Description

COMPOSITION TARGOTECT 600 Each vial contains Teicoplanin BP...........600mg Excipients................q.s. Combipack with one ampoule of 3ml of Sterile Water for Injections IP Targotect - 400/ Targotect 200mg Each vial contains Teicoplanin BP...........400mg/200mg Excipients................q.s. Combipack with one ampoule of 3ml of Sterile Water for Injections IP Powder for reconstitution and IM/IV use only. PHARMACOLOGY Teicoplanin is a glycopeptide antibiotic that has shown in vitro bactericidal activity against both aerobic and anaerobic grampositive organisms. Teicoplanin inhibits the growth of susceptible organisms by interfering with cell wall biosynthesis at a site different from that affected by â-lactams. It is active against staphylococci (including those resistant to methicillin and other â- lactam antibiotics), streptococci, enterococci, Listeria monocytogenes, corynebacteria and gram-positive anaerobes including Clostridium difficile and peptococci. Bactericidal synergy has been demonstrated in vitro with teicoplanin when combined with aminoglycosides against Staphylococcus aureus and enterococci; synergism has also been demonstrated with imipenem against these organisms. The in vitro combination of teicoplanin and rifampin has shown additive and synergistic effects against Staphylococcus aureus. In vitro synergy with ciprofloxacin against Staphylococcus epidermidis has also been observed. Teicoplanin does not show crossresistance with other classes of antibiotics. Some cross-resistance is observed between teicoplanin and the glycopeptide vancomycin among enterococci. Teicoplanin is taken up by leukocytes and macrophages, and retains antistaphylococcal activity within these cells. Pharmacokinetics: Teicoplanin is administered by parenteral injection. The bioavailability of a single 3-6 mg/kg IM injection is >90%. Following oral administration, teicoplanin is not systemically absorbed from the normal gastrointestinal tract; 40% of the administered dose is present in the feces in a microbiologically active form. Following IV administration of 3-6 mg/kg, the plasma concentration declines with a terminal elimination half-life of about 150 hrs; total plasma clearance ranges from 11.9-14.7 mL/hr/kg. This long half-life allows once a day administration. At 6 mg/kg administered IV at 0, 12, 24 hrs and every 24 hrs thereafter as 30-min infusion, a predicted trough serum concentration of 10 mg/L would be reached by day 4. Predicted steady-state peak and trough serum concentrations of approximately 64 and 19 mg/L, respectively, would be attained by day 28. Teicoplanin distributes readily into the skin (subcutaneous fat) and blister fluid, myocardium, pulmonary tissue and pleural fluid, bone and synovial fluid but not readily into cerebrospinal fluid (CSF). It is 90-95% bound with weak affinity to plasma proteins. Steady-state volume of distribution after 3-6 mg/kg IV ranges from 0.94-1.4 L/kg. When administered parenterally, the metabolic transformation is minor, about 3%; about 80% of administered drug is excreted in the urine. Renal clearance after 3-6 mg/kg IV ranges from 10.4-12.1 mL/hr/kg. INDICATIONS The effectiveness of teicoplanin has been documented in the following infections:- skin and soft tissue infections, urinary tract infections, lower respiratory tract infections, joint and bone infections, septicaemia, endocarditis and peritonitis. CONTRAINDICATIONS Teicoplanin is contraindicated in patients who have exhibited previous hypersensitivity to the drug. WARNINGS AND PRECAUTIONS Teicoplanin should be administered with caution in patients 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 for teicoplanin. Thrombocytopenia has been reported with teicoplanin especially at higher doses than those usually recommended. It is advisable for periodic haematological studies to be performed during treatment. Liver and renal function tests are advised during treatment. Serial renal and auditory function tests should be undertaken in the following circumstances: i) Prolonged treatment in patients with renal insufficiency. ii) Concurrent and sequential use of other drugs, which may have neurotoxic,and/or nephrotoxic properties. These include aminoglycosides, colistin,amphotericin B, cyclosporin, cisplatin, frusemide and ethacrynic acid. Superinfection as with other antibiotics, the use of teicoplanin, especially if prolonged, may result in overgrowth of nonsusceptible organisms. Repeated evaluation of the patient’s condition is essential. If superinfection occurs during therapy, appropriate measures should be taken. Pregnancy Teicoplanin should not be used during confirmed or presumed pregnancy unless a physician considers that the potential benefits outweigh the possible risk. Lactation There is no information about the excretion of Teicoplanin in milk or placental transfer of