| Fluoroquinolones withdrawn from US: | 1 Grepafloxacin (Raxar) - Adverse Cardiac events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 Fluoroquinolones | 1 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 Fluoroquinolones | 1 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 Phototoxicity | 1 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 Fluoroquinolones | 1 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 1999 | 1 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 |
