Pharm - Hyperlipidemics

Question 1

Atorvastatin

Answer 1

Lipitor
HMG-CoA reductase inhibitor, Statin

14 hours

Question 2

Niacin

Answer 2

nicotinic acid, vitamin B3

Question 3

fenofibrate

Answer 3

fibric acid derivative

Question 4

gemfibrozil

Answer 4

fibric acid derivative

Question 5

fluvastatin

Answer 5

Lescol, HMG-CoA reductase inhibitor, Statin

Question 6

lovastatin

Answer 6

Mevacor, HMG-CoA reductase inhibitor, Statin

Question 7

Pitavastatin

Answer 7

Livalo - HMG-CoA reductase inhibitor, Statin

Question 8

Pravastatin

Answer 8

Pravachol - HMG-CoA reductase inhibitor, Statin

Question 9

Rosuvastatin

Answer 9

Crestor - HMG-CoA reductase inhibitor, Statin

19 hours

Question 10

Simvastatin

Answer 10

Zocor - HMG-CoA reductase inhibitor, Statin

Question 11

cholestyramine

Answer 11

Bile acid seqestrant, resin

Question 12

colesevelam

Answer 12

Bile acid seqestrant, resin

Question 13

colestipol

Answer 13

Bile acid seqestrant, resin

Question 14

Ezetimibe

Answer 14

cholesterol absorption inhibitor

Question 15

lomitapide

Answer 15

new tx. for homozygous familial
hypercholesterolemia

• Once daily oral dose
  MOA: binds and inhibits microsomal triglyceride transfer proteins and prevents assembly of apoB

ADR’s: GI diarrhea and nausea, increased liver transmainases, hepatic fat accumulation

CI’s: DON’T USE PREGNANCY

Question 16

mipomersen

Answer 16

new tx. for homozygous familial hypercholesterolemia

• Once weekly injection
• adjunct to diet and other lipid lowering therapy

MOA: inhibits apo B-100 synthesis (Apo B is the main component of LDL and VLDL). Binds mRNA if apoB thus reducing formation

ADRs: flu like sx, h/a, elevation of liver transaminases

CI’s: moderate or severe hepatic impairment, active liver disease

Question 17

what is optimal target for therpay?

Answer 17

optimal = <160

Question 18

HMG-CoA Reductase inhibitors

Answer 18

• Statin: decreased LDL levels
• inhibit the rate limiting enzyme in cholesterol synthesis –> decreased cholesterol synth –> increased LDL receptor production –> pulls more LDLS out of the blood
• Pravastatin is only drug not metabolized by CYP’s (good for pt. already taking a lot of drugs)
  CI: DON’T USE for pregnant women

ADRs: LFT elevation, CPK elevation, rhabdomyolysis, myopathy

• Combination not shown to be beneficial, rather maximizing statin intesnsity reduceds ASCVD events

Question 19

Nicotinic Acid

Answer 19

• Niacin: inhibits lipolysis of triglycerides in adipose tissue, thus reduces circulation of FFA’s
• results in increased HDL levels, decreased LDL levels
• ADR’s: cutaneous flush, pruritis, acanthosis nigricans, hepatotoxicity
• CIs: hepatic disease, active PUD, caution with DM

Question 20

Fibric Acid

Answer 20

• MOA: results in decreasing pt. triglyceride levels - PPARalpha agonists, increase expression of LPL
• Gemfibrozil, fenofibrate
• useful in management of hypertriglyceridemias where VLDL predominates
• ADR’s: GI, lithiasis, myositis, myopathy
• CI’s: hepatic or renal dysfunction, pregnancy
• DI’s: warfarin increases risk of rhabdomyolysis in combo with statins

Question 21

Resins

Answer 21

= Bile Acid Sequestrants, result in cholesterol conversion being increased into bile acids –> greater chance of LDL clearance

• (bind bile acids increasing excretion 10x, increased LDL clearance)
• Colestipol, cholestyramine, colesevelam
• ADR’s: GI constipation and nausea, impaired ADEK
• CI’s: caution in divertibulitis, bowel disease, cholestasis
• ***DI’s: impairs drug absorption - need seperate administration

Question 22

Cholesterol Absorption inhibitor

Answer 22

• Agent: ezetimibe
• : inhibits NPC1L1, inhibits absorption of cholesterol and plant sterols
• ADR’s: diarrhea
• DI’s: avoid administration with bile acid sequestrants

Question 23

what decreases LDL most?

Answer 23

statins, bile acid sequesterants second

Question 24

what decreases TG’s most?

Answer 24

Fibrates

Question 25

what increases HDL most?

Answer 25

Niacin

Question 26

when to prescribe statins?

Answer 26

1. Clinical ASCVD 2. Primary elevation of LDL-C ≥ 190 mg/dL 3. Age 40-75 years with diabetes and LDL-C 70-189 mg/dL 4. No clinical ASCVD or diabetes who are 40-75 years and LDL-C 70-189 mg/dL with ASCVD risk of ≥ 7.5%

Question 27

Two high intensity statins?

Answer 27

atorvastatin: 40-80mg | Rosuvastatin 20 mg

Question 28

metabolized by CYP3A4?

Answer 28

lovastatin, simvastatin, atorvastatin

Question 29

metabolized by CYP2C9?

Answer 29

fluvastatin rosuvastatin

Question 30

CYP450?

Answer 30

pitavastatin

Question 31

what are statins used for?

Answer 31

plaque stabilization, improvement of coronary endothelial fn, inhibition of platelet thormbus formation, anti-inflamm. effects Can reduce LDL levels by 20-50%

Question 32

potency of statins

Answer 32

rosuvastatin > atorvastatin >>simvastatin >pitavastatin = lovastatin = pravastatin >fluvastatin statins should be given in evening as cholesterol synth occurs mainly at night

Question 33

adverse effects of statins?

Answer 33

elevation of serum animotransferase in liver (don't use with alcoholics or liver disease) muscle: CK activity may increase in patients with high level of physical activity rhabdomyolysis --> myoglobinuria can occur and sometimes lead to renal injury Statins increase warfarin levels contraindicated in pregnancy, liver disease, skeletal myopathies

Question 34

adverse effects of Niacin?

Answer 34

intense cutaneous flush, pruritis, rashes, acanthosis nigricans, hepatotoxicity CI: hepatic disease, active peptic ulcer use with caution in pt. w/ DM

Question 35

adverse effects of fibrates?

Answer 35

GI disturbances, lithiasis, myositis, myopathy avoid use in pt w/ hepatic or renal dysfunction can increase the risk of cholesterol gallstones - don't use in pt. with biliary tract disease

Question 36

what used to tx. pt. with primary hypercholesterolemia?

Answer 36

bile acid sequesterins = resins

Question 37

adverse effects of resins?

Answer 37

GI effects, impaired absorption of fat-soluble vitamins at high doses avoid use in pt. w/ diverticulitis, bowel disease, cholestasis