ofloxacin
Floxin, Ocuflox

Available forms
Available by prescription only
Injection: 200 mg in 50 ml D₅W; 400 mg in water for injection in 10-ml single-use vials; 400 mg in 100 ml D₅W.
Ophthalmic solution: 0.3%
Otic solution: 0.3%
Tablets: 200 mg, 300 mg, 400 mg

Indications and dosages
 Conjunctivitis caused by known organisms. Adults and children older than age 1: Instill 1 to 2 drops in conjunctival sac q 2 to 4 hours, while awake, for first 2 days and then q.i.d. for up to 5 additional days.
 Bacterial keratitis. Adults and children older than age 1: 1 to 2 drops in affected eye q 30 minutes while awake and q 4 to 6 hours after retiring for 2 days. On day 3, apply 1 to 2 drops to the affected eye q 1 hour while awake for an additional 4 to 6 days. Then, 1 to 2 drops q.i.d. until clinical cure is achieved.
 Acute bacterial exacerbations of chronic bronchitis, uncomplicated skin and skin-structure infections, and community-acquired pneumonia. Adults: 400 mg P.O. or I.V. q 12 hours for 10 days.
 Sexually transmitted diseases, such as acute uncomplicated urethral and cervical gonorrhea, nongonococcal urethritis and cervicitis, and mixed infections of urethra and cervix. Adults: For acute uncomplicated gonorrhea, 400 mg P.O. or I.V. once as a single dose; for cervicitis and urethritis, 300 mg P.O. or I.V. q 12 hours for 7 days.
 Urinary tract infections. Adults: For cystitis caused by Escherichia coli or Klebsiella pneumoniae, 200 mg P.O. or I.V. q 12 hours for 3 days; for cystitis caused by other organisms, 200 mg P.O. or I.V. q 12 hours for 7 days.
 Complicated urinary tract infections. Adults: 200 mg P.O. or I.V. q 12 hours for 10 days.
 Prostatitis from E. coli. Adults: 300 mg P.O. or I.V. q 12 hours for 6 weeks. Change I.V. administration to P.O. after 10 days.
 Pelvic inflammatory disease. Adults: 400 mg P.O. or I.V. q 12 hours in combination with metronidazole for 10 to 14 days.
 Otitis externa. Adults and children age 12 and older: 10 drops into affected ear b.i.d. for 10 days.
Children ages 1 to 12: 5 drops instilled into affected ear b.i.d. for 10 days.
 Acute otitis media in pediatric patients with tympanostomy tubes. Children ages 1 to 12: Instill 5 drops into affected ear b.i.d. for 10 days.
 Chronic suppurative otitis media with perforated tympanic membrane. Adults and children age 12 and older: Instill 10 drops into affected ear b.i.d. for 14 days.
 Traveler’s diarrhea ◇. Adults: 300 mg P.O. b.i.d. for 3 days.
≡ Dosage adjustment. For patients with creatinine clearance less than 20 ml/ minute, give initial dose as recommended; then give 50% of recommended dose q 24 hours for additional doses. Maximum daily dose in patients with hepatic function disorders is 400 mg.

Pharmacodynamics
Antibacterial action: Ofloxacin interferes with DNA gyrase, which is needed for synthesis of bacterial DNA. Spectrum of action includes many gram-positive and gram-negative aerobic bacteria including Enterobacteriaceae and Pseudomonas aeruginosa. Also, drug has some in vitro activity against chlamydia, mycoplasma, mycobacterium, plasmodium, and rickettsia.

Pharmacokinetics
Absorption: Well absorbed after oral administration. Because oral bioavailability of ofloxacin is about 98%, oral and I.V. dosages are the same.
Distribution: Widely distributed to body tissues and fluids.
Metabolism: Less than 10% of a single dose is metabolized.
Excretion: 70% to 80% excreted unchanged in urine; less than 5% in feces.

Contraindications and precautions
Contraindicated in patients hypersensitive to drug or other fluoroquinolones. Use oral and I.V. forms cautiously in patients with seizure disorders, CNS diseases such as cerebral arteriosclerosis, hepatic disorders, or renal failure and during pregnancy.

Interactions
Drug-drug. Antacids (containing calcium, magnesium, or aluminum), sucralfate, divalent or trivalent cations (such as iron or zinc), or didanosine (chewable/buffered tablets or pediatric powder for oral solution): Interferes with GI absorption of ofloxacin. Give these drugs 2 hours before or 2 hours after taking ofloxacin.
Antidiabetics: May affect blood glucose levels, causing hypoglycemia or hyperglycemia. Monitor patient closely.
Theophylline: May increase serum theophylline levels. Monitor patient closely and adjust theophylline dosage as needed.
Warfarin: May prolong PT and INR. Monitor PT and INR.
Drug-lifestyle. Sun exposure: May cause photosensitivity reactions. Advise patient to take precautions.

Adverse reactions
CNS: dizziness; headache, fatigue, lethargy, malaise, drowsiness, sleep disorders, nervousness, insomnia, visual disturbances, seizures (with oral or I.V. form), fever.
CV: chest pain (with oral or I.V. form).
EENT: transient ocular burning or discomfort, stinging, redness, itching, photophobia, lacrimation, eye dryness (with ophthalmic form).
GI: nausea, pseudomembranous colitis, anorexia, abdominal pain or discomfort, diarrhea, vomiting, constipation, dry mouth, flatulence, dysgeusia (with oral or I.V. form).
GU: hematuria, glucosuria, proteinuria, vaginitis, vaginal discharge, genital pruritus (with oral or I.V. form).
Hematologic: eosinophilia, leukopenia, neutropenia, anemia, leukocytosis.
Metabolic: hyperglycemia, hypoglycemia.
Musculoskeletal: body pain (with oral or I.V. form).
Skin: rash, pruritus, photosensitivity (with oral or I.V. form).
Other: hypersensitivity reactions(anaphylactoid reaction), phlebitis (with oral or I.V. form).

Effects on lab test results
• May increase BUN, creatinine, and liver enzyme levels. May increase or decrease glucose levels.
• May increase erythrocyte sedimentation rate and eosinophil count. May decrease hemoglobin, hematocrit, and neutrophil count. May increase or decrease WBC count.

Overdose and treatment
Empty the stomach and maintain hydration. Observe patient and treat symptomatically.

Special considerations
• Give I.V. ofloxacin by slow infusion only; don’t give I.M., S.C., intrathecally, or by intraperitoneal injection. Administer over at least 60 minutes and avoid rapid or bolus injection. Compatible with most common I.V. solutions, including D₅W injection, normal saline injection, dextrose 5% in normal saline injection, dextrose 5% in 0.45% saline injection, 5% dextrose in lactated Ringer’s solution, and 5% sodium bicarbonate injection. Dilute 20- to 40-mg/ml vials to solution containing 4 mg/ml.
• Administer drug I.V. for no longer than 10 days; after 10 days, change I.V. to P.O.
• Drug isn’t recommended for syphilis.
• Ofloxacin is one of two quinolones that would most likely produce false-positive opiate assay results.
• Periodically assess organ system functions during prolonged therapy.
• Monitor patient for overgrowth of nonsusceptible organisms.
• Monitor renal and hepatic test results and CBC in prolonged therapy.
Breast-feeding patients
• Ofloxacin appears in breast milk in levels similar to those found in plasma. Safety hasn’t been established in breast-feeding women.
Pediatric patients
• Safety and efficacy in children younger than age 18 haven’t been established. Similar drugs have caused arthropathy in juvenile animals.

Patient education
• Tell patient to drink fluids liberally.
• Advise patient to separate doses of antacids, vitamins, and ofloxacin by 2 hours.
• Tell patient drug may be taken without regard to meals.
• Warn patient that dizziness and light-headedness may occur. Advise caution when driving or operating hazardous machinery until effects of drug are known.
• Warn patient that hypersensitivity reactions may follow first dose; he should discontinue drug at first sign of rash or other allergic reaction and call immediately.
• Advise patient to avoid prolonged exposure to direct sunlight and to use a sunscreen when outdoors.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use