Antihyperlipidemics

Cholestyramine and colestipol are resins that complex bile salts, preventing their reabsorption from the GI tract — 4 feedback inhibition of 7 alpha hydroxylase — T synthesis of new bile salts —liver cholesterol — T LDL receptors —plasma LDL. 

Bloating, constipation, l absorption of digoxin, thiazides, tetracyclines, warfarin, and vitamin K. 

Lovastatin and the other statins inhibit HMG-CoA reductase, the rate-limiting step in cholesterol synthesis. This induces the following  

They also increase NO and decrease mRNA for endothelin-1 (potent vasoconstrictor). 

Diarrhea, myalgia/myopathy (watch CK), rhabdomyolysis (T with gemfibrozil and nicotinic acid), T LFTs, possible enhanced toxicity with P450 inhibitors. 

Class Name Laboratory Findings Indicated drugs 

Type I Exogenous hyperlipemia (1LPL, i apo CII) Flyperchylomicronemia NONE diet 

Type Ha Familial hypercholesterolemia (1LDL receptors) tUjL Increased LDL colestipol, cholestyramine, lovastatin, nicotinic acid 

Treatment goal is to LDL cholesterol and atheroma plaque formation 

An aberrant serum lipid profile is associated with increased risk of artherosclerosis and cardiac heart disease. 

Lovastatin and the other statins inhibit the rate-limiting step in cholesterol synthesis, HMG-CoA reductase. This lowers liver cholesterol, plasma LDL, and the hepatic synthesis of VLDL and apo B. Statins also cause a small increase in HDL, and atorvastatin lowers triglycerides (TGs). The adverse effects are listed. 

Cholestyramine and colestipol are bile acid sequestrants that enhance cholesterol loss into the feces, thereby stimulating new bile salt synthesis, which lowers liver cholesterol levels and consequently plasma LDL levels. Their adverse effects are also listed. 

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Nicotinyl alcohol (3-pyridinylcarbinol, 3-pyridinemethanol) (27) has use as an antilipemic and peripheral vasodilator. It is available from either the reductions of nicotinic acid esters or preferably, the reduction of the nitrile to the amine followed by dia2otation and nucleophilic displacement. It is frequently adininistered in the form of the tartrate (Eig. 7). Nicotinic acid is frequently used as a salt in conjunction with basic dmgs such as the peripheral vasodilator xanthinol niacinate (28). Nicotinic acid and its derivatives have widespread use as antihyperlipidemic agents and peripheral vasodilators (1). 

Pharmacological management of risk factors through antihypertensive, antihyperlipidemic, and antidiabetic therapy coupled with antiplatelet drugs comprise the... 

Discuss the general actions, uses, adverse reactions, contraindications, precautions, and interactions of antihyperlipidemic drugs. 

Discuss important preadministration and ongoing assessment activities the nurse should perform on the patient taking an antihyperlipidemic drug. 

Discuss ways to promote an optimal response to therapy, how to manage common adverse reactions, and important points to keep in mind when educating patients about the use of an antihyperlipidemic drug. 

While the fibric acid derivatives have antihyperlipidemic effects, their use varies depending on the drug. For example, Clofibrate (Atromid-S) and gemfibrozil (Lopid) are used to treat individuals with very high serum triglyceride levels who present a risk of abdominal pain and pancreatitis and who do not experience a response to diet modifications. Clofibrate is not used for the treatment of other types of hyperlipidemia and is not thought to be effective for prevention of coronary heart disease. Fenofibrate (Tricor) is used as adjunctive treatment for the reduction of LDL, total cholesterol, and triglycerides in patients with hyperlipidemia. 

Because hyperlipidemia is often treated on an outpatient basis, die nurse explains die drug regimen and possible adverse reactions. If printed dietary guidelines are given to die patient, die nurse emphasizes the importance of following these recommendations. Drug dierapy usually is discontinued if the antihyperlipidemic drug is not effective after 3 months of treatment. 

OILE ACID SEQUESTRANTS. Fhtients taking the antihyperlipidemic dragp, particularly the bile acid sequestrants, may experience constipation. The dragp can produce or severely worsen preexisting constipation. The nurse instructs the patient to increase fluid intake, eat foods high in dietary fiber, and exercise daily to help prevent constipation. If the problem persists or becomes... 

HMG-CoA REDUCTASE INHIBITORS AND FlBRIC ACID DERIVATIVES. The antihyperlipidemic drugp, particularly die HMG-CoA reductase inhibitors, have been associated with skeletal muscle effects leading to rhab-domyolysis. Rhabdomyolysis is a very rare condition in which muscle damage results in die release of muscle cell contents into die bloodstream. Rhabdomyolysis may precipitate renal dysfunction or acute renal failure The nurse is alert for unexplained muscle pain, muscle tenderness, or weakness, especially if tiiey are accompanied by malaise or fever. These symptoms should be reported to die primary health care provider because the drug may be discontinued. 

Unit VI covers drag s that affect the cardiovascular system. This unit is divided into five chapters cardiotonics and miscellaneous inotropic drag s, antiar-rhythmic drugs, antianginal and peripheral dilating dragp, antihypertensives, and antihyperlipidemics. 

Table 2.1 shows the major therapy classes in terms of sales and the number of prescriptions dispensed in the United States in 2003. The top three therapy classes are antidepressants, antihyperlipidemics, and antiulcerants. They account for 39% of sales in this list of 17 therapy classes. There are significant changes to the growth of some therapy classes within a single year. This is... 

Microbial natural product chemistiy has generated a number of bioactive natural products. For instance cyclosporine A FK506 and rapamycin are used as immunosuppressants [16]. Other examples of microbial metabolites, having potential biomedical application include antihyperlipidemics, lovastatin and guggulsterone [17, 18]. The crude extracts of Mucor plumbeus exhibited acetylcholinesterase (AChE) enzyme inhibition activity. Our detailed chromatographic work on this crude extract resulted in the isolation of mucoralactone A (11), a novel steroid containing a lactone moeity incorporated in its structure. 

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