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Pharm > Hypolipidemics > Flashcards

Hypolipidemics Flashcards

1
Q

Niacin

Class

A

Nicotinic Acid

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2
Q

Niacin

MOA

A

Reduction of liver triglyceride synthesis –> less hepatic VLDL (thus, LDL) production; Dec lipolysis in adipose tissue –> dec FFA transport to liver (thus, less trigs); Dec hepatic clearance of ApoAl (raising HDL)

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3
Q

Niacin

Uses

A

Best agent to Inc HDL (30-40%);
As good as fibrates and statins at lowering Trigs (35-45%); Lowers LDL (20-30%);
Hypertriglyceridemia & low HDL

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4
Q

Niacin

Impt SE

A

Flushing
Pruritis of face/upper trunk
Rases
Acanthosis Nigricans (hyperpigmentation)

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5
Q

Niacin

Other SE

A 
Hepatotoxicity
Hyperuricemia
Hyperglycemia
Dyspepsia/Reactivation of PUD
Toxic ambylopia (rare)
Tachyarrhythmias (afib in elderly)
Myopathy
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6
Q

Niacin

Misc

A

Water sol B vit complex at [low]; Hypolipidemic at [high];
SE limit compliance (<50%)
Prevent flushing/pruritis with ASA

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7
Q

Niacin

Contraindications

A

DM

Gout

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8
Q

Name the two Fibric Acid Derivatives (GF)

A

Gemfibrozil

Fenofibrate

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9
Q

Gemfibrozil & Fenofibrate

Class

A

Fibric Acid Derivatives

Fibrates

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10
Q

Gemfibrozil & Fenofibrate

MOA

A

Unknown; may interact with peroxisome proliferator-activated receptor (PPAR-alpha) to stimulate LPL synthesis –> enhance TG-rich lipoprotein clearance; Inhibits apoC-III expression –> inc VLDL clearance; Stimulation of apoA-I and apoA-II –> inc HDL

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11
Q

Gemfibrozil & Fenofibrate

Uses

A

Severe Hypertriglyceridemia;
Marked reduction in VLDL (thus, Trigs);
Variable and small effect on LDL;
Small inc in HDL (10%)

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12
Q

Gemfibrozil & Fenofibrate

Impt SE

A

Potentiates oral anticoagulants (displace from albumin);
Increase Bile Lithogenicity;
Myositis Flu-like syndrome (5% of pts)

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13
Q

Gemfibrozil & Fenofibrate

Misc

A

Inadvisible to give with a statin due to higher myositis risk

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14
Q

Name the 3 Bile Acid Sequestrants (CCC)

A

Colestipol
Cholestyramine
Colesevelam

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15
Q

Bile Acid Sequestrants
MOA
(Colestipol, Colestyramine, Colesevelam)

A

Very positively charged resins bind negatively charged bile acids –> inhibit their reabsorption and inc cholesterol loss;
Leads to increase in LDL receptors in liver, thus dec LDL in blood

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16
Q

Bile Acid Sequestrants
Uses
(Colestipol, Colestyramine, Colesevelam)

A 
Decrease LDL (25%);
Slight inc (5%) in TG and HDL
17
Q

Bile Acid Sequestrants
Impt SE
(Colestipol, Colestyramine, Colesevelam)

A

Very safe;
Only hypolipidemic indicated for children bc not systemically absorbed;
Impairs fat sol vit absorption;
Binds other drugs (cardiac glycosides, coumarins)

18
Q

Bile Acid Sequestrants
Other SE
(Colestipol, Colestyramine, Colesevelam)

A

Bloating
Dyspepsia
Constipation
Gritty/Bad taste

19
Q

Bile Acid Sequestrants
Misc
(Colestipol, Colestyramine, Colesevelam)

A

Standard Tx in combo with statins;

Contraindicated in hypertriglyceridemia

20
Q

STATINS

  • Loyal
  • Sexual
  • Partners
  • Fear
  • Adorable
  • Rabbit
  • Pitas
A 
Lovastatin
Simvastatin
Pravastatin
Fluvastatin
Atorvastatin
Rosuvastatin
Pitavastatin
21
Q

Statins - Class

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

A

HMG-CoA Reductase Inhibitors

22
Q

Statins - MOA

Lo-, Sim-, Pra-, Flu-, Ator-, Rosu-, Pita-

A

Inhibits HMG-CoA reductase formation of mevalonate –> activation of SREBP (membrane bound transcription factor that increases LDL-R synthesis and lessens degradation); Reduction in cholesterol dec VLDL syn –> Lowering TG

23
Q

Statins - Uses

Lo-, Sim-, Pra-, Flu-, Ator-, Rosu-, Pita-

A 
Reduce LDL (20-55%)
Reduce TG (25%)
Increase HDL (5-10%)
Dyslipidemia (dec fatal/non-fatal CHD/strokes; total 20% mortality dec)
24
Q

Statins - Impt SE

Lo-, Sim-, Pra-, Flu-, Ator-, Rosu-, Pita-

A

Very few
Hepatic Dysfunction in 1%
Myopathy/Rhabdo (reduced if factors inhibiting statin catabolism lacking)

25
Q

Lovastatin & Simvastatin (zocor)

Misc

A 
Lactone Prodrugs (modified in liver to hydroxy acid form);
Must be taken in evening;
Lovastatin + Niacin = Advicor
Simvastatin + Ezetemibe = Vytorin
26
Q

Pravastatin & Fluvastatin

Misc

A

Must be taken in evening

27
Q

Atorvastatin (lipitor), Rosuvastatin (crestor), Pitavastatin

Misc

A

Longer-half life therefore can be taken anytime per day

28
Q

Ezetimbe

Class

A

Inhibits enterocyte absorption of cholesterol in intestine

29
Q

Ezetimbe

MOA

A

Decreases LDL-C alone (15-20%) or in combo with statin (60%)

30
Q

Ezetimbe

Uses

A

Inhibits cholesterol absorption by enterocytes in jejunum –> less cholesterol in chylomicrons;
Reduction in chylomicron remnant cholesterol delivery to liver; May also dec atherogenesis directly

31
Q

Ezetimbe

Misc

A 
No SEs (rare allergy)
Long-term benefit not yet proven

Pharm (7 decks)

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