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Infection - penicillins

Infection - penicillins

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Infection - penicillins

  1. 1. Penicillins
  2. 2. 2 MOA: Cell wall synthesis inhibitors • PBP • Inhibition of transpeptidase • Production of autolysis  Bactericidal  Time-dependant  Pregnancy Category B
  3. 3. Members:  Natural Penicillin: Penicillin V (PO) & Penicillin G (IV).  Synthetic Penicillins: Ampicillin (IV) & Amoxicillin (PO)/clavulanic acid.  Penicillinase Resistant: Cloxacillin,Nafcillin.  Extended Spectrum: Piperacillin ±tazobactam, Ticarcillin ±Clavulanic acid 3
  4. 4. Dosage Forms: Amoxicillin: PO Ampicillin: PO Cloxacillin: PO, IV, IM Nafcillin: IV,IM Penicillin G: IV Penicillin V: PO Piperacillin: IV,IM Ticarcillin: IV
  5. 5. 5 Coverage: • Narrow spectrum agent; mostly aerobic gram positive cocci • Useful against:  ß- hemolytic streptococci (Group A, B, C)  Treponema pallidum (Syphillis) – Gram negative spirochete  N. menigitidis: *note: resistance 1-3%  oral anaerobes  Enteroccocus (E. facaelis, NOT E. faecium) • NOT useful against:  most gram negative organisms  Beta-lactamase producing organisms (S. aureus - ~90%) Penicillin (G)/(V)
  6. 6. 6 Dose Adjustment: Penicllin G:  needs renal dose adjustment at CrCl ≤50ml/min
  7. 7. 7 Coverage: • narrow spectrum agent; mostly Gram positive aerobes, some Gram negative aerobes • covers everything that penicillin does (streptococcus, enterococcus, oral anaerobes) • Gram negative coverage (HiPEEL) - Non-beta-lactamase producing  H. influenzae (~25% resistance)  Proteus mirabilis  E. coli (~30% resistance) • Gram positive coverage  better coverage of enterococcus (E.faecalis vs. penicillin)  Listeria monocytogenes (HiPEEL) • Useful against: ß- hemolytic streptococci (Group A, B, C), E. faecalis ( <1% resistance), Listeria Amoxicillin/Ampicillin
  8. 8. 8 Coverage: • broad-spectrum agent • extends spectrum of amoxicillin to cover more gram negatives (E.coli, H. influenzae, Salmonella, Shigella) + gut anaerobes (B. fragilis) • Not useful against: Pseudomonas • “Like pip/tazo (minus Pseudomonal coverage)” Amoxicillin-Clavulanic Acid
  9. 9. 9 Dose Adjustment: Amoxicillin:  needs renal dose adjustment at CrCl ≤30ml/min Ampicillin:  needs renal dose adjustment at CrCl ≤50ml/min
  10. 10. 10 Coverage: • Piperacillin + ß-lactamase inhibitor • Most broad-spectrum penicillin • aerobic Gram positives (including MSSA, E. faecalis), • difficult aerobic Gram negatives (including Pseudomonas, Acinetobacter), • anaerobes (including B. fragilis) • Useful against: Pseudomonas, harder to kill Gram negatives (traditional ß-lactamase producers), most aerobic Gram positives (including MSSA) • NOT useful against: MRSA, E. faecium, ESBL Piperacillin-Tazobactam
  11. 11. 11 • Active against Pseudomonas aeruginosa and many gram-negative bacilli • Do not cover Klebsiella • + clavulanic acid or tazobactam: Covers penicillinase-producing organisms (for example, most Enterobacteriaceae and Bacteroides species). Coverage: Ticarcillin
  12. 12. 12 Dose Adjustment:  Piperacillin:  needs renal dose adjustment at CrCl ≤40ml/min  No hepatic Dose Adjustment  Ticarcillin:  needs renal dose adjustment at CrCl ≤60 ml/min  Hepatic: only with concomitant renal dysfunction (CrCl ≤10 ml/min)
  13. 13. 13 Coverage: • Very narrow spectrum; gram positive aerobes • drug of choice for MSSA • maintains coverage for Streptococci (less so than penicillin/ amoxicillin) • some oral anaerobic coverage (less so than penicillin/amoxicillin) • Not useful against: Enterococci, N. meningitis Cloxacillin
  14. 14. 14 • Cover penicillinase-producing staphylococci, including methicillinsensitive Staphylococcus aureus (MSSA). Coverage: Nafcillin
  15. 15. 15 Dose Adjustment:  Cloxacillin  Nafcillin  no need for hepatic or renal dose adjustment
  16. 16. 16 Mechanism of Resistance:  Natural Resistance:  Occur in organisms that lack a peptidoglycan cell wall (mycoplasma pneumoniae)  Organisms have cell wall that is impermeable to drugs.  β-Lactamase activity  Decreased permeability to the drug  Altered PBPs:
  17. 17. 17  Hypersensitivity  Diarrhea  Nephritis  Neurotoxicity  Hematologic toxicities Contraindications:  Hypersensitivity. Side effects:
  18. 18. Macrolides
  19. 19. 19 MOA: Protein synthesis inhibition; they inhibit 50S ribosomal subunit  Bacteriostatic (bactericidal at higher doses)  Concentration dependant.
  20. 20. Members, dosage form & Pregnancy Category Clarithromycin: PO (Cat C) Erythromycin: PO, IV (Cat B) Azithromycin: PO, IV (Cat B)
  21. 21. 21 Relatively broad-spectrum • Gram positives: Streptococci (note increasing resistance with S. pneumoniae ~20%) • some Gram negatives (A & C only): H. influenzae, M. cattarhalis • atypicals • NO anaerobic coverage • Not useful for: MRSA, enterococcus Coverage
  22. 22. 22 Dose Adjustment:  Clarithromycin  needs renal dose adjustment at CrCl <30ml/min  Erythromycin:  No renal or hepatic Dose Adjustment  Azithromycin:  No renal Dose Adjustment (use w/ caution w/ GFR <10ml/min)
  23. 23. 23 Mechanism of resistance: 1) the inability of the organism to take up the antibiotic, 2) the presence of efflux pumps, 3) a decreased affinity of the 50S ribosomal subunit for the antibiotic. 4) the presence of plasmid-associated erythromycin esterases in gram-negative organisms such as Enterobacteriaceae.
  24. 24. 24 Side Effects: 1. Gastric distress and motility 2. Cholestatic jaundice 3. Ototoxicity  Contraindications: Severe hepatic failure & QT prolongation (Clarithromycin)
  25. 25. Monobactams
  26. 26. 26 Members : Aztreonam • MOA : cell wall synthesis inhibitors • Coverage : gram negative aerobic including P.aeruginosa and Enterobacteriaceae,  lack activity against gram positive organisms and anaerobes • Bactericidal • time dependent
  27. 27. • Dosage form : IM, IV, inhalation • Pregnancy category: B  needs renal dose adjustment at CrCl <30ml/min
  28. 28. 28 •Elevated hepatic transaminases. •GI: diarrhea, N/V. •Pain at site of injection, Phlebitis. •Neutropenia, eosinophilia, thrombocytopenia. •C/I: hypersensitivity Adverse effects:
  29. 29. Chloramphenicol
  30. 30. 30 • MOA: inhibit protein synthesis at the peptidyl transferase rxn (50S ribosomal unit) • Coverage: active against chlamydiae, rickettsiae, spirochetes, and anaerobes. • bacteriostatic, but depending on the dose and organism, it may be bactericidal. • Time-dependent • Resistance: 1) presence of enzymes that inactivate chloramphenicol. 2) decreased ability to penetrate the organism and ribosomal binding site alterations.
  31. 31. 31 • Dosage form: IV • Pregnancy category C • S:E Anemia, Grey baby syndrome, bone marrow suppression • C/I: Hypersensitivity, blood dyscrasias (box warning) • No renal or hepatic dose adjustment needed.

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