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Drug Therapy Indian Pediatrics 2001; 38: 372-375 |
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Teicoplanin |
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Teicoplanin is a narrow spectrum antibiotic, which was formerly known as teichmycin A2(1). It belongs to group glycopeptides and resembles vancomycin in its structure. It is produced by Actinoplanes teichomyceticus. It interferes with cell wall synthesis by inhibiting polymerization of peptidoglycan(2).
Teicoplanin is active only against Gram-positive organisms. It acts against both methicillin sensitive and methicillin resistant Staphylococcus aureus (S. aureus). It is as efficacious as vancomycin against these organisms. The efficacy of teicoplanin against Staphylococcus aureus can be improved by addition of aminoglycosides for synergistic effect. Teicoplanin is more efficacious than vancomycin for some of the streptococci especially enterococci. Teicoplanin is also effective against Listeria monocytogenes, Corynebacterium spp., Clostridium spp., and anaerobic Gram-positive cocci(2).
Teicoplanin has bioavailability of 90-95% and its half-life is as long as 100 hours in patients with normal renal functions. Therefore, once daily dosage is sufficient for most of the infections. It is rapidly and extensively absorbed from muscle and peritoneal cavity, but very poorly from gastrointestinal tract. It penetrates slowly and poorly into cerebrospinal fluid. but relatively rapidly and effectively in synovial and pleural fluid and soft tissue(3). Its main route of excretion is through kidneys, so dosage needs to be modified in patients with renal insufficiency(2). In renal insufficiency, dose needs to be modified according to creatinine clearance. If creatinine clearance is less than 20 ml/min, dose should be reduced to 1/10th of the recommended dosage. If creatinine clearance is 20-50 ml/min. dose should be reduced to half(4).
Both these drugs have similar chemical structure, mechanism of action and clinical spectrum of activity. Teicoplanin has a longer half-life, so can be given once daily, whereas vancomycin needs to be given in 3-4 divided doses. Unlike vancomycin, teicoplanin can be used by intramuscular route. Teicoplanin is well tolerated intramuscularly for as long as 4 weeks(1).
Skin rash is the main side effect with teicoplanin(2). Liu et al. have shown that vancomycin is more nephrotoxic than teicoplanin(5). Toxicological studies have shown that teicoplanin does not cause oto-toxicity, whereas vancomycin is a potentially ototoxic drug(6). However Bibler et al. have reported an asymptomatic decrease in high frequency auditory threshold in one patient, one week after discontinuation of teico-planin(7). Dagon et al. used teicoplanin in 64 children and observed transient decrease in white blood cell count in 4 patients, elevation of liver transminase in 3 patients and elevation of creatinine in 1 patient. All these side effects were mild and transient and did not necessitate cessation of therapy(8). Drug fever, hyper-sensitivity reactions, eosinophilia and bronchospasm are other side effects reported with teicoplanin(2,7,9). In some individuals, teicoplanin can cause mild long lasting pain at the site of injection(6). Bibler et al.(7) have shown in a study that there was no episode of catheter related phlebitis with teicoplanin, whereas it is a common occurrence with vancomycin(10).
Teicoplanin can be used for methicillin sensitive as well as methicillin resistant Staphylococcus aureus(5,8). Dagon et al. have concluded from their study that teicoplanin is a safe and efficacious drug for outpatient and inpatient treatment of serious Gram positive infections in children including S. aureus and Streptococcus pyogenes(8). Auwera et al. used vancomycin in 71 patients with immuno-compromised patients having Gram-positive bacterial infections. Most common organisms were S. epidermidis followed by S. aureus. Microbiological cure was achieved in 23/35 in teicoplanin group and 28/36 in patients treated with vancomycin(11). Resistance of S. aureus to teicoplanin has been reported during therapy of endocarditis. The exact mechanism of this resistance is not clear, but this resistance was not plasmid mediated and was also not associated with changes in the cytoplasmic membrane proteins(12). Goldstein et al. studied the distribution of teicoplanin and vancomycin resistant strains among coagulase negative staphylococci (CONS) and have shown that teicoplanin is less effective than vancomycin against CONS and the most resistant strain is S. hemolyticus(13). Del Alamo et al. also studied antimicrobial susceptibility of 239 CONS from blood cultures. In their study, teicoplanin resistance was found in 9 isolates. However, these isolates remained susceptible to vancomycin(14). These studies suggest that teicoplanin is an effective drug for CONS, however, resistant is more common with teicoplanin as compared to vancomycin. Teicoplanin is an effective drug for serious entercoccal infections. However, it should be combined with aminoglycosides for bactericidal action. Some strains of enterococci resistant to vancomycin are also resistant to teicoplanin. Vancomycin resistant enterococci having Van A phenotype also determine resistance to teicoplanin(15). However, Van B resistant enterococci remains susceptible to teicoplanin, because teicoplanin is probably a poor inducer of enzymes responsible for the cell wall synthesis(2). Menichetti et al. have shown that teicoplanin is as efficacious as vancomycin as empirical antibiotic regimen for febrile neutropenic patients with hematologic malignancies(16). De Lalla et al. have shown that oral teicoplanin is efficacious and safe in the treatment of pseudomembranous colitis and C. difficile associated diarrhea(17). Intrathecal teicoplanin has been used successfully along with other parenteral antibiotics in shunt infections caused by organisms like S. aureus, S. epidermidis and Enterococcus fecalis(18,19).
The recommended dosage of teicoplanin by manufacturer is 10 mg/kg by intravenous route every 12 hourly for first three doses, then 6 mg/kg/day by inramuscular or intravenous route. For neonates, dosage is 16 mg/kg for first day followed by 8 mg/kg/day and dosage should be given as intravenous infusion over 30 minutes. Teicoplanin is available as Targocid in 200 mg and 400 mg vials by Hoechst Marion Roussel Company. The cost of 200 mg vial is Rs. 730 and 400 mg vial is Rs. 1200. Oral preparation of teicoplanin is not available in India. Competing interests:
None stated.
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