Term
Lovastatin
and other "statin"s |
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Definition
CH 35 Agents Used in Dyslipidemia
Competitive inhibitors of HMG-CoA reductase (1st committed step in sterol synthesis)
↑ LDL receptors = ↑ LDL catabolism and liver’s extraction of LDL precursors (VLDL) from the blood = ↓ plasma LDL
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Myositis, rhabdomyolysis
Hepatic toxicity (malaise,
anorexia, decreases in LDL)due to ↑ of aminotransferase activity
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Atherosclerosis vascular disease, acute coronary syndromes
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Term
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Definition
CH 35 Agents Used in Dyslipidemia
Inhibits VLDL secretion, in turn ↓ LDL production. ↑ VLDL clearance via the LDL pathway reduces triglycerides.
↓ HDL catabolism (= ↑HDL).
↓ lipoprotein(a)
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Gastric irritation, cutaneous flushing, low incidence of hepatic toxicity, may ↓ glucose tolerance
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Low HDL, elevated VLDL, LDL, Lp(a)
Rx: hypercholesterolemia
(normalizes LDL), severe
mixed lipemia
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Term
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Definition
CH 35 Agents Used in Dyslipidemia
Fibrates
Agonist for peroxisome proliferator-activated receptor-alpha (PPAR-α) = ↑ transcription of lipoprotein lipase (LPL)
↓VLDL secretion, , ↑HDL
↑ oxidation of fatty acids
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Myopathy, hepatic dysfunction
Gallstones due to ↑ in cholesterol content of bile
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Hypertriglyceridemia, low HDL
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Term
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Definition
CH 35 Agents Used in Dyslipidemia
Fibrates
Agonist for peroxisome proliferator-activated receptor-alpha (PPAR-α) = ↑ transcription of lipoprotein lipase (LPL)
↓VLDL secretion, , ↑HDL
↑ oxidation of fatty acids
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Myopathy, hepatic dysfunction
Gallstones due to ↑ in cholesterol content of bile
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Hypertriglyceridemia, low HDL
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Term
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Definition
CH 35 Agents Used in Dyslipidemia
Binds to bile acids in the gut preventing reabsorption. ↑ Bile acid excretion => ↑ cholesterol conversion to bile acids.
Upregulates LDL receptors. ↑LDL & IDL uptake from plasma.
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Constipation/bloating, steatorrhea,
malabsorption (vitamin K, folic
acid, charged drugs)
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Elevated LDL, digitalis toxicity, pruritis
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Term
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Definition
CH 35 Agents Used in Dyslipidemia
Binds to bile acids in the gut preventing reabsorption. ↑ Bile acid excretion => ↑ cholesterol conversion to bile acids.
Upregulates LDL receptors. ↑LDL & IDL uptake from plasma.
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Constipation/bloating, steatorrhea,
malabsorption (vitamin K, folic
acid, charged drugs)
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Elevated LDL, digitalis toxicity, pruritis
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Term
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Definition
CH 35 Agents Used in Dyslipidemia
Selective inhibitor of intestinal absorption of cholesterol and phytosterols. Blocks sterol transporter NPC1L1 in intestine brush border inhibiting reabsorption of cholesterol excreted in bile
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Low incidence of hepatic dysfunction, myositis
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Elevated LDL, phytosterolemia
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Term
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Definition
CH 35 Agents Used in Dyslipidemia
Dietary Aids
Inhibits cholesterol (re)absorption
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Malabsorption of fat-soluble
vitamins
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Rx: ↑ LDL, ↑ cholesterol
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Term
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Definition
CH 35 Agents Used in Dyslipidemia
Dietary Aids
inhibits gastric and pancreatic lipases => triglycerides are not hydrolyzed into absorbable free FAs, and are excreted undigested
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Malabsorption of fat-soluble
vitamins, steatorrhea, flatulence
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Rx: weight loss
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Term
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Definition
CH 35 Agents Used in Dyslipidemia
Dietary Aids
Indigestible fat substitute in food
8 FA chains attached to sucrose
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Malabsorption of fat-soluble
vitamins, diarrhea
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Lower or eliminate fat content of high-fat foods
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