Antibacterials Drugs and Spectrum Exam 2 Flashcards
What are the β-lactams?
- penicillin G
- penicillin V
- oxacillin
- ampicillin
- amoxicillin
- piperacillin
- amoxicillin + clavulanic acid
- piperacillin + tazobactam
- meropenem + vaborbactam
- nafcillin
- dicloxacillin
penicillin G spectrum
Narrow, Gram +
penicillin V spectrum
Narrow, Gram +
oxacillin spectrum
Narrow, Gram +
ampicillin spectrum
Extended spectrum
amoxicillin spectrum
Extended spectrum
piperacillin spectrum
- Extended spectrum (broadest in this group)
- good activity against Pseudomonas aeruginosa
amoxicillin + clavulanic acid spectrum
Extended to broad spectrum
piperacillin + tazobactam spectrum
Extended to broad spectrum (BROAD)
meropenem + vaborbactam spectrum
Extended to broad spectrum
nafcillin spectrum
Narrow Gram + spectrum
dicloxacillin spectrum
Narrow Gram + spectrum
When would you use oxacillin, nafcillin, or dicloxacillin?
when Staphylococcus aureus is the suspected pathogen
What are the Penicillinase-Resistant Penicillins?
- oxacillin
- nafcillin
- dicloxacillin
What are the Aminopenicillins?
- Ampicillin
- amoxicillin
- piperacillin
What is special about the Aminopenicillins?
- extended antibacterial spectrum
- form ziwtterions at body pH
- increased penetration across the outer membrane of Gram – bacteria
What are the β-lactamases inhibitors?
- Clavulanic acid
- tazobactam
- vaborbactam
What are the combinations of PCN + β-lactamases inhibitors?
- Amoxicillin + clavulanic acid
- Piperacillin + tazobactam
- Meropenem + vaborbactam
What are the first generation Cephalosporins?
- Cefazolin
- cephalexin
- cefadroxil
First generation Cephalosporin spectrum
- Extended G+ spectrum
- the G- that they target: Proteus, E. coli, Klebsiella (PEcK)
What are the Second Generation Cephalosporins?
- Cefoxitin
- cefuroxime
- cefaclor
- cefprozil
Second Generation Cephalosporins spectrum
- (More) Extended G+ spectrum
- Hemophilus, Enterobacter, Neisseria (HENPEcK)
- Less sensitive to β-lactamases compared to first generation
What are the Third Generation Cephalosporins?
- Cefotaxime
- Ceftriaxone
- Ceftazidime
Third Generation Cephalosporins spectrum
- Broad spectrum antibiotics
- Gram +, but less active on Gram + than first generation
- Most enterobacteriaceae (rod-shaped Gram -)
- Resistant to β-lactamases
Ceftazidime spectrum
unusual high activity against Pseudomonas aeruginosa (NOT an enterobacteriaceae)
Ceftaroline spectrum
- Broad Spectrum
- Resistant to β-lactamases
- Unusually good activity against MRSA, and even against vancomycin-resistant Staph. aureus (VRSA)
- First β-LACTAM approved to treat MRSA and VRSA
- Not active against P. aeruginosa
What are the Fourth Generation Cephalosporins?
Cefepime
Fourth Generation Cephalosporins (Cefepime) spectrum
- Broad spectrum
- Better activity than third generation on G+
- Active on most enterobacteriaceae (like third gen.)
- Excellent activity against P. aeruginosa
- Resistant to β-lactamases
What are the Fifth Generation Cephalosporins?
Ceftaroline
β-lactam: Carbapenems spectrum
- Extremely Broad Spectrum (broadest of the PCN group)
- G+ except MRSA, G- including P. aeruginosa, most anaerobic bacteria
- Resistant to β-lactamases
What are the Carbapenems?
- Imipenem
- meropenem
- doripenem
- ertapenem
β-lactam: Monobactams spectrum
- Narrow G- Spectrum
- Gram – only, including P. aeruginosa, aerobic only
What are the Monobactams?
Aztreonam
What can you use to treat MRSA (class)?
- Glycopeptides / lipoglycopeptides
- Lipopeptides
- Oxazolidinones (best oral for this indication)
- Streptogramins
- Lincosamides
Glycopeptides spectrum
- Narrow Gram + spectrum
- Streptococci
- Enterococci
- MRSA infections
- Clostrodium difficile (G+, anaerobic)
Vancomycin uses for oral
Clostridium difficile diarrhea
What are the Lipoglycopeptides?
- Oritavancin
- Telavancin
- Dalbavancin
Which drug is useful against VRSA?
Oritavancin
What are the lipopeptide?
- Daptomycin
Lipopeptides spectrum
- Narrow Gram +
- resistant Gram + MRSA and VRSA
What are the oxazolidinones?
- Linezolid
- Tedizolid
Oxazolidionones spectrum
- Narrow Gram +
- Most cocci, Staphylococci including MRSA, VRSA, Streptococci
- penicillin-resistant Strep. pneumoniae, Enterococci including VRE
- The best oral drug for MRSA infections
What are the Streptrogramins?
Quinupristin / Dalfopristin
Streptrogramins spectrum
- Narrow Gram + spectrum
- Gram +, most cocci: Staphylococci, MRSA, VRSA, Streptococci, Enterococci (not E. fecalis), VRE
- Considered last resort antibiotic
Lincosamide spectrum
- Narrow Gram +
- Most typical aerobic Gram + (Staph., Strep.), some strains of MRSA respond
- Many anaerobic Gram +
- Special property: Activity against some anaerobic Gram
- Used for Gram + and anaerobic infections
What are the Lincosamides?
Clindamycin
Macrolide spectrum
- hydrophobicity will help macrolides cross the outer membrane of some G-
What are the Macrolides?
- Erythromycin
- Clarithromycin
- Azithromycin
What is a ketolide?
- Telithromycin
- binds MLS(b)
and another site - inhibits some MLS resistant bacteria
Macrolides spectrum
- Extended G+
- Primarily active against Gram +, but Strep. pneumoniae wide-spread resistance in the USA is becoming a serious threat
- Not active against MRSA
- Gram -, major respiratory pathogens (Hemophilus influenzae), some atypical pathogens. Not active against typical G- (E. coli, P. aeruginosa) so not classified as broad spectrum
Clarithromycin spepctrum
Macrolide spectrm + Active against some anaerobes and better activity on G+
Azithromycin spepctrum
Macrolide spectrm + better activity on G-; Not active against anaerobes
Sulfamethoxazole spectrum
Broad spectrum
Trimethoprim spectrum
Broad spectrum
Sulfamethoxazole plus trimethoprim spectrum
Many MRSA strains respond
What are the ansamycins?
Rifamycin: rifampin, rifabutin, Rifaximin
Ansamycins spectrum
- Broad
- Especially active against Mycobacteria
- Primarily used for Tuberculosis
What are the fluoro/quinolones?
- ozenoxacin
- ciprofloxacin
- ofloxacin
- levofloxacin
- moxifloxacin
- Delafloxacin,
Fluoro/quinolones spectrum
Broad
ciprofloxacin, ofloxacin spectrum
more active against G – , including P. aeruginosa
levofloxacin, moxifloxacin spectrum
improved activity against G+, not active against MRSA
Delafloxacin spectrum
- better activity against G+
- active against some MRSA,
- less resistance develops
- more active at acidic pHs.
moxifloxacin spectrum within its own class
best activity against anaerobes
What are the Tetracyclines?
- Tetracycline
- Doxycycline
- Doxycycline
- Tigecycline
- omadacycline
- omadacycline
Tetracyclines spectrum
- Usually more active against G+ than G-, not active against P. aeruginosa
- Tetracycline is not active against MRSA
- Doxycycline and Minocycline are active on some MRSA
- Tigecycline, omadacycline and eravacycline are active against more MRSA and multiresistant organisms
What are the aminoglycosides?
- Gentamicin
- Tobramycin
- Amikacin
- Plazomicin
Aminoglycosides spectrum
- Extended G-
Active against G -, including P. aeruginosa, Plazomicin is also active against multidrug resistant G - - Some G + but many are resistant, not active against MRSA
- ransporters are oxygen-dependent so these drugs are inactive on anaerobic bacteria
What are the polypeptides?
- Colistin
- Belong to the polymyxin family of molecules
Polypeptide spectrum
- Narrow G -
- Gram -, especially Pseudomonas, Escherichia, and Klebsiella species
- Active against multidrug resistant G -
What are the nitromidazoles?
- Metronidazole
- Secnidazole
Nitromidazole spectrum
- Gram + and Gram - anaerobes
- Metronidazole no longer recommended for Clostrodium difficile infections
- Secnidazole (single oral dose) was approved for bacterial vaginosis
