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[MT 6314] Pharmacology & Toxicology > [3S] Chemotherapeutic Agents Summary > Flashcards

[3S] Chemotherapeutic Agents Summary Flashcards

1
Q

MOA

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

A

Pen G, Cefazolin, Imipenemcilastatin, Aztreonam

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2
Q

Effects

Rapid bactericidal activity against susceptible bacteria

A

Pen G, Cefazolin, Imipenemcilastatin, Aztreonam

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3
Q

Clinical Applications

Streptococcal infections, meningococcal infections,
neurosyphilis

A

Pen G

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4
Q

ROA Pen G

A

IV/IM

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5
Q

PKINETICS

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

A

Pen G

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6
Q

Interactions

Immediate hypersensitivity, rash, seizures

A

Pen G

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7
Q

Penicillin

Oral, low systemic levels limit widespread use

A

Penicillin V

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8
Q

Penicillin

Oral, low systemic levels limit widespread use

A

Penicillin V

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9
Q

Penicillin

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

A

Ampicillin, amoxicillin, piperacillin:

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10
Q

Penicillin

Intramuscular, long-acting formulations

A

Benzathine penicillin, procaine penicillin

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11
Q

Penicillin

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

A

Nafcillin, oxacillin

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12
Q

PKINETICS

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

A

Cephalosporins: Cefazolin

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13
Q

Clinical Applications

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

A

Cephalosporins: Cefazolin

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14
Q

Toxicity

Rash, drug fever

A

Cephalosporins: Cefazolin

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15
Q

Cephalosporins

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

A

Cephalexin

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16
Q

Cephalosporins

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

A

Cefuroxime

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17
Q

Cephalosporins

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

A

Cefotetan, cefoxitin

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18
Q

Cephalosporins

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

A

Ceftriaxone

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19
Q

Cephalosporins

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

A

Cefotaxime

20
Q

Cephalosporins

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

A

Ceftazidime

21
Q

Cephalosporins

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

A

Cefepime

22
Q

Cephalosporins

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

A

Ceftaroline

23
Q

Cephalosporins

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

A

Ceftazidime-avibactam, ceftolozane-tazobactam

24
Q

Clinical Applications

Serious infections such as pneumonia and sepsis

A

Carbapenems: Imipenemcilastatin

25
Q

PKINETICS

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

A

Carbapenems: Imipenemcilastatin

26
Q

Toxicity

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

A

Carbapenems: Imipenemcilastatin

27
Q

Carbapenems

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

A

Meropenem, meropenem-vaborbactam, doripenem

28
Q

Carbapenems

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

A

Ertapenem

29
Q

Clinical Applications

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

A

Monobactams: Aztreonam

30
Q

PKINETICS

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

A

Monobactams: Aztreonam

31
Q

Clinical Applications

No cross-allergenicity with penicillins

A

Monobactams: Aztreonam

32
Q

MOA

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

A

Glycopeptide: Vancomycin

33
Q

Effects

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

A

Glycopeptide: Vancomycin

34
Q

Clinical Applications

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

A

Glycopeptide: Vancomycin

35
Q

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

A

Glycopeptide: Vancomycin

36
Q

Toxicity

“Red man” syndrome
nephrotoxicity

A

Glycopeptide: Vancomycin

37
Q

Glycopeptide

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

A

Teicoplanin

38
Q

Glycopeptide

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

A

Dalbavancin

39
Q

Glycopeptide

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

A

Dalbavancin & Oritavancin

40
Q

Glycopeptide

Intravenous, once-daily dosing

A

Telavancin

41
Q

MOA

Binds to cell membrane, causing depolarization
and rapid cell death

A

Lipopeptide: Daptomycin

42
Q

Effects

Bactericidal activity against susceptible bacteria
more rapidly bactericidal than vancomycin

A

Lipopeptide: Daptomycin

43
Q

Clinical Applications

Infections caused by gram-positive bacteria including sepsis and endocarditis

A

Lipopeptide: Daptomycin

44
Q

PKINETICS

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

A

Lipopeptide: Daptomycin

45
Q

Toxicity

Myopathy
Monitoring of weekly creatine phosphokinase levels recommended

A

Lipopeptide: Daptomycin

[MT 6314] Pharmacology & Toxicology (20 decks)

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