Penicillin beta-lactams

Headshot of Joanna Breems, MD, FACP · Clinical Assistant Professor
Joanna Breems
MD, FACP · Clinical Assistant Professor
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Table of Contents

Penicillin (PCN)

  • Class(es)

    Penicillins/Beta-Lactams.

  • Clinical use(s)

    FDA approved: Syphilis, anthrax, listeria infections, meningococcal infections, pasteurella, serious gram-positive infections.
    Off-label/clinical use: CAP (children), group B strep, osteomyelitis, SSTI.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits bacterial cell wall synthesis during active multiplication.

  • Key adverse effects

    Nausea, vomiting, diarrhea, seizure (rare).

  • Key drug/food interactions

    Tetracyclines (may ↓ effectiveness)
    Food (may ↓ peak penicillin concentrations)

  • Special considerations

    Renally adjusted: CrCl < 10 ml/min.

Amoxicillin (Amoxil)

  • Class(es)

    Penicillins/Beta-lactam antibiotic

  • Clinical use(s)

    FDA approved: Ear, nose and throat bacterial infection, skin and soft tissue infection
    Off-label/clinical use: Uncomplicated acute otitis media

  • Mechanism(s) of action

    Binds penicillin binding protein, which prevents cell wall synthesis

  • Key adverse effects

    Allergy (~10%), N/V/D (>1%)

  • Key drug/food interactions

    Concurrent use of PENICILLINS and TETRACYCLINES may decrease effectiveness.

  • Special considerations

    Available in oral form only. Contraindicated in serious hypersensitivity reactions to Beta Lactam antibiotics. Cross-sensitivity with cephalosporin antibiotics has been reported to be between .2% and 10%.

Ampicillin

  • Class(es)

    Penicillins/Beta-Lactams

  • Clinical use(s)

    FDA approved: Bacterial meningitis, gonorrhea, endocarditis, respiratory tract infection, sepsis, genitourinary/digestive tract infections.
    Off-label/clinical use: Bacterial endocarditis (prophylaxis), bacteremia associated with IV line.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Diarrhea, anaphylaxis.

  • Key drug/food interactions

    Tetracyclines, bupropion/donepezil (lowers seizure threshold).

  • Special considerations

    Rapid infusion may cause seizures.
    Renally adjusted: CrCl < 50 ml/min.

Dicloxacillin (Dynapen)

  • Class(es)

    Penicillins/Beta-Lactams

  • Clinical use(s)

    FDA approved: Infection due to staph aureus (MSSA).
    Off-label/clinical use: Impetigo, SSTI.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Neurotoxicity (high doses), hypokalemia, bone marrow suppression, diarrhea

  • Key drug/food interactions

    Tetracylines, bupropion/donepezil (lowers seizure threshold), Food (may ↓ dicloxacillin concentrations)

  • Special considerations

    CYP3A4 inducer

Nafcillin (Nafcil, Nallpen)

  • Class(es)

    Pencillins/Beta-Lactams

  • Clinical use(s)

    FDA approved: Confirmed MSSA—meningitis, endocarditis.
    Off-label/clinical use: Skin/soft tissue necrotizing infection, streptococcal skin infection, surgical site infection, catheter-related bacteremia.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Neurotoxicity (high doses), hypokalemia, bone marrow suppression, diarrhea.

  • Key drug/food interactions

    Fentanyl, cyclosporine, tetracylines, Food (may ↓ nafcillin concentrations).

  • Special considerations

    CYP3A4 inducer.
    Dose adjust for severe renal and hepatic impairment.

Amoxicillin/Clavulanate (Augmentin)

  • Class(es)

    Aminopenicillins beta lactamase inhibitors

  • Clinical use(s)

    FDA approved: Acute otitis media, CAP, impetigo, SSTI, LRTI, sinusitis, UTI  
    Off-label/clinical use: Febrile neutropenia, streptococcal pharyngitis.

  • Mechanism(s) of action

    Amoxicillin: Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs).
    Clavulanic acid: Inactivates beta-lactamase enzymes.

  • Key adverse effects

    Diarrhea, nausea, vomiting

  • Key drug/food interactions

    Tetracyclines

  • Special considerations

    Renally adjusted: CrCl < 30 ml/min.
    Do not use ER and 875 mg tablet in HD patients and CrCl < 30 ml/min.
    Take with food.

Piperacillin/Tazobactam (Zosyn)

  • Class(es)

    Extended Spectrum Pencillins/Beta-Lactams.

  • Clinical use(s)

    FDA approved: Appendicitis, CAP/HAP, SSTI, pelvic inflammatory disease, peritonitis, puerperal endometritis.
    Off-label/clinical use: Bacteremia associated with IV line, febrile neutropenia, infectious disease of abdomen.

  • Mechanism(s) of action

    Piperacillin: Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs). Tazobactam: Inhibits many beta-lactamases.

  • Key adverse effects

    Diarrhea, nausea, headache, neutropenia.

  • Key drug/food interactions

    Tetracycline, vancomycin (↑ risk AKI).

  • Special considerations

    Renally adjusted: CrCl < 40 ml/min.

Meropenem (Merrem)

  • Class(es)

    Carbapenem.

  • Clinical use(s)

    FDA approved: Bacterial meningitis, SSTI, infection of the abdomen.
    Off-label/clinical use: Bacteremia associated w/ IV line, cystic fibrosis, febrile neutropenia, HAP.

  • Mechanism(s) of action

    Exerts bactericidal activity by inhibiting cell wall synthesis by penetrating the cell wall of most gram-positive and gram-negative bacteria to reach penicillin-binding–protein (PBP) targets.

  • Key adverse effects

    Diarrhea, N/V, rash, anemia, headache.

  • Key drug/food interactions

    Valproic acid, cholera vaccine, live typhoid vaccine, probenecid.

  • Special considerations

    Injection only.
    Renal impairment: CrCl <50 ml/min—dose adjust.

Aztreonam (Azactam)

  • Class(es)

    Monobactam.

  • Clinical use(s)

    FDA approved: Cystic fibrosis, disease w/ Gram negative bacteria, endometritis, female genital infection, SSTI, LRTI, peritonitis, sepsis, UTI.
    Off-label/clinical use: Meningitis, musculoskeletal infection, febrile neutropenia, gonorrhea, post-op prophylaxis, traveler’s diarrhea.

  • Mechanism(s) of action

    Bactericidal against gram-negative aerobic bacteria by binding to penicillin-binding protein-3(PBP-3), which results in inhibition of bacterial cell wall synthesis.

  • Key adverse effects

    Chest discomfort, ALT/AST elevation, SCr elevation, cough, congestion.

  • Key drug/food interactions

    Cholera vaccine.

  • Special considerations

    Injection and inhalation routes.
    Renal impairment: CrCl <30 ml/min—dose adjust.