post-therapy, a total of 18 patients(26.9%) in the gemifloxacin 160mg group and 22 patients(31.4%) in the 320mg group reported at least one adverse event(AE). The most frequently reported AE was abdominal pain(3/67 patients, 4.5%) in the gemifloxacin 160mg group and increased level of hepatic enzyme(5/70 patients, 7.1%) in the 320mg group. The overall AE profiles for the two treatment groups were similar. Two out of 67 patients(3.0%) in the gemifloxacin 160mg group and 1/70 patients(1.4%) in the 320mg group reported at least one serious AE, however, none of which was considered by the investigator to be of suspected or probable relationship to study medication. CONCLUSION: The results of this study showed that gemifloxacin at doses of 160mg or 320mg once daily for 7 days in the treatment of acute exacerbations of chronic bronchitis(AECB) in adult Koreans was a very effective and safe treatment both clinically and bacteriologically.

In vitro Activity of Gemifloxacin Against Recent Clinical Isolates of Bacteria in Korea

Gemifloxacin is an enhanced-affinity fluoroquinolone with broad-spectrum antibacterial activity. In Korea, resistant bacteria are relatively more prevalent than in other industrialized countries. In this study, we studied the in vitro activities of gemifloxacin, gatifloxacin, moxifloxacin, levofloxacin, ciprofloxacin, and other commonly used antimicrobial agents against 1,689 bacterial strains isolated at four Korean university hospitals during 1999-2000. Minimum inhibitory concentrations (MICs) were determined using the agar dilution method of National Committee for Clinical Laboratory Standards. Gemifloxacin had the lowest MICs for the respiratory pathogens: 90% of Streptococcus pneumoniae, Moraxella catarrhalis, and Haemophilus influenzae were inhibited by 0.06, 0.03, and 0.03 mg/L, respectively. Gemifloxacin was more active than the other fluoroquinolones against methicillin-susceptible Staphylococcus aureus, coagulase-negative staphylococci, streptococci, and Enterococcus faecalis. The MIC90s of gemifloxacin for Klebsiella oxytoca, Proteus vulgaris, and nontyphoidal Salmonella spp. were 0.25, 1.0, and 0.12 mg/L, respectively, while those for other Gram-negative bacilli were 4-64 mg/L. In conclusion, gemifloxacin was the most active among the comparative agents against Gram-positive species, including respiratory pathogens isolated in Korea.