Pharm - Inhibitors Of Cell-Wall Synthesis Flashcards

0
Q

What is the weakest bond in the lactam and what is special about it?

A

The bond between the nitrogen and the carbonyl group, which is the working site of B-lactamases!

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1
Q

Which Cell-Wall synthesis inhibitor is not a lactam?

A

Vancomycin

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2
Q

All lactams have 3 mechanisms of action..

A

1 Bind PBPs
2 Inhibit transpeptidation
3 Inhibit crosslinking

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3
Q

All lactams can be disabled my 3 mechanisms of resistance..

A

1 Penicillinases
2 Structural change in PBPs (MRSA) - use vancomycin!
3 Change in porin structure

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4
Q

On what spirochete is the the narrow spectrum Penicillin G and Penicillin V effective?

A

Treponema pallidum which causes syphilis.

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5
Q

Two broadspectrum, betalactamase sensitive penicillins?

A

Amoxicillin and ampicillin are used against:
1 gram + cocci(not staph)
2 gram - E. coli, H. influenzae, H. pylori
3 Borrelia

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6
Q

Clavulanic acid, sulbactam, tazobactam are …………

A

Clavulanic acid, sulbactam, tazobactam are beta-lactamase inhibitors

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7
Q

Two penicillins that are eliminated largely in bile?

A

Nafcillin and oxacillin are more lipid soluble and are therefore excreted primarily in bile.

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8
Q

Two penicillins where you will not have to adjust the dose in people with decreased renal function?

A

Nafcillin and Oxacillin - excreted in bile.

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9
Q

What is Jarisch - Herxhermer reaction?

A

Treatment of syphilis with antibiotics that destroys the Treponema and releases it into the blood stream - causing systemic infection.

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10
Q

Cephalosporin mechanism of action?

A

Like penicillins

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11
Q

Two first generation cephalosporins? Area of use?

A

Cefazolin and cephalexin. Used in surgical prophylaxis because of their long half-life that can protect against entry of bacteria from skin.

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12
Q

Second generation cephalosporin: first cephalosporin to cross the BBB?

A

Cefuroxime. Used in meningitis.

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13
Q

Cephalosporins used in empirical management of sepsis and meningitis?

A

Third generation cephalosporins: esp. ceftriaxone.

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14
Q

Third generation cephalosporin do not work against?

A

LAME

Listeria, Atypicals, MRSA & Enterococci

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15
Q

To treat MRSA we use….

A

Vancomycin

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16
Q

Two cephalosporins that are eliminated primarily through bile?

A

Cefoperazone and ceftriaxone.

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17
Q

What to use in case of allergies to lactams?

A

macrolides or aztreonam(only gram neg rods - Pseudomonas)

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18
Q

Most potent lactams?

A

Imipenem and meropenem

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19
Q

What is the reason for the high potency of imipenem and meropenem?

A

Resistant to beta - lactamases.

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20
Q

imipenem must be coadministered with ……….

A

cilastatin.

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21
Q

What i Cilastatin?

A

A renal dehydropeptidase inhibitor.

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22
Q

Aztreonam mechanism of action?

A

Same as cephalosporins and penicillins.

23
Q

We use aztreonam to treat against ………

A

gram negative rod ONLY

24
Q

Drug that have no cross - allergenicity with penicillins and cephalosporins?

A

Aztreonam - working against gram negative rods.

25
Q

Vancomyocin mechanism of action?

A

binding at D-ala-D-ala Muramyl pentapeptide that interferes with transpeptidatioin(elongation of peptidoglycan cell wall)

26
Q

Enterococci mechanism of resistance against vancomycin?

A

changing the terminal D-ala with a D-lactate, thereby removing the binding-target used by vancomycin.

27
Q

VRE and VRSA are?

A

Vancomycin Resistant Enterococcus & Vancomycin Resistant Staphylococcus Aureus.

28
Q

Two drugs used against VRE and VRSA?

A

Linezolid and Streptogranins

29
Q

Describe host determinants for choice of drug?

A
  • history of drug reactions
  • site of infection
  • renal status
  • hepatic status
  • immune status
  • pregnancy/lactation
  • metabolic abnormalities
30
Q

Group of bacteria that are particularly suceptible to penicillins?

A

gram positives

31
Q

Common beta-lactamase producing organisms include..?

A

S. aureus, E. coli, Salmonella, Pseudomonas, N. gonnhore, Bacillus, Proteus, Bacteroides spp.

32
Q

nafcillin, oxacillin and clidoxacillin primary target?

A

S. aureus. NOT MRSA

33
Q

Name two anti-pseudomonal ab and their target organisms?

A

Ticarcillin/piperacillin kills pseudomonas, E. coli, Salmonella, Proteus, Enterobacter and Klebsiella.

34
Q

Amoxicillin + clavulanic acid =

A

Augmentin

35
Q

Clavulanic acid moa?

A

irreversible inhibitor of Beta-lactamases

36
Q

Hypersensitivity reactions are seen in how many patients?

A

10% is the answer to this question. 10 % is also the answer to how much I want to stay in the czytelnia at the present moment.

37
Q

Endocarditis prophylaxis is indicated in…….

A
  • GI surgery
  • Pulmonary surgery
  • Major dental surgery
  • Genitourinal surgery
38
Q

What drugs are used in prophylactic treatment of endocarditis?

A

amoxicillin and ampicillin. IF hypersensitive to penicillins use clindamycin or azithromycin.

39
Q

Describe the structure of sephalosporins

A

7-aminocephalosporic acid nucleus + B-lactam ring = BOOM!

40
Q

Cephalosporin mechanism of action?

A

same as penicillins

41
Q

General characteristics of 3rd and 4th generation cephalosporins?

A
  • Parenteral administration
  • B-lactamase resistant
  • penetrates CNS
42
Q

The newer cephalosporins are increasingly effective against what?

A

penicillinases/B-lactamases

43
Q

Name a drug that decrease the secretion of cephalosporins

A

Probenecid

44
Q

3rd generation cephalosporins are increasingly effective against……

A

gram negs mahn! I be talkin’ bout dem gram negs

45
Q

Adverse effects cephalosporins?

A
  • hypersensitivity
  • disulfiram-like effects
  • bleeding(vitamin K)
  • nephrotoxicity
  • Clostridium Difficile Colitis
46
Q

Important hypersensitivity association w/ azetreonam =

A

no cross-reaction with penicillins and cephalosporins

47
Q

3 most important carbapenems?

A

imirenem
meroprenem
azetreonam

48
Q

Imipenem + cilastatin =

A

Primaxin

49
Q

Cilastatin mechanism of action?

A

inhibitor of of renal dehydropeptidase I, which inactivates imipenem.

50
Q

Carbapenem target organisms?

A
  • penicillinase producing Staph aureus
  • E .coli
  • Pseudomonas
  • H. influenzae
51
Q

Vancomycin + aminoglycosides relationship =

A
  • synergistic effect

- adverse effects include ototoxicity + nephrotoxicity

52
Q

Vancomycin and CNS?

A

penetrates only during inflammation

53
Q

Vancomycin and hypersensitivity?

A
  • slow IV infusion - rapid infusion may precipitate anaphylaxis(red neck)
  • no cross reaction with penicillins or cephalosporins
54
Q

Bacitracin general picture?

A
  • gram positives
  • inhibit reuse and synthesis on N-AM
  • Only topical administration
55
Q

Cycloserine general picture?

A
  • inhibit alanine racemase

- mycobacteria and gram negatives

56
Q

Skin lesions with large number of gram positive cocci. Administer?

A

Nafcillin - Nafcillin is resistant to penicillinases and is effective against most S. aureus and common streptococci