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Hypolipidemic Drugs and plasma expanders PowerPoint Presentation

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Description : Check out this medical PowerPoint presentation titled "Hypolipidemic Drugs and plasma expanders" by Dr. Rishi Pal.

This medical PowerPoint presentation talks about Hypolipidemic Drugs and plasma expanders. Hypolipidemic drugs are medications used to lower lipid levels in the blood, primarily cholesterol and triglycerides. Plasma expanders, on the other hand, are substances used to increase the volume of blood plasma, which can be useful in certain medical conditions such as shock or dehydration.

Tags : Hypolipidemic Drugs, plasma expanders, cardiology

Published on : Mar 17, 2023 | Views : 3115 | Downloads : 11

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Slide 1-

Hypolipidemic Drugs and plasma expanders Dr. Rishi Pal Assistant Prof. Deptt. of Pharmacology
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Cholesterol Critical substrate for the body: Fundamental building block of steroid hormones Essential for building cell membranes, the myelin sheath, and the brain Core component of bile salts, which helps in digest dietary fats 29-2
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Lipoproteins There are several different lipoproteins: Low-density lipoprotein (LDL) Very-low-density lipoprotein (VLDL) High-density lipoprotein (HDL) 29-3
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Triglycerides Main form of fat from diet Provide body with energy Chylomicrons: Very large lipoproteins that deliver triglycerides to muscle and fat tissue 29-4
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Hypolipidemic Drugs There are five groups of drugs used in the management of hyperlipidemia: HMG-CoA reductase inhibitors Cholesterol absorption inhibitors Bile acid sequestrants Fibric acid derivatives Nicotinic acid 29-7
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Atherosclerosis Atherosclerosis is a progressive condition that leads to CAD and PAD. Fat buildup inside the arteries—plaque CAD—coronary artery disease PAD—peripheral artery disease 29-9
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Atherosclerosis There are two types of plaque buildup: Stable Unstable Plaque buildup can block arteries, causing: Angina TIA Stroke Intermittent claudication 29-11
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Monitoring the Disease Risk factors for atherosclerosis Age History of smoking Hypertension Premature menopause Obesity Diabetes mellitus Hyperthyroidism 29-12
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Monitoring the Disease The goals of treatment are: Lowering LDL cholesterol Reducing total serum cholesterol and triglycerides Increasing HDL cholesterol 29-13
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HMG-CoA Reductase inhibitors Atorvasatatin Simvastatin Lovastatin Pravastatin Fluavastatin Rosuvastatin
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Bile acid binding resins Cholestyramine Colestipol Colesevelam
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Intestinal cholesterol absorption inhibitors Stanol esters Ezetimibe
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Activators of lipoprotein lipase (Fibrates) Gemfibrozil Benafibrate Fenofibrate Ciprofibrate
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Inhibitor of VLDL secretion and lipolysis Niacin (Nicotinic acid) Miscellaneous: Gugulipid and fish oil derivatives
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LIPID-LOWERING DRUGS
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HMG-CoA Reductase Inhibitors Also referred to as statins MOA—inhibit enzyme that causes cholesterol synthesis IND—adjunct to dietary treatment to decrease total serum and LDL cholesterol: Reduce LDL level up to 30% Raise HDL level up to 20% 29-21
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HMG-CoA Reductase Inhibitors An early, very important step in this process is the conversion of acetyl-CoA molecules into HMG-CoA, which is then converted to mevalonic acid by HMG-CoA reductase. Mevalonic acid is a rate-limiting pivotal step in steroid and cholesterol biosynthesis The liver makes two-thirds of the daily cholesterol requirement. 1-22
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HMG-CoA Reductase Inhibitor All of the statins reduce LDL up to 30 percent. When a greater reduction of LDL is required, simvastatin (Zocor), atorvastatin (Lipitor), and rosuvastatin (Crestor) reduce more than 45 percent; in fact, rosuvastatin and atorvastatin have been demonstrated to reduce up to 60 percent. All of the statins raise the HDL level up to 20 percent. Again, simvastatin (Zocor), atorvastatin (Lipitor), and rosuvastatin (Crestor) increase HDL more than 30 percent. 1-23
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HMG-CoA Reductase Inhibitors Adverse effects: Headache, dizziness, alteration of taste, insomnia, abdominal cramping and photosensitivity May cause myalgias, leg ache, and muscle weakness Contraindicated during pregancy 29-25
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Cholesterol Absorption Inhibitors Ezetimibe: MOA—blocks absorption of cholesterol in the intestines Decreases VLDL Decreases circulating LDL cholesterol IND—treatment of hyperlipidemia in conjunction with diet alteration 29-26
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Cholesterol Absorption Inhibitors Ezetimibe: Modestly reduces total cholesterol, LDL, and triglyceride blood levels Ideal to combine with other hypolipidemic drugs Adverse effects—abdominal pain, fatigue, coughing, diarrhea, back pain, and arthralgia 29-27
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Bile Acid Sequestrants MOA—bind bile salts and cholesterol in the GI tract, preventing absorption of both IND—hyperlipidemia: Increased elimination of bile salts, cholesterol, and other fats in the faeces. Adverse effects include GI disturbances, severe constipation, and fecal impaction. Most serious adverse effect is intestinal obstruction. 29-28
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Nicotinic Acid MOA—affects cholesterol synthesis through a G proteins coupled receptor: Inhibits triglyceride lipase Stimulates lipoprotein lipase Decreases free fatty acid release and removes triglycerides IND—hyperlipidemia Adverse effects—flushing, nausea, vomiting, and diarrhea 29-29
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Fibric Acid Derivatives (Fibrates) Gemfibrozil: MOA—inhibits breakdown of fat into triglycerides, and limits liver production of triglycerides IND—to decrease triglycerides Adverse effects—nausea, vomiting, diarrhea, and flatulence 29-30
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Gugulipid Consists of Z and E gugulsterone Inhibit cholestrol biosynthesis and also enhance rate of cholesterol excretion Dose 25 mg 3 times a day Reduced total CH, LDL-C with an elevation of HDL-C It is well tolerated, no side effect, except loose stool
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Fish oil derivative Omega-3-fatty acids Eicosa-pentanoic and docosa-hexanoic acid Prophylaxis use in high risk patient of CAD Usually formulated with vit.E
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Combination drug therapy Bile acid binding resins+Fibrates Bile acid binding resins+Niacin Bile acid binding resins+Statins Bile acid binding resins+Niacin+ Statins Niacin+Statin (Atorva 10+ Nia 500) Statins+Ezetimibe Statins+Fibrate
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Hypolipidemic Drugs 29-34
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Preferred Therapy All hypolipidemic drugs are indicated as adjunctive therapy to reduce elevated cholesterol levels. HMG-CoA reductase inhibitors are the most prescribed. Cholestyramine can also be used in the treatment of partial biliary obstruction. 29-35
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Contraindications Systemic hypolipidemic drugs should not be used in patients with liver dysfunction. Bile acid sequestrants should not be used in patients with biliary obstruction. Statins should not be used in pregnant women. 29-36
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Drug Interactions 29-37
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New drugs Cholesteryl ester transfer protein (CETP) Torcetrapib Anacetrapib
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Blood substitutes and plasma expenders
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Hypovolaemia Shock is a state of acute circulatory failure So, it is essential to restore intravascular blood volume as quickly as possible Intravenous fluid therapy
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Types of fluid used for replacement Whole blood and plasma Plasma substitute: a) Colloidal: Dextran, hydroxyethyl starch polyvenyl pyrrolidone, oxypolygelatin. b) crystalline: NaCl, dextrose solution
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Desirable properties of plasma expenders Should exert oncotic pressure comparable to plasma. Should retain in circulation and not leak out in tissues or too rapidly disposed. Should be pharmacodynamically inert. Should not be pyrogenic or antigenic Should not interfere with grouping and cross matching of blood. Should be stable and easily sterilizable and cheap.
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Substance employed are Human albumin Dextran Polygeline Hetastarch
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Albumin 100ml of 20% human albumin solution is osmotic equivalent of about 400ml of fresh frozen plasma or 800 ml of whole blood. Not interfere with blood group and coagulation process. Crystalloid solutions must be infused concurrently for optimum benefit. It is expensive.
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Dextran Dextran-40: 10% in dextrose or in NaCl Dextran-70, expends plasma volume for 24 hr. 500-1000 ml in 30 min. and 100 ml by continuous infusion for 2-3 days. Be careful in patients of Renal impairment, CHF or Polycythaemia. Dextran-70 & dextran 110: 6% in dextrose or in NaCl, used for hypovolaemic or haemorrhagic shock
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Polyvenylpyrrolidone It is synthetic water soluble preparation with MW 35,000-40,000. It is sterile solution in buffered physiological saline It has tendency to bind with insulin and penicillin
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Gelatin MW 30,000 500-1000 ml of 3.5-4% used in low blood volume Expends plasma volume for 12 hr More expensive than dextran
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Contraindications Severe anemia Cardiac failure Pulmonary edema Liver disease Renal insufficiency
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Electrolyte and water replacement Normal saline (0.9%) Dextrose 5%