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level: Level 2 of Fluoroquinolones

Questions and Answers List

level questions: Level 2 of Fluoroquinolones

QuestionAnswer
Fluoroquinolones withdrawn from US:1 Grepafloxacin (Raxar) - Adverse Cardiac events 2 Sparfloxacin (Zagam) - Qt prolongation and phototoxicity 3 Trovafloxacin (Trovan) - Hepatic toxicity 4 Gatifloxacin (Tequin) - Increased risk of hypoglycemia and hyperglycemia 5 Norfloxacin (Noroxin) - Commercial reason
Toxicity Associated with Fluoroquinolones1 GI: Nausea, vomiting, diarrhea, abdominal pain 2 CNS: Dizziness, sleep disturbance, confusion, seizure 3 Liver: Hepatitis, liver failure 4 Kidney: Hematuria, Crystalluria, Nephritis, Renal failure 5 Musculoskeletal: Tendinitis, arthropathy, tendon rupture 6 Cardiovascular: Hypotension, Tachycardia, with QTc changes 7 Skin: Rash, Pruritis, Photosensitivity 8 Endocrine: Disturbance in glucose homeostasis
Frequent Side Effects: Structure Activity Relationship of Fluoroquinolones1 Complexation of metallic ions (FE, AL, MG, CA) 2 Phototoxicity 3 Drug Interactions: Inhibition of CYTP450
1 Why Fluoroquinolones cause CNS toxicity?1 because of GABA Antagonism receptor (Rare because low penetration to brain)
Fluoroquinolones with High Phototoxicity1 Fleroxacin 2 Sparfloxacin 3 Lomefloxacin 4 Bay 3118
How fluoroquinolones cause metal complexation?Cations Ca2+, Zn2+, Fe2+, Bi3+. Because of this, there is an interaction between quinolones and mineral containing drugs These complexes are water insoluble, so there are bivalent metal ions in the urine, causes crystalluria
Rare side effects of Fluoroquinolones1 Renal Toxicity (Crystalluria, Hematuria, Interstitial nephritis, acute renal failure) 2 Cardiac Toxicity (QT prolongation) 3 Hepatotoxicity ( Temafloxacin syndrome / Trovafloxacin syndrome)
Other severe toxicity 1 happened in 1992 2 happened in 19991 Temafloxacin syndrome - discoloured urine - jaundice, nausea, vomiting - abdominal pain - coagulopathy - hepatic and renal dysfunction 0.056% incident, 2 Trovafloxacin syndrome - Laboratory abnoormalities (ALT, bilirubin, encephalopaties, Necrotic inflammation) 0.0056% incidence 5 transplants 6 deaths