J01AA12 - Tigecycline |
Propably not porphyrinogenic |
PNP |
Rationale
Tigecycline is not a substrate or an inhibitor of CYP450 enzymes. It is not listed as an inducer and is therefore probably not porphyrinogenic. Side effects such as nausea, vomiting and diarrhoea may be potentially porphyrinogenic through reduction in carbohydrate intake.
Chemical description
Tigecycline is a glycylcycline, a tetracycline analogue.
Therapeutic characteristics
Tigecycline is used for the treatment of complicated skin and skin structure infections caused by susceptible organisms, and is administered intravenously. Nausea, vomiting and diarrhoea are reported as very common side effects.
Metabolism and pharmakokinetics
In vitro studies have shown that tigecycline is not metabolized by CYP450 (Peterson 2008) and data indicates that it is not a mechanism-based inhibitor of CYP2C9, CYP2C19, CYP2D6 and CYP3A (SPC 2013). It is not listed as an inducer of CYP enzymes.
It is metabolized in liver via glucuronidation, N-acetylation and epimerization. The epimere of tigecycline is formed through a nonenzymatic process (Agwuh 2006, Meagher 2005). The major route of elimination is through faeces (59%) and urine (33%), both of them primarily as unchanged drug. Half-life elimination: single dose 27 hours; following multiple doses: 42 hours.
References
- Scientific articles
- Agwuh K. N. and MacGowan A. Pharmacokinetics and pharmacodynamics of the tetracyclines including glycyclines. Journal of Antimicrobial Chemotherapy. 2006;58:256â-265. #1614
- Meagher AK, Ambrose PG et al. Pharmacokinetic/pharmacodynamic profile for tigecycline-a new glycylcycline antimicrobial agent. Diagn Microbiol Infect Dis. 2005 Jul;52(3):165-71. PMID 16105560. #1626
- Peterson LR. A review of tigecycline the first glycylcycline. Int J Antimicrob Agents. 2008 Dec;32(4):215-22. PMID 19134522. #1627
- Drug reference publications
- Up to date. Tigecycline. #1629
- Summary of Product Characteristics
- Norwegian medicines agency. Summary of Product Characteristics (SPC). Tigecyklin. #1628
Similar drugs
© NAPOS 2024