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Microbiology > Antibiotics: Agents Interfering with Bacterial Protein and DNA Synthesis > Flashcards

Antibiotics: Agents Interfering with Bacterial Protein and DNA Synthesis Flashcards

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1
Q

Aminoglycosides

A 
Streptyomycin
Tobramycin 
Gentamicin
Amikacin
Neomycin
Kanamycin
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2
Q

Aminoglycosides (Mechanism of Action)

A

Bind to 30S ribosomal subunit and interfere with protein synthesis in the following 3 ways:

  1. Blocking the initiation step
  2. Blocking the ribosomal translocation step
  3. Causing mistranslation
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3
Q

Aminoglycosides - Effects

A

Rapidly bactericidal vs. many aerobic GRAM NEGATIVE bacteria
Associated with a significant POSTANTIBIOTIC EFFECT

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4
Q

Streptomycin - primary clinical indications

A

2nd line agent for treatment of tuberculosis in combination with another agent (ex. INH)

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5
Q

Tobramycin and Gentamicin: primary clinical indications

A

Treatment of serious systemic infections caused by Gram-negative organisms.
Often used in combination with a BETA-lactam drug because of synergistic effects and reduced emergence of resistance.

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6
Q

Amikacin: primary clinical indications

A

Used in cases of resistance to tobramycin and gentamicin caused by inactivating enzymes

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7
Q

Neomycin and Kanamycin: primary clinical indications

A

Limited to topical use (skin and eyes)

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8
Q

Primary Toxicities of Aminoglycosides

A

Nephrotoxicity: reversible with cessation of therapy
Ototoxicity: auditory damage, vestibular damage, IRREVERSIBLE, even upon cessation of therapy
Toxicities are more likely with >5 days of therapy

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9
Q

Tetracyclines (List 6)

A 
Tetracycline
Oxytetracycline
Demeclocycline
Minocycline
Doxycycline
Tigecycline (glycylcyline)
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10
Q

Tetracycline Mechanism of Action?

A

Bind to 30S ribosomal subunit and interfere with protein synthesis by blocking the peptide elongation step

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11
Q

Effects of Tetracyclines?

A

Bacteriostatic vs. many aerobic and anaerobic Gram-POSITIVE and Gram-NEGATIVE bacteria

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12
Q

PCI: Rickettsial Infections

A

TETRACYCLINES

Rocky Mountain spotted fever, typhus, and Q fever

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13
Q

PCI: STI

A

TETRACYCLINES

Chlamydia, urethritis, cervicitis, and epididymititis

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14
Q

PCI: Respiratory infections

A

TETRACYCLINES

Community-acquired pneumonia

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15
Q

PCI: Skin and Soft-Tissue Infections

A

TETRACYCLINES

Community-acquired Staph and acne

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16
Q

PCI: Infections caused by MDR Bacteria

A

Tigecycline (IV ONLY) is used for MDR intra-abdominal, skin, and soft-tissue infections, and community-acquired pneumonia

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17
Q

Doxycycline

A

Doxycycline is used in the treatment of anthrax, malaria, and Lyme Disease

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18
Q

Primary Toxicities of Tetracyclines:

A

GI Disturbances: Nausea, vomiting, diarrhea
Teeth and Bone: Tooth discoloration, growth deformity and inhibition in children under 8!!!
Photosensitization
Hepatotoxicity during pregnancy

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19
Q

Macrolides (4)

A

Erythromycin
Clarithromycin
Azithromycin
Telithromycin (ketolide)

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20
Q

Macrolide: Mechanism of Action

A

Bind to 50S ribosomal subunit and interfere with protein synthesis by blocking the RIBOSOMAL TRANSLOCATION STEP

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21
Q

Macrolide: Effects

A

Generally bacteriostatic vs. aerobic Gram-POSITIVE and some Gram-NEGATIVE bacteria

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22
Q

PCI of Macrolides

A

Respiratory Infections: Community-acquired pneumonia, acute exacerbations of chronic bronchitis
Skin and Soft-Tissue infections: Substitute for penicillin in allergic individuals with susceptible Staph infections
Acute otitis media
Streptococcal pharyngitis
Chlamydial infections
Diptheria
Pertussis (whooping cough)

23
Q

Toxicities of Macrolides

A

GI Disturbances
Hepatotoxicity - cholestatic hepatitis (has caused the approved use of TELITHROMYCIN to be restricted to community-acquired pneumonia)

24
Q

Example of Lincosamide

A

Clindamycin

25
Q

Clindamycin mechanism of action

A

Bind to 50S ribosomal subunit and interferes with protein synthesis by blocking the RIBOSOMAL TRANSLOCATION STEP

26
Q

Clindamycin Effects

A

Bacteriostatic vs. aerobic and anaerobic Gram-positive bacteria

27
Q

Clindamycin PCI

A

skin and soft-tissue infections

28
Q

Toxicities of Clindamycin

A

Diarrhea
Pseudomembranous colitis caused by C. difficile
Skin rashes

29
Q

Example of Streptogramins

A

Quinupristin/Dalfopristin

30
Q

Mechanism of action of Streptogramins

A

Bind to 50S ribosomal subunit and interfere with protein synthesis by blocking the ribosomal translocation step and inhibiting peptide elongation

31
Q

Effects of Streptogramins

A 
Active vs. most Gram-
positive bacteria 
• Combination is
bactericidal vs.
streptococci and most
staphylococci, but
bacteriostatic vs.
enterococci.
32
Q

PCI of Streptogramins

A 
Treatment of infections
caused by vancomycin-
resistant E. faecium
(VRE) 
• Treatment of
complicated skin
infections caused by
MSSA
33
Q

Toxicities of Streptogramins

A

Infusion related effects of the IV only combination
Arthalgia
Myalgias

34
Q

Example of Oxazolidinone

A

LINEZOLID

35
Q

Mechanism of Linezolid

A 
•  Binds to 50S ribosomal
subunit and interferes
with protein synthesis
by blocking the initiation
step
36
Q

Effects of Linezolid

A 
• Active vs. aerobic and
anaerobic Gram-positive
bacteria • Bactericidal vs.
streptococci, but
bacteriostatic vs.
staphylococci and
enterococci.
37
Q

PCI of Linezolid

A 
Treatment of infections
caused by MDR Gram-
positive bacteria (MRSA,
VRE, and penicillin-
resistant streptococci)
38
Q

Toxicity of Linezolid

A 
Myelosuppression
(leukopenia,
pancytopenia, and
thrombocytopenia) with
treatment durations >2
weeks.
39
Q

Anti-Folates - Sulfonamides

A

Sulfisoxazole Sulfamethoxazole (SMX) Sulfasalazine

40
Q

Anti-Folates - Sulfonamides (Mechanism of Action)

A

Competitive
antagonists of
dihydropteroate
synthase

41
Q

Effects of Anti-Folate-Sulfonamides

A 
Bacteriostatic vs.
numerous Gram-
negative and some
Gram-positive
bacteria
42
Q

PCI of Anti-Folate-Sulfonamides

A 
Urinary tract
infections (usually in
combination with
other drugs) 
• Sulfasalazine is used in
the treatment of
ulcerative colitis and
enteritis.
43
Q

Toxicities of Sulfonamides

A 
Allergic reactions
(rash, fever, urticaria,
photosensitivity, GI
effects) •  
Crystalluria •  
Hematuria
44
Q

Anti-Folates – Trimethoprim/Sulfamethoxazole (TMP-SMX) Combination

A

Trimethoprim/Sulfamethoxazole (TMP-SMX)

45
Q

TMP-SMX Mechanism of Action

A

TMP is a competitive
antagonist of
dihydrofolate
reductase

46
Q

TMP-SMX Effects

A 
• Like the sulfonamides,
TMP is bacteriostatic
vs. numerous Gram-
negative and some
Gram-positive
bacteria • The TMP-SMX
combination is
bactericidal
47
Q

PCI of TMP-SMX

A

• Uncomplicated urinary
tract infections • Pneumocystis jiroveci
pneumonia • Shigellosis • Systemic Salmonella
infections • Prostatitis • Acute exacerbations of
chronic bronchitis

48
Q

Toxicities of TMP-SMX

A 
With treatment
duration 5 days,
hematologic effects
(megaloblastic
anemia, leukopenia)
can occur.
49
Q

Fluoroquinolones

A

Ciprofloxacin Lomefloxacin Levofloxacin
Ofloxacin
Gemifloxacin
Moxifloxacin

50
Q

Fluoroquinolones Mechanism of Action

A 
Inhibitors of
topoisomerase II
(DNA gyrase) in Gram-
negative bacteria and
topoisomerase IV in
Gram-positive
bacteria
51
Q

Effects of Fluoroquinolones

A

Bactericidal vs. both
Gram-negative and
Gram-positive
bacteria

52
Q

PCI of Fluoroquinolones

A 
Urinary tract
infections • Ciprofloxacin is used
for prevention and
treatment of anthrax • Diarrhea caused by
Shigella, Salmonella,
and toxigenic E. coli • Soft-tissue, bone, and
joint infections • Intra-abdominal
infections • Respiratory tract
infections
(levofloxacin,
gemifloxacin, and
moxifloxacin are
particularly effective)
53
Q

Toxicities of Fluoroquinolones

A 
Generally well
tolerated •  
GI disturbances
include nausea,
vomiting, and
diarrhea

Microbiology (1 decks)

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