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Antimicrobial's pharmacology > B-lactam wall inhibitors > Flashcards

B-lactam wall inhibitors Flashcards

1
Q

Groups of drugs that inhibit the cell wall (6)

A

Penicillins and aminopenicillins
B-lactamase inhibitors
Cephalosporins
Carbapenems
Monobactams
Non-B-lactam cell wall inhibitors

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2
Q

Natural penicillins

A

Benzylpenicillin (penicillin G)
Benzathine penicillin G
Procaine penicillin G
Penicillin V

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3
Q

Long acting natural penicillins

A

Benzathine penicillin G
Procaine penicillin G

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4
Q

Mechanism of action of natural penicillins

A

Inhibition of peptidoglycan synthesis by blocking the transpeptidation reaction of D-alanyl-D-alanine –> acetilation of transpeptidases by binding PBPs (bactericidal)

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5
Q

Benzylpenicillin Penicillin G spectrum - Gram positive bacteria

A
  • Streptococci: Rheumatic fever, endocarditis (S. viridans, S. bovis), Group B strep prophylaxis (S. agalactiae)
  • Clostridium perfringens (gas gangrene)
  • S. pyogenes, S. pneumoniae (w/ vancomycin + 3rd-gen cephalosporin)
  • Actinomyces israelii (agent of choice)
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6
Q

Benzylpenicillin Penicillin G spectrum - Gram negative bacteria

A
  • Actinomyces israelii
  • Pasteurella multocida (dog/cat bites)
  • Listeria monocytogenes (agent of choice, combined with gentamicin)
  • n. Meningitis
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7
Q

Benzylpenicillin Penicillin G spectrum - Spirochetes

A
  • Leptospira spp. (leptospirosis)
  • Treponema pallidum (syphilis)
  • Borrelia burgdorferi (Lyme disease)
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8
Q

Adverse effects of penicillin G

A
  • IgE-mediated hypersensitivity reactions
  • Direct Coombs+ hemolytic anemia
  • Drug-induced interstitial nephritis
  • Impaired hemostasis
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9
Q

Contraindications & cautions of benzylpenicilline (Penicillin G)

A
  • Never IV with benzathine formulation → toxicity
  • Uremia or Probenecid use → toxic CNS levels → seizures
  • Better CSF penetration if meninges are inflamed
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10
Q

Resistance mechanisms of Penicillin G (benzylpenicilline)

A
  • Ineffective against most S. aureus & S. epidermidis
  • β-lactamases (penicillinases) cleave β-lactam ring
  • Mutations in PBPs → decreased binding affinity
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11
Q

Long acting form of penicillin G

A

Benzathine Penicillin G = slow absorption

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12
Q

Difference in uses between penicillins G

A
  • Benzylpenicillin G = severe infections (endocarditis, meningitis, syphilis)
  • Benzathine penicillin G = long term therapy or prohylaxis
  • Procaine penicillin G = less frequent dosing
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13
Q

Main contraindication of procaine penicillin

A

IM ONLY NEVER IV (toxicity risk)

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14
Q

Procaine penicillin Spectrum – Gram-Positive Bacteria

A
  • Rheumatic fever prophylaxis
  • Left-sided endocarditis (S. viridans, S. bovis) + gentamicin
  • Group B strep (S. agalactiae) intrapartum prophylaxis
  • Clostridium perfringens (gas gangrene)
  • Streptococcus pyogenes
  • Streptococcus pneumoniae (with vancomycin + 3rd-gen cephalosporin)
  • Actinomyces israelii (agent of choice)
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15
Q

Procaine penicillin Spectrum – Gram-Negative Bacteria

A
  • Actinomyces israelii
  • Streptobacillus moniliformis
  • Pasteurella multocida (dog/cat bites)
  • Listeria monocytogenes (agent of choice, with gentamicin)
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16
Q

Procaine penicillin Spectrum – Spirochetes

A
  • Leptospira spp. (Leptospirosis)
  • Treponema pallidum (Syphilis)
  • Borrelia burgdorferi (Lyme disease)
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17
Q

Procaine penicillin G adverse effects

A
  • IgE-mediated hypersensitivity reactions
  • Direct Coombs+ hemolytic anemia
  • Drug-induced interstitial nephritis
  • Impaired hemostasis
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18
Q

Procaine penicillin G contraindications & cautions

A
  • NEVER IV → Risk of Hoigné syndrome (CNS toxicity: hallucinations, seizures, anxiety, dizziness)
  • Risk of CNS toxicity (seizures) in uremic patients or when combined with Probenecid
  • Penetrates CSF better if meninges are inflamed
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19
Q

Procaine penicillin G resistance mechanisms and which are resistant microorganisms

A
  • Ineffective against most S. aureus & S. epidermidis
  • β-lactamases (penicillinases) cleave β-lactam ring
  • Mutations in PBPs → decreased binding affinity
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20
Q

Forms of administration of penicillin G

A
  • Benzylpenicillin G = IM, IV
  • Benzathine penicillin G = IM ONLY
  • Procaine penicillin G = IM ONLY
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21
Q

Aminopenicillins

A

Ampicillin
Amoxicillin

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22
Q

Ampicillin administration

A

PO and IM

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23
Q

Mechanism of action of ampicillin

A

Inhibit peptidoglycan synthesis by blocking the transpeptidation reaction of D-alanyl-D-alanine

Acylates transpeptidases by binding PBPs

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24
Q

Without with clavulanic acid for β-lactamase protection, ampicillin is…

A

Penicillinase-sensitive

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25
Q

Gram-positive bacteria with ampicillin coverage

A
  • Enterococci (more sensitive than to penicillin)
  • Endocarditis (combine with gentamicin or ceftriaxone)
  • Listeria monocytogenes
  • Meningitis (combine with vancomycin + 3rd-gen cephalosporin)
  • Streptococcus pyogenes
  • Streptococcus pneumoniae
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26
Q

Gram-negative bacteria with ampicillin coverage (HHELPSS)

A
  • Haemophilus influenzae
  • Helicobacter pylori
  • Escherichia coli (non-resistant strains)
  • Listeria monocytogenes
  • Proteus mirabilis
  • Salmonella
  • Shigella
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27
Q

Major adverse effects of ampicillin

A
  • Hypersensitivity reactions
  • Rash
  • Pseudomembranous colitis (C. difficile overgrowth)
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28
Q

Contraindications of ampicillin

A
  • Infectious Mononucleosis (IM) / Epstein-Barr Virus Infection → Rash
  • Severe renal impairment (without dose adjustment)
  • Interaction with Allopurinol (increases rash risk)
  • Hepatotoxic in severe liver disease
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29
Q

Ampicillin adverse effects

A
  • Increased risk of C. difficile colitis (gut flora disruption)
  • Hepatotoxic in severe liver disease
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29
Q

Resistance mechanism of ampicillin

A
  • β-lactamase hydrolyzes the drug → Requires β-lactamase inhibitor (e.g., clavulanate, sulbactam)
  • Penicillinase cleaves β-lactam ring
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30
Q

Role of clavulanate or sulbactam in ampicillin use

A

Expands activity spectrum against β-lactamase-producing bacteria

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31
Q

Administration method of amoxicillin

A

Oral intake (food does not interfere with absorption)

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32
Q

Amoxicillin MOA

A

Inhibit peptidoglycan synthesis by blocking the transpeptidation reaction of D-alanyl-D-alanine

Acylates transpeptidases by binding PBPs

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33
Q

Gram-positive espectrum of amoxicillin

A
  • Enterococci
    - UTIS || combine with clavulanate
    • Lysteria monocytogenes
    • S. pneumoniae
    • S. pyogenes
  • Staph
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34
Q

Gram-negative espectrum of amoxicillin

A

Gram negative bacteria
- Klebsiella
- UTIs || combine with clavulanate
- H. influenzae
- H. pylori
- E. coli (non-resistant strains)
- Proteus mirabilis
- Salmonella
- Shigella (↓↓ effective than ampicilin)

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35
Q

Amoxicillin works as empiric treatment for

A

Community acquired pneumonia

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36
Q

Alternative treatment to penicillin for bacterial pharyngitis

A

Amoxicillin + clavulanate

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37
Q

Adverse effects of amoxicillin

A
  • Hypersensitivity reactions
  • Rash
  • Pseudomembranous colitis
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38
Q

When should you NOT give amoxicillin?

A
  • History of severe hypersensitivity reactions
  • Infectious mononucleosis or Epstein-Barr virus
  • Severe renal impairment
  • When taking ALLOPURINOL
  • In hepatic dysfunction
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39
Q

Amoxicillin mechanism of resistance

A
  • Hydrolization by B-lactamases
  • Penicillinase cleaves B-lactam ring
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40
Q
A
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41
Q

Antipseudomonal carboxypenecillins

A
  • Carbenicillin
  • Ticarcillin
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42
Q

Admin. of carbenicillin

A

PO

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43
Q

Antipseudomonal carboxypenicillins mechanism of action

A

Inhibit peptidoglycan synthesis by blocking the transpeptidation reaction of D-alanyl-D-alanine

Acylates transpeptidases by binding PBPs

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43
Q

Antipseudomonal carboxypenicillins (carbenicillin & ticarcillin) therapeutic use

A

ONLY urinary infections by proteus spp. and pseudomonnas aeruginosa

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44
Q

Antipseudomonal carboxypenicillins (carbenicillin & ticarcillin) adverse effects

A
  • Hypersensitivity reactions (Anaphylaxis)
  • Impaired hemostasis (platelet disfunction and neutropenia)
  • Hypokalemia
  • Nephrotoxicity
  • GI effects
  • Neurotoxicity
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45
Q

Food absorption and aminopenicillins

A

Amoxicillin - doesn’t affect
Ampicillin - reduces absorption

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46
Q

Carbenicillin resistant microorganism

A

P. mirabilis

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47
Q

Carboxypenicillins mechanisms of resistance

A
  • B-lactamase production
  • Altered PBPs
  • Efflux pumps
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48
Q

Resistance to carboxypenicillins by Pseudomonas aeruginosa occurs because of

A

Porin mutations in the gram-negative bacteria

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49
Q

Antipseudomonal Ureidopenicillin

A

Piperacillin (Puperacillin)

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50
Q

Acid stable carboxypenicillin (PO)

A

Carbenicillin

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51
Q

Discontinued IV carboxypenicillin

A

Ticarcillin

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52
Q

Divisions of antipseudomonal B-lactamase-inhibitors

A

Carboxypenicillins and ureidopenicillins

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53
Q

Combined with tazobactam (B-lactamase inhibitor) this antipseudomonal ureidopenicillin has the broadest spectrum of penicillins

A

Piperacillin

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54
Q

Admin form of piperacillin

A

IV

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55
Q

Piperacillin MOA

A

Inhibit peptidoglycan synthesis by blocking the transpeptidation reaction of D-alanyl-D-alanine

Acylates transpeptidases by binding PBPs

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56
Q

Therapeutic uses of piperacillin

A

Bacteremias
Pneumonias (P. aeruginosa, H. influenzae)
Infections following burns
UTIs (resistant to ampicillin; Klebsiella)
Mixed intra-abdominal infections (E. coli)

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57
Q

Piperacillin gram-positive bacteria spectrum

A

E. faecalis and MSSA

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58
Q

Gram-negative spectrum of piperacillin

A
  • P. aeruginosa
  • Enterobacterales (non-ß-lactamase producing)
  • Bacteroides spp.
  • H. influenzae
  • B. fragilis
  • E. coli
  • Klebsiella
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59
Q

Piperacillin adverse effects

A
  • Hypersensitivity reactions (anaphylaxia)
  • Impaired hemostasis (platelet disfunction and neutropenia)
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60
Q

Piperacillin contraindications

A

Allergy to penicillins or beta-lactams
History of severe hypersensitivity reactions
Renal impairment
Concurrent use with methotrexate (increased toxicity risk)
Severe electrolyte imbalance

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61
Q

Dicloxacillin, Nafcillin, Oxacillin, Floxacillin and Methicillin belong to…

A

Penicillinase-resistant penicillins

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62
Q

Administration of Dicloxacillin, Nafcillin, Oxacillin, Floxacillin and Methicillin

A

Oral or IV

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63
Q

Why are penicillinase-resistant penicillins effective?

A

Penicillinase resistant because bulky R group (side chains) blocks access of β-lactamase to β-lactam ring and its further hydrolyzation

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64
Q

MOA of penicillinase-resistant penicillins

A

Inhibit peptidoglycan synthesis by blocking the transpeptidation reaction of D-alanyl-D-alanine

Acylates transpeptidases by binding PBPs

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65
Q

Gram positive spectrum of PR-Penicillins

A

S. aureus NON MRSA (Gram positive aerobes)

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66
Q

Penicillinase-resistant penicillins adverse effects

A

Hypersensitivity reactions
Interstitial nephritis (methicillin)
Hepatitis

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67
Q

Doxacillin, oxacillin, methicillin, nafcillin and foxacillin contraindications

A

Hypersensitivity

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68
Q

Mechanism of resistance of penicillin-resistant-penicillins

A
  • Alteration of PBP binding site = reduced affinity = pathogen is not bound or inactivated by B-lactam
  • MRSA alteration of PBP target is one of its main virulence factors
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69
Q

Penicillins are effective against amebae, plasmodia, rickettsiae, fungi or viruses

A

FALSE

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70
Q

Interaction of PROBENECID + penicillins

A

Decreases tubular secretion and VOD of penicillins

Penicillins stay more time on the body

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71
Q

Interaction between food and penicillins

A

Food ingestion may interfere with enteric absorption of ALL penicillins

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72
Q

Clavulanate acid, Clavulanate, Sulbactam, Tazobactam and Avibactam are…

A

B-lactamase inhibitors

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73
Q

ADME of clavulanate and clavulanate acid

A

PO and parenteral

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74
Q

PO form of clavulanate must be combined with

A

Amoxicilin

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75
Q

Parenteral form of clavulanate must be combined with

A

Ticarcilin

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76
Q

Older B-lactamase inhibitors (Clavulanate, sulbactam, tazobactam) MOA

A

Inactivate plasmid-encoded B lactamases

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77
Q

Older B-lactamase inhibitors fail to provide protection against…

A

AmpC β-lactamases encoded chromosomally in some gram-negative bacilli and carbapenemases

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78
Q

Amoxicillin + clavulanate target

A

Staphylococcus aureus
Haemophilus influenzae
Certain enterobacterales

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79
Q

Clavulanate/clavulanate acid adverse effects

A

GI disturbances; nausea and diarrhea
Hypersensitivity
Hepatotoxicity

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80
Q

Clavulanate contraindications

A

Allergy to penicillins or B lactams
Severe liver disease

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81
Q

Clavulanate and food

A

Better tolerated
Delayed absorption (not significant)

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82
Q

B-lactamase inhibitors + methrotexate

A

Reduction of renal clearance of methotrexate = increased toxicity risk

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83
Q

Clavulanate or sulbactam + warfarin

A

Enhanced anticoagulant effects = more bleeding risk

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84
Q

B-lactamase inhibitors + probenecid

A

Increased drug levels and prolonged effects

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85
Q

Amoxicillin + clavulanate and allopurinol increase the risk of…

A

Rash

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86
Q

Sulbactam ADME

A

IV or IM
Combined with ampicillin and cefoperazone

87
Q

Sulbactam therapeutic use

A

Activity against Acinetobacter spp

Multidrug-resistant acinetobacter infections

88
Q

Sulbactam adverse effects

A

Local injection site reactions
Hypersensitivity
Hepatotoxicity

89
Q

Sulbactam and tazobactam contraindications

A

Allergy to penicillins or B lactams
Severe renal impairment

90
Q

Resistance in sulbctam is due to:

A

AmpC β-lactamases and carbapenemase-producing bacteria

91
Q

Tazobactam ADME

A

Parenteral
Combinated with piperacillin and ceftolozane

92
Q

Tazobactam + piperacillin attacks

A

Pseudomonas aeruginosa
Enterobacterales
Anaerobes

93
Q

Tazobactam + ceftolozane

A

ESBL-producing gram negative bacteria

94
Q

Tazobactam side effects

A

GI disturbances
Hypersensitivity reactions
Elevated liver enzymes

95
Q

Resistance to tazobactam is due to

A

AmpC β-lactamases and metallo-β-lactamases

96
Q

New generation B-lactamase

97
Q

Avibactam is coformulated with

A

Ceftazidime

98
Q

Avibactam MOA

A

Narrow- and extended-spectrum β-lactamase (ESBL)-type
Chromosomal AmpC
KPC-type β-lactamases

99
Q

Avibactam has no action against

A

metallo-B-lactamases

100
Q

Avibactam + ceftazidime therapeutic uses

A

Carbapenem-resistant enterobacterales

Multidrug resistant pseudomonas aeruginosa

101
Q

Avibactam adverse effects

A

GI disturbances
CNS effects
Hypersensitivity reactions

102
Q

Avibactam contraindications

A

Allergy to cephalosporins
Severe renal impairment

103
Q

Why is there no food interaction with sulbactam, tazobactam or avibactam?

A

They’re given parenterally

104
Q

Cephalosporins MOA

A

Inhibition of cell wall synthesis but PBPs differ somewhat from penicillins

105
Q

1st gen cephalosporins

A

Cephalexin
Cefazolin
Cefalotin

106
Q

2nd gen cephalosporins

A

Cefaclor
Cefuroxime
Cefoxitin
Cefotetan

“Fake fox furious for tea”

107
Q

3rd generation cephalosporins

A

Ceftriaxone
Cefotaxime
Ceftizoxime
Ceftixime
Ceftazidime

108
Q

4th gen cephalosporins

A

Cefepime
Cefpirome
Cefpiramide

109
Q

5th generation

A

Ceftaroline
Ceftobiprole
Ceftolozane

110
Q

First generation cephalosporins adme

111
Q

1st gen cephalosporin of choice for surgical prophylacxis

A

Cephazoline - prevent S. aureus infections

112
Q

Cephazolin IM is preferred for

A

Endocarditis

113
Q

First gen cephalosporins therapeutic uses

A

Skin and soft­tissue infections

Serious infections due to MSSA

Perioperative surgical prophylaxis

UTI infections

114
Q

1st gen cephalosporins have excellent effect on…

A

Gram positive streptococcus and MSSA

115
Q

1st gen cephalosporins PEcK

A

Gram negative infections:
Proteus
E. coli
Klebsiella

116
Q

1st gen cephalosporin resistance mechanisms

A

Inactivation by hydrolisis of the B-lactam ring

Susceptible to hydrolisis by inducible ampC B-lactamases in gram-negative bacteria

Inactivation by cephalosporinase

Change in PBP structure

117
Q

Cephalosporin generation against upper respiratory tract infections (sinusitis, otitis media)

A

2nd generation

118
Q

Cefoxitin/Cefotetan main therapeutic uses are:

A

Gynecologic infections, perioperative surgical prophylaxis

119
Q

2nd generation cephalosporins have good activity against these gram positive microbes

A

MSSA
Streptococci

120
Q

Gram negative spectrum of 2nd generation cephalosporins (HENSPEcK)

A

H. influenzae
E. aerogenes
Neisseria spp
Serratia marcescens
Proteus mirabilis
E. coli
Klebsiella

121
Q

2nd generation meds with some activity against B. fragilis

A

Cefotetan
Cefoxitin

122
Q

Main resistance mechanism of 2nd generation cephalosporins

A

Susceptible to hydrolysis by inducible ampC B-lactamases in gram-negative bacteria (Citrobacter, Enterobacter and Pseudomonas)

123
Q

ADME of 3rd generation cephalosporins

A

IV
Ceftriaxone = IM

124
Q

3rd gen cephalosporins that cross BBB

A

Ceftriaxone and cefotaxime

125
Q

Main therapeutic uses of 3rd gen cephalosporins

A

Community ­acquired pneumonia
Meningitis
Urinary tract infections Streptococcal endocarditis Gonorrhea
Severe Lyme disease

126
Q

3rd gen cephalosporin that treats borrelia burdorferi lyme disease gonorrhea

A

Ceftriaxone (IM)

127
Q

3rd generation cephalosporin that treats Pseudomonaz

A

CeftAZidime

128
Q

3rd gen drugs that treat meningitis by S. pneumoniae

A

Ceftriaxone
Cefotaxime

129
Q

3rd generation resistance mechanisms

A

Alterations in two PBPs (1A and 2X)

Change in transpeptidase (PBP) structure

hHydrolysis by inducible ampC B-lactamases in gram-negative bacteria

Cephalosporinases

130
Q

Antipseudomonal cephalosporins

A

4th generation
Cefepime
Cefpirome
Cefpiramide

131
Q

ADME of 4th generation cephalosporins

A

Parenteral IV

132
Q

4th gen cephalosporins main therapeutic use

A

Nosocomial infections: pneumonia, meningitis, urinary tract infections, intra­abdominal infections

133
Q

4th gen cephalosporins have excellent activity against

A

H. influenzae
Proteus
E. coli
Klebsiella
Serratia
Neisseria
streptococci
MSSA
Pseudomonas aeruginosa

134
Q

Cephalosporin generation that works against MRSA

135
Q

5th gen cephalosporins (IV)

A

Ceftaroline
Ceftobiprole
Ceftolozane

136
Q

Ceftaroline fosamil therapeutic uses

A

MRSA
Penicillin-resistant S. pneumoniae
Gram negative activity

137
Q

Ceftobiprole medocaril

A

MRSA
Penicillin resistant S. pneumoniae
Pseudomonas spp.

138
Q

Generation susceptible to resistance because of EFFLUX, hydrolysis by ESBLs and to a significant extent to KPCs

139
Q

Generations that cross BBB

A

3rd and 4th

140
Q

Organisms not covered by 1-4th generation are LAME

A

Listeria
Atypical chlamydia, mycoplasma
MRSA
Enterococci

141
Q

At high doses, —— can cause encephalopathy

142
Q

Cephalosporin generations with good CSF penetration

143
Q

Ceftaroline is mostly used for:

A

Community ­acquired pneumonia
Skin and soft­ tissue infections

144
Q

Most important cephalosporins adverse effects

A

Autoinmune hemolytic anemia
Vitamin K deficiency
Disulfram-like reaction (flushing, tachycardia, hypotension)
Neurotoxicicty
Positive coombs reaction
Granulocytopenia

145
Q

Effects of cephalosporins in neonates

A

Hyperbilirrunemia or jaundice - ceftriaxone

Administer cefotaxime

146
Q

Cephalosporins + aminoglycosides cause

A

NEPHROTOXIC EFFECT

147
Q

When using cephalosporins for intra-abdominal infections, ——- is required

A

Anaerobic coverage (ex. metronidazole)

148
Q

C. difficile and campylobacter jejuni can be treated with cephalosporins

149
Q

Patients with mononucleosis or epstein barr should not take

A

Ampicillin

150
Q

Ampicillin + allopurinol

A

Increases rash risk

151
Q

Combo para tratar la meningitis por l. monocytogenes

A

Ampicillin + vancomycin + 3rd gen cephalosporin

152
Q

tx. empirico para meningitis por s. pneumoniae

A

Vancomicina + ceftriaxona

153
Q

Tx. para meningitis por H. influenzae

A

Ceftriaxona (3rd gen cephalosporine)

154
Q

Resistance mechanism against Ampicillin

A

Hydrolization by ß-lactamases

Penicillinase cleaves the ß-lactam ring

155
Q

Based on the resistance mechanisms, what must be applied with ampicillin

A

A b-lactamase inhibitor (clavulanate, tazobactam or sulbactam)

156
Q

Happens when you add clavulanate or sulbactam to ampicillin

A

Activity spectrum against resistan microorganisms expands

157
Q

Aminopenicillin that is not affected by food ingestion

A

Amoxicillin

158
Q

Effective concentrations of oral ——– stay 2x as long in plasma than ———

A

amoxicillin
ampicillin

159
Q

Effect of probenecid on amoxicillin

A

Delays excretion

160
Q

Aminopenicillins MOA

A

Inhibition of peptidoglycan synthesis by blocking the transpeptidation reaction of D-alanyl-D-alanine

161
Q

Carbapenems and Monobactams are…

A

B-lactam wall inhibitors

162
Q

-nems (imipenem, meropenem, ertapenem and doripenem) are classified as

A

Carbapenems

163
Q

Carbapenems MOA

A

Bind to PBP’s to disrupts bacterial cell wall synthesis and dead to susceptible microorganisms

164
Q

Are carbapenems bactericidal or bacteriostatic?

A

Bactericidal

165
Q

In general, carbapenems are used for nosocomial infections such as:

A

UTIs
LRTI (pneumonia)
Intraabdominal and gynecologic infections
Skin, soft tissue, bone and joint infections

166
Q

why is imipenem combined with cilastatin?

A

Cilastatin inhibits tubular degradation and extends t1/2

167
Q

Why are cilastatin + relabactam added to imipinem?

A

Cilastatin extends half life
Relebactam contains a ß-lactamase inhibitor against carbapenemases

168
Q

Imipinem’s primary role

A

Empiric treatment of serious infections in hospitalized patients at risk for resistant pathogens

169
Q

Carbapenems act against:

A

Gram positive cocci
Gram negative rods
Anaerobes

170
Q

Imipenem’s main gram positive targets

A

Staph aureus
Streptococcus (pneumoniae, pyogenes, agalactiae)
Enterococcus faecalis

171
Q

Imipenem’s gram negative targets (EKEPPA)

A

Enterobacterales
E coli
Klebsiella
Enterobacter
Proteus
Pseudomonas
Acinetobacter

172
Q

Imipinem is not effective against

A

MRSA and C. difficile

173
Q

Imipinem’s anaerobe sprectrum

A

Bacteroides
Clostridium
Fusobacterium

174
Q

Drug combo reserved for treatment of gram negative pathogens resistant to all or almost all other antibiotics

A

Imipinem + relabactam

175
Q

Imipinem adverse effects

A

Nausea
Vomiting
Seizures
Hypersensitivity

176
Q

Meropenem is less active then imipinem when treating —— but more active when treating ——–

A

Gram + (enterococcus)
Gram negative

177
Q

Preferred carbapenem for the treatment of meningitis

178
Q

Meropenem + vaborbactam are reserved for

A

Multi-drug resistant gram negative pathogens

179
Q

Therapeutic use of meropenem

A

Hospital-onset infections when cephalosporin or penicillin-resistant organisms are suspected
RTI
GI
UTIs

180
Q

Meropenem is less likely to cause —— but SHOULD NOT be administered with ——-

A

Seizures
Valproic acid

181
Q

Meropenem is combined with ——– ro reduce resistance

A

Vaborbactam (ß-lactase inhibitor)

182
Q

Ertapenem administration

183
Q

Ertapenem MOA

A

Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs)

184
Q

Ertapenem has ——– activity

A

Bactericidal

185
Q

Ertapenem therapeutic uses

A

Complicated
UTIs
Skin and soft tissue inf.
CAP
Pelvic infections

186
Q

Ertapenem and doripenem adverse effects

A

GI distress
Headache
Injection side reactions
Hypersensitivity
Anaphylaxis
Seizures

187
Q

Ertapenem and doripenem should not be administered in cases of

A

Hypersensitivity to other ß-lactams
Seizure disorders like epilepsy
Severe renal impairment

188
Q

Ertapenems and doripenems major resistant issue

A

Carbapenemase-producing Enterobacterales (CPE)

189
Q

Other resistance mechanisms to Ertapenem and Doripenem

A

Efflux pumps
Porin mutations
ESBL-producing bacteria

190
Q

Gram positive spectrum of ertapenem and doripenem

A

S. pneumoniae
S. pyogenes
S. agalactiae
MSSA

191
Q

Gram negative spectrum of ertapenem KHEEP

A

Klebsiella pneumoniae
Haemophilus influenzae
E. coli
Enterobacter
Proteus mirabilis

192
Q

Bacteroidis fragilis, prevotella and fusobacterium are anaerobes treated with

A

Ertapenem or Doripenem

193
Q

Doripenem ADME

194
Q

Doripenem ADME

A

Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs)

195
Q

Doripenem has —– action with —— activity

A

Bactericidal
Broad spectrum

196
Q

Doripenem therapeutic uses

A

Complicated intra abdominal infections
Complicated UTIs
Nosocomial pneumonia

197
Q

Indicated ß-lactam antibiotic for pyelonephritis

198
Q

Doripenem is highly effective against…

A

Multi-drug resistant gram negative infections

199
Q

Carbapenem used for pseudomonas aeruginosa

200
Q

Regarding gram - bacteria, doripenem is more active against ——- than ertapenem

A

Pseudomonas aeruginosa

201
Q

Aztreonam is classified as a

A

Monobactam

202
Q

Aztreonam ADME

A

IV, IM, inhalation

203
Q

B-lactam used in cystic fibrosis patients

A

Aztreonam (inhalation formulation)

204
Q

Aztreonam MOA

A

Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs)

205
Q

Aztreonam is bactericidal against…

A

Gram negative susceptible bacteria

206
Q

Aztreonam is stable against most β-lactamases, but not effective against

A

ESBL or carbapenemase-producing bacteria

207
Q

T or F: Aztreonam has high activity against gram-positive bacteria or anaerobes

208
Q

Aztreonam is highly active against

A

H. influenzae

209
Q

Inhaled aztreonam is used for

A

Reduction of pseudomonas-associated pulmonary exacerbations in cystic fibrosis patients

210
Q

Monobactam used for serious gram negative infections like pneumonia, UTIs and sepsis

211
Q

Monobactam used as an alternative for penicillin-allergic patients

212
Q

Aztreonam causes ——- especially in infants and young children

A

Hepatotoxicity (elevated liver enzymes)

213
Q

Aztreonam contraindications

A

Hypersensitivity against ceftazidime
Severe renal impairment

214
Q

ESBL (extended-spectrum β-lactamases) and Carbapenemases (KPC, NDM, OXA-type enzymes) are resistance mechanisms of

215
Q

Aztreonam bacterial spectrum KHEEPP

A

Klebsiella pneumoniae
H. influenza
E. coli
Enterobacter
Proteus
Pseudomonas

216
Q

Preferred treatment for ESBL infections

A

Carbapenems

217
Q

Should be avoided in ESBL infections

A

Penicillins, most cephalosporins, aztreonam

Antimicrobial's pharmacology (7 decks)

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