Pharmacology - Antimicrobial Therapy I - Jeffrey Steele Flashcards
Class: Penicillins
Beta-lactam
Class: Cephalosporins
Beta-lactam
Class: Aztreonam
Monobactam
Class: Vancomycin
Glycopeptides
Class: Telavancin
Dalbavancin
Oritavancin
Lipoglycopeptides
Beta lactams, Monobactams, Glycopeptides and Lipoglycopeptides all act:
on the cell wall of bacteria
MOA: Beta-lactams
Bind to (acylation of) PBPs (penicillin binding proteins)
- -PBPs polymeriza the glycan strand (transglycosylation)
- -PBPs cross-link between glycan chains (transpeptidation)
What are mechanisms of resistance against beta lactams?
Enzymatic Destruction - by gram negative bacteria;
Reduced permeability;
Target site alteration
Beta-lactams do not work on:
Mycoplasma pneumoniae;
Chlamydophilia pneumoniae
–these bugs lack cell walls
Legionella MRSA (except for ceteroline = 5th gen cephalosporin)
Side effects: Beta lactams
Drug fever Acute interstitial nephritis Seizures at high doses Diarrhea Delayed hypersensitivity reaction - rash
What are the natural penicillins?
Penicillin G
Penicillin V
Class: Oxacillin
Nafcillin
Dicloxacillin
Penicillinase-resistant penicillins aka antistaphylococcal penicillins
Penicillins - Beta-lactams
Class: Ampicillin
Amoxicillin
Aminopenicillins
Amino group increases hydrophilicity - improved penetration into gram negative cell membrane
Class: Ticarcillin
Piperacillin
Anti-pseudomonal penicillins
Use: Penicillin G, G procaine, G benzthine, V
Streps;
Mostly gram pos aerobic organisms;
Spirochetes - Treponema palladium;
Some enterobacteriaciae
Addition of what to Penicillin is recommended for use against odontogenic infections?
Metronidazole
recommended for b-lactamase producing aerobes
Use: Anti-staph penicillins ie oxacillin
MSSA - skin and soft tissue infections, joint infection, bacteremia, endocarditis;
(Strep)
T/F: Anti-staph penicillins are superior to vancomycin for MSSA infections.
True
Oxacillin
Nafcillin
Dicloxacillin
Adverse events: Oxacillin
Hepatotoxicity, neutropenia (delayed)
Adverse events: Nafcillin
Hepatotoxicity, neutropenia (delayed) and thrombophlebitis
What anti-staph penicillins require frequent dosing due to their short half life?
Oxacillin, Nafcillin
What is the drug of choice for enterococci?
Ampicillin (Aminopenicillin class)
–also for Listeria
Use: Amoxicillin
Otitis media; Upper and lower RTI; Lyme disease; Streps ie S. Pneumo **also covers haemophilus which causes upper ear/RTI stuff (for the unvaccinated child)
Use: IV Ampicillin
Listeria - meningitis;
Enterococcal infections
Used with gentamycin for endocarditis
Which aminopenicillin has better bioavailability?
Amoxicillin > Ampicillin
The antipseudomonal penicillins, piperacillin and ticarcillin, are always used in conjunction with:
B-lactamase inhibitors to expand spectrum to include beta-lactamase-producing organisms
Class: Ampicillin/sulbactam (IV) (Unasyn)
Extended spectrum penicillin/beta lactamase inhibitor combinations
Class: Amoxicillin/clavulanate (PO) (Augmentin)
Extended spectrum penicillin/beta lactamase inhibitor combinations
Class: Piperacillin/tazobactam (IV) (Zosyn)
Extended spectrum penicillin/beta lactamase inhibitor combinations
Class: Ticarcillin/clavulanate (IV) (Timentin)
Extended spectrum penicillin/beta lactamase inhibitor combinations
Uses: Extended spectrum penicillin/beta lactamase inhibitor combinations ie Ampicillin/sulbactam Amoxicillin/clavulanate Piperacillin/tazobactam Ticarcillin/clavulanate
Gram pos - MSSA;
Gram neg - Enterobacteriaceae;
Anaerobes ie Bacteroides, Fusobacterium, Prevotella
What drugs are recommended for Pseudomonas aeruginosa?
Piperacillin/tazobactam;
Ticarcillin/clavulanate
What unique strength does sulbactam have?
Activity against nosocomial bug Acinetobacter baumanni
What cephalosporins have activity against Pseudomonas aeruginosa?
Ceftazidime;
Cefepime
Class: Ceftaroline
5th gen cephalosporin
Ceftriaxone should be avoided in neonates because:
AE - biliary sludging
What cephalosporins are responsible for causing a disulfiram-like reaction w/ ethanol?
Cefamandole;
Cefotetan;
Cefoperazone
Class: Cefazolin (IV)
1st gen cephalosporin
Class: Cephalexin (PO)
1st gen cephalosporin
Class: Cephadroxil (PO)
1st gen cephalosporin
Use: 1st gen cephalosporin
Cefazolin
Cephalexin
Cephadroxil
MSSA - joint, SSTI (skin and soft tissue infections), bacteremia
Streptococci
Some enteric GNRs
Side effects: 1st gen cephalosporin
Cefazolin
Cephalexin
Cephadroxil
Hypersensitivity rxns
Better tolerated than anti-staph penicillins (oxacillin, nafcillin)
Do 1st gen cephalosporins, is Cefazolin, Cephalexin, Cephadroxil cross the BBB?
No. can’t use for CNS infections
Class: Cefuroxime (IV/PO) Cefaclor (PO) Loracarbef (PO) Cephamycins (Cefoxitin, Cefotetan)
2nd gen cephalosporins
Use: 2nd gen cephalosporins
Most commonly post colon surgery
Some staph, strep but less active than 1st gen cephalosporins;
Gram neg: some enterobacteriaceae, h. influenzae, m. catarrhalis, N. gonorrheae
Class: Cefotaxime (IV)
3rd gen cephalosporin
Class: Ceftriaxone (IV)
3rd gen cephalosporin
Class: Ceftazidime (IV)
3rd gen cephalosporin
Class: Cefdinir (PO)
3rd gen cephalosporin
Class: Cefpodoxime (PO)
3rd gen cephalosporin
Class: Ceftibutin (PO)
3rd gen cephalosporin
Class: Cefixime (PO)
3rd gen cephalosporin
Use: Ceftazidime
Pseudomonas
less active against Staph and Strep
3rd gen cephalosporin
Which generation of cephalosporins is more active against staphylococci?
1st gen better than 3rd gen
Uses: Ceftriaxone (3rd gen)
Community-acquired pneumonia - use w/ azithromycin;
Meningitis;
Complicated UTI;
Intra-abdominal infection w/ metronidazole;
CSF Lyme disease;
Strep endocarditis;
Gonococcal infection and PID
Side effects: 3rd gen cephalosporins
Greater correlation w/ C. diff infection than other drugs;
Development of resistant organisms (ESBLs)
Side effects: Ceftriaxone (3rd gen)
Concerns in neonates - biliary sludging, kernicterus, interaction with calcium-containing solutions causing precipitation
What drug should be used instead of Ceftriaxone in neonates?
Cefotaxime
T/F: Ceftriazone, Cefotaxime, Ceftazidime have effective penetration across the BBB.
True
Is dose-adjustment necessary for patients with renal dysfunction who are administered Ceftriaxone?
No
Class: Cefepime
4th gen cephalosporin
MOA: Cefepime (4th gen)
Zwitterion - neutral molecule with pos and neg Q
Permits rapid entry into outer membrane of gram neg bacteria
Cephalosporins have notably no effect on what class of bacteria?
Enterococcus
Use: Cefepime (4th gen)
Geared toward nosocomial infections
Enterobacteriaceae; Pseudomonas Meningitis MSSA Strep pneumo, including all strains resistant to penicillin
Side effects: Cefepime (4th gen)
Akinetic seizures
MOA: Ceftaroline (5th gen)
Has a side chain that mimics a portion of the cell wall structure and acts as a trojan horse allowing access to the PBP2a