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PHRM 865: Theraputics V > Lecture 10: Vancomycin and Friends > Flashcards

Lecture 10: Vancomycin and Friends Flashcards

MAINLY GRAM (+)

1
Q

What is the Mechanism of Action for Vancomycin?

A
  • Inhibit cell wall synthesis 2nd stage [binding to D-Ala-D-Ala] preventing the cross-linking
  • Slow Bactericidal
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2
Q

What is the mechanism of Resistance for Vancomycin?

VRE and VRSA

A
  • VRE: Modifications of the D-Ala-D-Ala site to D-Lac by VanA [or VanC-E]
  • VISA: Thinker cell wall
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3
Q

What is the Spectrum of Activity for Vancomycin?

A
  • Gram (+): Group/Viridan Strep, MSSA, MRSA [THE DOC], C. Diff
  • Gram (-): Not active
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4
Q

What is important to know about the Pharmacology of Vancomycin?

ADME?

A
  • PK: Vd and Cl; AUC/MIC = 400-600
  • Absorption: Bad Orally so should be IV NOT IM
  • Distribution: Body tissues and Fluids [even Adipose tissue] & takes 1h to move
  • Elimination: Kidneys with t = 6-8h

D: Vd = 0.6-0.7; <120kg = 0.7; >120kg = 0.6

E: Half Life increases as Renal Function decreases

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5
Q

What are the Clinical Uses of Vancomycin?

A
  • MRSA Infections [bacteremia, pneumonia, endocarditis…]
  • Gram (+) infections when allergic to b-lactams
  • PRSP
  • ORAL is good for C. Diff
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6
Q

What are some of the Adverse Effects of Vancomycin?

A
  • Red-Man Syndrome [Cause by high infusion rate; 1g per 1h]
  • Nephrotoxicity & ototoxicity [by high doses or renal issues]
  • Dermatologic [Rashs]
  • Hematologic
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7
Q

What are the Streptogramins that are used?

A
  • Quinupristin - Dalfopristin
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8
Q

What is the Mechanism of Action for Quinupristin - Dalfopristin?

A
  • Act seperatly on 50S to inhibit bacteria synthesis
  • Alone = Bacteriostatic; Together = Bactericidal
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9
Q

What is the Mechanism of Resistance for Quinupristin - Dalfopristin?

A
  • Alteration of Ribosomal binding site - encoded by erm
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10
Q

What is the Spectrum of Active for Quinupristin - Dalfopristin?

A
  • Gram (+): Group/Viridan Strep, PRSP, Enterococcus Faecium ONLY [VRE], MRSA, MSSA
  • Gram (-): Limited activity [Neissera…]
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11
Q

What is important to know about the Pharmacology of Quinupristin - Dalfopristin?

A
  • Time-dependent bactericidal Activity with PAE
  • Absorption: Only Parenterally
  • Distrubition: Tissues, Lungs, Bile…
  • Elimination: Hepatic or Biliary Clearance; Dosage Adjustments unnecessary for Renal but Suggested with Hepatic
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12
Q

What are the Clinical Uses for Quinupristin - Dalfopristin?

A
  • ONLY consider what Vancomycin, Linezolid, Daptomycin CANNOT be used
  • Entercoccus Faecium [VRE]
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13
Q

What are some of the interactions with Quinupristin - Dalfopristin?

A
  • Lipid-Lowering Agents [Statins increased Conc.]
  • Immunosuppressive Agents [Increased Conc.
  • Carbamazepine [Increased Conc.]

3A4 Inhibitor so its not going to break down as much

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14
Q

What are some of the Adverse Effects of Quinupristin - Dalfopristin?

A
  • Venous Irritation, GI issues, Myalgias, Arthralgias, Rashes
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15
Q

What are the Oxazolidinones that are used?

A
  • Linezolid and Tedizolid
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16
Q

What is the Mechanism of Action for the Oxazolidinones?

A
  • Binds to 50s near the 30s, inhibiting the 70s; Inhibiting protein synthesis
  • Bacteriostatic
17
Q

What is the Mechanism of Resistance for the Oxazolidinones?

A
  • Alteration of the target site - encoding 23s
  • Cross resistance between the two
18
Q

What is the Spectrum of Activity for the Oxazolidinones?

A
  • Gram (+): Group/Viridan Strep, PRSP, Entercoccus Faecium & Faecalis [VRE], MSSA, MRSA, VISA, VRSA
  • Gram (-): INACTIVE
19
Q

What is important to know about the Pharmacology of the Oxazoildinones?

A
  • Bacteriostatic; T>MIC; PAE
  • Absorption: L = 100% & T = 91%
  • Distribution: Into Tissues [L maybe into CSF??]
  • Elimination: BOTH renal and nonrenal

NO Renal Adjustments

20
Q

What are the Clinical Uses for the Oxazolidinones?

A
  • Where Vancomycin or b-lactams cannot be used
  • VRE Infections [bacteremia or UTI]
  • Nosocomial Pneumonia
  • MRSA
21
Q

What are some of the Drug Interactions with the Oxazoildinones?

A
  • Weak Inhibitors of Monoamine Oxidase
  • Risk of Serotonin Syndrome
22
Q

What are some of the Adverse Effects of Oxazoildinones?

A
  • GI issues, CNS [Headache…], Thrombocytopenia
23
Q

What is the Mechanism of Action for Daptomycin?

A
  • Binds and inserts lipophilic tail into the cell wall; leakaging out contents and causing death
24
Q

What is the Spectrum of Activity for Daptomycin?

A
  • Gram (+): Group/Viridan Strep, PRSP, Enterococcus Faecium & Faecilis [VRE], MSSA, MRSA, VISA, VRSA, LRSA
  • Gram (-): Nope
25
Q

What is important to know about the Pharmacology of Daptomycin/

A
  • Rapid Concentration Dependent Bactericidal Activity
  • Distribution: Tissues [highly protein bound]
  • Elimination: Kidney

DOSAGE adjustment are require in renal issues

26
Q

What are some of the Clinical uses for Daptomycin?

A
  • Where Vancomycin and/or Linezoild cannot be used
  • S. Aureus Bacteremia & Endocarditis
  • NOT used for Pneumonia since is inactived by pulmonary surfactant
27
Q

What are some of the drug interactions with Daptomycin?

A
  • Statins: may increase myopathy
28
Q

What are some of the Adverse Effects if Daptomycin?

A
  • GI issues, Headache, Injection Site Reactions, Rash….
29
Q

What are the Lipoglycopeptides that are used?

A
  • Telvancin, Dalcavancin, Oritavancin
30
Q

What is the Mechanism of Action for the Lipoglyopeptides?

A
  • Affect the making of D-Ala-D-Ala
  • Orita & Tel have same MOA as Dapto
31
Q

What is the Mechanism of Resistance for the Lipoglycopeptides?

A
  • Alteration to peptidoglycan terminus [VanA]
  • Same MOR as Vancomycin
32
Q

What is the Spectrum of Activity for the Lipoglycopeptides?

A
  • Gram (+): Group/Viridan Strep, PRSP, Enterococcus Faecium & Faecilis [VRE], MSSA, MRSA, VISA, VRSA [Ortia mostly]
  • Gram (-): Nope
33
Q

What is important to know about the Pharmacology of the Lipoglycopeptides?

A
  • Concentration Dependent Bactericidal Activity
  • Distribution: into tissues; NOT CSF tho
  • Elimination: Tel = Kidneys; Dala = Poo/pee; Orita = ??

Half Life: T = 7.5h, D = 346h, O = 245h

34
Q

What are the Clinical Effects of the Lipoglycopeptides?

A
  • Where Vancomycin, Linezoild, AND Daptomycin cannot be used
35
Q

What are some of the Drug Interaction for the Lipoglycopeptides?

A
  • None
36
Q

What are some of the Adverse Effects of the Lipoglycopeptides?

A
  • Red Man Syndrome
  • Nephrotoxocity [Have Renal issues, other nephrotoxins, >65 years]
  • QTc prolongation
  • Taste?

PHRM 865: Theraputics V (42 decks)

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