Efficacy and safety of levofloxacin in the context of other contemporary fluoroquinolones: a review

Abstract

Background: In recent years, fluoroquinolone research has focused on achieving several goals, including (1) enhanced potency against gram-positive cocci, notably Streptococcus pneumoniae, and anaerobes, while (2) maintaining potency against gram-negative pathogens, (3) optimizing pharmacokinetics and pharmacodynamics (PK/PD), and (4) minimizing potential adverse drug reactions through recognition and avoidance of structural configurations that have characterized earlier, reactive compounds.Objective: This review examines the efficacy and safety of fluoroquinolones and the specific clinical evidence regarding levofloxacin.Methods: Using published literature collected over time by the author, a review was conducted, focusing on the efficacy and safety profile of levofloxacin and other fluoroquinolones.Results: The newer fluoroquinolones have fulfilled many of the research goals described above. Levofloxacin has improved anti-gram-positive potency, PK/PD properties, a proven clinical trial record (particularly for communityacquired pneumonia [CAP]), and an excellent safety profile-in the context of the treatment of Ͼ250 million patients worldwide in the past decade. It is licensed for management of drug-resistant S pneumoniae infections in the United States and has gained widespread formulary acceptance and guideline inclusion. Studies assessing levofloxacin for CAP therapy show significant advantages over standard therapy, such as trends toward reduced IV therapy and length of hospitalization, reduced mortality, and significant associated cost reduction. In addition, levofloxacin has proved highly effective in acute exacerbations of

Quinolones-Induced Musculoskeletal, Neurological, and Psychiatric ADRs: A Pharmacovigilance Study Based on Data From the Italian Spontaneous Reporting System

“…In line with our findings, Ball P reported that the most common predisposing factor for quinolones-induced ADRs is advanced age (risk increases with age after 60 years) (Ball, 2003). In this regard, one can suppose that the altered renal function, which is relatively common in older people, may affect the excretion of quinolones leading to higher risk in the occurrence of musculoskeletal, neurological, and psychiatric ADRs.…”

“…Although the exact pathologic mechanisms underlying quinolone-induced musculoskeletal ADRs are still poorly understood, it was suggested that such antibiotics might alter tendon fibroblast metabolism, leading to collagen damage (Shakibaei et al, 2000;Williams et al, 2000). These ADRs seem to be rare, affecting <1 in 5,000 patients receiving quinolones with an overall incidence of three cases per 1,000 patient years, even though some quinolones, such as pefloxacin, show an increased risk (Ball, 2003). On the other hand, the occurrence of both neurological and psychiatric ADRs may have several underlying factors, including the higher penetration of quinolones across the blood-brain barrier (such as pefloxacin that shows convulsant activity) (Kushner et al, 2001;Sarro and Sarro, 2012) and the interaction with the activity of neurotransmitters, including the displacement of GABA from its receptors GABA-A or the direct effect on excitatory brain pathways on N-methyl-D-aspartate and a-amino-3-hydroxy-5methyl-4-isoxazolepropionic acid receptors (Mehlhorn and Brown, 2007;Rubio-Nazabal et al, 2013).…”

Consumption Patterns and In Vitro Resistance of Streptococcus pneumoniae to Fluoroquinolones

“…This shows that the principal use of fluoroquinolones was for the treatment of urinary tract infections (36% of con- sumption; volume of 0.95 DIDs) and lower respiratory tract infections (26% of consumption; volume of 0.70 DIDs). This suggests that fluoroquinolones were used primarily for those indications where they have been shown to yield clinical benefit (1,2). Fluoroquinolones were used marginally for the management of upper respiratory tract infections, with a share of consumption of 2% (volume of 0.21 DIDs).…”

Treating respiratory tract infections in ambulatory care in Belgium: fluoroquinolone consumption and resistance development

“…3 shows that the principal use of fluoroquinolones was in the treatment of urinary tract infections (35% of consumption; volume of 1.06 DID) and lower respiratory tract infections (24% of consumption; volume of 0.71 DID). Management of upper respiratory tract infections with fluoroquinolones amounted to 9% of consumption (volume [12,13].…”