Pronunciation:

(lee voe FLOKS a sin)

U.S. Brand Names:

Generic Available:

Canadian Brand Names:

Use:

Systemic: Treatment of mild, moderate, or severe infections caused by susceptible organisms. Includes the treatment of community-acquired pneumonia, including multidrug resistant strains of S. pneumoniae (MDRSP); nosocomial pneumonia; chronic bronchitis (acute bacterial exacerbation); acute maxillary sinusitis; urinary tract infection (uncomplicated or complicated), including acute pyelonephritis caused by E. coli; prostatitis (chronic bacterial); skin or skin structure infections (uncomplicated or complicated); prevention of inhalational anthrax (postexposure)

Ophthalmic: Treatment of bacterial conjunctivitis caused by susceptible organisms (Quixin™ 0.5% ophthalmic solution); treatment of corneal ulcer caused by susceptible organisms (Iquix® 1.5% ophthalmic solution)

Pregnancy Risk Factor:

Pregnancy Implications:

Lactation:

Contraindications:

Warnings/Precautions:

Systemic: Not recommended in children <18 years of age; CNS stimulation may occur (tremor, restlessness, confusion, and very rarely hallucinations or seizures); use with caution in patients with known or suspected CNS disorders or renal dysfunction; use caution to avoid possible photosensitivity reactions during and for several days following fluoroquinolone therapy

Rare cases of torsade de pointes have been reported in patients receiving levofloxacin. Risk may be minimized by avoiding use in patients with known prolongation of 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 or 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. Tendon inflammation and/or rupture has been reported; 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 levofloxacin use; discontinue if numbness, tingling, or weakness develops. Quinolones may exacerbate myasthenia gravis; use with caution (rare, potentially life-threatening weakness of respiratory muscles may occur).

Ophthalmic solution: For topical use only. Do not inject subconjunctivally or introduce into anterior chamber of the eye. Contact lenses should not be worn during treatment for bacterial conjunctivitis. Safety and efficacy in children <1 year of age (Quixin™) or <6 years of age (Iquix®) have not been established. Note: Indications for ophthalmic solutions are product concentration-specific and should not be used interchangeably.

Adverse Reactions:

1% to 10%:

Central nervous system: Dizziness, fever, headache, insomnia

Gastrointestinal: Abdominal pain, constipation, diarrhea, dyspepsia, nausea, vomiting

Ocular (with ophthalmic solution use): Decreased vision (transient), foreign body sensation, transient ocular burning, ocular pain or discomfort, photophobia

Respiratory: Dyspnea, pharyngitis

<1% (Limited to important or life-threatening):

Systemic: Acute renal failure; allergic reaction (including pneumonitis rash, pneumonitis, and anaphylaxis); agranulocytosis, anaphylactoid reaction, arrhythmia (including ventricular tachycardia and torsade de pointes), arthralgia, bradycardia, cardiac failure, dysphonia, eosinophilia, erythema multiforme, granulocytopenia, hemolytic anemia, hepatic failure, hypertension, INR/prothrombin time increased, intracranial hypertension, involuntary muscle contractions, jaundice, leukocytosis, leukopenia, leukorrhea, peripheral neuropathy, photosensitivity (<0.1%), pseudomembraneous colitis, pulmonary embolism, QTc prolongation, rhabdomyolysis, seizure, Stevens-Johnson syndrome, tachycardia, taste perversion, tendon rupture, transaminases increased, thrombocytopenia, tremor

Ophthalmic solution: Allergic reaction, lid edema, ocular dryness, ocular itching

Postmarketing and/or case reports: Systemic: EEG abnormalities, encephalopathy

Overdosage/Toxicology:

Symptoms of overdose include acute renal failure, seizures

Treatment should include GI decontamination and supportive care; not removed by peritoneal or hemodialysis

Drug Interactions:

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

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. Levofloxacin should be administered 2 hours before or 2 hours after these agents.

Probenecid: May decrease renal secretion of levofloxacin.

QTc-prolonging agents: Effects may be additive with levofloxacin. Avoid concurrent use with Class Ia and Class III antiarrhythmics, erythromycin, cisapride, antipsychotics, and cyclic antidepressants.

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

Stability:

Solution for injection:

Vial: Store at room temperature; protect from light. When diluted to 5 mg/mL in a compatible I.V. fluid, solution is stable for 72 hours when stored at room temperature; stable for 14 days when stored under refrigeration. When frozen, stable for 6 months; do not refreeze. Do not thaw in microwave or by bath immersion.

Premixed: Store at 25°C (77°F); protect from freezing and light.

Tablet, oral solution: Store at 25°C (77°F); excursions permitted to 15°C to 25°C (59°F to 77°F).

Ophthalmic solution: Store at 15°C to 25°C (59°F to 77°F).

Compatibility:

Y-site administration: Compatible: Amikacin, aminophylline, ampicillin, caffeine citrate, cefotaxime, cimetidine, clindamycin, dexamethasone sodium phosphate, dobutamine, dopamine, epinephrine, fentanyl, gentamicin, isoproterenol, lidocaine, linezolid, lorazepam, metoclopramide, morphine, oxacillin, pancuronium, penicillin G sodium, phenobarbital, phenylephrine, sodium bicarbonate, vancomycin. Incompatible: Acyclovir, alprostadil, furosemide, heparin, indomethacin, nitroglycerin, sodium nitroprusside. Variable (consult detailed reference): Insulin (regular)

Mechanism of Action:

Pharmacodynamics/Kinetics:

Absorption: Rapid and complete

Distribution: Vd: 1.25 L/kg; CSF concentrations ~15% of serum levels; high concentrations are achieved in prostate, lung, and gynecological tissues, sinus, saliva

Protein binding: 50%

Metabolism: Minimally hepatic

Bioavailability: 99%

Half-life elimination: 6-8 hours

Time to peak, serum: 1-2 hours

Excretion: Primarily urine (as unchanged drug)

Dosage:

Oral, I.V.: Adults:

Note: Sequential therapy (intravenous to oral) may be instituted based on prescriber's discretion.

Chronic bronchitis (acute bacterial exacerbation): 500 mg every 24 hours for at least 7 days

Inhalational anthrax: 500 mg every 24 hours for 60 days, beginning as soon as possible after exposure

Maxillary sinusitis (acute): 500 mg every 24 hours for 10-14 days

Pneumonia:

Community-acquired: 500 mg every 24 hours for 7-14 days or 750 mg every 24 hours for 5 days (efficacy of 5-day regimen for MDRSP not established)

Nosocomial: 750 mg every 24 hours for 7-14 days

Prostatitis (chronic bacterial): 500 mg every 24 hours for 28 days

Skin infections:

Uncomplicated: 500 mg every 24 hours for 7-10 days

Complicated: 750 mg every 24 hours for 7-14 days

Urinary tract infections:

Uncomplicated: 250 mg once daily for 3 days

Complicated, including acute pyelonephritis: 250 mg every 24 hours for 10 days

Ophthalmic:

Conjunctivitis (0.5% ophthalmic solution): Children 1 year and Adults:

Treatment day 1 and day 2: Instill 1-2 drops into affected eye(s) every 2 hours while awake, up to 8 times/day

Treatment day 3 through day 7: Instill 1-2 drops into affected eye(s) every 4 hours while awake, up to 4 times/day

Corneal ulceration (1.5% ophthalmic solution): Children 6 years and Adults:

Treatment day 1 through day 3: Instill 1-2 drops into affected eye(s) every 30 minutes to 2 hours while awake and ~4-6 hours after retiring.

Treatment day 4 to treatment completion: Instill 1-2 drops into affected eye(s) every 1-4 hours while awake.

Dosing adjustment in renal impairment: Administer first dose as indicated in patients with normal renal function, then adjust dose as follows:

Chronic bronchitis, acute maxillary sinusitis, uncomplicated skin infection, community-acquired pneumonia, chronic bacterial prostatitis, or inhalational anthrax:

Clcr 20-49 mL/minute: 250 mg every 24 hours

Clcr 10-19 mL/minute: 250 mg every 48 hours

Hemodialysis/CAPD: 250 mg every 48 hours

Uncomplicated UTI: No dosage adjustment required

Complicated UTI, acute pyelonephritis: Clcr 10-19 mL/minute: 250 mg every 48 hours

Complicated skin infection, community-acquired pneumonia, or nosocomial pneumonia:

Clcr 20-49 mL/minute: Administer 750 mg every 48 hours

Clcr 10-19 mL/minute: Administer 500 mg every 48 hours

Hemodialysis/CAPD: 250 mg every 48 hours

Administration:

Oral: Tablets may be administered without regard to meals. Oral solution should be administered 1 hour before or 2 hours after meals.

I.V.: Infuse 250-500 mg I.V. solution over 60 minutes; infuse 750 mg I.V. solution over 90 minutes. Too rapid of infusion can lead to hypotension. Avoid administration through an intravenous line with a solution containing multivalent cations (eg, magnesium, calcium).

Monitoring Parameters:

Dietary Considerations:

Patient Education:

Ophthalmic: Wash hands before instilling solution. Sit or lie down to instill. Open eye, look at ceiling, and instill prescribed amount of solution. Close eye and roll eye in all directions, and apply gentle pressure to inner corner of eye. Do not let tip of applicator touch eye; do not contaminate tip of applicator (may cause eye infection, eye damage, or vision loss). Temporary stinging or blurred vision may occur. Report persistent pain, burning, vision changes, swelling, itching, or worsening of condition. Discontinue medication and contact prescriber immediately if you develop a rash or allergic reaction. Do not wear contact lenses.

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

Dosage Forms:

Infusion [premixed in D5W] (Levaquin®): 250 mg (50 mL); 500 mg (100 mL); 750 mg (150 mL)

Injection, solution [preservative free] (Levaquin®): 25 mg/mL (20 mL, 30 mL)

Solution, ophthalmic:

Iquix®: 1.5% (5 mL)

Quixin™: 0.5% (5 mL) [contains benzalkonium chloride]

Solution, oral (Levaquin®): 25 mg/mL (480 mL) [contains benzyl alcohol]

Tablet (Levaquin®): 250 mg, 500 mg, 750 mg

Levaquin® Leva-Pak: 750 mg (5s)

International Brand Names: