Loracarbef

Pronunciation

(lor a KAR bef)

U.S. Brand Names

Lorabid®

Generic Available

Canadian Brand Names

Lorabid®

Use

Infections caused by susceptible organisms involving the respiratory tract, acute otitis media, sinusitis, skin and skin structure, bone and joint, and urinary tract and gynecologic

Pregnancy Risk Factor

Lactation

Excretion in breast milk unknown/use caution

Contraindications

Hypersensitivity to loracarbef, any component of the formulation, or cephalosporins

Warnings/Precautions

Modify dosage in patients with severe renal impairment; prolonged use may result in superinfection; use with caution in patients with a previous history of hypersensitivity to other beta-lactam antibiotics (eg, penicillins, cephalosporins)

Adverse Reactions

1%:

Central nervous system: Headache (1% to 3%), somnolence (<2%)

Dermatologic: Rash (1% to 3%)

Gastrointestinal: Diarrhea (4% to 6%), nausea (2%), vomiting (1% to 3%), anorexia (<2%), abdominal pain (1%)

Genitourinary: Vaginitis (1%)

Respiratory: Rhinitis (2% to 6%)

<1%: Anaphylaxis, arthralgia, candidiasis, cholestasis, eosinophilia, hemolytic anemia, interstitial nephritis, jaundice, nephrotoxicity with transient elevations of BUN/creatinine, nervousness, neutropenia, positive Coombs' test, pruritus, pseudomembranous colitis, seizure (with high doses and renal dysfunction), serum sickness-like reaction, slightly increased AST/ALT, Stevens-Johnson syndrome, thrombocytopenia, urticaria

Overdosage/Toxicology

Symptoms of overdose include abdominal discomfort and diarrhea. Treatment is supportive.

Drug Interactions

Increased effect: Probenecid may decrease cephalosporin elimination; may cause prolongation of PT/INR in patients receiving warfarin

Increased toxicity: Furosemide, aminoglycosides may be a possible additive to nephrotoxicity

Ethanol/Nutrition/Herb Interactions

Food: Administration with food decreases and delays the peak plasma concentration.

Stability

Suspension may be kept at room temperature for 14 days

Mechanism of Action

Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin binding proteins (PBPs); inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. It is thought that beta-lactam antibiotics inactivate transpeptidase via acylation of the enzyme with cleavage of the CO-N bond of the beta-lactam ring. Upon exposure to beta-lactam antibiotics, bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.

Pharmacodynamics/Kinetics

Absorption: Rapid

Half-life elimination: ~1 hour

Time to peak, serum: ~1 hour

Excretion: Clearance: Plasma: ~200-300 mL/minute

Dosage

Oral:

Children:

Acute otitis media: 15 mg/kg twice daily for 10 days

Pharyngitis and impetigo: 7.5-15 mg/kg twice daily for 10 days

Adults:

Uncomplicated urinary tract infections: 200 mg once daily for 7 days

Skin and soft tissue: 200-400 mg every 12-24 hours

Uncomplicated pyelonephritis: 400 mg every 12 hours for 14 days

Upper/lower respiratory tract infection: 200-400 mg every 12-24 hours for 7-14 days

Dosing comments in renal impairment:

Clcr 10-49 mL/minute: 50% of usual dose at usual interval or usual dose given half as often

Clcr<10 mL/minute: Administer usual dose every 3-5 days

Hemodialysis: Doses should be administered after dialysis sessions

Administration

Take on an empty stomach at least 1 hour before or 2 hours after meals. Finish all medication. Shake suspension well before using.

Dietary Considerations

Should be taken on an empty stomach at least 1 hour before or 2 hours after meals.

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, preferably on an empty stomach, 1 hour before or 2 hours after meals. Take entire prescription even if feeling better. Shake suspension well before using. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. You may experience nausea, vomiting, or anorexia (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report immediately any signs of skin rash, joint or back pain, or respiratory difficulty. Report unusual fever, chills, vaginal itching or foul-smelling vaginal discharge, or easy bruising or bleeding. Breast-feeding precaution: Consult prescriber if breast-feeding.

Nursing Implications

Finish all medication; shake suspension well before using

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause nervousness; cephalosporins reported to cause illusions, delusion, depersonalization, and euphoria

Mental Health: Effects on Psychiatric Treatment

May cause neutropenia; use caution with clozapine and carbamazepine

Dosage Forms

Capsule: 200 mg, 400 mg

Powder for oral suspension: 100 mg/5 mL (100 mL); 200 mg/5 mL (100 mL) [strawberry bubble gum flavor]

References

DeSante KA and Zeckel ML, "Pharmacokinetic Profile of Loracarbef," Am J Med , 1992, 92(6A):16S-9S.

Force RW and Nahata MC, "Loracarbef: A New Orally Administered Carbacephem Antibiotic," Ann Pharmacother , 1993, 27(3):321-9.

Foshee WS, "Loracarbef (LY163892) Versus Amoxicillin-Clavulanate in the Treatment of Acute Otitis Media With Effusion," J Pediatr , 1992, 120(6):980-6.

Nelson JD, Shelton S, and Kusmiesz H, "Pharmacokinetics of LY163892 in Infants and Children," Antimicrob Agents Chemother , 1988, 32(11):1738-9.

Schatz BS, Karavokiros KT, Taeubel MA, et al, "Comparison of Cefprozil, Cefpodoxime Proxetil, Loracarbef, Cefixime, and Ceftibuten," Ann Pharmacother , 1996, 30(3):258-68.

International Brand Names

Carbac® (MX); Lorabid™ (CA); Lorabid® (MX, RO, SE, TR, ZA); Lorafem® (DE); Lorax® (NL)

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