Agent | Bioavailability | Clearance | Metabolism | Inhibition or induction of metabolism | Elimination half-life | Notes |
Ciprofloxacin | 70% (range 50 to 85%). Avoid taking with most antacids, mineral supplements, and certain oral medications: Decreased bioavailability in some cases by >90%.* May be taken with most foods or on an empty stomach. However, avoid taking with milk or dairy products: Decreased bioavailability up to 40%.[1] | Oral administration:
IV administration:
| Hepatic metabolism is poorly characterized; some metabolites are active. | Inhibitor of CYP1A2. Can increase blood levels of CYP1A2 substrate drugs (eg, clozapine, erlotinib, ibrutinib, ropinirole, theophylline, tizanidine); refer to drug interactions program included within UpToDate for detail. | 3 to 5 hours. Prolonged in older adults and in renal impairment (up to 8 hours in advanced chronic kidney disease). | Some drug interactions require dose adjustment or avoidance of certain combinations; refer to drug interactions program included within UpToDate for detail. |
Delafloxacin | 59%. Avoid taking with most antacids, mineral supplements, and certain oral medications: Decreased bioavailability in some cases by >90%.* May be taken with or without food. | Oral administration:
IV administration:
| Does not undergo CYP450 metabolism. Minimally metabolized via glucuronidation. | Does not inhibit or induce hepatic CYP450 enzymes to a clinically relevant extent. | IV: 3.7 hours; oral: 4.2 to 8.5 hours. Prolonged in renal impairment. | IV formulation contains cyclodextrin vehicle, which accumulates in renal impairment. IV form is not recommended in patients with eGFR of <15 mL/minute/1.73 m2. |
GemifloxacinΔ (oral only) | 71%. Avoid taking with most antacids, mineral supplements, and certain oral medications: Decreased bioavailability in some cases by >90%.* May be taken with or without food. | Oral administration:
| Does not undergo CYP450 metabolism. Metabolized via glucuronidation. | Does not inhibit or induce hepatic CYP450 enzymes. | 7 hours (range 4 to 12 hours). Prolonged in renal impairment. | |
Levofloxacin | 99%. Avoid taking with most antacids, mineral supplements, and certain oral medications: Decreased bioavailability in some cases by >90%.* May be taken with or without food. | Oral/IV administration:
| Does not undergo CYP450 metabolism. Minimally metabolized via glucuronidation. | Does not inhibit or induce hepatic CYP450 enzymes. | 6 to 8 hours. Prolonged up to 35 hours in advanced chronic kidney disease. | |
Moxifloxacin | 90%. Avoid taking with most antacids, mineral supplements, and certain oral medications: Decreased bioavailability in some cases by >90%.* May be taken with or without food. | Oral/IV administration:
| Does not undergo CYP450 metabolism. Metabolized via glucuronidation and sulfate conjugation. | Does not inhibit or induce hepatic CYP450 enzymes. | 10 to 14 hours. | |
NorfloxacinΔ (oral only) | 30 to 40%. Avoid taking with most antacids, mineral supplements, and certain oral medications: Decreased bioavailability in some cases by >90%.* May be taken with most foods or on an empty stomach, but food may delay absorption. However, avoid taking with milk or dairy products: decreased bioavailability up to 40%.[2] | Oral administration:
| Undergoes modest hepatic metabolism; however, its metabolism has not been well characterized. | Can increase blood levels of theophylline.[3] May alter cyclosporine levels; monitoring suggested.[4] Refer to drug interactions program included within UpToDate for detail. | 3 to 4 hours. Prolonged up to 6.5 hours in advanced chronic kidney disease. | Some drug interactions require dose adjustment or avoidance of certain combinations; refer to drug interactions program included within UpToDate for detail. |
Ofloxacin | >90%. Avoid taking with most antacids, mineral supplements, and certain oral medications: Decreased bioavailability in some cases by >90%.* May be taken with or without food. | Oral/IV administration:
| Does not undergo CYP450 metabolism. Metabolized via glucuronidation. | Does not inhibit or induce hepatic CYP450 enzymes. | 5 to 7.5 hours. Prolonged in renal impairment. |
CYP450: cytochrome P450 hepatic metabolism; eGFR: estimated glomerular filtration rate; INR: international normalized ratio; IV: intravenous.
* Fluoroquinolones form chelation complexes with medications containing multivalent cations that can significantly impair absorption resulting in subtherapeutic serum concentrations and treatment failure. Examples include but are not limited to: Aluminum, magnesium, and calcium-containing antacids, mineral supplements (calcium, iron, magnesium, zinc), phosphate binders (eg, sevelamer, lanthanum), sodium polystyrene sulfonate, sucralfate, and buffered didanosine. Administering oral fluoroquinolones at least 2 to 4 hours before or 3 to 8 hours after these medications or supplements may minimize but not eliminate these interactions. Enteral nutrition formulas may also impair absorption of fluoroquinolones depending upon tube terminus placement and timing of administration. H2 receptor antagonists and proton pump inhibitors do not appear to significantly alter absorption of fluoroquinolones.[1]
¶ Requires dose adjustment in renal impairment.
Δ Not available in the United States; in most countries where it is available, only an oral formulation is marketed.Data from:
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