[3S] Chemotherapeutic Agents Summary

Question 1

MOA

Prevents bacterial cell wall synthesis by binding to and inhibiting cell wall transpeptidases

Answer 1

Pen G, Cefazolin, Imipenemcilastatin, Aztreonam

Question 2

Effects

Rapid bactericidal activity against susceptible bacteria

Answer 2

Pen G, Cefazolin, Imipenemcilastatin, Aztreonam

Question 3

Clinical Applications

Streptococcal infections, meningococcal infections,
neurosyphilis

Answer 3

Pen G

Question 4

ROA Pen G

Answer 4

IV/IM

Question 5

PKINETICS

rapid renal clearance (half-life 30 min, so requires dosing every 4 h)

Answer 5

Pen G

Question 6

Interactions

Immediate hypersensitivity, rash, seizures

Answer 6

Pen G

Question 7

Penicillin

Oral, low systemic levels limit widespread use

Answer 7

Penicillin V

Question 8

Penicillin

Oral, low systemic levels limit widespread use

Answer 8

Penicillin V

Question 9

Penicillin

Greater activity versus gram-negative bacteria; addition of β-lactamase inhibitor restores activity against many βlactamase-producing bacteria

Answer 9

Ampicillin, amoxicillin, piperacillin:

Question 10

Penicillin

Intramuscular, long-acting formulations

Answer 10

Benzathine penicillin, procaine penicillin

Question 11

Penicillin

Intravenous, added stability to staphylococcal β-lactamase, biliary clearance

Answer 11

Nafcillin, oxacillin

Question 12

PKINETICS

IV administration
renal clearance (half-life 1.5 h)
given every 8 h
poor penetration into the central nervous system

Answer 12

Cephalosporins: Cefazolin

Question 13

Clinical Applications

Skin and soft tissue infections, urinary tract
infections, surgical prophylaxis

Answer 13

Cephalosporins: Cefazolin

Question 14

Toxicity

Rash, drug fever

Answer 14

Cephalosporins: Cefazolin

Question 15

Cephalosporins

Oral, first-generation drug used for treating skin and soft tissue infections and urinary tract infections

Answer 15

Cephalexin

Question 16

Cephalosporins

Oral and intravenous, second-generation drug, improved activity versus pneumococcus and Haemophilus influenzae

Answer 16

Cefuroxime

Question 17

Cephalosporins

Intravenous, second-generation drugs, activity versus Bacteroides fragilis allows for use in abdominal/pelvic infections

Answer 17

Cefotetan, cefoxitin

Question 18

Cephalosporins

Intravenous, third-generation drug, mixed clearance with long half-life (6 hours), good CNS penetration, many uses including pneumonia, meningitis, pyelonephritis, and gonorrhea

Answer 18

Ceftriaxone

Question 19

Cephalosporins

Intravenous, third-generation, similar to ceftriaxone; however, clearance is renal and half-life is 1 hour

Answer 19

Cefotaxime

Question 20

Cephalosporins

Intravenous, third-generation drug, poor gram-positive activity, good activity versus Pseudomonas aeruginosa

Answer 20

Ceftazidime

Question 21

Cephalosporins

Intravenous, fourth-generation drug, broad activity with improved stability to chromosomal β-lactamases

Answer 21

Cefepime

Question 22

Cephalosporins

Intravenous, active against methicillin-resistant staphylococci, broad gram-negative activity not including Pseudomonas aeruginosa

Answer 22

Ceftaroline

Question 23

Cephalosporins

Intravenous, cephalosporin-β-lactamase inhibitor combination drugs, broad activity with improved
stability to chromosomal β-lactamase and some extended-spectrum β-lactamases

Answer 23

Ceftazidime-avibactam, ceftolozane-tazobactam

Question 24

Clinical Applications

Serious infections such as pneumonia and sepsis

Answer 24

Carbapenems: Imipenemcilastatin

Question 25

PKINETICS IV administration renal clearance (half-life 1 h), dosed every 6–8 h, cilastatin added to prevent hydrolysis by renal dehydropeptidase

Answer 25

Carbapenems: Imipenemcilastatin

Question 26

Toxicity Seizures especially in renal failure or with high doses (>2 g/d)

Answer 26

Carbapenems: Imipenemcilastatin

Question 27

Carbapenems Intravenous, similar activity to imipenem; stable to renal dehydropeptidase, lower incidence of seizures

Answer 27

Meropenem, meropenem-vaborbactam, doripenem

Question 28

Carbapenems Intravenous, longer half-life allows for once-daily dosing, lacks activity versus Pseudomonas aeruginosa and Acinetobacter

Answer 28

Ertapenem

Question 29

Clinical Applications Infections caused by aerobic, gram-negative bacteria in patients with immediate hypersensitivity to penicillins

Answer 29

Monobactams: Aztreonam

Question 30

PKINETICS IV administration renal clearance half-life 1.5 h dosed every 8 h

Answer 30

Monobactams: Aztreonam

Question 31

Clinical Applications No cross-allergenicity with penicillins

Answer 31

Monobactams: Aztreonam

Question 32

MOA Inhibits cell wall synthesis by binding to the d-Ala-d-Ala terminus of nascent peptidoglycan

Answer 32

Glycopeptide: Vancomycin

Question 33

Effects Bactericidal activity against susceptible bacteria, slower kill than β-lactam antibiotics

Answer 33

Glycopeptide: Vancomycin

Question 34

Clinical Applications Infections caused by gram-positive bacteria including sepsis, endocarditis, and meningitis C difficile colitis (oral formulation)

Answer 34

Glycopeptide: Vancomycin

Question 35

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

Answer 35

Glycopeptide: Vancomycin

Question 36

Toxicity “Red man” syndrome nephrotoxicity

Answer 36

Glycopeptide: Vancomycin

Question 37

Glycopeptide Intravenous, similar to vancomycin except that long half-life (45–70 h) permits once-daily dosing

Answer 37

Teicoplanin

Question 38

Glycopeptide Intravenous, very long half-life (>10 days) permits once-weekly dosing

Answer 38

Dalbavancin

Question 39

Glycopeptide Intravenous, very long half-life (>10 days) permits once-weekly dosing

Answer 39

Dalbavancin & Oritavancin

Question 40

Glycopeptide Intravenous, once-daily dosing

Answer 40

Telavancin

Question 41

MOA Binds to cell membrane, causing depolarization and rapid cell death

Answer 41

Lipopeptide: Daptomycin

Question 42

Effects Bactericidal activity against susceptible bacteria more rapidly bactericidal than vancomycin

Answer 42

Lipopeptide: Daptomycin

Question 43

Clinical Applications Infections caused by gram-positive bacteria including sepsis and endocarditis

Answer 43

Lipopeptide: Daptomycin

Question 44

PKINETICS IV administration renal clearance (half-life 8 h) dosed once daily inactivated by pulmonary surfactant so cannot be used to treat pneumonia

Answer 44

Lipopeptide: Daptomycin

Question 45

Toxicity Myopathy Monitoring of weekly creatine phosphokinase levels recommended

Answer 45

Lipopeptide: Daptomycin