Ofloxacin

Pronunciation

(oh FLOKS a sin)

U.S. Brand Names

Floxin®; Ocuflox®

Synonyms

Floxin Otic Singles

Generic Available

Yes: Tablet, ophthalmic solution

Canadian Brand Names

Apo-Oflox®; Floxin®; Ocuflox®

Use

Quinolone antibiotic for the treatment of acute exacerbations of chronic bronchitis, community-acquired pneumonia, skin and skin structure infections (uncomplicated), urethral and cervical gonorrhea (acute, uncomplicated), urethritis and cervicitis (nongonococcal), mixed infections of the urethra and cervix, pelvic inflammatory disease (acute), cystitis (uncomplicated), urinary tract infections (complicated), prostatitis

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

Otic: Otitis externa, chronic suppurative otitis media, acute otitis media

Use - Unlabeled/Investigational

Epididymitis (gonorrhea)

Pregnancy Risk Factor

Pregnancy Implications

Reports of arthropathy (observed in immature animals and reported rarely in humans) have limited the use of fluoroquinolones in pregnancy. Teratogenic effects were not observed with ofloxacin in animal studies; however, decreased fetal body weight and increased fetal mortality were observed in some species. Ofloxacin crosses the placenta. Although quinolone antibiotics should not be used as first-line agents during pregnancy, when considering treatment for life-threatening infection and/or prolonged duration of therapy, the potential risk to the fetus must be balanced against the severity of the potential illness.

Lactation

Enters breast milk/not recommended (AAP rates "compatible")

Contraindications

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

Warnings/Precautions

Use with caution in patients with epilepsy or other CNS diseases which could predispose seizures; use with caution in patients with renal or hepatic impairment. Tendon inflammation and/or rupture have been reported with quinolone antibiotics, including ofloxacin. Risk may be increased with concurrent corticosteroids, particularly in the elderly. Discontinue at first sign of tendon inflammation or pain. Peripheral neuropathies have been linked to ofloxacin use; discontinue if numbness, tingling, or weakness develops.

Rare cases of torsade de pointes have been reported in patients receiving ofloxacin and other quinolones. Risk may be minimized by avoiding use in patients with known prolongation of the QT interval, bradycardia, hypokalemia, hypomagnesemia, cardiomyopathy, or in those receiving concurrent therapy with Class Ia or Class III antiarrhythmics.

Severe hypersensitivity reactions, including anaphylaxis, have occurred with quinolone therapy. If an allergic reaction occurs (itching, urticaria, dyspnea, facial edema, loss of consciousness, tingling, cardiovascular collapse), discontinue drug immediately. Prolonged use may result in superinfection; pseudomembranous colitis may occur and should be considered in all patients who present with diarrhea. Quinolones may exacerbate myasthenia gravis, use with caution (rare, potentially life-threatening weakness of respiratory muscles may occur).

Adverse Reactions

Systemic:

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 (1% to 3%), nervousness (1% to 3%), pyrexia (1% to 3%)

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

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

Genitourinary: Vaginitis (1% to 5%), external genital pruritus in women (1% to 3%)

Ocular: Visual disturbances (1% to 3%)

Respiratory: Pharyngitis (1% to 3%)

Miscellaneous: Trunk pain

<1%, postmarketing, and/or case reports (limited to important or life-threatening): Anaphylaxis reactions, anxiety, blurred vision, chills, cognitive change, cough, depression, dream abnormality, ecchymosis, edema, erythema nodosum, euphoria, extremity pain, hallucinations, hearing acuity decreased, hepatic dysfunction, hepatitis, hyper/hypoglycemia, hypertension, interstitial nephritis, lightheadedness, malaise, myasthenia gravis exacerbation, palpitation, paresthesia, peripheral neuropathy, photophobia, photosensitivity, psychotic reactions, rhabdomyolysis, seizure, Stevens-Johnson syndrome, syncope, tendonitis and tendon rupture, thirst, tinnitus, torsade de pointes, Tourette's syndrome, toxic epidermal necrolysis, vasculitis, vasodilation, vertigo, weakness, weight loss

Ophthalmic: Frequency not defined:

Central nervous system: Dizziness

Gastrointestinal: Nausea

Ocular: Blurred vision, burning, chemical conjunctivitis/keratitis, discomfort, dryness, edema, eye pain, foreign body sensation, itching, photophobia, redness, stinging, tearing

Otic:

>10%: Local: Application site reaction (<1% to 17%)

1% to 10%:

Central nervous system: Dizziness ( 1%), vertigo ( 1%)

Dermatologic: Pruritus (1% to 4%), rash (1%)

Gastrointestinal: Taste perversion (7%)

Neuromuscular & skeletal: Paresthesia (1%)

<1% (Limited to important or life-threatening): Diarrhea, fever, headache, hearing loss, hypertension, nausea, otorrhagia, tinnitus, tremor, vomiting, xerostomia

Postmarketing and/case reports: Transient neuropsychiatric disturbances

Overdosage/Toxicology

Symptoms of overdose include acute renal failure, seizures, nausea, and vomiting. Treatment includes GI decontamination, if possible, and supportive care. Not removed by peritoneal or hemodialysis.

Drug Interactions

Inhibits CYP1A2 (strong)

Corticosteroids: Concurrent use may increase the risk of tendon rupture, particularly in elderly patients (overall incidence rare).

CYP1A2 substrates: Ofloxacin may increase the levels/effects of CYP1A2 substrates. Example substrates include aminophylline, fluvoxamine, mexiletine, mirtazapine, ropinirole, and trifluoperazine.

Glyburide: Quinolones may increase the effect of glyburide; monitor.

Metal cations (aluminum, calcium, iron, magnesium, and zinc) bind quinolones in the gastrointestinal tract and inhibit absorption. Concurrent administration of most antacids, oral electrolyte supplements, quinapril, sucralfate, and some didanosine formulations (chewable/buffered tablets and pediatric powder for oral suspension) should be avoided. Ofloxacin should be administered 2 hours before or 2 hours after these agents.

Probenecid: May decrease renal secretion of ofloxacin.

QTc-prolonging agents: Effects may be additive with ofloxacin. Avoid concurrent use with Class Ia and Class III antiarrhythmics; use caution with other drugs known to prolong QTc, including erythromycin, cisapride, antipsychotics, and cyclic antidepressants.

Theophylline: Ofloxacin may increase plasma levels of theophylline. Monitor.

Warfarin: The hypoprothrombinemic effect of warfarin may be enhanced by some quinolone antibiotics; monitor INR.

Ethanol/Nutrition/Herb Interactions

Food: Ofloxacin average peak serum concentrations may be decreased by 20% if taken with food.

Herb/Nutraceutical: Avoid dong quai, St John's wort (may also cause photosensitization).

Mechanism of Action

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

Pharmacodynamics/Kinetics

Absorption: Well absorbed; food causes only minor alterations

Distribution: Vd: 2.4-3.5 L/kg

Protein binding: 20%

Bioavailability: Oral: 98%

Half-life elimination: Biphasic: 5-7.5 hours and 20-25 hours (accounts for <5%); prolonged with renal impairment

Excretion: Primarily urine (as unchanged drug)

Dosage

Oral: Adults:

Chronic bronchitis (acute exacerbation), community-acquired pneumonia, skin and skin structure infections (uncomplicated): 400 mg every 12 hours for 10 days

Urethral and cervical gonorrhea (acute, uncomplicated): 400 mg as a single dose

Cervicitis/urethritis (nongonococcal) due to C. trachomatis , mixed infection of urethra and cervix due to C. trachomatis and N. gonorrhoeae : 300 mg every 12 hours for 7 days

Pelvic inflammatory disease (acute): 400 mg every 12 hours for 10-14 days

Cystitis (uncomplicated):

Due to E. coli or K. pneumoniae : 200 mg every 12 hours for 3 days

Due to other organisms: 200 mg every 12 hours for 7 days

UTI (complicated): 200 mg every 12 hours for 10 days

Prostatitis: 200 mg every 12 hours for 6 weeks

Epididymitis (gonorrhea; unlabeled use): 300 mg twice daily for 10 days

Ophthalmic: Children >1 year and Adults:

Conjunctivitis: 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

Corneal ulcer: Instill 1-2 drops every 30 minutes while awake and every 4-6 hours after retiring for the first 2 days; beginning on day 3, instill 1-2 drops every hour while awake for 4-6 additional days; thereafter, 1-2 drops 4 times/day until clinical cure.

Otic:

Acute otitis media with tympanostomy tubes: Children 1-12 years: Instill 5 drops (or the contents of 1 single-dose container) into affected ear(s) twice daily for 10 days

Chronic suppurative otitis media with perforated tympanic membranes: Children >12 years and Adults: Instill 10 drops (or the contents of 2 single-dose containers) into affected ear twice daily for 14 days

Otitis externa:

Children 6 months to 13 years: Instill 5 drops (or the contents of 1 single-dose container) into affected ear(s) once daily for 7 days

Children 13 years and Adults: Instill 10 drops (or the contents of 2 single-dose containers) into affected ear(s) once daily for 7 days

Dosing adjustment/interval in renal impairment: Adults: Oral: After a normal initial dose, adjust as follows:

Clcr 20-50 mL/minute: Administer usual dose every 24 hours

Clcr<20 mL/minute: Administer half the usual dose every 24 hours

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

Dosing adjustment in hepatic impairment: Severe impairment: Maximum dose: 400 mg/day

Administration

Ophthalmic: For ophthalmic use only; avoid touching tip of applicator to eye or other surfaces.

Oral: Do not take within 2 hours of food or any antacids which contain zinc, magnesium, or aluminum.

Otic: Prior to use, warm solution by holding container in hands for 1-2 minutes. Patient should lie down with affected ear upward and medication instilled. Pump tragus 4 times to ensure penetration of medication. Patient should remain in this position for 5 minutes.

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber.

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 advised by prescriber to restrict fluids. May cause dizziness, lightheadedness, or headache (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). If inflammation or tendon pain occurs, discontinue use immediately and report to prescriber. If chest pain, palpitations, rapid heart beat, or unusual dizziness occurs, contact prescriber immediately. If sign of allergic reaction (eg, itching, urticaria, respiratory difficulty, facial edema or difficulty swallowing, loss of consciousness, tingling, chest pain, palpitations) occurs, discontinue use immediately and report to prescriber. Report GI disturbances; CNS changes (eg, excessive sleepiness, agitation, or tremors); skin rash; vision changes; respiratory difficulty; signs of opportunistic infection (eg, 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 become pregnant. Breast-feeding is not recommended.

Ophthalmic: Tilt head back, instill 1-2 drops in affected eye as frequently as prescribed. Do not let tip of applicator touch eye; do not contaminate tip of applicator (may cause eye infection, eye damage, or vision loss). May cause some stinging or burning or a bad taste in you mouth after instillation. Report persistent pain, burning, swelling, or visual disturbances.

Otic: Wash hands before and after applying drops. Lie with affected ear up and instill prescribed number of drops into ear. Remain on side with ear up for 5 minutes.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

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

Mental Health: Effects on Psychiatric Treatment

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

Oncology: Emetic Potential

Very low (<10%)

Oncology: Vesicant

Dosage Forms

Solution, ophthalmic (Ocuflox®): 0.3% (5 mL, 10 mL) [contains benzalkonium chloride]

Solution, otic:

Floxin®: 0.3% (5 mL, 10 mL) [contains benzalkonium chloride]

Floxin® Otic Singles™: 0.3% (0.25 mL) [contains benzalkonium chloride; packaged as 2 single-dose containers per pouch, 10 pouches per carton, total net volume 5 mL]

Tablet (Floxin®): 200 mg, 300 mg, 400 mg

References

Abramowicz M, "Antimicrobial Prophylaxis in Surgery," Medical Letter on Drugs and Therapeutics, Handbook of Antimicrobial Therapy , 16th ed, New York, NY: Medical Letter, 2002.

"American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk," Pediatrics , 2001, 108(3):776-89.

Centers for Disease Control and Prevention, " Sexually Transmitted Diseases Treatment Guidelines - 2002," MMWR Recom Rep , MMWR Recomm Rep , 2002, 51(RR-6):1-78. Available at: http://www.cdc.gov/mmwr/preview/mmwrhtml/rr5106a1.htm. Accessed June 8, 2004.

Giamarellou H, Kolokythas E, Petrikkos G, et al, "Pharmacokinetics of Three Newer Quinolones in Pregnant and Lactating Women," Am J Med , 1989, 87(Suppl 5A):49-51.

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.

Jacobs MR, Felmingham D, Appelbaum PC, et al, "The Alexander Project 1998-2000: Susceptibility of Pathogens Isolated From Community-Acquired Respiratory Tract Infection to Commonly Used Antimicrobial Agents," J Antimicrob Chemother , 2003, 52(2):229-46.

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

Loebstein R, Lalkin A, Addis A, et al, "Pregnancy Outcome After Gestational Exposure to Terfenadine: A Multicenter, Prospective Controlled Study," J Allergy Clin Immunol , 1999, 104(5):953-6.

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.

Peled Y, Friedman S, Hod M, et al, "Ofloxacin during the second trimester of pregnancy," DICP , 1991, 25(11):1181-2.

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 Kidney Dis , 1998, 32(4):642-5.

Thomas RJ and Reagan DR, "Association of a Tourette-like Syndrome With Ofloxacin," Ann Pharmacother , 1996, 30(2):138-41.

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

International Brand Names

Adco-Ofloxacin® (ZA); Akilen® (ID); Apo-Oflox® (CA); Bactocin® (MX); Bactoflox® (PT); Betaflox® (ID); Bioquil® (PT); Cilox® (CY); Danoflox® (ID); Drovid® (TR); Efexin® (ID); Ethiflox® (ID); Exocin® (DK, ES, FI, GB, IE, IT, PT, TR, ZA); Exocine® (FR); Flobacin® (IT); Floxal® (AT, CH, CZ, DE, HU, PL); Floxan® (ID); Floxika® (ID); Floxil® (AR, MX); Floxin® (CA); Floxstat® (BR, CO, CR, DO, EC, GT, HN, MX, PA, SV); Floxur® (IN); Girasid® (TR); Gyroflox® (DE); Hyflox® (TH); Inoflox® (PH, SG); Konovid® (TH); Kozoksin® (TR); Liflox® (ID); Loxinter® (ID); Maxifloxina® (DO); Medofloxine® (BG); Mefoxa® (ID); Megasin® (PT); Menefloks® (TR); Meneflox® (RO); Monoflocet® (FR); Novalid® (ID); Novecin® (JO, RO); Nufafloqo® (ID); Occidal® (TH); Octin® (ZA); Ocuflox® (AU, CA, MX); Ofcin® (SG); Ofkozin® (TR); Oflin® (IN); Oflocee® (TH); Oflocet® (FR, PT); Oflocet® [inj.] (PT); Oflocide® (TR); Oflocin® (IT); Oflodinex® (PL); oflodura® (DE); Oflohexal® (DE); Ofloks® (TR); Oflo TAD® (DE); Oflovir® (ES); Ofloxacin AbZ® (DE); Ofloxacin AL® (DE); Ofloxacina Poen® (AR); Ofloxacin Arcana® (AT); Ofloxacin® (GB, ID, RO); Ofloxacin Heumann® (DE); Ofloxacin Hoechst® (DE); Ofloxacino® (BR); Ofloxacin-ratiopharm® (AT, DE); Ofloxacin Stada® (DE); Ofloxacin-Teva® (IL); Ofloxan® (BR); Oflox® (AR, AT, BR, CL, CO, DE, EC, IL); Ofloxa® (TH); Oflox-AZU® (DE); Oflox Basics® (DE); Ofloxbeta® (DE); Ofloxin® (CZ, PL, RO, RU, TH); Ofloxin INF® (CZ); Oflox-Puren® (DE); Oflox-Sandoz® (DE); O-Flox® (TH); oflox von ct® (DE); Oflox-Wolff® (DE); Ostrid® (ID); Otoflox® (AR); Pharflox® (ID); Poncoquin® (ID); Qinolon® (PH, TH); Qipro® (ID); Quinoflox® (DO); Quinomed® (AR); Quinovid® (ID); Rafocilina® (AR); Rilox® (ID); Rutix® (BD); Seracin® (TH); Surnox® (ES); Surnox® [inj.] (ES); Tafloc® (ZA); Tariflox® (ID); Tarivid® (AT, BE, CH, CZ, DE, DK, FI, GB, HK, HU, ID, IE, IL, IN, JP, LU, NO, PT, RU, SE, SG, SI, TH, TR, ZA); Tarivid® [inj.] (AT, BE, DE, HU, ID, IE, IN, NL, NO, PL, SI, TR); Tarivid Ophtalmic® (ID, TH); Taroflox® (CZ); Trafloxal® (BE, NL); Uniflox® (YU); Urosin® (TR); Uro-Tarivid® (IL); Viotisone® (TH); Visiren® (YU); Zanocin® (HU, IN, PL, RO, RU, ZA)

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