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Disease & Defense - Unit 2 > Protein Synthesis Inhibitors > Flashcards

Protein Synthesis Inhibitors Flashcards

1
Q

Classes of antibacterial protein synthesis inhhibtors

A
  • macrolides
  • tetracyclines
  • aminglycosides
  • lincomycins (clindamycin)
  • oxazolidinones
  • streptogamins
  • chloramphenicol
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2
Q

Macrolides: examples

A
  • erythromycin
  • clarithromycin
  • azithromycin
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3
Q

Macrolides: mechanism of action

A
  • blocks protein synthesis
  • binds 50S ribosomal subunit and blocks translocation
  • bacteriostatic
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4
Q

Macrolides: pharmocokinetics

A
  • good oral –> can be absorbed in GI tract
  • wide distribution except to brain/CSF
  • metabolism involves both liver and kidney
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5
Q

Macrolides: spectrum/clinical use

A
  • gram+ cocci/rods (strep, staph, pneumococci)
  • some gram- cocci
  • gram- bacilli (pertussis, H. flu, H. pylori)
  • atypical: mycoplasma/chlamydia
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6
Q

Macrolides: adverse reactions

A
  • GI disturbances

- some drug interactions possible

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7
Q

Tetracyclines: examples

A
  • tetracycline
  • doxycycline
  • minocycline
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8
Q

Tetracyclines: mechanism of action

A
  • protein synthesis inhibitor
  • bacteriostatic
  • binds 30S ribosome
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9
Q

Tetracyclines: pharmacokinetics

A
  • good oral (on empty stomach, impaired by milk)
  • excellent tissue penetration
  • concentrated in liver, most excreted in urine (except doxy/mino)
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10
Q

Tetracyclines: spectrum/clinical uses

A
  • broad spectrum agent (many organisms now resistant)
  • gram+ cocci (MRSA)
  • atypical organisms: chlamydia, mycoplasma
  • spirochetes
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11
Q

Tetracyclines: adverse reaction

A
  • avoid during 2nd half of pregnancy and children < 8yo
  • GI disturbance
  • yeast infection
  • drug interaction w/antacids and iron supplements –> decreased bioavailability
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12
Q

Clindamycin: mechanism of action

A
  • inhibit protein synthesis
  • binding 50S subunit
  • bacteriostatic
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13
Q

Clindamycin: pharmacokinetics

A
  • good oral
  • penetrates most tissue well, especially bone (not CSF)
  • liver metabolism
  • excreted in breast milk
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14
Q

Clindamycin: spectrum/clinical uses

A
  • treatment of severe anaerobic infections
  • narrow spectrum
  • gram+ cocci (strep, MSSA osteomyelitis, MRSA cutaneous)
  • anaerobes (bacteroides fragilis)
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15
Q

Clindamycin: adverse reactions

A
  • pseudomembranous colitis

- severe diarrhea

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16
Q

Aminglycosides: examples

A
  • streptomycin
  • tobramycin
  • gentamicin
17
Q

Aminglycosides: mechanism of action

A
  • protein synthesis inhibitor
  • bactericidal
  • inhibits protein synthesis initiation
18
Q

Aminglycosides: pharmacokinetics

A
  • poor oral, good IV or IM
  • distributes only to ECF
  • renal excretion
19
Q

Aminglycosides: spectrum/clinical uses

A
  • limited by toxicity
  • narrow spectrum
  • gram- bacilli aerobes (pseudomonoas, E. coli)
20
Q

Aminglycosides: adverse reactions

A
  • very toxic
  • eighth nerve damage (auditory, vestibular)
  • reversible renal toxicity
  • drug-drug interactions w/B-lactams (enhance) and penicilinns (inhibit)
21
Q

Chloramphenicol: mechanism of actions

A
  • inhibit protein synthesis
  • binding to 50S ribosome
  • mostly bacteriostatic
22
Q

Chloramphenicol: pharmacokinetics

A
  • good oral
  • widely distributed, including CNS/CSF
  • liver metabolism
  • excreted in breast milk
23
Q

Chloramphenicol: spectrum/clinical uses

A
  • broad spectrum (limited by toxicity)
  • gram+/- cocci (N. meningitis)
  • gram- bacilli (H. flu, salmonella typhi=typhoid fever)
  • anaerobes (bacteroides)
  • atypical organisms (rickettsia)
24
Q

Chloramphenicol: adverse reactions

A
  • bone marrow toxicity
  • gray baby syndrome
  • GI disturbances
25
Q

Oxazolidinone (Linezolid): mechanism of action

A
  • novel protein synthesis inhibitor
  • bacteriostatic
  • binds 50S ribosome
26
Q

Oxazolidinone (Linezolid): pharmacokinetics

A
  • good oral (IV available)
  • readily distributed to well-perfused tissue
  • nonenzymatic metabolism; some renal excretion
27
Q

Oxazolidinone (Linezolid): spectrum/clinical uses

A
  • used for life-threatening infections

- gram+ cocci: enterococci (+VRE), staphylococci (+MRSA), streptococci

28
Q

Oxazolidinone (Linezolid): adverse reactions

A
  • minor

- inhibits MAO; linezolid+SSRI–>hypertensive response

29
Q

Streptogramin (Quinupristin/Dalfopristin): mechanism of action

A
  • protein synthesis inhibitor
  • binds 50S ribosome
  • bactericidal
30
Q

Streptogramin (Quinupristin/Dalfopristin): pharmacokinetics

A
  • IV only

- liver metabolism + biliary excretion (no renal)

31
Q

Streptogramin (Quinupristin/Dalfopristin): spectrum/clinical uses

A
  • used for life-threatening infections

- gram+ cocci: enterococci (+VRE), staphylococci (+MRSA), streptococci

32
Q

Streptogramin (Quinupristin/Dalfopristin): adverse reactions

A
  • infusion site irritation

- inhibits CYP3A4 –> increase plasma levels of drugs metabolized by that enzyme

Disease & Defense - Unit 2 (10 decks)

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