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Pharmacology > Inhibitors of Bacterial Cell Wall Synthesis > Flashcards

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
Q

Carbapenem that binds both PBP-2 and PBP-3

A

Meropenem

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26
Q

Penicillin G - Clinical use

A 
Gram-positive cocci
Syphilis-Treponema pallidum
Endocarditis- Viridans, streptococci, enterococci
Meningitis - Meningococci
Pneumonia -Pneumococci
Streptococci 
Enterococci
Gas gangrene – Clostridium perfringes
Actinomyces
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27
Q

Penicillin G+V, Dicloxacillin, Nafcillin, Methicillin, Piperacillin, Ticarcillin - Adverse effects

A 
High dose: seizures
Diarrhea
Superinfections
Psuedomembranous colitis 
Hypersensitivity:
Uritcaria (hives)
Anaphylactic shock
Serum sickness
Interstitial nephritis
Hepatitis
Rashes
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28
Q

Penicillin G - Interactions

A

Probenecid: inhibits renal secretion – increased serum concentration
Benzathine: prolonged half-life.

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29
Q

Penicillin V - Clinical use

A

Gram-positive cocci

Pharyngitis – Streptococcus pyogenes

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30
Q

Dicloxacillin and Nafcillin - Clinical use

A 
Milder infections of penicillinase positive staphylococci 
Osteomyelitis
Endocarditis
Pneumonia
Skin and soft tissue infections
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31
Q

Nafcillin - Special considerations

A

IV adm for serious infections

Excreted in bile

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32
Q

Nafcillin - Interactions

A

Probenecid: inhibits renal secretion – increased serum concentration

33
Q

Metchicillin - Clinical use

A

Seldom used because of resistance and adverse effects

34
Q

Metchicillin - Special considerations

A

Original drug in this pharm class. Resistance by MRSA

35
Q

Amoxicillin - Clinical use

A 
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
Q

Amoxicillin - Special considerations

A

Bec of resistance: use clavulanate for H. influenzae + M. catarrhalis.

Uptake is not impaired by food, unlike the other penicillins

37
Q

Amoxicillin - Adverse effects

A 
High dose: seizures
Diarrhea
Superinfections
Psuedomembranous colitis 
Hypersensitivity:
Uritcaria (hives)
Anaphylactic shock
Serum sickness
Interstitial nephritis
Hepatitis
Rashes
38
Q

Amoxicillin - Interactions

A

Clavulanate: β-lactamase inhibitor
Probenecid: inhibits renal secretion – increased serum concentration
Contraceptive: Decreased effectiveness

39
Q

Amoxicillin - Similar drugs

A

Ampicillin
Piperacillin
Ticarcillin

40
Q

Ampicillin - Clinical use

A

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
Q

Ampicillin - Adverse effects

A 
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
Q

Ampicillin - Interactions

A

Sulbactam: β-lactamase inhibitor

43
Q

Piperacillin, Ticarcillin - Clinical use

A

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
Q

Piperacillin Ticarcillin - Interactions

A 
Tazobactam: β-lactamase inhibitor
Aminoglycosides
Probenecid: inhibits renal secretion – increased serum concentration
Contraceptivse: Decreased effectiveness
Clavulanate: β-lactamase inhibitor
Aminoglycoside
45
Q

Cephalexin - Clinical use

A

Skin and soft tissue infections (impetigo, cellulitis) caused by gram (+)
UTIs -Streptococci, staphylococci

46
Q

Cephalosporins - Adverse effects

A

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
Q

Cefazolin - Clinical use

A

Prophylaxis of surgical infections – Staphylococci, E. coli, K. pneumoniae
Alternative to antistaph. penicillin

48
Q

Cefprozil, Cefuroxime - Clinical use

A

Otitis media – H. influenzae strains resistant to amoxicillin and other drugs

Respiratory tract, skin and soft tissue infections (pneumococci, H. influenzae, M. catarrhalis)

49
Q

Cefotetan - Clinical use

A

Aerobic and anaerobic gram-negative bacilli, including Bacteroides fragilis

Intra-abdominal, gynecological, biliary tract infections

50
Q

Cefotetan - Interactions

A

Anticoagulants: more potent effect (risk of bleeding!)
Alcohol: disulfiram-like reaction

51
Q

Cefoxitin - Clinical use

A

Surgical prophylaxis for gram-neg

52
Q

Ceftazidime - Clinical use

A

AVYCAZ: ceftazidime + avibactam

Intraabdominal infections
UTIs
Pneumonia

P. aeruginosa and other gram-negative bacteria

53
Q

Ceftazidime - Special considerations

A

Resistant to some Class-C β-lactamases such as Amp C cephalosporins, TEM, SHV

54
Q

Cefpodoxime, Cefotaxime - Clinical use

A

Gonorrhea

55
Q

Ceftriaxone - Clinical use

A

Gonorrhea, UTIs, otitis, meningitis, pneumonia, Lyme disease – Gonococci, pneumococci, meningococci, B. burgdorferi, H. influenzae

56
Q

Cefepime - Clinical use

A

Intraabdmonial infections
UTIs
Pneumonia
Skin and soft tissue infections

Drug-resistant gram-negative bacilli, including Citrobacter and Enterobacter species

57
Q

Ceftaroline - Clinical use

A

Community-acquired pneumonia
Skin and soft tissue infections

MRSA, Drug resistant pneumococci

58
Q

Aztreonam - Pharmacologic class + Clinical use

A

Monobactam

Aerobic gram-negative bacilli

Enterobacter, Citrobacter, Klebsiella, Proteus, P. aeruginosa

UTIs, gynecological, intra-abdominal, skin, lung infections
Pneumonia
Meningitis
Sepsis

59
Q

Azetreonam - Special considerations

A

Cross-sensitivity for penicillin is not common

Resistant to most beta-lactamses

60
Q

Azetreonam - Adverse effects

A

Hypersensitivity reactions
Thrombophlebitis
Skin rashes
Increases level of serum aminotransferase

61
Q

Carbapenems - Clinical use

A

Active against gram (-) rods- P. Aeruginosa, and gram (+) org.
Endocarditis
Pneumonia
UTIs
Pelvic, skin, soft tissue, intra-abdominal inf.
Meningitis, febrile neutropenia,
sepsis

62
Q

Imipenem - Special considerations + Contraindications

A

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
Q

Carbapenems - Adverse effects

A 
Cross-sensitivity with penicillin allergy
Seizures in patients with epilepsy and renal failure
Diarrhea
Vomiting
Anemia
Leukopenia
Thrombocytopenia
Altered bleeding time
64
Q

Imipenem - Interactions

A

Cilastatin: dehydropeptidase inhibitor that increases time of activity of imipenem.

65
Q

Vancomycin - Clinical use

A

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
Q

Vancomycin, Telavancin - Adverse effects

A

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
Q

Vancomycin - Interactions

A

Aminoglycosides and amphothericin B: Increased nephrotoxicity

68
Q

Telavancin - Clinical use

A

Skin and soft tissue inf by MSSA+ MRSA + vancomycin-sensitive E. faecalis

69
Q

Telavancin - Contraindications

A

Do not administer to pregnant women, it is teratogenic

70
Q

Bacitracin - Clinical use

A

Gram-positive cocci, including staphylococci and streptococci

Skin and eye infections

Combined with polymyxin and neomycin

71
Q

Bacitracin - Special considerations

A

Used only for topical treatment

72
Q

Bacitracin - Adverse effects

A

Very nephrotoxic

73
Q

Fosfomycin - Clinical use

A

Enterococci and many gram-negative enteric bacilli, including E. coli, Citrobacter, Klebsiella, Proteus, Serratia marcescens

Uncomplicated UTIs by E. coli or E. faecalis

74
Q

Fosfomycin - Adverse effects

A

Diarrhea

75
Q

Beta lactam antibiotics (Penicillins, cephalosporins, monobactam, carbapenems) - MoA

A

Binds to PBPs, inhibiting cross-linking of peptidoglycan -> inhibition of bacterial cell wall synthesis.

76
Q

Bacitracin - MoA

A

Inhibition of regeneration of bactoprenol phosphate (C55-isoprenyl P)

77
Q

Fosfomycin - MoA

A

Inhibiton of enolpyruvyl transferase, blocks the addition of phosphoenolpyruvate to UDP-GlcNAc, prevents synthesis of UDP-MurNAc
–> Blocks synthesis of peptidoglycan

78
Q

Vancomycin - MoA

A

Binds to peptidoglycan and prevents cross lining–> inhibits cell wall synthesis

Pharmacology (55 decks)

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