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Ciprofloxacin: Pharmacology, Side Effects, Contraindications and Dosage

Ciprofloxacin 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 Ciprofloxacin

Ciprofloxacin is bactericidal; it interferes with the bacterial DNA synthesis via inhibition of the DNA gyrase (topoisomerase type II).

Indications for Ciprofloxacin

Due to side effects, ciprofloxacin 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 Ciprofloxacin

Good bioavailability after oral administration, maximum concentration in serum after 60–90 min of oral administration.
Good tissue penetration
Half-life of 3–5 h, renal elimination.

Side Effects of Ciprofloxacin

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

Interactions:

No oral administration of ciprofloxacin 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 Ciprofloxacin

Oral dosage: 250–500 mg p.o. 1-0-1
Intravenous dosage: 200–400 mg i.v. 1-0-1
Dosage depends on the severity of the infection and sensitivity of the pathogen. Reduce the dosage below a GFR of 30 ml/min (one dose per day).

Fluoroquinolones

Index

Levofloxacin

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

Auquer u.a. 2002 AUQUER, F. ; CORDON, F. ; GORINA, E. ; CABALLERO, J. C. ; ADALID, C. ; BATLLE, J.: Single-dose ciprofloxacin versus 3 days of norfloxacin in uncomplicated urinary tract infections in women.
In: Clin Microbiol Infect
8 (2002), Nr. 1, S. 50–4

Henry u.a. 2002 HENRY, Jr. ; BETTIS, R. B. ; RIFFER, E. ; HAVERSTOCK, D. C. ; KOWALSKY, S. F. ; MANNING, K. ; HAMED, K. A. ; CHURCH, D. A.: Comparison of once-daily extended-release ciprofloxacin and conventional twice-daily ciprofloxacin for the treatment of uncomplicated urinary tract infection in women.
In: Clin Ther
24 (2002), Nr. 12, S. 2088–104

Krcmery und Naber 1999 KRCMERY, S. ; NABER, K. G.: Ciprofloxacin once versus twice daily in the treatment of complicated urinary tract infections. German Ciprofloxacin UTI Study Group.
In: Int J Antimicrob Agents
11 (1999), Nr. 2, S. 133–8

Mombelli u.a. 1999 MOMBELLI, G. ; PEZZOLI, R. ; PINOJA-LUTZ, G. ; MONOTTI, R. ; MARONE, C. ; FRANCIOLLI, M.: Oral vs. intravenous ciprofloxacin in the initial empirical management of severe pyelonephritis or complicated urinary tract infections: a prospective randomized clinical trial.
In: Arch Intern Med
159 (1999), Nr. 1, S. 53–8

Naber u.a. 1999 NABER, K. G. ; THEURETZBACHER, U. ; MONEVA-KOUCHEVA, G. ; STASS, H.: Urinary excretion and bactericidal activity of intravenous ciprofloxacin compared with oral ciprofloxacin.
In: Eur J Clin Microbiol Infect Dis
18 (1999), Nr. 11, S. 783–9

Talan u.a. 2004 TALAN, D. A. ; KLIMBERG, I. W. ; NICOLLE, L. E. ; SONG, J. ; KOWALSKY, S. F. ; CHURCH, D. A.: Once daily, extended release ciprofloxacin for complicated urinary tract infections and acute uncomplicated pyelonephritis.
In: J Urol
171 (2004), Nr. 2 Pt 1, S. 734–9

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

Deutsche Version: Nebenwirkungen, Kontraindikationen und Dosierung von Ciprofloxacin