HLD drugs Flashcards

1
Q

Rate limiting step of cholesterol synthesis inhibited by statins

A

HMG-CoA reductase

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2
Q

Result in liver from blocking intrinsic cholesterol synthesis

A

Upregulation of hepatic LDL receptors resulting in decreased plasma LDL

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3
Q

Therapeutic effect of statins

A

Decrease in LDL, VLDL, and triglycerides
Mild increase in HDL

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4
Q

Secondary prevention of heart disease by statins

A

Improve endothelial function
Modulate inflammatory response
Maintain plaque stability
Increase NO and decrease mRNA for endothelin-1 –> vasodilation

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5
Q

Drug interactions of statins

A

Inhibitors of CyP450 –> grapefruit juice and red yeast rice

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6
Q

Adverse effects of statins

A

Myopathy
Hepatoxicity

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7
Q

Risk of myopathy in statins increases with what?

A

Concurrent therapy of gemfibrozil and/or nicotinic acid (niacin/vit B3)

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8
Q

Types of bile acid sequestrants used for HLD

A

Cholestyramine
Colestipol
Colesevelam

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9
Q

Secondary use of cholestyramine (not HLD)

A

Used in pruritis due to biliary obstruction

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10
Q

Mechanism of bile acid sequestrans

A

Bind bile acids in GIT to form insoluble complex that is excreted in the feces

Cholesterol used to make more bile –> results in lowered LDL

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11
Q

Contraindication of bile acid sequestrants

A

Hypertriglyceridemia –> increases VLDL and triglycerides

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12
Q

Adverse effects of bile acid sequestrants

A

Fat malabsorption –> steatorrhea
Malabsorption of fat soluble vitamins

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13
Q

Vitamin with lipid lowering effect at high doses

A

Niacin/nicotinic acid/vit B3

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14
Q

Mechanism of high dose niacin in HLD

A

Inhibit hepatic production of VLDL and LDL
Decreases HDL clearance
Increases lipoprotein lipase activity

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15
Q

Catalyzes hydrolysis of triacylglycerol component of circulating chylomicrons and VLDL

A

Lipoprotein lipase

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16
Q

Therapeutic effects of high dose niacin

A

Lower VLDL, LDL, and triglycerides
Increases HDL

17
Q

Fibrates used for HLD

A

Fenofibrate
Gemfibrozil

18
Q

Peroxisome proliferator-activated receptor alpha (PPAR-alpha) agonists that regulates gene transcription controlling carbohydrate and fat metabolism to increase activation of lipoprotein lipase.

A

Fibrates

19
Q

Therapeutic effect of fibrates for HLD

A

Decrease VLDL, triglycerides, and LDL
Mild increase in HLD

20
Q

Clinical indication for use of fibrates

A

Hypertriglyceridemia (>500 mg/dL)

21
Q

Adverse effects of fibrates

A

Myositis (with statin)
Hepatitis
Cholelithiasis

22
Q

Cholesterol uptake inhibitor that inhibits Niemann Pick C1 like protein, a cholesterol transporter, in the intestine

A

Ezetimibe

23
Q

Used effectively with statin to reach LDL goals in pts post MI

A

Ezetimibe

24
Q

Therapeutic effect of ezetimibe

A

Moderate decrease in LDL

25
Q

Adverse effects of ezetimibe

A

HA
Myalgia
Sinusitis and pharyngitis

26
Q

Antisense oligonucleotide against Apo B-100 mRNA used for homozygous familial hypercholesterolemia

A

Mipomerson (subQ injection)

27
Q

Adverse effects of Mipomerson

A

Hepatic fat accumulation
Pain at injection site

28
Q

PCSK9 inhibitors that decrease recycling of LDL

A

Evolocumab (Repatha)
Alirocumab (Praluent)

29
Q

Indications for use of PCSK9 inhibitors

A

Heterozygous familial hypercholesterolemia
Adjunct to statin
In pts who cannot tolerate statin

30
Q

Adverse effects of PCSK9 inhibitors

A

Injection site reaction
Hypersensitivity reaction
Increase in ALT and AST
Musculoskeletal pain

31
Q

Amphetamine derivatives that increase norepinephrine release. They have an anorexiant effect used for weight loss

A

Phentermine
Diethylpropion

32
Q

Mechanism of Orlistat

A

Blacks gastric and pancreatic lipases to decrease fat absorption

33
Q

Mechanism of Lorcaserin

A

5-HT2c agonist with anorexiant effect