Rema MN
Department of Pharmacology, Amala Institute of Medical Science

Corresponding Author: Dr. Rema MN, MD Professor & HOD, Pharmacology, Amala Institute of Medical Science; President, TC Medical Council. E-mail: imaksb@yahoo.co.in

ABSTRACT

Introduction: The inevitable consequence of the widespread use of antimicrobial agents has been the emergence of antibiotic-resistant pathogens, fueling an ever-increasing need for new antimicrobial agents.

Methodology: The clinical use and therapeutic effects of the new drug Tigecycline is described.

Result: Tigecycline is an example of a new drug developed in response to the growing prevalence of antibiotic resistance in bacteria such as Staphylococcus aureus. It was approved by FDA in 2005

Unlike other diseases antimicrobial therapy is aimed at the pathogen. The inevitable consequence of the widespread use of antimicrobial agents has been the emergence of antibiotic-resistant pathogens, fueling an ever-increasing need for new antimicrobial agents (AMA).  Tigecycline is an example of a new AMA developed in response to the growing prevalence of antibiotic resistance in bacteria such as Staphylococcus aureus.  It was approved by FDA in 2005

Tigecycline is a glycyl cycline structurally related to minocycline (N, N-dimethylglycylamido)-6- demethyl-6-deoxytetracycline.

Mechanism of action

It binds  to the 30 S ribosomal unit  in the bacterial cell. Consequently the binding  of aminoacyl t RNA to the  mRNA ribosome complex is interfered with. The peptide chain elongation  does not occur  and thus inhibits protein synthesis and multiplication. It is a bacteriostatic agent.

Bacterial spectrum

Tigecycline has expanded broad – spectrum antimicrobial activity. It is active against many Gram +ve  bacteria, Gram  -ve  bacteria and  anaerobes, including  Methicillin resistant Staphylococcus aureus (MRSA) and multi-drug resistant strains of Acinetobacter baumannii. It has no activity  against Pseudomonas spp or Proteus  spp.

Dose

There is no oral form available at present. It is given by slow  intravenous infusion  (30 to 60 minutes). A single dose of l 00 mg is given  first, followed by 50 mg every  twelve  hours. It is not licensed for  use in children.

Kinetics

71-89 % is protein  bound and is not metabolised in the  body.  Excretion is  59%  biliary, 33% renal. Patients with impaired liver function need to be given a lower  dose.  No adjustment is needed  for patients with impaired kidney function.

Indications

Tigecycline is  efficacious for  the  treatment of complicated intra abdominal  infections and complicated   skin  and  skin  structure infections suppurative wound infections, IJV line infection and bacterial  endocarditis caused  by MRSA.

Adverse drug reaction (ADR)

Allergic potential is less. Common ADR    are diarrhea, nausea  and vomiting, dizziness, asthenia, raised  SGOT, alkaline phosphatase and  LDH. Nausea and vomiting is mild or moderate and usually occurs  during  the first  two days  of therapy.  Other side effects include pain at the injection site, swelling and irritation. Like tetracycline, it shows   increased sensitivity to sunlight. It affects  bone and teeth and avoid  use in children and pregnancy. As with other antibiot1cs, overgrowth of  organisms that  are  not susceptible to tigecycline can  occur.

Drug interaction

With co-administered Warfarin, INR is raised.

AMA resistance

Decreased susceptibility to the development of resistance when compared with other tetracycline antibiotics.

End Note

Author Information

Dr. Rema MN, MD Professor & HOD,
Pharmacology, Amala Institute of Medical Science; President, TC Medical Council.

Conflict of Interest: None declared

References

  1. Greer ND. Tigecycline (Tygacil): the first in the glycylcycline class of antibiotics. Proc (Bayl Univ Med Cent). 2006 Apr;19(2):155–61. [Pubmed]
  2. Tigecycline_ Wikipedia, the free encyclopedia.