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Anti-microbials > Beta Lactams > Flashcards

Beta Lactams Flashcards

1
Q

List the natural antibiotics

A

Penicillin, tetracycline, cephalosporin, streptomycin

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2
Q

List the synthetic antibiotics

A

Fluoroquinolone, sulfonamides

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3
Q

List the bacteriostatic drugs

(T..)

A

TCS=
Tetracycline
Chloroamphenicol
Sulphonamides

Concentration dependent bacteriostatic drugs:
Macrolides, Tetracyclines, clindamycin

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4
Q

List the bactericidal drugs

A

PICAR=
Penicillin
Ioniazid
Cephalosporin
Aminoglycosides
Rifampicin

Concentration-dependent:
Metronidazole
Aminoglycosides
Quinolones

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5
Q

T…for bacterisostatic

Differentiate between time-dependent and concentration-dependent efficacy

A

Time-dependent:
- Concentration should be above the MIC for a long period of time
- Slow bactericidal action
- Moderate post-antibiotic effect
- Penicillins and Beta Lactams

Concentration-dependent
-Outcome dependent on the peak concentration relative to the MIC
- Strong post-antibiotic effect
Bactericidal: MAQ= Metronidazole, aminoglycosides and quinolones
Bacteriostatic: MTC= Macrolides, tetracyclines and clindamycin

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6
Q

Classify the antibiotics into 3 categories

A
  1. Inhibition of cell wall synthesis
  2. Inhibition of ribosomal protein synthesis
  3. Inhibition of nucleic acid synthesis
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7
Q

List the drugs part of the inhibition of cell wall synthesis

A
  1. Penicllins
  2. cephalosporins or cephamycins
  3. Monobactams
  4. Carbapenems
  5. Glycopeptides
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8
Q

Describe the mechanism of action of penicillin

A
  1. Penicillin interferes with the transpeptidation reactions. The cell wall is comprised of NAM and NAG cross-linked together by D alanine, synthesis of cell wall
  2. Interference with transpeptidation can result in rupture due to osmotic pressure
  3. Loss of cell wall integrity, cell lysis and death
  4. Bactericidal, time-dependent killing
  5. Binds to the penicillin-binding protein
  6. Inactivate an inhibitor of autolytic enzyme in the cell wall
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9
Q

Classify penicllins

A
  1. Narrow spectrum beta lactamase sensitive
  2. Broad spectrum beta lactamase sensitive
  3. Beta lactamase resistant
  4. Extended spectrum
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10
Q

List the penicillin groups and the antimicrobial activity

A
  1. Benzyl Penicillin/Penicillin G
    - Streptococci penicillin
    - Gram + with some gram -
    - Little activity against gram - rods
    - Tx. of choice for many infections
    - Streptococci and pneumococcal pneumonia
    - Endocarditis
    - Anthrax, syhillis, clostridia and diptheria
    - Meningococcal meningitis
  2. Penicllin V:
    - less potent than Penicllin G
    - Oral preparation
    - Strep Pharyngitis
  3. Benzathain Penicllin
    - Strep Pharyngitis
    - syphillis
  4. Procain Penicillin
    - Gonorrhea
    - Pneumococcal pneumonia
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11
Q

Discuss the broad spectrum beta-lactamase sensitive drugs
- Examples
- Antimicrobial activity
- Clinical use of ampicillin
- Side effects
- use of beta lactamsae inhibitors

A

e.g. Amoxycillin, ampicillin
SESH:
Some gram -ve bacteria
Enterococci
Streptococci
H. Influenza
- Ineffective against P. aeruginosa
- Spectrum similar to benzyl penicillin but greater activity against gram -ve bacteria
- Ampicllin= Meningitis, oral abscess, pneumonia
- Associated with C. difficile
- Comnination with beta lactamase inhibitors to protect beta lactamase
1. Clauvanic acid + Amxoycillin= co-amoxyclav
2. Ampicillin + Salbactam= Ampicillin-Salbactam

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12
Q

describe the beta-lactamase resistant penicillins
- examples
- Antimicrobial activity

A
  • Antistaphylococcal penicllins
  • Dicloxacillin, Cloxacillin, Oxacillin
  • Limited to staph and strep infections
  • Not effective against anaerobic bacteria, enterococci and gram -ve rods or cocci
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13
Q

C for examples….C in speCtrum

Describe the Extended Spectrum
- examples
- Antimicrobial activity
- Beta lactamse inhibitors

A
  • Anti-pseudomonal penicllins
  • CAPT= Cabernicillin, Azolocillin, piperacillin and ticarcillin
  • Spectrum similar to broad spectrum penicillins plus pseudomas and proteus species
  • Beta lactamase inhibitors can be combined:
    1. Clauvanic acid + Ticarcillin
    2. Salbactam + piperacillin
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14
Q

Discuss the pharmacokinetics of penicillins

A
  1. well absorbed orally
  2. Interference with food. Need to eat 1-2 hours before or after
  3. Benzyl penicillin IV> IM, local irritation at site
    Benzathaine and procaine= IM
  4. Excretion via the kidneys
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15
Q

What are the adverse reactions with penicillins?

What do males want to alwasys do?

A

SHAG=
Super infections: Pseudomonas, staph, yeasts. Pseudomembranous collitis (treated with Vancomycin or metronidazole)

Hypersensitivity Reactions:
Rash
Urticaria
Angioedema
Acute anaphylactic shock
Interstitial Nephritis

Alteration to the GIT bacterial flora

GIT disturbances: Nausea, vomiting, diarrhoea

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16
Q

Discuss the clinical uses of penicillin in dentistry

A
  1. Orofacial infection= Amxoycillin + Penicllin V
  2. Periodontal infection= Amoxycillin + Metronidazole
  3. Beta lactamase producing: Beta lactamase resistant, or erythromycin/ clindamycin
17
Q

Explain the antimicrobial activity, characteristics and MOA of cephalosporins and cephamycins

A
  • Similar MOA to penicllins
  • More stable against beta lactamses except for strains of E.coli and Kliebsellia
  • Not effective against enterococci ***
  • Time dependent killing
18
Q

Discuss the generations of cephalosporin, examples, antimicrobial activity, clinical uses

A

1st generation:
e.g. Cefazolin, Cephalexin
- gram + cocci= Streptococci, methicillin-sensitive staph aureus
Some gram - bacilli
- Klebsiella pneumoniae and proteus mirabilis
Clinical uses: Oral agents for urinary tract infections
Cefazolin: Surgical prophylaxis, Alternative to antistap penicllin in allergic patients (I.e. beta lactamase resistant penicillin)

2nd Generation:
e.g. Cefaclor, Cefuroxime
- First generation coverage (Staph and strep, kliebsellia and proteus–(extended spectrum) plus H. Influenza (Broad spectrum beta lactamase sensitive)
- Extended gram -ve coverage
clinical uses: sinusitis, LRTI, Otitis

3rd generation:
Cefixime, Ceftazidime, Cefttriaxone
- Second generation PLUS expanded gram negative coverage
- Greater stability against beta-lactamases
- Greatest activity against P. aeruginosa
‘antipseudomonal cephalosporins’ *** Ceftazidine especially
- Less active against staphylococci
Clinical uses: Meningitis, pneumonia and sepsis
(Pneumonia and meningtis was also covered by ampicillin)

4th Generation:
e.g. cefepime
- More resistant against Beta-lactamases
- Good activity against P. aerginosa, staph aureus, S. Pneumonia enterbacteraciea e.g. E.coli
- High activity against Nesseria and Haemophillus
Skin and soft tissue infections

5th Generation
Ceftaroline Fosamil
- MRSA

19
Q

sporeins = sperm

Discuss the adverse effects of cephalosporins

A

SHAG=
Super infections= canida albicans
Hypersensitivity reations
Rare ADVERSE effects: nephrotoxicity, thrombocytopenia
GIT: Diarrhoea

20
Q

Explain how bacteria resist Penicillins and Cephalosporins

A
  1. Lack of a cell wall e.g. mycoplasma
  2. Alteration in the permeability of the cell wall (gram -v)
  3. Alteration of the penicillin binding site (methicillin resistant staph)
  4. Efflux pump
  5. Production of beta lactamases e.g. Staphylococci
21
Q

Carbapenems

Explain the Carbapenems in terms of example, antibacterial coverage, characteristics, clinical uses, side effects and the diadvantage

A

e.g. imipenem
- Broadest spectrum of all the antibiotics
- gram + and gram - aerobic and anaerobic bacteria
- Effective against P aeruginosa **more potent than 3rd generation e.g. cefixime, ceftzaidine, cefttriaxone
- resistant to hydrolysis by beta-lactamases
- Acquired resistance uncommon
- Septecemia of renal origin, intra-abdominal infection and noscomial pneumonia (carba- carbohydrates =intrasabdominal)
- renal function impaired
Side effects: blood disorders, confusion, convulsion, allergic rxn
- Has to be given with cilastatin (prevents inactivation and toxicity) Inhibits dihypropeptidase i

22
Q

Discuss the characteristics of Meropenem and its advantage

A
  • This is a carbapenem
  • Similar to imipenem
  • Doesn’t have to be given with cilastatin
  • Not associated with nausea or convulsions
23
Q

Discuss the characterisitcs and MOA of vancomycin

A
  • glycopeptide, bactericidal
  • different site of action from beta-lactams
  • Inhibits transglycosylase—> prevents elongation and cross linking
  • Bactericidal against clostridia
  • effective against all strains of S. aureus
  • Gram + bacteria
24
Q

red deaf alibi

Discuss the clinical uses and side effects of vancomycin and an alternative agent

A
  • MRSA
  • Collitis
    -In combination with cephalosporins (meningitis)–> 3rd generation

Side effects:
Auditory damage
Allergic reactions
Red person syndrome- maculopapular rash

Metronidazole

Anti-microbials (8 decks)

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