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ofloxacin (Floxin, Ocuflox, Floxin Otic)
Tradenames: Floxin, Ocuflox (ophthalmic)
Indications:
1) bacterial infections due to susceptible organisms
- skin or soft tissue infections
- lower respiratory tract infections
- urinary tract infections
- sexually transmitted diseases
- prostatitis
- traveler's diarrhea
- anthrax [6]
2) Otic solution: (Floxin Otic)
- treatment of otitis externa
- otitis media in pediatric patients with tympanostomy tubes
- chronic suppurative otitis media in patients > 12 years of age with perforated tympanic membranes
3) Ophthalmic agent
- susceptible eye infections
- cornel ulcer [6]
Contraindications:
- ophthalmic agent
1) epithelial herpes simplex keratitis
2) vaccinia
3) varicella
4) mycobacterial infections of the eye
5) fungal eye infections
6) use of steroids after uncomplicated removal of corneal foreign body
Caution:
- seizure disorder
Dosage:
1) systemic agent
- 200-400 IV/PO every 12 hours for 7-10 days
- prostatitis: 200-400 IV/PO every 12 hours for 6 weeks
- gonorrhea: 400 mg PO single dose
2) Ophthalmic agent: 1 drop every 1-6 hours
Tabs: 200, 300, 400 mg
Solution: (ophthalmic) 0.35% (5 mL)
Dosage adjustment in renal failure:
1) initial dose is the same, regardless of renal failure
2) creatinine clearance 10-50 mL/min: QD dosing
3) creatinine clearance < 10 mL: 50% of dose with QD dosing
4) 100-200 mg IV after hemodialysis
Pharmacokinetics:
1) well absorbed after oral administration
a) unaffected by food
b) aral route achieves similar concentration to parenteral route
2) widely distributed to body tissues & fluids
a) crosses placenta
b) distributed to breast milk
3) protein binding 20-32%
4) elimination 1/2life: 4-8 hours (28-37 hours ESRD)
5) excreted primarily unchanged in the urine
Antimicrobial activity:
Gram positive
- Streptococcus (+/-)
- Streptococcus group A (+/-)
- Streptococcus group B (+/-)
- Streptococcus group C (+/-)
- Streptococcus group G (+/-)
- Streptococcus pneumonia (+/-)*
- Staphylococcus aureus (MSSA)
- Staphylococcus epidermidis
Gram negative
- Neisseria gonorrhoeae
- Neisseria meningitidis
- Moraxella catarrhalis
- Haemophilus influenzae
- Escherichia coli
- Klebsiella species
- 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
- Pasteurella multocida
Atypical bacteria
- Chlamydia species*
- Mycoplasma pneumonia
Anaerobes
- Actinomyces (+/-)
- Clostridium species (+/-)
- Peptostreptococcus species (+/-) *Among the quinolones, ofloxacin has the best activity against Chlamydia & pneumococci.
Ofloxacin & ciprofloxacin are used in multidrug regimens for treatment of drug-resistant Mycobacterium tuberculosis.
Adverse effects:
1) not common (1-10%)
- superinfection (ophthalmic), photophobia, lacrimation, dry eyes, stinging
2) uncommon (< 1%)
- dizziness
3) GI effects: nausea, diarrhea
4) headache, insomnia
Drug interactions:
1) sucralfate, aluminum & magnesium containing antacids, products containing zinc, calcium or iron may decrease bioavailability of ofloxacin
2) probenecid may decrease renal clearance of ofloxacin
3) ofloxacin may increase anticoagulant effect of warfarin
Laboratory:
1) ofloxacin in serum/plasma
- specimen: serum, plasma (heparin)
2) methods: HPLC, MB
3) interferences:
- other anti-microbials may interfere with microbiologic (MB) assay
Interactions
drug interactions
drug adverse effects of fluoroquinolones
Specific
Ofloxacin Ophthalmic
General
fluoroquinolone
Properties
INHIBITS: DNA gyrase
MISC-INFO: elimination route LIVER
KIDNEY
1/2life 5-8 HOURS
therapeutic-range 1.6-8.1 UG/ML
protein-binding 25%
elimination by hemodialysis +
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Harrison's Principles of Internal Medicine, 13th ed.
Companion Handbook. Isselbacher et al (eds),
McGraw-Hill Inc. NY, 1995, pg 165
- Sanford Guide to antimicrobial therapy 1997
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed.,
W.B. Saunders, 1995
- Deprecated Reference
- Department of Veterans Affairs, VA National Formulary