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Pharmacology > Penicillins, Cephalosporins, and Other β-Lactam Antibiotics > Flashcards

Penicillins, Cephalosporins, and Other β-Lactam Antibiotics Flashcards

1
Q

Β-lactam Antibiotics

A

Penicillins Cephalosporins Carbapenems

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2
Q

MOA of B-lactam antibiotics

A

inhibition of synthesis of the bacterial peptidoglycan cell wall

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3
Q

What is acylated by b-lactam antiobiotics?

A

the transpeptidase via cleavage of the –CO-N- bond of the B-lactam ring - Inhibit the transpeptidation reaction (last step in peptidoglycan synthesis - There are additional, related targets collectively known as Penicillin-binding Protein (PBP) – e.g. Transpeptidase

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4
Q

MECHANISMS OF BACTERIAL RESISTANCE TO PENICILLINS AND CEPHALOSPORINS

A
  1. Mutations -that decrease the affinity of PBPs for the antibiotic
  2. Acquisition of an additional high-molecular-weight PBP (via a transposon) with a very low affinity for all β-lactam antibiotics - Methicillin-resistant Staphylococcus aureus MRSA
  3. Inability of the agent to penetrate to its site of action
  4. Active efflux pumps remove the antibiotic from its site of action before it can act
  5. Destruction of antibiotics enzymatically via the action of β-lactamases - (4 classes: A to D)
  6. Microorganisms adhering to implanted prosthetic devices (e.g. catheters, artificial joints, prosthetic heart valves) -produce biofilms – produce extracellular polysaccharides – less sensitive to antibiotic
  7. Bacteria that survive inside viable cells of the host generally are protected from the action of β-lactam antibiotics.
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5
Q

MRSA MOA

A

Acquisition of an additional high-molecular-weight PBP (via a transposon) with a very low affinity for all β-lactam antibiotics

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6
Q

Highly active against Gram +

A

Penicillin G Penicillin V

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7
Q

Readily hydrolyzed by Penicillinase

A

Penicillin G Penicillin V

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8
Q

Ineffective against S. aureus

A

Penicillin G Penicillin V

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9
Q

First choice for treatment of penicillinase-producing S. aureus and S. epidermidis

A

Penicillinase-resistant Methicillin, Nafcillin, Oxacillin, Cloxacillin, Dicloxacillin (DMONC)

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10
Q

Antimicrobial activity against Gram – organisms (H. influenzae, E. coli & Proteus mirabiis)

A

Ampicillin, Amoxicillin + Clavulanate or Sulbactam (β-lactamase inhibitor)

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11
Q

Antimicrobial activity against Pseudomonas, Enterobacter, Proteus spp

A

Carbenicillin, Carbenicillin indantyl, Ticarcillin

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12
Q

Inferior to Ampicillin against Gram + cocci & Listeria monocytogenes

A

Carbenicillin, Carbenicillin indantyl, Ticarcillin

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13
Q

Less active than Piperacillin against Pseudomonas

A

Carbenicillin, Carbenicillin indantyl, Ticarcillin

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14
Q

Excellent antimicrobial activity against Pseudomonas, Klebsiella, & certain other Gram – microorganisms

A

Mezlocillin, Azlocillin, Piperacillin (MAP)

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15
Q

Retains activity of Ampicillin against Gram + cocci and L. monocytogenes

A

Mezlocillin, Azlocillin, Piperacillin (MAP)

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16
Q

Rheumatic Fever prophylaxis

A

Penicillin G - Gastric pH 2 – destroys antibiotic

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17
Q

More stable in acidic medium: Penicillin V or G?

A

Penicillin V

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18
Q

↓ tubular secretion of Penicillin ↑ plasma concentration

A

Probenecid

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19
Q

T/F: Penicillin G penetrates when meninges are inflamed

A

True

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20
Q

inhibits transport of Penicillin from CSF to bloodstream

A

Probenecid

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21
Q

Pneumococcal Infections

A

Penicillin G - agent of choice

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22
Q

Pneumococcal Pneumonia

A

3rd Generation CEPHALOSPORINS (Ceftriaxome) 20-24 M units of Penicilin G for 7-10 days

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23
Q

Pneumococcal Meningitits

A

Vancomycin + 3rd generation Cephalosporin 20-24 M units for 14 days of Pen G;

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24
Q

Streptococcal Pharyngitis

A

Pen V 500 mg q6 PO for 10 days

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25
Q

Scarlet Fever

A

Pen V 500 mg q6 PO for 10 days

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26
Q

S. Pyogenes (group A β-hemolytic Streptococcus) – cause RHD

A

Pen V 500 mg q6 PO for 10 days

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27
Q

Streptococcal Toxic Shock & Necrotizing Fascitis

A

Penicillin + Clindamycin

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28
Q

Streptococcal Pneumonia, Arthritis, Meningitis & Endocarditis (S. pyogenes)

A

Pen G 12-20M units IV 2-4 weeks Endocarditis: for 4 weeks

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29
Q

Streptococcus viridans

A

Pen G 12-20 M units IV Pen G for 2 weeks (4 weeks if alone) + Gentamycin 1mg /kg q8

30
Q

Enterococcal endocarditis

A

Pen G/ Ampicillin + Gentamicin - Pen G 20M units or Ampicillin 12g IV + Gentamicin for 6 weeks

31
Q

Meningococcal

A

Penicillin

32
Q

Gonococcal

A

Ceftriaxone

33
Q

Staphylococcal Infections MRSA

A

Penicillinase producing organism; resistant to Penicillin; Vancomycin, Linezolid, Daptomycin Trimethoprim-Sulfamethoxazole, Doxycycline, Clindamycin

34
Q

10, 20 & Latent Syphilis < 1 year duration

A

Pen G Procaine 2.4M units/day IM + Probenecid for 10 days

35
Q

Late latent syphilis, neurosyphilis, CV syphilis

A

Pen G 20M units for 10 days

36
Q

Congenital Syphilis

A

Aqueous Pen G 50,000/kg in 2 divided doses or Procaine Pen G 50,000/kg OD for 10 days

37
Q

Treatment for Jarisch-Herxheimer reaction

A

Aspirin - Therapy w/ Penicillin should NOT be discontinued

38
Q

In Jarisch-Herxheimer reaction, Several hours after the 1st injection of penicillin manifestations

A

chills, fever, headache, myalgias, and arthralgias

39
Q

Actinomycosis

40
Q

Diphtheria

A

Pen G -Pen G eliminates the carrier state Pen G 2-3M units/day for 10-12 days

41
Q

Clostridial Infections (Gas Gangrene)

A

Pen G agent of choice as adjunct to antitoxin

42
Q

Fusospirochetal Infection (Trench mouth)

A

Pen V 500mg q6

43
Q

Rat-bite fever (Spirillum minor, Stretobacillus moniliformis)

A

Pen G – therapeutic agent of choice

44
Q

Listeria monocytogenes

A

Pen G & Ampicillin + Gentamicin

45
Q

Lyme disease : early disease

A

Tetracycline

46
Q

Lyme disease: Severe

A

Pen g or 3rd gen cephalosporin

47
Q

Penicillinase-resistant penicillins

A

Oxacillin, Cloxacillin, Dicloxacillin, Nafcillin

48
Q

most active of the penicillinase-resistant penicillins

49
Q

Treatment of staphylococcal meningitis

50
Q

MRSA - resistant to:

A

Resistance to penicillinase-resistant penicillins & cephalosporins

51
Q

MRSA: Hospital Acquired

A

resistant to aminoglycosides, tetracyclines, erythromycin, & clindamycin

52
Q

MRSA: Community Acquired

A

resistant to macrolides Vancomycin (drug of choice) + Rifampin

53
Q

MRSA: Drug of Choice

A

Vancomycin (drug of choice) + Rifampin

54
Q

AMINOpenicillins

A

Ampicillin, Amoxicillin, & their Congeners

55
Q

Enterobacteriacea (E. coli)

A

Ampicillin + Sulbactam (β-lactamase inhibitor) Amoxicillin + Clavulanate

56
Q

Shigellosis

A

Amoxicillin less effective than Ampicillin for Shigellosis

57
Q

Salmonella

A

Ampicillin high dose

58
Q

Tx use of Aminopenicillin

A
  1. Upper Respiratory 2. UTI 3. Meningitis 4. Salmonella infection
59
Q

ANTI-PSEUDOMONAL penicillins

A

Carboxypenicillins (Carbenicillin, Ticarcillin) Ureidopenicillins (Mezlocillin, Piperacillin)

60
Q

supplied as disodium salt; CHF results from excessive Na+

A

Carbenicillin

61
Q

Broadest antibacterial spectrum of the penicillins

A

Piperacillin + Tazobactam (β-lactamase inhibitor )

62
Q

UNTOWARD REACTIONS TO PENICILLINS

A
  • Hypersensitivity Reactions - Bone marrow depression - Granulocytopenia - Hepatitis (Oxacillin, Nafcillin) -Pain, Sterile Inflammatory reactions at IM site
63
Q

first source isolated in 1948 by Brotzu from the sea near a sewer outlet off the Sardinian coast

A

Cephalosporium acremonium

64
Q

Mechanisms of Bacterial Resistance: Cephalosporin

A

inability of the antibiotic to reach its sites of action * alterations in the penicillin-binding proteins (PBPs) – antibiotics bind to bacterial enzymes (β-lactamases) that can hydrolyze the β-lactam ring and inactivate the cephalosporin

65
Q

2nd Generation Cephalosporin

65
Q

1st Generation

66
Q

3rd gen

67
Q

4th gen cephalosporin

68
Q

Carbapenems

A
  • Imipenem
  • Meropenem
  • Doripenem
  • Ertapenem
  • Aztreonam
  • Broader spectrum of activity
  • Binds to Penicillin-binding Proteins
  • Disrupts bacterial cell wall synthesis
  • Death of susceptible microorganisms
  • Very resistant to hydrolysis by most β-lactamases
69
Q

β-LACTAMASE INHIBITORS

A
  • CLAVULANIC ACID
  • SULBACTAM
  • TAZOBACTAM

Pharmacology (4 decks)

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