Protein Synthesis Flashcards

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1
Q
  • Selectively inhibit bacterial protein synthesis
  • Protein synthesis in microorganisms is not identical to **mammalian **
    cells
  • **70S **ribosomes in **bacteria **
  • 80S ribosomes in mammalians
A

Protein Synthesis Inhibitors

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2
Q

MECHANISM OF ACTION

A
  • Bacteriostatic
  • Bactericidal – Oxazolidinones and Pleuromutilins
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3
Q

BACTERIAL PROTEIN SYNTHESIS INHIBITORs

  • Chloramphenicol
  • Tetracyclines
A

Broad spectrum

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4
Q

BACTERIAL PROTEIN SYNTHESIS INHIBITORS

  • Macrolides
  • Ketolides
A

Moderate spectrum

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5
Q

BACTERIAL PROTEIN SYNTHESIS INHIBITORS

  • Lincosamides
  • Streptogramins
  • Linezolid
A

Narrow spectrum

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6
Q
  • **Simple **and **Distinctive structure **
  • Effective Orally and Parenterally
  • MOA: Inhibits microbial protein synthesis and is bacteriostatic against most susceptible organisms.
  • It binds reversibly to the 50S subunit of the bacterial ribosome and inhibits peptide bond formation
A

Chloramphenicol
Chlo/ram/phe/ni/col

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7
Q

Antimicrobial Activity

  • **Broad spectrum **
  • Active against both aerobic and anaerobic gram-positive and gram- negative organisms.
  • Bacteriostatic
  • Bactericidal - strains of H, influenzae, N. meningitidis, and some strains of Bacteroides
  • Not active against Chlamydia species.
  • Resistance is plasmid-mediated
  • formation of chloramphenicol acetyltransferases
A

Chloramphenicol

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8
Q

Absorption : TETRACYCLINE

  • 60-70%
  • Administered on an empty stomach.
A
  • Tetracycline
  • Demeclocycline
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9
Q

Absorption : TETRACYCLINE

  • 95-100%
  • Not impaired by food.
A
  • Doxycycline
  • Minocycline
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10
Q

Absorption : TETRACYCLINE

  • 35%
  • Absorption is impaired by:
    Multivalent cations (Ca2+, Mg2+, Fe2+, Al3+)
    Dairy products
    Antacids (contain multivalent cations)
    Alkaline pH
A

Omadacycline

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11
Q

Tetracycline

It is Given IV

A
  • Tigecycline
  • Eravacycline
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12
Q

Tetracycline

A
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13
Q

Tetracycline

Excretion ?

A

Feces

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14
Q

Tetracycline

Wide tissue distribution except in ?

A

CSF

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15
Q

Tetracycline

A
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16
Q

Tetracycline

A
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17
Q

Tetracycline

A
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18
Q

Tetracycline

A
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19
Q

Tetracycline

A
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20
Q

Tetracycline

A
21
Q

Tetracycline

Short-acting
6-8 hours serum half-life

A
  • Tetracycline
  • Chlortetracycline
  • Oxytetracycline
22
Q

Tetracycline

Intermediate-acting
12 hours

A

Demeclocyline

23
Q

Tetracycline

Long-acting
16-18 hours

A
  • Once daily: Doxycycline, Minocycline
  • By convention, usually administered twice daily
24
Q

Tetracycline

Long half-lives
36, 20, and 16 hours (respectively)

A
  1. Twice-daily dosing:
    * Tigecycline
    * Eravacycline
  2. Once daily:
    * Omadacycline
25
Q

Tetracycline

What is the MOA ?
Tetracycline
Chlortetracycline
Oxytetracycline

A

Oral

26
Q

Tetracycline

What is the MOA ?
Demeclocyline

A

Oral

27
Q

Tetracycline

What is the MOA ?
Doxycycline

A

Oral

28
Q

Tetracycline

What is the MOA ?
Tigecycline
Eravacycline

A

IV

29
Q

Tetracycline

What is the MOA ?
Minocycline

A

IV

30
Q

Tetracycline

What is the MOA ?
Omadacycline

A

Oral and IV

31
Q

Tetracycline

Primary uses

A
  • Mycoplasma pneumoniae (in adults)
  • Chlamydiae, including STIs
  • Rickettsiae
  • Borrelia sp.
  • Vibrios (Vibrio cholerae)
  • Some spirochetes
  • Anaplasma phagocytophilum
  • Ehrlichia sp
32
Q

Tetracycline

Secondary uses

A

Alternative :
* Community-acquired pneumonia (CAP)
* Syphilis
* Chronic bronchitis
* Leptospirosis
* Acne

33
Q

In-vitro activity against:
MRSA
ESBL-producing Gr(-)’s
Acinetobacter sp

A

Tigecycline

34
Q
  • Non Inferiority to:
    Moxifloxacin in the treatment of community-acquired bacterial pneumonia
    Linezolid in the treatment of acute bacterial skin and skin structure infections
  • Not affected by the most common resistance mechanisms; retains ​​activity against a broad array of pathogens resistant to older drugs.
  • Co-administration with any food leads to substantial decreases in the absorption of the oral form, it must be administered at least 4 hours after and 2 hours before any food or liquid other than water.
A

Omadacycline

35
Q

Tetracycline

Toxicity

A
  1. GI disturbances :
    * Nausea, vomiting, and diarrhea
    * Tigecycline: Nausea
    * Esophageal ulceration (rare)
    * Life-threatening enterocolitis
    * Oral and vaginal candidiasis
    * Renal toxicity
    - Tetracyclines, especially demeclocycline
    * Photosensitivity
    - Tetracyclines, especially Demeclocycline
    * Vestibular toxicity
    - Doxycycline and minocycline
36
Q

MACROLIDES : ERYTHROMYCIN, AZITHROMYCIN, CLARITHROMYCIN

Prototype

A

Erythromycin

37
Q

Semisynthetic derivatives of erythromycin are ?

A
  • Clarithromycin
  • Azithromycine
38
Q

Macrolides is what s ?

A

50s

39
Q

Macrolide antibiotics prolong ?

A

the electrocardiographic QT interval

40
Q

Torsades de Pointes arrhythmia.

A

Macrolides

41
Q

Macrolides

Good oral bioavailability.

A

Azithromycin

42
Q

Macrolides

absorption is impeded by food.

A

Azithromycin

43
Q

Macrolides

Distributed to most body tissues.

A

Azithromycin

44
Q

Macrolides is primarily what metabolism ?

A

Hepatic Metabolism.

45
Q

macrolides

2 hours half-life

A

Erythromycin

46
Q

macrolides

2 - 4 Days

A

Azithromycin

47
Q

macrolides

6 Hours

A

Clarithromycin

48
Q
A