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Pharmacokinetics and drug interactions of systemic fluoroquinolones in adults

Pharmacokinetics and drug interactions of systemic fluoroquinolones in adults
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:
  • 30 to 50% renally cleared
  • 15% metabolized
  • 30% presystemic clearance (hepatobiliary and fecal)
IV administration:
  • 70% renally cleared
  • 10% metabolized
 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 Lexicomp drug interactions program 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 Lexicomp drug interactions program 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:
  • 50% renally cleared
  • 1% metabolized
  • 48% fecal clearance
IV administration:
  • 65% renally cleared
  • 1% metabolized
  • 28% fecal clearance
 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:
  • 36% renally cleared
  • <10% metabolized
  • 61% fecal clearance
 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:
  • 87% renally cleared
  • <1% metabolized
  • <4% fecal clearance
 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:
  • 20% renally cleared
  • 52% metabolized
  • 25% fecal clearance
 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:
  • 30% renally cleared
  • 5 to 8% metabolized
  • 30% fecal clearance
 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 Lexicomp drug interactions program 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 Lexicomp drug interactions program 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:
  • 80% renally cleared
  • 4% metabolized
  • 4 to 8% fecal clearance
 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.		  
  • Data on clearance and metabolism are provided to assess potential for pharmacokinetic drug interactions and risk of drug accumulation in organ failure. This table does not address potential pharmacodynamic interactions of fluoroquinolones with other drugs (eg, additive QTc prolongation). Refer to Lexicomp drug interactions program included with UpToDate for specific drug interactions.
  • Patients receiving warfarin should have INR monitored when treated with a fluoroquinolone; an increased risk of bleeding has been observed.[5]

IV: intravenous; CYP450: cytochrome P450 hepatic metabolism; eGFR: estimated glomerular filtration rate; INR: international normalized ratio.

* 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.
References:
  1. Bolhuis MS, Panday PN, Pranger AD, et al. Pharmacokinetic drug interactions of antimicrobial drugs: A systematic review on oxazolidinones, rifamycines, macrolides, fluoroquinolones, and beta-lactams. Pharmaceutics 2011; 3:865.
  2. Kivisto KT, Ojala-Karlsson P, Neuvonen PJ. Inhibition of norfloxacin absorption by dairy products. Antimicrob Agents Chemother 1992; 36:489.
  3. Tierney MG, Ho G, Dales RE. Effect of norfloxacin on theophylline pharmacokinetics. Clin Pharmacol Ther 1988; 43:156.
  4. McLellan RA, Drobitch RK, McLellan H, et al. Norfloxacin interferes with cyclosporine disposition in pediatric patients undergoing renal transplantation. Clin Pharmacol Ther 1995; 58:322.
  5. Baillargeon J, Holmes HM, Lin YL, et al. Concurrent use of warfarin and antibiotics and the risk of bleeding in older adults. Am J Med 2012; 125:183.

Data from:

  1. US Food & Drug Administration prescribing information. Available at: https://www.accessdata.fda.gov/scripts/cder/daf/ (Accessed on October 19, 2017).
  2. Lexicomp Online. Copyright © 1978-2024 Lexicomp, Inc. All Rights Reserved.
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