[3S] BETA-LACTAM & OTHER CELL WALL-AND MEMBRANE-ACTIVE ANTIBIOTICS (Table) Flashcards
(166 cards)
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
2
Q
NARROW SPECTRUM PENICILLINS PKINETICS
Pen G excretion & ROA
A
Kidneys
IM/IV
3
Q
PENICILLINS MOA
- Bactericidal
- Prevents bacterial cell wall synthesis by binding to and inhibiting cell wall transpeptidases
- Inhibition of transpeptidase enzyme that act to cross-link linear peptidoglycan chains
- Activation of autolytic enzymes that cause lesions in the bacterial cell wall
A
Narrow Spectrum Penicillins
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
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
6
Q
NARROW SPECTRUM PENICILLINS PKINETICS
● Delayed absorption;
● Can cross the BBB at MIC.
A
Benzathin & Procaine Pen G
7
Q
NARROW SPECTRUM PENICILLINS
Benzathin & Procaine Pen G ROA
A
IM
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
9
Q
NARROW SPECTRUM PENICILLINS CA
1st line in Syphilis
A
Benzathine Penicillin
10
Q
NARROW SPECTRUM PENICILLINS CA
Pneumococcal
Gonorrhea
A
Procaine Pen G
11
Q
NARROW SPECTRUM PENICILLINS PKINETICS
Low bioavailability; absorption is impaired by food
A
Pen V
12
Q
NARROW SPECTRUM PENICILLINS PKINETICS
Pen V excretion & ROA
A
Kidney
PO
13
Q
NARROW SPECTRUM PENICILLINS CA
Oropharyngeal infections
Infections by aerobic Gram (+) bacteria and some Gram (-) cocci (gonococci and meningococci)
A
Pen V
14
Q
VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS PKINETICS
Excretion
A
Partly excreted in bile
15
Q
VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS PKINETICS
Highly protein bound
A
Nafcillin
16
Q
VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS ROA
Methicillin, Nafcillin, Oxacillin
A
IM/IV
17
Q
VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS CA
Prototype antistaphylococcal drug
A
Methicillin
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
19
Q
VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS CA
Serious staphylococcal infections (endocarditis)
A
Nafcillin & Oxacillin
20
Q
VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS TOXICITY
Neutropenia
Interstitial nephritis
A
Nafcillin
21
Q
VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS TOXICITY
Hepatitis
A
Oxacillin
22
Q
VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS
Acid-stable & ROA
A
Dicloxacillin - PO
23
Q
VERY NARROW SPECTRUM PENICILLINASE RESISTANT AGENTS AGAINST S. AUREUS CA
Mild to moderate localized staphylococcal infections
A
Dicloxacillin
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
25
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS
Absorption is impaired by food
Ampicillin
26
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS
Ampicillin ROA & combined with _____
PO/IM/IV
Sulbactam
27
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS CA
Pneumococcal infections (drug of choice)
Serious infections caused by susceptible organisms
Ampicillin
28
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.
Ampicillin & Amoxicillin
29
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS
Amoxicillin ROA & combined with _____
PO
Clavulanic Acid
30
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS CA
● Most active - Pneumococci
● Bacterial sinusitis
● Bacterial otitis
● Lower RTIs
Amoxicillin
31
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS TOXICITY
Skin rashes in the setting of viral illness
Amoxicillin
32
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS
Combined with penicillinase inhibitors
Piperacillin & Ticarcillin
33
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS PKINETICS
Piperacillin ROA & combined with ______
IV (same w Ticarcillin)
Tazobactam
34
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS CA
Enhanced selectivity against Gr(-) rods
● Pseudomonas – nosocomial infections
● Enterobacter
● Klebsiella
● P. aeuriginosa
Piperacillin & Ticarcillin
35
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS CA
________ with β-lactamase inhibitors:
● S. aureus
Piperacillin
36
WIDER SPECTRUM PENICILLINASE SUSCEPTIBLE DRUGS TOXICITY
With tazobactam:
Greater incidence of acute kidney injury (with vancomycin)
Piperacillin
37
CEPHALOSPORINS AND CEPHAMYCINS CA
● Gr(+) cocci
● E. coli
● K pneumoniae
● Proteus mirabilis
1st Gen
38
CEPHALOSPORINS AND CEPHAMYCINS CA
Extended Gr(-) activity:
o Klebsiella
o H. influenzae
o Bacteroides fragilis
o Serratia
2nd Gen
39
CEPHALOSPORINS AND CEPHAMYCINS CA
Expanded Gr(-) coverage
o Citrobacter
o Serratia
o Providencia
o Pseudomona
3rd Gen
40
CEPHALOSPORINS AND CEPHAMYCINS CA
● Pseduomonas
● Enterobacteriaceae
● Methicillin-susceptible S.aureus
● S. pneumoniae
● Haemophilus
● Neisseria sp.
4th Gen
41
T/F: 2nd & 3rd gen are not useful against Enterobacter
T
42
T/F: All 3rd gen drugs are able to cross BBB.
F; pera & fixi can’t cross, the rest can
43
1ST GENERATION CEPHALOSPORINS PKINETICS
Cefazolin excretion & ROA
Renal
IV/IM
44
CEPHALOSPORINS MOA
● Binds to PBPs to inhibit bacterial cell wall synthesis.
● Inhibits autolysin inhibitor and induces cell lysis through autolysins
1st Gen
45
1ST GENERATION CEPHALOSPORINS CA
● Gram-positive cocci (streptococci & staphylococci)
● Drug of choice for surgical prophylaxis
● UTI, cellulitis, soft tissue abscesses
Cafazolin & Cephalexin
46
1ST GENERATION CEPHALOSPORINS CA
● Can’t be used on meningitis
● Better tolerated than antistaphylococcal penicillins
Cefazolin
47
1ST GENERATION CEPHALOSPORINS TOXICITIES
● Surgical prophylaxis
● IV therapy
● Bacteremia
● Mild penicillin allergy
Cefazolin
48
1ST GENERATION CEPHALOSPORINS TOXICITIES
Pharyngitis
Cephalexin & Cefadroxil
49
1ST GENERATION CEPHALOSPORINS PKIENTICS
Cephalexin excretion & ROA
Renal
PO
50
2ND GENERATION CEPHALOSPORINS PKINETICS
Needs frequent reapplications due to short half- lives (41 to 59 min)
Cefoxitin & Cefotetan
51
2ND GENERATION CEPHALOSPORINS PKINETICS
Cefoxitin excretion & ROA
Renal
IV/IM
52
2ND GENERATION CEPHALOSPORINS MOA
Inhibits cell wall synthesis
Cefoxitin & Cefotetan
53
2ND GENERATION CEPHALOSPORINS CA
Anaerobic infections such as peritonitis, diverticulitis, and pelvic inflammatory disease
Cefoxitin & Cefotetan
54
2ND GENERATION CEPHALOSPORINS CA
● B. fragilis and some Serratia strains
● Also effective against gram-positive organisms
Cefoxitin & Cefotetan
55
2ND GENERATION CEPHALOSPORINS TOXICITIES
2nd-3rd & 5th main toxicity
Allergy, complete cross-reactivity among cephalosporins and partial to penicillins
56
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
2nd, 3rd, 5th Gen
57
2ND GENERATION CEPHALOSPORINS PKINETICS
Cefotetan excretion & ROA
Renal
IV/IM
58
2ND GENERATION CEPHALOSPORINS TOXICITIES
Bleeding disroders
o Hypothrombinemia or disulfiram-like reactions with ethanol
Cefotetan & Cefamandole
59
2ND GENERATION CEPHALOSPORINS PKINETICS
Cefamandole excretion & ROA
Mainly renal partially bile
IV/IM
60
2ND GENERATION CEPHALOSPORINS MOA
Binds to PBPs to inhibit bacterial cell wall synthesis. Inhibits autolysin inhibitor
Cefamandole, Cefuroxime & Cefaclor
61
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
Cefamandole
62
2ND GENERATION CEPHALOSPORINS PKINETICS
Cefuroxime excretion & ROA
Renal
PO/IV/IM
63
2ND GENERATION CEPHALOSPORINS CA
● H. influenzae and M. catarrhalis
● Less active against B. fragilis and Serratia
● Also effective against gram-positive organisms
Cefuroxime & Cefaclor
64
2ND GENERATION CEPHALOSPORINS CA
● Can treat meningitis to a lesser extent than ceftriaxone or cefotaxime
● CAP
● Pneumococci
Cefuroxime
65
2ND GENERATION CEPHALOSPORINS CA
● crosses BBB
● CAP/COB
Cefuroxime Sodium
66
2ND GENERATION CEPHALOSPORINS CA
Active against B-lactamase producing bacteria
Cefuroxime axetil
67
3RD GENERATION CEPHALOSPORINS PKINETICS
Ceftazidime excretion & ROA
Kidney
IV/IM
68
3RD GENERATION CEPHALOSPORINS MOA
Binds to PBPs, primarily PBP3 to inhibit bacterial cell wall synthesis.
Ceftazidime & Cefoperazone
69
3RD GENERATION CEPHALOSPORINS CA
● GR(+), GR(-)
● P. aeruginosa infections
Cetazidime
70
3RD GENERATION CEPHALOSPORINS PKINETICS
Cefoperazone excretion and ROA
Bile
IV/IM
71
3RD GENERATION CEPHALOSPORINS CA
● GR(+), GR(-)
● Cannot penetrate the BBB (alongside cefixime)
● Pseudomonas
Cefoperazone
72
3RD GENERATION CEPHALOSPORINS MOA
Binds to PBPs to inhibit bacterial cell wall synthesis.
Has better affinity with PBP 1b and PBP3
Cefotaxime
73
3RD GENERATION CEPHALOSPORINS CA
● GR(+), GR(-)
● Primarily used to treat gonorrhea, meningitis and kidney infections.
Cefotaxime
74
3RD GENERATION CEPHALOSPORINS CA
Most active against penicillin-non-susceptible pneumococci
Cefotaxime
75
3RD GENERATION CEPHALOSPORINS CA
Meningitis:
Pneumococci, Meningococci, H. influenzae, Enteric gram (-) rods.
Cefotaxime
76
3RD GENERATION CEPHALOSPORINS PKINETICS
Ceftriaxone excretion & ROA
Bile
IV/IM
77
3RD GENERATION CEPHALOSPORINS MOA
Binds to carboxypeptidases, endopeptidases, and transpeptidases to inhibit peptidoglycan synthesis
Ceftriaxone
78
3RD GENERATION CEPHALOSPORINS CA
● Administer with azithromycin for gonococcal infections
● Meningitis, Acute otitis media, Gonorrhea (with cefixime)
Ceftriaxone
79
3RD GENERATION CEPHALOSPORINS PKINETICS
Resistant to gastric acid for oral absorption
Cefixime
80
3RD GENERATION CEPHALOSPORINS PKINETICS
Cefixime excretion & ROA
Renal
PO
81
3RD GENERATION CEPHALOSPORINS MOA
Binds to PBPs to inhibit bacterial cell wall synthesis.
Cefixime & Ceftizoxime
82
3RD GENERATION CEPHALOSPORINS CA
● Gonorrhea (with ceftriaxone)
● Less active against pneumococci and poor activity against S. aureus
Cefixime
83
3RD GENERATION CEPHALOSPORINS PKINETICS
Ceftizoxime excretion & ROA
Renal and partly bile
IV/IM
84
3RD GENERATION CEPHALOSPORINS CA
B. fragilis infections
Ceftizoxime
85
4TH GEN CEPHALOSPORINS PKINETICS
Cefepime excretion & ROA
Kidneys, partially liver
IV/IM
86
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
4th Gen: Cefepime
87
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
4th Gen: Cefepime
88
CEPHALOSPORINS CA
● Resistant to beta- lactamases
● Penicillin-non-susceptible
● Febrile Neutropenia
4th Gen: Cefepime
89
CEPHALOSPORINS TOXICITY
Encephalopathy, myoclonus, seizures, excitability nonconvulsive epilepticus neuromuscular and status
4th Gen: Cefepime
90
5TH GENERATION CEPHALOSPHORINS PKINETICS
Ceftaroline Fosamil excretion & ROA
Kidney
IV/IM
91
5TH GENERATION CEPHALOSPHORINS PKINETICS
Prodrug
Ceftaroline Fosalim
92
5TH GENERATION CEPHALOSPHORINS MOA
Increases binding to PBP2a, lowering staphylococci’s methicillin resistance
Ceftaroline Fosamil
93
5TH GENERATION CEPHALOSPHORINS CA
● MRSA
● Enterococci (some)
● Broad Gr(-) coverage similar to ceftriaxone
Ceftaroline Fosamil
94
5TH GENERATION CEPHALOSPHORINS CA
● Skin and soft tissue infections
● CAP
● Off-label:
o Bacteremia
o Endocarditis
o Osteomyelitis
Ceftaroline Fosamil
95
5TH GENERATION CEPHALOSPHORINS PKINETICS
Ceftolozane Tazobactam excretion and ROA
Kidneys, remaining: single metabolite
IV
96
5TH GENERATION CEPHALOSPHORINS PKINETICS
Cefiderocol excretion & ROA
Kidneys, portian is excreted as metabolites and in feces
IV
97
5TH GENERATION CEPHALOSPHORINS MOA
● Binds to PBPs to inhibit bacterial cell wall synthesis
● Tazobactam is utilized with piperacillin and ceftolozane to increase their effectiveness
Ceftolozane Tazobactam
98
5TH GENERATION CEPHALOSPHORINS MOA
● Binds to PBP Bound by active iron transporters
● Pumped into the cell wall at high concentrations
● Passive transport
Cefiderocol
99
5TH GENERATION CEPHALOSPHORINS CA
Gr(-)
● P. aeruginosa
● Extended β-lactamase-producing Enterobacter
● Intra-abdominal infections
● UTIs
Ceftolozane Tazobactam
100
5TH GENERATION CEPHALOSPHORINS CA
Effective against aerobic gram-negative organisms
● Enterobacteriaceae
● P. aeruginosa
● A. baumannii
● carbapenemase producing bacteria
Cefiderocol
101
5TH GENERATION CEPHALOSPHORINS CA
Carbapenemase-producing organisms
Ceftazidime-avibactam
102
OTHER B-LACTAM DRUGS PKINETICS
Tolerated by penicillin-allergic patients
Aztreonam
103
OTHER B-LACTAM DRUGS PKINETICS
Aztreonam elimination & ROA
Renal tubular secretion
IV
104
OTHER B-LACTAM DRUGS PKINETICS
Monobactam 1st drug
Imipenem
105
OTHER B-LACTAM DRUGS PKINETICS
● Rapidly deactivated by renal dehydropeptidases I
Imipenem
106
OTHER B-LACTAM DRUGS PKINETICS
Inhibits renal dehydropeptidases I, increases half life, and inhibits formation of nephrotoxic metabolites
Monobactam: Imipenem-cilastatin
107
OTHER B-LACTAM DRUGS PKINETICS
Carbapanems: Imipenem excretion & ROA
Renal
IV
108
OTHER B-LACTAM DRUGS PKINETICS
● Similar to imipenem
● Not metabolized by dehydropeptidases
Carbapanems: Meropenem
109
OTHER Β-LACTAM DRUGS PKINETICS
Carbapanems: Meropenem excretion & ROA
Renal
IV
110
OTHER Β-LACTAM DRUGS PKINETICS
Longest half-life among the carbapenems (4 hours)
Ertapenem
111
OTHER Β-LACTAM DRUGS PKINETICS
Ertapenem excretion & ROA
Renal
IV/IM
112
OTHER Β-LACTAM DRUGS MOA
● Covalently binds to PBPs
● Susceptible to carbapenemase and metallo-B-lactamases
Carbapanems
113
OTHER Β-LACTAM DRUGS MOA
● Inhibitor of cell wall synthesis binding to PBP3
● Synergistic with aminoglycosides
Monobactam: Aztreonam
114
OTHER Β-LACTAM DRUGS CA
● Klebsiella, pseudomonas, serratia
● Pneumonia
● Meningitis
● Sepsis (with history of penicillin anaphylaxis)
Monobactam: Aztreonam
115
OTHER Β-LACTAM DRUGS CA
Not active against gram (+) and anaerobes
Monobactam: Aztreonam
116
OTHER Β-LACTAM DRUGS CA
● Gram (+) cocci, gram (-) rods, anaerobes
● Combine with aminoglycosides for pseudomonas infections
● Enterobacter
Carbapanems
117
OTHER Β-LACTAM DRUGS CA
● Used against P. aeruginosa and penicillin-non-
susceptible pneumococci
● Febrile neutropenia
Carbapanems: Imipenem & Meropenem
118
OTHER Β-LACTAM DRUGS TOXICITIES
● Nausea
● Vomiting
● Diarrhea
● Skin rashes
● Reactions at infusion sites
● Renal failure
Carbapanems: Imipenem
119
OTHER Β-LACTAM DRUGS TOXICITIES
Less likely to cause seizures
Carbapanems: Meropenem
120
BETA-LACTAMASE INHIBITORS PKINETICS
Clavulanic Acid excretion & ROA
Unchanged in Urine
PO/IV
121
BETA-LACTAMASE INHIBITORS PKINETICS
Sulbactam excretion & ROA
Unchanged in urine
IM/IV
122
BETA-LACTAMASE INHIBITORS PKINETICS
Tazobactam elimination & ROA
Kidneys
IV
123
BETA-LACTAMASE INHIBITORS PKINETICS
● Does not undergo significant metabolism
● Can be found mostly unchanged in plasma
Relebactam
124
BETA-LACTAMASE INHIBITORS PKINETICS
Relebactam ROA
IV
125
BETA-LACTAMASE INHIBITORS PKINETICS
Avibactam & Vaborbactam excretion & ROA
Renal
IV
126
BETA-LACTAMASE INHIBITORS MOA
Combined with?
1. Clavulanic Acid
2. Sulbactam
3. Tazobactam
4. Ceftazidime
5. Meropenem
1. Amoxicillin
2, Ampicillim
3. Piperacillin / Ceftolozane
4. Avibactam
5. Avorbactam
127
BETA-LACTAMASE INHIBITORS MOA
Prevents bacteria from the hydrolysis of imipenem
Relebactam
128
BETA-LACTAMASE INHIBITORS CA
Plasmid-encoded beta-lactamases: gonococci, streptococci, E. coli, H. influenzae
Clavulanic Acid
Sulbactam
Tazobactam
129
BETA-LACTAMASE INHIBITORS CA
Imipenem nonsusceptible P. aeruginosa
Similar activity with avibactam
Relebactam
130
BETA-LACTAMASE INHIBITORS CA
Novel; active against Abler Class a, C, and D B-lactamases
Avibactam
Avorbactam
131
BETA-LACTAMASE INHIBITORS TOXICITIES
● Allergic reactions (skin rash, itching, swelling of lipid, throat, face)
● Liver injury, severe diarrhea, fever
Clavulanic Acid
132
BETA-LACTAMASE INHIBITORS TOXICITIES
● Changes in skin color, diarrhea
● Pain, tenderness, or swelling of the foot or leg
Sulbactam
133
BETA-LACTAMASE INHIBITORS TOXICITIES
Rash, itching, hives, difficulty breathing or swallowing, wheezing, severe diarrhea
Tazobactam
134
BETA-LACTAMASE INHIBITORS TOXICITIES
Confusion, headache, nausea, decreased urine input
Relebactam
135
BETA-LACTAMASE INHIBITORS TOXICITIES
Nausea, vomiting, constipation, or anxiety
Avibactam
136
BETA-LACTAMASE INHIBITORS TOXICITIES
Headache, Phlebitis, Diarrhea, Hypersensitivity, etc.
Avorbactam
137
GLYCOPEPTIDES PKINETICS
Poorly absorbed by GI tract; only use orally for colitis (C. difficile)
Vancomycin
138
GLYCOPEPTIDES PKINETICS
Vancomycin excretion & ROA
Renal
IV
139
GLYCOPEPTIDES PKINETICS
Teicoplanin ROA
IV/IM
140
GLYCOPEPTIDES PKINETICS
Telavancin ROA
IV
141
GLYCOPEPTIDES PKINETICS
Dalbavancin & Oritavancin ROA
IV (+ longest half-life)
142
GLYCOPEPTIDES MOA
● Bactericidal
● Binds to D-Ala-D-Ala terminal
● Inhibits transglycosylase
● Weakens peptidoglycan; becomes susceptible to lysis
Vancomycin & Teicoplanin
143
GLYCOPEPTIDES MOA
● Binds to D-Ala-D-Ala terminal Increases membrane permeability
● Disrupts bacterial cell membrane potential
Telavancin
144
GLYCOPEPTIDES MOA
Inhibits RNA synthesis
Oritavancin
145
GLYCOPEPTIDES CA
● Gr(+) cocci
● Gr(+) anaerobes
o C. difficile
● MRSA
● Staphylococcus
Vancomycin & Teicoplanin
146
GLYCOPEPTIDES CA
● With gentamicin and streptomycin
o Enterococcus faecium
o Enterococcus faecalis
Vancomycin & Teicoplanin
147
GLYCOPEPTIDES CA
● With gentamicin: Enterococcal endocariditis
● With cefotaxime/ ceftriaxone / rifampin: Meningitis
● Colitis (oral; caused by C. difficile)
Vancomycin & Teicoplanin
148
GLYCOPEPTIDES CA
Specific Bacteria:
● Gr(+)
● Strains with reduced susceptibility to vancomycin
Infection:
● Complicated skin and soft tissue infections
● Hospital-acquired pneumonia
Telavancin
149
GLYCOPEPTIDES CA
Lower MICs against Gram (+) bacteria including MRSA and VRE.
Dalba & Orita
150
GLYCOPEPTIDES CA
Osteomyelitis
Dalba
151
GLYCOPEPTIDES TOXICITIES
● Phlebitis
● Chills and fever
● Ototoxicity (rare)
● Nephrotoxicity
● Red man syndrome
Vancomycin & Teicoplanin
152
GLYCOPEPTIDES TOXICITIES
● Nephrotoxicity (associated)
● Teratogenic (potential)
Telavancin
153
GLYCOPEPTIDES TOXICITIES
Mild to moderate renal or hepatic impairment
Dalba & Orita
154
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS PKINETICS
Excretion & ROA
ALL: Renal
Daptom: IV
Fosfomycin: IM/IV/PO
Bacitracin: Topical
Cycloserine: PO
155
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS MOA
● Calcium-dependent insertion to cell membrane
● Depolarization
● Potassium efflux
● Rapid cell death
Daptomycin
156
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
Fosfomycin
157
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS MOA
Interferes with dephosphorylation in the cycling of the lipid carrier that transfers peptidoglycan subunits
Bacitracin
158
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS MOA
● Inhibits incorporation of d- alanine into peptidoglycan pentapeptide
● Inhibits alanine racemase
Cycloserine
159
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS CA
● Similar activity to vancomycin
● Active against vancomycin- resistant strains of
enterococci and S. aureus (VRE & VRSA)
Daptomycin
160
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS CA
● Gram (+) and gram (-)
● UTI, pyelonephritis
● Safe for pregnancy
Fosfomycin
161
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS CA
● Bacterial infections on surface skin lesions or mucous membranes
o Gr(+)
Bacitracin
162
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS CA
● Tuberculosis resistant to first-line agents
o strains of Mycobacterium tuberculosis
Cycloserine
163
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS TOXICITIES
● Myopathy
● Allergic pneumonitis
● Not used for pneumonia (antagonized by pulmonary surfactant)
Daptomycin
164
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS TOXICITIES
Diarrhea, nausea, headache fungal vaginitis, allergy, etc.
Fosfomycin
165
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS TOXICITIES
● Highly nephrotoxic (systemic administration)
● Hypersensitivity
Bacitracin
166
OTHER CELL WALL- OR MEMBRANE-ACTIVE AGENTS TOXICITIES
Neurotoxicity - tremors, seizures, convulsions, psychosis
Cycloserine
