Khamesipour F, Hashemian S. M, Tabarsi P, Velayati A. A. A Review of Teicoplanin Used in the Prevention and Treatment of Serious Infections Caused by Gram-Positive Bacteria and Compared Its Effects with Some other Antibiotics. Biomed Pharmacol J 2015;8(1)

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Faham Khamesipour¹, Seyed Mohammadreza Hashemian^2*, Ali Akbar Velayati² and Payam Tabarsi³

¹Young Researchers and Elite Club, Shahrekord Branch, Islamic Azad University, Shahrekord, Iran. ²Clinical Tuberculosis and Epidemiology Research Center, National Research Institute of Tuberculosis and Lung Diseases (NRITLD), Shahid Beheshti University of Medical Sciences, Tehran, Iran. ³National Research Institute of Tuberculosis and Lung Diseases, Masih Daneshvari Hospital, Shahid Beheshti University of Medical Sciences, Tehran, Iran. Correspondence author: E-mail:Dr_Faham@yahoo.com

DOI : https://dx.doi.org/10.13005/bpj/641

Abstract

Teicoplanin is an antibiotic used in the prevention and treatment of serious infections caused by gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcusfaecalis. It is a semi-synthetic glycopeptide antibiotic with a spectrum of activities similar to vancomycin. Its mechanism of action is inhibition of bacterial cell wall synthesis:Teicoplanin is marketed by Sanofi Aventis Coperation under the brand name of Targocid. It has been shown that oral administration of teicoplanin is effective in the treatment of Pseudomembranous colitis and Clostridium difficile-associated diarrhoea, with comparable efficacy to vancomycin.The effectiveness of this antibiotic is associated with its carbon chain length.It’s tried in this review article to introduce teicoplanin synthases, structure and its structure effect on treatment and also introduce the advantages of teicoplanin in bacterial infection treatment and compared its effects with some other antibiotics like vancomycin and linezolid.Based on the above data, it can be concluded that Teicoplanin usage, specially intervenes injection of it, is a successful antibiotic treatment against bacterial infections caused by Gram-positive bacteria, particularly methicillin-resistant Staphylococcus aurous (MRSA). The teicoplanin effect is directly related to the length of its carbon chain. It was shown that treatment with combination of teicoplanin and vancomycin or teicoplanin and linezolid have more influence over the treatment process. The most important advantage of teicoplanin usage in treatments is its lower side effects on patients than other antibiotics.

Keywords

carbon chain; gram-positive; methicillin-resistant Staphylococcus aureus (MRSA); Teicoplanin

Introduction

Chemical Structure

In fact,Teicoplanin is composed of several chemicals,5large parts called teicoplanin A₂-1 through A2-5 and 4 small parts called teicoplanin R_S-1 through R_S-4 and has aglycopeptide core called teicoplanin A₃-1[1].This ring binds to mannose and N-acetyl glucosamine[2].The major and minor components also contain a third carbohydrate moiety-β-D-glucosamine and differ only by the length and conformation of a side chain attached to it[3, 4]. The overall structure of this compound can be seen in Figure 1.

Teicoplanin Biosynthesis

Teicoplanin refers to a set of natural products isolated from the fermentation broth of a strain of Actinoplanesteichomyceticus, consisting of five subcategories[5]. These subcategories possess a common aglycone, or core, composed of seven amino acids bound by peptide and ether bonds to form a four-ring system and differ by the fatty acyl side-chain attached to the sugar[6]. The origin of these seven amino acids in teicoplanin biosynthesis was studied by ¹H and ¹³C nuclear magnetic resonance. The resultsshow that amino acids AA1, AA2, AA4, AA5, and AA6 are derived from tyrosine, and amino acids AA3 and AA7 are derived from acetate. Specifically, teicoplanin contains 4-hydroxyphenylglycine and 3,5-dihydroxyphenylglycine residues, a chlorine atom attached on each of the tyrosine residues, and three sugar moieties, including N-fatty acyl-β-D-glucosamine, N-acetyl-β-D-glucosamine, and D-mannose[7].

Gene Cluster

The investigation of teicoplanin biosynthesis gene cluster shows OFR 49 in the path of biosynthesis, transfer, resistance, and regulation of gene expression[8, 9].OFR 35 identified in this path is similar to gene clusters relevant to in other glycopeptide genes. The function of each of these genes is described by Li and co-workers[10].

Heptapeptide Backbone Synthesis

Analysis indicated tyrosine and three types of non-proteinogenic amino acids, (S)-4-hydroxyphenylglycine, 3,5-dihydroxyphenylglycine, and β-hydroxytyrosine as the glycopeptidebuilding blocks of teicoplanin [11]. In total, six of the seven total amino acids composing teicoplanin backbone are composed of nonproteinogenic or modified amino acids[12]. Cooperation and activity of eleven enzymes are responsible for preparation and synthesis of these six residues. Teicoplanin contains two chlorinated positions, 2 (3-Cl-Tyr) and 6 (3-Cl-β-Hty) [6, 10, 13]. Halogenase ORF8* has been proposed to have a role in catalyzing the halogenation process of these amino acids[14]. It seems that chlorination process occurs at early stages in Teicoplanin biosynthesis and prior to phenolic oxidative coupling, with the possibility of tyrosine or β-hydroxytyrosine being the substrate of chlorination[15].The biosynthesis of heptapeptideroot is performed by four nonribosomal peptide synthetases called TeiA, TeiB, TeiC, and TeiD[5, 16]. Each module has a domain for amino acid selection and activation through aminoacyl-AMP. The catalytic domain in modules 3 and 4 of non-ribosomal peptide synthetase are linearly and activated by (S)-4-hydroxyphenylglycine and 3, 5-dihydroxyphenylglycine. In addition to these modules for amino acid selection and activation, each module has a thiolation domain modified with phosphopantetheine to provide a thiol for covalent aminoacyl-S-enzyme formation[17, 18].

Modification After Heptapeptide Backbone Formation

Once the heptapeptide backbone has been formed and synthesized, the process of catalyzing the linear structure is begun[19].Studies on gene disruption indicate that cytochrome P450 oxygenaseis an enzyme performing the coupling reactions. OxyB has been suggested to form the first ring with coupling residues 4 and 6. Then, OxyA couples residues 2 and 4, followed by the formation of a C-C bond between residues 5 and 7 by OxyC. Fourth enzyme catalyzes the coupling of residues 1 and 3 that for this purpose,OxyB/OxyA/OxyCplay a role[19, 20].

The process of specific glycosylation occurs after the formation of the heptpeptideaglycone[21]. Given to the data collected for glycosylation of the teicoplanin aglycone it is shown that three separate glycosyltransferases are required[22]. Two of these glycosyltransferases are involved in the addition of the N-fatty acyl-β-D-glucosamine and N-acetyl-β-D-glucosamine units. The third enzyme, which is a mannosyltransferase, is responsible for the addition of the D-mannose unit onto residue 7. The fatty acyl chain is connected by amide bond to the glucosamine moiety by the action of an acyl transferase. In addition to glycosylation, some genes have been suggested to code for deacetylases[23, 24]

Summary of Antibacterial Activity of Teicoplanin

Previous studies have indicated high inhibitory activity of Teicoplanin against Staphylococcus aureus, as well asthoseresistant tomethicillin andoxacillin[25, 26].The general similarity of teicoplanin and vancomycin are also shown. All Streptococci are sensitive to Teicoplanin[27], although the relative susceptibility of coagulase-negative staphylococci to teicoplanin and vancomyc in varied. Studies have shown that Clostridium species such as C. diffilce, C.perjringense, Peptostreptococcus species, Propionibacteriumacens, Corynebacteriumjeikeium and resistant species of Corynebacterium group D2are sensitive to low concentrations of Teicoplanin[28, 29].

The minimum bactericidal concentration(MBC) forteicoplanin is usually less than or equal to 2 dilutions higher than the minimum inhibitory concentration 90% (MIC₉₀)for Streptococcuspneumoniae, S. aureus, S.epidermidis and in some studies for some samples of coagulase-negative staphylococci[25, 30]. The in vitrobactericidalactionfor the teicoplanin, similar tovancomycin, is slow.Teicoplanin in combination with aminoglycosides shows synergistic inhibitory activity against most bacteria ofS. aureus, coagulase negative staphylococci and enterococci.Susceptibility of E. faecium to various antibiotics has been shown a significant increase in resistance to penicillin Gandgentamicin, but susceptibility to teicoplanin and vancomycin is stable. In animal models of gram-positive endocarditis, teicoplanin and vancomycin similarly, reduction of bacterial titers in cardiac valvularvegetations was examined a few hours after drug administration, but 10 days after treatment, higher percentage of vegetation by teicoplanin was free of contamination[31-33].

Introducing The Pharmacokinetic Properties Of Teicoplanin

Result of injecting 6 mg/kg teicoplanin in the mean peak serum concentration at 30 minutes and 4 hours after intravenous and in tramuscular injection has been reported 43 and 12 mg/l, respectively. Insteady state, the concentration of intravenous teicoplanin after intravenouslyinjecting 6 and 12 mg/kg after 12 hours has been reported 14 and 23 mg/l, respectively. And the same results were obtained after 24 hours. Teicoplanin absorption rate after intramuscular administration is equivalent to the rate after intravenous injection. It seems that injecting a dose of 15 mg/kg is needed after a dose of 8mg/kgin day thereafter to maintain the concentration above 10 mg/l of teicoplanin in neonates[34].

Apparent volume of distribution at steady state after intravenous injection of 6 to 15mg/kg teicoplanin was approximately0.8 to 1.6kg/l that was higher than reports in previous studies in which serum samples were collected for a short period. The average concentration of teicoplanin in atrial appendage was 8 / 2-7 / 3 times the average concentration simultaneously obtained in serum, and the highest concentrations in the heart and pericardium tissue was 4 hours after an intravenous dose of 800 mg. Penetration into the cerebrospinal fluid is minimal after in travenous administration, but drug concentrations in the cerebrospinal fluid is reported more than 40 milligrams per liter after intravenous administration of teicoplanin at a dose of 20mg per 24 or48 hours[35, 36].

Body metabolism rate for teicoplanin is slight (about 3%). Total body clearance of teicoplanin after intravenous administration of3 to30 mg/kgin healthy volunteers is in the range 10-13 ml/h/kg. Renal clearance is 8 to 12 ml/h/kg which implies that it is almost eliminated by renalmechanismsare.On average, studies in which the duration of sample collection is 3 weeks after the last dose have shown that elimination half-life of teicoplanin will be 155-168 h after intravenous administration and 182 hours after the intramuscular injection.

Total body and renalclearanceratesforteicoplanin correlates with creatinine clearance and reduces inpatients with impaired renal function. Teicoplanin cannot be removed by hemodialysis cycle, regardless of the dialysis membrane[37, 38].

Inpatients with a history of intravenous drug use treated with teicoplanin for bacterial endocarditis, the average amount of total body andrenal clearanceis reported higher and more diversified than that in healthy subjects and elimination half-life is reduced[39, 40].

An Example of Teicoplanin Treatment Effects

Studies relevant to the teicoplanin effects in treating bacteraemia and intravascular infections in patients without neutropenia stay largely non-comparative. Comparative investigations have shown that daily administration of 6 mg/kg teicoplanin has the same effect with12-hour administration of 15 mg/kg vancomycin. Daily use of only 400-800 mg teicoplanin cures 84 to 93% of patients with bacteraemia caused mostly byS.aureus clinically and bacteriologically and is successful in 90 to 100% of patients with streptococcalorenterococcalendocarditis[41].

Recovery is obtained in 89 to 100% of patients with skin and soft-tissue infections (caused mainly by S. aureusorS.epidermidis) treated with 200 to 800 mg teicoplanin once a day intravenouslyor intramuscularly [42, 43].

Non-comparative tests of teicoplanin (usually 6 mg/kg once daily) in patients with acute/ chronic Osteomyelitis or Septic Arthritis caused by gram-positive bacteria, have led to clinical cure in 83 to 100% of patients[44, 45].

A combination of teicoplanin and ciprofloxacin is significantly more effective than either ciprofloxacin or ceftriaxone alone in relieving respiratory tract infections.  In non-comparative studies, teicoplaninalone results in clinical cure or improvement in approximately 91% of patients with respiratory tract infections. In the treatment of Clostridium difficile resulting in severe diarrhea and colitis, oral administration of 100 mg teicoplanin twice a day and 500 mg vancomycin four times a day can improve 96% and 100% of patients, respectively[46-48].

Once teicoplanin is used as the initial treatment in patients with cancer and neutropenia, its effect is similar to that of vancomycin. Teicoplanin was associated with a more tolerant with a lower incidence of super infection caused by Candida species, indicating that teicoplanin is a viable alternative to vancomycin. Adding teicoplanin to piperacillinplusamikacin has no clinical effectiveness. Controversy still remains over the need for these drugs, from drugs election and timing for the introduction of antibiotics to experimental diets that all depends on environmental conditions[49-51].

While no improvement was observed in patients, they were prescribed with teicoplanin, and positive results were shown in patients with gram-positive bacterial infection.Teicoplanin was effective for secondary treatment of patients who had a negative response to experimental treatment with either ceftazidime alone or in combination with amikacin, piperacillinplusamikacin, or one of the cephalosporiumandaminoglycoside antibiotics[52, 53].

Inpatients undergoing hip and knee arthroplasty, only intravenous dose of 400 mg teicoplanin has a similar effectiveness with 4 post-surgery doses of cefamandole or 5 post-surgery doses of cefazolinin anesthesia induction. Clinical experience with teicoplaninis limited in infants and children. However, preliminary data in children with sepsis, upper and lower respiratory tract infection, skin or soft tissue infection and in febrile children with neutropenia shows that 6 to10mg/kg teicoplanin once a day is effective in the treatment of gram-positive infections[54-56].

As a result of the efficiency of teicoplanin against gram-positive infections, once-daily intravenous orintramuscular injection of teicoplanin is suitable for out patients.  After the success ofteicoplanin in outpatients or patients at first hospitalization and thereafter, it showed success in cares after discharge. Teicoplanin has been successfully used to treat skin and soft tissue infection, bone and joint infection, and mediastinitisaftercoronary artery bypass surgery[57].

Comparing the Effect of Teicoplanin and Linezolid

Linezolid is the only commercially available oxazolidinone using for gram-positive infections, although, a few papers are published particularly on its use in acute illnesses [58, 59]. Therefore, a prospective randomized study was conducted to compare linezolid with glycopeptide antibiotic, teicoplanin, for suspicious or proven treatment of gram-positive infections in intensive care unit population by Cepedaet al.[58].

In this regard, a perspective double-blind double-dummy study was designed. The patients were randomly divided into two groups: A) patients who received intravenous linezolid(600 mg /12hours) plus intravenous placebo-teicoplanin (one doses every 12hours and after three injections, one doseper24hours). B)  Patients who received teicoplanin(3 injections per 12 hours at a dose of 400 mg and then one injection per 12 hours) plus placebo-linezolid (one dose per 12 hours and after three injections, one doseper 24 hours).   Other antibiotics were used in combination with testing drugs in experimental treatment. Clinical and microbiological evaluation of the first week was done daily and then, in day 8 and 21.

In this study, 100 patients received linezolid plus placebo-teicoplanin and 102 patients received teicoplanin plus placebo-linezolid. Figures obtained from population were similar in both groups. At the end of treatment, clinical success [71 (78.9%) linezolid versus 67 (72.8%) teicoplanin] and microbiological success [49 (70.0%) versus 45 (66 .2%)] were similar. Side effects and the success rate of short-term and long-term follow-up were also the same. Linezolid was superior in the initial distance against the colonization of methicillin-resistant Staphylococcusaureus (end of treatment, 51.1% versus 18.6%, P = 0.002). The results of researches indicated two MRSA samples less sensitive toteicoplanin. The results of this study showed that linezolid has a similar effectiveness with teicoplanin in the treatment of infections caused by gram-positive bacteria. The difference is that MRSA short-term clearance achieved by linezolid represents its better penetration in to the skin and mucosa[59].

Figure 1: Teicoplanin core. Click here to View figure

Comparing the Effect of Teicoplanin and Vancomycin

Teicoplanin and vancomycin are two commonly used treatments forgram-positive bacterial infections, especially methicillin-resistant Staphylococcusaureus (MRSA)[60, 61]. There is an uncertainty about the effects ofteicoplanin compared with vancomycin in their effectiveness on renal function. Some previous studies have shown that   teicoplaninislessnephrotoxicthanvancomycin. To evaluate the efficacy and safety of vancomycin in comparison with teicoplanin in patients with proven or suspected infection, Cavalcanti et al., searched articles published in different languages in association with comparing the efficacy of teicoplanin and vancomycin. They evaluated independently methodological quality and data extracted using a standardized data extraction form in various articles. They gathered information from 24 independent studies and concluded that teicoplanin reduces the risk of nephrotoxicity compared with vancomycin (risk ratio 0.66, 95% confidence interval 0.48 to 90).They reported the effect of teicoplanin and vancomycin the same for clinical improvement (RR 1.03, 95% CI 0.98 to 1.08), microbiological cure (RR 0.98, 95% CI 0.93 to 1.03) and mortality(RR 1.02, 95% CI 0.79 to 1.30). Side effects including skin rash (RR 0.57, 95% CI 0.35 to 0.92),red man syndrome(RR 0.21, 95% CI 0.08 to 0.59)and total side effects (RR 0.73, 95% CI 0.53 to 1.00) resulted from administrating teicoplanin compared to vancomycin were observed less. The risk of nephrotoxicity with teicoplaninin patients with (RR 0.51, 95% CI 0.30 to 0.88)or with out(RR 0.31, 95% 0.07 to 1.50)aminoglycosides has been less.

Finally and generally, these studies showed that, teicoplanin and vancomycin are effective in treating patients with provenor suspected infection. Yet, incidence of adverse effects, including nephrotoxicity with teicoplanin administration will be lower. Since the group was not able to assess patients with acute kidney injury requiring dialysis, it did not become clear that different effects on kidney function should be under the impression of what antibiotic is prescribed.Although it seems logical that teicoplanin to be prescribed for patients with a high risk of AKI requiring dialysis due to the lower risk of nephrotoxicity resulted from antibiotic usage[31].

Based on the above data, it can be concluded that Teicoplanin usage, specially intervenes injection of it, is a successful antibiotic treatment against bacterial infections caused by Gram-positive bacteria, particularly methicillin-resistant Staphylococcus aurous (MRSA).The teicoplanin effect is directly related to the length of its carbon chain. It was shown that treatment with combination of teicoplanin and vancomycin or teicoplanin and linezolid have more influence over the treatment process. The most important advantage of teicoplanin usage in treatments is its lower side effects on patients than other antibiotics.

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