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CVS Pharmacology > Lipid Lowering Drugs > Flashcards

Lipid Lowering Drugs Flashcards

1
Q

Type I hyperlipoproteinaemia

A

Familial hyperchylomicronemia.
Deficiency in LPL results in elevated CM levels.
Cholesterol (+) and TG (+++)

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2
Q

Type IIa hyperlipoproteinaemia

A

Familial hypercholesterolemia.
Decreased LDL-R levels results in elevated LDL.
Cholesterol (++)

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3
Q

Type IIb hyperlipoproteinaemia

A

Familial combined (mixed) hyperlipidemia.
Overproduction of VLDL by the liver. Elevated VLDL and LDL.
Cholesterol (++) and TG (++)

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4
Q

Type III hyperlipoproteinaemia

A

Familial dysbetalipoproteinemia.
Overproduction or underutilisation of IDL resulting in elevated beta VLDL (IDL) and CM remnants.
Cholesterol (++) and TG (++)

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5
Q

Type IV hyperlipoproteinaemia

A

Familial hypertriglyceridemia.
Overproduction and/or decreased removal of VLDL triacylglycerol; elevated VLDL.
Cholesterol (+) and TG (++)

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6
Q

Type V hyperlipoproteinaemia

A

Familial mixed hypertriglyceridemia.
Increased production or decreased clearance of VLDL and CM; elevated VLDL and CM.
Cholesterol (+) and TG (++)

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7
Q

Name the 7 classes of drugs used in hyperlipidemias.

A
  1. Omega-3 acid ethyl esthers
  2. PCSK9 inhibitors
  3. Niacin
  4. Fibrates
  5. Resins
  6. HMG-CoA reductase inhibitors (“statins”)
  7. Ezetimibe
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8
Q

MOA of statins

A
  1. Inhibits HMG-CoA reductase, the rate-limiting step in de novo cholesterol synthesis
  2. Upregulates LDL receptors on the cell surface due to depletion of intraceullar cholesterol
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9
Q

Two clinical uses of statins

A
  1. Reduce plasma LDL-C levels in all types of hyperlipidaemias
  2. Reduce risk of coronary events and mortality in patients with ischaemic heart disease
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10
Q

How are statins administered?

A

Orally; in the evening

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11
Q

Why are statins administered in the evening?

A

Inhibits de novo synthesis of cholesterol when its rate is the highest due to the lack of dietary intake of cholesterol.

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12
Q

Three adverse effects of statins

A
  1. Biomedical abnormalities in liver function
  2. Myopathy and rhabdomyolysis
  3. CI: pregnancy, nursing mothers, children and teenagers (affects neurodevelopment of fetus and child)
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13
Q

Name the two PCSK9 inhibitors.

A

Evolocumab, alirocumab

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14
Q

MOA of PCSK9 inhibitors

A
  1. Inhibition of hepatic PCSK9 which targets LDL receptors for degradation in lysosomes
  2. More LDL-R on the cell surface that can bind and internalise LDL-C in circulation
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15
Q

Two clinical uses of PCSK9 inhibitors

A
  1. Lowering of LDL-C in familial hypercholesterolaemia, esp. if intolerant to statins
  2. In patients with clinically significant atherosclerotic CVD requiring additional LDL-C lowering even after diet control and maximally tolerated statin therapy
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16
Q

How are PCSK9 inhibitors administered?

A

Injection, max. serum conc. after 3 or more days, dosing every 2-4 weeks

17
Q

Three adverse effects of PCSK9 inhibitors

A
  1. Hypersensitivity reactions e.g. vasculitis or serious allergies
  2. Injection site inflammatory reactions (erythema, itchiness, swelling, pain, tenderness)
  3. Nasopharyngitis and sinusitis
    (Also expensive, and difficult to store and transport)
18
Q

Name the two fibrates.

A

Gemfibrozil, Fenofibrate

19
Q

MOA of fibrates

A
  1. Ligands for PPAR-alpha, increasing activity of LPL (alters gene exp, slow onset)
  2. Decrease in plasma TG levels
  3. Decrease plasma VLDL due to decreased secretion by the liver
  4. Rise in HDL levels
20
Q

Clinical use of fibrates

A

Treat hypertriglyceridaemias with elevated VLDL esp. dysbetalipoproteinaemia

21
Q

Name 4 adverse effects of fibrates

A
  1. GI effects; nausea
  2. Skin rashes
  3. Gallstones
  4. Myositis
22
Q

MOA of omega-3-acid ethyl esters (Omacor)

A
  1. Reduces hepatic TG production and increases TG clearance from VLDL
  2. FUNCTIONAL inhibition of diglyceride acyltransferase (TG biosynthesis) as EPA and DHA are poor substrates
  3. Increase free fatty acid breakdown (beta-ox)
  4. Increases LPL activity
23
Q

Name two clinical uses of Omacor.

A
  1. Hypertriglyceridaemia (Type IV) monotherapy
  2. Familial combined hyperlipidaemia (Type IIb) in combination with statins
24
Q

How is Omacor administered?

A

Orally (2-4g or more) with food

25
Q

Name three adverse effects of Omacor.

A
  1. GI symptoms (abdominal distension, pain, constipation, diarrhoea, dyspepsia, flatulence)
  2. DHA may increase LDL-C
  3. Reduces production of TXA2, may lead to increased bleeding time (esp. if patients on aspirin and warfarin)
  4. CI: fish allergy
26
Q

MOA of niacin (Vit B3)

A
  1. Increases HDL-cholesterol
  2. Strongly inhibits lipolysis in adipose tissue, decreasing plasma TG (in VLDL) and cholesterol (in VLDL and LDL)
  3. Decreases circulating fibrinogen and increases tPA, reverses thrombosis associated with atherosclerosis
27
Q

Clinical uses of niacin

A

Treatment of Type IIb and Type IV hyperlipoproteinemia

28
Q

How is niacin administered?

A

Orally, converted to nicotinamide in the body.

29
Q

Name two adverse effects of niacin.

A
  1. Intense cutaneous flush and pruritus
  2. Hyperuricemia and gout
30
Q

MOA of bile acid binding resins (cholestyramine)

A
  1. Bind negatively charged bile acids and bile salts in the small intestine, prevents recycling of bile acids
  2. Lowering bile acid concentration causes hepatocytes to increase conversion of cholesterol to bile acids, decreasing intracellular concentration of cholesterol
  3. Activates increased hepatic uptake of LDL-cholesterol, decreasing plasma LDL
  4. May increase VLDL
31
Q

Clinical uses of cholestyramine

A
  1. Primary hypercholesterolaemia (Type IIa)
  2. In conjunction with niacin for LDL elevations in combined hyperlipidaemia (Type IIb)
32
Q

How is cholestyramine administered?

A

Orally

33
Q

Name two adverse effects of cholestyramine.

A
  1. GI effects: constipation, nausea and flatulence
  2. Impaired absorption of fat-soluble vitamins: A, D, E, K
34
Q

What is ezetimibe?

A

Selective inhibitor of cholesterol transport protein, NPC1L1, thus reducing intestinal sterol absorption

35
Q

Clinical uses of ezetimibe

A

Reduction of LDL, may be used in conjunction with simvastatin (Vytorin)

36
Q

How is ezetimibe administered?

A

Orally

37
Q

Name one adverse effect of ezetimibe.

A

Reversible impaired hepatic function

CVS Pharmacology (3 decks)

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