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Levofloxacin: Pharmacology, Side Effects, Contraindications and Dosage

Levofloxacin has a broad spectrum of activity against gram-negative pathogens, including Pseudomonas. It also has extended antibacterial activity against atypical (mycoplasma, chlamydia) and gram-positive pathogens (staphylococci and streptococci), but enterococci are not covered.

Mechanism of Action of Levofloxacin

Levofloxacin is a fluoroquinolone antibiotic, which interferes with the bacterial DNA synthesis via inhibition of the DNA gyrase (topoisomerase type II). Fluoroquinolone antibiotics are bactericidal.

Indications for Levofloxacin

Due to side effects, levofloxacin should only be prescribed for strict indications and without equivalent alternatives. Urological indications for fluoroquinolones are severe or complicated bacterial urinary tract infections (acute pyelonephritis, prostatitis, or epididymitis), urosepsis, or severe soft tissue infections. Due to its good effectiveness against pneumococci and atypical pathogens, levofloxacin is also used for respiratory tract infections. No indications for levofloxacin are self-limiting or mild infections (such as uncomplicated urinary tract infections), prevention of recurrent urinary tract infections, non-bacterial (chronic) prostatitis, or prophylactic perioperative use.

Pharmacokinetics of Levofloxacin

Complete bioavailability after oral administration, maximum concentration in serum within 60 min after oral administration.
Good tissue penetration
Half-life of 6–8 h, renal elimination.

Side Effects of Levofloxacin

Numerous warnings have been published regarding the side effects of levofloxacin (BfArM, EMA or FDA), as some serious side effects can lead to long-lasting and possibly irreversible patient impairment.

Gastrointestinal tract:

Nausea, vomiting, diarrhea, pseudomembranous colitis.

CNS:

Neurotoxic side effects with headache, dizziness, insomnia, psychosis to seizures, depression, fatigue, impaired memory and impaired vision, hearing, smell and taste.

Skin:

Allergic skin reactions, very rarely severe. Photosensitization.

Musculoskeletal system:

Cartilage damage, tendinitis, tendon rupture, myalgia, muscle weakness, arthralgia, and abnormal gait.

Cardiovascular system:

QT prolongation with dangerous arrhythmias, increased risk of aortic aneurysm and its rupture.

Blood:

Rare changes in blood count.

Interactions with Levofloxacin:

Interactions:

No oral administration of levofloxacin with iron preparations or antacids containing magnesium or aluminum, as otherwise absorption is prevented.
Inhibition of degradation and, thus, increase in the concentration of ciclosporin, oral anticoagulants, theophylline, methotrexate, and glibenclamide.

Contraindications to Ciprofloxacin

Pregnancy and lactation
Increased risk for seizures.
Severe chronic kidney disease
QT-prolongation
Children: cartilage damage

Dosage of Levofloxacin

Oral or intravenous dosage: 250–500 mg levofloxacin once daily, depending on the severity of the infection and sensitivity of the pathogen.
Dose reduction in patients with renal insufficiency: after the above-mentioned first dose, the daily dose is halved for the following days if the GFR is between 50–20 ml/min; if the GFR is below 20 ml/min or in dialysis patients, the further daily doses are quartered, or half the daily dose is only administered every second day.

Fluoroquinolones

Index

Ofloxacin

Index: 1–9 A B C D E F G H I J K L M N O P Q R S T U V W X Y Z

References

EMA Warning: https://www.ema.europa.eu/en/news/fluoroquinolone-antibiotics-reminder-measures-reduce-risk-long-lasting-disabling-potentially-irreversible-side-effects

FDA Warning regarding fluoroquinolone antibiotics: https://www.fda.gov/news-events/press-announcements/fda-updates-warnings-fluoroquinolone-antibiotics

Arzneikommission der deutschen Ärzteschaft “Drug Safety Mail 2019-40: Information zu Fluorchinolonen: Prophylaktische Anwendung im Zuge urologischer Eingriffe,” 2019. [Online]. Available: https://www.akdae.de/Arzneimittelsicherheit/DSM/Archiv/2019-40.html.

G. Bonkat, R. Bartoletti, F. Bruyère, S. E. Geerlings, F. Wagenlehner, and B. Wullt, “EAU Guideline: Urological Infections.” [Online]. Available: https://uroweb.org/guidelines/urological-infections/

W. Bundrick et al., “Levofloxacin versus ciprofloxacin in the treatment of chronic bacterial prostatitis: a randomized double-blind multicenter study,” Urology, vol. 62, no. 3, pp. 537–41, 2003.

Martin u.a. 1998 MARTIN, S. J. ; MEYER, J. M. ; CHUCK, S. K. ; JUNG, R. ; MESSICK, C. R. ; PENDLAND, S. L.: Levofloxacin and sparfloxacin: new quinolone antibiotics.
In: Ann Pharmacother
32 (1998), Nr. 3, S. 320–36

Deutsche Version: Nebenwirkungen, Kontraindikationen und Dosierung von Levofloxacin

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