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    35 Drugs Used Dyslipidemia

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    Nibshian Dela Rosa
    The document discusses drugs used to treat hyperlipidemias, including statins which work by inhibiting HMG-CoA reductase to lower cholesterol levels, resins which bind bile acids to reduce cholesterol absorption, ezetimibe which prevents cholesterol absorption, and niacin which reduces triglyceride and VLDL secretion. The drugs are generally well-tolerated oral therapies but can have side effects like liver toxicity, myopathy, and gastrointestinal issues that require monitoring. Lifestyle modifications like a low-cholesterol diet are also important treatment strategies.

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    35 Drugs Used Dyslipidemia

    Uploaded by

    Nibshian Dela Rosa
    152 views58 pages
    The document discusses drugs used to treat hyperlipidemias, including statins which work by inhibiting HMG-CoA reductase to lower cholesterol levels, resins which bind bile acids to reduce cholesterol absorption, ezetimibe which prevents cholesterol absorption, and niacin which reduces triglyceride and VLDL secretion. The drugs are generally well-tolerated oral therapies but can have side effects like liver toxicity, myopathy, and gastrointestinal issues that require monitoring. Lifestyle modifications like a low-cholesterol diet are also important treatment strategies.

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    The document discusses drugs used to treat hyperlipidemias, including statins which work by inhibiting HMG-CoA reductase to lower cholesterol levels, resins which bind bile acids to reduce cholesterol absorption, ezetimibe which prevents cholesterol absorption, and niacin which reduces triglyceride and VLDL secretion. The drugs are generally well-tolerated oral therapies but can have side effects like liver toxicity, myopathy, and gastrointestinal issues that require monitoring. Lifestyle modifications like a low-cholesterol diet are also important treatment strategies.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    152 views58 pages

    35 Drugs Used Dyslipidemia

    Uploaded by

    Nibshian Dela Rosa
    The document discusses drugs used to treat hyperlipidemias, including statins which work by inhibiting HMG-CoA reductase to lower cholesterol levels, resins which bind bile acids to reduce cholesterol absorption, ezetimibe which prevents cholesterol absorption, and niacin which reduces triglyceride and VLDL secretion. The drugs are generally well-tolerated oral therapies but can have side effects like liver toxicity, myopathy, and gastrointestinal issues that require monitoring. Lifestyle modifications like a low-cholesterol diet are also important treatment strategies.

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    A. Q.

    Sangalang, MD, FPOGS, RMT


    FACULTY OF PHARMACY
    UNIVERSITY OF SANTO TOMAS
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS
    METABOLISM
    OF PLASMA
    LIPOPROTEINS Loading...
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    METABOLISM
    OF PLASMA
    LIPOPROTEINS
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HYPERLIPOPROTEINEMIA
    PATHOGENESIS
    Premature or accelerated development of atherosclerosis
    Elevated levels of certain plasma lipoproteins

    Loading...
    Low-density lipoproteins (LDLs)
    Participate in cholesterol transport
    Depressed level of high-density lipoproteins
    (HDLs)
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    Chylomicronemia
    Occurrence of chylomicrons in the serum while fasting
    Recessive trait that is correlated with a high incidence of acute
    pancreatitis
    Restriction of total fat intake
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    Regulation of plasma lipoprotein levels involves a balance


    Dietary fat intake
    Hepatic processing
    Utilization in peripheral tissues
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    Diet
    Alcohol raises levels of
    Tricglycerides
    Very-low-density liporoteins (VLDL)
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    Primary disturbances in regulation


    Occur in various familial diseases
    Secondary disturbances
    Associated with
    Western diet
    Endocrine conditions
    Diseases of the liver or kidneys
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    TREATMENT STRATEGIES
    Diet
    First method of management
    May be sufficient to reduce lipoprotein levels to a safe range
    Cholesterol and saturated fats
    Primary factors that contribute to elevated levels of plasma lipoproteins
    Triglyceride and VLDL
    Elevated by alcohol intake
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    TREATMENT STRATEGIES
    Drugs
    Drug therapy
    All drugs given oral
    Loading...
    Can modify hepatic cholesterol synthesis
    Hepatic hydroxymethylglutaryl coenzyme A
    (HMG-CoA) reductase inhibitors
    Reduce cholesterol
    Ezetimibe
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    TREATMENT STRATEGIES
    Drugs
    Drug therapy
    Reduce bile acid
    Resins
    Reduce absorption from the intestines and decrease secretion of
    lipoproteins
    Niacin
    Increase peripheral clearance of lipoproteins
    Fibrates
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE INHIBITORS


    MECHANISM AND EFFECTS
    Lovastatin and Simvastatin
    Inactive lactone prodrugs
    Pravastatin
    Open active lactone ring
    Atorvastatin, Fluvastatin, Rosuvastatin
    Active fluorine-containing congeners
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE INHIBITORS


    MECHANISM AND EFFECTS
    Structural analogs that competitively inhibit
    mevalonate synthesis by HMG-CoA reductase
    First committed step in cholesterol biosynthesis in the liver
    Most effective in reducing LDL
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE INHIBITORS


    MECHANISM AND EFFECTS
    Minimal total serum cholesterol-lowering effect
    Greater effect in the reduction of the tightly
    regulated hepatic pool of cholesterol
    Liver compensates by increasing high affinity
    LDL receptors that clear LDL from the blood
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE INHIBITORS


    MECHANISM AND EFFECTS
    Have direct anti-atherosclerotic effects
    It prevents bone loss
    DRUGS USED IN THE TREATMENT OF

    DRUGS USED IN THE TREATMENT OF


    HYPERLIPIDEMIAS
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE INHIBITORS


    CLINICAL USE
    Statins
    Reduce LDL cholesterol levels dramatically
    when used in combination with other drugs
    Used commonly
    Effective and well tolerated
    Standard practice to initiate therapy after acute coronary syndrome
    regardless of lipid levels
    Reduces risk of coronary events, mortality among patients with IHD, risk
    of ischemic stroke
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE INHIBITORS


    CLINICAL USE
    Cholesterol synthesis occurs predominantly at night
    Should be given in the evening
    Except for Atorvastatin and Rosuvastatin
    Absorption is enhanced by food
    Except Pravastatin
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE INHIBITORS


    CLINICAL USE
    Rosuvastatin, Atorvastatin, Simvastatin
    Higher efficacy than other reductase inhibitors
    Reduce triglycerides and increase HDL levels in patients with trigly levels
    of >250mg/dL
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE INHIBITORS


    CLINICAL USE
    Rosuvastatin
    Most efficacious agent for severe hypercholesterolemia

    Fluvastatin
    Less maximal efficacy than the other drugs
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE INHIBITORS


    TOXICITY
    Mild elevations of serum aminotransferase not often associated with hepatic
    damage
    More severe reactions in patients with
    preexisting liver disease
    Monitor at baseline, at 1-2 months then every 6-12 months
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE INHIBITORS


    TOXICITY
    Increase in creatine kinase
    Released from skeletal muscles
    10% of patients
    Severe muscle pain in few patients
    Rhabdomyolysis and myoglobinuria may occur
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HMG-CoA REDUCTASE
    INHIBITORS
    TOXICITY
    Metabolized by the cytochrome P450
    Drugs or food (e.g., grapefruit
    juice) that inhibit cytochrome P450
    activity
    Increase the risk of
    hepatotoxicity and myopathy
    Teratogenic
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    RESINS
    MECHANISMS AND EFFECTS
    Cholestyramine, Colestipol, and Colesevelam
    Bile acid-binding resins
    Large nonabsorbable polymers that bind
    bile acids and similar steroids in the intestine
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    RESINS
    MECHANISMS AND EFFECTS
    Bile acids, metabolites of cholesterol are absorbed in the jejunum and ileum
    Excretion is increased up to 10 fold when resins are given
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    RESINS
    MECHANISMS AND EFFECTS
    Prevents absorption of dietary cholesterol
    and reduces reabsorption of bile acids
    secreted by the liver
    Divert hepatic cholesterol to the synthesis
    of new bile acids
    Reduces the amount of cholesterol in a
    tightly regulated pool
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    RESINS
    MECHANISMS AND EFFECTS
    Liver compensates by increasing high affinity LDL receptors that clear LDL
    from the blood
    Modest reduction in LDL
    Loading...
    Useful only for isolated increases of LDL
    Little effect on the HDL or triglycerides
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    RESINS
    CLINICAL USE
    Patients with hypercholesterolemia
    Reduce pruritus in patients with cholestasis
    and bile salt accumulation
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    RESINS
    TOXICITY
    Bloating
    Constipation
    Unpleasant gritty taste
    Absorption of the following is impaired
    Vitamins (Vitamin K, dietary folates)
    Drugs (Pravastatin, Fluvastatin, Digitalis, Warfarin, Thiazides)
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    EZETIMIBE
    MECHANISM AND EFFECTS
    Prodrug
    Converted in the liver to active glucuronide
    Prevents GI uptake of cholesterol and phytosterols
    (plant sterols that normally enter GI epithelial cell
    but are immediately transported back into the
    intestinal lumen)
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    EZETIMIBE
    MECHANISM AND EFFECTS
    Prevents absorption of dietary cholesterol and cholesterol excreted from
    the bile
    Reduces the cholesterol in the tightly regulated hepatic pool
    Liver compensates by increasing high affinity LDL receptors that clear
    LDL from the blood
    LDL from the blood
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    EZETIMIBE
    MECHANISM AND EFFECTS
    As monotherapy
    Reduces LDL cholesterol by about 18%
    More effective when combined with a reductase inhibitor
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    EZETIMIBE
    CLINICAL USE
    Treatment of hypercholesterolemia
    Phytosterolemia
    Rare genetic disorder that results from impaired export of
    phytosterols
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    EZETIMIBE
    TOXICITY
    Well tolerated
    When combined with reductase inhibitors
    May increase the risk of hepatic toxicity
    Serum concentrations of the glucuronide form
    Increased by fibrates
    Reduced by cholestyramine
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    NIACIN (NICOTINIC ACID)


    MECHANISM AND EFFECTS
    Niacin (but not Nicotinamide)
    Directly reduces the secretion of triglycerides, VLDL and LDL
    Increases HDL level
    Reduced catabolic rate for HDL
    Inhibits hepatic synthesis of apolipoproteins or cholesterol
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    NIACIN (NICOTINIC ACID)


    TOXICITY
    Cutaneous flushing
    Common
    Pretreatment with aspirin or other NSAIDs
    Reduces the intensity of cutaneous flushing
    Mediated by prostaglandin release
    Tolerance to the flushing reaction develops
    within a few days
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    NIACIN (NICOTINIC ACID)


    TOXICITY
    Dose-dependent nausea
    Abdominal discomfort
    Pruritus
    Other skin problems
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    NIACIN (NICOTINIC ACID)


    TOXICITY
    Moderate elevations of liver enzymes
    Severe hepatotoxicity
    Hyperuricemia
    20% of patients
    Carbohydrate tolerance may be moderately impaired
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    SITES OF ACTION OF
    HMG-COA REDUCTASE
    INHIBITORS, NIACIN,
    EZETIMIBE, AND RESINS
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    FIBRIC ACID DERIVATIVES


    MECHANISM AND EFFECTS
    Gemfibrozil, Fenofibrate, Clofibrate, Bezafibrate
    Ligands for the peroxisome proliferator
    -activated receptor-alpha (PPAR-) protein
    Receptor that regulates transcription of genes involved
    in lipid metabolism
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    FIBRIC ACID DERIVATIVES


    MECHANISM AND EFFECTS
    Increases activity of lipoprotein lipase
    Enhances clearance of triglyceride-rich lipoproteins
    Cholesterol biosynthesis in the liver is secondarily reduced
    Stimulate fatty acid oxidation limits supply of triglycerides
    decreases VLDL synthesis
    Decreases expression of apoC-III impedes clearance
    of VLDL
    Increases expression of apoA-I and apoA-II increases HDL levels
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    HEPATIC AND
    PERIPHERAL EFFECTS
    OF FIBRATES
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    FIBRIC ACID DERIVATIVES


    MECHANISM AND EFFECTS
    Reduce serum triglyceride concentrations
    Small reduction in LDL
    Small increase in HDL levels
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    FIBRIC ACID DERIVATIVES


    CLINICAL USE
    Treatment of hypertriglyceridemia
    Modest effects on LDL cholesterol
    Combined with other cholesterol-lowering drugs
    Patients with elevated concentrations of both LDL and VLDL
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    FIBRIC ACID DERIVATIVES


    TOXICITY
    Nausea is most common with all the drugs
    Skin rashes
    Common with Gemfibrozil
    Decreases in white blood count or hematocrit
    Can potentiate the action of anticoagulants

    Can potentiate the action of anticoagulants


    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    FIBRIC ACID DERIVATIVES


    TOXICITY
    Increased risk of cholesterol gallstones
    Caution in patients with a history of cholelithiasis
    When combined with reductase inhibitors

    Increase risk of myopathy


    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    COMBINATION THERAPY
    Dietary modification
    First treatment for all patients with hyperlipidemia
    Often insufficient and drugs must be added
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    COMBINATION THERAPY
    Drug combinations
    Often required to achieve the maximum lowering
    possible
    Minimum toxicity
    Achieve the desired effect on the various lipoproteins (LDL, VLDL,
    HDL)
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    COMBINATION THERAPY
    Presents as a challenge
    Resins
    Interfere with the absorption of certain reductase inhibitors
    Pravastatin, Cerivastatin, Atorvastatin, and Fluvastatin
    Given at least 1 hour before or 4 hours
    after the resins
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

    COMBINATION THERAPY
    Presents as a challenge
    Combination of reductase inhibitors with either fibrates or niacin
    Increases the risk of myopathy
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS
    DRUGS USED IN THE TREATMENT OF
    HYPERLIPIDEMIAS

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