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32 Cards in this Set
- Front
- Back
Niacin: effects?
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lower VLDL and LDL conc. in blood
lowered triglycerides and cholesterol lowers circulating fibrinogen increases t-PA release decreases Lp(a) |
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Niacin: Pharmocokinetics?
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good oral availibility
t-1/2= 1 hr |
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Niacin: mechanism of action?
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inhibits lipolysis in adipose tissue
causes deficiency of free fatty acids needed to make triglycerides in liver, that are in turn needed to make VLDL decreased secretion of VLDL causes decreased LDL and increased HDL |
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Niacin: adverse effects?
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flushing
prurtisis (itching) vomiting, nausea, peptic ulcers |
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Niacin: therapeutic uses?
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all types of hyperlipidemia, except Type I
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Fibric Acids: names of drugs?
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Gemfibrozil
Fenofibrate |
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Fibric Acids: effects?
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lower VLDL conc. in blood
lowered triglycerides and cholesterol |
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Fibric Acids: pharmacokinetics?
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oral administration
t-1/2= 1.5 hrs 70% eliminated by kidneys |
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Fibric Acids: mechanism of action?
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ligand for a nuclear transcription regulator
increased clearance of VLDL by LPL decreases lipolysis in adipose tissue Only modest effects on LDL |
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Fibric Acids: adverse effects
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mild GI effects
increased risk of gallstones potentiates warfarin(anticoagulant) myositis contraindicated in pts. w/ impaired hepatic or renal function and in pregnant or nursing women |
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Fibric acids: therapeutic uses?
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reduces cholesterol and triglycerides
reduces myocardial infarctions |
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Bile acid binding resins: names of drugs?
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Cholestipol
Cholestyramine Colesevelam |
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Bile acid binding resins: effects?
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lowers LDL conc. in blood
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Bile acid binding resins: pharmacokinetics
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not absorbed from GI tract
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Bile acid binding resins: mechanism of action?
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bind cholesterol in bile in intestine
conversion of cholesterol to bile acids is increased LDL receptors upregulated more LDL taken up by liver |
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Bile acid binding resins: adverse effects?
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constipation
nausea Absorption of vitamins or drugs may be impaired |
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Bile acid binding resins: therapeutic uses?
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Type II hyperlipedemia, except homozygous LDL receptor defect
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Ezetimibe (Inhibitor of Intestinal sterol absorption): effects
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lowers LDL levels in blood
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Ezetimibe: Pharmacokinetics
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absorbed in the intestine and conjugated to glucuronide
t-1/2= 22 hrs peak levels at 12 hrs 80% excreted in feces |
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Ezetimibe: mechanism of action
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Selective inhibitor of intestinal absorption of cholesterol
inhibits reabsorption of bile cholesterol |
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Ezetimibe: adverse effects?
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not metabolized by liver
some impaired liver function |
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Inhibitors of HMG-CoA reductase: names of drugs?
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Lovastatin
Simvastatin Atorvastatin Pravastatin Fluvastatin Rosuvastatin |
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Inhibitors of HMG-CoA reductase: effects
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lower plasma LDL levels
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Inhibitors of HMG-CoA reductase: pharmacokinetics?
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absorption in gut varies
high first pass effect, most of drug sequestered in liver most of absorbed drug excretedin bile |
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Inhibitors of HMG-CoA reductase: mechanism of action?
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hydrolyzed in gut
inhibitor blocks first committed step of cholesterol synthesis LDL receptor upregulation in liver decrease in plasma LDL |
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Inhibitors of HMG-CoA reductase: adverse effects?
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liver toxicity (monitor levels of aminotransferase)
Myopathies (monitor creatine kinase) |
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Inhibitors of HMG-Coa reductase: therapeutic uses?
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Type II hyperlipidemia, except homozygous LDL receptor defect
not used in pregnant or nursing women |
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THIAZIDE DIURETICS
Chlorothiazide Hydrochlorothiazide |
USE
Control BP in Stage 1 HT pts. and Stage 2 HT pts. Used in combo to control fluid retention and edema caused by other anti-HT drugs Increase plasma renin MECHANISM Increase sodium and H20 excretion by inhibiting reabsorption of Na and Cl in nephron Decrease plasma vol. and CO; this can activate cardiopulmonary reflexes increasing resistance, HR, and plasma renin levels, however w/ continued therapy the reflex subsides Decrease systemic vascular resistance ADVERSE EFX Muscle weakness Fatigue Potassium loss: Cardiac arrythmia and muscle cramp Hyperglycemia Increase VLDL and LDL Impotence |
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POTASSIUM SPARING DIURETICS
Spironolactone Triamterene Amiloride |
Use
Combined w/ Thiazide and Loop diuretics to maintain normal potassium levels in plasma |
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Loop Diuretics
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Use
Combined w/ hypertensives to control edema formation and fluid retention Used in renal insufficiency pts. |
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Lipid Soluble B-blockers
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MECHANISM
Non-selective B-blocker ADVERSE EFX Cross the BBB/CSF Confusion Memory Loss Vivid dreams Inability to concentrate |
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CA+2 CHANNEL BLOCKERS
Nifedipine Verapamil Diltiazem |
USE
used alone in Stages 1,2,& 3 HT Combined w/ thiazide diuretic or an ACE inhibitor for all stages of HT MECHANISM Block L-type Ca+2 channels in SA & AV nodes to decrease cardiac automaticity, AV conduction velocity and cardiac contractility Block L-type Ca+2 channels in vascular SM & myocardium to cause vasodilation and deceased contractility |