Tigecycline

Antibiotic Class:

Glycylcycline

Antimicrobial Spectrum:

Streptococcus spp., Staphylococcus spp.,(including MRSA and VRSA) H. influenzae, E. coli, K. pneumoniae, Entercoccus spp., M. catarrhalis, N. meningitidis, M. pneumoniae, C. pneumoniae

Mechanism of Action:

Binds to the 30S ribosomal subunit of rRNA and inhibits the binding of amino acyl-tRNA

Pharmacodynamics:

Time-dependent killing

Pharmacokinetics:

Cmax (300mg IV): 2.8mcg/ml

AUC (300mg IV): 17.9mcg/ml

Half-life: May be dose dependent

Adverse Effects:

GI: nausea, vomiting, abdominal pain

Dosage:

IV: 50mg vial

Adults: 100mg IV x 1, then 50mg IV q 12 hours

Children: Safety and efficacy have not been determined in patients < 18 years old

Disease state based dosing:

Renal failure:  Dosing adjustments not necessary (including hemodialysis)

Hepatic failure:  In severe hepatic impairment (Childs-Pugh class C) patients should be given the normal loading dose with the maintenance dose administered as 25mg IV q 12 hours

Contraindications/Warnings/Precautions:

Warning:  Tigecycline may cause fetal harm in pregnant women (Pregnancy class D)

Precautions: Tigecycline is a similar to the tetracyclines and may chelate calcium ions and discolor teeth if administered to patients during tooth development (< 8 years old).

Drug Interactions:

Tigecycline does not inhibit metabolism of agents via CYP pathways 1A2, 2C8, 2C9, 2C19, 2D6, and 3A4.

Warfarin – Tigecycline decreases clearance of R-warfarin and S-warfarin. Monitoring of PT times and INR may be warranted

Pregnancy:

Category D: Risk established, but benefits may outweigh risk.

Monitoring Requirements:

Therapeutic: Culture and sensitivities, signs and symptoms of infection

Toxic: 

Brand names/Manufacturer: Tygacil/Wyeth Pharmaceuticals