DrugindexOnline^{2nd edition}

Pronouncation: (oh-FLOX-uh-SIN)
Class: Antibiotic, Fluoroquinolone

Trade Names:
Floxin Otic
- Solution, otic 3 mg/mL

Trade Names:
Ocuflox
- Solution, ophthalmic 3 mg/mL

Trade Names:
Ofloxacin
- Tablets 200 mg
- Tablets 300 mg
- Tablets 400 mg

Apo-Oflox (Canada)

Mechanism of Action

Pharmacology

Interferes with microbial DNA synthesis.

Pharmacokinetics

Absorption

C _max is 2.7 to 4 mcg/mL. T _max is 1 to 2 h (oral).

Distribution

Widely distributed to body tissues and fluids. 32% protein bound. Bioavailability is 98%.

Metabolism

Pyridobenzoxazine ring appears to decrease the extent of parent compound metabolism.

Elimination

The t _½ is 4 to 5 hr (oral). Less than 5% is eliminated by the kidneys as desmethyl or N-oxide metabolites; 4% to 8% by feces.

Special Populations

Renal Function Impairment

Cl is reduced in patients with Ccr less than 50 mL/min. Dosage adjustment is necessary.

Elderly

Longer plasma t _½ is approximately 6.4 to 7.4 h.

Indications and Usage

Treatment of acute bacterial exacerbations of chronic bronchitis, community acquired pneumonia, uncomplicated skin and skin structure infections, acute uncomplicated urethral and cervical gonorrhea, nongonococcal urethritis, cervicitis, acute pelvic inflammatory disease, uncomplicated cystitis, complicated UTI, prostatitis caused by Escherichia coli .

Ophthalmic

Treatment of conjunctivitis and corneal ulcer infections caused by susceptible organisms.

Otic

Treatment of otitis externa, chronic suppurative otitis media in patients with perforated tympanic membranes, and acute otitis media in children with tympanostomy tubes.

Contraindications

Standard considerations.

Ophthalmic

Epithelial herpes simplex keratitis; vaccinia; varicella; fungal disease of ocular structure; mycobacterial infections of the eye.

Dosage and Administration

Acute Otitis Media in Children with Tympanostomy Tubes
Children 1 to 12 yr of age

Otic 5 gtt (0.25 mL, 0.75 mg ofloxacin) instilled into affected ear twice daily for 10 days.

Acute Pelvic Inflammatory Disease
Adults

PO 400 mg every 12 h for 10 to 14 days.

Acute Uncomplicated Urethral and Cervical Gonorrhea
Adults

PO 400 mg as single dose.

Bacterial Conjunctivitis
Adults and Children 1 yr of age or older

Ophthalmic Days 1 and 2 instill 1 to 2 gtt every 2 to 4 h in affected eye(s). Days 3 through 7 instill 1 to 2 gtt 4 times daily.

Bacterial Corneal Ulcer
Adults and Children 1 yr of age or older

Ophthalmic Days 1 and 2 instill 1 to 2 gtt into affected eye every 30 min while awake, awaken at approximately 4 to 6 h after retiring and instill 1 to 2 gtt; days 3 through 7 to 9 instill 1 to 2 gtt every h while awake; days 7 to 9 instill 1 to 2 gtt 4 times daily.

Cervicitis/Urethritis
Adults

PO 300 mg every 12 h for 7 days.

Chronic Bronchitis, Community-Acquired Pneumonia, Uncomplicated Skin and Skin Structure Infections
Adults

PO 400 mg every 12 h for 10 days.

Chronic Suppurative Otitis Media with Perforated Tympanic Membranes
Adults and children 12 yr of age and older

Otic 10 gtt (0.5 mL, 1.5 mg ofloxacin) instilled into affected ear twice daily for 10 days.

Complicated UTI
Adults

PO 200 mg every 12 h for 10 days.

Epididymitis
Adults

PO 300 mg twice daily for 10 days.

Otitis Externa
Adults and children 12 yr of age and older

Otic 10 gtt (0.5 mL, 1.5 mg ofloxacin) instilled into affected ear twice daily for 10 days.

Children 1 to 12 yr of age

Otic 5 gtt (0.25 mL, 0.75 mg ofloxacin) instilled into affected ear twice daily for 10 days.

Prostatitis
Adults

PO 300 mg every 12 h for 6 wk.

Uncomplicated Cystitis Caused by E. Coli or Klebsiella Pneumoniae
Adults

PO 200 mg every 12 h for 3 days.

Uncomplicated Cystitis Caused by Other Pathogens
Adults

PO 200 mg every 12 h for 7 days.

Storage/Stability

Store at 59° to 86°F. Protect from light.

Drug Interactions

Antacids, didanosine, iron salts, sucralfate, zinc salts

May decrease oral absorption of ofloxacin.

Antineoplastic agents

Serum ofloxacin levels may be decreased.

NSAIDs

Coadministration with ofloxacin may increase risk of CNS stimulation and seizures.

Procainamide

Plasma levels of procainamide may be elevated, increasing the risk of toxicity.

Theophylline

Decreased Cl and increased plasma levels of theophylline may result in toxicity.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Chest pain.

CNS

Dizziness, vertigo (1%, otic); headache; dizziness; fatigue; lethargy; drowsiness; insomnia; nervousness.

Dermatologic

Pruritus, rash (4%, otic); rash, pruritus.

EENT

Tearing, dryness, eye pain, visual disturbances, transient burning, itching, stinging, inflammation, facial edema (ophthalmic); earache (otic).

GI

Taste perversion (7%, otic); diarrhea; nausea; vomiting; abdominal pain or discomfort; dry or painful mouth; flatulence; dysgeusia.

Genitourinary

Vaginal discharge; genital pruritus.

Hematologic

Eosinophilia; lymphocytopenia.

Hepatic

Increased ALT, AST.

Miscellaneous

Application site reaction (3%), paresthesia (otic); vaginitis; fever; decreased appetite. Ophthalmic use may possibly cause same adverse reactions seen with systemic use because of absorption.

Precautions

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established in children younger than 1 yr of age. Safety and efficacy not established in children younger than 18 yr of age (otic).

Hypersensitivity

Serious and occasionally fatal reactions (eg, anaphylactic) have occurred, some after the first dose.

Renal Function

Reduced Ccr may occur; decrease dose accordingly.

Superinfection

May result in bacterial or fungal overgrowth of nonsusceptible microorganisms.

Photosensitivity

Moderate to severe reactions may occur; avoid excessive sunlight and ultraviolet light.

Convulsions/Toxic psychosis

CNS stimulation can occur; use drug with caution in patients with known or suspected CNS disorders.

Pseudomembranous colitis

Consider possibility in patients who develop diarrhea.

Syphilis

Not effective for treating syphilis.

Tendonitis

Inflammation and rupture of tendons have been associated with the use of fluoroquinolone antibiotics.

Overdosage

Symptoms

Nausea, dizziness, crystalluria, facial swelling and numbness, vomiting, drowsiness, hot and cold flushes.

Patient Information

• Instruct patient to avoid taking antacids, sucralfate, vitamins with iron or minerals within 2 h before or 2 h after dose.
• Advise diabetic patient to discontinue and notify health care provider if a hypoglycemic reaction occurs.
• Encourage patient to drink fluids liberally.
• Caution patient to avoid exposure to sunlight, and to use sunscreen or wear protective clothing to avoid photosensitivity reaction.
• Advise patient to notify health care provider of signs of superinfection.
• Caution patient to report the following symptoms to health care provider: seizures, nausea, rash, itching, diarrhea, shortness of breath, dizziness, headache.
• Instruct patient to complete full course of therapy, even if symptoms have resolved.
• Instruct patient to stop treatment and inform health care provider if experiencing pain, inflammation, or rupture of tendon, and to rest or refrain from exercise until diagnosis of tendonitis or tendon rupture is excluded.

• Ophthalmic
• Demonstrate and observe correct technique for instillation of ophthalmic drops.
• Advise patient using ophthalmic solution to discontinue medication and notify health care provider of rash or allergic reaction.

• Otic
• Caution patient to avoid contaminating the applicator tip with material from fingers or other sources.
• Instruct patient to warm the solution by holding the bottle in the hand for 1 or 2 min to avoid dizziness, which may result from the instillation of cold solution.