Trade Names:Iquix- Solution, ophthalmic 1.5%
Trade Names:Levaquin- Tablets 250 mg- Tablets 500 mg- Tablets 750 mg- Solution, oral 25 mg/mL- Injection, solution, concentrate 500 mg (25 mg/mL)- Injection, solution, concentrate 750 mg (25 mg/mL)- Injection, solution (premix) 250 mg (5 mg/mL)- Injection, solution (premix) 500 mg (5 mg/mL)- Injection, solution (premix) 750 mg (5 mg/mL)
Trade Names:Quixin- Solution, ophthalmic 0.5% (5 mg/mL)
Interferes with microbial DNA synthesis.
T max is 1 to 2 h. Food slightly prolongs T max (1 h) and decreases C max 14%. Can be administered with or without food. About 99% bioavailable. Steady state is reached within 48 h following 500 mg dose. C max is 5.7 mcg/mL and C min is 0.5 mcg/mL following multiple oral doses of 500 mg; for multiple doses of 750 mg, C max is 8.6 mcg/mL and C min is 1.1 mcg/mL.Oral solution
Peak concentration decreased 25% when taken with food. Administer 1 h before or 2 h after eating.Injection
C max is about 6.2 mcg/mL after 500 mg dose infused over 60 min and about 11.5 mcg/mL after 750 mg dose infused over 90 min. Steady state is reached within 48 h following a once-daily (500 or 750 mg) regimen.
Oral and IV formulations are equivalent in AUC; therefore, route of administration is interchangeable.
Vd is 74 to 112 L. Protein binding is approximately 24% to 38%.
Undergoes limited metabolism. Desmethyl and N-oxide, the only metabolites identified in humans, have little relevant pharmacological activity.
Total body Cl is 144 to 226 mL/min. Renal Cl is 96 to 142 mL/min. Terminal half-life is 6 to 8 h.Oral
Primarily excreted as unchanged drug in urine (87%), less than 4% in the feces.
Cl is reduced and half-life prolonged in patients with CrCl less than 50 mL/min. Dosage adjustment required. Hemodialysis and peritoneal dialysis do not remove levofloxacin from the body.Hepatic Function Impairment
Pharmacokinetics not expected to be affected by hepatic function impairment.Children
Cl is increased in children 6 mo to 16 yr of age, resulting in lower plasma levels.
Treatment of acute bacterial exacerbation of chronic bronchitis, acute bacterial sinusitis, acute pyelonephritis, anthrax (inhalational, postexposure), chronic bacterial prostatitis, community-acquired pneumonia, complicated and uncomplicated skin and skin-structure infections, complicated and uncomplicated UTI, and nosocomial pneumonia caused by susceptible strains of specific microorganisms.Ophthalmic use
Treatment of conjunctivitis caused by susceptible strains of aerobic gram-positive and aerobic gram-negative microorganisms.
Disseminated gonococcal infections; traveler's diarrhea.
Hypersensitivity to fluoroquinolones, quinolone antibiotics, or any product component.
PO / IV 500 mg every 24 h for 7 days.Acute Bacterial SinusitisAdults
PO / IV 500 mg every 24 h for 10 to 14 days or 750 mg every 24 h for 5 days.Inhalational Anthrax (Postexposure)Adults and Children more than 50 kg and 6 mo of age and older
PO/IV 500 mg every 24 h for 60 days.Children less than 50 kg and 6 mo of age and older
PO 8 mg/kg (max, 250 mg/dose) every 12 h for 60 days.Chronic Bacterial ProstatitisAdults
PO / IV 500 mg every 24 h for 28 days.Community-Acquired PneumoniaAdults
PO / IV 500 mg every 24 h for 7 to 14 days, or 750 mg every 24 h for 5 days.Complicated UTIs; Acute PyelonephritisAdults
PO / IVComplicated UTIs caused by Escherichia coli , Klebsiella pneumoniae , or Proteus mirabilis , and acute pyelonephritis caused by E. coli , including cases with concurrent bacteremia
750 mg every 24 h for 5 days.Complicated UTIs caused by Enterococcus faecalis , Enterococcus cloacae , E. coli , K. pneumoniae , P. mirabilis , or Pseudomonas aeruginosa , and for acute pyelonephritis caused by E. coli
250 mg every 24 h for 10 days.Complicated Skin and Skin Structure Infections; Nosocomial PneumoniaAdults
PO / IV 750 mg every 24 h for 7 to 14 days.Uncomplicated Skin and Skin Structure InfectionsAdults
PO / IV 500 mg every 24 h for 7 to 10 days.Uncomplicated UTIsAdults
PO / IV 250 mg every 24 h for 3 days.Bacterial ConjunctivitisAdults and children 1 yr of age and older Quixin Days 1 and 2
Topical Instill 1 to 2 drops in affected eye(s) every 2 h while awake, up to 8 times daily.Days 3 through 7
Topical Instill 1 to 2 drops in affected eye(s) every 4 h while awake, up to 4 times daily.Iquix Days 1 through 3
Topical Instill 1 to 2 drops in the affected eye(s) every 30 min to 2 h while awake and approximately 4 and 6 h after retiring.Days 4 through treatment completion
Topical Instill 1 or 2 drops in the affected eye(s) every 1 to 4 h while awake.
Oral and IV routes of administration are interchangeable on a mg-to-mg basis.
Store at controlled room temperature (59° to 86°F).Injection
Store injection concentrate at controlled room temperature (59° to 86°F). Protect from light. Reconstituted injection is stable for 72 h when stored at or below 77°F, for 14 days if refrigerated at 41°F in plastic IV containers, or for 6 mo if frozen (−4°F). Thaw frozen container at room temperature (77°F) or under refrigeration (46°F). Do not force thawing by immersion in water or by microwave irradiation. Do not refreeze after initial thawing. Store premix at or below 77°F. Brief exposure up to 104°F does not adversely affect the product. Avoid excessive heat, and protect from freezing and light.Ophthalmic solution
Store at 59° to 77°F. Protect from freezing. Keep container tightly closed.
May decrease oral absorption of levofloxacin. Stagger administration times by at least 2 h.Antiarrhythmic agents (class Ia [eg, quinidine] and class III [eg, amiodarone])
Because of increased risk of life-threatening cardiac arrhythmias, including torsades de pointes, avoid coadministration of levofloxacin.Antidiabetic agents
Hyperglycemia or hypoglycemia may occur.Antineoplastic agents (eg, cytarabine, doxorubicin)
Antineoplastic agents may decrease levofloxacin absorption by altering the intestinal mucosa.Erythromycin, fluconazole, methadone, phenothiazines, tricyclic antidepressants, ziprasidone
Risk of life-threatening cardiac arrhythmias may be increased.NSAIDs
May increase risk of CNS stimulation and convulsive seizures.Warfarin
May increase bleeding.
May produce false-positive urine screening results for opiates using commercially available immunoassay kits.
Prolonged QT interval, tachycardia, torsades de pointes, vasodilatation (postmarketing).
Headache (6%); insomnia (4%); dizziness (3%); abnormal EEG, ageusia, anosmia, dysgeusia, dysphonia, encephalopathy, paranoia, parosmia, peripheral neuropathy, psychosis, suicide attempts and ideation (postmarketing).Ophthalmic
Headache (8% to 10%).
Rash (2%); pruritus (1%); bullous eruptions, including erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis; leukocytoclastic vasculitis; photosensitivity; phototoxicity (postmarketing).
Blurred vision, hypoacusis, reduced visual acuity, scotoma, tinnitus, visual disturbances including diplopia (postmarketing).Ophthalmic
Decreased/blurred vision, foreign body sensation, installation-site irritation/discomfort, ocular infection, ocular pain, pharyngitis, photophobia, throat irritation, transient ocular burning or discomfort (1% to 3%).
Nausea (7%); diarrhea (5%); constipation (3%); abdominal pain, dyspepsia, vomiting (2%).Ophthalmic
Taste disturbance (8% to 10%); diarrhea, dyspepsia, nausea (1% to 2%).
Vaginitis (1%); interstitial nephritis (postmarketing).
Aplastic anemia, eosinophilia, hemolytic anemia, leukopenia, pancytopenia (postmarketing).
Hepatic failure, hepatitis, jaundice (postmarketing).
Hypersensitivity reactions, sometimes fatal, including anaphylactic/anaphylactoid reactions, anaphylactic shock, angioneurotic edema, and serum sickness (postmarketing).
Increased muscle enzymes, prolonged INR and PT (postmarketing).
Injection-site reaction (1%).
Muscle injury and rupture, rhabdomyolysis, tendon rupture (postmarketing).
Dyspnea (1%); allergic pneumonitis (postmarketing).
Edema, chest pain, moniliasis (1%); multiorgan failure, pyrexia (postmarketing).Ophthalmic
Fever, infection (1% to 3%).
Fluoroquinolones, including levofloxacin, are associated with an increased risk of tendonitis and tendon rupture in patients of all ages. The risk is further increased in patients older than 60 yr of age, in patients taking corticosteroids, and in patients with kidney, heart, or lung transplants.
Category C .
Undetermined; however, other drugs in this class are excreted in breast milk.
Except for inhalational anthrax (postexposure), safety and efficacy have not been established in children.Inhalational anthrax (postexposure)
Safety and efficacy not established in children younger than 6 mo of age.Ophthalmic
Safety and efficacy not established in children younger than 1 yr of age.
Elderly patients are at increased risk for developing severe tendon disorder and severe and sometimes fatal hepatotoxicity. In addition, because elderly patients are more likely to have decreased renal function, use caution in dose selection and consider monitoring renal function.
Serious and potentially fatal reactions have occurred with drugs in this class. Discontinue drug if allergic reaction occurs.
Reduced Cl may occur; adjust dose downward accordingly in CrCl less than 50 mL/min. Refer to manufacturer's package insert for dose calculations.
Prolonged use may result in overgrowth of nonsusceptible organisms.
Moderate to severe reactions may occur; avoid excessive sunlight and ultraviolet light.
Levofloxacin has been associated with prolonged QT interval and infrequent cases of arrhythmia. Avoid in patients with known prolongation of QT interval or uncorrected hypokalemia, and in patients receiving class IA or III antiarrhythmic agents.
Disturbances of blood glucose, including symptomatic hyperglycemia and hypoglycemia, have been reported, usually in patients with diabetes receiving an oral hypoglycemic agent or insulin.
CNS stimulation can occur; use drug with caution in patients with known or suspected CNS disorders (eg, seizure disorders, psychoses).
Severe hepatotoxicity, including acute hepatitis and fatal events, has been reported during postmarketing experience.
Compared with controls, pediatric patients have experienced an increased incidence of musculoskeletal disorders (eg, arthralgia, arthritis, gait abnormalities, tendonopathy).
Rare cases resulting in dysesthesias, hypesthesias, paresthesias, and weakness have been reported.
Consider possibility in patients who develop diarrhea.
Clinical manifestations of serious and sometimes fatal reactions that have been reported with levofloxacin include acute hepatic necrosis or failure, acute renal insufficiency or failure, agranulocytosis, allergic pneumonitis, anemia (including hemolytic and aplastic), arthralgia, fever, hepatitis, interstitial nephritis, jaundice, leukopenia, myalgia, pancytopenia, rash, serum sickness, Stevens-Johnson syndrome, thrombocytopenia (including thrombotic thrombocytopenic purpura), toxic epidermal necrolysis, and vasculitis.
Low potential for acute toxicity.
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