C.12. Tetracyclines and Glycylcyclines Flashcards

1
Q

list the mechanisms of action of Tetracyclines

A
  1. binds to the 30S ribosomal subunit–> inhibit binding of charged tRNA to the acceptor site
  2. act as chelators. they bind to divalent cations (Ca², Mg², Fe²)–> ↓ their absorption
  3. accumulation in bone and teeth (due to ↑ Ca² content)
  4. bacteriostatic effect
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2
Q

do Tetracyclines enter the CNS?

A

no

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3
Q

list the tetracyclines

A

Tetracycline
Minocycline
Doxycycline
Demeclocycline

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4
Q

what is Tigecycline?

A

a Glycylcycline

derived from tetracycline

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5
Q

contraindications of Tetracyclines

A

children<10 years of age
pregnancy
pre-existing liver disease

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6
Q

which tetracycline is safe to use in renal dysfunction?

A

Doxycycline

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7
Q

how is Tigecycline given?

A

IV only

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8
Q

how are tetracycline, Minocycline and Demeclocycline given?

A

orally

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9
Q

what is the T1/2 of Tigecycline?

A

40 hours

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10
Q

how is Tigecycline excreted?

A

in the bile

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11
Q

how is Doxycycline excreted?

A

in the feces

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12
Q

what are the side effects of Tetracyclines and Glycyclcyclines?

A
  1. GI distress (superinfections may lead to severe colitis or candidiasis)
  2. Enamel dysplasia, bone growth abnormalities
  3. Hepatotoxicity
  4. Nephrotoxicity (RTA,Fanconi syndrome)
  5. Photosensitivity
  6. Vestibular toxicity (dose-dependent, reversible)
  7. Teratogenic
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13
Q

spectrum and clinical use of Tetracycline

A

broad:

  1. gram - and + aerobes, anaerobes, intracellular, spirochetes
  2. chlamydia (3rd choice) & mycoplasma
  3. Rickettsia, Vibrio, H. pylori
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14
Q

clinical use of Minocycline

A

Meningococcal carrier state

Dental procedures

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15
Q

clinical use of Doxycycline

A
  1. alternative treatment to macrolides in community-acquired pneumonia
  2. 2nd line for campylobacter enteritis (1st is macrolides)
  3. Gonorrhea, chlamydia
  4. zoonotic diseases
  5. acne treatment (propionibacterium acne)
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16
Q

when do we give Tigecycline?

A

in organisms resistant to standard tetracycline

MRSA strains, VRE strains

17
Q

when do we give Demeclocycline?

A

SIADH, inhibit the renal activity of ADH

18
Q

what organisms are resistant to Tigecycline

A

pseudomonas and proteus

19
Q

mechanism of resistance of tetracyclines

A
  1. efflux pump expressed by bacteria–> lowers effective drug concentration
  2. alteration of ribosomal binding site
  3. formation of ribosomal protecting proteins that interfere with drug binding