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Pharmacology, Side Effects, Contraindications and Dosage

Ofloxacin has a broad spectrum of activity against Gram-negative pathogens, including Pseudomonas. There is also some antibacterial activity against atypical bacteria and Gram-positive pathogens, but streptococci and enterococci are not covered.

Mechanism of Action of Ofloxacin

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

Indications for Ofloxacin

Due to side effects, Ofloxacin 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, treatment of gonorrhea (with proven sensitivity), or severe soft tissue infections. No indications for fluoroquinolones 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 Ofloxacin

Good bioavailability after oral administration, maximum concentration in serum within 60 min after oral administration.
Good tissue penetration
Half-life of 6–7 h, renal elimination to 80–90%.

Side Effects of Ofloxacin

Numerous warnings have been published regarding the side effects of Ofloxacin (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 Ofloxacin:

No oral administration of Ofloxacin 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 Ofloxacin

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

Dosage of Ofloxacin

Normal dosage of ofloxacin is 100–200 mg 1-0-1 p.o., depending on the severity of the infection and sensitivity of the pathogen. Ofloxacin is no longer available as an intravenous formulation in Europe and the USA. Treatment of uncomplicated gonorrhea with a single dose 400 mg p.o.

Dose reduction in renal insufficiency: With a GFR between 50–20 ml/min, the dosing interval is 24 hours. With a GFR below 20 ml/min or in dialysis patients, the dosing interval is 48 hours, and the serum concentration should be monitored.

Levofloxacin

Index

Urological Pharmacology

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

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/

Raz u.a. 2000 RAZ, R. ; NABER, K. G. ; RAIZENBERG, C. ; ROHANA, Y. ; UNAMBA-OPARAH, I. ; KORFMAN, G. ; YANIV, I.: Ciprofloxacin 250 mg twice daily versus ofloxacin 200 mg twice daily in the treatment of complicated urinary tract infections in women.
In: Eur J Clin Microbiol Infect Dis
19 (2000), Nr. 5, S. 327–31

Reid u.a. 2000 REID, G. ; POTTER, P. ; DELANEY, G. ; HSIEH, J. ; NICOSIA, S. ; HAYES, K.: Ofloxacin for the treatment of urinary tract infections and biofilms in spinal cord injury.
In: Int J Antimicrob Agents
13 (2000), Nr. 4, S. 305–7

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

Deutsche Version: Nebenwirkungen, Kontraindikationen und Dosierung von Ofloxacin