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Pharm Block 1 > Drug management of Angina > Flashcards

Drug management of Angina Flashcards

1
Q

To what drug class does Nitroglycerin belong?

A

Pharmacologic class: organic nitrate
Therapeutic class: antianginal, vasodilator, venodilator

*Nitroglycerin (TNG/NitroStat™ $4 per month)

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2
Q

Describe the pharmacodynamics of Nitroglycerin.

A
  • Reacts directly with nitrate receptor on SM cell
  • Sulfhydryl groups in receptor reduce organic nitrate (R-ONO2) to NO2 and then NO
  • NO crosses into SM cells, activates guanylate cyclase, leading to production of cGMP from GTP
  • cGMP acts to relax SM cells => produces venodilation and vasodilation
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3
Q

Describe the pharmacokinetics of Nitroglycerin.

A
  • Well absorbed po, but very high first pass effect
  • Prompt onset (1-2 min) when taken as sublingual tablet or spray
  • Can be given transdermally or iv
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4
Q

What toxicity is associated with Nitroglycerin?

A
  • Excessive hypotension (esp if patient is volume depleted)
  • Throbbing headache
  • Flushing
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5
Q

What drug-drug reactions should be considered with patients on Nitroglycerin?

A
  • Excessive hypotension with other vasodilators
  • Severe hypotension if taken with Viagra™ (because it blocks phosphodiesterase type V => increase nitroglycerin effects)
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6
Q

What special considerations should be made for patients on Nitroglycerin?

A
  • Remove transdermal patch before defibrillation
  • Use only fresh TNG tablets
  • Tolerance can develop quickly (don’t take at night/don’t leave patch on at night)
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7
Q

What are the indications/dose/route for Nitroglycerin?

A

For angina => 0.15-0.3-0.4-0.6 mg sublingual tablets

  • Take one tablet every 5 minutes up to three
  • Also available as transdermal paste, IV solution
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8
Q

What are the major actions of beta blockers?

A

All Beta blockers serve to decrease HR, contractility, CO, BP (afterload), and wall tension => thereby reducing oxygen demand

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9
Q

What are 3 major Beta blockers?

A

Propranolol, metoprolol, atenolol

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10
Q

Why should abrupt withdrawal of a beta blocker be avoided?

A

Abrupt withdrawal of a beta blocker can be very dangerous, since the abrupt increase in HR, BP, contractility, etc can lead to abrupt increase in agina, or even MI

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11
Q

What other drugs can be used for angina (apart from beta blockers)?

A
  • Verapamil and Diltiazem => exertional angina

- Nifedipine (of the dihydropyridine class) => used less due to decreased clinical benefit

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12
Q

What drugs are used in the treatment of vasospastic angina?

A
  • Nitrates and Calcium entry blocker

* Beta blockers are CONTRAindicated

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13
Q

How should unstable angina be treated?

A

Unstable angina should be treated via suppression of platelet adhesion and platelet aggregation

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14
Q

To what drug class does Aspirin (Bayer™, Ascriptin™, Halfprin™) belong?

A

Pharmacologic class => salicylate

Therapeutic class => analgesic, anti-inflammatory, antiplatelet, antipyretic, prevention of MI

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15
Q

Describe the pharmacodynamics of aspirin.

A
  • At low doses ( vasodilator/inhibitor of platelet aggregation
    • Tends to irreversibly inhibit COX (1) in platelets
    • Decreased formation of TBX A2 (vasocontrictor, platelet aggregator)
    • Transiently inhibit COX(2) in endothelium
    • Transient decreased formation of prostacyclin (PGI2)
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16
Q

Describe the pharmacokinetics of aspirin.

A
  • F~60%
  • Tmax variable (e.g. AlkaSeltzer)
  • Metabolized to salicylate
  • Half-life 3-4 h
  • Duration 4-24+ h
  • 90% excreted as salicylate metabolites in urine
17
Q

What toxicity is associated with aspirin?

A

At high doses => can cause ulceration of GI tract, bleeding disorders, tinnitus

18
Q

What drug-drug interactions should be considered for patients on aspirin?

A
  • Inhibit tubular secretion of methotrexate

- Potentiate bleeding from warfarin

19
Q

What special considerations should be made for patients on aspirin?

A
  • Avoid in patients with nasal polyps and asthma

- Regular, buffered, enteric coated

20
Q

What is the indication/dose/route for aspirin?

A
  • For anti platelet effects
    • 81-325 mg per day
  • For arthritis
    • 2.4-3.6 g/day in divided doses
21
Q

To what drug class does Clopidogrel (Plavix™) belong?

A

Pharmacologic => thienopyridine
Therapeutic class=> platelet aggregation inhibitor

  • very expensive
22
Q

Describe the pharmacodynamics of clopidogrel.

A
  • Blocks ADP receptors => prevent aggregation mediated by ADP released by an activated platelet
    • Prevents recruitment of other platelets
  • Useful in primary or secondary prevention of TIA, stroke, angina, MI, angioplasty, stent placement, ACS, etc
23
Q

Describe the pharmacokinetics of clopidogrel.

A
  • Well absorbed
  • Onset 1-2 h after oral dose
  • Hepatic metabolism
  • Half-life ~8h
24
Q

What toxicity is associated with clopidogrel?

A

Hemorrhage at virtually any site

25
Q

What interactions should be considered with patients on clopidogrel?

A

May inhibit CYP 3A4

26
Q

What is the indication/dose/route for clopidogrel?

A
  • For acute coronary syndrome

- LD 300 mg up front, then 75 mg once daily (in conjunction with ASA 81-325 mg daily)

27
Q

To what drug class does Abciximab/ReoPro™ (also tirofiban/Aggrastat™, eptifibatide/Integrilin™) belong?

A

Pharmacologic class => Fab fragment chimeric monoclonal antibody
Therapeutic class => adjunct to PCI to prevent ischemic complications; treatment of MI

  • Expensive
28
Q

Describe the pharmacodynamics of Abciximab.

A
  • Noncompetitive inhibitor of the GP IIb/IIIa receptor
    • Prevents binding of fibrinogen, vWF, etc to the receptor on activated platelets.
    • Need to block >80% of these receptors to maximially inhibit platelet
29
Q

Describe the pharmacokinetics of Abciximab.

A
  • IV bolus followed by IV infusion
  • Half-life about 30 min.
  • Bleeding time declines to <12 min within 12 h of stopping infusion
30
Q

What toxicity is associated with Abciximab?

A
  • Contraindicated in presence of aneurysm
  • AV malformation
  • Bleeding, coagulopathy, GI bleed, intracranial mass, retinal bleeding
  • Stroke, surgery, low platelets, trauma, vasculitis
31
Q

What drug-drug interactions should be considered with patients on Abciximab?

A

Additive effects with aspirin, clopidogrel, heparin, low dose t-PA

32
Q

What are the indications/dose/route for Abxicimab?

A
  • When PCI is planned to treat ACS

- 0.25 mg/kg bolus (e.g. 20 mg) followed by 10 mcg/min for 18-24 h

33
Q

What is NO (nitric oxide)?

A

NO is an endothelium derived relaxing factor that inhibits platelet aggregation, phagocytosis, and excitatory neurotransmission in CNS

Pharm Block 1 (16 decks)

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