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Pharmacology > Anti-anginal & Anti-thrombotic > Flashcards

Anti-anginal & Anti-thrombotic Flashcards

1
Q

Angina pectoris

A

an imbalance btwn oxygen supply and demand, resulting in inadequate oxygen supply to myocardium

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2
Q

chronic stable angina (CSA)

A

symptom reversibility (rest/NTG), repetitive attacks, occurs over mo. to yrs

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3
Q

Nitrates, role in therapy

A

immediate sx relief, prevention of stress induced angina

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4
Q

Nitrates MOA

A

relaxation of vascular sm. mm. vasodilation d/t the effect these drugs have on cGMP; venous relaxation reduces preload, which in turn reduces oxygen consumption

**venous dilation > arterial dilation

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5
Q

Nitrate s/e

A

hypotension, HA, flushing, light headedness

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6
Q

Nitroglycerin (NTG) class

A

nitrate

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7
Q

When is Nitroglycerin (NTG) indicated?

A

Angina (prophylactic and acute)

Can use before exercise or stress to prevent ischemic episodes

**more fast-acting; quick relief agent of nitrates

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8
Q

Nitroglycerin (NTG) should not be used with

A

PDE-5 inhibitors (e.g. Sildenafil)

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9
Q

Nitroglycerin (NTG) pharmacokinetics

A

1) onset is 1-3 min SL (primary use), 30 min patch, 60 min ER
2) duration is 25 min SL, 10-12 hr patch, 4-8 hr ER
3) extensive first pass metabolism and some non-hepaticmetabolism in RBC and vascular walls

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10
Q

What is preferred dosage form of Nitroglycerin (NTG)?

A

SL

  • quick onset of action
  • NTG has extensive first-pass metabolism in the liver
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11
Q

Isosorbide Mononitrate class

A

Nitrate

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12
Q

Isosorbide Mononitrate indications

A

anginal pectoris

**more of a long-acting, preventative agent

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13
Q

Isosorbide Mononitrate pharmacokinetics

A

1) onset is 30-45 min via IR and ER
2) duration is > 6 hr IR, 12- >24 hr ER
3) extensive first pass metabolism and some non-hepaticmetabolism in RBC and vascular walls

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14
Q

What natural products do nitrates interact with?

A

1) coleus (major)
2) hawthorn (major)
3) L-citrulline (major)
4) N-acetyl cysteine (major)

**any with hypotensive properties

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15
Q

What is the interaction between nitrates and coleus?

A

might cause additive coronary vasodilatory effects

Major

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16
Q

What is the interaction between nitrates and hawthorn?

A

might cause additive coronary vasodilatory effects

Major

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17
Q

What is the interaction between nitrates and L-citrulline (converted to L-arginine)

A

might cause additive coronary vasodilatory effects

Major

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18
Q

What is the interaction between nitrates and NAC?

A

severe hypotension, intolerable HA, anticoagulation

Major

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19
Q

Why should combination of nitrates with sildenafil be avoided?

A

too much of a build-up of cGMP –> dangerous hypotension

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20
Q

Are nitrates more specific to arterial or venous blood vessels?

A

venous

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21
Q

Beta-blockers role in therapy

A

1) prophylactic (first-line prophylactic tx)
2) blunts cardiac stimulation
3) *prevents reflex tachycardia
4) decreases HR, contractility, and BP

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22
Q

What is tachyphylaxis?

A

when people build up a tolerance to medicine with repetitive dosing

happens with isosorbide mononitrate; pt. needs to take a break to prevent tolerance

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23
Q

Beta-blockers MOA

A

blocks beta adrenergic receptors (can be selective or non-selective)

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24
Q

Beta-blockers s/e

A

bradycardia, heart block, HA, fatigue, exercise intolerance, hypotension, erectile dysfn

s/e vary with selectivity, but these tend to have a lot of s/e (“achilles heel” of this med)

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25
Q

Why should you avoid the use of beta-blockers with intrinsic sympathomimetic activity (ISA)?

A

they simultaneously block beta receptors and stimulates the sympathomimetic pathway; with heart pathology we generally want to avoid sympathomimetic stimulation

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26
Q

Where are Beta-3 receptors found?

A

adipose tissue and heart

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27
Q

Beta-blocker considerations

A

1) taper gradually or pt. may get reflex tachycardia
2) selectivity changes effect
3) CNS adverse s/e are common - dizziness, fatigue, depression, etc.
4) caution in elderly (> 65 y/o)
5) sx of hypoglycemia are often blunted

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28
Q

Metoprolol class

A

Beta blocker

Cardioselective (B1) competitive antagonist

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29
Q

Metoprolol indications

A

MI, CHF, angina, HTN

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30
Q

Metoprolol cautions

A

avoid in persons with heart block or severe bradycardia (HR < 60)

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31
Q

Metoprolol ________ is extended release (ER) or tablet and ________ is immediate release (IR)

A

1) Succinate

2) Tartrate

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32
Q

Metoprolol pharmacokinetics

A

1) onset: w/in 1 hr
2) duration: 3-6 IR, 24 hr ER
3) metabolism: CYP2C19 (minor) and CYP2D6 (major)

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33
Q

Metoprolol natural products interactions

A

many moderate (“be cautious”) warnings

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34
Q

Atenolol class

A

Beta-blocker

Cardioselective (B1) competitive antagonist

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35
Q

Atenolol indications

A

MI, HTN, angina

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36
Q

Atenolol cautions

A

avoid in persons with heart block or severe bradycardia (HR < 60)

**concerns about safety b/c in some populations, more ppl are dying on this drug than other beta blockers; although better mortality rates in silent ischemia population

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37
Q

Atenolol pharmacokinetics

A

1) onset < 1 hr
2) duration 12-24 hr
3) limited hepatic metabolism, 50% feces, 40% urine (unchanged drug)

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38
Q

What is the significance of Atenolol limited hepatic metabolism?

A

potentially less subject to interactions, as most drug interactions occur via CYP450 pathways in liver

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39
Q

Atenolol natural products interactions

A

1) many moderate (“be cautious”) warnings

2) major interaction with apple (reduced Atenolol concentrations)

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40
Q

Propranolol class

A

Beta blocker

Nonselective (B1 and B2)

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41
Q

Propranolol indications

A

MI (tx and prevention), HTN, angina, migraine prophylaxis, SV arrhythmias

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42
Q

Propranolol cautions

A

avoid in persons with heart block or severe bradycardia (HR < 60)

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43
Q

Propranolol pharmacokinetics

A

1) onset 1-2 hr
2) duration: 6-12 hr IR, 24-72 hr ER
3) metabolism: CYP1A2 (major), CYP2C19 (minor), CYP2D6 (major), CYP3A4 (minor), p-glycoprotein

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44
Q

Propranolol natural products interactions

A

1) many moderate (“be cautious”) warnings
2) major interaction with Rauwolfia (Indian snakeroot) - enhanced beta-blockade
3) major interaction with Hypericum - increased metabolism

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45
Q

Carvedilol class

A

Beta-blocker

nonselective with alpha-1 adrenergic blockade activity

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46
Q

Carvedilol indications

A

MI, HTN, CHF, angina (off-label)

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47
Q

Carvedilol cautions

A

avoid in persons with heart blockage or severe bradycardia (HR < 60)

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48
Q

Carvedilol pharmacokinetics

A

1) onset: < 1 hr
2) duration: 24 hr
3) metabolism: CYP1A2 (minor), CYP2C9 (minor), CYP2D6 (major), CYP2E1 (minor), CYPE3A4 (minor), P-glycoproteins

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49
Q

Carvedilol natural products interactions

A

1) many moderate (“be cautious”) warnings

2) major interaction w/ grapefruit juice (increases bioavailability)

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50
Q

Which beta blockers are more likely to interact with beta-agonists used in asthma?

A

non-selective

51
Q

Which beta-blocker covers both beta and alpha receptors?

A

carvedilol

although it turned out to be no more effective than other beta blockers

52
Q

CCBs role in therapy

A
  • prophylactic tx
  • decreases BP
  • dilates coronary b.v.
  • dilates peripheral b.v.

(second-line angina tx)

53
Q

CCBs MOA

A

blocks calcium influx leading to relaxation of cardiac and smooth muscles

54
Q

CCBs s/e

A

**Tachycardia, **edema (esp. lower extremity), HA, fatigue, exercise intolerance, hypotension

vary with selectivity

rebound sx w/ abrupt d/c is less of a concern

55
Q

Avoid IR nifidipine for _______ d/t poor outcomes

A

stable angina

56
Q

Avoid non-dihydropyridines in pt with __________ and in pt. also taking __________

A

1) ejection fraction < 35% (heart failure)

2) beta-blockers

57
Q

Amlodipine class

A

DHP CCB

58
Q

Amlodipine indications

A

HTN, chronic stable angina, variant angina, heart failure, d/o of CV system (prophylaxis)

59
Q

Amlodipine pharmacokinetics

A

1) onset 24 hr (slowest)
2) duration > 24 hr (longest T 1/2)
3) CYP3A4 metabolism

60
Q

Amlodipine natural products interactions

A

1) many moderate interactions
2) Cholea - increased vasodilatory effects
3) Grapefruit (CYP3A4 inhibitor)
4) Hypericum (CYP3A4 inducer)

61
Q

Verapamil class

A

Non-DHP

phenylalklamine CCB

62
Q

Verapamil indications

A

HTN, CSA, variant angina, SVT, Afib/Aflutt

63
Q

Verapamil pharmacokinetics

A

1) onset 1-2 hr
2) duration 6-8 hr IR, 24 hr ER
3) metabolism: CYP1A2 (minor), CYP2B6 (minor), CYP2C9 (minor), CYP2E1 (minor), CYP3A4 (major), P-glycoprotein

64
Q

Verapamil natural products interactions

A

1) many moderate interactions
2) Cholea - increased vasodilatory effects
3) Grapefruit (CYP3A4 inhibitor)
4) Hypericum (CYP3A4 inducer)
5) Alcohol (incr. hepatotoxicity)

65
Q

Diltiazem class

A

Non-DHP

Benzothiazepine CCB

66
Q

Diltiazem indications

A

atrial arrhythmia, HTN, SVT, angina

67
Q

Diltiazem cautions

A

avoid w/ hypotension, LVEF < 30%, AV block, sick-sinus syndrome, certain arrhythmias (WPW, accessory tract arrhyth.)

68
Q

Diltiazem pharmacokinetics

A

1) onset: 15-60 min
2) duration: 6 hr IR, 24 hr ER
3) metabolism: CYP2C0 (minor), CYP2D6 (minor), CYP3A4 (major), p-glycoprotein

69
Q

Diltiazem natural product interactions

A

1) many moderate interactions
2) Cholea - increased vasodilatory effects
3) Grapefruit (CYP3A4 inhibitor)
4) Hypericum (CYP3A4 inducer)

70
Q

How do the mechanisms differ between DHP and non-DHP CCBs?

A

DHP primarily work in the periphery and non-DHP primarily work in the heart

*if pt. is not already on a beta-blocker, you would lean more twd non-DHP meds

71
Q

Why are CCBs more likely to have drug interactions w/ other therapeutic moieties?

A

first-pass metabolism in liver with so many diff CYP’s

72
Q

Aspirin class

A

anti-platelet

73
Q

Aspirin MOA

A

non-selective, irreversible COX inhibitor

**this action is what is responsible for aspirin’s cardioprotective effects

74
Q

How long is the lifespan of a platelet?

A

7-10 days

75
Q

Aspirin caution

A

1) avoid in pt. < 18 y/o d/t association w/ Reye’s Syndrome
2) increased bleeding (GI)
3) Disruption of renal perfusion

76
Q

Aspirin pharmacokinetics

A

1) onset w/in 1 hr if chewed
2) hydrolyzed to salicylate (active form) by esterases in GI, RBC, synovial fluid, and blood; quickly broken down (< 3 hr) via hepatic conjugation…so it only has 3 hr to bing to as many platelets as possible, but once bound it binds to life of platelet

77
Q

Aspirin natural products interactions

A

1) Cocoa
2) Danshen
3) Dong Quai
4) Evening primrose
5) policosanol
6) willow bark

**incr. bleeding

78
Q

Do NSAIDs other than aspirin have effects on platelets?

A

YES

it’s just that they don’t have cardioprotective capabilities because the bind reversibly to COX-1 (they do still cz incr. bleeding)

79
Q

Clopidogrel (Plavix) class

A

antiplatelet

80
Q

Clopidogrel (Plavix) MOA

A

irreversibly blocks P2Y_12 component of ADP receptors on platelets surface –> reduces platelet aggregation

**just as effective as aspirin but doesn’t affect PG production, so see less GI bleeding

81
Q

Clopidogrel (Plavix) indications

A

post NSTEMI, ACS, CVA, PCI, and arterial occlusive dz to prevent clots

82
Q

Clopidogrel (Plavix) pharmacokinetics

A

1) onset: detected 2nd day of tx
2) lasts lifespan of platelet
3) primarily metabolism in liver via CYP450-mediated rxn

83
Q

Clopidogrel (Plavix) natural interactions

A

1) Cocoa
2) Danshen
3) Dong Quai
4) Evening primrose
5) policosanol
6) willow bark
* *incr. bleeding

7) Grapfruit (CYP34A inhibitor)
8) Hypericum (CYP34A inducer)

84
Q

Ticagrelor (Brilinta) class

A

antiplatelet

85
Q

Ticagrelor (Brilinta) MOA

A

reversibly blocks P2Y_12 component of ADP receptors on platelets surface –> reduces platelet aggregation

86
Q

Ticagrelor (Brilinta) indications

A

prophylaxis post ACS, MI, or PCI

87
Q

Ticagrelor (Brilinta) cautions

A

increased risk of bleeding, increased uric acid levels

88
Q

Ticagrelor (Brilinta) pharmacokinetics

A

1) onset: ~41% platelet inhibition w/in 30 min
2) duration depends on concentration of drug (not lifespan of platelet) - up to 24 hr
3) Metabolism: CYP34A (major)

89
Q

Ticagrelor (Brilinta) interactions

A

1) Cocoa
2) Danshen
3) Dong Quai
4) Evening primrose
5) policosanol
6) willow bark
* *incr. bleeding

7) Grapfruit (CYP34A inhibitor)
8) Hypericum (CYP34A inducer)

90
Q

Prasugrel (Effient) class

A

antiplatelet

91
Q

Prasugrel (Effient) MOA

A

irreversibly blocks the P2Y_12 component of ADP receptors on platelets surface –> reduces platelet aggregation

92
Q

Prasugrel (Effient) cautions

A
  • avoid in persons who have had a prior TIA or stroke (higher risk of cerebral hemorrhage)
  • incr. risk for bleeding w/ body weight < 60 kg
93
Q

Prasugrel (Effient) pharmacokinetics

A

1) onset < 30 min
2) duration lasts lifetime of platelets
3) CYP450-mediated pathway (CYP3A4 and CYP2B6) converts it into its active form

94
Q

Do drug interactions affecting CYP enzymes tend to increase or decrease the effectiveness of P2Y_12 inhibitors?

A

depends on the drug and how it’s metabolized

s/t CYP enzymes metabolize drug into active form and s/t they metabolize drug into inactive form

95
Q

Warfarin (Coumadin) class

A

anticoagulants

96
Q

Warfarin (Coumadin) MOA

A

inhibits vitamin K oxide reductase (enzyme responsible for regenerating vit K so it can activate clotting factors)

97
Q

Warfarin (Coumadin) cautions

A

1) genetic polymorphisms affect safety/efficacy
2) antidote is Vit K, but process is slow and cumbersome
3) **must do lifetime INR monitoring
4) many drug interactions

98
Q

Vitamin K dependent clotting factors

A

II, VII, IX, X

99
Q

Warfarin (Coumadin) pharmacokinetics

A

1) onset: effects INR w/in 2-5 days
2) T 1/2 = 20-60 hr
3) Metabolism: CYP1A1 (minor) CYP2C19 (minor), CYP2C9 (major), CYP34A (minor)

100
Q

Warfarin (Coumadin) natural products interactions

A

alfalfa, American ginseng, alcohol, cocoa, danshen, dong quai, EDTA, evening primrose oil, glucosamine HCl and sulfate, grapefruit, licorice, N-acetyl glucosamine, policosanol, Hypericum, Vit K, willow bark, wintergreen

101
Q

What is the INR?

A

International Normalized Ratio

INR is the std unit used to report prothrombin time (PT)

We tend to want a target INR of 2-3 (risk of bleeding incr. significantly at INR above 5)

102
Q

Rivaroxaban (Xarelto) class

A

novel oral anticoagulant

Xa-inhibitor

103
Q

Rivaroxaban (Xarelto) MOA

A

direct, reversible inhibition of factor Xa –> prevents activation of thrombin (factor II) and downstream prevents conversion of fibrinogen to fibrin

104
Q

Rivaroxaban (Xarelto) cautions

A

1) Taking w/out food can significantly reduce absorption
2) Must monitor renal fn (but do not need INR)
3) Onset is quick but T1/2 is short so they dose a lot of drug at once time - increases risks

105
Q

Rivaroxaban (Xarelto) pharmacokinetics

A

1) onset 2-4 hr
2) T 1/2 5-9 hr
3) Metabolism: hepatic via CYP3A4/5 and CYP2J2

106
Q

Rivaroxaban (Xarelto) interactions with natural products

A

cocoa, danshen, dong quia, EPO, grapefruit, policosanol, Hypericum, Willow bark

107
Q

Apixaban (Eliquis) class

A

novel oral anticoagulant

Xa-inhibitor

108
Q

Apixaban (Eliquis) MOA

A

direct, reversible inhibition of factor Xa –> prevents activation of thrombin (factor II) and downstream prevents conversion of fibrinogen to fibrin

109
Q

Apixaban (Eliquis) cautions

A

1) Must monitor renal fn (but do not need INR)

more favorable safety/efficacy than warfarin or rivaroxaban

110
Q

Apixaban (Eliquis) pharmacokinetics

A

1) onset 3-4 hr
2) T1/2 = 12 hr
3) Metabolism: hepatic mainly via CYP3A4/5

111
Q

What is the only novel oral anticoagulant that is not renally adjusted?

A

Apixaban (Eliquis)

dosage is determined by SCr, weight, and age

112
Q

Apixaban (Eliquis) natural product interactions

A

Coca, danshen, dong quai, EPO, grapefruit, policosanol, Hypericum, willow bark

113
Q

Dabigatron (Pradaxa) class

A

Novel oral anticoagulants

IIa (thrombin) inhibitor

114
Q

Dabigatron (Pradaxa) MOA

A

direct thrombi (activated factor II) inhibitor –> prevents conversion of fibrinogen to fibrin

115
Q

Dabigatron (Pradaxa) cautions

A

similar safety and efficacy to warfarin (concern for GI bleed, MI)

116
Q

Dabigatron (Pradaxa) pharmacokinetics

A

1) onset 1 hr (delayed 2 hr by food)

2) Metabolism is mostly renal; prodrug hydrolyzed to active form hepatically

117
Q

Dabigatron (Pradaxa) reversal agent

A

Praxbind (idarucizumab) - monoclonal antibody that rapidly binds pradaxa

118
Q

Dabigatron (Pradaxa) natural products interactions

A

cocoa, danshen, dong quai, EPO, policosanol, Hypericum, willow bark

119
Q

Does warfarin target more or fewer targets compared to NOACs to elicit its anticoagulant effects?

A

more

120
Q

Which of the NOACs is dosed once per day?

A

Rivaroxaban (Xarelto)

121
Q

What is Enoxaparin (Lovenox)

A

low molecular weight “fractioned” heparin (LMWH)

enhances inhibition rate of clotting proteases (more factor Xa inhibition compared to factor IIa)

122
Q

What is reversal agent for warfarin?

A

Vitamin K (PO and IV) - slow and cumbersome

leafy greens, cabbage, broccoli

123
Q

Compared to unfractioned heparins, LMWHs have less activity at which factor?

A

IIa

Pharmacology (14 decks)

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