Loracarbef

Antibiotic Class:

Second-Generation Cephalosporin (2^nd generation cephalosporin)

Antimicrobial Spectrum:

Staphylococcus aureus (methicillin susceptible), Coagulase negative Staphylococci, Streptococcus pneumoniae (penicillin susceptible), Streptococcus spp. Haemophilus influenzae, Moraxella catarrhalis, Neisseria meningitides, Neisseria gonorrhoeae

Mechanism of Action:

Cephalosporins exert bactericidal activity by interfering with bacterial cell wall synthesis and inhibiting cross-linking of the peptidoglycan. The cephalosporins are also thought to play a role in the activation of bacterical cell autolysins which may contribute to bacterial cell lysis.

Pharmacodynamics:

Cephalosporins exhibit time-dependent killing (T > MIC)

Pharmacokinetics:

Dose of 400mg: Cmax: 15.4 mcg/L; Tmax: 1.2 hours; Half-life: 1.3 hours; Table 10

Adverse Effects:

Hypersensitivity: Maculopapular rash, Urticaria, Pruritis, Anaphylaxis/angioedema, eosinophilia

Hematologic: Neutropenia, Leukopenia, Thrombocytopenia

GI: Diarrhea, C. difficile disease

Renal: Interstitial nephritis

Table 14

Dosage:

PO: 200mg, 400mg capsule

       Powder for Suspension: 100mg/5mL, 200mg/5mL

Dosing in adults:

Acute exacerbation of chronic bronchitis: 400 mg PO q12h x 7 days

Uncomplicated cystitis: 200mg PO q24h x 7 days

Uncomplicated skin and/or subcutaneous tissue infection: 200 mg PO q12h x 7 days

Acute Maxillary sinusitis: 400mg PO q12h x 10 days

Pyelonephritis: 400 mg PO q12h x 14 days

Table 12

Dosing in pediatrics:

15-30mg/kg/day divided PO q12h

Disease state based dosing:

Renal failure:  CrCl ³ 50mL/min: usual dose

                        CrCl 10-49 mL/min: one-half the recommended dose at usual dosing interval,                           

                        CrCl < 10 mL/min: usual dose at intervals of 3 to 5 days

Hepatic failure:  No dosing changes recommended at this time.

Contraindications/Warnings/Precautions:

Precautions: hypersensitivity to penicillins, history of gastrointestinal disease, particularly colitis, renal impairment

Drug Interactions:

Live Typhoid Vaccine - decreased immunological response to the typhoid vaccine

Pregnancy:

Category B: No evidence of risk in humans but studies inadequate.

Monitoring Requirements:

Therapeutic:  Culture and sensitivities, serum levels, signs and symptoms of infection, white blood cell count

Toxic: Urinalysis, BUN, SCr, AST and ALT, skin rash, Neutropenia and leukopenia, Prothrombin time in patients with renal or hepatic impairment or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy, and patients previously stabilized on anticoagulant therapy.

Brand names/Manufacturer: 

Lorabid Ò/Monarch Pharmaceuticals; Loracarbef Ò/Eli Lilly; Prenatal Plus New Formula Ò/Pecos Pharmaceuticals