Sparfloxacin

Pronunciation

U.S. Brand Names

Zagam®

Generic Available

Use

Treatment of adults with community-acquired pneumonia caused by C. pneumoniae , H. influenzae , H. parainfluenzae , M. catarrhalis , M. pneumoniae or S. pneumoniae ; treatment of acute bacterial exacerbations of chronic bronchitis caused by C. pneumoniae , E. cloacae , H. influenzae , H. parainfluenzae , K. pneumoniae , M. catarrhalis , S. aureus or S. pneumoniae

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 reported with sparfloxacin in animal studies. 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

Enters breast milk/not recommended

Contraindications

Hypersensitivity to sparfloxacin, any component of the formulation, or other quinolones; a concurrent administration with drugs which increase the QT interval including amiodarone, bepridil, bretylium, cisapride, disopyramide, furosemide, procainamide, quinidine, sotalol, albuterol, chloroquine, halofantrine, phenothiazines, prednisone, and tricyclic antidepressants

Warnings/Precautions

Not recommended in children <18 years of age, other quinolones have caused transient arthropathy in children; CNS stimulation may occur (tremor, restlessness, confusion, and very rarely hallucinations or seizures); use with caution in patients with known or suspected CNS disorder or renal dysfunction; prolonged use may result in superinfection. Moderate to severe photosensitivity reactions may occur in patients exposed to direct or indirect sunlight, or to artificial ultraviolet light. Patients should avoid unnecessary sunlight exposure during treatment and for 5 days following therapy. Pseudomembranous colitis may occur and should be considered in patients who present with diarrhea. Tendon inflammation and/or rupture have been reported with other quinolone antibiotics. Risk may be increased with concurrent corticosteroids, particularly in the elderly. Discontinue at first sign of tendon inflammation or pain.

Severe hypersensitivity reactions, including anaphylaxis, have occurred with quinolone therapy. If an allergic reaction occurs (itching, urticaria, dyspnea, facial edema, loss of consciousness, tingling, cardiovascular collapse), discontinue drug immediately. Although quinolones may exacerbate myasthenia gravis, sparfloxacin appears to be an exception; caution is still warranted.

Adverse Reactions

1% to 10%:

Cardiovascular: QTc interval prolongation (1%), vasodilation (1%)

Central nervous system: Insomnia (2%), dizziness (2%), headache (4%)

Dermatologic: Photosensitivity reaction (8%; severe <1%), pruritus (2%)

Gastrointestinal: Diarrhea (5%), dyspepsia (2%), nausea (4%), abdominal pain (2%), vomiting (1%), flatulence (1%), taste perversion (2%)

Hepatic: Increased LFTs

<1% (Limited to important or life-threatening): Allergic reaction, anaphylactoid reaction, anemia, angina pectoris, angioedema, anxiety, arrhythmia, asthma, atrial fibrillation, atrial flutter, complete AV block, confusion, dry mouth, dyspnea, ecchymosis, eosinophilia, exfoliative dermatitis, hallucinations, leukopenia, migraine, postural hypotension, rash, sleep disorder, vertigo

Postmarketing and/or case reports: Agranulocytosis, anaphylactic shock, cerebral thrombosis, erythema nodosum, hepatic failure, hepatic necrosis, interstitial pneumonia, manic reaction, myasthenia gravis (exacerbation), pancytopenia, psychosis, renal failure, rhabdomyolysis, seizure, Stevens-Johnson syndrome, tendon rupture, tendonitis, torsade de pointes, toxic epidermal necrolysis, vasculitis

Overdosage/Toxicology

Symptoms include acute renal failure and seizures. Treatment consists of GI decontamination and supportive care; it is not known if sparfloxacin is dialyzable.

Drug Interactions

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

Probenecid: May decrease renal secretion of sparfloxacin.

QTc-prolonging agents: Effects may be additive with sparfloxacin. Avoid concurrent use with Class Ia and Class III antiarrhythmics, erythromycin, cisapride, antipsychotics, and cyclic antidepressants.

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

Ethanol/Nutrition/Herb Interactions

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

Mechanism of Action

Inhibits DNA-gyrase in susceptible organisms; inhibits relaxation of supercoiled DNA and promotes breakage of double-stranded DNA

Pharmacodynamics/Kinetics

Absorption: Unaffected by food or milk; reduced ~50% by concurrent administration of aluminum- and magnesium-containing antacids

Distribution: Widely throughout the body; Vd: 3.9 L/kg

Protein binding: 45%

Metabolism: Hepatic, primarily by phase II glucuronidation

Half-life elimination: Mean terminal: 20 hours (range: 16-30 hours)

Time to peak, serum: 3-5 hours

Excretion: Urine (50%; ~10% as unchanged drug); feces (50%)

Dosage

Adults: Oral:

Loading dose: 400 mg on day 1

Maintenance: 200 mg/day for 10 days total therapy

Dosing adjustment in renal impairment: Clcr<50 mL/minute: Administer 400 mg on day 1, then 200 mg every 48 hours for a total of 9 days of therapy (total 6 tablets)

Administration

May be taken without regard to meals, however, should be administered at the same time each day. Antacids containing aluminum or magnesium; products containing iron, zinc, or calcium; and sucralfate and didanosine should all be given >4 hours after sparfloxacin.

Monitoring Parameters

Evaluation of organ system functions (renal, hepatic, ophthalmologic, and hematopoietic) is recommended periodically during therapy; the possibility of crystalluria should be assessed; WBC and signs and symptoms of infection

Dietary Considerations

May be taken without regard to meals; should be taken at the same time each day.

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 as directed, at the same time each day - do not take with antacids. Take entire prescription even if feeling better, if dose is missed take as soon as possible, do not double doses. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. May cause dizziness, lightheadedness, or anxiety (use caution when driving or engaging in tasks that require alertness until response to drug is known); nausea, vomiting, or dry mouth (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); photosensitivity (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight during and for several days following therapy). If inflammation or tendon pain occurs, discontinue use immediately and report to prescriber. If allergic reaction occurs (itching urticaria, respiratory difficulty, facial edema or difficulty swallowing, loss of consciousness, tingling, chest pain, palpitations), discontinue use immediately and report to prescriber. Report palpitations or chest pain; persistent diarrhea or constipation; or signs of superinfection (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

Sparfloxacin causes a dose-dependent QT prolongation. Coadministration of sparfloxacin with other drugs that also prolong the QT interval or induce bradycardia (eg, beta-blockers, amiodarone) should be avoided. Careful consideration should be given in the use of sparfloxacin in patients with cardiovascular disease, particularly in those with conduction abnormalities.

Cardiovascular Considerations

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Taste perversion.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause agitation, anxiety, insomnia, or delirium; quinolones reported to cause restlessness, hallucinations, euphoria, depression, panic, and paranoia

Mental Health: Effects on Psychiatric Treatment

May cause leukopenia; use caution with clozapine and carbamazepine. Contraindicated with TCAs, phenothiazines, and ziprasidone.

Dosage Forms

Tablet [film coated]: 200 mg

References

Aubier M, Verster R, Regamey C, et al, "Once-Daily Sparfloxacin Versus High-Dosage Amoxicillin in the Treatment of Community-Acquired, Suspected Pneumococcal Pneumonia in Adults. Sparfloxacin European Study Group," Clin Infect Dis , 1998, 26(6):1312-20.

Ballow CH, Jones RN, Johnson DM, et al, "Comparative In Vitro Assessment of Sparfloxacin Activity and Spectrum Using Results From Over 14,000 Pathogens Isolated at 190 Medical Centers in the USA. SPAR Study Group," Diagn Microbiol Infect Dis , 1997, 29(3):173-86.

DeAbate CA, Henry D, Bensch G, et al, "Sparfloxacin vs Ofloxacin in the Treatment of Acute Bacterial Exacerbations of Chronic Bronchitis: A Multicenter, Double-Blind, Randomized, Comparative Study. Sparfloxacin Multicenter ABECB Study Group," Chest , 1998, 114(1):120-30.

Goa KL, Bryson HM, and Markham A, "Sparfloxacin. A Review of Its Antibacterial Activity, Pharmacokinetic Properties, Clinical Efficacy, and Tolerability in Lower Respiratory Tract Infections," Drugs , 1997, 53(4):700-25.

Henry D, Ellison W, Sullivan J, et al, "Treatment of Community-Acquired Acute Uncomplicated Urinary Tract Infection With Sparfloxacin Versus Ofloxacin. The Sparfloxacin Multi Center UUTI Study Group," Antimicrob Agents Chemother , 1998, 42(9):2262-6.

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.

Jones RN, Ballow CH, Schentag JJ, et al, " In Vitro Evaluation of Sparfloxacin Activity and Spectrum Against 24,940 Pathogens Isolated in the United States and Canada, the Final Analysis," Diagn Microbiol Infect Dis , 1998, 31(1):313-25.

Martin SJ, Meyer JM, Chuck SK, et al, "Levofloxacin and Sparfloxacin: New Quinolone Antibiotics," Ann Pharmacother , 1998, 32(3):320-36.

Pfaller MA and Jones RN, "Comparative Antistreptococcal Activity of Two Newer Fluoroquinolones, Levofloxacin and Sparfloxacin," Diagn Microbiol Infect Dis , 1997, 29(3):199-201.

"Sparfloxacin and Levofloxacin," Med Lett Drugs Ther , 1997, 39(999):41-3.

Stein GE and Havlichek DH, "Sparfloxacin: Potential Clinical and Economic Impact in the Treatment of Respiratory Infections," Pharmacotherapy , 1997, 17(6):1139-47.

Trautman M, Ruhnke M, Borner K, et al, "Pharmacokinetics of Sparfloxacin and Serum Bactericidal Activity Against Pneumococci," Antimicrob Agents Chemother , 1996, 40(3):776-9.

Zix JA, Geerdes-Fenge HF, Rau M, et al, "Pharmacokinetics of Sparfloxacin and Interaction With Cisapride and Sucralfate," Antimicrob Agents Chemother , 1997, 41(8):1668-72.

International Brand Names

Neospectra® (BD); Newspar® (ID); Redspar® (ID); Resflok® (ID); Spacin® (BD); Spara® (JP); Spardac® (IN); Spargam® (JO, RO); Sparlox® (BD); Sparos® (ID); Sparx® (IN, ZA); Zagam® (LU, PL)

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