Can statins continue to be used if transaminase is elevated?

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Can statins continue to be used if transaminase is elevated?

Can statins continue to be used if transaminase is elevated?  Statins, namely hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors, exert a lipid-lowering effect by inhibiting the synthesis of cholesterol in the body, while also stabilizing atherosclerotic plaque, anti-inflammatory, and improving The stability of vascular endothelial cells is widely used clinically for secondary prevention of coronary heart disease, stroke and other diseases.

However, clinically, many patients using statins have elevated transaminases during treatment, and some patients even develop drug-induced hepatitis. So, can statins continue to be used after abnormal liver function? How should the indications and strategies of drug adjustment be defined?

1. What are the characteristics of elevated transaminase caused by statins?

Relevant data show that all statins may cause elevated transaminases. Among all patients receiving statin therapy, about 1% to 2% have increased liver enzyme levels that exceed the upper limit of normal by 3 times.

The elevation of transaminase caused by statin drugs usually occurs within 3 months after the start of the drug, and is dose-dependent. The liver enzyme level can decrease after the drug is stopped. The specific mechanism is not clear.
At present, most scholars believe that transaminase transient beyond the normal range is the result of the process of organ adapting to statins and the result of lowering cholesterol, not a sign of liver damage.

2. How to adjust the medication when the transaminase is elevated?

1) For asymptomatic patients with simple transaminase elevation (transaminase <3ULN), there is no need to adjust the dose or discontinue treatment;

2) During medication, if AST and (or) ALT ≥ 3ULN, you should consider stopping or reducing the dose, and review liver function weekly until it returns to normal;

3) Patients with elevated transaminases accompanied by hepatomegaly, jaundice, elevated direct bilirubin or prolonged clotting time should consider discontinuing the drug;

4) Patients with non-alcoholic fatty liver (NAFLD), hepatitis B (HBV), hepatitis C (HCV) and compensated liver cirrhosis with mildly impaired liver function are safe to use statins. Among them, carry HBV and compensated liver Patients with cirrhosis should strengthen liver function monitoring;

5) Patients with active liver disease, decompensated liver cirrhosis, and acute liver failure should not use statins;
6) Rosuvastatin is hydrophilic, 90% of which is excreted through the kidneys in its original form, and should be used for patients with liver insufficiency;

7) Atorvastatin, simvastatin, etc. are mainly metabolized by the liver and cleared by bile. Patients with renal insufficiency should be used.

3. Or alternative drugs

1) Ezetimibe

As a cholesterol absorption inhibitor, ezetimibe is currently the first-line second-line medication for statin intolerance or when statin therapy alone does not meet the standard.

In a clinical controlled study using ezetimibe alone, the incidence of elevated transaminase (ALT/AST ≥ 3ULN) caused by ezetimibe and placebo was similar;

For patients with mild hepatic insufficiency (Child-Pugh score 5-6 points), there is no need to adjust the dosage; patients with moderate to severe hepatic dysfunction are not recommended to use ezetimibe.

2) Bile acid chelator

It is a basic anion exchange resin that binds with bile acids in the small intestine to prevent its reabsorption, promotes the synthesis of bile acids from cholesterol in the liver, increases the activity of LDL-C receptors in the liver, and removes LDL-C in the plasma.

Common adverse reactions include gastrointestinal discomfort, constipation and affecting the absorption of certain drugs. The absolute contraindications of these drugs are complete biliary atresia, abnormal β lipoproteinemia, and serum TG> 4.5 mmol/L (400 mg/dL).

3) PCSK9 inhibitor

PCSK9 is a secreted serine protease synthesized by the liver, which can bind to and degrade LDL receptors, thereby reducing the clearance of serum LDL-C by LDL receptors. By inhibiting PCSK9, it can prevent the degradation of LDL receptors and promote the clearance of LDL-C.

The results of the study showed that PCSK9 inhibitors, whether used alone or in combination with statins, significantly reduced serum LDL-C levels, while improving other blood lipid indicators.

Preliminary clinical research results show that the drug can reduce LDL-C by 40% to 70% and reduce cardiovascular events. So far, no serious or life-threatening adverse reactions have been reported.

(source:internet, reference only)

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