Mechanisms of Action of Abs Flashcards

1
Q

What is Pharmacokinetics?

A

Encompasses all the ways that the body manipulates a drug

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2
Q

What are the ways the body manipulates the drug?

A

Absorption
Distribution
Metabolism
Excretion

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3
Q

What is Pharmocodynamics?

A

Describes biochemical and physiological effects of the drug and its mechanism of action on the bacteria

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4
Q

What is a Bacteriostatic?

A

Antimicrobial agents that INHIBIT the growth/reproduction of the infecting agent
BUT do not actually kill it

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5
Q

What are some examples of Bacteriostatics? (6)

A
Ma-cro-lids --> (E-ry-thro-my-cin)
Clin-da-my-cin
Sulfa-me-thox-a-zole
Tri-me-thro-pin
Te-tra-cy-clins
Chlo-ram-phe-ni-col
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6
Q

What is a Bacteriocidal?

A

Antimicrobial agent that is capable of causing IRREVERSIBLE damage/death to the organism

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7
Q

What are some ex of Bacteriocidals? (5)

A

Beta-lactam Abt –> (Penicillins and Ce-pha-la-sporins)
Va-co-my-cin
Amino-gly-co-sides –> (Gen-ta-my-cin)
Fluo-ro-qui-no-lones (Ci-pro-flox-a-cin)

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8
Q

What factor affects wether a drug exhibits bacterio -static or -cidal?

A

It is the antimicrobial concentration at the site of action

ATM may be -static at low [C], but -cidal at high [C]

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9
Q

What is Minimal Inhibitory Concentration?

A

Minimal amount of antimicrobial that will inhibit the visible growth of a microorganism after overnight incubation

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10
Q

What are broad spectrum Ab?

A

One that is active against a wide range of bacteria (gram +/-)
Used priorly to ID’ing the causative bacteria

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11
Q

What are narrow spectrum Ab?

A

ACtive against a select group of baterial types

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12
Q

What are the FIVE mechanisms of action, that Abs use to inhibit or kill bacteria?

A

Interference with cell wall synthesis (MOST COMMON)
Interference with protein synthesis
Interference with cytoplasmic mem function
Interference with nucleic acid synthesis
Interference with metabolic PW

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13
Q

What do most agents in the “inhibitors of cell wall synthesis” interfere with?

A

Peptidoglycan synthesis and murein assembly

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14
Q

What agents are included in “inhibitors of cell wall synthesis”?

A

Beta-lactam Abs

Glycopeptides

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15
Q

What are the Beta-lactam ABs? (5)

A

Penicillins
Cephalosporins
Monobactams
Carbapenems

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16
Q

What is the mechanism of action of Beta-lactam Abs?

A

Bind at active site of the transpeptidase En that cross-links the peptidoglycan strands - IRREVERSIBLY inhibits En
–>Formation of cell wall is prevented

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17
Q

What are the four generations in cephalosporin?

A

Each generation exhibits increased spectrum of activity as well as increased RESISTANCE to destruction by
Beta-lactamase En’s

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18
Q

What are Monobactams active against?

A

Aerobin gram (-) BACILLI

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19
Q

What are Carbapenems active against?

A

All pathogenic organisms ans resistant to destruction by the extended spectrum B-lactamses (ESBL’s)

20
Q

What are glycopeptides (vancomycin)?

A

They are another type of antimicrobials that interfere with cell wall synthesis

21
Q

How are glycopeptides inhibitors of cell wall synthesis?

A

They act by BINDING to the D-alanyl-D-alanine residues – preventing the cross linking of the peptidoglycan sheets

EFFECTIVE ONLY AGAINST GRAM (+)

22
Q

How is Fosfomycin an inhibitor of “cell wall” synthesis?

A

Inhibits phos-pho-enel pyruvate –> halting MURAMIC ACID synthesis (outside of acid-fast bacteria)

23
Q

What are the 3 main mechanisms in which “agents of the inhibitors of protein synthesis” inhibit protein synthesis?

A

1- Interfere with the formation of the 30S initiation complex (mRNA, 30S, tRNA)
2- Interfere with the formation of the 70S ribosome (30S initiation complex and 50S ribosome)
3- Block elongation process of assembling A.A’s into polypeptides

24
Q

What are the main agents in this group? (6)

A
Aminoglycosides
Linezoid
Macrolids
Lincosamides
Chloramphenicol
Tetracyclines
25
What do aminoglycosides do?
Bind to the 30S ribosome and change its shape -->inhibits protein synthesis by causing a misreading of mRNA BACTERIOCIDAL
26
What do Linezoids do?
Block translation of the initiation complex by binding to the 23S portion of the 50S subunit BACTERIOSTATIC
27
What do Macrolids do?
Bind to 23S rRNA molecule (in 50S subunit) -->Block exit of growing polypeptide chain BACTERIOSTATIC
28
What do Lincosamides do?
Bind to 50S Disrupt protein synthesis by interfering with the transpeptidation reaction -->inhibits early chain elongation BACTERIOSTATIC
29
What do Chloramphenicals do?
Binds to residues in 23S (on 50S) Preventing peptide formation BACTERIOSTATIC
30
What do Tetracyclines do?
Block attachment of the tRNA to the 30S ribosome subunit Inhibitors of the codon-anticodon interaction Can inhibit protein synthesis in both 70S and 80S BACTERIOSTATIC
31
What agents interfere with cytoplasmic mem func?
Polymyxins Bacitracin Anti-fungals
32
How do Polymyxins do it?
With cationic detergent-like activity
33
How do Bacitracin do it?
Disrupt cytoplasmic membranes
34
How do anti-fungals do it?
Alteration of sterol structure and function
35
How is nucleic acid synthesis inhibited by agents? (3)
They interfere with DNA They interfere with RNA They are nucleoside anologs
36
What are the agents that interfere with DNA? (2)
Quinolones/Fluoroquinolones | Metronidazole
37
What do Quinolones/Fluoroquinolones do?
inhibit DNA gyrases or topoisomerases (required for supercoiling) BACTERIOCIDAL
38
What do Metronidazoles do?
Cause metabolic cytotoxic byprodcuts -->disrupt DNA BACTERIOCIDAL
39
What are the agents the agents that interfere with RNA? (2)
Rifampin | Bacitracin
40
How does Rifampin do it?
Binds to DNA-dependent RNA polymerase -->inhibiting initiation of RNA synthesis BACTERIOCIDAL
41
How does Bacitracin do it?
inhibits RNA transcription | BACTERIOCIDAL
42
What are the nucleoside analogs for viruses?
Acy-clovir
43
What are the nucleoside analogs for retroviruses?
Zido-vu-dine
44
What are the agents that can cause interference in the metabolic PW? (5)
Sulfonamides and Dapsone Trimethropim Trimethropim and Sulfamethoxazole
45
How does Sulfonamides and Dapsone do it?
Sulfonamides is a BACTERIOSTATIC and Dapsone in a BACTERIOCIDAL Compete with p-aminobenzoic acid (PABA) -->Prevent synthesis of folic acid
46
How does Trimethropim do it?
inhibits dihydrofolate reductase -->preventing synthesis of folic acid BACTERIOSTATIC
47
How does Trimethropim and Sulfamethoxazole do it?
Drugs used in combination (BACTRIM) Are synergetic in activity BACTERIOCIDAL