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PHRM 865 > Streptogramin and Oxazolidinone > Flashcards

Streptogramin and Oxazolidinone Flashcards

1
Q

Which antibiotics are in streptogramin?

A
  • quinupristin
  • dalfopristin
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2
Q

What drug is this?

A

quinpristin

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3
Q

What drug is this?

A

dalfopristin

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4
Q

Which structures of quinpristin and dalfopristin (Synercid) allow for salt formation and enhance water solubility?

A
  • amino side chains
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5
Q

Explain how Synercid, quinpristin, and dalfopristin compare with regards to bacteriostatic vs bacteriocidal.

A
  • quinpristin and dalfopristina re both bacteriostatic alone
  • syndercid is bacteriostatic against enterococcus faecium and bactericidal against strains of methicillin-susceptible and methicillin-resistant staphylococci.
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6
Q

What is the route of administration of Synercid?

A

parenterally

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7
Q

What is the mechanism of action of dalfopristin?

A
  • Interferes with the peptidyl transferase-catalyzed step of peptide synthesis
  • prevents the formation of a peptide bond
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8
Q

What is the mechanism of action of quinpristin?

A
  • Quinpristin binds in the ribosomal tunnel and causes blockage of the tunnel
  • inhibits protein synthesis
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9
Q

What are the therapeutic uses for Synercid?

A
  1. VRE bacteremia
  2. MRSA
  3. VRE UTI
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10
Q

What are the different resistance mechanisms to quinpristin?

A
  • adenine methylation of A2058 in the 23 S rRNA
  • efflux and enzymatic inactivation by resistant bacteria
  • tx of VRE (overuse)
  • use in animal feeds
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11
Q

What are the side effects of synercid?

A
  • inflammation
  • injection site pain
  • GI
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12
Q

What are the characteristics of Synercid pharmacokinetics?

A
  • different elimination rates for each component
  • linear relationship between the dose and the AUC
  • BBB not penetrated
  • clearance is 75% through biliary excretion
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13
Q

What drug interactions is synercid involved in?

A
  • streptogramins inhibit CYP 3A4
  • a lot of potential interactions
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14
Q

What drug is this?

A

linezolid

oxazolidinones

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15
Q

What is the mechanism of action of oxazolidinones?

linezolid

A
  • Linezolid binds to 50S ribosomal subunit.
  • This interaction prevents formation of the 70S initiation complex –> which then prevents translation and bacterial protein synthesis
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16
Q

What are the therapeutic uses for linezolid?

A
  • VRE
  • nosocomial pneumonia caused by methicillin-resistant strains of staphylococcus aureus
  • skin infections caused by methicillin-resistant strains of staphylococcus aureus

  • VRE = vancomycin resistant enterococcus faecium
17
Q

Why should linezolid be used only to treat or prevent infections that are proven or strongly suspected to be caused by multiple drug-resistant gram-positive bacteria?

A
  • to reduce development of drug-resistant bacteria
  • to maintain the effectiveness
18
Q

What is the resistance mechanism for linezolid?

A
  • target site modification

  • G to U subsitution in the peptidyl transferase center of 23S rRNA at position 2576
  • leads to reduced affinity of linezolid for 50S subunit
19
Q

What are the side effects of linezolid?

A
  • GI side effects
  • headache
  • tongue discoloration
  • thrush
  • anemia
  • linezolid induced neuropathy
20
Q

What is the main metabolic pathway of linezolid?

A
  • linezolid is metabolized via morpholine ring oxidation
21
Q

What are the pharacokinetics for linezolid?

A
  • 100% bioavailable after oral administration
  • half-life: 4-6 hours

can be administered IV or PO

22
Q

Is linezolid involved with CYP450 interactions?

A

No :)

23
Q

What potential drug interactions is linezolid involved with?

A

Linezolid inhibits monoamine oxidase (MAO) which means it can potentially interact with adrenergic and serotonergic agents

24
Q

What are counseling points for linezolid?

A
  • avoid consuming large quantities of foods with tyramine in order to avoid pressor response
  • use in caution in patients who are sensitive to increases in BP due to preexisting conditions
25
Q

How does tedizolid phosphate compare to linezolid?

A
  • tedizolid is more potent than linezolid vs MRSA
  • the mechanism of action is the same

2nd gen oxazolidinone, prodrug

PHRM 865 (12 decks)

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