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Does tigecycline's metabolism cause variable drug levels?

See the DrugPatentWatch profile for tigecycline

Tigecycline's metabolism is not a significant factor in causing variable drug levels. Instead, the drug is primarily eliminated unchanged through biliary and intestinal excretion [1].

How is tigecycline eliminated from the body?


Tigecycline is eliminated largely in unchanged form, with approximately 59% of a dose excreted in feces and 26% in urine [1]. Studies indicate that minimal metabolism occurs, with no significant metabolites identified in plasma, urine, or feces [1].

What factors influence tigecycline drug levels?


While metabolism is not a primary driver of variability, other factors can influence tigecycline drug levels. These can include patient-specific characteristics such as renal and hepatic function, as well as drug-drug interactions [2].

Are there concerns about tigecycline dosing?


Concerns regarding tigecycline dosing have arisen due to a boxed warning highlighting an increased risk of death compared to other treatments in certain serious infections [3]. This warning is based on a meta-analysis of clinical trials, and the reasons for this increased mortality are not fully understood [3].

How does tigecycline compare to other antibiotics?


Tigecycline is a glycylcycline antibiotic that is active against a broad spectrum of bacteria, including many Gram-positive, Gram-negative, and anaerobic pathogens [1]. It is often used for complicated skin and intra-abdominal infections, as well as community-acquired bacterial pneumonia, particularly when other treatments have failed or are not suitable [4].

What are the side effects of tigecycline?


The most common side effects associated with tigecycline include nausea, vomiting, and diarrhea [1].

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1. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021903s026lbl.pdf
2. https://pubmed.ncbi.nlm.nih.gov/22623751/
3. https://www.fda.gov/drugs/drug-safety-and-availability/fda-drug-safety-communication-fda-will-not-require-label-changes-regarding-increased-mortality-risk
4. https://www.nejm.org/doi/full/10.1056/nejmoa1113753



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