doc. Teicoplanin (Targocid) antibiotic

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It is a glycopeptide antibiotic, produced by fermentation of
Actinoplanes teichomyceticus [mixture of glycopeptide
components which have the same core glycopeptide structure
composed of a linear heptapeptide aglycone, an α-D-mannose and
an acetyl–β-D-glucosamine]
Mechanism of action
It has bactericidal activity; Binds to the terminal D-Ala-D-Ala
sequence of peptides forming the bacterial cell wall and, by
stearically hindering the transglycosylation reaction, inhibits the
formation of peptidoglycan
Spectrum of activity
It is active against both aerobic and anaerobic Gram-positive
bacteria
Species usually sensitive (MIC less than or equal to 16 mg/l):
Staphyloccocus aureus and coagulase negative staphylococci
(sensitive or resistant to methicillin), streptococci, Enterococci,
Listeria monocytogenes, micrococci, Eikenella corradens, group
JK corynebacteria and Gram-positive anaerobes including
Clostridium difficile, and peptococci.
Species usually resistant (MIC superior to 16 mg/l): Nocardia,
asteroides, Lactobacillus spp, Leucononostoc and all Gram-
negative bacteria (since its large Polar molecules thus cannot
penetrate the lipid membrane of Gram-negativebacteria)

2. Bactericidal synergy has been demonstrated in vitro with
aminoglycosides against group D streptococci and staphylococci.
In vitro combinations of teicoplanin with Rifampicin or fluorinated
quinolones show primarily additive effects and sometimes synergy
Clinical uses & Therapeutic dosage
I. [Doses in moderate infection 3 mg/kg while in severe
infection 6 mg/kg I.M or I.V q12hr for 3 doses then q24hr]
II. In potentially serious Gram-positive infections including
those which cannot be treated with other antimicrobial drugs
As Septicaemia, endocarditis, intravenous catheter-associated
inf. and peritonitis related to continuous ambulatory
peritoneal dialysis [10 mg/kg q12hr for 3-5 doses then q24hr]
III. Skin and soft tissue infections
IV. Urinary tract infections
V. Lower respiratory tract infections
VI. Joint and bone infections [12 mg/kg q12hr for 3-5 doses then
q24hr- associated with high risk fever & rash]
VII. For antimicrobial prophylaxis in orthopaedic surgery at risk
of Gram-positive infection (MRSA) [Up to 30 min. before
procedure as I.V. inj. 400mg”UNLICENSED”or as I.V.
Inf.800 mg]
VIII. clostridium difficile inf. (oral application not used for
systemic inf. because of non significant GIT absorption)
[100–200 mg BID for 10–14 days]
IX. treat Gram-positive infections in children from the age of 2
months [For severe infections & neutropenic patients rec-
ommended dose is 10 mg/kg q12hr for the 1st 3 doses;
thereafter 6 mg/kg should be administered each day while
recommended dosage regimen for neonates is a loading of 16
mg/kg followed by 8 mg/kg daily]

3. Pharmacokinetic
Distribution & half life: the plasma level profile after intravenous
administration indicates a biphasic distribution with a terminal
elimination T1/2 of about 150 hr. [It has a longer half-life than
vancomycin (159 hr Vs 11 hr)]
it rapidly penetrates into tissues, including skin, fat blister
exudates, joint fluid, neutrophils (it enhances their bactericidal
activity), and bones and reaches the highest concentrations in the
kidney, trachea, lungs and adrenals while it does not readily
penetrate into the cerebrospinal fluid neither penetrate red blood
cells
Plasma protein binding: Approximately 90-95% teicoplanin is
bound with weak affinity to plasma proteins
Elimination: No metabolites of teicoplanin have been identified;
more than 97% of the administered teicoplanin is excreted
unchanged mainly in the urine.
Effectiveness: Therapeutic response shown within 48-72 hours
among majority of pt., in endocarditis and Osteomyelitis, treatment
for 3 weeks or longer is recommended, though in severe infections,
trough serum concentrations should not be less than 10 mg/l.
Special considerations
For patients with impaired renal function, reduction of dosage is
not required until the fourth day of Targocid treatment.
[In mild renal insufficiency: creatinine clearance between 40 and
60 ml/min or eGFR 30-80 ml/min/1.73 m2, Targocid dose should
be halved, either by administering the initial unit dose every two
days, or by administering half of this dose once a day]
[In severe renal insufficiency: creatinine clearance less than 40
ml/min-eGFR ˂30 ml/min/1.73 m2 and in haemodialysed patients,
Targocid dose should be one third of the normal either by

4. administering the initial unit dose every third day, or by
administering one third of this dose once a day. Teicoplanin is not
removed by dialysis.
In continuous ambulatory peritoneal dialysis: after a single loading
IV dose for 400 mg if the patient
is febrile, the recommended dosage is 20 mg/l per bag in the first
week, 20 mg/l in alternate bags in the second week and 20 mg/l in
the overnight dwell bag only during the third week
Cautions /Adverse reactions & possible interactions
I. It should be administered with caution in pt. known to be
hypersensitive to vancomycin since cross hypersensitivity may
occur. However, a history of the “Red Man Syndrome” that can
occur with vancomycin is not a contraindication to Teicoplanin
Reported anaphylactic reactions include anaphylactic shock, rigors,
urticaria, angioedema, rare reports of exfoliative dermatitis, toxic
epidermal necrolysis, rare cases of erythema multiforme including
SJS. & infusion-related events, such as erythema or flushing of the
upper body, have been rarely reported
II. Eosinophilia, leucopenia, thrombocytopenia, thrombocytosis,
neutropenia and rare cases of reversible agranulocytosis have been
reported, especially at higher doses than those usually
recommended. (It is advisable for periodic hematological studies to
be performed during treatment)
III. Renal and auditory function tests should be undertaken in the
following circumstances: (Prolonged treatment in patients with
renal insufficiency/Concurrent and sequential use of other drugs
which may have neurotoxic and or nephrotoxic properties as
aminoglycosides, cephaloridine, colistin, amphotericin B,
cyclosporin, cisplatin, frusemide and ethacrynic acid)

5. IV. Superinfections: the use of teicoplanin, especially if prolonged,
may result in overgrowth of non-susceptible organisms
V. It is recommended that Teicoplanin should not be used during
confirmed or presumed pregnancy or during lactation unless the
potential benefits outweigh any possible risk (preg. category D).
There is no information about the excretion of teicoplanin in milk
or placental transfer of the drug
VI. Other A.R as Gastro-intestinal: nausea, vomiting,
diarrhoea/Central nervous system: dizziness, headache
VII. Interactions
..Solutions of teicoplanin and aminoglycosides are incompatible when
mixed directly and should not be mixed before injection.
..Liver function: increases in serum transaminases and/or serum
alkaline phosphatase.
..Renal function: transient elevations of serum creatinine, renal
failure.