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Inhibitors of Bacterial Cell Wall Synthesis Flashcards

1
Q

Gram-negative membrane

A

Lipid A portion of lipopolysaccharide - endotoxin responsible for gram-negative sepsis

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2
Q

Cell wall protects the bacteria from

A

Osmotic lysis if it is placed in a hypotonic solution

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3
Q

Antibiotics secreted in bile

A

Nafcillin
Ampicillin
Ceftriaxone

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4
Q

Two forms of long-acting penicillin G and their administration

A

Procaine penicillin G and Benzathine penicillin G

Intramuscular administration

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5
Q

Benzathine penicillin G plasma concentration

A

Low plasma concentration of the drug for a few weeks

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6
Q

Procaine penicillin G plasma concentration

A

Higher plasma concentrations of penicillin for about 24 hours

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7
Q

Extended spectrum Carboxypenicillins

A

Carbenicillin

Ticarcillin

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8
Q

Extended spectrum Ureidopenicillins

A

Piperacillin
Mezlocillin
Azlocillin

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9
Q

Extended spectrum Aminopenicillins

A

Ampicillin

Amoxicillin

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10
Q

Extended spectrum Ureidopenicillins active against

A

Selected gram-negative bacilli, such as Klebsiella pneumoniae

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11
Q

Penicillinase-Resistant Antistaphylococcal Penicillins

A 
Methicillin
Nafcillin
Oxacillin (Isoxazolyl penicillin)
Cloxacillin (Isoxazolyl penicillin)
Dicloxacillin (Isoxazolyl penicillin)
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12
Q

Narrow-Spectrum Penicillins

A

Penicillin G

Penicillin V

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13
Q

First-generation cephalosporins

A

Cefazolin

Cephalexin

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14
Q

Second-generation cephalosporins

A

Cefuroxime
Cefprozil
Cefoxitin
Cefotetan

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15
Q

Third-generation cephalosporins

A

Cefotaxime
Ceftazidime
Ceftriaxone
Cefpodoxime

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16
Q

First-generation cephalosporins active against

A

Gram-positive cocci, such as pneumococci, streptococci, and staphylococci. They are also active against a few gram-negative enteric bacilli including E. coli and K. pneumoniae

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17
Q

Second-generation cephalosporins active against

A

Similar activity against gram-positive cocci as the first-generation while demonstrating increased activity against gram-negative bacilli

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18
Q

Third-generation cephalosporins active against

A

Wider range of gram-negative organisms including enteric gram-negative bacilli (Enterobacteriaceae), H. influenzae, and M. catarrhalis

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19
Q

Which bacteria have acquired plasmin-mediated TEM and SHV b-lactamases?

A

Many strains of Enterobacteriaceae, including Escherichia Coli and Klebsiella pneumoniae

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20
Q

Avibactam

A

b-lactamase inhibitor with a unique non-b-lactame structure

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21
Q

Avibactam active against

A

Several types of b-lactamases, including AmpC b-lactamases and other extended-spectrum b-lactamases expressed by cephalosporin-resistant gram-negative bacteria

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22
Q

Fourth and Advanced (fifth)-generation cephalosporin

A

Cefepime

Ceftaroline

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23
Q

Fourth-generation cephalosporin active against

A

P aeruginosa, Enterobacteriaceae, S aureus, and S pneumoniae. It is highly active against Haemophilus and Neisseria sp.

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24
Q

Carbapenem with high affinity for PBP-2

A

Imipenem

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25
Carbapenem that binds both PBP-2 and PBP-3
Meropenem
26
Penicillin G - Clinical use
``` Gram-positive cocci Syphilis-Treponema pallidum Endocarditis- Viridans, streptococci, enterococci Meningitis - Meningococci Pneumonia -Pneumococci Streptococci Enterococci Gas gangrene – Clostridium perfringes Actinomyces ```
27
Penicillin G+V, Dicloxacillin, Nafcillin, Methicillin, Piperacillin, Ticarcillin - Adverse effects
``` High dose: seizures Diarrhea Superinfections Psuedomembranous colitis Hypersensitivity: Uritcaria (hives) Anaphylactic shock Serum sickness Interstitial nephritis Hepatitis Rashes ```
28
Penicillin G - Interactions
Probenecid: inhibits renal secretion – increased serum concentration Benzathine: prolonged half-life.
29
Penicillin V - Clinical use
Gram-positive cocci Pharyngitis – Streptococcus pyogenes
30
Dicloxacillin and Nafcillin - Clinical use
``` Milder infections of penicillinase positive staphylococci Osteomyelitis Endocarditis Pneumonia Skin and soft tissue infections ```
31
Nafcillin - Special considerations
IV adm for serious infections Excreted in bile
32
Nafcillin - Interactions
Probenecid: inhibits renal secretion – increased serum concentration
33
Metchicillin - Clinical use
Seldom used because of resistance and adverse effects
34
Metchicillin - Special considerations
Original drug in this pharm class. Resistance by MRSA
35
Amoxicillin - Clinical use
``` Otitis media Upper respiratory tract infections Skin and soft tissue infections UTI’s Sinusitis Bronchitis Community acquired pneumonia ``` Prophylaxis of bacterial endocarditis in persons with heart valve defects Pneumococci, streptococci, staphylococci, Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli, Pasteurella multocida Bite wound infections – Pasteurella multocida, S. aureus(with clavulanate) Impetigo (with clavulanate) - S. aureus, S. pyogenes
36
Amoxicillin - Special considerations
Bec of resistance: use clavulanate for H. influenzae + M. catarrhalis. Uptake is not impaired by food, unlike the other penicillins
37
Amoxicillin - Adverse effects
``` High dose: seizures Diarrhea Superinfections Psuedomembranous colitis Hypersensitivity: Uritcaria (hives) Anaphylactic shock Serum sickness Interstitial nephritis Hepatitis Rashes ```
38
Amoxicillin - Interactions
Clavulanate: β-lactamase inhibitor Probenecid: inhibits renal secretion – increased serum concentration Contraceptive: Decreased effectiveness
39
Amoxicillin - Similar drugs
Ampicillin Piperacillin Ticarcillin
40
Ampicillin - Clinical use
Meningitis, listeriosis – Listeria monocytogenes Decubitus, diabetic foot ulcers – Gram-positive and anaerobic organisms Endocarditis – Streptococci, enterococci Lyme disease – Borrelia burgdorferi Shigellosis Uncomplicated salmonella Gastroenteritis E.coli Non b-lactamase producing strains of H. influenzae Bite wounds and diabetic foot ulcers (with sulbactam) Combined with aminoglycoside (E.g., gentamicin) to treat enterococcal infections, such as enterococcal endocarditis
41
Ampicillin - Adverse effects
``` Maculopapular rash (viral inf. Like mononucleosis) High dose: seizures Diarrhea Superinfections Psuedomembranous colitis Vaginal candidiasis Hypersensitivity: Uritcaria (hives) Anaphylactic shock Serum sickness Interstitial nephritis Hepatitis Rashes ```
42
Ampicillin - Interactions
Sulbactam: β-lactamase inhibitor
43
Piperacillin, Ticarcillin - Clinical use
Gram-positive and gram-negative aerobic and anaerobic bacteria + some strains of Pseudomonas aeruginosa and Klebsiella pneumonia Intraabdominal, skin, soft tissue, lower respiratory tract, complicated urinary tract, gynecologic Febrile neutropenia pneumonia. Active against P.aeruginosa (UTIs)
44
Piperacillin Ticarcillin - Interactions
``` Tazobactam: β-lactamase inhibitor Aminoglycosides Probenecid: inhibits renal secretion – increased serum concentration Contraceptivse: Decreased effectiveness Clavulanate: β-lactamase inhibitor Aminoglycoside ```
45
Cephalexin - Clinical use
Skin and soft tissue infections (impetigo, cellulitis) caused by gram (+) UTIs -Streptococci, staphylococci
46
Cephalosporins - Adverse effects
Hypersensitivity: (rare, cross-sensitivity to penicillins) Anaphylaxis, fever, skin rashes, nephritis, granulocytopenia, hemolytic anemia Local irritation: pain after IM injection, thrombophlebitis after IV Renal toxicity (intersitial nephritis, tubular necrosis) Cefotetan: + Platelet dysfunction and bleeding Cefepime: + Drug-induced encephalopathy
47
Cefazolin - Clinical use
Prophylaxis of surgical infections – Staphylococci, E. coli, K. pneumoniae Alternative to antistaph. penicillin
48
Cefprozil, Cefuroxime - Clinical use
Otitis media – H. influenzae strains resistant to amoxicillin and other drugs Respiratory tract, skin and soft tissue infections (pneumococci, H. influenzae, M. catarrhalis)
49
Cefotetan - Clinical use
Aerobic and anaerobic gram-negative bacilli, including Bacteroides fragilis Intra-abdominal, gynecological, biliary tract infections
50
Cefotetan - Interactions
Anticoagulants: more potent effect (risk of bleeding!) Alcohol: disulfiram-like reaction
51
Cefoxitin - Clinical use
Surgical prophylaxis for gram-neg
52
Ceftazidime - Clinical use
AVYCAZ: ceftazidime + avibactam Intraabdominal infections UTIs Pneumonia P. aeruginosa and other gram-negative bacteria
53
Ceftazidime - Special considerations
Resistant to some Class-C β-lactamases such as Amp C cephalosporins, TEM, SHV
54
Cefpodoxime, Cefotaxime - Clinical use
Gonorrhea
55
Ceftriaxone - Clinical use
Gonorrhea, UTIs, otitis, meningitis, pneumonia, Lyme disease – Gonococci, pneumococci, meningococci, B. burgdorferi, H. influenzae
56
Cefepime - Clinical use
Intraabdmonial infections UTIs Pneumonia Skin and soft tissue infections Drug-resistant gram-negative bacilli, including Citrobacter and Enterobacter species
57
Ceftaroline - Clinical use
Community-acquired pneumonia Skin and soft tissue infections MRSA, Drug resistant pneumococci
58
Aztreonam - Pharmacologic class + Clinical use
Monobactam Aerobic gram-negative bacilli Enterobacter, Citrobacter, Klebsiella, Proteus, P. aeruginosa UTIs, gynecological, intra-abdominal, skin, lung infections Pneumonia Meningitis Sepsis
59
Azetreonam - Special considerations
Cross-sensitivity for penicillin is not common Resistant to most beta-lactamses
60
Azetreonam - Adverse effects
Hypersensitivity reactions Thrombophlebitis Skin rashes Increases level of serum aminotransferase
61
Carbapenems - Clinical use
Active against gram (-) rods- P. Aeruginosa, and gram (+) org. Endocarditis Pneumonia UTIs Pelvic, skin, soft tissue, intra-abdominal inf. Meningitis, febrile neutropenia, sepsis
62
Imipenem - Special considerations + Contraindications
Resistant to most b-lactamases but not carbapenemase of metallo b-lactamase. Excessive levels of imipenem in patients with renal failure may lead to seizures
63
Carbapenems - Adverse effects
``` Cross-sensitivity with penicillin allergy Seizures in patients with epilepsy and renal failure Diarrhea Vomiting Anemia Leukopenia Thrombocytopenia Altered bleeding time ```
64
Imipenem - Interactions
Cilastatin: dehydropeptidase inhibitor that increases time of activity of imipenem.
65
Vancomycin - Clinical use
Gram-positive cocci and bacilli, MRSA Streptococcal and enterococcal infections caused by penicillin-resistant organisms, including endocarditis and necrotizing fasciitis Meningitis caused by penicillin-resistant strain of pneumococcus (in combination with cefotaxime, ceftriaxone, or rifampin) Bacillus, Clostridium, Cornyebacterium species Bone and joint, skin and soft tissue infections Pneumonia Septicemia Endocarditis
66
Vancomycin, Telavancin - Adverse effects
Reduced nephro- and ototoxicity now compared to before Hypotension and erythematous rash with to quick infusion (called red man syndrome) Vestibular dysfunction (ataxia, vertigo, nystagmus, nausea) Cochlear dysfunction (tinnitus, hearing loss) Irritating to tissue phlebitis at site of injection Chills, fever
67
Vancomycin - Interactions
Aminoglycosides and amphothericin B: Increased nephrotoxicity
68
Telavancin - Clinical use
Skin and soft tissue inf by MSSA+ MRSA + vancomycin-sensitive E. faecalis
69
Telavancin - Contraindications
Do not administer to pregnant women, it is teratogenic
70
Bacitracin - Clinical use
Gram-positive cocci, including staphylococci and streptococci Skin and eye infections Combined with polymyxin and neomycin
71
Bacitracin - Special considerations
Used only for topical treatment
72
Bacitracin - Adverse effects
Very nephrotoxic
73
Fosfomycin - Clinical use
Enterococci and many gram-negative enteric bacilli, including E. coli, Citrobacter, Klebsiella, Proteus, Serratia marcescens Uncomplicated UTIs by E. coli or E. faecalis
74
Fosfomycin - Adverse effects
Diarrhea
75
Beta lactam antibiotics (Penicillins, cephalosporins, monobactam, carbapenems) - MoA
Binds to PBPs, inhibiting cross-linking of peptidoglycan -> inhibition of bacterial cell wall synthesis.
76
Bacitracin - MoA
Inhibition of regeneration of bactoprenol phosphate (C55-isoprenyl P)
77
Fosfomycin - MoA
Inhibiton of enolpyruvyl transferase, blocks the addition of phosphoenolpyruvate to UDP-GlcNAc, prevents synthesis of UDP-MurNAc --> Blocks synthesis of peptidoglycan
78
Vancomycin - MoA
Binds to peptidoglycan and prevents cross lining--> inhibits cell wall synthesis

Pharmacology (55 decks)

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