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Pharmacology > MCPHS PA Pharmacology Lipid Lowering Drug practical Info Exam 3 > Flashcards

MCPHS PA Pharmacology Lipid Lowering Drug practical Info Exam 3 Flashcards

1
Q

What is the Primary Target of Statins?

A

LDL

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2
Q

Which Statins are recommended for a PT complaining of statin associated muscle complications?

A

The Hydrophilic options

Pravastatin / Rosuvastatin

or

Fluvastatin

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3
Q

Which Statins have CYP interactions?

A

CYP2C9

Fluvastatin

CYP3A4

Lovastatin

Sinvastatin

Atorvastatin

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4
Q

What is the Secondary target for clinical use of Statins?

A

PTs with clinically evident ASCVD

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5
Q

What are the adverse effects of Statins?

A

Hepatic Dysfunction (not Liver Damage)

Headache, Constipation

Teratogenic

New Onset Diabetes

Muscle Complications

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6
Q

What are the Muscle complications associated with Statins?

A

Myalgia (Muscle pain and tenderness, but no elevations in CK)

Myopathy (inflammation of muscle fibers w/ symptoms similar to myalgia plus an elevation in CK (<10 x ULN))

Rhabdomyolysis (Pain, muscle weakness&swelling, myoglobinuria & marked Elevation in CK (>10-100 x ULN))

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7
Q

What factors put an individual at risk for Statin induced muscle complications?

A

Age >80

Women > Men

Impaired Liver function

Alcohol Abuse

DDI

CYP 3A4 interactions with Grapefruit juice

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8
Q

Other than changing to a different Statin, what else can be done to help alleviate Statin associated muscle complications?

A

Lower the Statin Dose to a level that can be tolerated, and possibly use a secondary agent.

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9
Q

Which Statin has less tendency to increase risk of Diabetes?

A

Pitavastatin

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10
Q

What are the primary concerns for DDI’s with Statins?

A

CYP3A4 Inhibitors (i.e. Verapamil, Diltiazem, Grapefruit Juice etc)

CYP2C9 Inhibitors (Omeprazole, Ritonavir, etc)

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11
Q

What Statins should you prescribe to PTs currently taking CYP3A4 or CYP2C9 inhibitors?

A

Pravastatin or Rosuvastatin

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12
Q

What is Red Yeast Rice?

A

A type of rice that used to contain monacolin K (a substance identical to lovaststatin). It no longer does, and no longer has any type of medical efficacy.

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13
Q

Which Bile Acid Sequestrant (BAS) is administered as a Tablet instead of a powder?

A

Colesevelam

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14
Q

What is the Primary treament target of Bile Acid Sequestrants (BAS)?

A

Lowering LDL

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15
Q

How do BAS work?

A

BAS stop the reabsorption of Bile acids (metabolites of cholesterol) in the GI tract.

This forces the breakdown of cholesterol to make more Bile Acids, which in turn means the liver expresses more LDL receptors, and there is less LDL in the blood.

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16
Q

What is the number one problem with BAS?

A

They are very poorly tolerated causing GI bloating, constipation and abnormal taste.

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17
Q

What DDIs do BAS have?

A

They decrease the absorption of VItamins A,D,E, and K causing interactions with Warfarin, levothyroxine, digoxin, statins.

To get around this give these meds 1 hour before or 4 hours post BAS.

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18
Q

What Lipid lowering drugs are usable for Pregnant women?

A

BAS are usuable during pregnancy or in children

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19
Q

What Lipid Lowering agent may raise TG levels in PTs with Familial Cholesterol issues?

A

BAS

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20
Q

Other than major GI issues what other adherance concerns do BAS have?

A

Powders, Big Pills, and multiple daily dosing.

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21
Q

Where do BAS sit when looking at drugs to prescribe for lowering LDL?

A

Last Line drug due to tolerability and DDI issues.

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22
Q

What is the primary Target of Niacin?

A

Niacin primarily lowers TG

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23
Q

What is the MOA of Niacin?

A

Decreaes VLDL synthesis in Liver -> reduction of metabolite LDL

Increase in Lipoprotein Lipase (LPL) activity

Decrease FFA release from adipose tissue

Reduction of catabolic rate of HDL

24
Q

What is the most common adverse effect of NIacin?

A

Flushing and puritis, easily dealt with by taking low dose ASA or NSAID 30 minutes prior to use.

25
Q

Other than Flushing and puritis, what other adverse effects does Niacin have?

A

Competes with Uric Acid for secretion (increases Uric Acid)

Nausea / Abdominal discomfort

Not for use in pregnancy

Hepatically metabolized

26
Q

Niacin has been shown to have an 11% decrease in Coronary mortality vs Placebo, Does it have an impoved CV outcome vs Statins alone?

A

No, and it is not to be used in conjuction with statins (may increase Strokes), but may have a role in helping Statin intolerant PTs.

27
Q

What is the Primary target of Cholesterol Absorption Inhibitors (Ezetimibe)?

A

A 2nd Line LDL lowering drug.

28
Q

What is the mechanism and site of action of Cholesterol Absorption Inhibitors (Ezetimibe)?

A

Prevents Cholesterol absorption at the brush border of the intestine / GI tract.

Less Cholesterol in Chylomicrons

Liver notes less cholesterol on chylomicron remain uptake

Increased LDL receptors on liver, and less serum LDL

29
Q

What are the side effects of Cholesterol Absorption Inhibitors?

A

Fairly well tolerated but can cause Diarrhea, sinusitis, and Headache.

30
Q

Do Cholesterol absorption inhibitrs have any DDIs?

A

BAS can inhibit the absorption of CAIs and should be avoided while taking.

31
Q

How is Ezetimibe clinically used?

A

It is the preferred second line agent used after Statins to lower LDL, It is also used in combination with Statins to provide additional LDL reduction. (approx 17%)

32
Q

What is the primary target of Fibrate agents?

A

Lowering TGs

33
Q

What is the MoA of Fibrates?

A

PPAR agonist

Decreased VLDL synthesis in Liver

Increases Lipoprotein Lipase (LPL) mediated lipolysis.

34
Q

Can Fibrates be used in conjunction with any other Lipid Lowering Drugs?

A

Omega 3 FA

Niacin

Can be used with some Statins, but generally not recommened.

Genfibrozil is contraindicated with Simvaststain.

35
Q

What ADRs do Fibrates have?

A

Myopathy (additive with statins)

Elevated Liver transaminases

Nausea / GI upset

Skin Rash

36
Q

What are the clinical uses of Fibrates?

A

Reserved for PTs with high TG (more than 500 mg/dL), despite lifestyle modification. Consider use as monotherapy

37
Q

What are Omega-3 Fatty Acid’s primary target?

A

Lowers TG

38
Q

What is the MoA of Omega-3 Fatty Acids?

A

Inhibits Hepatic secretion of TG and promotes metabolism of TG

39
Q

What are the ADR’s of Omega-3 Fatty Acids?

A

Gross tatse (fishy)

Burps

Antiplatelet effects at high dose (monitor bleeding)

Requires very High dose (expensive)

40
Q

Are Omega-3 Fatty Acids cardioprotective?

A

No

41
Q

What is the primary target of PCSK-9 inhibitors?

A

Lowering LDL cholesterol

42
Q

What is the MoA of PCSK-9 inhibitors?

A

These are Monoclonal Antibodies that inhibit the protein (PCSK-9) which binds to and metabolize the LDL receptors on the liver. By inhibiting these proteins we ensure more LDL receptors stay avauilable to decrease blood LDL.

43
Q

When would a PCSK-9 inhibitor be used?

A

It is a 3rd line agent for lowering LDL primarily meant to be used with PT’s that have Familial Hypercholesterolemia not responding to statin.

44
Q

What are the ADRs of PCSK-9 inhibitors?

A

Headache, Arthralgia, Myalgia, limb pain, fatigue

Injection site reaction

Neurocognitive effects

45
Q

What issues other than ADR’s do PCSK-9 inhibitors have?

A

The cost! 4500-13000 a year.

46
Q

Which Lipid Lowering drugs focus on lowering LDL?

A

Statin

Ezetimibe

PCSK-9 inhibitors

BAS

Maybe Niacin

47
Q

Which Lipid Lowering drugs focus on lowering TG?

A

Omega-3 FA

Fibrate

Niacin

48
Q

Which Lipid Lowering agent combos are used to Lower LDL?

A

Statin + Ezetimibe

Statin + PCSK-9 inhibitor

Maybe NIacin + Ezetimibe

49
Q

Which Lipid Lowering agent combos are used to Lower TG?

A

Fibrate + Omega-3 FA

Fibrate + Niacin

Niacin + Omega-3 FA

50
Q

Can any of the Lipid Lowering Agents we covered raise LDL?

A

Omega-3 Fatty Acids

51
Q

What is the MoA of Statins?

A

Statins are HMG-CoA Reductase inhibitors which block the creation of Cholesterol. This forces the Liver to express more LDL receptors, causing increased LDL reuptake from circulation and lowered levels of LDL in Serum.

52
Q

What are the precautions for Statin Use?

A

Do not use Statins with active / chronic liver disease.

Do not use while pregnant

53
Q

What are the precautions for BAS use?

A

Do not use if TG > 400 mg/dL

Do not use with Bowel Obstruction

54
Q

What are the precautions for Niacin use?

A

Do not use with Chronic Liver disease

Do not use with Severe Gout

Do not use with active peptic ulcer disease (PUD)

55
Q

What are the precautions for Fibrate use?

A

Consider use as monotherapy

Not recommended to be used with statins due to risk of Myopathy. (No evidence of improved CV outcomes vs Statin alone)

Pharmacology (14 decks)

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