Antibiotic, Quinolone

Treatment of mild to moderate community-acquired pneumonia, acute bacterial exacerbation of chronic bronchitis, and acute bacterial sinusitis

C

No adequate or well-controlled studies in pregnant women. Should be used during pregnancy only when the potential benefit justifies the potential risk to the fetus. Moxifloxacin may be excreted in human breast milk. Breast-feeding is not recommended.

Hypersensitivity to moxifloxacin, other quinolone antibiotics, or any component

Use with caution in patients with significant bradycardia or acute myocardial ischemia. Moxifloxacin causes a dose-dependent Q-T prolongation. Coadministration of moxifloxacin with other drugs that also prolong the Q-T interval or induce bradycardia (eg, beta-blockers, amiodarone) should be avoided. Careful consideration should be given in the use of moxifloxacin in patients with cardiovascular disease, particularly in those with conduction abnormalities. Safety and effectiveness in pediatric patients (<18 years of age) have not been established. Experience in immature animals has resulted in permanent arthropathy. Use with caution in individuals at risk of seizures (CNS disorders or concurrent therapy with medications which may lower seizure threshold). Discontinue in patients who experience significant CNS adverse effects (dizziness, hallucinations, suicidal ideation or actions). Not recommended in patients with moderate to severe hepatic insufficiency. Use with caution in diabetes; glucose regulation may be altered.

1% to 10%:

Central nervous system: Dizziness (3%), headache (2%)

Gastrointestinal: Nausea (8%), diarrhea (6%), abdominal pain (2%), vomiting (2%), dyspepsia (1%), taste perversion (1%)

Hepatic: Abnormal liver function test (1%)

<1% (Limited to important or life-threatening symptoms): Asthenia, moniliasis, pain, malaise, allergic reaction, leg pain, back pain, fever, chills, chest pain, palpitation, vasodilation, tachycardia, hypertension, peripheral edema, hypotension, insomnia, nervousness, anxiety, confusion, hallucinations, depersonalization, hypertonia, incoordination, somnolence, tremor, vertigo, paresthesia, dry mouth, constipation, anorexia, stomatitis, gastritis, glossitis, cholestatic jaundice, GGTP increased, decreased prothrombin time, increased prothrombin time, thrombocytopenia, eosinophilia, leukopenia, increased amylase, hyperglycemia, hyperlipidemia, increased LDH, arthralgia, myalgia, asthma, dyspnea, increased cough, pneumonia, pharyngitis, rhinitis, sinusitis, rash, pruritus, sweating, urticaria, dry skin, tinnitus, amblyopia, vaginitis, cystitis, abnormal renal function, Q-T prolongation (see Warnings/Precautions)

Potential symptoms of overdose may include CNS excitation, seizures, QT prolongation, and arrhythmias (including torsade de pointes). Patients should be monitored by continuous EKG in the event of an overdose. Management is supportive and symptomatic. Not removed by dialysis.

Drugs which prolong QT interval (including Class Ia and Class III antiarrhythmics, erythromycin, cisapride, antipsychotics, and cyclic antidepressants) are contraindicated with moxifloxacin.

Metal cations (magnesium, aluminum, iron, and zinc) bind quinolones in the gastrointestinal tract and inhibit absorption (by up to 98%). Antacids, electrolyte supplements, sucralfate, quinapril, and some didanosine formulations should be avoided. Moxifloxacin should be administered 4 hours before or 8 hours after these agents.

Antineoplastic agents may decrease the absorption of quinolones.

Cimetidine, and other H₂ antagonists may inhibit renal elimination of quinolones.

Digoxin levels may be increased in some patients by quinolones; monitor for increased effect/concentrations.

Foscarnet has been associated with an increased risk of seizures with some quinolones.

Loop diuretics: Serum levels of some quinolones are increased by loop diuretic administration. May diminish renal excretion.

NSAIDs: The CNS stimulating effect of some quinolones may be enhanced, resulting in neuroexcitation and/or seizures. This effect has not been observed with moxifloxacin.

Probenecid: Blocks renal secretion of quinolones, increasing concentrations.

Warfarin: The hypoprothrombinemic effect of warfarin is enhanced by some quinolone antibiotics. No significant effect has been demonstrated for moxifloxacin, however, monitoring of the INR during concurrent therapy is recommended by the manufacturer.

Store at 25°C (77°F)

Moxifloxacin is a DNA gyrase inhibitor, and also inhibits topoisomerase IV. DNA gyrase (topoisomerase II) 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; inhibition is bactericidal.

Absorption: Well absorbed; not affected by administration with a high fat meal or yogurt

Distribution: V_d: 1.7 to 2.7 L/kg; tissue concentrations often exceed plasma concentrations in respiratory tissues, alveolar macrophages, and sinus tissues

Protein binding: 50%

Metabolism: Hepatic, via glucuronide (14%) and sulfate (38%) conjugation

Bioavailability: 90%

Half-life: 12 hours

Elimination: Approximately 45% excreted as unchanged drug (20% in urine and 25% in feces). Sulfate conjugates are excreted in the feces, glucuronide conjugates are excreted in the urine.

Adult: Oral:

Chronic bronchitis, acute bacterial exacerbation: 400 mg every 24 hours for 5 days

Dosage adjustment in renal impairment: No dosage adjustment is required.

Dosage adjustment in hepatic impairment: No dosage adjustment is required in mild hepatic insufficiency (Child-Pugh Class A). Not recommended in patients with moderate to severe hepatic insufficiency.

Elderly: No dosage adjustments are required based on age.

WBC, signs of infection

No information available to require special precautions

No effects or complications reported

May be taken with or without food. Drink plenty of fluids. Avoid direct exposure to direct sunlight during therapy and for several days following. Do not take antacids within 4 hours before or 8 hours after dosing. Contact your physician immediately if signs of allergy occur. Contact your physician immediately if signs of tendon inflammation or pain occur. Do not discontinue therapy until your course has been completed. Take a missed dose as soon as possible, unless it is almost time for your next dose.

Tablet: 400 mg

Balfour JA and Wiseman LR, "Moxifloxacin," Drugs, 1999, 57(3):363-73.

Blondeau JM, "Expanded Activity and Utility of the New Fluoroquinolones: A Review," Clinical Therapeutics, 1999, 21(1):3-40.

"Gatifloxacin and Moxifloxacin: Two New Fluoroquinolones," The Medical Letter, 2000, Vol 42, 1072:15.