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Pharmacology 2. A topics > 18. Cefalosporins, monobactams and carbapenems > Flashcards

18. Cefalosporins, monobactams and carbapenems Flashcards

1
Q

Structure of cephalosporins

A

Penicillins - 5 member ring (thiazolidine ring), cephalosporins - 6 member ring -› not as easy can be inhibited by beta-lactamase

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2
Q

Mechanism of action of cephalosporins

A

Same as in penicillins

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3
Q

Mode of action of cephalosporins

A

BACTERIACIDAL, time-dependent
+ PAE (postantibiotic effect) - 1-4 hours

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4
Q

Drug list of cephalosporins:

A

1 generation:
- cefazolin
- cefapirin
- cefalexin
- cefalonium
- cefadroxil

2 generation:
- cefuroxime

3 generation:
- ceftiofur
- cefovecin
- cefoperazone
- ceftriaxone
- cefotaxime
- ceftazidime

4 generation:
- cefepime
- cefquinome

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5
Q

Resistance of bacteria against cephalosporins

A

Same as in penicillins:
- ab ovo
- beta-lactamase production
- PBP-mutation

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6
Q

Antibacterial spectrum of 1st generation of cephalosporins:

A

Similar to amoxicilin.

Good activity against Gram+ bacteria
Gram—: NOT against lactamase producers, not good against anaerobic bacteria

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7
Q

Antibacterial spectrum of 2nd generation of cephalosporins:

A

Worse than 1st generation against Gram+ bacteria

Gram—: active against several lactamase producers! (E. coli, Salmonella, Klebsiella …)

Anaerobic bacteria: rarely

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8
Q

Antibacterial spectrum of 3d generation of cephalosporins:

A

Weak against Gram+ bacteria
Gram—: active against most lactamase producers and fastidious and anaerobic bacteria

+ Pseudomonas aeruginosa (cefoperazone, ceftazidime)

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9
Q

Antibacterial spectrum of 4th generation of cephalosporins:

A

Almost perfect
Good activity against Gram+
Gram—: most lactamase producers

Also 4th generation cephalosporins are more active (MICs are lower)

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10
Q

Pharmacokinetics of cephalosporins :

A

Absorption:
1,2 gen. - orally/parenterally
3,4 gen. - parenteral

Distribution:
1,2: not very good
3,4: pretty good

Metabolism
cefovecin, ceftiofur (3) - veeeeery long half-life

Excretion: kidney (exc.: cefoperazone, ceftriaxone (3) - through bile)

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11
Q

Side effects of cephalosporins

A
  • allergy (~5% cross allergy - 5% chance that if patient is allergic to penicillins it will be allergic to cephalosporins too)
  • dysbacteriosis
  • haematological (anaemia)
  • tissue irritation (depending on drug)
  • mild nephrotoxicity
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12
Q

Cefalexin

A
  • 1st generation
  • good against Staphylococcus
  • skin soft tissue infections: dermatitis, mastitis (Gram+)
  • orally
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13
Q

Cefazolin

A
  • 1st generation
  • main indication: pre- and postoperatic IV in case of long surgery (›1hour)
  • parenteral administration
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14
Q

Cephapirin

A
  • 1st generation
  • Staphylococcus caused mastitis
  • parenteral administration
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15
Q

Cefuroxime

A
  • 2nd generation
  • UTI, resp. Infections, otitis
  • oral/parenteral administration
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16
Q

Cefoperazone

A
  • 3d generation
  • good against Gram— caused mastitis (e.g. Enterobacteria)
  • good against Pseudomonas
  • excreted via bile (!)
17
Q

Ceftiofur

A
  • 3d generation
  • in large animals against almost everything - mastitis, resp. diseases, foot rot (Fusobacterium)
  • covers anaerobic bacteria too
  • long half-life
  • parenteral administration
18
Q

Cefovecin

A
  • 3d generation
  • oral cavity infections, UTI, dermatitis
  • long half-life
19
Q

Cefotaxime, ceftriaxone

A
  • 3d generation
  • can go through BBB -› meningitis, encephalitis, second choice in osteomyelitis (1 - clindamycin), second choice for Lyme-disease (1 - doxycyclin)
  • ceftriaxone is excreted via bile
20
Q

Cefquinome, cefepime

A
  • 4th generation
  • only for large animals
  • work good against almost everything
21
Q

General indications for cephalosporins

A
  • mastitis/metritis
  • dermatitis, soft tissue infections
  • resp. Infections (best - 3/4 gen)
  • UTI (if not excreted through bile like cefoperazone and ceftriaxone)
  • meningitis, encephalitis
  • preoperative, postoperative prophylaxis (cefazolin)
  • osteomyelitis (1st choice is clindamycin)
22
Q

What cephalosporins are effective against Pseudomonas aeruginosa

A
  • cefoperazone
  • ceftazidime
23
Q

Cephasporins ‹-› AMEG classification

A

3d and 4th gen. -› category B: restrict - CIA highest priority

1st and 2nd gen. -› category C: caution

24
Q

Monobactams

A
  • excellent activity against gram-
  • primary UTI

Aztreonam (parental)
Tigemonam (p.o)

category A (AMEG)

25
Q

Carbapenems

A

Meropenem
Imipenem

last resort antibiotics, highly active against all important known pathogenic bacteria

Category A: avoid

Pharmacology 2. A topics (16 decks)

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