Monograph
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 pharmacokinetics
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
# | Citation details | PMID |
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* | Scientific articles | |
1. | N. and MacGowan A. Pharmacokinetics and pharmacodynamics of the tetracyclines including glycyclines.
Agwuh K. Journal of Antimicrobial Chemotherapy. 2006;58:256â-265. |
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2. | Pharmacokinetic/pharmacodynamic profile for tigecycline-a new glycylcycline antimicrobial agent.
Meagher AK, Ambrose PG et al. Diagn Microbiol Infect Dis. 2005 Jul;52(3):165-71. |
16105560 |
3. | A review of tigecycline the first glycylcycline.
Peterson LR. Int J Antimicrob Agents. 2008 Dec;32(4):215-22. |
19134522 |
* | Drug reference publications | |
4. | Up to date. Tigecycline.
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* | Summary of Product Characteristics | |
5. | Norwegian medicines agency. Summary of Product Characteristics (SPC). Tigecyklin.
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Similar drugs
Tradenames and packages
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Netherlands
Tigecycline · Tigecycline Accord 50 mg, poeder voor oplossing voor infusie · Tigecycline Eureco-Pharma 50 mg, poeder voor oplossing voor infusie · Tigecycline Hikma 50 mg poeder voor oplossing voor infusie · Tygacil · Tygacil, poeder voor concentraat voor oplossing voor intraveneuze infusie 10 mg/mlBelgium
Tigecycline · Tigecycline Accord 50 mg sol. perf. (pdr.) i.v. flac. · Tygacil · Tygacil 50 mg sol. perf. (pdr.) i.v. flac.United Kingdom
Tigecycline · Tigecycline 50mg powder for solution for infusion vials · Tygacil · Tygacil 50mg powder for solution for infusion vialsDenmark
Tigecycline · Tigecycline "Accord" · Tigecycline "EQL Pharma" · Tigecycline "Panpharma" · TygacilNorway
Tigecycline Accord · TygacilPoland
Tigecycline Accord · Tigecycline AptaPharma · Tigecycline Fresenius Kabi · Tigecycline Mylan · Tigecycline Sandoz · Tigecycline Solinea · Tigecycline TZF · TygacilLuxembourg
TYGACILIceland
Tigecycline · Tigecycline Accord · TygacilFinland
Tigecycline Accord · Tigecycline Eql Pharma · Tigecycline Panpharma · TygacilLatvia
Tigecycline · Tigecycline Accord · TygacilSerbia
Tigeciklin · Tigeciklin Anfarm · Tigilin · Tigilin® · Tygacil · Tygacil®
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