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Pharmacology > 24) Cell Wall Inhibitors > Flashcards

24) Cell Wall Inhibitors Flashcards

1
Q

Beta-lactam antibiotics

A
  • Drugs with structures containing a beta-lactam ring

- Includes penicillins, cephalosporins and carbapenems

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2
Q

Beta-lactamases

A
  • Bacterial enzymes (penicillinases, cephalosporinases) that hydrolyze the beta-lactam ring
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3
Q

Minimal inhibitory concentration (MIC)

A
  • Lowest concentration of antimicrobial drug capable of inhibiting growth of an organism in a defined growth medium
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4
Q

Penicillin-binding protein (PBPs)

A
  • Bacterial cytoplasmic membrane proteins that act as the initial receptors for penicillins and other beta-lactam antibiotics
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5
Q

Peptidoglycans

A
  • Chains of polysaccharides that are cross-linked to form the bacterial cell wall
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6
Q

Selective toxicity

A
  • More toxic to the invader than to the host
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7
Q

Transpeptidases

A
  • Bacterial enzymes involved in the cross-linking of linear peptidoglycan chains, the final step in cell wall synthesis
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8
Q

Bactericidal

A
  • An antimicrobial drug that can eradicate an infection in the absence of host defense mechanisms
  • Kills bacteria
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9
Q

Bacteriostatic

A
  • An antimicrobial drug that inhibits antimicrobial growth but requires host defense mechanisms to eradicate the infection
  • Does not kill bacteria
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10
Q

Bactericidal agents

A
  • Aminoglycosides
  • Bacitracin
  • Beta-lactam antibiotics
  • Daptomycin
  • Fosfomycin
  • Glycopeptide antibiotics
  • Isoniazid
  • Fidaxomicin
  • Metronidazole
  • Polymixins
  • Pyrazinamide
  • Fluoroquinolones
  • Rifampin
  • Streptogramins
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11
Q

Bacteriostatic agents

A
  • Chloramphenicol
  • Clindamycin
  • Ethambutol
  • Macrolides
  • Nitrofurantoin
  • Oxazolidinones
  • Sulfonamides
  • Tetracyclines
  • Tigecycline
  • Trimethoprim
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12
Q

Antibiotic classes that are bacterial cell wall/membrane inhibitors

A
  • Penicillins
  • Beta-lactamase inhibitors
  • Cephalosporins
  • Carbapenems
  • Monobactams
  • Polymixins
  • Glycopeptides
  • Lipopeptides
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13
Q

Antibiotic classes that are bcterial protein synthesis inhibitors

A
  • Macrolides
  • Lincosamides
  • Aminoglycosides
  • Tetracyclines
  • Glycylcycline
  • Oxazolidinones
  • Streptogramins
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14
Q

Antibiotic classes that inhibit bacterial DNA/RNA

A
  • Fluoroquinolones
  • Folate antagonists
  • Rifamycin derivatives
  • Anti-clostridium agent
  • Nitroimidazole
  • Nitrofurans
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15
Q

Anti-mycobacterials

A
  • Rifamycin derivatives
  • Isoniazid
  • Pyrazinamide
  • Ethambutol
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16
Q

Peptidoglycan (murein) layers are critical for bacterial survival

A
  • Protect against toxic outside influences

- Provide the strength required to resist high osmotic pressures (otherwise will lead to plasma membrane rupture)

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17
Q

Mycobacterium tuberculosis does not retain any common bacteriological stain due to

A
  • High lipid content in its wall

- Neither Gram-positive nor Gram-negative

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18
Q

Stages of cell wall synthesis

A
  • Cytoplasmic stage
  • Membrane stage
  • Extracellular stage
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19
Q

Cytoplasmic stage

A
  • Synthesis of precursors (NAG, NAM)

- Targeted by cycloserine and fosfomycin

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20
Q

Membrane stage

A
  • Transfer of the precursors from the cytosol to membrane
  • Incorporation into the growing peptidoglycan
  • Targeted by bacitracin, vancomycin
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21
Q

Extracellular stage

A
  • Cross-linking of linear chains of peptidoglycans by transpeptidases
  • Targeted by beta-lactams
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22
Q

NAG and NAM

A
  • N-acetyl glucosamine

- N-acetyl muramic acid

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23
Q

Fosfomycin

A
  • Inhibits enol pyruvate transferase specifically MurA (cytoplasmic stage)
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24
Q

Cycloserine

A
  • Inhibits racemase (cytoplasmic stage)
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25
Q

Bacitracin

A
  • Inhibits phosphatase (membrane stage)
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26
Q

Vancomycin and teicoplanin

A
  • Does not not inhibit an enzyme

- Binds to the D-Ala-D-Ala terminal of the growing peptide chain (membrane stage)

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27
Q

Extracelular stage steps

A
  • Neighboring peptidoglycan chains are cross-linked through their peptide chain by transpeptidases
  • Cross-linking makes the cell wall stronger
  • Transpeptidase is one of the penicillin binding protein (PBP)
  • When the covalent bond occurs with the D-alanine (in purple) the second D-alanine leaves
  • Beta-lactams inhibit transpeptidase
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28
Q

Beta-lactams MOA

A
  • Bind to the penicillin binding protein (PBPs) specifically transpeptidase in the cytoplasmic membrane of the bacteria
  • Inhibit transpeptidation reaction (cross-linking)
  • Activate the autolytic enzyme that cause lesions in the cell wall
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29
Q

Molecular mechanism of interaction between beta-lactam and bacterial cell wall

A
  • Formation of a covalent bond between serine and beta-lactam (irreversible)
  • Serine in the bacterial cell wall is not a free nucleophile anymore and cannot help in building the bacterial cell wall
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30
Q

Mechanism of resistance between beta-lactam and bacterial cell wall interaction

A
  • When beta-lactamase are released from bacteria they target beta-lactam antibiotics
  • Hydroxyl group of the serine linked to the beta-lactamase will form a covalent bond with the beta-lactam
  • Opens the ring leading to an ineffective antibiotic
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31
Q

Properties of PNC

A
  • Rapidly eliminated by kidneys

- Short half lives of 30-90 min

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32
Q

Broad spectrum β-lactams cover

A
  • Gram positive bacteria

- Gram negative bacteria

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33
Q

Narrow spectrum β-lactams cover

A
  • Gram positive bacteria only
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34
Q

To penetrate the outer membrane in Gram negative bacteria,

A
  • Hydrophilic antibiotics pass through the porins better than hydrophobic ones
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35
Q

Hydrophilic antibiotics tend to have

A
  • Broader spectrum
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36
Q

Hydrophobic drugs tend to have

A
  • Narrow spectrum of action
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37
Q

Hydrophobic drugs

A
  • Axacillin
  • Dicloxacillin
  • Nafcillin
  • Methicillin
  • Penicillin G
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38
Q

Hydrophilic drugs

A
  • Ampicillin
  • Amoxicillin
  • Piperacillin
  • Ticarcillin
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39
Q

Properties providing resistance to β-lactam

A
  • Bacteria acquiring β-lactamase encoding gene
  • Altering transpeptidase or PBP by changing its ability to bind to β-lactam
  • Inability to penetrate β-lactam site of action (decreased permeability or porin reduction)
  • Activating efflux pump systems that remove β-lactam from its site of action
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40
Q

Hypersensitivity to β-lactam may cause

A
  • Anaphylactic reaction (rash, itchiness, nausea, vomiting and shortness of breath)
  • Potential cross-sensitivity between β-lactams
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41
Q

PNC eliminates the GI microflora leading to

A
  • Potential superinfection

- Risk of Chlostridium difficile associated diarrhea CDAD

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42
Q

Drug-induced hemolytic anemia (red blood cells are destroyed faster than they can be made)

A
  • PNCs modify the protein on the surface of RBCs (β-lactam binds to the RBC)
  • Complex is phagocytosed by macrophage
  • Antigen presented to CD4
  • Leads to stimulation of B cells, and formation of IgG antibodies specific to β-lactam-modified epitope
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43
Q

Penicillin G, Benzathine U.S. box warning

A
  • Not for IV use because of cardiopulmonary arrest
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44
Q

Penicillin G, Benzathine CI/warnings

A
  • Hypersensitivity to beta-lactam (anaphylactic)
  • Superinfection if prolonged use (Clostridium difficile colitis)
  • Seizures
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45
Q

Penicillin G, Benzathine cardio ADRs

A
  • Hypotension

- Tachycardia

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46
Q

Penicillin G, Benzathine CNS ADRs

A
  • Anxiety
  • Headaches
  • Fatigue
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47
Q

Penicillin G, Benzathine skin ADRs

A
  • Diaphoresis
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48
Q

Penicillin G, Benzathine GI ADRs

A
  • Bloody stool
  • Nausea, vomiting
  • Intestinal necrosis
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49
Q

Penicillin G, Benzathine genitourinary ADRs

A
  • Impotence

- Hematuria

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50
Q

Penicillin G, Benzathine hepatic ADRs

A
  • Increase AST
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51
Q

Penicillin G, Benzathine immune system ADRs

A
  • Jarish-Herxheimer reaction (shaking, chills, rise in temp, intensification of skin rashed)
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52
Q

Penicillin G, Benzathine renal ADRs

A
  • Increase serum creatinine, BUN
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53
Q

Penicillin G, Benzathine respiratory ADRs

A
  • Cyanosis
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54
Q

Penicillin G, Benzathine pharmacokinetics

A
  • Renal metabolism

- 60% protein binding

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55
Q

Penicillin G, procaine CI/warnings

A
  • Fibrosis and atrophy due to IM route
  • Methemoglobinemia after anesthesia or G6PD deficiency
  • Not IV because of neurovascular damage
  • Mental disturbances
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56
Q

Penicillin G, procaine ADRs

A
  • Not defined
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57
Q

Penicillin G, procaine pharmacokinetics

A
  • Renal metabolism

- 60% protein binding

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58
Q

Penicillin V, potassium ADRs

A
  • Nausea, vomiting
  • Diarrhea
  • Mild candidiasis
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59
Q

Penicillin V, potassium pharmacokinets

A
  • Renal metabolism

- 80% protein binding

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60
Q

Nafcillin CI/warnings

A
  • Hypersensitivity to beta-lactams (anaphylactic)
  • Extravasation when IV
  • Hepatic increase in LFT
  • Neurotoxicity
  • Superinfection if prolonged use (Clostridium difficile colitis)
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61
Q

Nafcillin cardio ADRs

A
  • Local thrombophlebitis
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62
Q

Nafcillin CNS ADRs

A
  • Neurotoxicity
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63
Q

Nafcillin GI ADRs

A
  • Cholestasis

- C. dificile associated diarrhea

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64
Q

Nafcillin hematological ADRs

A
  • Agranulocytosis
  • Bone marrow suppression
  • Neutropenia
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65
Q

Nafcillin hepatic ADRs

A
  • Increased LFT
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66
Q

Nafcillin pharmacokinetics

A
  • Hepatic metabolism
  • Enterohepatic circulation
  • Excretion in feces
  • 90% protein binding
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67
Q

Oxacillin CI/warnings

A
  • Hepatitis
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68
Q

Oxacillin ADRs

A
  • C. dificile associated diarrhea
  • Increased LFT (hepatic)
  • Actute renal tubular disease
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69
Q

Oxacilin pharmacokinetics

A
  • Metabolism not known

- 90% protein binding

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70
Q

Dicloxacillin CI/warnings

A
  • None
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71
Q

Dicloxacillin ADRs

A
  • Abdominal pain

- Nausea, vomiting

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72
Q

Dicloxacillin pharmacokinetics

A
  • CYP2C19 inducer
  • 90% protein binding
  • Excretion in feces and urine unchanged
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73
Q

Methicillin CI/warning

A
  • None
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74
Q

Methicillin ADRs

A
  • Neutropenia
  • Thrombocytopenia
  • Agranulogytosis
  • Increased LFTs
  • Acute renal disease
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75
Q

Methicillin pharmacokinetics

A
  • Hepatic metabolism

- Renal excretion

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76
Q

Methicillin family is linked to

A
  • Methicillin resistant staphylococcus aureus (MRSA)
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77
Q

Amino-PNC antibiotic names

A
  • Amoxicillin

- Ampicillin

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78
Q

Amoxicillin CI/warnings

A
  • Hypersensitivity to beta-lactams (anaphylactic)

- Superinfection if prolonged use (Clostridium difficile colitis)

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79
Q

Amoxicillin CNS ADRs

A
  • Headaches, agitation, seizures, confusion, mood
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80
Q

Amoxicilin GI ADRs

A
  • N,D,V

- C. difficile-associated diarrhea

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81
Q

Amoxicillin genitourinary ADRs

A
  • Vulvovaginal infection
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82
Q

Amoxicillin cardio/hematological ADRs

A
  • Hypersensitivity angitis
  • Neutropenia
  • Thrombocytopenia
  • Agranulocytosis
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83
Q

Amoxicillin systemic ADRs

A
  • Serum-sickness reaction

- Fever

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84
Q

Amoxicillin hepatic ADRs

A
  • Increase LFTs
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85
Q

Amoxicillin pharmacokinetics

A
  • Metabolism not known
  • 20% protein binding
  • Distributed broadly into tissues, but not CSF unless meningitis
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86
Q

Ampicillin CI/warnings

A
  • Non-allergic rash in kids
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87
Q

Ampicillin CNS ADRs

A
  • Headaches
  • Agitation
  • Seizures
  • Confusion
  • Mood
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88
Q

Ampicillin GI ADRs

A
  • Nausea, vomiting

- Diarrhea

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89
Q

Ampicillin hematological ADRs

A
  • Neutropenia
  • Thrombocytopenia
  • Agranulocytosis
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90
Q

Ampicillin hepatic ADRs

A
  • Increase LFTs
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91
Q

Ampicillin systemic ADRs

A
  • Serum-sickness reaction
92
Q

Ampicillin pharmacokinetics

A
  • Metabolism not known

- 15% protein binding

93
Q

Anti-pseudomonal peicillin

A
  • Piperacillin (ureidoPNC)

- Ticarcillin (carboxyPNC)

94
Q

Piperacillin (ureidoPNC) CI/warnings

A
  • Bleeding in renal impaired patients

- Leukopenia neutropenia

95
Q

Piperacillin (ureidoPNC) hematological ADRs

A
  • Local thrombophlebitis
  • Hemolytic anemia
  • Agranulocytosis
96
Q

Piperacillin (ureidoPNC) CNS ADRs

A
  • Confusion
  • Seizure
  • Drowsiness
97
Q

Piperacillin (ureidoPNC) dermatological ADRs

A
  • Skin rash

- Urticaria

98
Q

Piperacillin (ureidoPNC) renal ADRs

A
  • Hypokalemia

- Acute renal failure

99
Q

Piperacillin (ureidoPNC) systemic ADRs

A
  • Fever

- Jarisch-Herxheimer reaction

100
Q

Piperacillin (ureidoPNC) pharmacokinetics

A
  • Metabolism not known

- 25% protein binding

101
Q

Ticarcillin (carboxyPNC) CI/warnings

A
  • Bleeding in renal impaired patients

- Hypokalemia

102
Q

Ticarcillin (carboxyPNC) hematological ADRs

A
  • Local thrombophlebitis
103
Q

Ticarcillin (carboxyPNC) renal ADRs

A
  • Hypernatremia

- Hypokalemia

104
Q

Ticarcillin (carboxyPNC) CNS ADRs

A
  • Confusion
  • Seizure
  • Drowsiness
105
Q

Ticarcillin (carboxyPNC) dermatological ADRs

A
  • Skin rash
106
Q

Ticarcillin (carboxyPNC) pharmacokinetics

A
  • Metabolism not known

- Renally excreted

107
Q

β-lactamase inhibitors combinations generic/brand names

A
  • Amoxicillin/ticarcillin + clavulanic acid (Augmentin, Timentin)
  • Piperacillin + Tazobactam (Zosyn)
  • Ampicillin + Sulbactam (Unasyn)
  • Ceftazidime + Avibactam (Avycaz)
  • Meropenem + Varobactam (Vabomere)
108
Q

Amoxicillin/ticarcillin + clavulanic acid (Augmentin, Timentin) CI/warnings

A
  • Hypersensitivity to beta-lactams (anaphylactic)
  • Superinfection if prolonged use (Clostridium difficile colitis)
  • Diarrhea (higher than amoxicillin alone)
  • Hepatic dysfunction
109
Q

Piperacillin + Tazobactam (Zosyn) CI/warnings

A
  • Serious skin reaction (toxic epidermal necrolysis TEN)
  • High sodium content
  • Abnormal clotting times
  • Nephrotoxic
110
Q

Ampicillin + Sulbactam (Unasyn) CI/warnings

A
  • Hepatic dysfunction

- Rash

111
Q

Ceftazidime + Avibactam (Avycaz) CI/warnings

A
  • Neurotoxicity
112
Q

Meropenem + Varobactam (Vabomere) CI/warnings

A
  • Seizures

- Brain lesions

113
Q

Amoxicillin/ticarcillin + clavulanic acid (Augmentin, Timentin) ADRs

A
  • Diarrhea
  • Rash
  • Nausea, vomiting
  • Vaginitis
  • Candidiasis
114
Q

Amoxicillin/ticarcillin + clavulanic acid (Augmentin, Timentin) pharmacokinetics

A
  • Hepatically metabolized
  • 20% protein binding
  • Renally excreted
115
Q

Piperacillin + Tazobactam (Zosyn) ADRs

A
  • Vaginitis
  • Candidiasis
  • Hypotension, hypotension flushing
  • Hypoglycemia
116
Q

Piperacillin + Tazobactam (Zosyn) pharmacokinetics

A
  • 30% protein binding

- Renally excreted unchanged

117
Q

Ampicillin + Sulbactam (Unasyn) ADRs

A
  • Pain at injection site
118
Q

Ampicillin + Sulbactam (Unasyn) pharmacokinetics

A
  • 30% protein binding

- Renally excreted unchanged

119
Q

Ceftazidime + Avibactam (Avycaz) ADRs

A
  • Positive direct coombs test

- Pain at injection site

120
Q

Ceftazidime + Avibactam (Avycaz) pharmacokinetics

A
  • Not metabolized
  • Excreted in urine
  • 10% protein binding
121
Q

Meropenem + Varobactam (Vabomere) ADRs

A
  • Phlebitis
  • Headaches
  • Hypokalemia
  • Increased LFT
  • Fever
  • Injection pain
122
Q

Meropenem + Varobactam (Vabomere) pharmacokinetics

A
  • Not metabolized
  • Renally excreted
  • 30% protein binding
123
Q

1st generation cephalosporins

A
  • Cephalexin
  • Cefadroxil
  • Cefazolin
124
Q

1st generation cephalosporin spectrum

A
  • Gram+ cocci (staphylococci, streptococci)
125
Q

2nd generation cephalosporins

A
  • Cefuroxime
  • Cefotetan
  • Cefaclor
  • Cefoxitin
  • Cefprozil
126
Q

2nd generation cephalosporin spectrum

A
  • Less activity against G+

- More extended against G- (e.g. B. fragilis, H. influenzae; M. catarrhalis)

127
Q

3rd generation cephalosporins

A
  • Cefdinir
  • Cefotaxime
  • Ceftriaxone
  • Ceftazidime
  • Cefpodoxime
  • Cefixime
128
Q

3rd generation cephalosporin spectrum

A
  • Less activity against G+
  • More extended against G- resistant to other β-lactams and able to penetrate the BBB (except for cefixime) e.g. S. marcescens; beta-lactamase producing strains of H. influenzae; Neisseria
129
Q

3rd generation cephalosporins with anti-pseudonomal activity

A
  • Cefoperazone

- Ceftazidime

130
Q

4th generation cephalosporins

A
  • Cefepine
131
Q

4th generation cephalosporin spectrum

A
  • More resistant to beta-lactamase produced G- including Enterobacter, Haemophilius; Neisseria and anti-pseudomonal
  • Combines the G+ of the 1st generation and the G- of the 3rd generation of cephalosporins
132
Q

5th generation cephalosporins

A
  • Ceftaroline
133
Q

5th generation cephalosporin spectrum

A
  • Has G- and G+ coverage, especially against Methicillin-resistant Staphylococci (MRSA) and Vancomycin resistant Staphylococcus aureus (VRSA)
134
Q

Characteristics of cephalosporins

A
  • 2nd gen onward is more resistant to β-lactamases
  • Many are orally absorbed
  • Primarily excreted in the kidneys (dosage reduced if renal insufficiency)
135
Q

Cephalosporins and the CNS

A
  • Several (like ceftriaxone, cefotaxime, ceftazidime, cefepime) can enter CSF when meningitis is present
136
Q

Cephalosporin-induced disulfiram like reaction

A
  • Facial flushing
  • Angioedema
  • Hypotension shock
  • Death
137
Q

Cephalexin, cefadroxil, cefazolin (1st gen) CI/warnings

A
  • Hypersensitivity to beta-lactams (anaphylactic)
  • Superinfection if prolonged use (Clostridium difficile colitis)
  • Increase INR: Decrease synthesis of vitamin K leading to bleeding in patients on anticoagulants
  • PNC cross- allergy
  • Seizure; colitis
138
Q

Cephalexin, cefadroxil, cefazolin (1st gen) ADRs

A
  • CNS: agitation, confusion, fatigue
  • Dermatological: rash, Steven Johnson syndrome
  • GI: diarrhea, gastritis
  • Genital candidiasis, vaginitis
  • Renal: increase BUN, renal failure
  • Hemolytic anemia, neutropenia thrombocytopenia, eosinophilia
  • Increase LFTs
139
Q

Cefalexin (1st gen) pharmacokinetics

A
  • Metabolism unknown
  • Renally excreted unchanged
  • 10% protein binding
140
Q

Cefadroxil (1st gen) pharmacokinetics

A
  • Metabolism unknown
  • Renally excreted unchanged
  • 20% protein binding
141
Q

Cefazolin (1st gen) pharmacokinetics

A
  • Metabolism unknown
  • Renally excreted unchanged
  • 80% protein binding
142
Q

Cefuroxine (2nd gen) ADRs

A
  • Jarisch-Herxheimer reaction
143
Q

Cefuroxine (2nd gen) pharmacokinetics

A
  • 50% protein binding
144
Q

Cefotetan (2nd gen) CI/warnings

A
  • Hemolytic anemia
145
Q

Cefotetan (2nd gen) ADRs

A
  • Increase prothrombin time
146
Q

Cefotetan (2nd gen) pharmacokinetics

A
  • 80% protein binding
147
Q

Cefalcor (2nd gen) pharmacokinetics

A
  • Substrate of OAT1/3

- 25% protein binding

148
Q

Cefoxitin (2nd gen) pharmacokinetics

A
  • 80% protein binding
149
Q

Cefprozil (2nd gen) pharmacokinetics

A
  • 25% protein binding
150
Q

Cefdinir (3rd gen) CI/warnings

A
  • Hypersensitivity to beta-lactams (anaphylactic)
  • Superinfection if prolonged use (Clostridium difficile colitis)
  • PNC cross- allergy
  • Colitis
151
Q

Cefdinir (3rd gen) ADRs

A
  • Diarrhea
152
Q

Cefdinir (3rd gen) pharmacokinetics

A
  • Metabolism unknown

- 60-70% protein binding

153
Q

Cefotaxime (3rd gen) CI/warnings

A
  • Arrythmia

- Granulocytopenia

154
Q

Cefotaxime (3rd gen) pharmacokinetics

A
  • 50% protein binding
155
Q

Ceftriaxone (3rd gen) CI/warnings

A
  • Not in neonates with hyperbilirubinemia (displace bilirubin from albumin binding sites)
  • Increase INR; hemolytic anemia
  • Pancreatitis (secondary to biliary obstruction)
156
Q

Ceftriaxone (3rd gen) ADRs

A
  • Increase BUN
  • Abnormal gallbladder sonograms
  • Skin tightness
157
Q

Ceftriaxone (3rd gen) pharmacokinetics

A
  • 85% protein binding

- Eliminated in the bile

158
Q

Ceftazidime (3rd gen) CI/warnings

A
  • Neurotoxicity
159
Q

Ceftazidime (3rd gen) ADRs

A
  • Positive direct Coombs test (the blood has antibodies that fight against RBC)
160
Q

Ceftazidime (3rd gen) pharmacokinetics

A
  • Less than 10% protein binding
161
Q

Cefpodoxime (3rd gen) pharmacokinetics

A
  • 20% protein binding
162
Q

Cefixime (3rd gen) CI/warnings

A
  • Severe cutaneous reactions
  • Hemolytic
  • Renal failure
163
Q

Cefixime (3rd gen) pharmacokinetics

A

65% protein binding

164
Q

Cefepime (4th gen) CI/warnings

A
  • Increase INR
  • Neurotoxicity
  • Renal failure
165
Q

Cefepime (4th gen) ADRs

A
  • Positive direct Coombs test
166
Q

Cefepime (4th gen) pharamcokinetics

A
  • 20% protein binding
167
Q

Ceftaroline (5th gen) CI/warnings

A
  • Hemolytic anemia

- Renal failure

168
Q

Ceftaroline (5th gen) ADRs

A
  • Positive direct Coombs test
169
Q

Ceftaroline (5th gen) pharmacokinetics

A
  • 20% protein binding
170
Q

Carbapenems coverage

A
  • G+ cocci
  • G- rods
  • Anaerobes
171
Q

Carbapenems (names)

A
  • Imipenem
  • Meropenem
  • Doripenem
  • Ertapenem
172
Q

Imipinem CI/warnings

A
  • Hypersensitivity to beta-lactams (anaphylactic)
  • CNS disorders: Confusion and seizures
  • Superinfection if prolonged use (Clostridium difficile colitis)
  • Renal impairment
173
Q

Imipinem ADRs

A
  • Decrease hematocrit
  • Eosinophilia, thrombocytopenia, neutropenia
  • Increase LFTs
  • N;V;D
174
Q

Imipinem pharmacokinets

A
  • Administered with cilastatin because it is inactivated by renal dehydropeptidase 1 enzyme (Cilastatin inhibits dehydropeptidase 1)
  • Renally excreted
  • 30% protein binding
175
Q

Meropenem, Doripenem, Ertapenem CI/warnings

A
  • Severe cutaneous effects
176
Q

Meropenem ADRs

A
  • Cardiovascular hyper/hypotension
  • Bradychardia
  • Peripheral edema
  • Hypoglycemia
177
Q

Meropenem pharmacokinetics

A
  • 20% protein binding

- Renally excreted

178
Q

Doripenem pharmacokinetics

A
  • 8% protein binding

- Renally excreted

179
Q

Ertapenem ADRs

A
  • Edema

- Neutropenia

180
Q

Ertapenem pharmacokinetics

A
  • 85% protein binding
181
Q

Monobactam: Aztreonam coverage

A
  • Resistant to beta-lactamases produced by G- rods (Klebsiella, Pseudomonas, Serratia)
  • No activity against G+ bacteria
182
Q

Monobactam: Aztreonam warning

A
  • It can be used for patients with PNC hypersensitivity (has no cross-sensitivity with other beta-lactams except ceftazidime)
  • Superinfection if prolonged use (Clostridium difficile colitis)
183
Q

Monobactam: Aztreonam adverse effects

A
  • Neutropenia (mainly in children)
  • IV site phlebitis
  • Increase LFTs
  • NVD
  • Eosinophilia, thrombocytopenia
  • Skin rash
  • Increase serum creatinine (most in children)
184
Q

Monobactam: Aztreonam pharmacokinetics

A
  • Renally excreted

- Can distribute in CSF when meningitis

185
Q

Misc. characteristics about beta-lactams

A
  • They all inhibit transpeptidases
  • All lack activity against MRSA except ceftaroline (5th generation cephalosporin)
  • Because of the beta-lactam they cause hypersensitivity and potential cross-sensitivity
186
Q

Other non-beta-lactam cell wall inhibitors

A
  • Glycopeptides
  • Polymixin
  • Phosphonic acid derivative
  • Bacitracin
  • Lipopeptide
187
Q

Glycopeptides (non-beta-lactam cell wall inhibitors)

A
  • Vancomycin
  • Telavanin
  • Oritavancin
  • Dalbavancin
188
Q

Polymixin (non-beta-lactam cell wall inhibitors)

A
  • Polymixin B

- Colistin (polymixin E)

189
Q

Phosphonic acid derivative (non-beta-lactam cell wall inhibitors)

A
  • Fosfomycin
190
Q

Lipopeptide (non-beta-lactam cell wall inhibitors)

A
  • Daptomycin
191
Q

Glycopeptides MOA

A
  • Bactericidal glycoprotein that binds to the D-Ala D-Ala terminal of the peptidoglycan pentapeptide side chain
  • Inhibits transglycosylation (adding glycoside)
  • Prevents elongation of the peptidoglycan (cover G+ rod, cocci and MRSA)
192
Q

Fosfomycin MOA

A
  • Antimetabolite inhibitor of the cytosolic enolpyruvate transferase (MurA)
  • Prevents the formation of N-acetylmuramic acid (NAM), an essential precursor for the peptidoglycan chain formation
193
Q

Bacitracin MOA

A
  • Peptide that inhibits the phosphatase of bactroprenol
194
Q

Cycloserine MOA

A
  • Inhibits the racemase
195
Q

Polymixin MOA

A
  • Cationic polypeptide that binds to the phospholipid (lipopolysaccharide LPS of G-) of the outer membrane
  • Alters permeability and damage bacterial cytoplasmic membrane leading to leakage of intracellular content
196
Q

Daptomycin MOA

A
  • Cyclic lipopeptide
  • Inserts into the cytoplasmic membran
  • Causes potassium leak and cell death (integration into G+ bacteria)
197
Q

Fosfomycin warnings

A
  • Electrolyte abnormality
  • Hepatic injury
  • Hypersensitivity
  • Superinfection
198
Q

Fosfomycin ADRs

A
  • Headache
  • Rash
  • NVD
  • Vaginitis
199
Q

Fosfomycin pharmacokinetics

A
  • No protein binding metabolism unknown

- Renal/fecal elimination

200
Q

Polymixin warnings

A
  • US box warning: nephrotoxicity, neurotoxicity (respiratory paralysis)
201
Q

Polymixin ADRs

A
  • Facial flushing
  • Neurotoxicity
  • Rash
  • Hypocalcemia, hypochloremia, hypokalemia, hyponatremia
  • Pain on injection
  • Neuromuscular blockade
202
Q

Polymixin pharmacokinetics

A
  • Not absorbed in GI
  • Tissue distribution is poor
  • 60% protein binding
  • Renally excreted
203
Q

Colistin warnings

A
  • Bronchoconstriction when inhaled
  • CNS toxicity: neurological disturbances
  • Renal toxicity
  • Respiratory arrest
204
Q

Colistin ADRs

A
  • Neurotoxicity

- Acute renal failure

205
Q

Colistin pharmacokinetics

A
  • Not absorbed in GI
  • Renally excreted
  • 50% protein binding
206
Q

Bacitracin warnings

A
  • US box warning: nephrotoxicity
  • Anaphylaxis
  • Renal failure
207
Q

Bacitracin ADRs

A
  • Skin rash
  • Albuminuria
  • NV
  • Nephrotoxicity from tubular and glomerular necrosis
208
Q

Bacitracin pharmacokinetics

A
  • Renally excreted

- Well distributed

209
Q

Daptomycin warnings

A
  • Eosinophilia pneumonia
  • Hypersensitivity
  • Rhabdomyolysis
  • Myopathy
  • Peripheral neuropathy
210
Q

Daptomycin ADRs

A
  • Hypertension/hypotension
  • Headaches
  • Rash
  • Diarrhea
  • UTI
  • Abnormal LFTs
211
Q

Daptomycin pharmacokinetic

A
  • 90% protein binding

- Renally excreted

212
Q

Vancomycin warnings

A
  • US box warning: not during pregnancy
  • Extravasation and thrombophlebitis
  • Neurotoxicity
  • Neutropenia
  • Ototoxicity
  • Superinfection
213
Q

Vancomycin ADRs

A
  • Hypotension with flushing
  • Fever
  • Eosinophilia
  • Red man syndrome
214
Q

Vancomycin pharmacokinetics

A
  • Renally eliminated
215
Q

Telavancin warnings

A
  • US box warning: not during pregnancy; nephrotoxicity
  • Anaphylaxis
  • Cardiac conduction alteration
  • Infusion reaction rash
216
Q

Telavancin ADRs

A
  • Metallic taste
  • NVD
  • Increased SCr
217
Q

Telavancin pharmacokinetics

A
  • Renal/fecal excretion

- 90% protein binding

218
Q

Oritavancin warnings

A
  • Hypersensitivity infusion reaction

- Osteomyelitis

219
Q

Oritavancin ADRs

A
  • Tachycardia
  • Headache
  • Hyperuricemia
  • Hypoglycemia
  • Anemia
  • Increase LFT
  • Bronchospasm
  • Injection site pain
220
Q

Oritavancin pharmacokinetics

A
  • Renal/fecal excretion

- 85% protein binding

221
Q

Dalbavancin warnings

A
  • Hepatic effects

- Hypersensitivity infusion reactions

222
Q

Dalbavancin ADRs

A
  • Flushing
  • Phlebitis
  • Headache
  • Hypoglycemia
  • NDV
  • Hepatotoxicity
  • Increase INR
  • Leukopenia
  • Neutropenia
  • Thrombocytopenia
  • Red man syndrome
223
Q

Dalbavancin pharmacokinetics

A
  • 93% protein binding

- Renal/fecal excretion

224
Q

Red Man Syndrome

A
  • Anaphylaxis because of rapid infusion
  • Skin thickens
  • Rash on the face, neck, and upper torso
225
Q

Resistance mechanisms to glycopeptides

A
  • Overexpression of ligase enzymes (VanA) enzymes that catalyze the formation of D-Ala-D-lactate instead of D-ala-D-Ala
  • Vancomycin does not bind to D-Ala-D-lactate

Pharmacology (27 decks)

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