Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Boards Pharm 01: Antimicrobials > 2. Antibiotics - Protein / DNA Inhibitors > Flashcards

2. Antibiotics - Protein / DNA Inhibitors Flashcards

(44 cards)

Start Studying
1
Q

Protein Synthesis Inhibitors - Available Drugs and Drug Classes

A 
Aminoglycosides (cidal)
Tetracyclines (static)
Macrolides (static)
Chloramphenicol (static)
Clindamycin (static)
Linezolid (variable)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Protein Synthesis Inhibitors - Location of Drug Actions

A

“buy AT 30, CCEL(sell) at 50”

30s subunit inhbitors

    • Aminoglycosides (cidal)
    • Tetracyclines (static)

50s subunit inhibitors

    • Chloramphenicol (static)
    • Clindamycin (static)
    • Erythromycin [Macrolides] (static)
    • Linezolid (variable)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Aminoglycosides - Available Drugs

A 
"MEAN GNATS"
A(mean)oglycosides:
- Gentamicin
- Neomycin
- Amikacin
- Tobramycin
- Streptomycin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Aminoglycosides (Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin) - MOA

A

Cidal
- Bind 30s subunit and inhibit formation of initiation complex and cause misreading of mRNA.
“A INITIATES the alphabet”
- Requires O2 for uptake - ineffective against anaerobes.
“MEAN GNATS canNOT kill anaerobes”

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Aminoglycosides (Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin) - Clinical Use

A
  • Severe Gram (-) rod infections
  • Synergistic with B-Lactams
  • Neomycin for bowel surgery
  • Streptomycin for M. avium intracellulare
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Aminoglycosides (Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin) - Toxicities

A

Nephrotoxicity (especially when used with cephalosporins)
Ototoxicity (especially when used with loop diuretics)
Teratogen

“Mean GNATS canNOT kill anaerobes”

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Aminoglycosides (Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin) - Resistance

A

Transferase enzymes that inactivate the drug by acetylation, phosphorylation, or adenylation.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Tetracyclines - Available Drugs

A

Tetracycline
Doxycycline
Demeclocycline
Minocycline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Tetracyclines (Tetracycline, Doxycycline, Demeclocycline, Minocycline) - MOA

A

Static

  • Bind 30s and prevent attachment of aminoacyl tRNA.
  • Limited CNS penetration
  • Demeclocycline is an ADH antagonist, acts as a diuretic in SIADH
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Tetracyclines (Tetracycline, Doxycycline, Demeclocycline, Minocycline) - Clinical Use

A
  • Borrelia burgdorferi
  • M. pneumoniae
  • Very effective against Rickettsia and Chlamydia due to its ability to accumulate intracellularly
  • Minocycline for prophylaxis for Meningococcal infections.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Tetracyclines (Tetracycline, Doxycycline, Demeclocycline, Minocycline) - Toxicities

A
  • GI distress
  • Discoloration of teeth and inhibition of bone growth in children.
  • Photosensitivity
  • CI in pregnancy
  • Do not take with milk, antacids, or Fe containing preparations - divalent cations prevent absorption of the drug in the gut.
  • Doxycycline is fecally eliminated and is OK to use in renal failure.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Tetracyclines (Tetracycline, Doxycycline, Demeclocycline, Minocycline) - Resistance

A

Decreased uptake into cells or increased efflux out of cells by plasmid encoded transport pumps.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Macrolides - Available Drugs

A

Erythromycin
Azithromycin
Clarithromycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Macrolides (Erythromycin, Azithromycin, Clarithromycin) - MOA

A
  • Static
  • Bind 23S rRNA of the 50S ribosomal subunit to block translocation –> inhibit protein synthesis.

“MacroSLIDES”

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Macrolides (Erythromycin, Azithromycin, Clarithromycin) - Clinical Use

A
  • ATYPICAL PNEUMONIAS (MYCOPLASMA, CHLAMYDIA, LEGIONELLA)
  • URIs
  • STDs
  • Gram (+) cocci (Strep. infections in Pen. allergic patients)
  • Neisseria
  • Empiric therapy for community acquired pneumonia in the outpatient setting.

Azithromycin specific uses:

  • MAC (Mycobacterium avium intracellulare Complex) prophylaxis in HIV patients when CD4 < 50
  • Treatment and prophylaxis for M. avium intracellulare.
  • Empiric therapy, in combination with B-Lactam, for community acquired pneumonia in the ICU setting.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Macrolides (Erythromycin, Azithromycin, Clarithromycin) - Toxicities

A
  • Prolonged QT (especially Erythromycin)
  • GI discomfort (most common cause of non-compliance)
  • Acute cholestatic hepatitis, eosinophilia, skin rash.
  • Increases serum concentrations of theophyllines and oral anticoagulants.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Macrolides (Erythromycin, Azithromycin, Clarithromycin) - Resistance

A

Methylation of 23S rRNA binding site.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Chloramphenicol - MOA

Study These Flashcards
A
  • Static

- Blocks peptide bond formation at 50S ribosomal subunit.

19
Q

Chloramphenicol - Clinical Use

Study These Flashcards
A
  • MENINGITIS (H. influenzae, Neisseria meningitidis, Strep. pneumoniae)
  • Limited use due to toxicities, but often used in developing countries due to low cost.
20
Q

Chloramphenicol - Toxicities

Study These Flashcards
A
  • Anemia (dose dependent), aplastic anemia (dose independent)
  • Gray baby syndrome (in premature infants because they lack liver UDP-glucuronyl transferase)
21
Q

Chloramphenicol - Resistance

Study These Flashcards
A

Plasmid encoded acetyltransferase that inactivates drug.

22
Q

Clindamycin - MOA

Study These Flashcards
A
  • Static

- Block peptide Transfer (transpeptidation) at 50S ribosomal subunit.

23
Q

Clindamycin - Clinical Use

Study These Flashcards
A
  • ANAEROBIC INFECTIONS (eg Bacteroides fragilis, Clostridium perfringens) IN ASPIRATION PNEUMONIAE OR LUNG ABSCESSES
  • Above the diaphragm anaerobes (Metronidazole treats anaerobes below the diaphragm)
24
Q

Clindamycin - Toxicities

Study These Flashcards
A
  • Pseudomembranous colitis (C. difficile overgrowth)

- Fever, diarrhea

25
Sulfonamides - Available Drugs
Sulfamethoxazole (SMX) Sulfisoxazole Sulfadiazine
26
Sulfonamides (Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine) - MOA
- Static | - PABA antimetabolites inhibit dihydropteroate synthase.
27
Sulfonamides (Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine) - Clinical Use
- Gram (+) - Gram (-) - Nocardia - Chlamydia - Triple sulfas or SMX for simple UTI
28
Sulfonamides (Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine) - Toxicities
- Hypersensitivity - Hemolysis in G6PD deficiency - Nephrotoxicity (tubulointerstitial nephritis) - Photosensitivity - Kernicterus in infants - Displaces other drugs from albumin (eg Warfarin)
29
Sulfonamides (Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine) - Resistance
- Altered enzyme (bacterial dihydropteroate synthase) - Decrease uptake - Increased PABA synthesis
30
Trimethoprim - MOA
- Static | - Inhibits bacterial dihydrofolate reductase
31
Trimethoprim - Clinical Use
- Used in combination with sulfonamides (TMP-SMX) for: - UTI's (including for prophylaxis in history of recurrent UTI's) - Shigella, Salmonella, Pneumocystis jiroveci pneumonia - Prophylaxis against Pneumocystis pneumonia in HIV with CD4 < 200 - Prophylaxis against Pneumocystis pneumonia and toxoplasmosis in HIV with CD4 < 100
32
Trimethoprim - Toxicities
- Megaloblastic anemia, leukopenia, granulocytopenia - May alleviate with supplemental folinic acid (Leucovorin rescue) "TMP - Treats Marrow Poorly"
33
Fluoroquinolones - Available Drugs
Quinolone - Nalidixic acid Fluoroquinolones - Ciprofloxacin - Norfloxacin - Levofloxacin - Ofloxacin - Sparfloxacin - Moxifloxacin - Gatifloxacin - Enoxacin
34
Fluoroquinolones (Nalidixic acid, Ciprofloxacin, Norfloxacin, Levofloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin) - MOA
- Cidal | - Inhibit DNA gyrase (topoisomerase II)
35
Fluoroquinolones (Nalidixic acid, Ciprofloxacin, Norfloxacin, Levofloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin) - Clinical Use
- Gram (-) rods or urinary and GI tracts (including Pseudomonas) - Neisseria - Some Gram (+) - Ciprofloxacin is DOC for Prophylaxis of Meningococcal infections - Empiric therapy for community acquired pneumonia in the inpatient setting. - Empiric therapy, in combination with B-Lactam, for community acquired pneumonia in the ICU setting.
36
Fluoroquinolones (Nalidixic acid, Ciprofloxacin, Norfloxacin, Levofloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin) - Toxicities
- Do not take with antacids - GI upset, superinfections, skin rash, headache, dizziness. - CI in pregnancy and children --> Damage to cartilage - Tendonitis and tendon rupture in age 60+ or patients taking Prednisone - leg cramps, myalgias in any age group. "FluoroquinoLONES hurt attachments to the BONES"
37
Fluoroquinolones (Nalidixic acid, Ciprofloxacin, Norfloxacin, Levofloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin) - Resistance
Chromosome encoded mutation to DNA gyrase.
38
Metronidazole - MOA
- Cidal - Form free radical toxic metabolites in bacterial cell that damage bacterial DNA. - Antiprotozoal
39
Metronidazole - Clinical Use
- GIARDIA - ENTOMAEBA - TRICHIMONAS - GARDNERELLA vaginalis - ANAEROBES (Bacteroides, C. difficile) - h. PYLORI (triple therapy with bismuth and amoxycillin or tetracycline) - Anaerobes below the diaphragm "GET GAP on the METRO"
40
Metronidazole - Toxicities
- Disulfiram-like reaction with EtOH; headache, metallic taste.
41
Linezolid - MOA
- Binds 50s ribosomal subunit near 30s interface preventing formation of 70s complex --> inhibit protein synthesis
42
Linezolid - Clinical Use
- VRE - Vanc resistant Entrococci
43
Streptogramin - MOA
- Combination of Quinuprostin and Dalfopristin | - Each agent individually binds the 50s ribosomal subunits to inhibit early and late stages of protein synthesis.
44
Streptogramin - Clinical Use
- VRE - Vanc resistant Entrococci

Boards Pharm 01: Antimicrobials (7 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions