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Pharm Test 4 > Anti-Hyperlipidemia Drugs > Flashcards

Anti-Hyperlipidemia Drugs Flashcards

1
Q

Statins- available drugs

A 
Lovastatin
Simavastatin
Atorvastatin
Fluvastatin
Rosuvastatin
Pravastatin
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2
Q

Statins- Mech of action

A
  • inhibits HMG-CoA reductase & triggers SREBP transcription factor
  • leads to:

INCREASED LDL CLEARANCE
increased LDL-R expression

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3
Q

Statins- Effect on Serum Lipids

A 
decreased LDL (20-60%)
decreased TG (10-20%)
increased HDL (5-10%)
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4
Q

Statins- Adverse Effects/Contraindications

A

RHABDOMYOLYSIS
muscle myalgia/myopathy
hepatitis

CONTRAINDICATED IN SEVERE LIVER DISEASE

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5
Q

Statins- Drug Interactions- CYP34A inhibitors

A

increase [ ]s of L, S, and A

INCREASED RISK OF ADVERSE EFFECTS
ex: 
erythromycin
cyclosporin
ketaconazole
HIV protein inhibitors
grapefruit juice
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6
Q

Statins- Drug interactions- CYP3A4 inducers

A

lower [ ]s of L, S, and A

DECREASED CLINICAL EFFICACY
ex:
phenytoin
phenobarbital 
rifampin
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7
Q

Statins- Drug interactions- CYP2C9 inhibitors

A

increase [ ]s of F and R

ex.
ketoconazole
metronidazole

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8
Q

Statins- Drug interactions- other

A

Gemfibrozil

  • decreases OATP2, decreases glucoronidation= INCREASES [ALL STATINS]
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9
Q

Bile Acid Binding Resins- available drugs

A

Cholestryramine
Colestipol
Colesevelam

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10
Q

Bile Acid Binding Resins- Indications

A

high LDL

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11
Q

Statins- Indications

A

high LDL

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12
Q

Bile Acid Binding Resins- Mech of Action

A

binds bile acids and prevents reabsorption

= increased chol 7alpha-hydroxylase–> decreased cholesterol–> increased LDLR–> INCREASED LDL CLEARANCE

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13
Q

Bile Acid Binding Resins- Effect on serum lipids

A

decreased LDL (10-25%)

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14
Q

Bile Acid Binding Resins- Adverse Effects/Contraindications

A

CAN INCREASE TG LEVELS IN HYPERTRIGLYCERIDEMIA

CONTRAINDICATED WHEN TG > 400MG/DL

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15
Q

Bile Acid Binding Resins- Drug interactions

A

cholestyramine/colestipol interfere w/ absorption of a number of drugs

ex. 
warfarin
phenobarbital
digoxin
tetracycline
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16
Q

Ezetimibe- Indications

A

high LDL

17
Q

Ezetimibe- Mech of Action

A

inhibits intestinal absorption of cholesterol (via NPCL1)

= DECREASED HEPATIC CHOLESTEROL–> increased LDL-R expression–> INCREASED LDL CLEARANCE

18
Q

Ezetimibe- Effect on serum lipids

A

decreased LDL (about 18%)

19
Q

Ezetimibe- Adverse Effects/Contraindications

A
  • generally well tolerated
  • flatulence and diarrhea most common
  • myalgia and rhabdomyolysis can occur, but is very rare
  • low incidence of impaired liver function (reversible)
20
Q

Ezetimibe- Drug interactions

A

bile acid resins interfere w/ Ezetimibe absorption

21
Q

Niacin- Indications

A

high VLDL
high LDL
low HDL

22
Q

Niacin- Mech of Action

A
  1. acts via GPCR GPR109A to decrease lipolysis in adiposites
    = DECREASED [FFA]–> DECREASED VLDL
  2. increased apoAI expression
    = INCREASED HDL PRODUCTION
  3. DECREASED LP-A–> DECREASED THROMBOSIS
23
Q

Niacin- Effect on serum lipids

A 
decreased TG (30-80%)
decreased LDL (10-20%)
increased HDL (10-30%)
24
Q

Niacin- Adverse Effects/Contraindications

A
  • SKIN FLUSHING (TX-NSAID)
  • RISK OF GOUT
  • EXACERBATES PEPTIC ULCERS
  • risk of hyperglycemia
  • hepatitis
25
Q

Niacin- Drug interactions

A

none given

26
Q

Fibrates- available drugs

A

gemfibrozil

fenofibrate

27
Q

Fibrates- Indications

A

high VLDL

low HDL

28
Q

Fibrates- Mech of Action

A

LIGANDS FOR PPAR-ALPHA TRANSCRIPTION FACTOR

  1. decreased Apo C3, increased LPL expression, increased fatty acid oxidation
    = DECREASED VLDL SYNTHESIS, INCREASED VLDL CLEARANCE
  2. increased ApoAI expression
    = INCREASED HDL PRODUCTION
29
Q

Fibrates- Effect on serum lipids

A 
decreased TG (40-60%)
decreased LDL (10-20%)
increased HDL (10-20%)
30
Q

Fibrates- Adverse Effects/Contraindications

A

INCREASED GALLSTONES
RHABDOMYOLYSIS (more common with gemfibrozil)
hepatitis
myopathy

CONTRAINDICATED IN SEVERE RENAL/HEPATIC DISEASE

31
Q

Fibrates- Drug interactions

A

Strong protein binders:

  • increased warfarin–> increased risk of bleeding
  • increased sulfonylureas–> increased hypoglycemia

STATIN interaction:

  • inhibit OATP2/glucoronidation
  • increased [statins]–> increased rhabdomyolysis, esp. gemfibrozil

Pharm Test 4 (6 decks)

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