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Pharmacology Test 3 > HLD > Flashcards

HLD Flashcards

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1
Q

Hyperlipidemia

A
  • HDL
  • serum cholesterol >200mg/dL
  • HDL-Good; clean arteries
  • LDL-Bad, builds plaque
  • Cholesterol, made in liver, Hormones and bile acid formation vital in neurological function
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2
Q

HLD Causes

-Lifestyle Choices:

A
  • poor diet
  • lack of exercise
  • smoking, stress
  • obesity
  • diabetes (more triglycerides= lower HDL)
  • Secondary: Medications (
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3
Q

HLD Causes

-Secondary:

A
  • Medications: antipsychotics (risperdone), prednisone, diuretics, beta blockers (mild)
  • Hypothyroidism (check thyroid)
  • Primary: Genetics: Familial Hypercholesteremia
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4
Q

Atherosclerosis

A
  • from untreated HLD
  • build up of plaque
  • increases risk of: MI, CVA, PVD, CHF, CAD
  • Testing: fasting total cholest; HDL, LDL, and triglycerides. (Just total cholesterol ok for screen, but not a lot of info)
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5
Q

Arteriosclerosis

A

-hardening of the arteries

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6
Q

HLD Guidelines

A
  • LDL=Less than 130
  • HDL-
  • ——-Men=Greater than 60
  • ——-Women= Greater than 50
  • Triglycerides=less than 200
  • Ignore old guidelines
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7
Q

Start HLD Treatment

A
  • 1st Lifestyle Changes :
  • Diet=less salt, less sat fats, increase fiber, heart healthy foods
  • Exercise=reg 3-4/wk, healthy weight, (exercise increases HDL, lowers LDL and triglycerides)
  • less smoking and ETOH!
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8
Q

HLD Treatment

Risk Factors

A
  • age
  • fam hx
  • smoking
  • systolic bp
  • total cholesterol
  • HDL
  • diabetes
  • Assess w/ Farmingham Scale (only good for pts 20 and older)
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9
Q

HLD Treatment

A
  • high risk or very high risk?

- LDL goal for high risk is

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10
Q

HLD MED START

A
  • diabetes
  • CAD
  • hereditary
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11
Q

HLD Meds

A
  • HMG-CoA Reductase Inhibitors
  • Azetidinones, Ezetimibe (Zetia)
  • Bile Acid Resins
  • Niacin (Nictinic Acid)
  • Fibric Acid Derivatives (gemfibrozil, fenofibrate)
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12
Q

-HMG-CoA Reductase Inhibitors

A
  • HLD
  • Simvastatin, Atorvastatin, Pravastatin
  • SAFE IN Heterozygous familial hypercholesteremia
  • By Inhibiting this enzyme LDL production is decreased and more LDL is catabolized, DECREASING LDLs
  • Myopathy(Muscle aches)
  • Arthraglia
  • Diarrhea
  • Increased LFTs
  • MONITOR: LFTs, lipids, (CPK-with interacting drug combination, can cause myalgia)=if CPK bad try another STATIN
  • ALWAYS get a BASELINE LFT and perform a 4-6 week FOLLOW UP VISIT
  • If patient is on other medications:
  • —-Inducers – increase statin dose
  • —-Inhibitors – decrease statin dose
  • NOT SAFE in PREGNANCY, BREASTFEEDING.
  • SAFE in pediatrics >10 y.o.
  • INSTRUCT to take with evening meal or at bedtime (more effective and DECREASES A.E.)
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13
Q

-HMG-CoA Reductase Inhibitors
-Simvastatin, Atorvastatin, Pravastatin
MOA

A

-By Inhibiting this enzyme LDL production is decreased and more LDL is catabolized, DECREASING LDLs

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14
Q

-HMG-CoA Reductase Inhibitors
-Simvastatin, Atorvastatin, Pravastatin
PHARM

A
  • Not well absorbed (14%)
  • Metabolized in liver via CYP3A4 (not pravatstatin)
  • Excreted in bile
  • Genotypes can increase risk of toxicity, increase bioavailability
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15
Q

-HMG-CoA Reductase Inhibitors
-Simvastatin, Atorvastatin, Pravastatin
CONTRA

A
  • Severe hepatic disease

- Persistent elevation of LFTs

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16
Q

-HMG-CoA Reductase Inhibitors
-Simvastatin, Atorvastatin, Pravastatin
SE

A
  • Myopathy (muscle aches)
  • Arthraglia
  • Diarrhea
  • Increased LFTs
  • MONITOR: LFTs, lipids, (CPK-with interacting drug combination, can cause myalgia)
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17
Q

-HMG-CoA Reductase Inhibitors
-Simvastatin, Atorvastatin, Pravastatin
PTS

A
  • SAFE IN Heterozygous familial hypercholesteremia
  • ALWAYS get a BASELINE LFT and perform a 4-6 week FOLLOW UP VISIT
  • MONITOR: LFTs, lipids, (CPK-with interacting drug combination, can cause myalgia)=if CPK bad try another STATIN
  • If patient is on other medications:
  • —-Inducers – increase statin dose
  • —-Inhibitors – decrease statin dose
  • NOT SAFE in PREGNANCY, BREASTFEEDING.
  • SAFE in pediatrics >10 y.o.
  • INSTRUCT to take with evening meal or at bedtime (more effective and DECREASES A.E.)
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18
Q

STATIN Drug Interactions

A
  • metabolized through CYP3A4
  • Inducers=will reduce plasma concentration=increase dose of statin
  • Inhibitors=will increase concentration=decrease dose of statin
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19
Q

Azetidinones

A
  • HLD
  • Ezetimibe (Zetia)
  • INHIBITS sterol transporter at brush border to cause decrease in intestinal absorption
  • DECREASES cholesterol deposition in liver and cholesterol stores
  • Has NO food effect.
  • INCREASED LFTS (esp if given additionally with reductase inhibitors)
  • MONITOR LFTs (carefully), lipids
  • UNEXPLAINED LFTs
  • GOOD to combine with statins, BUT!! MONITOR EFFECTS IF PLACING WITH A STATIN
  • AVOID in breastmilk
  • PREG C
  • used in combo w/ STATIN
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20
Q

Azetidinones
-Ezetimibe (Zetia)
MOA

A
  • INHIBITS sterol transporter at brush border to cause decrease in intestinal absorption
  • DECREASES cholesterol deposition in liver and cholesterol stores
  • in combo w/ statin
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21
Q

Azetidinones
-Ezetimibe (Zetia)
PHARM

A
  • Has NO food effect.
  • Variable absorption
  • 90% Protein Bound
  • Metabolized primarily via glucuronide conjucation, also liver
  • Excreted in stool
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22
Q

Azetidinones
-Ezetimibe (Zetia)
SE

A
  • Arthralgia
  • Diarrhea
  • Fatigue
  • INCREASED LFTS (esp if given additionally with reductase inhibitors)
  • MONITOR LFTs, lipids
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23
Q

Azetidinones
-Ezetimibe (Zetia)
CONTRA

A
  • Severe lipid disease

- UNEXPLAINED LFTs

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24
Q

Azetidinones
-Ezetimibe (Zetia)
PTS

A
  • GOOD to combine with statins, BUT!! MONITOR EFFECTS IF PLACING WITH A STATIN
  • Pregnancy: Cat C
  • AVOID in breastmilk
  • Safe in pediatrics >10 y.o.
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25
Bile Acid Resins
-HLD -Cholestyramine (Questran), Colesevelam (WelChol) -IDEALLY for PREGNANCY. Indicated for: Heterozygous familial hypercholesteremia -Binds to bile salts to form an insoluble compound, inhibiting uptake of cholesterol -CONSTIPATION -MONITOR: Lipids -Safe in pregnancy -Not excreted in breastmilk -Safe in pediatrics >10 y.o (HFH ONLY) -EDUCATE TO HYDRATE. Insoluble compounds ABSORB water causing constipation -take 1 hr before or 4 hrs after meds -take before meals
26
Bile Acid Resins -Cholestyramine (Questran), Colesevelam (WelChol) MOA
Binds to bile salts to form an insoluble compound, inhibiting uptake of cholesterol
27
Bile Acid Resins -Cholestyramine (Questran), Colesevelam (WelChol) PHARM
- Minimal absorption | - Primarily excreted in stool, small amount in urine
28
Bile Acid Resins -Cholestyramine (Questran), Colesevelam (WelChol) SE
- CONSTIPATION - GI upset - MONITOR: Lipids
29
Bile Acid Resins -Cholestyramine (Questran), Colesevelam (WelChol) CONTRA
Co administration with phenytoin and levothyroxine
30
Bile Acid Resins -Cholestyramine (Questran), Colesevelam (WelChol) PTS
- IDEALLY for PREGNANCY. - Indicated for: Heterozygous familial hypercholesteremia - Safe in pregnancy - Not excreted in breastmilk - Safe in pediatrics >10 y.o (HFH ONLY) - Cholestyramine safe in pediatrics - EDUCATE TO HYDRATE. Insoluble compounds ABSORB water causing constipation - take 1 hr before or 4 hrs after meds - take before meals
31
Nictinic Acid
- HLD - Niacin, aka Vitamin B3 - FLUSHING! (take asprin or motrin 30 mins before, prostaglandins) - INCREASED LFTs - MONITOR: LFTs and Lipids - UNKNOWN in breastfeeding
32
Nictinic Acid -Niacin, aka Vitamin B3 MOA
Not well understood but likely inhibits enzymes responsible for lipid synthesis
33
Nictinic Acid -Niacin, aka Vitamin B3 PHARM
- Good PO absorption - Unknown protein binding - Metabolized in liver - Excreted in urine
34
Nictinic Acid - Niacin, aka Vitamin B3 - SE
- FLUSHING! (take asprin or motrin 30 mins before, prostaglandins) - Diarrhea - Headache - INCREASED LFTs. - MONITOR: LFTs and Lipids
35
Nictinic Acid -Niacin, aka Vitamin B3 CONTRA
Liver Disease
36
Nictinic Acid -Niacin, aka Vitamin B3 PTS
- Safe in pregnancy at recommended doses (Cat A) - UNKNOWN in breastfeeding - Safe in pediatrics up to RDA
37
Fibric Acid Derivatives
- HLD - gemfibrozil (Lopid), fenofibrate (Tricor) - INCREASED LFTs - MONITOR: LFTs, CPK, lipids (Get baseline labs) - NOT safe in Pediatrics - NO BF - This drug can INCREASE HDL. - DOES NOT lower LDL - LOPID should NOT be given with statins (INCREASE MYOPATHY!)
38
Fibric Acid Derivatives -gemfibrozil (Lopid), fenofibrate (Tricor) MOA
- Inhibits peripheral lipolysis, decreases hepatic uptake of fatty acids - May increase HDL - Used in hypertriglyceridemia
39
Fibric Acid Derivatives -gemfibrozil (Lopid), fenofibrate (Tricor) PHARM
- 100 % Bioavailability - 99% Protein bound - Metabolized in liver - Excreted in urine and stool
40
Fibric Acid Derivatives -gemfibrozil (Lopid), fenofibrate (Tricor) SE
- Myalgia - GI upset - INCREASED LFTs - MONITOR: LFTs, CPK, lipids (Get baseline labs)
41
Fibric Acid Derivatives -gemfibrozil (Lopid), fenofibrate (Tricor) CONTRA
- Severe liver disease | - Gall bladder disease
42
Fibric Acid Derivatives -gemfibrozil (Lopid), fenofibrate (Tricor) PTS
- Pregnancy: Cat C - Unknown in breastmilk - NOT safe in Pediatrics - This drug can INCREASE HDL. - DOES NOT lower LDL - LOPID should NOT be given with statins (INCREASE MYOPATHY!)
43
Lipid Lowering Drugs: “-statin”
- MOA: inhibits HMG-CoA reductace in liver (more active around 8pm) - SE: myopathy, hepatotoxicity (basic, uncharged)-monitor liver enzymes, rhabdomyolysis Cause Rhabdomyolysis: FRIPS: fibrates, rifampin, INH, Prednisone, Statins - Clinical effects: decreases LDL (more), increases HDL, decreases triglycerides
44
2 most important HLD diagnostic tests are
are LFTs and Thyroid function
45
When initiating medicines
BASELINE LFTs and return visit 4-6 weeks for repeat LFTs
46
HMG COA Inhibitor
SAFE in HFH
47
DRUG DRUG INTERACTIONS: HLD
- If a STATIN is given with an INDUCER, INCREASE DOSE OF STATIN; - If a STATIN is given with an INHIBITOR, DECREASE DOSE OF STATIN
48
KNOW ALL THE SIDE EFFECTS OF STATINS
-Increase LFTS, myopathy, arthraglia, diarrhea. | Also, CHECK CPK if patient has myalgia
49
Zetia
good to combine with other statins HOWEVER, MUST MONITOR SIDE EFFECTS (MYALGIA)
50
Cholestyramine:
PREFERRED IN PREGNANCY and safe for HFH
51
Niacin:
CAUSES FLUSHING!! You can prescribe this with aspirin but advise to take aspiring 30 minutes prior
52
Fibric Acid Derivatives
INCREASE HDL, DOES NOT DECREASE LDL
53
Lopid
SHOULD NOT be given for statins. DO NOT COMBINE. It will increase myopathy
54
Niacin: Vitamin B3
- MOA: inhibits lipolysis in adipose tissue; decreases VLDL secretion liver - SE: myopathy, redness, flushing (prostaglandin synthesis which can be prophylaxed with aspirin), hyperglycemia, hyperuricemia (leads to gout), decreased BP - Clinical effects: decreases LDL, increases HDL (by 45%), decreases triglycerides
55
Bile Acid Resins: Cholestyramine, colestipol, colesevelam
- MOA: Block intestinal reabsorption of bile - SE: taste terrible, redness, flushing, hyperglycemia, hyperuricemia (leads to gout), gallstones - Clinical effects: decreases LDL, increases HDL, increase triglycerides
56
Fibrates: gemfibrozil, clofibrate, bezafibrate, fenofibrates (Type Four hyperlipidemia)
- MOA: upregulate LPL; increased lipoprotein lipolysis; increase triglyceride clearance; activate PPAR-alpha receptor for increased HDL synthesis - SE: myopathy, diarrhea, gallstones - Clinical effect: decreases triglycerides more than LDL, increase HDL
57
Ezetimibe:
- MOA: blocks intestinal absorption at enterocytes | - SE: diarrhea
58
Niacin
- flushing - may not improve - take no flush niacin or asprin/ ibuprofen
59
PREG - HTN - HLD
- HTN: Methladopa | - HLD: Cholestyramine
60
CYP3A4 Inducer
-need higher dose of that med
61
Statin w/ muscle pain and arthralgias
-get CPK
62
HLD TESTS
LIPIDS | THYROID
63
LFTS
CHECK BASELINE | RECHECK 4-6 WKS
64
MYALGIA AND MYOPATHY
MUSCLE PAIN/DISEASE STATINS -gemfibrozil (Lopid), fenofibrate (Tricor) ZETIA
65
CPK LEVELS
``` 22-198 MUSCLE DAMAGE MORE DRUGS, HIGHER NUMBERS STATINS -gemfibrozil (Lopid), fenofibrate (Tricor) ZETIA ```
66
INDUCER
INCREASE DOSE
67
INHIBITOR
DECREASE DOSE
68
ZETIA
CAN USE WITH A STATIN | MONITOR LABS CAREFULLY
69
BEST PREG MED
CHOLESTYRAMINE
70
NIACIN
FLUSHING PROSTAGLANDINS ASPRIN OR MOTRIN 30 MINS BEFORE
71
FIBRIC ACID
DOES NOT LOWER LDL

Pharmacology Test 3 (5 decks)

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