[3S] Chemotherapeutic Agents Summary Flashcards
MOA
Prevents bacterial cell wall synthesis by binding to and inhibiting cell wall transpeptidases
Pen G, Cefazolin, Imipenemcilastatin, Aztreonam
Effects
Rapid bactericidal activity against susceptible bacteria
Pen G, Cefazolin, Imipenemcilastatin, Aztreonam
Clinical Applications
Streptococcal infections, meningococcal infections,
neurosyphilis
Pen G
ROA Pen G
IV/IM
PKINETICS
rapid renal clearance (half-life 30 min, so requires dosing every 4 h)
Pen G
Interactions
Immediate hypersensitivity, rash, seizures
Pen G
Penicillin
Oral, low systemic levels limit widespread use
Penicillin V
Penicillin
Oral, low systemic levels limit widespread use
Penicillin V
Penicillin
Greater activity versus gram-negative bacteria; addition of β-lactamase inhibitor restores activity against many βlactamase-producing bacteria
Ampicillin, amoxicillin, piperacillin:
Penicillin
Intramuscular, long-acting formulations
Benzathine penicillin, procaine penicillin
Penicillin
Intravenous, added stability to staphylococcal β-lactamase, biliary clearance
Nafcillin, oxacillin
PKINETICS
IV administration
renal clearance (half-life 1.5 h)
given every 8 h
poor penetration into the central nervous system
Cephalosporins: Cefazolin
Clinical Applications
Skin and soft tissue infections, urinary tract
infections, surgical prophylaxis
Cephalosporins: Cefazolin
Toxicity
Rash, drug fever
Cephalosporins: Cefazolin
Cephalosporins
Oral, first-generation drug used for treating skin and soft tissue infections and urinary tract infections
Cephalexin
Cephalosporins
Oral and intravenous, second-generation drug, improved activity versus pneumococcus and Haemophilus influenzae
Cefuroxime
Cephalosporins
Intravenous, second-generation drugs, activity versus Bacteroides fragilis allows for use in abdominal/pelvic infections
Cefotetan, cefoxitin
Cephalosporins
Intravenous, third-generation drug, mixed clearance with long half-life (6 hours), good CNS penetration, many uses including pneumonia, meningitis, pyelonephritis, and gonorrhea
Ceftriaxone
Cephalosporins
Intravenous, third-generation, similar to ceftriaxone; however, clearance is renal and half-life is 1 hour
Cefotaxime
Cephalosporins
Intravenous, third-generation drug, poor gram-positive activity, good activity versus Pseudomonas aeruginosa
Ceftazidime
Cephalosporins
Intravenous, fourth-generation drug, broad activity with improved stability to chromosomal β-lactamases
Cefepime
Cephalosporins
Intravenous, active against methicillin-resistant staphylococci, broad gram-negative activity not including Pseudomonas aeruginosa
Ceftaroline
Cephalosporins
Intravenous, cephalosporin-β-lactamase inhibitor combination drugs, broad activity with improved
stability to chromosomal β-lactamase and some extended-spectrum β-lactamases
Ceftazidime-avibactam, ceftolozane-tazobactam
Clinical Applications
Serious infections such as pneumonia and sepsis
Carbapenems: Imipenemcilastatin
PKINETICS
IV administration
renal clearance (half-life 1 h), dosed every
6–8 h, cilastatin added to prevent hydrolysis by renal
dehydropeptidase
Carbapenems: Imipenemcilastatin
Toxicity
Seizures especially in renal failure or with high doses (>2 g/d)
Carbapenems: Imipenemcilastatin
Carbapenems
Intravenous, similar activity to imipenem; stable to renal dehydropeptidase, lower incidence of
seizures
Meropenem, meropenem-vaborbactam, doripenem
Carbapenems
Intravenous, longer half-life allows for once-daily dosing, lacks activity versus Pseudomonas aeruginosa and Acinetobacter
Ertapenem
Clinical Applications
Infections caused by aerobic, gram-negative
bacteria in patients with immediate hypersensitivity to
penicillins
Monobactams: Aztreonam
PKINETICS
IV administration
renal clearance half-life 1.5 h
dosed every 8 h
Monobactams: Aztreonam
Clinical Applications
No cross-allergenicity with penicillins
Monobactams: Aztreonam
MOA
Inhibits cell wall synthesis by binding to the d-Ala-d-Ala terminus of nascent peptidoglycan
Glycopeptide: Vancomycin
Effects
Bactericidal activity against susceptible
bacteria, slower kill than β-lactam antibiotics
Glycopeptide: Vancomycin
Clinical Applications
Infections caused by gram-positive bacteria including sepsis, endocarditis, and meningitis
C difficile colitis (oral formulation)
Glycopeptide: Vancomycin
PKINETICS
Oral, IV administration
renal clearance (half-life 6 h) starting dose of 30 mg/kg/d in two or three divided doses in
patients with normal renal function
trough concentrations of 10–15 mcg/mL sufficient for most infections
Glycopeptide: Vancomycin
Toxicity
“Red man” syndrome
nephrotoxicity
Glycopeptide: Vancomycin
Glycopeptide
Intravenous, similar to vancomycin except that long half-life (45–70 h) permits once-daily dosing
Teicoplanin
Glycopeptide
Intravenous, very long half-life (>10 days) permits once-weekly dosing
Dalbavancin
Glycopeptide
Intravenous, very long half-life (>10 days) permits once-weekly dosing
Dalbavancin & Oritavancin
Glycopeptide
Intravenous, once-daily dosing
Telavancin
MOA
Binds to cell membrane, causing depolarization
and rapid cell death
Lipopeptide: Daptomycin
Effects
Bactericidal activity against susceptible bacteria
more rapidly bactericidal than vancomycin
Lipopeptide: Daptomycin
Clinical Applications
Infections caused by gram-positive bacteria including sepsis and endocarditis
Lipopeptide: Daptomycin
PKINETICS
IV administration
renal clearance (half-life 8 h)
dosed once daily
inactivated by pulmonary surfactant so cannot be used to treat pneumonia
Lipopeptide: Daptomycin
Toxicity
Myopathy
Monitoring of weekly creatine phosphokinase levels recommended
Lipopeptide: Daptomycin
