Sparfloxacin

Pronunciation: spar-FLOX-ah-sin
Class: Fluoroquinolone

Trade Names:
Zagam
- Tablets 200 mg

Pharmacology

Interferes with microbial DNA synthesis.

Pharmacokinetics

Absorption

Oral bioavailability of sparfloxacin is 92%; antacids containing aluminum hydroxide or magnesium hydroxide reduce bioavailability by as much as 50%. C max is approximately 1.3 mcg/mL; AUC is approximately 34 mcg•h/mL; T max is between 3 and 6 h. Oral absorption is unaffected by milk, food, or high fat meals.

Distribution

Sparfloxacin distributes well into the body. Vd is approximately 3.9 L/kg. Sparfloxacin has low protein binding (approximately 45%).

Metabolism

Sparfloxacin is metabolized by the liver and does not interfere with CYP-450.

Elimination

Total Cl is approximately 11.4 L/h; renal Cl is approximately 1.5 L/h. Ten percent of an orally administered dose is excreted in urine. Sparfloxacin t ½ is about 20 h.

Special Populations

Renal Function Impairment

In CrCl below 50 mL/min, t ½ is lengthened. Single or multiple doses in patients with varying degrees of renal impairment typically produce plasma concentrations that are twice those observed in healthy subjects.

Hepatic Function Impairment

The kinetics of sparfloxacin are not altered in patients with mild to moderate hepatic impairment without cholestasis.

Indications and Usage

Treatment of community acquired pneumonia or bacterial exacerbation of chronic bronchitis caused by susceptible organisms.

Contraindications

History of hypersensitivity or photosensitivity reactions; drugs known to prolong the electrocardiogram QT c interval such as disopyramide and amiodarone or patients with underlying QT c prolongation (torsades de pointes has been reported in such patients); patients whose lifestyle or occupation prevents avoidance of sun, bright natural light, or ultraviolet rays while taking this drug and for 5 days after treatment is stopped; tendonitis or tendon rupture associated with quinolone use.

Dosage and Administration

Adults

PO 400 mg on day 1 (loading dose) followed by 200 mg every day for a total 10 days of therapy.

Renal Function Impairment (CrCl less than 50 mL)
Adults

PO 400 mg on day 1 (loading dose) followed by 200 mg every 48 h for a total of 9 days of therapy.

Tuberculosis
Adults

PO 200 mg/day (max, 200 mg/day).

Storage/Stability

Store at room temperature in tightly closed container.

Drug Interactions

Aluminum-magnesium antacids, sucralfate, zinc, iron salts

Reduced absorption leading to lower bioavailability and efficacy.

Bepridil, cisapride, erythromycin, pentamidine, phenothiazines and related antipsychotics, tricyclic antidepressants, any other drug known to prolong the QT c interval

Increased risk of torsades de pointes or other malignant ventricular arrhythmias.

Laboratory Test Interactions

False-negative results for Mycobacterium tuberculosis cultures.

Adverse Reactions

Cardiovascular

QT c prolongation (possibly leading to serious ventricular arrhythmias); vasodilation.

CNS

Headache; dizziness; insomnia; somnolence.

Dermatologic

Photosensitivity; pruritus; rash.

EENT

Taste perversion.

GI

Diarrhea; nausea; dyspepsia; abdominal pain; dry mouth; vomiting; flatulence.

Genitourinary

Vaginal moniliasis.

Miscellaneous

Asthenia.

Precautions

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Hypersensitivity

Acute anaphylactic reactions and serious dermatologic hypersensitivity reactions have been reported. Stop sparfloxacin if a rash or any other sign of photosensitivity develops.

Renal Function

Dose adjustment necessary if CrCl is less than 50 mL/min.

Superinfection

Use of antibiotics may result in bacterial or fungal overgrowth.

Phototoxicity

Moderate to severe phototoxic reactions have been reported. Patients must avoid exposure to direct or indirect sunlight or other sources of UV light while taking this medication and for 5 days thereafter. Patients must discontinue therapy at first sign or symptom of a phototoxic reaction (eg, sensation of skin burning, redness, swelling, blistering, rash, itching, dermatitis).

Convulsions and toxic psychosis

CNS stimulation, lowering of the seizure threshold, and psychotic reactions have been reported. Use with caution in patients with seizures or other CNS disorders.

Pseudomembranous colitis

Consider possibility in patients with diarrhea.

Tendonitis

Inflammation and rupture of tendons has been associated with the use of fluoroquinolone antibiotics.

QT interval

May be prolonged in some patients.

Overdosage

Symptoms

Possible QT c prolongation.

Patient Information

  • Instruct patient to take medication as directed with a full glass of water without regard to meals.
  • Instruct patient that sparfloxacin may be taken with food or milk. However, mineral supplements, vitamins with iron, zinc calcium, and magnesium- and aluminum-containing antacids, and sucralfate should be taken 4 h after antibiotic administration.
  • Instruct patients to drink fluids liberally while taking medication.
  • Advise patient to avoid exposure to direct or indirect sunlight (including through glass, while using sunscreen or sunblocks, reflected sunlight, and cloudy weather) and exposure to artificial UV light during treatment with sparfloxacin and for at least 5 days after therapy. If exposure to sun cannot be avoided, patient should cover as much of the skin as possible with clothing.
  • Caution patient to discontinue sparfloxacin therapy at first sign or symptom of phototoxicity (eg, sensation of skin burning, redness, swelling, blisters, rash, itching, dermatitis) and to contact the primary care provider at once.
  • Advise patient who has experienced a phototoxic reaction to the medicine to avoid further exposure to sunlight or artificial UV light until completely recovered from the reaction or for 5 days following discontinuation of treatment, whichever is longer. In rare cases, reactions have recurred up to several weeks following discontinuation.
  • Advise patient not to drive, operate machinery, or engage in other activities that require mental alertness and coordination until reaction to sparfloxacin is known (eg, dizziness, light-headedness).
  • Instruct patient to discontinue medication and inform primary caregiver if pain or inflammation of a tendon is experienced and to rest and not exercise until tendonitis or tendon rupture has been ruled out.
  • Instruct patient to report these symptoms to health care provider: diarrhea, foul-smelling stools, stomatitis, vaginitis, black, furry appearance of tongue.
  • Instruct patient to discontinue the drug and to contact health care provider at the first sign of a rash or other allergic reaction.
  • Instruct patient to complete full course of therapy, even if symptoms of infection have resolved.
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