Is there any difference in hepatotoxicity, specifically LFT elevations, amongst statins?

Comment by InpharmD Researcher

Several meta-analyses report an association between transaminase elevations and statin use, with varying levels of risks for each statin. Despite conflicting evidence on ranking the statins based on their risk of hypertransaminasemia, atorvastatin has been associated with the highest odds of elevated transaminase development. Case reports of statin-associated hepatotoxicity similarly rank atorvastatin as being one of the agents most associated with substantial liver injury, although this data should be interpreted with caution due to the likelihood of selection bias.

Background

A 2019 systematic review and meta-analysis assessed the effects of statins compared to placebo on the risk of developing hypertransaminasemia. A total of 73 randomized controlled trials (RCTs) were included, comprising 123,051 patients. Overall, there was a notable rise in hypertransaminasemia observed in individuals undergoing statin treatment when compared to those receiving placebo (odds ratio [OR] 1.45; 95% confidence interval [CI] 1.24 to 1.69; p<0.001; I2= 14%). Treatment with rosuvastatin and lovastatin was linked to a 35% and 53% increase in the odds of developing hypertransaminasemia, respectively. Conversely, pravastatin, simvastatin, and fluvastatin did not increase the odds of developing high transaminase levels compared to placebo. Among all statins, atorvastatin demonstrated the highest odds (OR 2.66; 95% CI 1.74 to 4.06; p<0.001; absolute effect of 10 more per 1,000 patients), followed by rosuvastatin (OR 1.35; 95% CI 1.06 to 1.70; p<0.01; absolute effect of 3 more per 1,000 patients), and lovastatin (OR 1.53; 95% CI 1.03 to 2.28; p<0.04; absolute effect of 3 more per 1,000 patients). High doses of atorvastatin resulted in an absolute increase of 48 events per 1,000 patients. While fluvastatin similarly raised the absolute risk of developing hypertransaminases, the odds ratio did not reach statistical significance, and the level of evidence certainty was low. [1]

The overall class analysis was stratified based on high-dose statins and standard doses of statins against placebo. High-dose statin treatment significantly increased the risk of hypertransaminasemia compared to placebo (OR 1.64; 95% CI 1.30 to 2.06; p<0.001). Notably, fluvastatin, pravastatin, and simvastatin did not exhibit a significant difference in odds compared to placebo. Elevated odds of hypertransaminasemia were observed with high doses of atorvastatin (78% increase), rosuvastatin (47% increase), and lovastatin (53% increase). The same analysis was performed with standard doses of statins, to which findings demonstrated no difference compared with placebo (OR 1.19; 95% CI 0.98 to 1.46; p= 0.08; I2= 0%). In trials with standard doses of lovastatin, pravastatin, and fluvastatin, hypertransaminasemia did not occur. Atorvastatin sensitivity analysis revealed an elevated risk of liver toxicity across all subgroups, with the highest rates observed in those with acute coronary syndrome (ACS) and acute cerebrovascular events. Atorvastatin sensitivity analysis showed no effects from diabetes, hypercholesterolemia, or renal failure. However, focusing solely on studies involving ACS or cerebrovascular events significantly increased the overall risk (OR 4.49; 95% CI 2.79 to 7.22; p<0.001; I2= 0%). It was suggested that various statin types and doses exhibit distinct potentials for increasing hypertransaminasemia incidence. High doses of atorvastatin, rosuvastatin, and lovastatin pose higher risks of liver function tests (LFT) abnormalities. [1]

A 2022 meta-analysis (N= 47 RCTs; 107,752 participants) explored the association of transaminase elevations with varying statin types and dosages. Participants with established atherosclerotic cardiovascular diseases (ASCVD) and statin treatments (either monotherapy or add-on) were followed for up to ~4 years. Studies with less than 4 weeks of intervention or less than 100 patients were excluded. Compared to non-statin treatments, statins were associated with an increased risk of transaminase elevations (OR 1.62; 95% CI 1.20 to 2.18). Of the statins, atorvastatin exhibited a higher risk of transaminase elevations versus non-statin control (OR 4.0; 95% CI 2.2 to 7.6), pravastatin (OR 3.49; 95% CI 1.77 to 6.92), and simvastatin (OR 2.77; 95% CI 1.31 to 5.09). When directly comparing treatments (N= 35 RCTs), simvastatin was associated with a lower risk of muscle problems versus atorvastatin (OR 0.70; 95% CI 0.55 to 0.90), whereas rosuvastatin was associated with a higher risk versus atorvastatin (OR 1.75; 95% CI 1.17 to 2.61). Based on surface under the cumulative ranking values, of the statins, pravastatin had the highest rank (i.e., a better outcome for the intervention) for transaminase elevations (76.3%), followed by simvastatin (62.0%), lovastatin (56.2%), rosuvastatin (43.0%), fluvastatin (37.2%), pitavastatin (22.8%), and atorvastatin (15.3%). Based on these analyses, the investigators advise avoiding atorvastatin use in the event of transaminase elevations, especially high-intensity doses, and that pravastatin may be preferable instead. [2]

A 2021 meta-analysis (N= 62 RCTs; 120,456 participants) evaluated the association between statins and adverse events in primary prevention of cardiovascular disease while exploring variations in these associations based on statin types and dosages. The analysis identified several adverse events associated with statin use, including increased risks of self-reported muscle symptoms, liver dysfunction, renal insufficiency, and eye conditions. The findings revealed that statin use was associated with an increased risk of liver dysfunction, characterized by elevated serum liver enzyme concentrations across all studies (N= 21 trials; OR 1.33; 95% CI 1.12 to 1.58). In the comparative analysis of different statin types atorvastatin (N= 17 studies; OR 1.41; 95% CI 1.08 to 1.85) and lovastatin (N= 5 trials; OR 1.81; 95% CI 1.23 to 2.66) were associated with increased risks of liver dysfunction. However, there were no statistically significant risks associated with other statins. Notably, a dose-response analysis revealed that atorvastatin exhibited a maximum effect, doubling the risk of liver dysfunction compared to non-statin controls (maximum OR 2.03; 95% credible interval 1.03 to 12.64). Conversely, the analysis did not find any significant dose-response relationships for the other statins concerning adverse effects. Based on these findings, it was concluded that statins showcased a small increased risk of liver dysfunction in patients without a history of cardiovascular disease. However, it is essential to note that many of the analyses lacked sufficient power to detect differences between groups, and some trials excluded vulnerable patients who may have been more likely to experience adverse events. Additionally, many of the included trials (27/62) had follow-up periods ≤ 6 months, potentially resulting in an underestimation of severe long-term complications such as significant liver injury. [3]

A 2017 review examined the hepatotoxicity associated with statins and other lipid-lowering drugs. Notably, the analysis on statins revealed distinct patterns in their association with hepatotoxicity. Categorization, based on case reports, places both simvastatin (68 cases) and atorvastatin (65 cases) within Category A (drugs with more than 50 well-documented cases of hepatotoxicity), showcasing instances of positive rechallenge and reported fatal liver injury. Fluvastatin (28 cases) also exhibited substantial hepatotoxicity and documented positive rechallenge; however, there was no incidence of fatal liver injuries within these reports. In contrast, rosuvastatin, lovastatin, and pravastatin, with 13, 12, and 11 reported cases, respectively, showed no associations with positive rechallenge or fatal liver injury based on available reports. Regarding the tolerance of other statins in patients with statin-induced liver injury, it was highlighted that data remains limited. One case report describes a patient recovering from fluvastatin-induced liver injury subsequently experiencing liver injury with atorvastatin. However, in a Swedish study, five cases switched to another statin post-recovery without subsequent liver injury during follow-up. Importantly, these statin transitions were successful without causing further liver-related issues. Overall, it is essential to interpret these findings with caution as they are based solely on reported cases and do not consider the varying prescription rates of each statin. [4]

References:

[1] Villani R, Navarese EP, Cavallone F, et al. Risk of Statin-Induced Hypertransaminasemia: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Mayo Clin Proc Innov Qual Outcomes. 2019;3(2):131-140. Published 2019 May 5. doi:10.1016/j.mayocpiqo.2019.01.003
[2] Wang X, Li J, Wang T, et al. Associations between statins and adverse events in secondary prevention of cardiovascular disease: Pairwise, network, and dose-response meta-analyses of 47 randomized controlled trials. Front Cardiovasc Med. 2022;9:929020. Published 2022 Aug 25. doi:10.3389/fcvm.2022.929020
[3] Cai T, Abel L, Langford O, et al. Associations between statins and adverse events in primary prevention of cardiovascular disease: systematic review with pairwise, network, and dose-response meta-analyses. BMJ. 2021;374:n1537. Published 2021 Jul 14. doi:10.1136/bmj.n1537
[4] Björnsson ES. Hepatotoxicity of statins and other lipid-lowering agents. Liver Int. 2017;37(2):173-178. doi:10.1111/liv.13308

Literature Review

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

Is there any difference in hepatotoxicity, specifically LFT elevations, amongst statins?

Level of evidence

B - One high-quality study or multiple studies with limitations  Read more→



Please see Tables 1-2 for your response.


 

High Dose Atorvastatin Associated with Increased Risk of Significant Hepatotoxicity in Comparison to Simvastatin in UK GPRD Cohort

Design

Retrospective Cohort Study; N=242,023

Objective

To compare the risk of hepatotoxicity in atorvastatin relative to simvastatin treatment 

Study Groups

Simvastatin (n=165,188)

Atorvastatin (n=76,835)

Inclusion Criteria

Age ≥18, first prescription of atorvastatin or simvastatin during the study period (index date), permanently registered with the practice for a minimum of 12 months prior to index date 

Exclusion Criteria

Alcohol-related diagnosis, pre-existing liver disease, abnormal liver function, previous prescription of a statin 

Methods

Patients were identified on the UK General Practice Research Database (GPRD) for having a first-time prescription for atorvastatin (n=76,835) or simvastatin (n=165,188). High-dose statins were classified as 40-80 mg daily whereas low-dose statins were 10-20mg daily. 

Patients were followed up either until the end of the study period, if they changed or stopped the statin, dose of statin was altered, the patient died, or were within a 90-day period of a code recording liver disease that was not drug-induced.  

Duration

January 1st 1997- December 31st 2006

Outcome Measures

Primary Outcome:

  • Episode of moderate to severe hepatotoxicity (bilirubin ≥ 60 μmol/L, AST or ALT ≥ 200 U/L [5 x ULN] or ALP > 4 x ULN or ≥ 1200 U/L) within the first six months of follow-up after initiation of therapy

Secondary Outcomes:

  • Mild liver dysfunction (bilirubin 40-59 μmol/L, AST or ALT 120-199 U/L or ALP 2-4 x ULN or 600-1199 U/L)
  • Severe liver dysfunction (bilirubin ≥80 μmol/L, AST or ALT ≥ 400 U/L or ALP >6 x ULN or ≥ 1800 U/L)

Baseline Characteristics

  

Simvastatin 10-20 mg 

Simvastatin 40-80 mg

Atorvastatin 10-20 mg   Atorvastatin 40-80 mg 

Age, years

 

 66 ± 12   65 ± 12   64 ± 12   62 ± 13

Male

 

 61,299  (50.9%)   24,659  (55%)   37,341  (51.3%)  2,355 (57.55%) 

BMI

 

 27.9 ± 5.2  28.3 ± 5.5   28.3 ± 5.3   28.2 ± 5.4

Serum cholesterol, mmol/L

 

 6.3 ± 1.1  6.2 ± 1.2  6.5 ± 1.2  6.5 ± 1.6 

Length of follow-up, years

 

1.9 ± 2 1.3 ± 1.2  2.4 ± 1.9   1.4 ± 1.3
 

Endpoint

 

Simvastatin 10-20 mg

Simvastatin 40-80 mg

Atorvastatin 10-20 mg    Atorvastatin 40-80 mg 

Bilirubin

 Mild

 Moderate

 Severe 

 10 (17%)

  2 (3%)

  8 (11%)

 5 (16%)

 2 (6%)

 1 (3%)

 7 (14%)

 2 (4%)

 9 (18%) 

 1 (6%)

 2 (12%)

 0 (0%)

AST  

 Mild

 Moderate

 Severe

  1 (2%)

 19 (45%)

 10 (24%)

  3 (9%)

 21 (62%)

  7 (21%)

  4 (9%)

 23 (53%)

 10 (23%) 

 1 (7%) 

 9 (64%) 

 3 (21%) 

ALT

 Mild

 Moderate

 Severe

 2 (9%)

 8 (35%)

 6 (26%)

 2 (18%)

 6 (55%)

 1 (9%)

 3 (23%)

 5 (38%)

 3 (23%)

 2 (40%)

 2 (40%)

 1 (20%)

ALP

 Mild

 Moderate

 Severe

 20 (33%)

 10 (16%)

  7 (11%)

 1 (3%)

 2 (6%)

 3 (10%)

 12 (23%)

 11 (21%)

  7 (13%)

 6 (35%)

 4 (24%)

 4 (24%)

  • Mild liver dysfunction (bilirubin 40-59 μmol/L, AST or ALT 120-199 U/L or ALP 2-4 x ULN or 600-1199 U/L)
  • Moderate liver dysfunction (bilirubin 60-79 μmol/L, AST or ALT 200-399 U/L or ALP 4-6 x ULN or 1200-1799 U/L)
  • Severe liver dysfunction (bilirubin ≥80 μmol/L, AST or ALT ≥ 400 U/L or ALP >6 x ULN or ≥ 1800 U/L)

Adverse Events

Common Adverse Events: N/A

Serious Adverse Events: Hepatotoxicity (atorvastatin 0.09% and simvastatin 0.06%)

Percentage that Discontinued due to Adverse Events: N/A

Study Author Conclusions

In conclusion, patients on atorvastatin were found to have an overall increased risk of hepatotoxicity in comparison to those on simvastatin. This increased risk was predominantly experienced by patients on high-dose atorvastatin. This risk of measured hepatic events was significantly higher than previously reported studies which were based upon healthcare reporting and may reflect under-reporting in such systems. Low-dose statin therapy appears to be relatively safer than high-dose atorvastatin in our study. 

InpharmD Researcher Critique

The study has a high frequency of missing data due to variation among the clinicians with recording data within the retrospective database. Additionally, since the reference ranges for laboratory values differ between practices, the study utilized set laboratory criteria for mild, moderate, and severe hepatotoxicity. 



References:

Clarke AT, Johnson PC, Hall GC, Ford I, Mills PR. High Dose Atorvastatin Associated with Increased Risk of Significant Hepatotoxicity in Comparison to Simvastatin in UK GPRD Cohort. PLoS One. 2016;11(3):e0151587. doi:10.1371/journal.pone.0151587

 

Spectrum of statin hepatotoxicity: experience of the drug-induced liver injury network

Design

Report of an ongoing multicenter, prospective study

N= 22

Objective

To provide detailed information on the presentation and course of 22 cases of statin-induced liver injury which underwent expert adjudication and standardized collection of clinical data, laboratory tests, and when available liver biopsy findings

Study Groups

Statin-induced liver injury (N= 22)

Inclusion Criteria

Patients prospectively entered into the U.S. Drug-Induced Liver Injury Network (DILIN):

Age > 2 years, enrolled within 6 months of a liver injury onset due to a drug or herbal product, appearance of one of the following laboratory criteria:

1. Serum liver biochemistries were normal prior to starting suspect drug serum ALT >5×ULN on two consecutive occasions or serum AST >5×ULN on two consecutive occasions or serum alkaline phosphatase >2×ULN on two consecutive occasions

2. Serum liver biochemistries were elevated prior to starting suspect drug serum ALT >5×pre-drug average on two consecutive occasions or serum AST >5×pre-drug average on two consecutive occasions or serum alkaline phosphatase >2×pre-drug average on two consecutive occasions

3. Serum total bilirubin >2.5mg/dL and an elevated AST, ALT or alkaline phosphatase (without known hemolysis or Gilbert’s syndrome)

4. INR >1.5 along with an elevated AST, ALT or alkaline phosphatase (without known coumadin therapy or vitamin K deficiency)

Exclusion Criteria

Acetaminophen toxicity, pre-existing liver disease, diseases that may confound diagnosis, liver/bone marrow transplant prior to enrollment, identifiable competing cause of liver injury

Methods

Patients consented to be entered in the DILIN to receive a full examination consisting of physical and medical history for suspected and concomitant drugs to analyze for causality with liver injury. 

The Roussel Uclaf Causality Assessment Method (RUCAM) was utilized to determine the causality between drug and liver injury. Expert opinion must have judged the cases to have at least a 74% or above likelihood for a drug to cause liver injury. Statin must have the highest causality score.

Out of 1,188 patients, 22 were found to have plausible statin-induced liver injury and were included for analysis.

Duration

Enrollment period: September 2004 to November 2012

Follow-up: 6 months

Outcome Measures

Peak alkaline phosphatase levels observed in each statin 

Baseline Characteristics

 

Statin-induced liver injury (N= 22)

Median age, years

60 (41 to 80)

Female

68% 

White

82% 

Body mass index, kg/m2

24 (19 to 38)

Onset

< 12 weeks

12 to 24 weeks

> 24 weeks

 

27%

27%

45%

Jaundice

68%

Itching

36%

Rash

18%

Initial Alkaline phosphatase, U/L

338 (79 to 1,952)

Severity score

Mild (1+)

Moderate (2+)

Moderate Hospitalized (3+)

Severe (4+)

Fatal (5+)

 

32%

32%

18%

14%

4%

Results

Endpoint

Statin-induced liver injury (N= 22)

Peak alkaline phosphatase levels, U/L

Atorvastatin (n= 8)

Fluvastatin (n= 2)

Lovastatin (n= 1)

Pravastatin (n= 2)

Rosuvastatin (n= 4)

Simvastatin (n= 5)

 

200 to 1,952

188, 208

724

95, 234

184 to 526

121 to 538

Outcome where the liver injury had resolved

Atorvastatin (n= 8)

Fluvastatin (n= 2)

Lovastatin (n= 1)

Pravastatin (n= 2)

Rosuvastatin (n= 4)

Simvastatin (n= 5)

 

8/8

1/2*

1/1

1/2*

2/4*

4/5^

*four total patients developed chronic liver injury

^One patient in the simvastatin group died

Study Author Conclusions

Drug-induced liver injury from statins is rare and characterized by variable patterns of injury, a range of latencies to onset, autoimmune features in some cases, and persistent or chronic injury in 18% of patients most of whom have an autoimmune phenotype.

InpharmD Researcher Critique

The information is limited but demonstrates that various statin agents can potentially elevate alkaline phosphatase levels. However, this study enrolled patients who had a diagnosis of liver injury. The risk of an asymptomatic increase in alkaline phosphatase levels from each statin is unknown. 



References:

Russo MW, Hoofnagle JH, Gu J, et al. Spectrum of statin hepatotoxicity: experience of the drug-induced liver injury network. Hepatology. 2014;60(2):679-686. doi:10.1002/hep.27157