Gram (+) Antibiotics Flashcards

1
Q

Vancomycin Mechanism of Action

A

Inhibits synthesis and assemble of bacterial cell wall (@ D-alanyl-D-alanine portion of wall, diff than B-Lactam site) ; prevents cross-linking and further elongation of peptidoglycan

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2
Q

Vancomycin- Bactericidal or Bacteriostatic?

A

Bactericida (time-dependent), except Enterococcus (bacteriostatic)

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3
Q

Mechanism of Resistance for Vancomysin

A

Modification of the D-alanyl-D-alanine vancomycin-binding site in VRE and VRSA

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4
Q

Vancomycin Spectrum of Activity

A
GRAM (+) AEROBIC AND ANAEROBIC BACTERIA
MSSA
MRSA
COAGULASE (-) STAPH
C-DIF
PRSP (Pen-Resistant Strep. pneumo)
others

NO ACTIVITY AGAINST GRAM (-) AEROBES OR ANAEROBES

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5
Q

Vancomycin Absorption

A

Negligible oral absorption, thus INTERMITTENT IV INFUSION IS PREFERRED ROUTE OF ADMINISTRATION

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6
Q

Vancomycin Distribution

A
  • TAKES 1 HOUR TO DISTRIBUTE FROM PLASMA INTO TISSUE
  • widely distributed, esp. to ADIPOSE
  • TOTAL BODY WEIGHT should be used for dosing
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7
Q

Vancomycin Elimination

A

Eliminated by kidney

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8
Q

Vancomycin Half-Life

A

1/2 life progressively increases with decreases in renal function
- in end stage renal disease, 1/2 life= 7-14 days

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9
Q

Vancomysin Serum Concentration Monitering

A

Peak should be drawn 60 MINUTES AFTER THE END OF INFUSION

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10
Q

Vancomysin Clinical Uses

A
MRSA
B-LACTAM ALLERGIC PATIENTS
PRSP
MODERATE TO SEVERE C-DIF (oral)
endocarditis or surgical prophylaxis in select cases
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11
Q

Vancomysin Adverse Effects

A
Red-Man Syndrome
Nephrotoxicity (Mississippi Mud!) & Ototoxicity
Dermatologic
Hematologic
Thrombophlebitis, interstitial nephritis
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12
Q

Red-Man Syndrome

A
  • Adverse effect of Vancomysin
  • related to RATE of IV infusion
  • flushing, pruruitus, erythematous rash on face, neck, and upper torso w/i 5-15 min.
  • resolves spontaneously after discontinuation
  • can lengthen infusion time
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13
Q

Oxazolidinones

A

Developed in response to need for abx w/ activity against resistant Gram (+) organisms, namely MRSA, VISA (GISA), VRE
Linezolid is the only drug in this class.
AVAILABLE PO AND IV.

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14
Q

Oxazolidinones/Linezolid Mech of Action

A

INHIBITS PROTEIN SYNTHESIS

binds to 50S RIBOSOMAL SUBUNIT, CAUSING INHIBITION OF 70S INITIATION COMPLEX

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15
Q

Oxazolidinones/Linezolid- Bactericidal or Bacteriostatic?

A

Bacteriostatic (time-dependent bacteriocidal against some bacteria)

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16
Q

Mechanism of Resistance against Oxazolidinones/Linezolid Abx

A

alteration of ribosomal subunit target site, has rarely emerged w/ Enterococcus and S. aureus

17
Q

Oxazolidinones/Linezolid Spectrum of Activity

A
Gram (+):
MSSA
MRSA
VANCOMYCIN-RESISTANT STAPH AUREUS
PRSP
E. FAECIUM AND FAECALIS, INCLUDING VRE
others

Relatively inactive against Gram (-) aerobes and not used with Atypical Bacteria

18
Q

Oxazolidinones/Linezolid Pharmacology

A

TIME-DEPENDENT BACTERICIDAL ACTIVITY is major predictor of efficacy
SIGNIFICANT PAE exists for Gram (+) organisms

19
Q

Oxazolidinones/Linezolid Absorption

A

RAPIDLY & COMPLETELY ABSORBED ORALLY W/ A BIOAVAILABILITY OF 100%

20
Q

Oxazolidinones/Linezolid Distribution

A

readily distributes into well-perfused tissues

CSF PENETRATION ~30%

21
Q

Oxazolidinones/Linezolid Elimination

A

eliminated by renal and non-renal routes

22
Q

Oxazolidinones/Linezolid Clinical uses

A
  • VERY EXPENSIVE
  • SERIOIUS/COMPLICATED INFECTIONS CAUSED BY RESISTANT GRAM POSITIVE INFECTIONS, esp. where vancomycin can’t be used
  • VRE BACTEREMIA OR UTIs
  • NOSOCOMIAL PNEUMONIA DUE TO MSSA OR MRSA
23
Q

Oxazolidinones/Linezolid Drug Interactions

A

Serotonin Syndrome w/ SSRIs (& MAOIs)

24
Q

Oxazolidinones/Linezolid Adverse Effects

A

LACTIC ACIDOSIS
PERIPHERAL NEUROPATHY
THROMBOCYTOPENIA OR ANEMIA 2-4%
headache

25
Q

Lipopeptides

A

Developed in response to need for abx w/ activity against Gram (+)s
Daptomycin is only drug discussed in this class.

26
Q

Lipopeptides/Daptomycin Mech of Action

A

Binds to bacterial membranes and causes rapid depolarization, causing inhibition of protein, DNA, and RNA synthesis

27
Q

Mechanism of Resistance to Lipopeptides/Daptomycin Abx

A

rarely reported in VRE and MRSA due to altered cell membrane binding

28
Q

Lipopeptides/Daptomycin Spectrum of Activity

A
Excellent Gram (+) Activity
MSSA
MRSA
VRSA
PRSP
E. FAECIUM AND FAECALIS, INCL. VRE

relatively inactive against Gram (-)

29
Q

Lipopeptides/Daptomycin- Bactericidal or Bacteriostatic?

A

RAPID, CONCENTRATION-DEPENDENT BACTERICIDAL ACTIVITY

30
Q

Lipopeptides/Daptomycin Pharmacology

A

only available parentally

31
Q

Lipopeptides/Daptomycin Distribution

A

readily distributes into well-perfused tissue, protein binding= 90%

32
Q

Lipopeptides/Daptomycin Elimination

A

excreted primarily by the kidneys, DOSAGE ADJUSTMENTS REQUIRED for renal insufficiency

33
Q

Lipopeptides/Daptomycin Clinical Uses and Dosing

A

COMPLICATED SKIN/SKIN STRUCTURE INFECTIONS CAUSED BY MSSA, MRSA, S. PYOGENES, ETC.)
SHOULD NOT BE USED FOR PNEUMONIA

34
Q

Lipopeptides/Daptomycin Adverse Effects

A
MYOPATHY & CPK ELEVATION
Gastrointestinal
Headache
Injection site reactions
Rash
35
Q

Lipopeptides/Daptomycin Drug Interactions

A

HMG CoA-reductase inhibitors (i.e. Statins)- may lead to increased incidence of myopathy b/c statins also have this side effect