Lipoglycopeptides

ByBrian J. Werth, PharmD, University of Washington School of Pharmacy
Reviewed/Revised May 2024
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antibacterials related to glycopeptides (eg, vancomycin).

Lipoglycopeptides have bactericidal activity exclusively against gram-positive bacteria. These antibiotics inhibit bacterial cell wall synthesis and disrupt cell membrane integrity.

Pharmacokinetics of Lipoglycopeptides

Lipoglycopeptides are not absorbed orally and are available only as IV formulations. Lipoglycopeptides penetrate well into pulmonary epithelial lining fluid and skin blisters.

Telavancin is excreted by the kidneys, so the dose must be adjusted in patients with renal insufficiency.

Indications for Lipoglycopeptides

Lipoglycopeptides are broadly active against gram-positive bacteria, including

vancomycin-resistant enterococci (VRE) strains that harbor the vanADalbavancin, oritavancin, and telavancin have activity against vanB VRE. All three lipoglycopeptides are active against S. aureus and S. epidermidis regardless of their susceptibility to methicillin. Only oritavancin is active against vancomycin-resistant S. aureus.

hospital-acquired and ventilator-acquired bacterial pneumonia caused by sensitive isolates of S. aureus.

Contraindications to Lipoglycopeptides

Lipoglycopeptides are contraindicated in patients who are allergic to them. They should be used with care in patients who are allergic to vancomycin or other glycopeptides because cross-reactivity is possible.

Use of Lipoglycopeptides During Pregnancy and Breastfeeding

Lipoglycopeptides have had some adverse effects on fetal development in animals; safety data in pregnant women are limited. Lipoglycopeptides should be used during pregnancy only if the potential benefit to the patient outweighs the potential risk to the fetus.

There are no data regarding excretion in breast milk in humans, but lipoglycopeptides are known to be excreted in the breast milk of rats.

Adverse Effects of Lipoglycopeptides

Common adverse effects of lipoglycopeptides include

  • Nausea and vomiting

  • Taste disturbance

  • Foamy urine

Telavancin interferes with urine protein assays.

Significant adverse effects include

  • Increased mortality in patients with pre-existing moderate/severe renal impairment (creatinine clearance ≤ 50 mL/minute) who were treated with telavancin for hospital-acquired bacterial pneumonia/ventilator-associated bacterial pneumonia versus vancomycin

  • A histamine-mediated pruritus and flushing of the face, neck, and shoulders, similar to

  • Nephrotoxicity, which may occur more often with telavancin than with vancomycin but has not been associated with dalbavancin or oritavancin

  • With telavancin, QTc prolongation

Nephrotoxicity with telavancin is more likely in patients with known kidney dysfunction, disorders that predispose to kidney dysfunction (eg, diabetes, hypertension, heart failure), or use of potentially nephrotoxic medications. Renal function should be assessed before starting telavancin and monitored at least every 48 to 72 hours.

Pruritus and flushing associated with rapid infusion of lipoglycopeptides can be prevented by infusing at a slower rate if the patient develops these signs.

QTc prolongationtelavancin should be used with caution or not be used in patients taking medications that prolong the QT interval. Telavancin should not be used in patients with congenital long QT syndrome, known QTc prolongation, uncompensated heart failure, or severe left ventricular hypertrophy (patients with these disorders were excluded from the clinical trials).

Dosing Considerations for Lipoglycopeptides

Drugs Mentioned In This Article
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