Glycopeptides
Glycopeptides is a group of antibiotics composed of glycosylated cyclic
or polycyclic nonribosomal peptides. The most common glycopeptide
antibiotics include vancomycin, teicoplanin, telavancin, bleomycin,
ramoplanin, and decaplanin. Vancomycin has been used in clinical
practice since 1958, teicoplanin from the middle of 1980th years. For the
last10 years the popularity of this group of antibacterial preparation is
increased because of high frequency of infections caused by grampositive microorganisms. Currently glycopeptides are used in the first line
treatment of infections caused by MRSA, MRSE and enterococcal
infections resistant to ampicillin and aminoglycosides.
Action mechanism
Glycopeptides work by interfering with synthesis of bacterial cell wall.
They exert bactericidal action, however, the effect against enterococci,
streptococci and coagulase-negative staphylococcus is bacteriostatic.
Spectrum of activity
Glycopeptides are active against Gram-positive aerobic and anaerobic
microorganisms: Staphylococcus (including MRSA, MRSE),
streptococci, pneumococci (including PRA), enterococci,
peptostreptococci, Listeria, corynebacteria, clostridia (including
C.difficile).
Gram-negative bacteria are resistant to glycopeptides.
The spectrum of activity of all Glycopeptides is almost similar. The
difference are in the level of activity and acquired resistance. For
example, teicoplanin is more active against S.aureus (including MRSA),
streptococci (including S.pneumoniae) and enterococci. Vancomycin is
more active against coagulase-negative staphylococcus. For the recent
1
years, there was found S.aureus with reduced susceptibility to
vancomycin and teicoplanin. The resistance to vancomycin develops
quickly.
Indications

Infections caused by MRSA and MRSE.

Staphylococcal infections in case of allergy to β-lactamase.

Severe infections caused by Enterococcus spp., C.jeikeium,
B.cereus, F.meningosepticum.

Infectious endocarditis caused by streptococci and S.bovis, with
allergies to β-lactamase.

Infective endocarditis caused by E.faecalis (in combination with
gentamicin).

Meningitis caused by S.pneumoniae, resistant to penicillin.

Empirical therapy of life-threatening infections:

Infectious endocarditis of the tricuspid valve or prosthetic valve (in
combination with gentamicin)

Catheter-associated sepsis Posttraumatic or postoperative
meningitis (in combination with cephalosporins III generation or
fluoroquinolones);

Peritonitis in peritoneal dialysis

Neutropenic fever

Antibiotic-associated diarrhea caused by C.difficile

Prevention of wound infection in orthopedic and cardiac surgery in
institutions with high

prevalence of MRSA or allergy to β-lactams;

Prevention of endocarditis in high risk patients
2
Contraindications
Hypersensitivity to any of the medication ingredients

Pregnancy

Breastfeeding
Warnings

Pregnancy. Glycopeptides are not recommended for use during
pregnancy because of high risk of oto-, neuro and nephrotoxicity.

Breastfeeding. Small amounts of Glycopeptides penetrate through
breast milk. Glycopeptides can change intestinal microflora in
children.

Pediatric use. Glycopeptides should be used with caution in
children because of high risk of oto-, neuro- and nephrotoxicity.
Glycopeptides are indicated when benefits of application
overweights possible risks.

Geriatric use. Glycopeptides should be used with caution in elderly
age because of high risk of nephrotoxicity. The dose of the
medications should be adjusted in patients with kidney diseases.

Urinary system. Kidney damage is more common for vancomycin,
The risk of renal failure is increased in patients with a history of
kidney diseases, hypovolemia, prolonged therapy, concomitant
application with nephrotoxic drugs (aminoglycosides, amphotericin
B, polymyxin B, cyclosporine, furosemide, ethacrynic acid).
During the treatment it is necessary to monitor urine outflow,
creatinine blood levels.

Residual concentrations of vancomycin in the blood should not
exceed 10 mg/liter.
3

Ototoxicity and vestibular disorders. Usually ototoxicity is
reversable, in rare cases irreversible deafness may develop.

Intravenous application. In rapid intravenous administration of
vancomycin, hypotension, chest pain, tachycardia, facial flushing
may occur.
Glycopeptides side effects

Urinary system: reversible renal failure (increase of creatinine and
urea blood levels, anuria) The frequency of nephrotoxic reactions
depends on dose, duration of treatment and patient's age. The risk
is increased when glycopeptides are used in combination with
aminoglycosides, furosemide, or ethacrynic acid. Nephrotoxicity
and renal failure are more common for vancomycin than for
teicoplanin

CNS: dizziness, headache

Ototoxicity: loss of hearing, vestibular disorders in patients with
impaired renal function which receive high doses of vancomycin

Local reactions: pain, burning sensation at the injection site,
phlebitis

Allergic reactions: rash, hives, fever, anaphylactic shock

Hematologic reactions: reversible leukopenia, thrombocytopenia

Gastrointestinal tract: nausea, vomiting, diarrhea

Liver: transient increase in activity of transaminases, alkaline
phosphatase
Vancomycin
Generic Name (active ingredient): Vancomycin
Vancomycin is an antibacterial drug, which was derived from
Amycolatopsis orientalis, the drug exerts bactericidal effects to a broad
spectrum of microorganisms.
4
Mechanism of action
The preparation works by blocking the synthesis of the bacterial cell wall,
however the drug does not work on the same fragment of the cell wall
like penicillins and cephalosporins, thus the resistance to these antibiotics
will not affect Vancomycin. The drug binds to the predecessor of the
cellular wall thus causing the cell to lyze. The drug also is able to
penetrate the cellular membrane of the bacteria and selectively inhibit
RNA synthesis. The drug is active against a broad spectrum of grampositive microorganisms. The preparation actively affects only bacterial
cells that are in the process of replication. Most of the gram-negative
bacteria are resistant to the drugs effect. The preparation does not express
cross resistance to other antibiotics.
5