Moxalactam  (PDF Version)

 

Antibiotic Class:

Second-Generation Cephalosporin (3rd generation cephamycin)

 

Antimicrobial Spectrum:

Methicillin-susceptible Staphylococcus aureus (MSSA), Coagulase negative Staphylococci, penicillin-susceptible Streptococcus pneumoniae, Streptococci spp. (less activity compared to 1st generation and 2nd generation cephalosporins), Haemophilus influenzae, Moraxella catarrhalis, Neisseria meningitides, Neisseria gonorrhoeae, Enterobacteriaceae

 

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:

IM bioavailability:  92%; Total protein binding: 52%; Volume of distribution: 0.18-0.44 L/kg; Half-life: 5.4-7.6 hours

 

Adverse Effects:

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

Hematologic: Hypoprothrombinemia, Neutropenia, Leukopenia, Thrombocytopenia

GI: Diarrhea, C. difficile disease

Renal: Interstitial nephritis

Table 14

 

Dosage:

IV: 1g, 2g

 

Dosing in adults:

Serious gram-negative infections:  1 to 2 g q8h

Gram-negative bacillary meningitis:  1 to 2 g q8h

IV/IM:  2 to 4 g/day in divided doses q8h or q12h for 5 to 10 days, or up to 14 days

Severe, life-threatening infections:  6 to 12 g/day IV in divided doses q8h or q12h

 

Dosing in pediatrics:

25-200mg/kg/day divided q6-12h

 

Disease state based dosing:

Renal failure: CrCl > 80mL/min: standard dosing

CrCl 50-80mL/min 0.5-1g q8h

CrCl 25-50mL/min 0.25-1g q12h

CrCl 2-25mL/min 0.25-0.5g q8h

Hepatic failure:  No dosing changes recommended at this time.

 

Contraindications/Warnings/Precautions:

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

 

Drug Interactions:

Heparin: increased risk of bleeding

Live Typhoid Vaccine: decreased immunological response to the typhoid vaccine

Warfarin: increased risk of bleeding

 

Pregnancy:

Category C. Risk established, but benefits may outweigh risk.

 

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:  MoxamÒ/Eli Lilly