Teicoplanin

(BAN, USAN, rINN)
Teicoplanin Chemical formula
Synonyms: A-8327; DL-507-IT; L-12507; MDL-507; Teichomycin A 2 ; Teicoplanina; Téicoplanine; Teicoplaninum; Teikoplaniini; Teikoplanin.
Cyrillic synonym: Тейкопланин.

💊 Chemical information

CAS — 61036-62-2 (teichomycin); 61036-64-4 (teichomycin A 2 ).
ATC — J01XA02.
ATC Vet — QJ01XA02.

Description.

A glycopeptide antibiotic obtained from cultures of Actinoplanes teichomyceticus or the same substance obtained by any other means.

Pharmacopoeias.

In Jpn.

💊 Adverse Effects and Precautions

Fever, skin rash and pruritus, and occasional bronchospasm and anaphylaxis have been reported with teicoplanin, but, in comparison with vancomycin, it appears to be better tolerated when given by rapid intravenous injection and, although erythema and flushing of the upper body have occurred, the ‘red-man syndrome’ has been reported less often. In addition, unlike vancomycin, teicoplanin does not appear to cause tis sue necrosis and can be given by intramuscular injection. Other hypersensitivity reactions have included rigors, angioedema, and, rarely, severe skin reactions including exfoliative dermatitis, erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis. Other reported reactions include gastrointestinal disturbances, dizziness, headache, thrombocytopenia (especially at high doses), leucopenia, neutropenia, eosinophilia, disturbances in liver enzyme values, and pain, erythema, and thrombophlebitis or abscess at the injection site. Rare cases of agranulocytosis have occurred. Renal impairment and ototoxicity have been reported but both appear to be less frequent than with vancomycin. Renal and auditory function should be monitored during prolonged therapy in patients with pre-existing renal impairment, and in those receiving other ototoxic or nephrotoxic drugs, although opinions conflict as to whether increased risk of nephrotoxicity exists with combined therapy with drugs such as the aminoglycosides. In general, periodic blood counts and liver- and renal-function tests are advised during treatment. No relationship has yet been established between plasma concentration and toxicity, and plasma-concentration monitoring is not generally considered necessary. Dosage adjustment is required in renal impairment.

Hypersensitivity.

Although there have been occasional reports of cross-sensitivity to teicoplanin in patients hypersensitive to vancomycin,1-4 the majority of reports suggest that cross-sensitivity is very rare and teicoplanin can usually be used in patients intolerant of vancomycin.5-7
1. McElrath MJ, et al. Allergic cross-reactivity of teicoplanin and vancomycin. Lancet 1986; i: 47
2. Grek V, et al. Allergic cross-reaction of teicoplanin and vancomycin. J Antimicrob Chemother 1991; 28: 476–7
3. Marshall C, et al. Glycopeptide-induced vasculitis—cross-reactivity between vancomycin and teicoplanin. J Infect 1998; 37: 82–3
4. Kwon HS, et al. A case of hypersensitivity syndrome to both vancomycin and teicoplanin. J Korean Med Sci 2006; 21: 1108–10
5. Schlemmer B, et al. Teicoplanin for patients allergic to vancomycin. N Engl J Med 1988; 318: 1127–8
6. Smith SR, et al. Teicoplanin administration in patients experiencing reactions to vancomycin. J Antimicrob Chemother 1989; 23: 810–12
7. Wood G, Whitby M. Teicoplanin in patients who are allergic to vancomycin. Med J Aust 1989; 150: 668.

Red-man syndrome.

Although teicoplanin is believed1,2 to be less likely than vancomycin to induce the red-man syndrome, symptoms consistent with the syndrome have nevertheless been reported after intravenous use.3
1. Sahai J, et al. Comparison of vancomycin- and teicoplanin-induced histamine release and "red man syndrome". Antimicrob Agents Chemother 1990; 34: 765–9
2. Rybak MJ, et al. Absence of "red man syndrome" in patients being treated with vancomycin or high-dose teicoplanin. Antimicrob Agents Chemother 1992; 36: 1204–7
3. Dubettier S, et al. Red man syndrome with teicoplanin. Rev Infect Dis 1991; 13: 770.

💊 Antimicrobial Action

As for Vancomycin Hydrochloride, although in general teicoplanin is more active against susceptible strains. In particular, it may be more active in vitro against enterococci and some anaerobic organisms, including strains of Clostridium. However, some coagulase-negative staphylococci are less sensitive to teicoplanin than to vancomycin. Acquired resistance to teicoplanin has developed in staphylococci during treatment with teicoplanin. Cross-resistance with vancomycin has occurred in staphylococci and enterococci.

💊 Pharmacokinetics

Teicoplanin is poorly absorbed from the gastrointestinal tract. After a 400-mg intravenous dose, peak plasma concentrations 1 hour later are reported to be in the range 20 to 50 micrograms/mL. It is well absorbed on intramuscular injection with a bioavailability of about 90%; after a dose of 3 mg/kg intramuscularly, peak plasma concentrations of 5 to 7 micrograms/mL have been reported after 2 to 4 hours. The pharmacokinetics of teicoplanin are triphasic, with a biphasic distribution and a prolonged elimination. Penetration into the CSF is poor. It is taken up into white blood cells, and about 90 to 95% of teicoplanin in plasma is protein bound. It is excreted almost entirely by glomerular filtration in the urine, as unchanged drug. The terminal half-life is prolonged, but reported half-lives have ranged from about 30 to 190 hours or longer, depending on the sampling time; an effective clinical half-life of about 60 hours has been suggested for use in calculating dosage regimens. Half-life is increased progressively with increasing degrees of renal impairment. Teicoplanin is not removed by haemodialysis. Teicoplanin is a mixture of several components, the pharmacokinetics of which have been shown to vary slightly, depending on their lipophilicity.
1. Wilson APR. Clinical pharmacokinetics of teicoplanin. Clin Pharmacokinet 2000; 39: 167–83.

💊 Uses and Administration

Teicoplanin is a glycopeptide antibiotic that may be used as an alternative to vancomycin in the treatment of serious Gram-positive infections where other drugs cannot be used, including the treatment and prophylaxis of infective endocarditis, peritonitis associated with continuous ambulatory peritoneal dialysis, and suspected infection in neutropenic or otherwise immunocompromised patients. Teicoplanin, given orally, has been suggested as a possible alternative to vancomycin or metronidazole in antibiotic-associated colitis. For details of these infections and their treatment, see under Choice of Antibacterial. Teicoplanin is given intravenously, as a bolus dose or by infusion over 30 minutes, or by intramuscular injection. The usual mean dose is 6 mg/kg intravenously or intramuscularly initially, followed by 3 mg/kg intravenously or intramuscularly on each subsequent day of treatment (in practice this equates to a usual dose of 400 mg initially followed by 200 mg daily, except in patients weighing more than 85 kg in whom it is adapted accordingly). In more severe infections, 6 mg/kg may be given every 12 hours for the first 3 doses, followed by 6 mg/kg daily. For the prophylaxis of endocarditis in high-risk patients undergoing dental or other procedures who are unable to receive penicillin, teicoplanin may be given in a single dose of 400 mg by intravenous injection, with gentamicin, before the procedure. A similar dose of teicoplanin is given for prophylaxis in orthopaedic surgery at induction of anaesthesia. In children, a loading dose of 10 mg/kg every 12 hours for 3 doses is followed by 6 to 10 mg/kg daily, depending on the severity of infection. In neonates, a loading dose of 16 mg/kg on the first day is followed by maintenance doses of 8 mg/kg daily, given by intravenous infusion. Although no relationship between plasma concentrations and toxicity has been established, the BNF suggests that the former may sometimes be used as a guide to optimise treatment: trough concentrations should be above 10 micrograms/mL (15 to 20 micrograms/mL in patients with endocarditis) but less than 60 micrograms/mL. Dosage should be adjusted in patients with impaired renal function (see Administration in Renal Impairment, below).
1. Brogden RN, Peters DH. Teicoplanin: a reappraisal of its antimicrobial activity, pharmacokinetic properties and therapeutic efficacy. Drugs 1994; 47: 823–54
2. Murphy S, Pinney RJ. Teicoplanin or vancomycin in the treatment of Gram-positive infections? J Clin Pharm Ther 1995; 20: 5–11
3. de Lalla F, Tramarin A. A risk-benefit assessment of teicoplanin in the treatment of infections. Drug Safety 1995; 13: 317–28
4. Periti P, et al. Antimicrobial prophylaxis in orthopaedic surgery: the role of teicoplanin. J Antimicrob Chemother 1998; 41: 329–40
5. Schaison G, et al. Teicoplanin in the treatment of serious infection. J Chemother 2000; 12 (suppl 5): 26–33.

Administration in renal impairment.

Doses of teicoplanin should be adjusted in patients with renal impairment, though reduction is not required until the fourth day of treatment. Teicoplanin should be given in usual doses for the first 3 days of therapy, thereafter the dose is adjusted according to creatinine clearance (CC):
CC 40 to 60 mL/minute: half initial dose given daily or initial dose given every 2 days
CC less than 40 mL/minute: one-third initial dose given daily or initial dose given every 3 days

💊 Preparations

Proprietary Preparations

Arg.: Targocid; Teicox; Teiklonal; Terbiox; Austral.: Tar g o c i d ; Austria: Tar gocid; Belg.: Tar g oc id ; Braz.: Bactomax; Coplaxil†; Kirom; Targocid; Teicon; Teiconin†; Teicozid; Chile: Tar g o c i d ; Cz.: Tar g o c i d ; Denm.: Tar g o c i d ; Fin.: Tar g o c i d ; Fr.: Tar g o c i d ; Ger.: Tar g o c i d ; Gr.: Tar g o c i d ; Hong Kong: Tar g ocid; Hung.: Tar g o c i d ; India: Targocid; Ticocin; Indon.: Tar g o c i d ; Irl.: Tar g ocid; Israel: Tar g o c i d ; Ital.: Tar g o s i d ; Jpn: Tar g o c i d ; Malaysia: Tar g o c i d ; Mex.: Tar go ci d ; Ter i po l ; Neth.: Tar g o c i d ; Norw.: Tar g o c i d ; NZ: Tar g o c i d ; Pol.: Tar g o c i d ; Port.: Tar g o s i d ; S.Afr.: Tar g o c i d ; Singapore: Tar g oci d; Spain: Tar g o c id ; Swed.: Tar g o c i d ; Switz.: Tar g o c i d ; Thai.: Tar g o c i d ; Turk.: Tar g o c i d ; UK: Tar g o c i d ; Venez.: Tar go cid . Multi-ingredient: Ger.: Tar g o b o n e .
Published May 08, 2019.