Lipoglycopeptides Flashcards
What is Telavancin
semi-synthetic derivative of vancomycin
Telavancin MOA
dual:
- interferes with cell wall synthesis by binding to the d-ala-d-ala terminus of peptidoglycan precursors
- binding to cell membranes causing membrane depolarization and increased membrane permeability
Telavancin spectrum coverage
ONLY GRAM +
dark purple: streptococcus, s. pneumoniae, viridans, MSSA, MRSA, E. faecalis, E. faecium
light purple: VRE
anaerobes: gram +
Dalbavancin spectrum coverage
ONLY GRAM +
dark purple: streptococcus, s. pneumoniae, viridans, MSSA, MRSA, E. faecalis, E. faecium
light purple: VRE
anaerobes: gram +
Oritavancin spectrum coverage
ONLY GRAM +
dark purple: streptococcus, s. pneumoniae, viridans, MSSA, MRSA, E. faecalis, E. faecium
light purple: VRE
anaerobes: gram +
Lipoglycopeptides have poor activity against
enterococcus species with VanA
Telavancin oral absorption
poor, IV only
Telavancin 1/2 life
6-8 hours; long
Telavancin elimination
64-76% renal
Telavancin dosing
usually 24-48 hours depending on CrCl
Telavancin adverse effects
*taste disturbance
*nausea
*vomiting
*foamy urine
renal
rigors
infusion-related
*red man syndrome
*QT prolongation
*contraindicated in pregnancy
clinicians are also cautioned to consider renal function
Telavancin is okay/not okay for pregnancy
NOT OKAY
Telavancin drug interactions
phospholipid agents used in measuring activated partial thromboplastin time, prothrombin time, and coag-based factor X assays
co-administration with heparin is contraindicated
Long acting lipoglycopeptides
Dalbavancin, ortivancin
Long acting lipoglycopeptide MOA
binds to d-ala-d-ala terminus of lipid II in peptidoglycan chain
Dalbavancin is a _____ lipoglycopeptide
semi-synthetic
Dalbavancin has enhanced ____activity
gram +
Dalbavancin has ___MICs compared to vancomycin to s. aureus
lower
Dalbavancin is active/inactive against enterococcus with vanB and vanC
active; potent
Dalbavancin is active/inactive against enterococcus with vanA
inactive
Dalbavancin oral absorption
poor, IV only
Dalbavancin 1/2 life
long 8.5 hours
Dalbavancin elimination
33% renal
PK/PD parameter used for glycopeptides and lipoglycopeptides
AUC:MIC
Dalbavancin is/is not dialyzable
is not
Dalbavancin is dosed
single or two-dose regimens; administer over 30 min
Dalbavancin reconstitutes with
sterile water or 5% dextrose
Dalbavancin adverse reactions
rapid infusion can cause red man syndrome
nausea
headache
diarrhea
Dalbavancin drug interactions
minimal
Oritavancin is a ____lipoglycopeptide
synthetic
Oritavancin has improved activity over
VSE and VRE
Oritavancin also have improved
anchoring to cell membrane and longer 1/2 life
Oritavancin is potent against
MSSA, MRSA, VRE, VSE, streptococcus
remains active against Van A VRE
Oritavancin oral absorption
poor, IV only
Oritavancin 1/2 life
245 hours REALLY LONG
Oritavancin elimination
very slow renal, <5%
Can Oritavancin be dialyzable?
no
Oritavancin PK/PD parameters
AUC:MIC and Cmax: MIC
Oritavancin dosing
1200mg administered over 3 HOURS
Oritavancin reconstitutes with
D5W, incompatible with NS
Oritavancin renal adjustment
no
What can happen if infusion is less than 3 hours for Oritavancin?
infusion-related reactions such as flushing, urticaria, pruritus, and rash
Oritavancin drug interactions
contraindicated with heparin
can prolong prothrombin time and international normalized ratio for up to 12 hours
(monitoring of warfarin is unreliable for up to 12 hours after dose)
Oritavancin adverse effects
nausea
vomiting
headache
more cases of osteomyelitis than in vancomycin
Indications for long acting lipoglycopeptides
avoidance of hospitalization
minimize extended hospitalization/early discharge
prevent need for IV therapy in select patient populations (non compliance or inability to maintain IV access)
Which of the following past medical history should be considered prior to administration of oritavancin?
a. DVT
b. Congestive heart failure
c. asthma
d. hypothyroidism
b since you have to reconstitute with 1000ml D5W
Telavancin has dual mechanism of action in that it acts at the:
a. cell membrane and ribosome
b. cell membrane and cell wall
c. cell wall and ribosome
d. ribosome and DNA gyrase
b
Which medication would you recommend for a homeless patient who has a history of 1 week cellulitis?
Dalbavancin bc can be given as a single dose and doesn’t need to be hospitalized/afford that kind of care
Lipoglycopeptides are bactericidal/bacteriostatic
bactericidal
