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Pharm Test 3 > Lipid-lowering > Flashcards

Lipid-lowering Flashcards

1
Q

Statins

A
  • Atorvastatin

* Pravastatin

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2
Q

Absorption blockers

A

ADJUCT TO STATIN

*Ezetimibe

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3
Q

Bile Acid Sequestrants/Resins

A

*Cholestyramine

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4
Q

Nicotinamide derivatives

A

*Gemfibrozil

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5
Q

PCSK9 inhibitors

A

Evolocumab

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6
Q

How to replenish hepatic cholesterol “pool”

A
  • UP biosynthesis of cholesterol (UP HMG-CoA reductase)

* UP LDL receptor expression –> UP LDL blood clearance (transcriptional up-regulation, response to statin therapy)

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7
Q

Insoluble fiber

A

*not digested
*lignins/cellulose/apple skin
COLON FUNCTION

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8
Q

Soluble Fiber

A
  • Oats, psyllium, pectin, metamucil) - gel-like

* resides in intestine

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9
Q

Fiber

Mech

A
  • absorbs cholesterol

* GI motility changes (up speed of passage, slow absorption of cholesterol

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10
Q

Omega-3 Polyunsaturated Fatty Acids (PUFAs)

A

LOVAZA = if HIGH TG level

*UP clearance TGs

NEED in MIs, Stroke deaths, Cardiac, sudden death

Fish 2x week = DOWN CHF, cardiac related death

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11
Q

Statins. molecule

A
  • stuctural analog = HMG-CoA (3-hydroxy-3-methylglutaryl

* Atrovastatin = Lipitor

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12
Q

Statin

Mech

A

*Inhibition of HMG CoA Reductase

  • DOWN chol synth
  • UP synthesis hepatic LDL receptors
  • UP LDL clearance = DOWN LDL cholesterol
  • small = Down TG, up HDL
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13
Q

Statins

Metab

A
  • most given at night , NOT ATORVASTATIN
  • ATORVASTATIN = CYP 3A4
  • PRAVASTATIN = metab sulfation, NOT P450, NOT protein bound (others are)
  • urine
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14
Q

Statin

Absorption

A

Atorvastatin, Pravastain = decreased w/ food

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15
Q

Intensity statin

A

LIPID LOWERING ABILITY

  • Atorvastatin = high intensity
  • Pravastatin = lower intensity
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16
Q

Statin

half lives

A

Atorvostatin - 14 hr (take any time of day)

Pravastatin = short, only take at night

17
Q

Statin

Lipophilic/ hydrophilic

A

Atrovastatin = Lipophilic

Pravastatin = Hydrophilic

18
Q

Statin

S.E.

A
  • Hepatic toxicity
  • Serum aminotransferase = activity elevation (liver dz/alcohol abuse)
  • ***Myopathy/Myalgia (not in trials)
19
Q

Statin

S.E. w/ other drugs

A
  • w/ Gemfribrozil = inhibits update + myopathy
  • Rx affectign CYP3A4/2C9
  • NONE w/ PRAVASTATIN
20
Q

Statins

Gemfibrozil blocks

A
  • OAT P1B1
  • OAT P1B3
  • OAT P2B1

Block statins transport of chol from blood to bile canaliculus

21
Q

Statins

Less common S.E.

A
  • Up DM

* CNS= cognitive dysfunction (not sure)

22
Q

Cholestrol Absorption blockers

Mech

A

ADJUNCT
*block chol absorption from intestine

*inhibits NPC1L1 (Niemann-Pick C1 like 1) (brush border)

  • DOWN intestinal chol delivery to liver => DOWN Cholesterol in chylomicrons/ remnants (atherogenics)
  • UPs LDL receptors = LDL clearance
23
Q

Ezetimibe

AMDE

A

(Chol absoprtion blocker)

  • NO P450 metab
  • both Rx + metabolite inhibit chol absorption
  • enterohepatic circulation (repeated) = long duration
24
Q

Cholestyramine

Mech

A

(Bile acid sequestrant)

  • binds bile acids, chol metabolites
  • stop reabsorption, more excretion, DEPLETES BILE ACIDS
  • more chol to bile
  • Up regulation LDL receptors = more clearance
  • UP regulation HMG-CoA reductase
25
Q

Cholestyramine

S.E.

A

(Bile acid sequestrant)

  • GI
  • Absorption other Rx impaired
26
Q

Niacin

Mech

A
  • **UP HDL ,
  • huge dose = DOWN TG + LDL (S.E.), also result of HDL raise
  • STOP lipolysis (lipase) in adipose tissue
  • DOWN free fatty acid transport to liver (DOWN VLDL synthesis)
  • DOWN TG synth in liver
27
Q

Niacin

Metab

A

*big 1st pass

28
Q

Niacin

S.E.

A
  • NO pregger
  • cutaneous Flushing = declines 1-2 weeks
  • Hepatotoxicity
  • GI = dyspepsia
29
Q

Fibrates

A

*DOWN TG (50%) varies

30
Q

Gemfibrozil

Mech

A

(Fibrate)

  • Agonist = PPAR-alpha receptor
  • DOWN TG = Up TG-rich lipoproteins
  • UP TG, UP VLDL clearance
31
Q

Gemfibrozil

T1/2?

Pregnancy?

A
  • half-life = short (1 hr)

* crosses placenta

32
Q

Gemfibrozil

Use

A

High TG

Drug of choice

33
Q

Gemfibrozil

S.E.

A
  • NO w/ renal/hepatic function
  • NO kids, preg
  • GI discomfort
  • Myopathy (w/ statin)

*Warfarin/Oral contraceptives = UP effect

34
Q

PCSK9 does?

A

Endocytoses LDL receptor, breaks it down (not recycled)

If inhibit = recycle LDL

35
Q

Evolocumab

S.E.

A

(PSK9 inhibitor)

*nasopharyngitis

36
Q

Evolocumab

Use

A
  • familial HTN

* combined with statin (max dose)

37
Q

PCSK9 Inhibitor

Results study

A

*DOWN composite CV death, MI, stroke ONLY WITH STATIN (+ all combined)

Pharm Test 3 (11 decks)

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