Antihyperlipidemic Drugs. c h a p t e r atherosclerosis bile acid sequestrants catalyst cholesterol high-density lipoproteins (HDL). HMG-CoA. Hypolipidemic agents, or antihyperlipidemic agents, are a diverse group of pharmaceuticals that are used in the treatment of high levels of fats (lipids), such as cholesterol, in the blood (hyperlipidemia). They are called lipid-lowering drugs . Contents. 1 Classes. Established. 2 Research; 3 References; 4 See also. Chapter 18 Antihyperlipidemic Agents LEARNING OBJECTIVES Define hyperlipidemia and atherosclerosis, and their causes Classify antihyperlipidemics.
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Automatically changes to Flash or non-Flash claasification. WordPress Embed Customize Embed. Presentation Description No description available. Anti Hyperlipidemic Drugs Dr. Lipid disorders Disorders of lipid metabolism are manifest by elevation of the plasma concentrations of the various lipid and lipoprotein fractions total and LDL cholesterol, VLDL, triglycerides, xrugs and they result in cardiovascular disease and atherosclerosis deposition of fats at walls of arteries, forming plaque PowerPoint Presentation: Familial mixed hypertriglyceridemia V: Secondary hyperlipidaemias results from: The most severe hyperlipidaemias usually occur In patients with concurrent conditions, e.
Diabetes Antihyperlipideimc with one of the primary hyperlipidaemias PowerPoint Presentation: Anti- hyperlipidemic drugs are mainly classified into 5 types: AtorvastatinFluvastatinLovastatinPravastatinSimvastatin. ColesevelamColestipolCholestyramine Antihypeelipidemic acid: Plasma total cholesterol and LDL-cholesterol fall to attain a maximum effect 1 month after therapy. Mechanism of action of statins: Mechanism of action of statins PowerPoint Presentation: These drugs are effective in lowering plasma cholesterol levels in all types of hyperlipidemias However, patients who are homozygous for familial hypercholesterolemia lack LDL receptors and, therefore, benefit much less from treatment with these drugs.
These drugs are often given in combination with other antihyperlipidemic drugs PowerPoint Presentation: Pravastatin and fluvastatin are almost completely absorbed after oral administration.
Excretion takes place through the bile and feces some urinary elimination also occurs.
Their half-lives range from 1. Because of a circadian rhythm to LDL-receptor synthesis, statins are a little more effective if given in the evening rather than in the morning Claxsification Presentation: Adverse effect of statins Transient, and minor abnormality of liver antihyperlipidemicc tests Myopathy and rhabdomyolysis disintegration or dissolution of muscle and elevation of muscle enzymes creatine hosphokinaseCPK: In patients with renal insufficiency In patients taking drugs such as cyclosporine, itraconazoleerythromycin, gemfibrozilor niacin.
Lipid-lowering agent – Wikipedia
Plasma creatine kinase levels should be determined regularly. Adverse effect of statins: Adverse effect of statins PowerPoint Presentation: Thus, it is important to evaluate INR Contraindications: These drugs are contraindicated during pregnancy and in nursing mothers.
They should not be used in children or teenagers. Pharmacokinetic of Fibric acid derivatives: Contraindication Where hepatic or renal function is severely impaired but gemfibrozil has been used in uraemic and nephrotic patients without aggravating deterioration in kidney function pregnant or lactating women PowerPoint Presentation: Adveres effect of fibric acid derivatives Gastrointestinal effects Lithiasis: Because these drugs increase biliary cholesterol excretion, there is a predisposition to the formation of gallstones.
Fibric acid derivatives may induce a Myopathy and rhabdomyolysis the risk is greater in: Patients with poor renal Function In patients taking a statin. Fibrates enhance the effect of co-administered oral Anticoagulants. In treatment of type IIA and IIB hyperlipidemias along with statins when response to statins is inadequate or they are contraindicated.
Medicinal Chemistry, 2nd Edition by P. Yogeeswari, D. Sriram
Orally given but neither absorbed nor metabolically altered by intestine, totally excreted in feces. At high doses, cholestyramine and colestipol impair the absorption of the fat-soluble vitamins A, D, E, and K.
Colesevelam has fewer gastrointestinal side effects and not Impaired cpassification PowerPoint Presentation: Tetracycline, warfarindigoxinthiazide diuretics, phenobarbitone and thyroid hormones should be taken 1 h-2h before or 4 h-6h after colestyramine to avoid impairment of their absorption Because the drug binds anions Niacin nicotinic acid: Niacin nicotinic acid Mechanism of action: Niacin lowers plasma levels of both cholesterol and triacylglycerol.
Therefore, it is particularly useful in the treatment of familial hyperlipidemias. Niacin is also used to treat other severe hypercholesterolemiasoften in combination with other antihyperlipidemic agents. In addition, it is the most potent antihyperlipidemic agent for raising plasma HDL levels, which is the most common indication for its clinical use.
Niacin nicotinic acid PowerPoint Presentation: Niacin is administered orally. Niacin, its nicotinamide derivative, and other metabolites are excreted in the urine.
Nicotinamide alone does not decrease plasma lipid levels. Cutaneous flush most common side effects accompanied by an uncomfortable feeling of warmth and pruritus. Administration of aspirin prior to taking niacin decreases the flush, which is prostaglandin mediated. Antihyprlipidemic sustained-release formulation of niacin, which is taken once daily at bedtime, reduces bothersome initial adverse effects.
List of Antihyperlipidemic agents – Generics Only –
Nausea and abdominal pain. Hyperuricemia and gout Niacin inhibits tubular secretion of uric acid Impaired glucose tolerance Hepatotoxicity PowerPoint Presentation: Pharmacokinetic of Ezetimibe Metabolized in the small intestine and liver via glucuronide conjugation a Phase II reactionwith subsequent biliary and renal excretion. Both ezetimibe and ezetimibe-glucuronide are slowly eliminated from plasma, with a half-life of approximately 22 hours.
Ezetimibe has no clinically meaningful effect on the plasma concentrations of the fat-soluble vitamins A, D, and E. Patients with moderate to severe hepatic insufficiency should not be treated with ezetimibe.
A formulation of ezetimibe and simvastatin has been shown to lower LDL levels more effectively than the statin alone PowerPoint Presentation: Alpha- tocopherol acetate vitamin E Has no effect on lipid levels but is a powerful antioxidant.
Considerable evidence points to oxidation of LDL as an essential step in the development of atheromaand therefore interest has centred on the role of either endogenous or therapeutic vitamin E in prevention of atheroma. Omega-3 marine triglycerides Maxepa contain the triglyceride precursors of two polyunsaturated fatty acids derived from oily fish. They have no place in treating hypercholesterolaemia. Some patients with moderate to severe hypertriglyceridaemia may respond to oral use, although LDLcholesterol may rise.
Orlistata weight-reducing agent, it is pancreatic lipase inhibitor lowers the Glycaemia of diabetes mellitus to a degree that Accords with the weight loss, and improves Hyperlipidaemia There is a risk of steatorrhoea and alabsorption of Fat-soluble vitamins A, D and E.
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Lipid disorders Disorders of lipid metabolism are manifest by elevation of the plasma concentrations of the various lipid and lipoprotein fractions total and LDL cholesterol, VLDL, triglycerides, chylomicrons and they result in cardiovascular disease and atherosclerosis deposition of fats at walls of arteries, forming plaque. Type of hyperlipidemia Primary hyperlipidemia Secondary hyperlipidemia.
Serum VLDL and chylomicrons are increased. Diabetes Mellitus antihuperlipidemic one of the primary hyperlipidaemias.
Alpha- tocopherol acetate vitamin E Omega-3 marine triglycerides Maxepa Orlistat. These drugs are often given in combination with other antihyperlipidemic drugs. Because of a circadian rhythm to LDL-receptor synthesis, statins are a little more claszification if given in the evening rather than in the morning.
Therapeutic uses Hypertriglyceridemia the most effective in reduction TGs – combined hyperlipidemia type III if statins are contraindicated. Contraindication Where hepatic or renal function is severely impaired but gemfibrozil has been used in uraemic and nephrotic patients without aggravating deterioration in antihypdrlipidemic function pregnant or lactating women.
Colesevelam has fewer gastrointestinal side effects and not Impaired absorptions. Tetracycline, warfarindigoxinthiazide diuretics, phenobarbitone and thyroid hormones should be taken 1 h-2h before or 4 h-6h after colestyramine to avoid impairment of their absorption Because the drug binds anions.
Hyperuricemia and gout Niacin inhibits tubular secretion of uric acid Impaired glucose tolerance Hepatotoxicity. A formulation of ezetimibe and simvastatin has been shown to lower LDL levels more effectively than the statin alone. You do not have the permission to view this presentation. In order to view it, please contact the author of the presentation. Go to Application Have a question?