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[MT 6314] Pharmacology & Toxicology > [3S] BETA-LACTAM & OTHER CELL WALL-AND MEMBRANE-ACTIVE ANTIBIOTICS (Table) > Flashcards

[3S] BETA-LACTAM & OTHER CELL WALL-AND MEMBRANE-ACTIVE ANTIBIOTICS (Table) Flashcards

1
Q

NARROW SPECTRUM PENICILLINS PKINETICS

● Long half-lives
● The drug is released slowly
● Cross the blood-brain barrier when meninges are inflamed

A

Penicillin G

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2
Q

NARROW SPECTRUM PENICILLINS PKINETICS

Pen G excretion & ROA

A

Kidneys
IM/IV

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3
Q

PENICILLINS MOA

  1. Bactericidal
  2. Prevents bacterial cell wall synthesis by binding to and inhibiting cell wall transpeptidases
  3. Inhibition of transpeptidase enzyme that act to cross-link linear peptidoglycan chains
  4. Activation of autolytic enzymes that cause lesions in the bacterial cell wall
A

Narrow Spectrum Penicillins

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4
Q

NARROW SPECTRUM PENICILLINS CA

Streptococci
Meningococci
Gram (+) bacilli and some gram (+) rods
Spirochetes
Treponema pallidum
Clostridium sp., Actinomyces
Lepstospira interrogans

A

Pen G

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5
Q

PENICILLINS TOXICITIES

● Allergy (penicilloic acid) - main toxicity
● Nausea, Vomiting, Diarrhea, Rashes, Abdominal pain, Muscle spasms, Fevers, Chills, Muscle Pains, Headaches, Flushing, Tachypnea Hypotensions, Urticaria, Tachycardia
● Jarisch-Herxheimer reaction - lesions, tachycardia, hypervetilation, myalgia, fever, sepsis; 1-3 hrs after antibiotics

A

Narrow Spectrum Penicillins

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6
Q

NARROW SPECTRUM PENICILLINS PKINETICS

● Delayed absorption;
● Can cross the BBB at MIC.

A

Benzathin & Procaine Pen G

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7
Q

NARROW SPECTRUM PENICILLINS

Benzathin & Procaine Pen G ROA

A

IM

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8
Q

NARROW SPECTRUM PENICILLINS CA

Treponema pallidum - neurosyphilis

B-hemolytic streptococcal pharyngitis Streptococci, meningococci, and pneumococci infections

Enterococci - enhanced with aminoglycosides

A

Benzathine & Procaine Pen G

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9
Q

NARROW SPECTRUM PENICILLINS CA

1st line in Syphilis

A

Benzathine Penicillin

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10
Q

NARROW SPECTRUM PENICILLINS CA

Pneumococcal
Gonorrhea

A

Procaine Pen G

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11
Q

NARROW SPECTRUM PENICILLINS PKINETICS

Low bioavailability; absorption is impaired by food

A

Pen V

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12
Q

NARROW SPECTRUM PENICILLINS PKINETICS

Pen V excretion & ROA

A

Kidney
PO

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13
Q

NARROW SPECTRUM PENICILLINS CA

Oropharyngeal infections
Infections by aerobic Gram (+) bacteria and some Gram (-) cocci (gonococci and meningococci)

A

Pen V

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14
Q

VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS PKINETICS

Excretion

A

Partly excreted in bile

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15
Q

VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS PKINETICS

Highly protein bound

A

Nafcillin

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16
Q

VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS ROA

Methicillin, Nafcillin, Oxacillin

A

IM/IV

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17
Q

VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS CA

Prototype antistaphylococcal drug

A

Methicillin

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18
Q

VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS TOXICITY

Interstitial nephritis
● useless against MRSA
● High rates of adverse effects (no longer used)

A

Methicillin

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19
Q

VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS CA

Serious staphylococcal infections (endocarditis)

A

Nafcillin & Oxacillin

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20
Q

VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS TOXICITY

Neutropenia
Interstitial nephritis

A

Nafcillin

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21
Q

VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS TOXICITY

Hepatitis

A

Oxacillin

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22
Q

VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS

Acid-stable & ROA

A

Dicloxacillin - PO

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23
Q

VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS CA

Mild to moderate localized staphylococcal infections

A

Dicloxacillin

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24
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS

● Acid-stable; can be orally absorbed
● Anti-β-lactam
● Enhanced when used with penicillinase

A

Ampicillin & Amoxicillin

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25
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS

Absorption is impaired by food

A

Ampicillin

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26
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS

Ampicillin ROA & combined with _____

A

PO/IM/IV
Sulbactam

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27
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS CA

Pneumococcal infections (drug of choice)

Serious infections caused by susceptible organisms

A

Ampicillin

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28
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS CA

● Shigella
● Anaerobes
● Enterococci
● L. monocytogenes
● β-lactamase-negative strains
o Gr(-) cocci o Gr(-) bacilli o E. coli
● Salmonella sp.

A

Ampicillin & Amoxicillin

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29
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS

Amoxicillin ROA & combined with _____

A

PO
Clavulanic Acid

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30
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS CA

● Most active - Pneumococci
● Bacterial sinusitis
● Bacterial otitis
● Lower RTIs

A

Amoxicillin

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31
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS TOXICITY

Skin rashes in the setting of viral illness

A

Amoxicillin

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32
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS

Combined with penicillinase inhibitors

A

Piperacillin & Ticarcillin

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33
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS

Piperacillin ROA & combined with ______

A

IV (same w Ticarcillin)
Tazobactam

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34
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS CA

Enhanced selectivity against Gr(-) rods
● Pseudomonas – nosocomial infections
● Enterobacter
● Klebsiella
● P. aeuriginosa

A

Piperacillin & Ticarcillin

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35
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS CA

________ with β-lactamase inhibitors:
● S. aureus

A

Piperacillin

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36
Q

WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS TOXICITY

With tazobactam:
Greater incidence of acute kidney injury (with vancomycin)

A

Piperacillin

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37
Q

CEPHALOSPORINS AND CEPHAMYCINS CA

● Gr(+) cocci
● E. coli
● K pneumoniae
● Proteus mirabilis

A

1st Gen

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38
Q

CEPHALOSPORINS AND CEPHAMYCINS CA

Extended Gr(-) activity:
o Klebsiella
o H. influenzae
o Bacteroides fragilis
o Serratia

A

2nd Gen

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39
Q

CEPHALOSPORINS AND CEPHAMYCINS CA

Expanded Gr(-) coverage
o Citrobacter
o Serratia
o Providencia
o Pseudomona

A

3rd Gen

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40
Q

CEPHALOSPORINS AND CEPHAMYCINS CA

● Pseduomonas
● Enterobacteriaceae
● Methicillin-susceptible S.aureus
● S. pneumoniae
● Haemophilus
● Neisseria sp.

A

4th Gen

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41
Q

T/F: 2nd & 3rd gen are not useful against Enterobacter

A

T

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42
Q

T/F: All 3rd gen drugs are able to cross BBB.

A

F; pera & fixi can’t cross, the rest can

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43
Q

1ST GENERATION CEPHALOSPORINS PKINETICS

Cefazolin excretion & ROA

A

Renal
IV/IM

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44
Q

CEPHALOSPORINS MOA

● Binds to PBPs to inhibit bacterial cell wall synthesis.
● Inhibits autolysin inhibitor and induces cell lysis through autolysins

A

1st Gen

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45
Q

1ST GENERATION CEPHALOSPORINS CA

● Gram-positive cocci (streptococci & staphylococci)
● Drug of choice for surgical prophylaxis
● UTI, cellulitis, soft tissue abscesses

A

Cafazolin & Cephalexin

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46
Q

1ST GENERATION CEPHALOSPORINS CA

● Can’t be used on meningitis
● Better tolerated than antistaphylococcal penicillins

A

Cefazolin

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47
Q

1ST GENERATION CEPHALOSPORINS TOXICITIES

● Surgical prophylaxis
● IV therapy
● Bacteremia
● Mild penicillin allergy

A

Cefazolin

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48
Q

1ST GENERATION CEPHALOSPORINS TOXICITIES

Pharyngitis

A

Cephalexin & Cefadroxil

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49
Q

1ST GENERATION CEPHALOSPORINS PKIENTICS

Cephalexin excretion & ROA

A

Renal
PO

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50
Q

2ND GENERATION CEPHALOSPORINS PKINETICS

Needs frequent reapplications due to short half- lives (41 to 59 min)

A

Cefoxitin & Cefotetan

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51
Q

2ND GENERATION CEPHALOSPORINS PKINETICS

Cefoxitin excretion & ROA

A

Renal
IV/IM

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52
Q

2ND GENERATION CEPHALOSPORINS MOA

Inhibits cell wall synthesis

A

Cefoxitin & Cefotetan

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53
Q

2ND GENERATION CEPHALOSPORINS CA

Anaerobic infections such as peritonitis, diverticulitis, and pelvic inflammatory disease

A

Cefoxitin & Cefotetan

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54
Q

2ND GENERATION CEPHALOSPORINS CA

● B. fragilis and some Serratia strains
● Also effective against gram-positive organisms

A

Cefoxitin & Cefotetan

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55
Q

2ND GENERATION CEPHALOSPORINS TOXICITIES

2nd-3rd & 5th main toxicity

A

Allergy, complete cross-reactivity among cephalosporins and partial to penicillins

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56
Q

2ND GENERATION CEPHALOSPORINS TOXICITIES

● May cause irritation after IM injection and thrombophlebitis after IV injection
● Possible renal toxicity, as well as interstitial nephritis and tubular necrosis

A

2nd, 3rd, 5th Gen

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57
Q

2ND GENERATION CEPHALOSPORINS PKINETICS

Cefotetan excretion & ROA

A

Renal
IV/IM

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58
Q

2ND GENERATION CEPHALOSPORINS TOXICITIES

Bleeding disroders
o Hypothrombinemia or disulfiram-like reactions with ethanol

A

Cefotetan & Cefamandole

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59
Q

2ND GENERATION CEPHALOSPORINS PKINETICS

Cefamandole excretion & ROA

A

Mainly renal partially bile
IV/IM

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60
Q

2ND GENERATION CEPHALOSPORINS MOA

Binds to PBPs to inhibit bacterial cell wall synthesis. Inhibits autolysin inhibitor

A

Cefamandole, Cefuroxime & Cefaclor

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61
Q

2ND GENERATION CEPHALOSPORINS CA

● Gram-negative organisms
● First to be effective against H. influenzae but was replaced by cefuroxime
● Also effective against gram-positive organisms
● M. catarrhalis

A

Cefamandole

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62
Q

2ND GENERATION CEPHALOSPORINS PKINETICS

Cefuroxime excretion & ROA

A

Renal
PO/IV/IM

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63
Q

2ND GENERATION CEPHALOSPORINS CA

● H. influenzae and M. catarrhalis
● Less active against B. fragilis and Serratia
● Also effective against gram-positive organisms

A

Cefuroxime & Cefaclor

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64
Q

2ND GENERATION CEPHALOSPORINS CA

● Can treat meningitis to a lesser extent than ceftriaxone or cefotaxime
● CAP
● Pneumococci

A

Cefuroxime

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65
Q

2ND GENERATION CEPHALOSPORINS CA

● crosses BBB
● CAP/COB

A

Cefuroxime Sodium

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66
Q

2ND GENERATION CEPHALOSPORINS CA

Active against B-lactamase producing bacteria

A

Cefuroxime axetil

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67
Q

3RD GENERATION CEPHALOSPORINS PKINETICS

Ceftazidime excretion & ROA

A

Kidney
IV/IM

68
Q

3RD GENERATION CEPHALOSPORINS MOA

Binds to PBPs, primarily PBP3 to inhibit bacterial cell wall synthesis.

A

Ceftazidime & Cefoperazone

69
Q

3RD GENERATION CEPHALOSPORINS CA

● GR(+), GR(-)
● P. aeruginosa infections

A

Cetazidime

70
Q

3RD GENERATION CEPHALOSPORINS PKINETICS

Cefoperazone excretion and ROA

A

Bile
IV/IM

71
Q

3RD GENERATION CEPHALOSPORINS CA

● GR(+), GR(-)
● Cannot penetrate the BBB (alongside cefixime)
● Pseudomonas

A

Cefoperazone

72
Q

3RD GENERATION CEPHALOSPORINS MOA

Binds to PBPs to inhibit bacterial cell wall synthesis.
Has better affinity with PBP 1b and PBP3

A

Cefotaxime

73
Q

3RD GENERATION CEPHALOSPORINS CA

● GR(+), GR(-)
● Primarily used to treat gonorrhea, meningitis and kidney infections.

A

Cefotaxime

74
Q

3RD GENERATION CEPHALOSPORINS CA

Most active against penicillin-non-susceptible pneumococci

A

Cefotaxime

75
Q

3RD GENERATION CEPHALOSPORINS CA

Meningitis:
Pneumococci, Meningococci, H. influenzae, Enteric gram (-) rods.

A

Cefotaxime

76
Q

3RD GENERATION CEPHALOSPORINS PKINETICS

Ceftriaxone excretion & ROA

A

Bile
IV/IM

77
Q

3RD GENERATION CEPHALOSPORINS MOA

Binds to carboxypeptidases, endopeptidases, and transpeptidases to inhibit peptidoglycan synthesis

A

Ceftriaxone

78
Q

3RD GENERATION CEPHALOSPORINS CA

● Administer with azithromycin for gonococcal infections
● Meningitis, Acute otitis media, Gonorrhea (with cefixime)

A

Ceftriaxone

79
Q

3RD GENERATION CEPHALOSPORINS PKINETICS

Resistant to gastric acid for oral absorption

A

Cefixime

80
Q

3RD GENERATION CEPHALOSPORINS PKINETICS

Cefixime excretion & ROA

A

Renal
PO

81
Q

3RD GENERATION CEPHALOSPORINS MOA

Binds to PBPs to inhibit bacterial cell wall synthesis.

A

Cefixime & Ceftizoxime

82
Q

3RD GENERATION CEPHALOSPORINS CA

● Gonorrhea (with ceftriaxone)
● Less active against pneumococci and poor activity against S. aureus

A

Cefixime

83
Q

3RD GENERATION CEPHALOSPORINS PKINETICS

Ceftizoxime excretion & ROA

A

Renal and partly bile
IV/IM

84
Q

3RD GENERATION CEPHALOSPORINS CA

B. fragilis infections

A

Ceftizoxime

85
Q

4TH GEN CEPHALOSPORINS PKINETICS

Cefepime excretion & ROA

A

Kidneys, partially liver
IV/IM

86
Q

CEPHALOSPORINS MOA

● Binds to PBPs to inhibit bacterial cell wall synthesis.
● Has better affinity with PBP 1 and PBP3 in E.coli & P. aeruginosa, and PBP2 in E. coli & E. cloacae

A

4th Gen: Cefepime

87
Q

CEPHALOSPORINS CA

Useful against GR(+) & GR(-) o P. aeruginosa
o Enterobacter
o MRSA
o S. pneumoniae
o Haemophilus
o Neisseria sp.
o Penicillin-non-susceptible streptococci strains

A

4th Gen: Cefepime

88
Q

CEPHALOSPORINS CA

● Resistant to beta- lactamases
● Penicillin-non-susceptible
● Febrile Neutropenia

A

4th Gen: Cefepime

89
Q

CEPHALOSPORINS TOXICITY

Encephalopathy, myoclonus, seizures, excitability nonconvulsive epilepticus neuromuscular and status

A

4th Gen: Cefepime

90
Q

5TH GENERATION CEPHALOSPHORINS PKINETICS

Ceftaroline Fosamil excretion & ROA

A

Kidney
IV/IM

91
Q

5TH GENERATION CEPHALOSPHORINS PKINETICS

Prodrug

A

Ceftaroline Fosalim

92
Q

5TH GENERATION CEPHALOSPHORINS MOA

Increases binding to PBP2a, lowering staphylococci’s methicillin resistance

A

Ceftaroline Fosamil

93
Q

5TH GENERATION CEPHALOSPHORINS CA

● MRSA
● Enterococci (some)
● Broad Gr(-) coverage similar to ceftriaxone

A

Ceftaroline Fosamil

94
Q

5TH GENERATION CEPHALOSPHORINS CA

● Skin and soft tissue infections
● CAP
● Off-label:
o Bacteremia
o Endocarditis
o Osteomyelitis

A

Ceftaroline Fosamil

95
Q

5TH GENERATION CEPHALOSPHORINS PKINETICS

Ceftolozane Tazobactam excretion and ROA

A

Kidneys, remaining: single metabolite
IV

96
Q

5TH GENERATION CEPHALOSPHORINS PKINETICS

Cefiderocol excretion & ROA

A

Kidneys, portian is excreted as metabolites and in feces
IV

97
Q

5TH GENERATION CEPHALOSPHORINS MOA

● Binds to PBPs to inhibit bacterial cell wall synthesis
● Tazobactam is utilized with piperacillin and ceftolozane to increase their effectiveness

A

Ceftolozane Tazobactam

98
Q

5TH GENERATION CEPHALOSPHORINS MOA

● Binds to PBP Bound by active iron transporters
● Pumped into the cell wall at high concentrations
● Passive transport

A

Cefiderocol

99
Q

5TH GENERATION CEPHALOSPHORINS CA

Gr(-)
● P. aeruginosa
● Extended β-lactamase-producing Enterobacter
● Intra-abdominal infections
● UTIs

A

Ceftolozane Tazobactam

100
Q

5TH GENERATION CEPHALOSPHORINS CA

Effective against aerobic gram-negative organisms
● Enterobacteriaceae
● P. aeruginosa
● A. baumannii
● carbapenemase producing bacteria

A

Cefiderocol

101
Q

5TH GENERATION CEPHALOSPHORINS CA

Carbapenemase-producing organisms

A

Ceftazidime-avibactam

102
Q

OTHER B-LACTAM DRUGS PKINETICS

Tolerated by penicillin-allergic patients

A

Aztreonam

103
Q

OTHER B-LACTAM DRUGS PKINETICS

Aztreonam elimination & ROA

A

Renal tubular secretion
IV

104
Q

OTHER B-LACTAM DRUGS PKINETICS

Monobactam 1st drug

A

Imipenem

105
Q

OTHER B-LACTAM DRUGS PKINETICS

● Rapidly deactivated by renal dehydropeptidases I

A

Imipenem

106
Q

OTHER B-LACTAM DRUGS PKINETICS

Inhibits renal dehydropeptidases I, increases half life, and inhibits formation of nephrotoxic metabolites

A

Monobactam: Imipenem-cilastatin

107
Q

OTHER B-LACTAM DRUGS PKINETICS

Carbapanems: Imipenem excretion & ROA

A

Renal
IV

108
Q

OTHER B-LACTAM DRUGS PKINETICS

● Similar to imipenem
● Not metabolized by dehydropeptidases

A

Carbapanems: Meropenem

109
Q

OTHER Β-LACTAM DRUGS PKINETICS

Carbapanems: Meropenem excretion & ROA

A

Renal
IV

110
Q

OTHER Β-LACTAM DRUGS PKINETICS

Longest half-life among the carbapenems (4 hours)

A

Ertapenem

111
Q

OTHER Β-LACTAM DRUGS PKINETICS

Ertapenem excretion & ROA

A

Renal
IV/IM

112
Q

OTHER Β-LACTAM DRUGS MOA

● Covalently binds to PBPs
● Susceptible to carbapenemase and metallo-B-lactamases

A

Carbapanems

113
Q

OTHER Β-LACTAM DRUGS MOA

● Inhibitor of cell wall synthesis binding to PBP3
● Synergistic with aminoglycosides

A

Monobactam: Aztreonam

114
Q

OTHER Β-LACTAM DRUGS CA

● Klebsiella, pseudomonas, serratia
● Pneumonia
● Meningitis
● Sepsis (with history of penicillin anaphylaxis)

A

Monobactam: Aztreonam

115
Q

OTHER Β-LACTAM DRUGS CA

Not active against gram (+) and anaerobes

A

Monobactam: Aztreonam

116
Q

OTHER Β-LACTAM DRUGS CA

● Gram (+) cocci, gram (-) rods, anaerobes
● Combine with aminoglycosides for pseudomonas infections
● Enterobacter

A

Carbapanems

117
Q

OTHER Β-LACTAM DRUGS CA

● Used against P. aeruginosa and penicillin-non-
susceptible pneumococci
● Febrile neutropenia

A

Carbapanems: Imipenem & Meropenem

118
Q

OTHER Β-LACTAM DRUGS TOXICITIES

● Nausea
● Vomiting
● Diarrhea
● Skin rashes
● Reactions at infusion sites
● Renal failure

A

Carbapanems: Imipenem

119
Q

OTHER Β-LACTAM DRUGS TOXICITIES

Less likely to cause seizures

A

Carbapanems: Meropenem

120
Q

BETA-LACTAMASE INHIBITORS PKINETICS

Clavulanic Acid excretion & ROA

A

Unchanged in Urine
PO/IV

121
Q

BETA-LACTAMASE INHIBITORS PKINETICS

Sulbactam excretion & ROA

A

Unchanged in urine
IM/IV

122
Q

BETA-LACTAMASE INHIBITORS PKINETICS

Tazobactam elimination & ROA

A

Kidneys
IV

123
Q

BETA-LACTAMASE INHIBITORS PKINETICS

● Does not undergo significant metabolism
● Can be found mostly unchanged in plasma

A

Relebactam

124
Q

BETA-LACTAMASE INHIBITORS PKINETICS

Relebactam ROA

A

IV

125
Q

BETA-LACTAMASE INHIBITORS PKINETICS

Avibactam & Vaborbactam excretion & ROA

A

Renal
IV

126
Q

BETA-LACTAMASE INHIBITORS MOA

Combined with?
1. Clavulanic Acid
2. Sulbactam
3. Tazobactam
4. Ceftazidime
5. Meropenem

A
  1. Amoxicillin
    2, Ampicillim
  2. Piperacillin / Ceftolozane
  3. Avibactam
  4. Avorbactam
127
Q

BETA-LACTAMASE INHIBITORS MOA

Prevents bacteria from the hydrolysis of imipenem

A

Relebactam

128
Q

BETA-LACTAMASE INHIBITORS CA

Plasmid-encoded beta-lactamases: gonococci, streptococci, E. coli, H. influenzae

A

Clavulanic Acid
Sulbactam
Tazobactam

129
Q

BETA-LACTAMASE INHIBITORS CA

Imipenem nonsusceptible P. aeruginosa
Similar activity with avibactam

A

Relebactam

130
Q

BETA-LACTAMASE INHIBITORS CA

Novel; active against Abler Class a, C, and D B-lactamases

A

Avibactam
Avorbactam

131
Q

BETA-LACTAMASE INHIBITORS TOXICITIES

● Allergic reactions (skin rash, itching, swelling of lipid, throat, face)
● Liver injury, severe diarrhea, fever

A

Clavulanic Acid

132
Q

BETA-LACTAMASE INHIBITORS TOXICITIES

● Changes in skin color, diarrhea
● Pain, tenderness, or swelling of the foot or leg

A

Sulbactam

133
Q

BETA-LACTAMASE INHIBITORS TOXICITIES

Rash, itching, hives, difficulty breathing or swallowing, wheezing, severe diarrhea

A

Tazobactam

134
Q

BETA-LACTAMASE INHIBITORS TOXICITIES

Confusion, headache, nausea, decreased urine input

A

Relebactam

135
Q

BETA-LACTAMASE INHIBITORS TOXICITIES

Nausea, vomiting, constipation, or anxiety

A

Avibactam

136
Q

BETA-LACTAMASE INHIBITORS TOXICITIES

Headache, Phlebitis, Diarrhea, Hypersensitivity, etc.

A

Avorbactam

137
Q

GLYCOPEPTIDES PKINETICS

Poorly absorbed by GI tract; only use orally for colitis (C. difficile)

A

Vancomycin

138
Q

GLYCOPEPTIDES PKINETICS

Vancomycin excretion & ROA

A

Renal
IV

139
Q

GLYCOPEPTIDES PKINETICS

Teicoplanin ROA

A

IV/IM

140
Q

GLYCOPEPTIDES PKINETICS

Telavancin ROA

A

IV

141
Q

GLYCOPEPTIDES PKINETICS

Dalbavancin & Oritavancin ROA

A

IV (+ longest half-life)

142
Q

GLYCOPEPTIDES MOA

● Bactericidal
● Binds to D-Ala-D-Ala terminal
● Inhibits transglycosylase
● Weakens peptidoglycan; becomes susceptible to lysis

A

Vancomycin & Teicoplanin

143
Q

GLYCOPEPTIDES MOA

● Binds to D-Ala-D-Ala terminal Increases membrane permeability
● Disrupts bacterial cell membrane potential

A

Telavancin

144
Q

GLYCOPEPTIDES MOA

Inhibits RNA synthesis

A

Oritavancin

145
Q

GLYCOPEPTIDES CA

● Gr(+) cocci
● Gr(+) anaerobes
o C. difficile
● MRSA
● Staphylococcus

A

Vancomycin & Teicoplanin

146
Q

GLYCOPEPTIDES CA

● With gentamicin and streptomycin
o Enterococcus faecium
o Enterococcus faecalis

A

Vancomycin & Teicoplanin

147
Q

GLYCOPEPTIDES CA

● With gentamicin: Enterococcal endocariditis
● With cefotaxime/ ceftriaxone / rifampin: Meningitis
● Colitis (oral; caused by C. difficile)

A

Vancomycin & Teicoplanin

148
Q

GLYCOPEPTIDES CA

Specific Bacteria:
● Gr(+)
● Strains with reduced susceptibility to vancomycin

Infection:
● Complicated skin and soft tissue infections
● Hospital-acquired pneumonia

A

Telavancin

149
Q

GLYCOPEPTIDES CA

Lower MICs against Gram (+) bacteria including MRSA and VRE.

A

Dalba & Orita

150
Q

GLYCOPEPTIDES CA

Osteomyelitis

A

Dalba

151
Q

GLYCOPEPTIDES TOXICITIES

● Phlebitis
● Chills and fever
● Ototoxicity (rare)
● Nephrotoxicity
● Red man syndrome

A

Vancomycin & Teicoplanin

152
Q

GLYCOPEPTIDES TOXICITIES

● Nephrotoxicity (associated)
● Teratogenic (potential)

A

Telavancin

153
Q

GLYCOPEPTIDES TOXICITIES

Mild to moderate renal or hepatic impairment

A

Dalba & Orita

154
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS PKINETICS

Excretion & ROA

A

ALL: Renal
Daptom: IV
Fosfomycin: IM/IV/PO
Bacitracin: Topical
Cycloserine: PO

155
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS MOA

● Calcium-dependent insertion to cell membrane
● Depolarization
● Potassium efflux
● Rapid cell death

A

Daptomycin

156
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS MOA

● Antimetabolite inhibitor of enolpyruvate transferase
● Binds covalently to cysteine residue
● Inhibits addition of phosphoenolpyruvate to UDP-N-acetylglucosamine

A

Fosfomycin

157
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS MOA

Interferes with dephosphorylation in the cycling of the lipid carrier that transfers peptidoglycan subunits

A

Bacitracin

158
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS MOA

● Inhibits incorporation of d- alanine into peptidoglycan pentapeptide
● Inhibits alanine racemase

A

Cycloserine

159
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS CA

● Similar activity to vancomycin
● Active against vancomycin- resistant strains of
enterococci and S. aureus (VRE & VRSA)

A

Daptomycin

160
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS CA

● Gram (+) and gram (-)
● UTI, pyelonephritis
● Safe for pregnancy

A

Fosfomycin

161
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS CA

● Bacterial infections on surface skin lesions or mucous membranes
o Gr(+)

A

Bacitracin

162
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS CA

● Tuberculosis resistant to first-line agents
o strains of Mycobacterium tuberculosis

A

Cycloserine

163
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS TOXICITIES

● Myopathy
● Allergic pneumonitis
● Not used for pneumonia (antagonized by pulmonary surfactant)

A

Daptomycin

164
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS TOXICITIES

Diarrhea, nausea, headache fungal vaginitis, allergy, etc.

A

Fosfomycin

165
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS TOXICITIES

● Highly nephrotoxic (systemic administration)
● Hypersensitivity

A

Bacitracin

166
Q

OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS TOXICITIES

Neurotoxicity - tremors, seizures, convulsions, psychosis

A

Cycloserine

[MT 6314] Pharmacology & Toxicology (20 decks)

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