Chloramphenicol, Tetracyclines, Macrolides, Clindamycin & Linezolid Flashcards

1
Q

What antibiotics bind to the 50s ribosomal subunit and block transpeptidation?

A

Chloramphenicol

Macrolides

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2
Q

What class of antibiotics bind to the 30s subunit and block the incoming charged tRNA?

A

Tetracyclines

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3
Q

What protein synthesis inhibitors are bactericidal?

A
Aminoglycosides
Linezolid (variable)
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4
Q

What is the MOA of chloramphenicol?

A

Binds to 50s ribosomal subunit

Blocks transpeptidation

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5
Q

What is the MOA of tetracyclines?

A

Binds to 30s ribosomal subunit

Blocks binding of charged tRNA

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6
Q

What is the MOA of macrolides?

A

Binds to 50s ribosomal subunit

Blocks transpeptidation

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7
Q

Chloramphenicol has limited use owing to toxicities but is often still used in developing countries because of the low cost. What toxicities are associated with chloramphenicol?

A

Anemia
Aplastic anemia
Gray baby syndrome

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8
Q

How do bacteria gain resistance to chloramphenicol?

A

Plasmid

Encodes acetyltransferase that inactivates the drug

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9
Q

What are the clinical uses of chloramphenicol?

A

Rocky Mountain spotted fever (Rickettsia rickettsii)

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10
Q

Although chloramphenicol can be used to treat Rocky Mountain spotted fever, what is the preferred agent?

A

Doxycycline

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11
Q

Is chloramphenicol bactericidal or bacteriostatic?

A

Bacteriostatic

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12
Q

List the tetracyclines.

A

Tetracycline
Doxycycline
Minocycline

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13
Q

What compounds inhibit tetracycline absorption in the gut?

A

Divalent cations

milk, antacids, iron

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14
Q

How do bacteria gain resistance against tetracyclines?

A

Plasmid

Decreased uptake or increased efflux by transport pumps

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15
Q

What is a contraindication for tetracycline use?

A

Pregnancy

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16
Q

What toxicities are associated with tetracyclines?

A

GI distress
Photosensitivity
Discoloration of teeth and inhibition of bone growth in children

17
Q

What are indications to use tetracyclines?

A
Borrelia burgdorferi
M. pneumoniae
Ricketssia
Chlamydia
Acne
18
Q

Why are tetracyclines very effective against Ricketssia and Chlamydia?

A

Accumulate intracellularly

19
Q

List the macrolides.

A

Erythromycin
Azithromycin
Clarithromycin

20
Q

Are tetracyclines bactericidal or bacteriostatic?

A

Bacteriostatic

21
Q

Are macrolides bactericidal or bacteriostatic?

A

Bacteriostatic

22
Q

What are the clinical uses of macrolides?

A

Atypical pneumonias
B. pertussis
STIs (Chlamydia)
Gram positive cocci in patients allergic to penicillin

23
Q

What is the treatment for N. gonorrhea?

A

Ceftriaxone

Azithromycin to empirically treat for Chlamydia

24
Q

How do bacteria gain resistance against macrolides?

A

Methylation of 23s rRNA binding site inhibits binding of drug

25
Q

What effect do clarithromycin and erythromycin have on the CYP450 enzyme system?

A

Inhibitors

26
Q

What are the toxicities associated with macrolides?

A
M: motility issues (GI)
A: arrhythmia (QT prolongation) 
C: cholestasis (acute cholestatic hepatitis)
R: rash
O: eOsinophilia
27
Q

What is the MOA of clindamycin?

A

Binds 50s ribosomal subunit

Blocks peptide transfer

28
Q

Is clindamycin bactericidal or bacteriostatic?

A

Bacteriostatic

29
Q

What are indications for clindamycin?

A

Treats anaerobic infections above the diaphragm

Group A strep

30
Q

What toxicities are associated with clindamycin?

A

Pseudomembranous colitis
Fever
Diarrhea

31
Q

What drug binds to the 50s ribosomal subunit and prevents formation of the initiation complex?

A

Linezolid

32
Q

When in linezolid used?

A

MRSA

VRE

33
Q

How do bacteria acquire resistance to linezolid?

A

Point mutation of ribosomal RNA

34
Q

What toxicities are associated with linezolid?

A

Bone marrow suppression (especially thrombocytopenia)
Peripheral neuropathy
Serotonin syndrome

35
Q

A bacteria aquires a methylase that adds a methyl group to the ribosomal binding site of azithromycin. What other drug, other than macrolides, will the bacteria be resistant to?

A

Clindamycin