Antibacterial agents Flashcards

(45 cards)

1
Q

List 5 ways bacterial resistance to antibiotics

A
efflux pump
decrease entry
altered target site
enzymatic degradation
Bypass pathways
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2
Q

Selective toxicity

A

affects microbes > hosts

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3
Q

Examples of selectivity toxicity

A

Folate metabolisms, protein/nucleic acid synthesis (ribosomes, gyrase), Cell walls, fungal cell membrane (cell wall diff structures)

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4
Q

Antibiotic spectrum (3)

A

Narrow
Extended
Broad

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5
Q

Narrow antibiotic

A

Gram + or -

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6
Q

Extended antibiotic

A

Gram + and -

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7
Q

Broad antibiotic

A

Gram + and - and atypical

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8
Q

Three categories of resistance

A

natural/intrinsic
escape
acquired

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9
Q

Natural/intrinisic resistance

A

lack drug targets

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10
Q

Escape resistance

A

Precursor still there. Drug stopped synthesis but source is not removed - important to surgically drain/remove precursors

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11
Q

Acquired resistance

A

Mutational (requires multiple steps/generations)
Plasmid mediated: Conjugation (physical contact), transduction (virus carrying resistance), Transformation (DNA from environment)

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12
Q

Drugs easily enter CSF

A

chloramphenicol
Sulfonamides - trimethoprim
Cephalosporins (3/4)
Rifampin - Metronidazole

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13
Q

Enter CNS with inflammation

A

Penicillins
vancomycin
ciprofloxacin
tetracycline

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14
Q

Enter CSF poorly

A

aminoglycosides
cephalosporins (1/2)
Erythromycin
Lindamycin

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15
Q

Cholesterol is in mammalian membrane as _______ is in fungal cell membran

A

ergosterol

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16
Q

Inhibition of synthesis of stage 1 cell wall

A

Alanine racemase: cycloserine; enolpyruvate transferase: fosfomycin

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17
Q

Inhibition of synthesis of stage 2 cell wall

A

D-ala-D-ala pentapeptide: Vancomycin; bactoprenol lipid carrier: bacitracin

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18
Q

Inhibition of synthesis of stage 3 cell wall

A

Transpeptidase: penicillins, cephalosporins, monobactams, carbapenems

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19
Q

inhibition of synthesis/damage to cell membrane

A

daptomycin, polymixin B

20
Q

Modification of synthesis or metabolism of nucleic acids

A

DNA gyrase: Fluoroquinolones
RNA pol: rifampin
DNA: metronidazole, nitrofurantonin

21
Q

Inhibition/modification of protein synthesis

A

30S: aminoglycosides (irrev), tetracyclines
50S: clindamycin, macrolides, chloramphenicol, treptogramins
Isoleucyl-tRNA synthetase: mupriocin

22
Q

Modification of intermediary metabolisms (ie. folate)

A

Dihydropteroate synthase: Sulfonamides

Dihydrofolate reductase: Trimethoprim

23
Q

bactericidal mechanisms

A

inhibition of cell wall synthesis
disruption of cell membrane function
interference with DNA function/synthesis

24
Q

Bacteriostatic mechanism

A

inhibition of protein synthesis (except aminoglycosides)

inhibitions of intermediary metabolic pathways

25
When to use bactericidal over bacteriostatics reasons (4)
1. severe infection 2. quickly/irreversible 3. impaired host defense 4. Not accessible to host immune system responses
26
example of altered targets
MRSA, s. pneumoniae, enterococci to b-lactam antibiotics (penicillin binding proteins) Enteroccci (VRE), staphylococci (VRSA) --> vancomycin (peptidoglycan side chain) S. aureus, pseudomonas to fluoroquinolones (DNA gyrase) Strep/staph/etnerococci to macrolides, clindamycin (50S methylation)
27
Examples of Enzymatic destruction
S. aureus, P. aeruginosa, bacteroides, enterococci to b-lactam antibiotic (b lactamase) Aminoglycosidesstaph/strepneisseria - chloramphenicol (acetyltransferase)
28
Examples of alternative resistant metabolic pathways
Streptococci to sulfonamides: over production of PABA or thymidine nucleotides
29
Examples of decreased entry (natural resistance)
b lactam antibiotics (pseudomonas aeruginosa) Fluoroquinolones (P species) Aminoglycosides (E. coli, pseudomonas)
30
Examples of increased efflux
Tetracyclines - strep, staph, entero Fluoroquinolones (P species) Macrolides
31
antimicrobial action outpatients vs hospitalized patients
hospital:culture sensitive within 24 hrs outpatient prescribed empirically based on symptoms, anatomic site, local patterns of infections, patient demographics
32
Selective distribution/accumulation (benefits)
Clindamycin - bone (osteomyelitis) Macrolides - pulmonary cells (URI/pneumonia) Tetracyclines - gingival crevicular fluids/sebum (periodontitis/acne) Nitrofurantoin - urine (UTI)
33
selective distribution (toxicity)
Aminoglycosides - inner ear/renal brush border (ototoxicity, nephrotoxicity) Tetracyclines bind Ca in developing bone/teeth (abnormal bone grwoth/tooth discoloration)
34
Renal excretion and formula between MD and CL
Antibiotics eliminated by renal excretions - monitored by serum creatinine and creatinine clearance (SCr and CrCl) MD/t = CPss x CL
35
Hepatic metabolisms considerations
Drug drug interactions interpatient rate difference (genetic polymorphism) Hepatotix action - generally avoid
36
List narrow spectrum antibiotic drugs
``` Aminoglycosides Penicillinase-resistant penicillin clindamycin Vancomycin Metronidazole Penicillin G, V ```
37
List of extended spectrum antibiotics drugs
aminopenicillins (amox, amp) Cephalosporins fluoroquinolones (cip, levo) Carbapenems
38
List of broad spectrum antibiotics drugs
``` Macrolides Chloramphenicol Fluorquinolones (Moxi, Gemi) Sulfonamides Tetracyclines Trimethoprim ```
39
Adverse reaction/toxicity types
DIrect to the drug Indirect - allergies, salt effects/fillers, drug drug interactions/affect CYP Distrubance of host microflora - superinfection - overgrowth of normal suppresed pathogenic organisms (ie. Clostridium difficile - pseudomembranous colitis)
40
stage 1 of bacterial cell wall synthesis
1: synthesis/assembly of cell wall subunits - in cytosol
41
stage 2 of bacterial cell wall synthesis
2. Linear polymerization of subunits - at cell membrane
42
Stage 3 of bacterial cell wall synthesis
3. Cross-linking of peptidoglycan polymers - at cell wall
43
Antibiotics that block stage 1
fosfomycin, cycloserine
44
Antibiotics that block stage 2
Bacitracin, vancomycin
45
Antibiotics that block stage 3
Penicillins, cephalosporins