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All about: Lomefloxacin Hydrochloride

Big Image Pronouncation: (low-MUH-FLOX-uh-sin HIGH-droe-KLOR-ide)
Class: Fluoroquinolone

Trade Names:
Maxaquin
- Tablets 400 mg

Mechanism of Action

Pharmacology

Interferes with microbial DNA synthesis.

Pharmacokinetics

Absorption

95% to 98% absorbed. T max is 0.8 to 1.4 h. C max is 0.8 mcg/mL, and AUC is 5.6 mcg•h/mL after 100 mg dose. Steady-state is achieved within 48 h. Food delays rate of absorption of drug; T max increased to 2 h and AUC is decreased 12%.

Distribution

About 10% protein bound.

Metabolism

Minimally metabolized. Major metabolite is glucuronide (about 9% of administered dose).

Elimination

The t ½ is about 8 h. About 65% of an oral dose is excreted unchanged in the urine. Mean renal Cl is 145 mL/min. About 10% is excreted unchanged in the feces.

Special Populations

Renal Function Impairment
CrCl 10 to 40 mL/min/1.73 m 2

AUC is increased 335%; t ½ is increased to 21 h. Dose adjustment is warranted.

CrCl less than 10 mL/min/1.73 m 2

AUC is increased 700%; t ½ is increased to 45 h. Dose adjustment is warranted.

Indications and Usage

Treatment of infections of the lower respiratory tract and urinary tract caused by susceptible organisms; prevention of UTIs in patients undergoing transurethral or transrectal procedures.

Contraindications

Standard considerations.

Dosage and Administration

Adults

PO 400 mg every day for 3 to 14 days.

Renal Function Impairment (CrCl 10 to 40 mL/min/1.73 m 2 )

Initial dose: 400 mg. Maintenance dose: 200 mg every day.

Surgical Prophylaxis
Adults

PO (Transurethral surgical procedures) 400 mg 2 to 6 h preoperatively.

Adults

PO (Transrectal prostate biopsy) 400 mg 1 to 6 h prior to procedure.

General Advice

  • Administer tablets with a full glass of water without regard to meals. Administer with food if GI upset occurs.
  • Administer lomefloxacin either 2 h before or 4 h after sucralfate, antacids containing magnesium or aluminum, didanosine-buffered tablets or pediatric powder, or other products containing iron or zinc.

Storage/Stability

Store tablets at controlled room temperature (59° to 77°F).

Drug Interactions

Antineoplastic agents

Decreased lomefloxacin serum levels.

Magnesium- or aluminum-containing antacids, iron salts, zinc salts, sucralfate, didanosine

Decreased oral absorption of lomefloxacin. Stagger administration times.

Probenecid

Decreased renal elimination of lomefloxacin.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (4%); dizziness (2%).

Dermatologic

Photosensitivity (2%).

GI

Nausea (4%); diarrhea, abdominal pain (1%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined; however, other fluoroquinolones have been shown to be excreted in breast milk.

Children

Safety and efficacy not established.

Elderly

Cl may be decreased.

Hypersensitivity

Serious and potentially fatal reactions have occurred. Discontinue if allergic reaction occurs.

Renal Function

Reduced Cl may occur; adjust dose accordingly.

Superinfection

Use may result in bacterial or fungal overgrowth.

Chronic bronchitis

Not indicated for empiric treatment of acute bacterial exacerbation of chronic bronchitis when Streptococcus pneumoniae is the probable pathogen.

Convulsions

CNS stimulation can occur; use with caution in patients with known or suspected CNS disorders.

Phototoxic reaction

Moderate to severe phototoxic reactions have occurred when exposed to direct, indirect, and ultraviolet light.

Pseudomembranous colitis

Consider in patients who develop diarrhea.

Tendonitis

Ruptures of the shoulder, hand, or Achilles tendon may occur. The risk may be increased in patients receiving corticosteroids, especially in the elderly.

Overdosage

Symptoms

Renal failure (severely decreased urine output, weight gain, confusion, dry flaky skin), tremor, seizures, dyspnea.

Patient Information

  • Advise patient to read patient information leaflet before starting therapy and with each refill.
  • Review dosing schedule and prescribed length of therapy with patient.
  • Advise patient that medication can be taken with a full glass of water without regard to meals but to take with food if GI upset occurs.
  • Advise patient to take each dose at least 12 h before exposure to the sun to reduce risk of photosensitivity reaction.
  • Advise patient that if a dose is missed to take as soon as remembered. However, if it is nearing the time for the next dose, to skip the dose and take the next dose at the regularly scheduled time.
  • Advise patient to take lomefloxacin either 2 h before or 4 h after sucralfate, antacids containing magnesium or aluminum, didanosine-buffered tablets or pediatric powder, or other products containing iron or zinc.
  • Remind patient to complete entire course of therapy, even if symptoms of infection have disappeared.
  • Advise patient to inform health care provider if infection does not appear to be improving or is getting worse.
  • Advise patient to drink fluids liberally (eg, eight 8 oz glasses of water daily) while taking this medication.
  • Advise patient to discontinue therapy and contact health care provider immediately if skin rash, hives, itching, shortness of breath, palpitations, fainting, or pain, tenderness or rupture of tendon occur.
  • Advise patient to report the following signs of superinfection to health care provider: black furry tongue, white patches in mouth, foul-smelling stools, vaginal itching or discharge.
  • Warn patient that diarrhea containing blood or pus may be a sign of a serious disorder and to seek medical care if noted and not treat at home.
  • Caution patient that drug may cause dizziness and lightheadedness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
  • Advise patient to avoid unnecessary exposure to direct and indirect sunlight or tanning lamps, to use sunscreen, and wear protective clothing to avoid photosensitivity reactions during therapy and for several days after stopping medication. Advise patient to discontinue therapy and notify health care provider if any of the following occur following exposure to sunlight or artificial UV light (eg, sunlamp): sensation of skin burning, redness, swelling, blistering; rash or itching.

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