No

Antibiotic, Quinolone

Quinolone antibiotic for skin and skin structure, lower respiratory and urinary tract infections and sexually-transmitted diseases. Active against many gram-positive and gram-negative aerobic bacteria.

Ophthalmic: Treatment of superficial ocular infections involving the conjunctiva or cornea due to strains of susceptible organisms

C

Hypersensitivity to ofloxacin or other members of the quinolone group such as nalidixic acid, oxolinic acid, cinoxacin, norfloxacin, and ciprofloxacin

Use with caution in patients with epilepsy or other CNS diseases which could predispose seizures; use with caution in patients with renal impairment; failure to respond to an ophthalmic antibiotic after 2-3 days may indicate the presence of resistant organisms, or another causative agent; use caution with systemic preparation in children <18 years of age due to association of other quinolones with transient arthropathy; has rarely caused ruptured tendons (discontinue immediately with signs of inflammation or tendon pain)

1% to 10%:

Cardiovascular: Chest pain (1% to 3%)

Central nervous system: Headache (1% to 9%), insomnia (3% to 7%), dizziness (1% to 5%), fatigue (1% to 3%), somnolence (1% to 3%), sleep disorders, nervousness (1% to 3%), pyrexia (1% to 3%), pain

Dermatologic: Rash/pruritus (1% to 3%)

Gastrointestinal: Diarrhea (1% to 4%), vomiting (1% to 3%), GI distress, cramps, abdominal cramps (1% to 3%), flatulence (1% to 3%), abnormal taste (1% to 3%), xerostomia (1% to 3%), decreased appetite, nausea (3% to 10%)

Genitourinary: Vaginitis (1% to 3%), external genital pruritus in women

Local: Pain at injection site

Ocular: Superinfection (ophthalmic), photophobia, lacrimation, dry eyes, stinging, visual disturbances (1% to 3%)

Miscellaneous: Trunk pain

<1%: Syncope, vasculitis, edema, hypertension, palpitations, vasodilation, anxiety, cognitive change, depression, dream abnormality, euphoria, hallucinations, vertigo, chills, malaise, extremity pain, weight loss, paresthesia, ruptured tendons, Tourette's syndrome, weakness, photophobia, photosensitivity, hepatitis, decreased hearing acuity, tinnitus, cough, thirst

Symptoms of overdose include acute renal failure, seizures, nausea, vomiting

Treatment includes GI decontamination, if possible, and supportive care

Decreased effect: Decreased absorption with antacids containing aluminum, magnesium, and/or calcium (by up to 98% if given at the same time), iron, vitamins with minerals, mineral supplements, sucralfate, or didanosine; fluoroquinolones may be decreased by antineoplastic agents

Increased toxicity/serum levels: Quinolones cause increased caffeine, warfarin, cyclosporine, procainamide, and possibly theophylline levels. Cimetidine and probenecid increase quinolone levels.

Ofloxacin is a DNA gyrase inhibitor. DNA gyrase is an essential bacterial enzyme that maintains the superhelical structure of DNA. DNA gyrase is required for DNA replication and transcription, DNA repair, recombination, and transposition; bactericidal

Absorption: Well absorbed; administration with food causes only minor alterations in absorption

Distribution: V_d: 2.4-3.5 L/kg

Protein binding: 20%

Half-life, elimination 5-7.5 hours

Elimination: Primarily unchanged in urine

Children >1 year and Adults: Ophthalmic: Instill 1-2 drops in affected eye(s) every 2-4 hours for the first 2 days, then use 4 times/day for an additional 5 days

Adults:

Lower respiratory tract infection: 400 mg every 12 hours for 10 days

Gonorrhea: 400 mg as a single dose

Cervicitis due to C. trachomatis and/or N. gonorrhoeae: 300 mg every 12 hours for 7 days

Skin/skin structure: 400 mg every 12 hours for 10 days

Urinary tract infection: 200-400 mg every 12 hours for 3-10 days

Prostatitis: 300 mg every 12 hours for 6 weeks

Dosing adjustment/interval in renal impairment: Adults: I.V., Oral:

Cl_cr 10-50 mL/minute: Administer 200-400 mg every 24 hours

Cl_cr <10 mL/minute: Administer 100-200 mg every 24 hours

Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects: Administer 300 mg every 24 hours

May cause drowsiness, dizziness, nervousness, or insomnia; quinolones reported to cause restlessness, hallucinations, euphoria, depression, panic, and paranoia

Inhibits CYP1A2 isoenzyme; use caution with clozapine and other psychotropics; monitor for adverse effects

No information available to require special precautions

No effects or complications reported

Oral: Take per recommended schedule; complete full course of therapy and do not skip doses. Take on an empty stomach (1 hour before or 2 hours after meals, dairy products, antacids, or other medication). Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake).

Oral/I.V.: You may experience dizziness, lightheadedness (use caution when driving or engaging in tasks that require alertness until response to drug is known); nausea, vomiting, or taste perversion (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); photosensitivity (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight). Report GI disturbances, CNS changes (excessive sleepiness, agitation, or tremors), skin rash, changes in vision, difficulty breathing, signs of opportunistic infection (sore throat, chills, fever, burning, itching on urination, vaginal discharge, white plaques in mouth), or worsening of condition. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Do not breast-feed.

Ophthalmic: Tilt head back, instill 1-2 drops in affected eye as frequently as prescribed. Do not allow tip of applicator to touch eye or any contaminated surface. You may experience some stinging or burning or a bad taste in you mouth after instillation. Report persistent pain, burning, swelling, or visual disturbances.

Hold antacids for 2-4 hours before and after administering dose

Injection: 200 mg (50 mL); 400 mg (10 mL, 20 mL, 100 mL)

Solution:

Ophthalmic: 0.3% (5 mL)

Otic: 0.3% (5 mL)

Tablet: 200 mg, 300 mg, 400 mg

Hoogkamp-Korstanje JA, " In vitro Activities of Ciprofloxacin, Levofloxacin, Lomefloxacin, Ofloxacin, Pefloxacin, Sparfloxacin, and Trovafloxacin Against Gram-Positive and Gram-Negative Pathogens From Respiratory Tract Infections," J Antimicrob Chemother, 1997, 40(3):427-31.

Hooper DC and Wolfson JS, "Fluoroquinolone Antimicrobial Agents," N Engl J Med, 1991, 324(6):384-94.

Kohler RB, Arkins N, and Tack KJ, "Accidental Overdose of Intravenous Ofloxacin With Benign Outcome," Antimicrob Agents Chemother, 1991, 35(6):1239-40.

Lomaestro BM and Bailie GR, "Quinolone-Cation Interactions: A Review," DICP, 1991, 25(11):1249-58.

Monk JP and Campoli-Richards DM, "Ofloxacin. A Review of Its Antibacterial Activity, Pharmacokinetic Properties and Therapeutic Use," Drugs, 1987, 33(4):346-91.

Nilsson-Ehle I and Ljungberg B, "Quinolone Disposition in the Elderly: Practical Implications," Drugs Aging, 1991, 1(4):279-88.

Stein GE, "The 4-Quinolone Antibiotics: Past, Present, and Future," Pharmacotherapy, 1988, 8(6):301-14.

Szarfman A, Chen M, and Blum MD, "More on Fluoroquinolone Antibiotics and Tendon Rupture," N Engl J Med, 1995, 332(3):193.

Thalhammer F, Kletzmayr J, El Menyawi I, et al, "Ofloxacin Clearance During Hemodialysis: A Comparison of Polysulfone and Cellulose Acetate Hemodialyzers," Am J Kid Dis, 1998, 32(4):642-5.

U.S. Department of Health and Human Services, "1993 Sexually Transmitted Diseases Treatment Guidelines," MMWR Morb Mortal Wkly Rep, 1993, 42(RR-14).

Walker RC and Wright AJ, "The Fluoroquinolones," Mayo Clin Proc, 1991, 66(12):1249-59.