No

Antibiotic, Quinolone

Uncomplicated urinary tract infections and cystitis caused by susceptible gram-negative and gram-positive bacteria; sexually transmitted disease (eg, uncomplicated urethral and cervical gonorrhea) caused by N. gonorrhoeae; prostatitis due to E. coli; ophthalmic solution for conjunctivitis

C

Known hypersensitivity to quinolones

Not recommended in children <18 years of age; other quinolones have caused transient arthropathy in children; CNS stimulation may occur which may lead to tremor, restlessness, confusion, and very rarely to hallucinations or convulsive seizures; use with caution in patients with known or suspected CNS disorders; has rarely caused ruptured tendons (discontinue immediately with signs of inflammation or tendon pain)

1% to 10%:

Central nervous system: Headache (2.7%), dizziness (1.8%), fatigue

Gastrointestinal: Nausea (2.8%)

<1%: Somnolence, depression, insomnia, fever, pruritus, hyperhidrosis, erythema, rash, abdominal pain, dyspepsia, constipation, flatulence, heartburn, xerostomia, diarrhea, vomiting, loose stools, anorexia, bitter taste, GI bleeding, increased liver enzymes, back pain, ruptured tendons, weakness, increased serum creatinine/BUN, acute renal failure, anaphylactoid reactions, angioedema, arthralgia, arthritis, dyspnea, myalgia, urticaria, vasculitis, hepatitis, jaundice, cholestatic jaundice, pancreatitis, pseudomembraneous colitis, hemolytic anemia (sometimes associated with G-6-PD deficiency), leukopenia, neutropenia, thrombocytopenia, exacerbation of myasthenia gravis, tendonitis, ataxia, seizures, myoclonus, Guillain-Barré syndrome, paresthesias, peripheral neuropathy, confusion, psychotic reactions, exfoliative dermatitis, photosensitivity, Stevens-Johnson syndrome, erythema multiforme, toix epidermal necrolysis, diplopia, transient hearing loss, tinnitus

Symptoms of overdose include acute renal failure, seizures

Following GI decontamination, use supportive measures

CYP1A2 and 3A3/4 enzyme inhibitor

Increased toxicity/serum levels: Quinolones cause increased levels or toxicity of digoxin, caffeine, warfarin, cyclosporine, and possibly theophylline. Cimetidine and probenecid increase quinolone levels.

Norfloxacin 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

Absorption: Oral: Rapid, up to 40%

Distribution: Crosses the placenta; small amounts appear in breast milk

Protein binding: 15%

Metabolism: In the liver

Half-life: 4.8 hours (can be higher with reduced glomerular filtration rates)

Time to peak serum concentration: Within 1-2 hours

Elimination: In urine and feces (30%)

Ophthalmic: Children >1 year and Adults: Instill 1-2 drops in affected eye(s) 4 times/day for up to 7 days

Oral: Adults:

Urinary tract infections: 400 mg twice daily for 3-21 days depending on severity of infection or organism sensitivity; maximum: 800 mg/day

Uncomplicated gonorrhea: 800 mg as a single dose (CDC recommends as an alternative regimen to ciprofloxacin or ofloxacin)

Prostatitis: 400 mg every 12 hours for 4 weeks

Dosing interval in renal impairment:

Cl_cr 10-30 mL/minute: Administer every 24 hours

Cl_cr <10 mL/minute: Do not use

Decreases absorption with food; should be administered on an empty stomach with water

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

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

No information available to require special precautions

No effects or complications reported

Oral: Take per recommended schedule, preferably on empty stomach (1 hour before or 2 hours after meals). Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). Take complete prescription; do not skip doses. Do not take with antacids. You may experience dizziness, lightheadedness; use caution when driving or engaging in tasks that require alertness until response to drug is known. Small frequent meals and frequent mouth care may reduce nausea or vomiting. You may experience photosensitivity; use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight. Report persistent diarrhea or GI disturbances; excessive sleepiness or agitation; tremors; rash; pain, inflammation, or rupture of tendon; or changes in vision. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Do not breast-feed.

Ophthalmic: Tilt head back and instill 1-2 drops in affected eye 4 times a day for length of time prescribed. Do not allow tip of applicator to touch eye or any contaminated surface. Do not wear contact lenses if being treated for a bacterial eye infection.

Hold antacids, sucralfate for 3-4 hours after giving

Solution, ophthalmic: 0.3% [3 mg/mL] (5 mL)

Tablet: 400 mg

Hooper DC and Wolfson JS, "Fluoroquinolone Antimicrobial Agents," N Engl J Med, 1991, 324(6):384-94.

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

Nilsson-Ehle I and Ljungberg B, "Quinolone Disposition in the Elderly: Practical Implications," Drugs Aging, 1991, 1(4):279-88.

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.