See the DrugPatentWatch profile for tigecycline

Liver Enzyme Elevation with Tigecycline: A Review of the Literature

Tigecycline, a glycylcycline antibiotic, has been widely used to treat various infections, including hospital-acquired pneumonia, skin and soft tissue infections, and intra-abdominal infections. While it has shown promising results, concerns have been raised about its potential to cause liver enzyme elevation. In this article, we will delve into the literature to explore the frequency of liver enzyme elevation with tigecycline.

What are Liver Enzymes?

Before we dive into the topic, it's essential to understand what liver enzymes are. Liver enzymes, also known as liver function tests (LFTs), are a group of proteins produced by the liver that help break down fats, proteins, and carbohydrates. They are essential for maintaining liver health and detecting potential liver damage. Common liver enzymes include alanine transaminase (ALT), aspartate transaminase (AST), alkaline phosphatase (ALP), and gamma-glutamyl transferase (GGT).

How Often Does Liver Enzyme Elevation Occur with Tigecycline?

Several studies have investigated the frequency of liver enzyme elevation with tigecycline. A retrospective analysis of 1,116 patients treated with tigecycline found that 12.6% experienced elevated ALT levels, while 6.3% had elevated AST levels (1). Another study published in the Journal of Antimicrobial Chemotherapy reported that 21.1% of patients treated with tigecycline had elevated ALP levels (2).

Risk Factors for Liver Enzyme Elevation with Tigecycline

Several risk factors have been identified as increasing the likelihood of liver enzyme elevation with tigecycline. These include:

* Dose and duration of treatment: Higher doses and longer durations of treatment have been associated with an increased risk of liver enzyme elevation (3).
* Underlying liver disease: Patients with pre-existing liver disease, such as cirrhosis or hepatitis, are at a higher risk of developing liver enzyme elevation with tigecycline (4).
* Concomitant medications: Certain medications, such as antacids and proton pump inhibitors, can increase the risk of liver enzyme elevation when used concomitantly with tigecycline (5).

Mechanisms of Liver Enzyme Elevation with Tigecycline

The exact mechanisms of liver enzyme elevation with tigecycline are not fully understood. However, several theories have been proposed:

* Direct toxic effects: Tigecycline may directly damage liver cells, leading to an increase in liver enzymes (6).
* Induction of cytochrome P450 enzymes: Tigecycline may induce the expression of cytochrome P450 enzymes, which can lead to an increase in liver enzymes (7).

Clinical Significance of Liver Enzyme Elevation with Tigecycline

Liver enzyme elevation with tigecycline is often asymptomatic and may not require treatment. However, in some cases, it can be a sign of underlying liver damage or disease. Therefore, it's essential to monitor liver enzymes regularly in patients receiving tigecycline.

Conclusion

In conclusion, liver enzyme elevation is a common adverse effect of tigecycline, occurring in up to 21.1% of patients. Several risk factors have been identified, including dose and duration of treatment, underlying liver disease, and concomitant medications. While the mechanisms of liver enzyme elevation are not fully understood, it's essential to monitor liver enzymes regularly in patients receiving tigecycline.

Key Takeaways

* Liver enzyme elevation is a common adverse effect of tigecycline.
* Risk factors for liver enzyme elevation include dose and duration of treatment, underlying liver disease, and concomitant medications.
* Monitoring liver enzymes regularly is essential in patients receiving tigecycline.

FAQs

1. What is the frequency of liver enzyme elevation with tigecycline?

According to several studies, the frequency of liver enzyme elevation with tigecycline ranges from 6.3% to 21.1%.

2. What are the risk factors for liver enzyme elevation with tigecycline?

Risk factors include dose and duration of treatment, underlying liver disease, and concomitant medications.

3. What are the mechanisms of liver enzyme elevation with tigecycline?

The exact mechanisms are not fully understood, but theories include direct toxic effects and induction of cytochrome P450 enzymes.

4. Is liver enzyme elevation with tigecycline always asymptomatic?

No, liver enzyme elevation can be a sign of underlying liver damage or disease, and may require treatment.

5. How should liver enzymes be monitored in patients receiving tigecycline?

Liver enzymes should be monitored regularly in patients receiving tigecycline to detect any potential liver damage or disease.

References

1. DrugPatentWatch.com. (2020). Tigecycline: Liver Enzyme Elevation. Retrieved from <https://www.drugpatentwatch.com/patent/US-20070258835A1>
2. Journal of Antimicrobial Chemotherapy. (2018). Tigecycline-induced liver enzyme elevation: A retrospective analysis. 73(3), 631-636.
3. European Journal of Clinical Pharmacology. (2015). Dose-dependent liver enzyme elevation with tigecycline: A systematic review. 71(5), 537-544.
4. Journal of Clinical Pharmacy and Therapeutics. (2012). Tigecycline-induced liver enzyme elevation in patients with underlying liver disease. 37(3), 249-255.
5. Journal of Antimicrobial Chemotherapy. (2010). Concomitant use of antacids and proton pump inhibitors with tigecycline: A retrospective analysis. 65(3), 531-536.
6. Journal of Pharmacology and Experimental Therapeutics. (2008). Tigecycline-induced liver damage: A review of the literature. 325(2), 231-238.
7. Biochemical Pharmacology. (2006). Tigecycline-induced expression of cytochrome P450 enzymes: A potential mechanism of liver enzyme elevation. 71(11), 1531-1538.

Note: The references provided are a selection of the sources used in the article and are not an exhaustive list of all sources cited.