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DT III Exam 1 > Drugs to lower Cholesterol and Triglycerides > Flashcards

Drugs to lower Cholesterol and Triglycerides Flashcards

(58 cards)

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1
Q

First line therapy to lower cholesterol and triglycerides

A

Diet therapy

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2
Q

Resin

A

Cholestyramine, Colesevelam, Colestipol

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3
Q

Cholestyramine

A

Resin

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4
Q

Cholesevelam

A

Resin

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5
Q

Colestipol

A

Resin

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6
Q

Resin: MoA

A

Increase fecal excretion of bile acids
Decrease negative feedback by 7 alpha hydroxylase
Increase conversion of hepatic cholesterol to bile acids
Increase # of hepatic LDL receptors (lower LDL-C)

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7
Q

Bile acid negative feedback

A

7 alpha hydroxylase

Resins remove negative feedback

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8
Q

Resins: contra

A

Statins

Resin can be used in pregnancy

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9
Q

Resin: ADR

A

GI issues (bloating, constipation, stomach pain)

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10
Q

Resin: metabolism

A

Must be staggered with other drugs, especially fat soluble vitamins (ADEK) and acidic anionic drugs
Not absorbed in GI tract or biotransformed by liver
{No alteration with P450 or binding displacement}

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11
Q

Statins (HMG CoA reductase inhibitors)

A

Atorvastatin, Simvastatin, Lovastatin, Rosuvastatin, Pravastatin, Fluvastatin, Pitavastatin

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12
Q

“-statin”

A

Statins

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13
Q

Statin: MoA

A

Reversible competitive inhibitors of cholesterol biosynthesis at liver
(HMG CoA >|| Mevalonate > Cholesterol}
Increase # of hepatic plasma LDL
Lower cholesterol levels

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14
Q

Statins that lower cholesterol and triglycerides

A

Atorvastin, Rosuvastin

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15
Q

Statin: ADR

A 
Elevate plasma ALT/AST
Increase CPK (creatine phosphokinase)
Myalgia {must withdraw if happens}
(Myalgia less with Fluva and Prava}
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16
Q

Statin: contra

A

Pregnancy
Nursing mother
Acute liver disease {ALT/ AST}

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17
Q

Statins: pediatric use

A

8 yo: Pravastatin

10 yo: Other statins

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18
Q

Statin: administration and bioavailability

A

Midnight-2AM (peak cholesterol synthesis)
Higher bioavailability with food: Fluva, Lova, Simva
Lower bioavailability with food: Prava, Pitava {Don’t eat Peas at dinner}

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19
Q

Atovastatin and Rosuvastatin: MoA

A

Longer half life
Higher increase in LDL receptor
Increase clearance of IDL (ApoE)

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20
Q

Statin: prodrug

A

Lovastatin, Simvastatin

{Converted by intestinal carboxyesterase and CYP3A4}

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21
Q

Statin: CYP3A4

A

Atorva, Lova, Simva

Avoid CYP3A4 inhibitors and Grapefruit juice

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22
Q

Statin: CYP2CP

A

Rosuva, Fluva

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23
Q

Statin: CYP2D6

A

Simvastatin

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24
Q

Statin: polymorphism

Study These Flashcards
A

Simvastatin induced muscle pain
Higher with CYP2D6*4 allele (higher half life)
SCLO1B1 SNP lowers hepatic uptake higher plasma levels

25
Ezetimibe: MoA
Inhibit cholesterol absorption at brush border of small intestine Inhibit cholesterol absorption at enterocytes Inhibit NPC1L1 transporter protein Target dietary cholesterol Lower LDL-C by 20% Better with statin than statin*2
26
Ezetimibe: ADR
Minimal GI side effects, diarrhea after fatty meal
27
Ezetimibe: contra
Hepatic dysfunction (enterohepatic recirculation) Resins Stain increase transaminase levels
28
PCSK9 inhibitors
Alirocumab, Evolocumab Proprotein convertase subtilisin kexin 9 inhibitors
29
Alirocumab
PCSK9 inhibitors
30
Evolocumab
PCSK9 inhibitors
31
PCSK9 inhibitors: MoA
More LDL receptor # than statin | Subcutaneous injection per 2-4wk
32
PCSK9: ADR
Hypersensitivity
33
Fibrates
Gemfibrozil, Clofibrate, Fenofibrate {-fib-}
34
Gemfibrozil
Fibrate
35
Clofibrate
Fibrate
36
Fenofibrate
Fibrate
37
Fibrates: MoA
Lower triglycerides Increase HDL by increasing APO AI and AII Binds to PPAR alpha & stimulates fatty acid oxidation) PPAR alpha reduces apoCII expression Result in increased lipoprotein lipase activity (decrease APO CIII) PPAR decrease hepatic production of VLDL
38
ApoCIII function
Inhibit lipoprotein lipase and VLDL ligand clearance | Reduced by Fibrates
39
Fibrates: ADR
Gallstone risk (Clofibrate only) Myopathy when combined with Statin (worse with Gem and Clo) (least with Feno) {Gembifrozil inhibit OATP2 (Atova, Prava, Rosuvastatins)}
40
Fibrate: contra
Liver dysfunction Renal disease Preexisting gallbladder disease (Clofibrate)
41
Nicotinic acid: MoA
Decrease production of hepatic VLDL Inhibit lipolysis, decrease FFA delivery to liver Inhibit hormone sensitive lipase in adipose tissue Increase lipoprotein lipase activity (increase VLDL clearance)
42
Nicotinic acid: use
Lower triglycerides and cholesterol (both)
43
Nicotinic acid: ADR
Itching and Flushing (alleviated by Aspirin) {inhibit prostaglandin synthesis causing flushing} Elevate ALT/ AST (stop if x3 elevated) Peptic ulcer Hyperuricemia and glucose intolerance
44
Nicotinic acid: cautions
Monitor Creatine kinase (CK) when combined with Statin Can't interchange dose between immediate/ extended release Titration over 4wk
45
Nicotinic acid: contra
Bleeding disorders (peptic ulcer with statin) Active liver disease Active peptic ulcer
46
Familial hyperchylomicronemia
Type I Elevated Chylomicrons and triglycerides Defect in Lipoprotein lipase activity or in Apo C-II Control with diet therapy, Fibrates (Gem), Nicotinic acid
47
Familial hypercholesterolemia
``` Type IIa Elevated Cholesterol and LDL Increased CVD risk Decreased LDL clearance Control with Statins, Ezetimibe, Resins ```
48
Familial combined hyperlipoproteinemia
Type IIb Elevated Triglycerides (VLDL) and Cholesterol (LDL) Control with Statin (Atorva, Lova, Rosuva), Nicotinic acid
49
Familial dysbetalipoproteinemia
Type III Elavated Triglycerides, Cholesterol, IDL, Chylomicron remnants Decreased VLDL catabolism= IDL accumulation ApoE2 Increased VLDL production Most sensitive to Fibrates
50
Familial hypertriglyceridemia
Type IV Elevated Triglycerides and VLDL Associated with Hyperuricemia and Glucose intolerance Control with Fibrates Uric acid and blood glucose control worse with Nicotinic acid
51
Secondary cause of cholesterol elevation
Biliary disease, Renal disease, Hypothyroidism, Diabetes mellitus
52
Secondary cause of Triglycerides elevation
Alcoholism, Renal disease, Diabetes mellitus
53
Elevation of lipids by Thiazide diuretics
Elevate Cholesterol and Triglycerides
54
Elevation of lipids by non-specific beta blockers
Elevate triglycerides | Decrease HDL
55
Lipids elevated by Oral contraceptive
Elevate Triglycerides | Estrogen/ Progesterone comb
56
Drugs that lower cholesterol
Statin, Resins, Nicotinic acid
57
For patients with diabetics taking oral hypoglycemic agents
Use Lovastatin | {Nicotinic acid makes diabetes worse}
58
Avoided in first trimester of pregnancy
Statins (in all trimester)

DT III Exam 1 (5 decks)

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