Antimicrobials- Protein Synthesis Inhibitors Flashcards

1
Q

What type of antimicrobials are the following and what subunit do they bind to?

Gentamycin
Amikacin
Tobramycin

A

Aminoglycosides which bind irreversibly to the 30s subunit

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2
Q

How do aminoglycosides, macrolides, lincosamides, and tetracyclines, and glycylcycline work?

A

They are protein synthesis inhibitors.

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3
Q

Which drugs have a post-antibacterial effect?

A

Aminoglycosides

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4
Q

What are the effects of aminoglycosides, and what dose is recommended?

A

Bactericidal. I higher concentration single dose

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5
Q

How do Marcolides inhibit protein synthesis?

A
  1. They prevent the translocation of tRNA (ribosome cannot move forward on the mRNA which prevents the tRNA from moving from the A-site to the P-site)
  2. They block initiating complex
  3. Cause misreading of the mRNA template
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6
Q

What type of antimicrobials are

Erythromycin
Azithromycin
Clarithromycin

A

Marcolides

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7
Q

How do macrolides and lincosamides inhibit protein synthesis?

A
  1. Binding reversibly to the 50S subunit and preventing transpeptidation. The amino acid at the p-site cannot be transferred to the growing peptide chain on the A site.
  2. Prevent translocation
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8
Q

What are the effects of macrolides and lincosamides at normal and high concentration?

A

Bacteriostatic at normal and bacteriocidal at very high (usual)

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9
Q

What is the suffix for macrolides?

A

-thromyocin

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10
Q

What type of antimicrobial is clindamycin?

A

Lacosamide

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11
Q

What type of drugs are

Tetracycline
Doxycycline
Minocycline

A

Tetracylines

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12
Q

How do tetracyclines and glycylcyclines work?

A

They reversibly bind to the 30s subunit and prevent tRNA from accessing the A site

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13
Q

What are the effects of tetracyclines and glycylcyclines?

A

Bacterial static

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14
Q

How are macrolides and lincosamides similar to chloramphenicol?

A

Macrolides, lincosamides, and chloramphenicol both reversibly bind to the 50s subunit and prevent transpeptidation. The amino acid at the p-site cannot be transferred to the growing peptide chain at the A-site. Both are bacteriostatic.

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15
Q

What type of drug is tigecycline and how does it work?

A

Tigecycline is a glycylcycline that reversibly binds to the 30s subunit and prevents tRNA from accessing the A site.

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16
Q

How do Quinupristin and Dalfopristin work?

A

Quinupristin reversibly binds to the 50S subunit and prevents translocation. The ribosome cannot advance on the mRNA and the tRNA cannot be transferred from the A-site to the P-site. Dalfopristin enhances the binding of Quinupristin.

17
Q

What are the effects of Quinupristin and Dalfopristin

A

Bactericidal

18
Q

What is the effect of linezolid?

A

Bacteriostatic

19
Q

How does linezolid work? What subunit do they bind to?

A

Binds to the 50s submit and prevents the formation of the initiation complex

20
Q

How does Chloramphenicol work?

A

Reversibly binds to the 50S subunit and blocks the transpeptidase reaction

21
Q

What other drug is given with aminoglycosides to achieve a synergistic effect and help the aminoglycoside penetrate the cell wall?

A

Cell wall inhibitors such as penicillin, cephalosporins, carbapenems, and monobactams.