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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
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.
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.
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
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
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most commonly tested facts,
treatments & management, and
much more!

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

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Pharmacology: Anti hyperlipidemic drugs flashcards

  • 2. 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 
  • 3. 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 
  • 4. 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 
  • 5. 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 
  • 6. 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!!) 
  • 7. 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) 
  • 8. 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% 
  • 9. 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 
  • 10. 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 
  • 11. INTESTINAL STEROL ABSORPTION INHIBITOR  Adverse Hypersensitivity reactions  Severe hepatic disease prolongs drug life   Uses  Combined with statins for hyperlipidemias
  • 12. RELATED PRODUCTS 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. 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. Get the eBook: HERE! Our site: Exam Masters Tutoring Service
  • 13. 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!
  • 14. RELATED PRODUCTS 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! View a sample Newsletter: HERE! Subscribe to this awesome Newsletter: HERE!