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52 Cards in this Set
- Front
- Back
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List the 5 classes of Anti-Hyperlipidemics
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1. HMG-CoA Reductase Ibx (3-hydroxy-3-methyl-glutaryl-CoA reductase or HMGCR/Statins)
2. Bile Acid Sequestrants 3. Cholesterol Absorption Ibx 4. PPAR-alpha Activators aka Fibrates (Peroxisome proliferator-activated receptor alpha) 5. Misc |
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Which 2 statins (HMGCR) are prodrugs?
Name a common anti-depressant that ibx these statins activation by CYP450 |
Lovastatin
Simvastatin ----lova simva are prodrugs Flustacine is drug that ibx their activation |
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What is MOA of Statins?
What does HMG-CoA Red. do? Secondary Effect of Statins? |
Competitively Ibx HMG-CoA Reducatase
-rate-limiting step in production of Mevalonate & cholesterol -Statins also UP-Regulate LDL receptors ---suck LDL-Chol (LDL-C) into cells for breakdown to TG, etc.= inc. in lipid metabolism |
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What are lipoprotein effects of statins on this panel:
LDL-C TG HDL Lp-a |
LDL-C reduced
TG reduced HDL raised Lp-a no appreciable affect |
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Name 3 most POTENT Statins---now more commonly used due to rampant hypercholesteremia and dosage limitations of less potent ones
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Pitava-
Rosuva- Atorva- statins most potent |
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Least potent statins (3)
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Simva-
Lova- Fluva- statins |
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Regarding Dosage, when does majority of LDL-C lowering occur on statins
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At lower doses, ie, diminishing returns on incremental dosage.
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Which organs are most considered for AEs on Statins?
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Liver and Muscle
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With Lova- and Simva-, statins, which drugs might inhibit them, be specific with enzyme
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Drugs that use up/Ibx CYP3A4/2C9
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What are Liver AEs of statins?
-Liver Fxn levels of what = cease drug? |
Asymptomatic AST/ALT elevations
-if 3x stop drug |
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What myopathy is worst cause AE of statins
--what enzyme levels are checked for ceasation of drug/ HALLMARK sign of problem? |
Rhabomyolysis
if CK 5-10x higher, quite drug --Rhabdo products try to squeeze through Kidneys = CocaCola Urine |
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Contraindications for Statins?
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Preggers (category x)
-of course, also in Acute/Chronic Liver and Renal Failure |
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Name the 3 Bile Acid Sequesterants.
(BAcSeqs) |
Cholestyramine
Colestipol colesvelam |
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Which BAcSeq is a powder form
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Cholestyramine is powder
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What is MOA for BAcSeq drugs in Hypercholesteremia?
Result of their MOA on Lipids |
Drugs are NON-absorbable Anion-Exhange Resins
--Will bind bile acids in lumen -Results in UP-reg of LDL-C Receptors & Cholesterol 7-alpha Hydroxylase (rate limit enz in syn of bile acid from Chol.) |
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What are BAcSeq effects on panel:
LDL-C TG HDL-C Lp-a |
LDL-C -- reduced--main effect
TG -- zero change/slight increase HDL-C -- mostly no effect/little positive Lp-a --- no effect --b/c slight inc in TG, sort of contraindication for those whose TG is already high |
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WHat are AEs of BAcSeqs in:
GI: Liver: Pancreas: Blood: |
GI--Constipation -- bloating, abdominal distention...obstruction possible
Liver: enzyme elevation Pancreas: pancreatitis Blood: Fat Soluble Vitamin Abs/depletion Vit ADEK =Bleeding/Hypoprothrombinemia |
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What drug must be watched if on BAcSeq
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Warfarin
& ALLLLL EXTENSIVE drug-drug interactions (just absorbs other drugs) -take BAcSeqs 1-2hours before OR 2-4hrs after other drugs/vitamins |
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What is biochem name for Niacin? Vitamin?
Name important dosing fact for niacin |
Nicotinic Acid -- Vitamin B3
---NOT Nicotinamide --Extended Release Tabs for reduction of cutaneous flushing. |
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MOA for Niacin?
Positive effects of MOA? |
Reduction in cellular hepatic synthesis of TG, VLDL-C and LDL-C
Effects: -Increased LDL-C receptor activity -Decreased HDL-C catabolism |
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What is primary affect for Niacin/what its best for? Rest of effects in panel:
TG T-C LDL-C HDL-C |
Niacin best for Inc. HDL--better than Statins
-TG: reduced T-C: reduced LDL-C: reduced HDL-C: increased ---GOOD drug to add to statin therapy for HDL boost |
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What are AEs of Nicotinic Acid/Vit B3
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-Cutaneous Flushing--(PGI2 generation---thus ASA can prophylax this/start low dose)
-GI Distress -Liver enzyme elevations -Elevation of Serum GLc AND Serum Uric Acid -Myopathy |
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What 2 co-morbities to hypocholesteremia may req watching niacin use?
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Diabetes--due to Glc inc in serum
Gout--due to Uric Acid |
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Contraindications for Niacin use?
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Chronic Liver/Gallbladder Dx
Severe Gout/Diabetes Peptic Ulcer Dx -Bleeding Dx/Thrombocytopenia/Warfarin Therapy (ie Pts with Stints or MI) -PReggers |
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The Following Contraindications are for what drugs--give class and names?
-Dysbetalipoproteinemia -Ileus -Dysphagia -Adv. Renal Dx--Cl- balance -Preggers -Hypertriglyceridemia |
BAcSeqs: Cholestyramine, Colestipol, Colesevelam
For preggers--colesevelam is bad |
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What doe Fibrates do?
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PPAR-alpha-Activators
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What Lipid drug has no significant Drug-Drug interactions
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Niacin/Nicotinic Acid/Vit B3
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Name the 2 fibrates
which is Prodrug? |
Fibrates/PPAR-alpha Acts
-Gemfibrozil -Fenofibrate |
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Which Fibrate is more effective?
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Fenofibrate
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What is MOA for Fibrates?
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via PPAR-alpha Activator: affect transcription of genes involved in lipoprotein metab
--Note: Fibrates involved at Transcriptional/Genetic level |
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By altering Lipoprotein metabolism/ breaking down VLDL-C/IDL-C with lipase, what is greatest effect of Fibrates
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Decreasing TGs on panel
--greatest bang for buck with TG or Chylomicron issues --Also work on Lp-a (lipoprotein like-a) |
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Given that Fibrates beat statins on TG, what is effect on this panel:
VLDL-C/IDL-C: Hepatic FFA extraction: Hepatic Acetyl CoA Carboxylase: HDL-C |
LDL-C/IDL-C: Inc Catab
Hepatic FFA extc: Decreased Hep A-CoA Carbase: Ibxs it (TG production step) HDL-C: Increased (via VLDL-C clearance |
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Basically for Fibrates, it?
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Decreases TGs the best
--Has decent decreases across panel where you want them + inc in HDL ---Can potentially inc LDL-C in some --- |
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AEs of Fibrates
Liver: Muscle: Gall: |
Liver: AST/ALT elevations
Muscle: myopathy Gall: predisp to gallstones |
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Drug drug interactions for Fibrates>
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Increased effects of Anti-Hyperglycemic drugs
Watch Diabetic's meds |
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Contraindications for Fibrates?
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Severe Renal/Hepatic
Biliary Cirrhosis/Cholelithiasis Preggers |
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What sort of drug is Ezetimibe?
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Cholesterol Absorption Ibx
-Ezetimibe |
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WHat is MOA for Ezetimibe for Cholesterol Absorption?
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Selectively ibx---at brush border--the small intestines abs of Chol and Phytosterols
--reduces delivery of Chol to Liver |
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What is primary effect of Ezetimibe? Compared to Statin?
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Total Chol reduction of 13% max-=not huge
--NO sig change in HDL-C |
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AEs of Ezetimibe?
general? liver? muscle? |
Diarrhea, Abd. Pain, Fatique, Back pain
-Increased AST/ALT & Myopathy (usually due to CO-Rx of Stain/Fibrate) |
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Contraindications for Ezetimibe
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Severe Hepatic Dx
Preggers |
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What other Misc/OTC Lipid drug is there. Be specific with all contents
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Fish Oil/ Omega-3 FA: EPA, DHA and ALA
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Which 2 classes have Greatest GI affects/ Why
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Cholesterol Ibx (ezetimibe) and BAcSeqs
--they are local inhibitors |
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What Vitamin is also often included in FishOil/Om3/EPA/DHA/ALA
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Vitamin E
Note: FDA approved product is Lovaza--but expensive, most use OTC |
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What sort of FA is Omega-3
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Unsaturated Fats --> Polyunsaturated Fats (omega 3 and 6 {sunflw/corn oils})
- fyi--monoUnsaturates are: Omega 9s like olive Animal fats/ butter/ lard are Saturated |
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OF the fats, which tend to be better
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The ones that are NOT Saturated
ie, Unsaturated: includes Mono- and Poly- Unsats |
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MOA for Fish Oils
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through IipoPR lipase the manufacturing of DECREASES TGs. Causes:
Total Chol decrease VLDL dec HDL inc Anti-Plt affects |
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AEs of Fish Oil
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===MILD---
GI --upset stomach, burping, reflux -Bleeding -- ASA/Warf/LMWH-UFH/etc Monitor Liver/Renal |
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With high enough dose, what is BEST effect for Fish Oil
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Red TG and Red VLDL
--but remember, Statins best, Niacin best of HDL |
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What is CETP?
Inbx or Act it |
Cholesterol EsterTransfer Protein
--CETP breaksdown HDL Block it and HDLs stay around = good. Drug is anacatrapib--don't think have to know --consider Niacin like Drug--ie raises HDL |
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What is prolly best used Lipid drug for preggers?
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Bile Acid Seqs, because they aren't absorbed.
Though this may be their only use nowadays |
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With elevated TC, what must be consdered
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when NO Tx is necessary b/c high number is due to high HDL
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