Lomefloxacin

Pronunciation

(loe me FLOKS a sin)

U.S. Brand Names

Maxaquin®

Synonyms

Lomefloxacin Hydrochloride

Generic Available

Use

Lower respiratory infections, acute bacterial exacerbation of chronic bronchitis, and urinary tract infections caused by E. coli , K. pneumoniae , P. mirabilis , P. aeruginosa ; also has gram-positive activity including S. pneumoniae and some staphylococci; surgical prophylaxis (transrectal prostate biopsy or transurethral procedures)

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 lomefloxacin in animal studies; however, an increase in fetal loss was observed in one species. Based on limited data, quinolones are not expected to be a major human teratogen. 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

Excretion in breast milk unknown/not recommended

Contraindications

Hypersensitivity to lomefloxacin, any component of the formulation, or other members of the quinolone group (such as, nalidixic acid, oxolinic acid, cinoxacin, norfloxacin, and ciprofloxacin); avoid use in children <18 years of age due to association of other quinolones with transient arthropathies

Warnings/Precautions

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

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. Quinolones may exacerbate myasthenia gravis, use with caution (rare, potentially life-threatening weakness of respiratory muscles may occur).

Adverse Reactions

1% to 10%:

Central nervous system: Headache (3%), dizziness (2%)

Dermatologic: Photosensitivity (2%)

Gastrointestinal: Nausea (4%)

<1%: Abdominal pain, abnormal taste, allergic reaction, angina pectoris, anuria, arrhythmia, back pain, bradycardia, cardiac failure, chest pain, chills, coma, constipation, convulsions, cough, cyanosis, decreased heat tolerance, diaphoresis (increased), discoloration of tongue, dyspnea, dysuria, earache, edema, epistaxis, extrasystoles, facial edema, fatigue, flatulence, flu-like symptoms, flushing, gout, hematuria, hyperkinesia, hyper-/hypotension, hypoglycemia, increased fibrinolysis, leg cramps, malaise, myalgia, MI; paresthesia, purpura, rash, syncope, tachycardia, thirst, thrombocytopenia, tremor, urinary disorders, vertigo, vomiting, weakness, xerostomia; quinolones have been associated with tendon rupture and tendonitis

Overdosage/Toxicology

Symptoms of overdose include acute renal failure and seizures. Treatment is supportive; not removed by peritoneal or hemodialysis.

Drug Interactions

Inhibits CYP1A2 (weak)

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. Lomefloxacin should be administered 2 hours before or 4 hours after these agents.

Probenecid: May decrease renal secretion of lomefloxacin.

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

Ethanol/Nutrition/Herb Interactions

Food: Lomefloxacin peak serum levels may be prolonged if taken with food.

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

Mechanism of Action

Inhibits DNA-gyrase in susceptible organisms thereby inhibits relaxation of supercoiled DNA and promotes breakage of DNA strands. DNA gyrase (topoisomerase II), is an essential bacterial enzyme that maintains the superhelical structure of DNA and is required for DNA replication and transcription, DNA repair, recombination, and transposition.

Pharmacodynamics/Kinetics

Absorption: Well absorbed

Distribution: Vd: 2.4-3.5 L/kg; into bronchus, prostatic tissue, and urine

Protein binding: 20%

Half-life elimination: 5-7.5 hours

Excretion: Primarily urine (as unchanged drug)

Dosage

Oral: Adults:

Lower respiratory and urinary tract infections (UTI): 400 mg once daily for 10-14 days

Urinary tract infection (UTI) due to susceptible organisms:

Females:

Uncomplicated cystitis caused by Escherichia coli : 400 mg once daily for 3 successive days

Uncomplicated cystitis caused by Klebsiella pneumoniae , Proteus mirabilis , or Staphylococcus saprophyticus : 400 mg once daily for 10 successive days

Complicated UTI caused by Escherichia coli , Klebsiella pneumoniae , Proteus mirabilis , or Pseudomonas aeruginosa : 400 mg once daily for 14 successive days

Surgical prophylaxis: 400 mg 2-6 hours before surgery

Elderly: No dosage adjustment is needed for elderly patients with normal renal function

Dosing adjustment in renal impairment:

Clcr 11-39 mL/minute: Loading dose: 400 mg, then 200 mg every day

Hemodialysis: Same as above

Dietary Considerations

May be taken without regard to meals.

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. Take exactly as directed: at least 4 hours before or 8 hours after antacids or other drug products containing calcium, iron, or zinc. Take entire prescription even if feeling better. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. You may experience dizziness, lightheadedness, or confusion (use caution when driving or engaging in tasks that require alertness until response to drug is known); nausea or vomiting (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); or photosensitivity (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight). Discontinue use immediately and report to prescriber if inflammation, tendon pain, or allergic reaction occurs (itching urticaria, respiratory difficulty, facial edema, difficulty swallowing, loss of consciousness, tingling, chest pain, palpitations). Report palpitations or chest pain; CNS changes (excitability, seizures); persistent diarrhea or constipation; signs of infection (unusual fever or chills, vaginal itching or foul-smelling vaginal discharge, easy bruising or bleeding). Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Do not breast-feed.

Anesthesia and Critical Care Concerns/Other Considerations

It is recommended that fluoroquinolone treatment should be discontinued at the first sign of tendon pain or inflammation and that patients refrain from exercise until the diagnosis of tendonitis can be confidently excluded.

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

Dizziness is common; may cause sedation; quinolones reported to cause restlessness, confusion, depression, paranoia, euphoria, panic, and hallucinations

Mental Health: Effects on Psychiatric Treatment

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

Dosage Forms

Tablet: 400 mg

References

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.

Kovarik JM, Hoepelman AI, Smit JM, et al, "Steady-State Pharmacokinetics and Sputum Penetration of Lomefloxacin in Patients With Chronic Obstructive Pulmonary Disease and Acute Respiratory Tract Infections," Antimicrob Agents Chemother , 1992, 36(11):2458-61.

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

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

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

International Brand Names

Bareon® (JP); Chimono® (IT); Décalogiflox® (FR); Floxaquil® (PT); Logiflox® (FR); Lomacin® (MX); Lomaday® (RO); Lomebact® (IT); Lomef® (IN); Lomeflon® (JP); Lomeflox® (BD, DO); Lomflox® (IN, RU, SG); Loxina® (PT); Maxaquin® (BR, CH, IT, MX, PT, RO, RU, TH, ZA); Monoquin® (PT); Nor-Floxin® (SV); Ocacin® (ES, RU); Okacin® (AR, AT, BD, BE, BG, CH, CO, CZ, DE, DK, FI, IL, IT, LU, PL, RO, SG, TH); Okacyn® (GB, ZA); Omniquin® (ID); Ontop® (IN); Senifar® (DO); Uniquin® (AT, IT, PT, ZA)

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