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    Home > Active Ingredient News > Endocrine System > Ten questions and answers: Clinical application of "statins" in the elderly population

    Ten questions and answers: Clinical application of "statins" in the elderly population

    • Last Update: 2023-01-07
    • Source: Internet
    • Author: User
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    Atherosclerotic cardiovascular disease (ASCVD) is the main cause of death and disability in the elderly, and the prevalence and mortality rate increase
    with age.
    Dyslipidemia is an independent risk factor for ASCVD and cardiovascular events, and there is substantial evidence that statins delay the onset and progression of ASCVD and reduce the risk of
    cardiovascular events and death.

     

    However, due to concerns about drug safety, the elderly population tends to have insufficient medication and high
    discontinuation rates.
    Combined with the "Chinese Expert Consensus on the Management of Dyslipidemia in the Elderly", this article talks about which elderly people should take statins and what details
    should be paid attention to when taking statins.

     

    What are the pharmacological effects and indications of statins?

     

    The main pharmacological effect is to inhibit the biosynthesis of HMG-CoA reductase and cholesterol in the liver, thereby reducing the concentration of cholesterol and serum lipoprotein in plasma, and is now mainly used for hypercholesterolemia, coronary heart disease, stroke patients and other people
    .


    What are the motility features of statins?

     

    High protein binding rate, extensive first-pass metabolism, most of the bioavailability is low, mainly metabolized by liver P450 enzyme, mainly excreted from feces through the biliary tract
    .

     

    Which older adults should take statins? What is the goal of lipid adjustment?

     

    1.
    Elderly patients with ASCVD: It is recommended that elderly patients with ASCVD actively use statins, and for elderly people at risk of cardiovascular disease, blood lipid management goals
    are formulated according to cardiovascular disease risk stratification.

     

    Table 1 Target values of lipid-regulating therapy for the elderly [mmol/L (mg/dl)]

     


    2.
    Statins
    are recommended for elderly people ≤ 75 years old but with multiple cardiovascular risk factors.

     

    3.
    For the elderly aged > 75 years old with high cardiovascular risk, comprehensive assessment of life expectancy, frailty, comorbid diseases, liver and kidney function, economic factors and other factors should be carried out, and the benefit-risk ratio, drug interactions, adverse reactions and personal willingness to decide whether to use low- and medium-dose statins should be weighed
    .

     

    What are the contraindications to statins?

     

    ➤ People who are allergic to statins;

    ➤ People with active liver disease;

    ➤ Unexplained persistent elevation of liver aminotransferases;

    Pregnant and lactating women, etc
    .

     

    Statins, when do they work well?

     

    ➤Lovastatin and simvastatin are easier to absorb when taken with food; rosuvastatin, atorvastatin, fluvastatin, and pitavastatin are not affected by food; Pravastatin is taken with food to reduce absorption
    .

     

    ➤Since the synthesis of cholesterol in the liver reaches its peak at night, fluvastatin, lovastatin, and simvastatin have short half-lives, it is recommended to take them at night;

     

    ➤Atorvastatin, pitavastatin, and rosuvastatin have long half-lives and can be taken
    at any time.

     

    Table 2 Statins reduce the amplitude and dose of LDL-C

     


    Note 4 details:

     

    ➤ The adverse reactions of statins increase with the increase of dose, and most elderly people can use medium and small doses of statins to achieve LDL-C standards;

    ➤ Statins should be started with small or moderate doses and adjusted according to efficacy, and the dose can be reduced or switched to different types of statins if they are intolerated;

    ➤ Elderly people whose TC or LDL-C decreases rapidly after taking low-dose statins should be investigated for tumors and other wasting diseases
    .

    ➤Lipid-regulating drugs should be used for a long time, and should not be discontinued without special reasons
    .
    After stopping the drug, blood lipids increased or even rebounded, which significantly increased cardiovascular events and mortality
    .

     

    What is the difference in statin dosage and intensity?


    ➤Low-intensity therapeutic doses: simvastatin 10mg, pravastatin 10-20mg, lovastatin 10-20mg, fluvastatin 20-40mg, pitavastatin 1mg;
    ➤Moderate intensity dose: atorvastatin 10-20mg, rosuvastatin 5-10mg, simvastatin 20-40mg, pravastatin 40-80mg, lovastatin 40mg, fluvastatin 80mg, pitavastatin 2-4mg;
    ➤High-intensity dosage: atorvastatin 40-80mg, rosuvastatin 20-40mg
    .

     

    Table 3 Statin strength and daily dosage


    What should I do if my blood lipids still do not meet the standard after using statins?

     

    When LDL-C at a tolerable dose of statins is not met, ezetimibe or PCSK9 inhibitors
    can be added.

     

    When total cholesterol (TG) is elevated, secondary factors should first be excluded or corrected and lifestyle interventions
    performed.
    For ASCVD patients or very high-risk elderly people, when non-HDL-C does not meet the standard or TG continues to rise (2.
    3~5.
    6 mmol/L) after statin therapy, fibrates or fish oil preparations can be combined with fibrates (high-purity EPA is preferred).

    Fasting TG ≥ 5.
    6 mmol/L, TG should be lowered first, and fibrates and fish oil preparations (high-purity EPA is preferred) are
    preferred.

     

    Statins, how safe are they?

     

    The safety and tolerability of statins in older adults is generally good, but related adverse effects
    should still be recognized and managed in a timely manner.
    In general, the adverse effects of statins increase with increasing dose, and common adverse effects include abnormal liver function, muscle damage, CKD, and newly diagnosed diabetes
    .

     

    When do I need to stop the drug?

     

    Blood lipids, muscle enzymes and liver and kidney function should be reviewed 4 weeks before and after taking statins, and adverse reactions such as myalgia, fatigue and digestive tract symptoms should be monitored when taking the drug, and long-term use should be followed up regularly
    .
    Patients who develop muscle or digestive symptoms after taking statins should have muscle enzymes and liver function
    monitored.

     

    ➤If the increase in blood creatine kinase (CK) does not exceed 4 times the upper limit of normal and the muscle symptoms are mild, or the elevation of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) does not exceed 3 times the upper limit of normal, statins can be continued and re-examined
    .

     

    ➤ If the blood CK is elevated more than 4 times the upper limit of normal or ALT, AST is more than 3 times the upper limit of normal and bilirubin is elevated, the dose of statins should be stopped or reduced, and the benefits/risks of statins should be evaluated again after returning to normal, and whether to continue taking statins or switch to other lipid-modifying drugs; If you need to continue to use lipid-modifying drugs, you can change the type or reduce the dose and observe
    closely.

     

    ➤ If CK is elevated more than 10 times the upper limit of normal, statins should be stopped immediately and admitted to the hospital for hydration therapy
    .
    If the standard is not met for 3~6 months, the dose or type of statin should be adjusted, and ezetimibe or PCSK9 inhibitors should be added if necessary, and rechecked
    every 6~12 months after reaching the standard.

     

    What medications may statins interact with?

     

    When the elderly have decreased liver and kidney function and combine with a variety of drugs, drug interactions and adverse reactions are prone to occur, and drugs with different metabolic pathways in the body should be selected
    .
    When statins are combined with other lipid-modifying drugs, they can increase the risk of liver and muscle damage, and it is necessary to pay attention to the individual characteristics and tolerance of the elderly, avoid high-dose combinations, and monitor drug interactions and adverse reactions
    .

     

    ➤ Statins combined with niacin or fibrates increase the risk of
    myopathy.

     

    ➤When statins are combined with drugs metabolized by CYP450 enzyme and affect P-glycoprotein (P-gp), the risk of adverse statin reactions increases
    .
    Specifically, inhibitors increase statin plasma concentrations by competing for binding sites or reducing enzyme and protein activity by increasing statin bioavailability or reducing statin clearance, and inducers increasing CYP450 enzyme or P-gp activity accelerate statin metabolism and reduce statin plasma concentration
    .

     

    Table 4 CYP450 enzyme and P-glycoprotein inhibitors and inducers affecting statin metabolism

     


    Resources:

    LIU Meilin, ZHANG Yumeng, FU Zhifang, et al.
    Chinese expert consensus on the management of dyslipidemia in the elderly[J].
    Chinese Journal of Internal Medicine, 2022, 61(10) : 1095-1118.
    DOI: 10.
    3760/cma.
    j.
    cn112138-20220407-11251.

    [2] Statin drug inserts.

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