levofloxacin (Levaquin)
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Introduction
Tradename: Levaquin, Leva-pak (50 mg QD for 5 days) levofloxacin is the S-enantiomer of the racemic drug ofloxacin.
Pharmacology
- rapidly & completely absorbed after oral administration
- peak plasma concentrations obtained 1-2 hours after oral dosing
- absolute bioavailability of 500 mg dose is 99%
- steady-state plasma levels reached in 48 hours after daily dosing
- plasma concentrations of 5.7 ug/mL (peak) & 0.5 ug/mL (trough) with 500 mg PO QD
- administration with food delays absorption by about 1 hour & diminished bioavailability by about 14%
- volume of distribution is 89-112 L
- protein binding 24-38%, mainly albumin
- limited metabolism to N-oxide & desmethyl derivatives
- 87% recovered unchanged in the urine
- renal clearance exceeds GFR, suggesting tubular secretion
- elimination 1/2 life is 6-8 hours (76 hours ESRD)
- NO significant differences in pharmacokinetics between young & elderly patients
Indications
- bacterial infections due to susceptible organisms
- urinary tract infection
- eye infection
Dosage
* 750 mg doses may be required for complicated skin infections, deep wounds, infected ulcers, pneumonia[5]
Tabs: 250, 500, 750 mg.
Dosage adjustment in renal failure
Table
| creatinine clearance | dosage |
|---|---|
| 10-50 mL/min* | 250 mg every 24-48 hours |
| < 10 mL/min# | 250 mg every 48 hours |
* same dose for continuous arteriovenous hemofiltration
# same dose for hemodialysis
Antimicrobial activity
(eradication rate in parenthesis)
- Streptococcus
- Enterococcus faecalis
- Staphylococcus aureus (MSSA) (88%)
- Staphylococcus aureus (MRSA) (+/-)
- Staphylococcus epidermidis
- Neisseria gonorrhoeae
- Neisseria meningitidis
- Moraxella catarrhalis (94%)
- Haemophilus influenzae (98%)
- Haemophilus parainfluenzae[7]
- Escherichia coli
- Klebsiella species (100%, K pneumoniae)
- Enterobacter species
- Serratia species
- Salmonella species
- Shigella species
- Proteus mirabilis
- Proteus vulgaris
- Providencia species
- Morganella species
- Citrobacter species
- Aeromonas species
- Acinetobacter species
- Pseudomonas aeruginosa
- Yersinia enterocolitica
- Legionella species
- Chlamydophila pnemoniae[7]
Adverse effects
- 3% discontinuation due to adverse effects
- most common adverse effects:
- gastrointestinal
- skin & mucous membrane
- CNS/psychosomatic
- other
- leukorrhea
- acute liver injury[6]
- severe hypoglycemia resulting in coma or death, usually in patients with diabetes mellitus taking oral hypglycemic agents &/or insulin[10]
- increased risk of nervousness, delirium, disorientation, inattention, or memory impairment[10]
- low risk of musculoskeletal complaints in children[9]
- higher risk of arrhythmia & mortality than amoxicillin[7]
Drug interactions
- antacids, sucralfate, metal ions & multivitamins may diminish GI absorption of levofloxacin
- co-administration of an NSAID may increase risk of CNS stimulation & convulsive seizure
- NO drug interactions with theophylline, warfarin, digoxin, cyclosporine
- drug interaction(s) anticonvulsants with anti-bacterial agents
- drug interaction(s) of antibiotics with warfarin
- drug interaction(s) of theophylline with fluoroquinolone
- drug interaction(s) of beta-adrenergic receptor antagonists with quinolones
- drug interaction(s) of fluroquinolones with amiodarone
- drug interaction(s) of fluroquinolones with sulfonylureas
- drug interaction(s) of fluoroquinolones with hypoglycemic agents
Notes
Physical properties:
- soluble in water 100 mg/mL pH 0.6-5.8 & 272 mg/mL at pH 6.7
- forms stable coordination compounds with many metals
More general terms
More specific terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Sanford Guide to antimicrobial therapy 1997
- ↑ Prescriber's Letter 7(10):57 2000
- ↑ PDR 2000
- ↑ Jump up to: 5.0 5.1 Prescriber's Letter 14(3): 2007 Empiric Antibiotic Treatment of Community-Acquired Pneumonia in Adults Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230302&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Jump up to: 6.0 6.1 Paterson JM et al Fluoroquinolone therapy and idiosyncratic acute liver injury: a population-based study CMAJ August 13, 2012 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/22891208 <Internet> http://www.cmaj.ca/content/early/2012/08/13/cmaj.111823.full.pdf+html
Hayashi PH and Chalasani NP Liver injury in the elderly due to fluoroquinolones: Should these drugs be avoided? CMAJ August 13, 2012 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/22891207 <Internet> http://www.cmaj.ca/content/early/2012/08/13/cmaj.121270 - ↑ Jump up to: 7.0 7.1 7.2 7.3 7.4 7.5 Deprecated Reference
- ↑ Rao GA et al Azithromycin and Levofloxacin Use and Increased Risk of Cardiac Arrhythmia and Death. Ann Fam Med 2014 vol. 12 no. 2 121-127 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/24615307 <Internet> http://annfammed.org/content/12/2/121
- ↑ Jump up to: 9.0 9.1 Bradley JS et al. Assessment of musculoskeletal toxicity 5 years after therapy with levofloxacin. Pediatrics 2014 Jun 2 PMID: https://www.ncbi.nlm.nih.gov/pubmed/24918220
- ↑ Jump up to: 10.0 10.1 10.2 Jansen Pharmaceuticals