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

2. Antibiotics - Protein / DNA Inhibitors Flashcards

1
Q

Protein Synthesis Inhibitors - Available Drugs and Drug Classes

A 
Aminoglycosides (cidal)
Tetracyclines (static)
Macrolides (static)
Chloramphenicol (static)
Clindamycin (static)
Linezolid (variable)
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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)
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3
Q

Aminoglycosides - Available Drugs

A 
"MEAN GNATS"
A(mean)oglycosides:
- Gentamicin
- Neomycin
- Amikacin
- Tobramycin
- Streptomycin
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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”

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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
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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”

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7
Q

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

A

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

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8
Q

Tetracyclines - Available Drugs

A

Tetracycline
Doxycycline
Demeclocycline
Minocycline

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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
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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.
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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.
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12
Q

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

A

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

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13
Q

Macrolides - Available Drugs

A

Erythromycin
Azithromycin
Clarithromycin

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14
Q

Macrolides (Erythromycin, Azithromycin, Clarithromycin) - MOA

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

“MacroSLIDES”

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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.
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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.
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17
Q

Macrolides (Erythromycin, Azithromycin, Clarithromycin) - Resistance

A

Methylation of 23S rRNA binding site.

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18
Q

Chloramphenicol - MOA

A
  • Static

- Blocks peptide bond formation at 50S ribosomal subunit.

19
Q

Chloramphenicol - Clinical Use

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

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

A

Plasmid encoded acetyltransferase that inactivates drug.

22
Q

Clindamycin - MOA

A
  • Static

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

23
Q

Clindamycin - Clinical Use

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

A
  • Pseudomembranous colitis (C. difficile overgrowth)

- Fever, diarrhea

25
Q

Sulfonamides - Available Drugs

A

Sulfamethoxazole (SMX)
Sulfisoxazole
Sulfadiazine

26
Q

Sulfonamides (Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine) - MOA

A
  • Static

- PABA antimetabolites inhibit dihydropteroate synthase.

27
Q

Sulfonamides (Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine) - Clinical Use

A
  • Gram (+)
  • Gram (-)
  • Nocardia
  • Chlamydia
  • Triple sulfas or SMX for simple UTI
28
Q

Sulfonamides (Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine) - Toxicities

A
  • Hypersensitivity
  • Hemolysis in G6PD deficiency
  • Nephrotoxicity (tubulointerstitial nephritis)
  • Photosensitivity
  • Kernicterus in infants
  • Displaces other drugs from albumin (eg Warfarin)
29
Q

Sulfonamides (Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine) - Resistance

A
  • Altered enzyme (bacterial dihydropteroate synthase)
  • Decrease uptake
  • Increased PABA synthesis
30
Q

Trimethoprim - MOA

A
  • Static

- Inhibits bacterial dihydrofolate reductase

31
Q

Trimethoprim - Clinical Use

A
  • 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
Q

Trimethoprim - Toxicities

A
  • Megaloblastic anemia, leukopenia, granulocytopenia
  • May alleviate with supplemental folinic acid (Leucovorin rescue)

“TMP - Treats Marrow Poorly”

33
Q

Fluoroquinolones - Available Drugs

A

Quinolone
- Nalidixic acid

Fluoroquinolones

  • Ciprofloxacin
  • Norfloxacin
  • Levofloxacin
  • Ofloxacin
  • Sparfloxacin
  • Moxifloxacin
  • Gatifloxacin
  • Enoxacin
34
Q

Fluoroquinolones (Nalidixic acid, Ciprofloxacin, Norfloxacin, Levofloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin) - MOA

A
  • Cidal

- Inhibit DNA gyrase (topoisomerase II)

35
Q

Fluoroquinolones (Nalidixic acid, Ciprofloxacin, Norfloxacin, Levofloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin) - Clinical Use

A
  • 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
Q

Fluoroquinolones (Nalidixic acid, Ciprofloxacin, Norfloxacin, Levofloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin) - Toxicities

A
  • 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
Q

Fluoroquinolones (Nalidixic acid, Ciprofloxacin, Norfloxacin, Levofloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin) - Resistance

A

Chromosome encoded mutation to DNA gyrase.

38
Q

Metronidazole - MOA

A
  • Cidal
  • Form free radical toxic metabolites in bacterial cell that damage bacterial DNA.
  • Antiprotozoal
39
Q

Metronidazole - Clinical Use

A
  • 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
Q

Metronidazole - Toxicities

A
  • Disulfiram-like reaction with EtOH; headache, metallic taste.
41
Q

Linezolid - MOA

A
  • Binds 50s ribosomal subunit near 30s interface preventing formation of 70s complex –> inhibit protein synthesis
42
Q

Linezolid - Clinical Use

A
  • VRE - Vanc resistant Entrococci
43
Q

Streptogramin - MOA

A
  • Combination of Quinuprostin and Dalfopristin

- Each agent individually binds the 50s ribosomal subunits to inhibit early and late stages of protein synthesis.

44
Q

Streptogramin - Clinical Use

A
  • VRE - Vanc resistant Entrococci

Boards Pharm 01: Antimicrobials (7 decks)

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