Professional Documents
Culture Documents
Spectrum of Activity
Broad Spectrum- ex: tetracyclines, carbapenems, 3rd gen quinolones, 2nd/3rd/4th gen cephalosporins, chloramphenicol,
PCN w/beta-lactamase inhibitors
Narrow Spectrum- ex: glycopeptides, bacitracin, aminoglycosides, sulfonamides, penicillin, lincosamides, macrolides,
vancomycin, aztreonam
*Think about what the ABX covers and the more it covers, the broader it is when treating infections.
Overview of Antibiotics
PCN Spectrum
Narrow
o Additional of beta lactamase inhibitor- Adds activity against MSSA, more Gram -, Gram – Anaerobes
o Antipseudomonal PCN (extended-spectrum PCN)- very broad coverage with expanded Gram -, Pseudomonas aeruginosa
o Antistaphylococcal PCN- enhanced activity with MSSA, lack Enterococcus activity
DDI:
o Probenecid can ↑ levels of PCN
o Bacteriostatic antibiotics (ex: tetracyclines) can ↓ effectiveness of PCN
o ↑ levels of methotrexate
o ↓ levels of mycophenolate active metabolites
o Nafcillin is a moderate CYP3A4 inhibitor
o Dicloxacillin & nafcillin can ↓ INR through ↑ metabolism of warfarin
Cephalosporins
Time-dependent killing and are bactericidal. Not active against Enterococcus, atypicals, Listeria, MRSA (except 5th Generation (LAME).
Coverage:
o 1st- Excel against Gram + (preferred cephalosporin against MSSA)
2nd- Split into 2 groups 1) Cefuroxime like agents cover more resistant S.pneumoniae, HNPEK; 2) Cephamycin drugs (Cefotetan,
Cefoxitin) have added anaerobic coverage
o 3rd- Ceftriaxone, Cefotaxime and oral drugs cover more resistant Streptococci and more Gram -; Ceftazidime lacks Gram + and covers
Pseudomonas
o 3rd w/beta lactamase inhibitor combo- added activity against MDR Pseudomonas and Gram -
o 4th- broad Gram -, including Pseudomonas, Gram +
o 5th- only beta-lactam with MRSA activity
DDI:
o Probenecid can ↑ levels of cephalosporins
o Enhance anticoagulant effect of warfarin by inhibiting production of clotting factors
o Drugs that ↓ stomach acid can ↓ bioavailability of some cephalosporins
Carbapenems
Time-dependent killing and are bactericidal. Not active against atypical, MRSA, VRE.
Coverage:
o VERY BROAD COVERAGE “BIG GUN”, generally used for MDR Gram -, most Gram +, Gram – (including ESBL producing bacteria),
anaerobes
o Ertapenem is different and has NO activity against Pseudomonas, Acinetobacter or Enterococcus
DDI:
o Probenecid can ↑ levels of cephalosporins
o ↓ levels of valproic acid leading to a loss of seizure control
o Use in caution in patients at risk for seizures
Monobactam
Aztreonam (similar to ceftazidime); acts like a beta-lactam, but it’s not…like splenda to sugar
Structure makes cross-reactivity with beta-lactam allergy unlikely, primarily used when beta-lactam allergy is present.
Coverage:
o Similar to Ceftazidime lacks Gram +, covers Gram - and covers Pseudomonas
Aminoglycosides
Concertation dependent killing and has post-antibiotic effect. Can use extended dose interval nomograms.
Coverage:
o Gram -, Pseudomonas
DDI:
o Use in caution with patients with impaired renal function
Quinolones
Concertation dependent killing and are bactericidal.
Coverage:
o Broad spectrum (Gram +, Gram -, Atypicals)
Macrolides
Bacteriostatic activity related to total exposure of the drug (AUC/MIC).
Coverage:
o Good Atypical activity
DDI:
o Erythromycin and clarithromycin are 3A4 inhibitors and substrates
o Azithromycin is a substrate for 3A4 and inhibitor of 1A2 and P-gp; it has fewer drug interactions
o ALL MACROLIDES: DO NOT USE WITH AGENTS THAT CAN PROLONG THE QT INTERVAL
Tetracyclines
Bacteriostatic activity related to total exposure of the drug (AUC/MIC).
Coverage:
o Many Gram +, Gram -, including respiratory flora
o Doxy- used in mild MRSA skin infections, VRE in UTI
o Mino- enhanced Gram + and preferred for skin infections (acne)
o Tetra- rarely used, can be used in H.pylori regimens
DDI:
o Absorption is impaired by medications that contain divalent cations
o Tetracycline is a substrate of 3A4 and an inhibitor
o Doxycycline is a weak 3A4 inhibitor
o Enhance the anticoagulant effect with warfarin
Sulfonamides
Individually they are bacteriostatic, but collectively they are bactericidal. Lacks Pseudomonas, Enterococci, atypical or anaerobic coverage.
Coverage:
o Gram +, including Staphylococci/MRSA, many Gram –
DDI:
o Inhibitors of 2C8/9
o Cause ↑ INR with warfarin
o ↑ levels of sulfonylureas, metformin, phenytoin, dofetilide, azathioprine, methotrexate and mercaptopurine
o Levels of SMX/TMP can be ↓ by 2C8/9 inducers
o ↑ in hyperkalemia when used with ACE inhibitors, ARBs, aliskiren, potassium-sparing diuretics, cyclosporine, tacrolimus and more
Glycopeptide
Vancomycin
Coverage:
o Gram +, MRSA, Streptococci, Enterococci (not VRE), C.difficile
DDI:
o ↑ toxicity of other nephrotoxic drugs and ototoxic drugs
Lipoglycopeptide
Concentration-dependent killing and are bactericidal; (similar to Vancomycin, but have extended MOA)
Coverage:
Daptomycin (Cubicin)
Concentration-dependent killing and are bactericidal.
Coverage:
o Gram +, MRSA, Streptococci, Enterococci, including VRE, *same coverage as Vancomycin but covers more organisms
DDI:
o Additive risk of muscle toxicity with statins
Oxazolidinones
Bacteriostatic activity.
Coverage:
o Gram +, MRSA, Streptococci, Enterococci, including VRE, *same coverage as Vancomycin but covers more organisms
DDI:
o Weak MAOI (caution in patients taking concurrent serotonergic or adrenergic drugs
o Avoid tyramine-containing foods
o Can exacerbate hypoglycemic episodes
Polymyxins
Concentration-dependent killing and bactericidal. Use in combo with another antibiotic due to the emergence of resistance.
Coverage:
o Gram -, Pseudomonas, used primarily with MDR Gram – pathogens
DDI:
o Other nephrotoxic agents can enhance nephrotoxicity
Chloramphenicol
Bactericidal
Coverage:
o Gram +, Gram -, anaerobes and atypicals
Lincosamides
Bacteriostatic
Coverage:
o Most aerobic and anaerobic Gram +, some MRSA, does not cover Enterococcus
Urinary Agents
Fosfomycin (Monurol)- inhibits bacterial cell wall synthesis by inactivating the enzyme pyruval transferase; bactericidal
Coverage:
o E.coli (including ESBLs) and E.faecalis (including VRE)
Nitrofurantoin (Macrodantin, Macrobid, Furadantin)- bacterial cell wall inhibitor; bactericidal
Coverage:
o E.coli, Klebsiella, Enterobacter, S.aureus, Enterococcus (VRE)
Storage
Refrigeration after reconstitution Refrigeration Recommended
Pen VK, Ampicillin, Augmentin, Cephalexin, Cefpodoxime, Amoxicillin (improves taste)
Cefprozil, Cefuroxime, Vancomycin (oral)
*all other do not refrigerate