Pharm (5b) Chol

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Created by:

dvirwin  on January 29, 2012

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Pharm (5b) Chol

***ATORVASTATIN:
• Class-
o HMG CoA reductase inhibitor (statins)
o GOLD STANDARD THERAPY FOR LIPIDS
• Action-
o CARDIOPROTECTIVE
o By blocking cholesterol synthesis, statins reduce LDL by increasing LDL receptor synthesis thus removing LDL from the blood
o Lowers secretion of VLDL
o Reduce triglycerides
• Indication-
o High cholesterol
o THE BEST
• Side-effect-
o ***HEPATOTOXICITY: (blood test needed and is supposed to be stable)
o ***MYOPATHY: (DOSE DEPENDENT. HIGHER OR MORE POWERFUL THE MORE LIKELY)
o IF MYOPATHY (MUSCLE WEAKNESS/CREATINE KINASE 10XS NORMAL) HAPPENS, STOP DRUG IMMEDIATELY
• Contra-
o PREGNANCY CATEGORY X
o ABSOLUTE CONTRAINDICATION ACTIVE LIVER DISEASE
• Pharm-
o Orally active, extensive first pass effect
• Misc-
o BLOOD TESTING NEEDED
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Definitions

***ATORVASTATIN:• Class-
o HMG CoA reductase inhibitor (statins)
o GOLD STANDARD THERAPY FOR LIPIDS
• Action-
o CARDIOPROTECTIVE
o By blocking cholesterol synthesis, statins reduce LDL by increasing LDL receptor synthesis thus removing LDL from the blood
o Lowers secretion of VLDL
o Reduce triglycerides
• Indication-
o High cholesterol
o THE BEST
• Side-effect-
o ***HEPATOTOXICITY: (blood test needed and is supposed to be stable)
o ***MYOPATHY: (DOSE DEPENDENT. HIGHER OR MORE POWERFUL THE MORE LIKELY)
o IF MYOPATHY (MUSCLE WEAKNESS/CREATINE KINASE 10XS NORMAL) HAPPENS, STOP DRUG IMMEDIATELY
• Contra-
o PREGNANCY CATEGORY X
o ABSOLUTE CONTRAINDICATION ACTIVE LIVER DISEASE
• Pharm-
o Orally active, extensive first pass effect
• Misc-
o BLOOD TESTING NEEDED
***SIMVASTATIN:• Class-
o HMG CoA reductase inhibitor (statins)
o GOLD STANDARD THERAPY FOR LIPIDS
• Action-
o CARDIOPROTECTIVE
o By blocking cholesterol synthesis, statins reduce LDL by increasing LDL receptor synthesis thus removing LDL from the blood
o Lowers secretion of VLDL
o Reduce triglycerides
• Indication-
o High cholesterol
• Side-effect-
o ***HEPATOTOXICITY: (blood test needed and is supposed to be stable)
o ***MYOPATHY: (DOSE DEPENDENT. HIGHER OR MORE POWERFUL THE MORE LIKELY)
o IF MYOPATHY (MUSCLE WEAKNESS/CREATINE KINASE 10XS NORMAL) HAPPENS, STOP DRUG IMMEDIATELY
• Contra-
o PREGNANCY CATEGORY X
o ABSOLUTE CONTRAINDICATION ACTIVE LIVER DISEASE
o GRAPEFRUIT JUICE
• Pharm-
o Orally active, extensive first pass effect
• Misc-
o Prodrug
o BLOOD TESTING NEEDED
***Rosuvastatin:• Class-
o HMG CoA reductase inhibitor (statins)
o GOLD STANDARD THERAPY FOR LIPIDS
• Action-
o CARDIOPROTECTIVE
o By blocking cholesterol synthesis, statins reduce LDL by increasing LDL receptor synthesis thus removing LDL from the blood
o Lowers secretion of VLDL
o Reduce triglycerides
• Indication-
o High cholesterol
• Side-effect-
o ***HEPATOTOXICITY: (blood test needed and is supposed to be stable)
o ***MYOPATHY: (DOSE DEPENDENT. HIGHER OR MORE POWERFUL THE MORE LIKELY)
o IF MYOPATHY (MUSCLE WEAKNESS/CREATINE KINASE 10XS NORMAL) HAPPENS, STOP DRUG IMMEDIATELY
• Contra-
o PREGNANCY CATEGORY X
o ABSOLUTE CONTRAINDICATION ACTIVE LIVER DISEASE
• Pharm-
o Orally active, extensive first pass effect
• Misc-
o BLOOD TESTING NEEDED
***Pitavastatin:• Class-
o HMG CoA reductase inhibitor (statins)
o GOLD STANDARD THERAPY FOR LIPIDS
• Action-
o CARDIOPROTECTIVE
o By blocking cholesterol synthesis, statins reduce LDL by increasing LDL receptor synthesis thus removing LDL from the blood
o Lowers secretion of VLDL
o Reduce triglycerides
• Indication-
o High cholesterol
• Side-effect-
o ***HEPATOTOXICITY: (blood test needed and is supposed to be stable)
o ***MYOPATHY: (DOSE DEPENDENT. HIGHER OR MORE POWERFUL THE MORE LIKELY)
o IF MYOPATHY (MUSCLE WEAKNESS/CREATINE KINASE 10XS NORMAL) HAPPENS, STOP DRUG IMMEDIATELY
• Contra-
o PREGNANCY CATEGORY X
o ABSOLUTE CONTRAINDICATION ACTIVE LIVER DISEASE
• Pharm-
o Orally active, extensive first pass effect
• Misc-
o BLOOD TESTING NEEDED
Fluvastatin:• Class-
o HMG CoA reductase inhibitor (statins)
o GOLD STANDARD THERAPY FOR LIPIDS
• Action-
o By blocking cholesterol synthesis, statins reduce LDL by increasing LDL receptor synthesis thus removing LDL from the blood
o Lowers secretion of VLDL
o Reduce triglycerides
• Indication-
o High cholesterol
• Side-effect-
o ***HEPATOTOXICITY: (blood test needed and is supposed to be stable)
o ***MYOPATHY: (DOSE DEPENDENT. HIGHER OR MORE POWERFUL THE MORE LIKELY)
o IF MYOPATHY (MUSCLE WEAKNESS/CREATINE KINASE 10XS NORMAL) HAPPENS, STOP DRUG IMMEDIATELY
• Contra-
o PREGNANCY CATEGORY X
o ABSOLUTE CONTRAINDICATION ACTIVE LIVER DISEASE
• Pharm-
o Orally active, extensive first pass effect
• Misc-
o BLOOD TESTING NEEDED
Lovastatin:• Class-
o HMG CoA reductase inhibitor (statins)
o GOLD STANDARD THERAPY FOR LIPIDS
• Action-
o By blocking cholesterol synthesis, statins reduce LDL by increasing LDL receptor synthesis thus removing LDL from the blood
o Lowers secretion of VLDL
o Reduce triglycerides
• Indication-
o High cholesterol
• Side-effect-
o ***HEPATOTOXICITY: (blood test needed and is supposed to be stable)
o ***MYOPATHY: (DOSE DEPENDENT. HIGHER OR MORE POWERFUL THE MORE LIKELY)
o IF MYOPATHY (MUSCLE WEAKNESS/CREATINE KINASE 10XS NORMAL) HAPPENS, STOP DRUG IMMEDIATELY
• Contra-
o PREGNANCY CATEGORY X
o ABSOLUTE CONTRAINDICATION ACTIVE LIVER DISEASE
o GRAPEFRUIT JUICE
• Pharm-
o Orally active, extensive first pass effect
• Misc-
o Prodrug
o BLOOD TESTING NEEDED
Pravastatin:• Class-
o HMG CoA reductase inhibitor (statins)
o GOLD STANDARD THERAPY FOR LIPIDS
• Action-
o By blocking cholesterol synthesis, statins reduce LDL by increasing LDL receptor synthesis thus removing LDL from the blood
o Lowers secretion of VLDL
o Reduce triglycerides
• Indication-
o High cholesterol
• Side-effect-
o ***HEPATOTOXICITY: (blood test needed and is supposed to be stable)
o ***MYOPATHY: (DOSE DEPENDENT. HIGHER OR MORE POWERFUL THE MORE LIKELY)
o IF MYOPATHY (MUSCLE WEAKNESS/CREATINE KINASE 10XS NORMAL) HAPPENS, STOP DRUG IMMEDIATELY
• Contra-
o PREGNANCY CATEGORY X
o ABSOLUTE CONTRAINDICATION ACTIVE LIVER DISEASE
• Pharm-
o Orally active, extensive first pass effect
• Misc-
o BLOOD TESTING NEEDED
Cholestyramine:• Class-
o Bile acid sequesterant
• Action-
o Positively charged resins that bind negatively charged bile acids thus decreasing hepatic cholesterol content and increasing LDL clearance from blood
• Indication:
o High cholesterol
o Preferred agent
• Side-effect-
o HYPERTRIGLYCERIDEMIA (triglyceride synthesis is stimulated)
o Bloating, dyspepsia, constipation & flatulence
o May interfere with fat soluble vitamin absorption (use vitamin supplement)
• Contra-
O DO NOT USE IN PTS WITH ELEVATED TRIGLYCERIDES
o Binding drugs (administer 1 hr before or 2-2 hrs after using sequesterants)
• Misc-
o NOT FOR USE IF TRYGLYCERIDES >400
Colestipol:• Class-
o Bile acid sequesterant
• Action-
o Positively charged resins that bind negatively charged bile acids thus decreasing hepatic cholesterol content and increasing LDL clearance from blood
• Indication:
o High cholesterol
o Preferred agent
• Side-effect-
o HYPERTRIGLYCERIDEMIA (triglyceride synthesis is stimulated)
o Bloating, dyspepsia, constipation & flatulence
o May interfere with fat soluble vitamin absorption (use vitamin supplement)
• Contra-
O DO NOT USE IN PTS WITH ELEVATED TRIGLYCERIDES
o Binding drugs (administer 1 hr before or 2-2 hrs after using sequesterants)
• Misc-
o NOT FOR USE IF TRYGLYCERIDES >400
Colesevelam:• Class-
o Bile acid sequesterant
• Action-
o Positively charged resins that bind negatively charged bile acids thus decreasing hepatic cholesterol content and increasing LDL clearance from blood
• Indication:
o High cholesterol
o Preferred agent
• Side-effect-
o HYPERTRIGLYCERIDEMIA (triglyceride synthesis is stimulated)
o Bloating, dyspepsia, constipation & flatulence
o May interfere with fat soluble vitamin absorption (use vitamin supplement)
• Contra-
O DO NOT USE IN PTS WITH ELEVATED TRIGLYCERIDES
o Binding drugs (administer 1 hr before or 2-2 hrs after using sequesterants)
• Misc-
o NOT FOR USE IF TRYGLYCERIDES >400
Ezetimibe:• Class-
o Cholesterol absorption inhibitors
• Action-
o Inhibits intestinal absorption of cholesterol and related phytosterols blocking intestinal transporters
o Not very effective
o Not cardioprotective
• Indication-
o High cholesterol
• Contra-
o Interacts with HMG CoA Reductase inhibitors
o Do not use in Pts with active liver disease or elevated serum transaminases
• Pharm-
o Does not affect fat soluble vitamin absorption
o May split pill to save $$$
Ezetimibe + Simvastatin:• Class-
o Cholesterol absorption inhibitors
• Action-
o Inhibits intestinal absorption of cholesterol and related phytosterols blocking intestinal transporters
o Super additive in lowering cholesterol but does not reduce morbidity or mortality
• Side-effect-
o Risk of myopathy may be elevated
• Indication-
o High cholesterol
• Pharm-
o Ezetimibe at fixed dose so tablets may NOT be split
o Ezetimibe has the mech, but simvastatin makes it work well
Vitamin B3, Niacin, Niaspan:• Action-
o INHIBITS TRIGLYCERIDE SYNTHESIS
o Reduces VLDL synthesis
o Reduces LDL levels
o Reduces HDL clearance
• Side-effect-
o FLUSHING AND PRURITUS (reduced by aspirin and may be more frequent when not compliant)
o Dyspepsia
o Hepatotoxicity
o Hyperglycemia in diabetics
o Hyperuricemia
• Contra-
o ***ABSOLUTE CONTRAINDICATION: LIVER DISEASE & GOUT
o Relative contraindication: diabetes, hyperuricemia, PUD
Gemfibrozil:• Class-
o Fibric acid
• Action-
o Unclear mechanism (activates PPAR-alpha to suppress genes associated with lipid metabolism)
o Reduces triglyceride-rich lipoproteins
o Increases HDLs
• Indication:
o Use in combo with statins to improve outcome
• Side-effect-
o Bone marrow suppression
o Myositis flu-like syndrome (myopathy)
• Contra-
o Severe renal disease
o Severe hepatic disease
• Misc-
o Does not improve outcome in diabetes
Fish oils: • Class-
o CAM
• Action-
o Omega-3 fatty acids lower triglycerides (MOA similar to fibrates)
• Side-effect-
o Excess bleeding
Red yeast rice: • Class-
o CAM
• Action-
o Contains monacolin K, which inhibits HMG-CoA reductase
• Indication-
o May be a supplement for Pts who can't take statins
• Side-effect-
o Adverse effects similar to statins
• Misc-
o No blood checks needed like statins
O PREGNANCY ISSUE

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