Tigecycline, a glycylcycline, inhibits protein translation in bacteria by binding to the 30S ribosomal subunit and blocking entry of amino-acyl tRNA molecules into the A site of the ribosome. This prevents incorporation of amino acid residues into elongating peptide chains. Tigecycline carries a glycylamido moiety attached to the 9-position of minocycline. The substitution pattern is not present in any naturally occurring or semisynthetic tetracycline and imparts certain microbiologic properties to tigecycline. Tigecycline is not affected by the two major tetracycline resistance mechanisms, ribosomal protection and efflux. Accordingly, tigecycline has demonstrated in vitro and in vivo activity against a broad spectrum of bacterial pathogens. There has been no cross resistance observed between tigecycline and other antibiotics. Tigecycline is not affected by resistance mechanisms such as beta-lactamases (including extended spectrum beta-lactamases), target site modifications, macrolide efflux pumps or enzyme target changes (e.g. gyrase/topoisomerase). In vitro studies have not demonstrated antagonism between tigecycline and other commonly used antibacterial drugs. In general, tigecycline is considered bacteriostatic.

Tigecycline is indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the conditions listed below:

Complicated Skin and Skin structure Infections: Complicated skin and skin structure infections caused by Escherichia coli, Enterococcus faecalis (vancomycin-susceptible isolates only), Staphylococcus aureus (methicillin-susceptible and -resistant isolates), Streptococcus agalactiae, Streptococcus anginosus grp. (includes S. anginosus, S. intermedius, and S. constellatus), Streptococcus pyogenes, Enterobacter cloacae, Klebsiella pneumoniae and Bacteroides fragilis.

Complicated Intra-Abdominal Infections: Complicated intra-abdominal infections caused by Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Klebsiella oxytoca, Klebsiella pneumoniae, Enterococcus faecalis (vancomycin-susceptible isolates only), Staphylococcus aureus (methicillin-susceptible and -resistant isolates), Streptococcus anginosus grp. (includes S. anginosus, S. intermedius, and S. constellatus), Bacteroides fragilis, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides vulgatus, Clostridium perfringens, and Peptostreptococcus micros.

Community-Acquired Bacterial Pneumonia: Community-acquired bacterial pneumonia caused by Streptococcus pneumoniae (penicillin-susceptible isolates), including cases with concurrent bacteremia, Haemophilus influenzae (beta-lactamase negative isolates), and Legionella pneumophila.

The duration of therapy should be guided by the severity and site of the infection and the patient's clinical and bacteriological progress. The recommended duration of treatment with Tigecycline for complicated skin and skin structure infections or for complicated intra-abdominal infections is 5 to 14 days and for community-acquired bacterial pneumonia is 7 to 14 days. The recommended daily dose is as follows:

Adults: The recommended dosage regimen for Tigecycline is an initial dose of 100 mg, followed by 50 mg every 12 hours. Intravenous (IV) infusions of Tigecycline should be administered over approximately 30 to 60 minutes every 12 hours.

Pediatric use: Safety and effectiveness in pediatric patients below the age of 18 years have not been established. 

Geriatric use: No unexpected overall differences in safety or effectiveness were observed between these subjects and younger subjects.

Tigecycline is contraindicated for use in patients who have known hypersensitivity to Tigecycline.

The most common treatment-emergent adverse events are nausea and vomiting which generally occurre during the first 1-2 days of therapy.

The following drug-related adverse events are reported infrequently in patients receiving Tigecycline: Injection site inflammation & pain, septic shock, allergic reaction, chills, thrombophlebitis, bradycardia, tachycardia, vasodilatation, anorexia, dry mouth, hypoglycemia, hyponatremia, prolonged prothrombin time, eosinophilia, thrombocytopenia, vaginal moniliasis, vaginitis, leukorrhea.

Overdose Effects

No specific information is available on the treatment of overdosage with Tigecycline. Intravenous administration of Tigecycline at a single dose of 300 mg over 60 minutes in healthy volunteers resulted in an increased incidence of nausea and vomiting.

Tigecycline is structurally similar to Tetracycline-class antibiotics and should be administered with caution in patients with known hypersensitivity to Tetracycline-class antibiotics

Pregnancy & Lactation

Pregnancy: Tigecycline should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: Caution should be exercised when Tigecycline is administered to a nursing woman.