Do SSRIs impair hepatic regeneration

Comment by InpharmD Researcher

Some evidence suggests that serotonin may play a role in liver regeneration, especially following partial hepatectomy or toxic injury; however, data specifically addressing the potential impact of serotonin reuptake inhibitors (SSRIs) in this context is limited. Serotonin is generally hypothesized to contribute to liver regeneration through liver toxicity induced by SSRIs or acute liver injury resulting from dysregulation of the 5-HT degradation system. Notably, findings from a retrospective study suggest that perioperative SSRI use in patients undergoing hepatic resection may be linked to impaired liver function and poorer postoperative outcomes (see Table 1). Nonetheless, further research is needed to elucidate the potential effects of SSRIs on liver regeneration.

Background

A 2024 review article discusses the role of serotonin (5-HT) in liver diseases, highlighting its involvement in liver regeneration as well as its contribution to the progression of conditions like cirrhosis, fatty liver disease, viral hepatitis, and hepatocellular carcinoma (HCC). Regarding 5-HT's role in liver injury, two main mechanisms are proposed: liver toxicity from serotonin reuptake inhibitors (SSRIs) and acute liver injury resulting from dysregulation of the 5-HT degradation system (5DS). Several case reports have documented liver toxicity associated with SSRIs, including severe cholestasis and hepatic cell damage, cholestatic liver injury, and liver dysfunction, all of which improved after discontinuation of the drugs. Additionally, a 2021 retrospective study suggested perioperative use of SSRIs in patients undergoing hepatic resection may potentially be linked to liver function impairment and poor postoperative outcomes, highlighting the need for caution during the perioperative period (see Table 1). Dysregulation of 5DS is thought to contribute to liver injury by increasing serotonin breakdown and overproducing reactive oxygen species. This activates signaling pathways like JNK, p38 MAPK, and STAT3, promoting apoptosis and inflammation in liver cells. The imbalance leads to the release of pro-inflammatory cytokines which worsen liver damage. Inhibiting 5DS with 5-HTR2A antagonists has shown potential in preventing liver toxicity, suggesting therapeutic opportunities for liver diseases, though further research is needed to fully understand its clinical applications. [1]

Serotonin, particularly platelet-derived 5-HT, may play a role in liver regeneration, especially following partial hepatectomy or toxic injury. In animal models, serotonin has been shown to be essential for effective liver regeneration, but clinical evidence in humans remains limited. One 2014 study involving 60 patients undergoing liver resection provided insights into the role of intraplatelet 5-HT in liver regeneration and liver dysfunction. The study found that intraplatelet 5-HT levels significantly decreased immediately after liver resection (p<0.001) but gradually recovered within the first week. Moreover, reduced preoperative intraplatelet 5-HT levels were associated with delayed hepatic regeneration and poor clinical outcomes. Specifically, low preoperative intraplatelet 5-HT (<73 ng/mL) was linked to a higher incidence of postoperative liver dysfunction (p= 0.045) and increased morbidity (p=0.021). Patients with reduced intraplatelet 5-HT levels throughout the perioperative period also experienced delayed liver regeneration and adverse outcomes. Overall, the findings suggested that intraplatelet 5-HT may serve as a potential clinical marker for predicting postoperative liver dysfunction and delayed hepatic regeneration in patients undergoing liver resection. However, the impact of SSRIs on this process was not assessed in this study, leaving their potential influence unclear. [2], [3]

A 2016 observational study examined the incidence of drug-induced liver injury (DILI) in psychiatric inpatients treated with antidepressants. Data from 184,234 psychiatric inpatients were analyzed, revealing 149 cases of DILI (0.08%). The incidence of DILI was highest with mianserine (0.36%), agomelatine (0.33%), and clomipramine (0.23%). In contrast, SSRIs, including escitalopram, citalopram, and fluoxetine, had the lowest rates of DILI (0.03%), with escitalopram being the least likely to cause liver injury (0.01%). The most common symptoms of DILI included nausea, fatigue, loss of appetite, and abdominal pain. Additionally, the study found that the dosage at the time of DILI onset was higher in seven of the nine antidepressants examined compared to their median overall dosage. Overall, the findings suggested that SSRIs are less likely than the other antidepressants examined to precipitate DILI. However, the authors emphasized that patients with preexisting liver damage were at higher risk of DILI, and advised caution when prescribing antidepressants with potential liver-related adverse effects to these patients. [4]

References:

[1] Mao B, Liu S, Zhu S, et al. The janus face of serotonin: Regenerative promoter and chronic liver disease aggravator. Heliyon. 2024;10(9):e30703. doi:10.1016/j.heliyon.2024.e30703
[2] Papadimas GK, Tzirogiannis KN, Mykoniatis MG, Grypioti AD, Manta GA, Panoutsopoulos GI. The emerging role of serotonin in liver regeneration. Swiss Med Wkly. 2012;142:w13548. Published 2012 Apr 11. doi:10.4414/smw.2012.13548
[3] Starlinger P, Assinger A, Haegele S, et al. Evidence for serotonin as a relevant inducer of liver regeneration after liver resection in humans. Hepatology. 2014;60(1):257-266. doi:10.1002/hep.26950
[4] Friedrich ME, Akimova E, Huf W, et al. Drug-Induced Liver Injury during Antidepressant Treatment: Results of AMSP, a Drug Surveillance Program. Int J Neuropsychopharmacol. 2016;19(4):pyv126. Published 2016 Apr 20. doi:10.1093/ijnp/pyv126

Literature Review

A search of the published medical literature revealed 2 studies investigating the researchable question:

Do SSRIs impair hepatic regeneration

Level of evidence

C - Multiple studies with limitations or conflicting results  Read more→



Please see Tables 1-2 for your response.


 

Consequences of Perioperative Serotonin Reuptake Inhibitor Treatment During Hepatic Surgery

Design

Retrospective cohort study

N= 1,249

Objective

To evaluate whether perioperative use of selective serotonin reuptake inhibitors or serotonin-norepinephrine reuptake inhibitors (SSRIs/SNRIs) affects outcome after hepatic resection

Study Groups

Exploration group, n= 754

SSRIs/SNRIs, n= 71

No SSRIs/SNRIs, n= 683

Validation group, n= 495

SSRIs/SNRIs, n= 50

No SSRIs/SNRIs, n= 445

Inclusion Criteria

Age 18 years and older; undergoing elective liver resection

Exclusion Criteria

Not disclosed

Methods

The exploration cohort represented patients from the Medical University of Vienna and the Medical University of Innsbruck in Austria. The validation cohort represented patients from the Mayo Clinic in Rochester, MN.

Serum and plasma preparations were performed immediately prior to surgery and on postoperative day 1 (POD1) as well as on POD5 after liver resection for intraplatelet serotonin assessment. 

Patients were classified as SSRI/SNRI positive if they received preoperative treatment of any duration. If patients only received a postoperative treatment, they were not classified as SSRI/SNRI positive. In the event that SSRIs/SNRIs were paused during or immediately after surgery, patients were still classified as SSRI/SNRI positive.

Duration

2000 to 2018

Outcome Measures

Postoperative liver dysfunction (LD), grade C LD, morbidity, severe morbidity

   

Exploration Group

Validation Group

Baseline Characteristics

 

SSRI/SNRI (n= 71)

No SSRI/SNRI (n= 683)

SSRI/SNRI (n= 50)

No SSRI/SNRI (n= 445)

Age, years (median)

65 (25 to 83) 63 (20 to 89) 60 (28 to 79) 62 (18 to 84)

Female

34 (47.9%) 263 (38.5%) 27 (52.9%) 210 (47.3%)

Hepatic resection

Minor (<3 segments)

Major (≥3 segments)

 

32 (45.1%)

39 (54.9%)

 

331 (48.5%)

352 (51.5%)

 

-

50 (100%)

 

-

444 (100%)

Comorbidities

Cardiovascular 

Pulmonary

Renal

Diabetes

Obesity

 

8 (13.6%)

4 (6.5%)

3 (4.8%)

6 (9.5%)

9 (14.3%)

 

64 (10.6%)

39 (6.4%)

10 (1.6%)

76 (12.2%)

150 (23.5%)

 

-

-

-

-

-

 

-

-

-

-

-

Cofactors

Fibrosis

F0

F1

F2

F3

F4/cirrhosis

Intraoperative RBC, (median)

Pringle applied

PVE

 

 

25 (39.1%)

20 (31.3%)

11 (17.2%)

2 (3.1%)

6 (9.4%)

0 (0 to 14)

7 (12.5%)

6 (11.1%)

 

 

287 (47.1%) 

196 (32.2%)

62 (10.2%)

28 (4.6%)

36 (5.9%)

0 (0 to 28)

75 (12.5%)

39 (6.9%)

 

 

-

-

-

-

-

-

-

-

 

 

-

-

-

-

-

-

-

-

Abbreviations: RBC= red blood cell, PVE= portal vein embolization

Results

Endpoint

Exploration Group OR (95% CI)  (n= 754)

Validation Group OR (95% CI) (n= 495)

LD

2.08 (1.09 to 3.77)

1.82 (0.89 to 3.52)

 

Grade C LD

2.65 (0.95 to 6.36) 1.76 (0.50 to 4.86)

Morbidity

1.39 (0.85 to 2.27)  1.99 (1.00 to 4.33)

Severe Morbidity 

1.73 (0.99 to 2.92)  2.09 (1.07 to 3.96)

Abbreviation: OR= odds ratio, CI= confidence interval, LD= liver dysfunction

Univariate and multivariate logistic regression analyses showed an increased risk of postoperative liver dysfunction with SSRI/SNRI use (2.08 OR 95% CI 1.09 to 3.77, p=0.02; 2.40 OR 95% CI 1.00 to 5.4, p= 0.040, respectively)

Adverse Events

The incidence of bleeding complications requiring intervention was not significant.

Study Author Conclusions

We observed a significant association of perioperative SSRI/SNRI intake with adverse postoperative outcomes after hepatic resection. This indicates that SSRIs/SNRIs should be avoided perioperatively in patients undergoing hepatic resections. 

InpharmD Researcher Critique

This study is limited due to its small sample size of patients receiving SSRI/SNRI medications.



References:

Starlinger P, Pereyra D, Hackl H, et al. Consequences of Perioperative Serotonin Reuptake Inhibitor Treatment During Hepatic Surgery. Hepatology. 2021;73(5):1956-1966. doi:10.1002/hep.31601

 

A Case of Sertraline-Induced Hepatotoxicity Correlated With Pharmacogenomic Testing

Design

 Case Report

Case presentation

A 73-year-old woman with fibromyalgia and anxiety presented with cholestatic hepatitis after starting sertraline 75 mg daily for chronic anxiety. Four weeks into treatment, she developed pruritus and dark urine, prompting discontinuation of the medication, but her symptoms persisted. Physical examination revealed scleral icterus and excoriations without hepatosplenomegaly or signs of chronic liver disease. Her laboratory tests showed elevated liver enzymes, including a total bilirubin of 4.7 mg/dL, alkaline phosphatase of 509 U/L, aspartate aminotransferase of 280 U/L, and alanine aminotransferase of 468 U/L, with unremarkable autoimmune and viral hepatitis workups. Magnetic resonance cholangiopancreatography showed no biliary obstruction, and liver biopsy confirmed resolving cholestatic hepatitis without fibrosis or autoimmune features. Due to the slow resolution of liver enzyme abnormalities, she underwent pharmacogenomic testing, which revealed polymorphisms in the SLC6A4 and HTR2A genes, indicating impaired serotonin metabolism. Her liver enzymes eventually normalized, and she was advised to avoid selective serotonin reuptake inhibitors (SSRIs) in the future.

Study Author Conclusions

Sertraline is a rare yet known culprit of DILI. There is no current reliable way of predicting one’s risk of developing DILI from SSRIs. PGx testing showed that she had two polymorphisms in sertraline metabolism. SLC6A4 encodes a serotonin transporter and augments the synaptic concentration of the drug. HTR2A changes are also associated with an increase in antidepressant response of higher serotonin levels. This possibly led to increased drug levels and side effects from poor metabolism of SSRIs. With further affordability, PGx testing can be considered before starting medications associated with DILI to avoid prescribing it to those who may be at higher risk of developing it.

References:

Gampa A, Dunnenberger M, Fimmel C. S2481 a case of sertraline-induced hepatotoxicity correlated with pharmacogenomic testing. Am J Gastroenterol. 2020;115(1):S1311-S1311. doi:10.14309/01.ajg.0000711972.61089.f6