Antibacterial Drugs Inhibitors Of Cell Wall Synthesis- Umd Medical School

Front 1

When are inhibitors of cell wall synthesis effective?

Back 1

Only when the cell is growing during the log phase of bacterial growth.

Front 2

Cycloserine Inhibts cell wall synthesis by?

Back 2

Inhibiting UDP-acetylmuramyl pentapeptide (the Park nuceotide). Does this by acting as a competitive inhibitor of the enzymes responsible for dipeptide formation.

Front 3

Vancomycin inhibits cell wall synthesis by?

Back 3

Binding with high affinity to D-alanyl-D-alanine terminus of cell wall precursur protein stoping realase of bactoprenal carrier stopping peptid. synthesis. Does this by inhibiting the polymerization or the transglycosylase reaction.

Front 4

Bacitracin inhibits cell wall synthesis by?

Back 4

Preventing the dephosphorylation of the bactoprenol carrier, this is the essential step for continued elongation of cell walll and regeneration of bactoprenol carrier.

Front 5

Beta-Lactam antibiotics (such as penecillins, cephalosporins and others do what???

Back 5

They bind to penicilin binding proteins which are transpeptidases are essential for cross linking peptidogylcan. They do this by occupying D-Alanyl-D-alanine

Front 6

Beta-lactamse (penicillinase) inhibitors aka Clavulanic Acid do what?

Back 6

This drug stops beta lactamase or pencillanase from working and keeps the beta lactam ring intact, which then inhibits the cross-linking of pepti. strands.
*******Clavulanic acid is combined with penicillin to be more effective

Front 7

Clavulanic acid inhibits which classes of Beta Lactamases?

Back 7

Class A and D

Front 8

Intrinsic penicillin resistance?

Back 8

Since penicillin is only affective against multipyling bacteria any stationary bacteria have an intrinsic resistance.

Also some gram negative cells keep penicillin from sites for action on the peptiglycan by having outer membranes and LPS (lipopolysaccharides)

Front 9

2 Types of Acquired Resistance?

Back 9

Inactivation of the Drug
Drug Target Change

Front 10

Aquired Resistance Inactivation of drug details?

Back 10

Most common type of acquired resistance occurs to penicillinase (beta-lactams) so that it is not inhibited by penicillin and can cleave beta lactam ring.
2. Also cause of penicillin amidase which degrades drug.

Front 11

Acquired resistance because drug target alteration. Details?

Back 11

Bacteria Produce altered penicillin binding proteins so that penicillin's affinity for them decreases so they bond less.

Front 12

Broad Spectrum Penecillins??

Back 12

Aminopenicillins,
Anti-pseudomal penicillins

Front 13

Penicillins work in which spectrums?

Back 13

Narrow and extended

Front 14

Penicillins differ based on 4 characteristics, what are they?

Back 14

Oral availability, spectrum of action, penetratin into CNS, penicillinase resistance

Front 15

4 Major Groups of Penicillins are?

Back 15

1. Penicillin V and G
2. Penicillinace Reistant Penicillins
3. Aminopenicillins
4. Anti-psuedomonal Penicillins

Front 16

Penicillin G and Penicillin V characteristics include?

Back 16

1. Highly active against G+ cocci
2. Penicillinase Sensitive
3. Repository preperation of Pencilin G
A formulation of penicillin G is slow to absorb and can achieve prolonged levels of the drug.

G is absorbed well after oral taking V is

Front 17

Penicillinase Resistant Penicilins incude what? and Why are they special?

Back 17

Dicloxacillin, oxacillin, Nafcillin.
Less potent antimicrobial activity against bacteria sensitive to Pen G, but drugs of choice for penicillinase producing S. aureus.

Dicloacillin and oxacillin good taken orally.
Nafcillin is variable when taken orally.

Front 18

Aminopenicillins include what? and why are they special?

Back 18

Ampicillin and Amoxicillin.
Extends spectrum of penicillins to include Gram (-) bacteria.

Ampicillin is good taken orally
Amoxicillin is excellent taken orally.

Front 19

Anti-pseudomoal penicillins include what? And do what?

Back 19

Ticarcillin and piperacillin (both are poorly abosbed when taken orally, so they aren't given.)
Broad activity against (-) G bacteria

Front 20

Penicillin and Beta lactamose inhibitors are?? Downsides/side effects/ benefits

Back 20

Drugs that include clavulanic acid.
1.Amoxicilin-clavulanic acid
2. ticarcillin-clavulanic acid
OFten leads to frequent diarhea when combined, sometimes nausea and abdominal pain. Very useful against amoxicillin resistant organisms and it expands the spectrum of amoxicillin.

Front 21

Abosrbtion of penicillin G is variable why? What characteristics make it a unique antibiotic? Who should take it most?

Back 21

Because it is acid labile, approximately 1/3 of pen. G is absorbed in the GI tract it is better absorbed in new borns and those over 60 because of decreased Gastric acid.

Is unique because it creates low but persistent levels of penicillin in the body, this is effective against certain diseases like Group A beta hemolytic strep or syphilis.

Front 22

Distribution and excretion of pen G?

Back 22

Rapid in kidney mainly by tubular secretion. (may lead to dose adjustment)

Not activated by metabolism so still active in urine.

Only enters cerebrospinal fluid when meninges are inflamed.

Front 23

Penicilin G, absorbtion after oral administratian? Resistance to Penicillinase? Useful antimicrobial Spectrum?

Back 23

Variable (poor)
No
Streptococcus species, Neisseria species, many anaerobes, spirochets, others

Front 24

Penicillin V, absorbtion after oral administratian? Resistance to Penicillinase? Useful antimicrobial Spectrum?

Back 24

Good
No
Streptococcus species, Neisseria species, many anaerobes, spirochets, others

Front 25

Pencillinase Resistant Penicillins, Oxaccilin.....
absorbtion after oral administratian? Resistance to Penicillinase? Useful antimicrobial Spectrum?

Back 25

Good
Yes
Staphyloccocus aureus

Front 26

Pencillinase Resistant Penicillins, dicloxaccilin.....
absorbtion after oral administratian? Resistance to Penicillinase? Useful antimicrobial Spectrum?

Back 26

Good
Yes
N/a

Front 27

Pencillinase Resistant Penicillins, Nafcillin.....
absorbtion after oral administratian? Resistance to Penicillinase? Useful antimicrobial Spectrum?

Back 27

Variable
Yes

Front 28

Aminopenicillins....
Ampicillin
absorbtion after oral administratian? Resistance to Penicillinase? Useful antimicrobial Spectrum?

Back 28

Good,
No
Extends spectrum of penicillin to include Haemophilus influenzae Proteus mirabilis, escherichia coli, Neisseria species

Front 29

Aminopenicillins...
Amoxicillin
absorbtion after oral administratian? Resistance to Penicillinase? Useful antimicrobial Spectrum?

Back 29

EXCELLENT!!!
NO
Extends spectrum of penicillin to include Haemophilus influenzae Proteus mirabilis, escherichia coli, Neisseria species

Front 30

Antipseudomonal Penicilins..

Ticarcillin

absorbtion after oral administratian? Resistance to Penicillinase? Useful antimicrobial Spectrum?

Back 30

Poor (not given orally)
No
Extends spectrum of amoxicllin to include Pseudomonas speciase, enterobacter species and Proteus

Front 31

Antipseudomonal penicillins

Piperacillin

absorbtion after oral administratian? Resistance to Penicillinase? Useful antimicrobial Spectrum?

Back 31

Poor (not given orally)
No
Pseudomonas species,
enterobacter species, many Klebsiella

Front 32

Hypersesitivity (allergy) to penicillins, BIGGEST TOXICITY complicates 0.7-4.0 treatment courses.

Immediate Response (2-30 min) Likely Causitive antibody?? Manifestations?/

Back 32

Ige or IgG
Anaphlaxis-diffuse or organ specific (cardiac)
Asthma, urticaria,
Laryngeal Edema

Front 33

Hypersesitivity (allergy) to penicillins, BIGGEST TOXICITY complicates 0.7-4.0 treatment courses.

Accelarated (1 to 72 hours) Likely Causitive antibody?? Manifestations?/

Back 33

IgG
Urticaria, laryngeal edema, asthma, local inflammatory reactions

Front 34

Hypersesitivity (allergy) to penicillins, BIGGEST TOXICITY complicates 0.7-4.0 treatment courses.

Late (more than 72 hours)
Likely Causitive antibody?? Manifestations?/

Back 34

IgM and other antibodies

Commonly causes
Urticaria-- Exantham, Fever, Arthralgia
Hemolysis-- granulocytopenia, interstitial nephritis, eosinophilia
Rarely causes
Acute renal insuffciency
Thrombocytopenia

Front 35

How does penicillin cause an allerigic reaction in your body?

Back 35

Pen. combines with our bodies proteins to form a hapten-protein complex that stiumulates immune response and results in production of antibodies to the supposed antigen.

Front 36

Major antigenic determinants of penicillin allergic reaction?

Back 36

Penicillin or penicillenic acid react with protein to form penicilloyl derivatives of tissue proteins. 95% of hapten ends up as a major antigenic determinent (penicilloyl-protein).

Front 37

Minor antigenic determinants in allergic reaction?

Back 37

Other reactive derivatives of penicillin react with proteins to cause antibody response. Major cause of anaphylactic reactions.

Front 38

What is the major antigenic determinant of a penicillin allergic reaction?

Back 38

penicilloyl-protein