ANTI-HYPERLIPIDEMIC DRUGS

HMG-COA INHIBITORS

Lovastatin; Atarvostatin Analogs of HMG (3-hydroxy-3 methylglutaryl-

CoA) HMG-CoA reductase catalyzes synthesis of

mevalonic acid from HMG-CoA and is the rate limiting step in cholesterol biosynthesis

Leads to up-regulation of LDL receptors in liver

ACTIONS Decrease LDL by 20 – 55% Decrease TG by 10 – 35% Slight increase in HDL

HMG-COA INHIBITORS

Adverse Hepatotoxicity (check ALT and AST, if >3x normal...stop

drug) Myopathy (w/ rhabodmyolysis) and may cause

myoglobinuria which may lead to urine obstruction (measure CPK levels) Increased chances when mixed with fibric acid

derivatives (gemfibrizol), niacin, or P450 3A4 inhibitors CATEGORY X in pregnancy

Therapeutic Uses Great for all hyperlipidemias involving increased levels

of LDL or cholesterol Atherosclerosis; stroke prevention Primary prevention of CAD

BILE ACID RESIN

Cholestyramine Anion-exchange resin – binds bile acids in

intestinal lumen preventing enterohepatic circulation (this increases excretion of bile which is made from cholesterol) this causes an up-regulation of hepatic LDL receptors and increased production of cholesterol

Action: decreases LDL by 10 – 35% Not absorbed at all

BILE ACID RESIN

Adverse Constipation, flatulence, dyspepsia Hypertriglyceridemia Hyperchloremic acidosis (since they exchange

Cl) Bind many things (drugs, vitamins, toxins,

anything fat soluble) which limits their absorption

Prexisting coagulopathy is a contraindication since they prevent absorption of vit K

Uses Hyperlipidemias involving ISOLATED

INCREASES OF LDL Diarrhea from excess fecal bile resins

VLDL SECRETION INHIBITORS

NIACIN (vit B3) MoA: inhibition of VLDL production by

hepatocyte decreases TG synthesis in liver; inhibition of Hormone sensitive lipase in adipose; stimulation of LPL which causes hydrolysis of VLDL

Actions Decreases LDL by 15-25% Decreases VLDL by 40% Decreases TG by 30 – 50% Increases HDL by 15-30% (niacin is MOST

EFFECTIVE in increasing HDL levels!!)

VLDL SECRETION INHIBITORS Adverse

Cutaneous flush (prevented with NSAID) Stimulates histamine release pruritis, rash, nausea, etc Decreased glucose tolerance (contra in DM pts) Hyperuricemia (inhibits tubular secretion of uric

acid) Lowers fibrinogen (good for AS; bad for coag

disorders) Hepatotoxicity (check AST, ALT levels) Rhabdomyolysis (especially when given with

Statins) Uses

Hyperlipidemias with very high VLDL and LDL Pts with very low HDL (despite risk factors you should

give niacin)

FIBRIC ACID DERIVATIVES

Gemfibrozil MoA: activation of nuclear transcription

receptor to increase LPL synthesis (removes TGs from lipoproteins); enhanced removal of VLDL from plasma

Actions Decreases TG by 30-60% Decreases VLDL by 30% Increases HDL by 5 – 10%

FIBRIC ACID DERIVATIVES

Adverse Myopathy (rhabdomyolysis) when

combined with statins Cholesterol levels may actually increase Cholethiasis due to increased biliary

excretion of cholesterol Therapeutic Uses

DOC fro type III lipoproteinemia (familial dysbetalipoproteinemia)

Hypertriglyceridemias

INTESTINAL STEROL ABSORPTION INHIBITOR

Ezetimibe Localizes at the brush border, selectively

inhibits intestinal absorption of cholesterol and related sterols (only blocks exogenous sterol intake)

Actions Decreases LDL by 15-20% Decreases TG by 5-8% THIS DRUG IS WEAK ALONE

INTESTINAL STEROL ABSORPTION INHIBITOR

Adverse Hypersensitivity reactions Severe hepatic disease prolongs drug life

Uses Combined with statins for hyperlipidemias

RELATED PRODUCTS

HIGHSCORE: Must Know Pharmacology Description: This is a book of 400+ flashcards covering 20 highly tested, and high-yield topics in pharmacology. It is designed so that you can use it anywhere on any device or print it out and use as flashcards.

If you enjoyed this presentation, please take a look at the rest of our products. Our website has many more FREE excellent presentations and tons of other FREE information.

Get the eBook: HERE!

Our site: Exam Masters Tutoring Service

RELATED PRODUCTS

HIGHSCORE: Comparisons of High Yield Topics for the Medical Boards Description: This book contains over 100 comparisons of some of the most highly tested diseases and topics on the USMLE Step 2 CK. The questions on the exam are much more vague than what you see in the practice question banks and it is very difficult to differentiate between two diseases with similar symptoms. So this book is designed to help students improve their score by targeting these types of difficult questions.

Get the Free Sample: HERE!

Get the whole eBook: HERE!

RELATED PRODUCTS

View a sample Newsletter: HERE!Subscribe to this awesome Newsletter: HERE!

USMLE STEP 2 CK TIDBITS & TIPS MONTHLY SUBSCRIPTION

Join hundreds of other students preparing for the USMLE Step 2 CK on our USMLE Step 2 CK Tidbits & Tips newsletter! It is an amazing newsletter with tons of great info. The monthly subscription entails a weekly newsletter with info such as high yield disease comparisons, most commonly tested facts, treatments & management, and much more!