Contents

Search

fluoroquinolone

Indications: 1) urinary tract infection* 2) prostatitis 3) uncomplicated cervicitis 4) pelvic inflammatory disease 5) lower respiratory tract infections caused by Gm- aerobes 6) Salmonella infections 7) osteomyelitis caused by Gm- aerobes 8) bacterial gastroenteritis * serious side effects generally outweigh the benefits for patients with sinusitis, bronchitis, & uncomplicated urinary tract infections [17] Contraindications: 1) pregnant women: effect on fetal development 2) children: effect on cartilage (ophthalmic agents OK) [4,6] 3) widened QRS complex may increase risk of QT prolongation Antimicrobial activity: 1) gram negative aerobic organisms 2) newer quinolones (levofloxacin, clinafloxacin ...) have better Gm+ & anaerobic activity Adverse effects: 1) generally well tolerated 2) gastrointestinal distress 3) central nervous system excitatory changes - seizures [3], hallucinations [18] 4) photosensitivity 5) arthralgias & myalgias, especially in children [4] 6) Achilles tendon rupture, especially in the elderly [5] 7) possible bone & joint injury in children [6] 8) retinal detachment [8] a) may occur within 5 days b) HR=4.5 [8]; RR=1.5 [18] - number needed to harm = 25000 [8] c) no increased risk with oral fluoroquinolones [13,20] 9) acute kidney injury (absolute risk is small) [9] - acute interstitial nephritis [24] 10) peripheral neuropathy from systemic fluoroquinolones - permanent nerve damage may occur [10,12] - oral fluoroquinolones are associated with a 1.5-2 fold increase in risk for polyneuropathy [14,29] - 1 additional case per 150,000 10-day fluoroquinolone courses [29] 11) hypoglycemia/hyperglycemia in patients with diabetes mellitus [26] 12) oral fluoroquinolones are not associated with increased risk for serious arrhythmia, compared with penicillin [15] 13) potentially permanent side effects of the tendons, muscles, joints, nerves, & central nervous system can occur together in the same patient [18] 14) 2-fold increased risk of miscarriage [19] 15) risk of aortic aneurysm or aortic dissection - no increased risk of aortic aneurysm or aortic dissection [20] - risk of aortic aneurysm or aortic dissection (RR=2-3) [27] - absolute risk of aortic aneurysm or aortic dissection 0.5 cases per 1000 patient years [25] - risk is marginal at best [30] - risk of aortic aneurysm for adults > 35 years of age is 7.5 cases per 10,000 fills vs 4.6 per 10,000 fills for comparable antibiotic [31] 16) fluoroquinolones may exacerbate myasthenia gravis [21] 17) increased risk for pseudotumor cerebri 5-fold within 15 days of oral fluoroquinolone [22] 18) increased risk of carpal tunnel syndrome (RR=1.34) [23] 19) mental health issues [26] - agitation, inattention, delirium, disorientation, memory impairment, nervousness 20) QT prolongation [1] 21) hypersensitivity: cross-reactivity among fluoroquinolones uncommon [32] Drug interactions: 1) absorption of oral forms inhibited by: a) antacids containing aluminum, magnesium or calcium b) coadministration of sucralfate c) iron or zinc-containing multivitamin/mineral formulas 2) hypoglycemia (especially gatifloxacin) in combination with sulfnonylureas & other hypoglycemic agents [2] 3) may be increased risk of Achilles tendon rupture when used in combination with glucocorticoids [5] Mechanism of action: - DNA gyrase inhibitor

Interactions

drug interactions drug adverse effects of fluoroquinolones

Specific

alatrofloxacin (Trovan IV) besifloxacin (Besivance) ciprofloxacin (Cipro, Ciloxan) clinafloxacin danofloxacin (Advocin) delafloxacin; delafloxacin meglumine (Baxdela) enoxacin (Penetrex) enrofloxacin (Baytril) finafloxacin (Xtoro) gatifloxacin (Tequin, Zymar) gemifloxacin (Factive) grepafloxacin (Raxar) levofloxacin (Levaquin) lomefloxacin (Maxaquin) marbofloxacin (Zeniquin) moxifloxacin (Avelox, Vigamox) norfloxacin (Noroxin, Chibroxin) ofloxacin (Floxin, Ocuflox, Floxin Otic) ophthalmic fluoroquinolone orbifloxacin (Orbax) pradofloxacin (Veraflox) respiratory fluoroquinolone sparfloxacin (Zagam) trovafloxacin (Trovan)

General

enzyme inhibitor quinolone antibiotic

Properties

INHIBITS: DNA gyrase

References

  1. Medical Knowledge Self Assessment Program (MKSAP) 11, 19. American College of Physicians, Philadelphia 1998, 2021
  2. Prescriber's Letter 9(11):64 2002
  3. Medications Can Cause Seizures Prescriber's Letter 10(3):16 2003 Detail-Document#: 190320 (subscription needed) http://www.prescribersletter.com
  4. Prescriber's Letter 10(7):40 2003
  5. Journal Watch 23(19):152, 2003 van der Linden PD et al, Arch Intern Med 163:1801, 2003
  6. Prescriber's Letter 11(5):29 2004 Use of Fluoroquinolone antibiotics in Children Detail-Document#: 200506 (subscription needed) http://www.prescribersletter.com
  7. Prescriber's Letter 11(9): 2004 Summary of Commonly Used Fluoroquinolones Detail-Document#: 200906 (subscription needed) http://www.prescribersletter.com
  8. Etminan M e al Oral Fluoroquinolones and the Risk of Retinal Detachment JAMA. 2012;307(13):1414-1419 PMID: 22474205 http://jama.ama-assn.org/content/307/13/1414.short
  9. Bird ST et al. Risk of acute kidney injury associated with the use of fluoroquinolones. CMAJ 2013 Jul 9; 185:E475 PMID: 23734036 http://www.cmaj.ca/content/185/10/E475?ijkey=719ce2e015f88fb295f33da8cfe395060fb60430&keytype2=tf_ipsecsha
  10. FDA MedWatch. August 15, 2013 Fluoroquinolone Antibacterial Drugs: Drug Safety Communication- Risk for possibly permanent nerve damage. http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm365302.htm
  11. Chou HW et al Risk of Severe Dysglycemia Among Diabetic Patients Receiving Levofloxacin, Ciprofloxacin, or Moxifloxacin in Taiwan. Clin Infect Dis. August 14, 2013 PMID: 23948133 http://cid.oxfordjournals.org/content/early/2013/07/23/cid.cit439.abstract
  12. Prescriber's Letter 20(10): 2013 Adverse Reactions with Systemic Quinolones Detail-Document#: 291004 (subscription needed) http://www.prescribersletter.com
  13. Pasternak B et al Association Between Oral Fluoroquinolone Use and Retinal Detachment. JAMA. 2013;310(20):2184-2190. PMID: 24281462 http://jama.jamanetwork.com/article.aspx?articleid=1785461 - Brett AS Oral Fluoroquinolone Use and Retinal Detachment Reconciling Conflicting Findings in Observational Research. JAMA. 2013;310(20):2151-2153 PMID: 24281459 http://jama.jamanetwork.com/article.aspx?articleid=1785435
  14. Etminan M et al. Oral fluoroquinolone use and risk of peripheral neuropathy: A pharmacoepidemiologic study. Neurology 2014 Aug 22 PMID: 25150290
  15. Inghammar M et al Oral fluoroquinolone use and serious arrhythmia: bi-national cohort study. BMJ 2016;352:i843 PMID: 26920666 http://www.bmj.com/content/352/bmj.i843
  16. Raguideau F et al. Association between oral fluoroquinolone use and retinal detachment. JAMA Ophthalmol 2016 Apr; 134:415 PMID: 26967005
  17. FDA Safety Watch. May 12, 2016 Fluoroquinolone Antibacterial Drugs: Drug Safety Communication - FDA Advises Restricting Use for Certain Uncomplicated Infections. http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm500665.htm - FDA Drug Safety Communication. May 12, 2016 FDA advises restricting fluoroquinolone antibiotic use for certain uncomplicated infections; warns about disabling side effects that can occur together http://www.fda.gov/Drugs/DrugSafety/ucm500143.htm
  18. FDA Safety Communication. July 26, 2016 Fluoroquinolone Antibacterial Drugs for Systemic Use: Drug Safety Communication - Warnings Updated Due to Disabling Side Effects. http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm513065.htm
  19. Muanda FT, Sheehy O, Berard A Use of antibiotics during pregnancy and risk of spontaneous abortion. CMAJ 2017 May 1;189:E625-33 PMID: 28461374 http://www.cmaj.ca/content/189/17/E625.full.pdf+html
  20. Brooks M FDA: Fluoroquinolones Not Linked to Retinal Detachment Medscape - May 11, 2017 http://www.medscape.com/viewarticle/879889 - FDA Drug Safety Communication. May 12, 2017 FDA updates warnings for oral and injectable fluoroquinolone antibiotics due to disabling side effects. https://www.fda.gov/Drugs/DrugSafety/ucm511530.htm
  21. Lowes R FDA Approves Delafloxacin (Baxdela) for Skin Infections Medscape - Jun 19, 2017. http://www.medscape.com/viewarticle/881827
  22. Sodhi M, Sheldon CA, Carleton B, Etminan M. Oral fluoroquinolones and risk of secondary pseudotumor cerebri syndrome: Nested case-control study. Neurology 2017 Jul 28 PMID: 28754842 http://www.neurology.org/content/89/8/792
  23. Cheng JZ, Sodhi M, Etminan M, Carleton BC. Fluoroquinolone Use and Risk of Carpal Tunnel Syndrome: A Pharmacoepidemiologic Study. Clin Infect Dis. 2017 Apr 24. PMID: 28444196
  24. Farid S, Mahmood M, Abu Saleh OM et al. Clinical manifestations and outcomes of fluoroquinolone- related acute interstitial nephritis. Mayo Clin Proc. 2018 Jan;93(1):25-31 PMID: 29157532 http://www.mayoclinicproceedings.org/article/S0025-6196(17)30695-X/fulltext
  25. Pasternak B et al. Fluoroquinolone use and risk of aortic aneurysm and dissection: Nationwide cohort study. BMJ 2018 Mar 8; 360:k678. PMID: 29519881 Free PMC Article - Juurlink DN. Fluoroquinolones and the aorta: Possible link with aortic pathology but the absolute risk appears very low. BMJ 2018 Mar 8; 360:k988. PMID: 29519782
  26. FDA Safety Alert. July 10, 2018 Fluoroquinolone Antibiotics: FDA Requires Labeling Changes Due to Low Blood Sugar Levels and Mental Health Side Effects. https://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm612979.htm - FDA News Release, July 10, 2018 FDA updates warnings for fluoroquinolone antibiotics on risks of mental health and low blood sugar adverse reactions. https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm612995.htm
  27. Walker M FDA Warns on Aortic Aneurysms With Fluoroquinolones. Adds to already long list of issues with popular antibiotic class. MedPage Today. Dec 20, 2018 https://www.medpagetoday.com/publichealthpolicy/fdageneral/77060 - FDA Safety Alert. Dec 20, 2018 Fluoroquinolone Antibiotics: Safety Communication - Increased Risk of Ruptures or Tears in the Aorta Blood Vessel in Certain Patients. https://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm628960.htm
  28. Lewis T, Cook J. Fluoroquinolones and tendinopathy: a guide for athletes and sports clinicians and a systematic review of the literature. J Athl Train. 2014 May-Jun;49(3):422-7. Review. PMID: 24762232 Free PMC Article
  29. Morales D, Pacurariu A, Slattery J et al. Association between peripheral neuropathy and exposure to oral fluoroquinolone or amoxicillin-clavulanate therapy. JAMA Neurol 2019 Jul; 76:827 PMID: 31034074 https://jamanetwork.com/journals/jamaneurology/fullarticle/2731583
  30. Gopalakrishnan C et al. Association of fluoroquinolones with the risk of aortic aneurysm or aortic dissection. JAMA Intern Med 2020 Sep 8; [e-pub] PMID: 32897307 https://jamanetwork.com/journals/jamainternalmedicine/fullarticle/2770379 - Dong Y-H et al. Association of infections and use of fluoroquinolones with the risk of aortic aneurysm or aortic dissection. JAMA Intern Med 2020 Sep 8; [e-pub]. PMID: 32897358 https://jamanetwork.com/journals/jamainternalmedicine/fullarticle/2770378
  31. Newton ER, Akerman AW, Strassle PD et al Association of Fluoroquinolone Use With Short-term Risk of Development of Aortic Aneurysm. JAMA Surg. Published online January 6, 2021 PMID: 33404647 https://jamanetwork.com/journals/jamasurgery/fullarticle/2774747
  32. Shah S et al. In-class cross-reactivity among hospitalized patients with hypersensitivity reactions to fluoroquinolones. Antimicrob Agents Chemother 2023 May 8; [e-pub]. PMID: 37154772 https://journals.asm.org/doi/10.1128/aac.00374-23 - Adams KK, Shah S. Health system evaluation of fluoroquinolone hypersensitivity: An assessment of cross-reactivity. J Antimicrob Chemother 2023 May 10; [e-pub] PMID: 37161664 https://academic.oup.com/jac/advance-article-abstract/doi/10.1093/jac/dkad136/7158810