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KG - Pharmacology 2 > KG - Pharm 2 Exam 2, Antianginal Drugs > Flashcards

KG - Pharm 2 Exam 2, Antianginal Drugs Flashcards

1
Q

etiology - “classic” angina

A

atheromatous obstruction of large coronary vessels, esp w/ exercise

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2
Q

treatment - “classic” angina

A

if uncontrolled by drugs may require coronary bypass or angioplasty

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3
Q

etiology - “varian” or “angiospastic” or “Printzmetal’s” angina

A

spasm or constriction in atherosclerotic coronary vessels

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4
Q

treatment - “varian” or “angiospastic” or “Printzmetal’s” angina

A

reversed by nitrates or CCBs

- you can’t stent a spasm so you must dilate w/ drugs

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5
Q

nitrates/nitrites MOA

A
  • vasodilation via NO –> cGMP
  • UNEVEN VASODILATION
  • large veins dilated, increased venous capacity, decreased preload
  • arterioles not dilated as much but still decreases afterload
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6
Q

DOC for ACUTE ANGINAL ATTACK?

A

nitrates/nitrites

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7
Q

nitrates/nitrites - the GOOD

A
  • decreased cardiac workload: decreased preload & afterload
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8
Q

nitrates/nitrites - the BAD

A
  • increased cardiac workload: decreased BP (so increased baroreflex) –> increased HR & contractility, decreased diastolic perfusion time
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9
Q

nitrates/nitrites provide ANGINAL RELIEF by ____

A

predominantly: decr myocardial O2 requirement
secondarily: redistribution of blood flow from normal to ischemic areas (even though total bflow unchanged)

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10
Q

nitrates also relax ___

A

smooth muscle in bronchi, GI, GU tracts

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11
Q

nitrates/nitrites pharmacokinetics

A
  • oral nitrates - have HIGH FIRST PASS, rapid liver metabolization
  • inhalation, sublingual, transdermal
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12
Q

why is sublingual nitrate/nitrite preferred?

A
  • AVOID HEPATIC DESTRUCTION
  • rapid absorption
  • immediate relief, short duration
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13
Q

which nitrate/nitrite is fastest acting?

A

inhaled Amyl nitrite:

  • volatile liquid
  • inhaled
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14
Q

which nitrate/nitrite is IV?

A

nitroprusside, also fast acting

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15
Q

describe isosorbide dinitrate

A
  • solid

- sublingual or oral tablet

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16
Q

nitrates/nitrites adverse effects

A

due to vasodilation:

  • orthostatic hypotension
  • tachycardia
  • THROBBING HEADACHES
  • frequent exposure to nitrates leads to TOLERANCE OR MARKED REDUCTION of most effects - CAN NOT USE LONG TERM
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17
Q

which CCB is indicated for HTN only?

A

slow release nifedipine - may provoke angina pectoris

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18
Q

which CCB increases HR?

A

nifedipine

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19
Q

which CCB decreases HR?

A

verapamil

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20
Q

what are CCBs good for in relation to angina?

A

for CHRONIC TREATMENT, not immediate relief

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21
Q

BENEFICIAL EFFECTS nifedipine/other -dipines

A

coronary vasodilation –> increased myocardial O2 supply & decr afterload

22
Q

HARMFUL EFFECTS nifedipine/other -dipines

A

enhanced by development of MI

- rapid hypotension –> baroreflex –> incr cardiac workload

23
Q

BENEFICIAL EFFECTS verapamil/diltiazem

A

(due to decr cardiac workload)

  • decr myocardial contractility
  • bradycardia caused by decr SA node automaticity/AV conduction
24
Q

HARMFUL EFFECTS verapamil/diltiazem

A

potential for SERIOUS CARDIAC DEPRESSION that can end in arrest, AV block, CHF

25
Q

which CCB is most likely to produce tachycardia?

A

nifedipine (highest vasodilation –> marked hypotension –> reflex tachycardia)

26
Q

why don’t verapamil and diltiazem not likely to elicit reflex tachycardia?

A

weaker dilatory effects, directly depress SA/AV node function

27
Q

beta blockers - effects

A
  • major = cardiac & vascular
  • ANGINAL RELIEF (less sympathetic activation, less cardiac activity, less vasoconstriction, hypotension/bradycardia, decr cardiac workload, decr myocardial O2 demand)
28
Q

what are the CV effects of beta blockers?

A
  • heart: decr CO (blocks receptors on heart)
  • kidneys: decr renin
  • CNS: decr sympathetic vasomotor tone
29
Q

BETA ADRENERGIC BLOCKADE IS INEFFECTIVE IN _____

A

PRODUCING CORONARY VASODILATION

30
Q

beta blockers - adverse effects

A
  • bronchoconstriction
  • increase triglycerides
  • recovery from insulin-induced hypoglycemia DELAYED
  • CNS side effects (fatigue, depression, sleep)
  • can be potentially HARMFUL IN VARIANT ANGINA bc by slowing HR/prolonging ejection time you incr LV end volume & increase myocardial O2 requirement
31
Q

ranolazine MOA

A
  • partial fatty acid oxidation (PFOX) inhibitor (decr O2 consumption)
  • inhibitors late inward Na+ current (decr contractility)
32
Q

ranolazine indications/therapeutic effects

A
  • decreased LVent wall stiffness
  • improves coronary circulation
  • USED WHEN OTHER ANTI-ANGINAL MEDS DO NOT WORK
33
Q

DOC for VARIANT or ANGIOSPASTIC ANGINA?

A

nitrates and CCBs (beta blockers will not dilate spastic vessels)

34
Q

how to get best effects of angina treatment?

A

use combos of 3 major drug classes

35
Q

most effective drug combos for angina pectoris?

A

beta blockers + vasodilator for long term

36
Q

how to prevent harmful effects of CCBs or beta blockers?

A

combine with nitrates

37
Q

how to minimize reflex tachycardia?

A

combine nitrates w/ CCBs or beta blockers

38
Q

asthma least & most preferred drugs? (for pts w/ angina)

A

Most: CCB, nitrate
Least: beta blocker

39
Q

DM least & most preferred drug? (for pts w/ angina)

A

most: CCB, nitrate
least: beta blocker

40
Q

heart failure least & most preferred drug? (for pts w/ angina)

A

most: nitrate
least: beta blocker, diltiazem, verapamil

41
Q

HTN least & most preferred drug? (for pts w/ angina)

A

most: beta blocker, CCB
least: nitrate

42
Q

peptic ulcer least & most preferred drug? (for pts w/ angina)

A

most: beta blocker, nitrate
least: CCB

43
Q

Sildenafil (Viagra) MOA

A

selective inhibitor of cGMP - specific PDE5

44
Q

Sildenafil (Viagra) indications/therapeutic effects

A
  • tx male ED

- pulmonary HTN

45
Q

Sildenafil (Viagra) pharmacokinetics

A
  • oral
  • rapidly absorbed, 40% bioavailability
  • PHK dose proportional through dose range
  • max conc. reached 30-120 min
  • 1/2 life 4 hrs
  • metabolized by CYP3A4
46
Q

Sildenafil (Viagra) adverse effects

A
  • transient to mild to mod effects
  • HA, flushing, dyspepsia, congestion, UTI
  • visual impairment w/ BLUE TINGE to vision, photophobia or blurred vision
47
Q

Sildenafil (Viagra) contraindications

A
  • NOT for pregnant/lactating women
  • NOT for nitrates/nitrite use
  • use w/ alpha blockers can lead to hypotension
48
Q

what drugs could reduce Sildenafil clearance (inhibitors of CYP3A4), resulting in increase of adverse effects?

A
  • Ritonavir, saquinovir
  • ketoconazole
  • cimetidine (zantac)
  • macrolides
  • quinidine
  • zafirlukast, zileuton
    ALSO: grapefruit juice
49
Q

which new PDE5 inhibitors have less visual disturbances than Sildenafil?

A

Vardenafil
Tadalafil

  • more selective for PDE5 than PDE6
50
Q

info: Vardenafil

A
  • achieves max concentration SOONER than sildenafil - faster onset of action
51
Q

info: Tadalafil

A

duration (24-36 hrs) is LONGER than Sildenafil

- Spontaneity!

KG - Pharmacology 2 (10 decks)

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