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Pharmacology > 1-10 (Anti-Anginals) > Flashcards

1-10 (Anti-Anginals) Flashcards

1
Q

____: Imbalance in myocardial oxygen demand and supply

A

Ischemia

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2
Q

What three factors affect myocardial oxygen demand?

A

1) HR
2) Cardiac Contractility
3) Wall Tension

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3
Q

The ____ is determine by coronary blood flow and regional/tissue specific blood flow

A

oxygen supply

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4
Q

CK-MB and Troponin T and Troponin I are common markers for what medical condition?

A

MI

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5
Q

True or False: Angina is a disease

A

False - angina is NOT a disease. Rather, it is a symptom of hidden cardiovascular complication (e.g CAD/Ischemic Heart Disease)

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6
Q

What are the four type of angina?

A

1) Stable Angina
2) Unstable Angina
3) Variant/Prinzmetal Angina
4) Microvascular Angina

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7
Q

Which type of angina is associated with no overt plaques, but intense vasospasm?

A

Variant/Prinzmetal Angina

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8
Q

What causes symptoms associated with Variant/Prinzmetal Angina?

A

Malfunctioning of NO mediated vasodilation

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9
Q

What type of angina is associated with plaque rupture, platelet aggregation, and thrombus formation?

A

Unstable Angina

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10
Q

Which type of angina is associated with inappropriate vasoconstriction and lumen narrowed by plaque?

A

Stable Angina

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11
Q

What are the four causes of impaired microvessels, as is seen in Microvascular Angina?

A

1) Imbalance in neural factors
2) Endothelial factors
3) Myogenic contribution
4) Metabolic stress

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12
Q

In general, how do anti-anginal medications work?

A

1) Decrease myocardial O2 demand
2) Increase myocardial O2 supply

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13
Q

True or False: Beta blockers and calcium channel blockers can be used to treat anginas

A

True

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14
Q

What type of drug class does Ranolazine belong to?

A

Inward sodium channel inhibitor

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15
Q

What type of drug class does Ivabradine belong to?

A

Hyperpolarization activated cyclin nucleotide gated channel inhibitor

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16
Q

What are 3 high potency nitrates?

A

1) GTN/Nitroglycerin
2) Pentaerythritol tetranitrate (PETN)

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17
Q

What are 2 low potency nitrates?

A

1) ISMN (Isosorbide mononitrate)
2) ISDN (isosorbide dintrate)

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18
Q

When administered at a low dose, GTN and PETN undergo bioactivation to form nitrite. Which enzyme allows for this conversion?

A

Mitochondrial aldehyde dehydrogenases (ALDH2)

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19
Q

When GTN/PETN are given in low dose, they are are converted to nitrite then to NO. What enzymes allow for conversion to NO?

A

Xanthine Oxidase or Mitochondrial Cytochrome

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20
Q

When GTN/PETN are given in high doses, they are activated via: ____ , ____, and by ER residing ___ system, allow for NO production

A

ALDH2 (mitochondrial aldehyde dehydrogenases), mitochondrial cytochrome oxidase, and P450

21
Q

What type of nitrates are known to utilize ER residing CYP 450 system to get bioactivated and release NO, irrespective of dose?

A

Low potency nitrates (ISDN, ISMN)

22
Q

When NO is released ___ is produced, leading to production of ___ and ___ = relaxation of VSM

A

sGC (soluble guanylate cyclase) -> cGMP -> cGK-1

23
Q

What are two systemic positive effects of nitrates?

A

1) VSM - increase venous capacitance, reduce pre-load (decrease change of getting MI or HF)

2) Increase cGMP inside platelets, prevents aggravation (THIS PROPERTY IS MADE USE OF IN UNSTABLE ANGINA!!)

24
Q

What is the most common AE associated with nitrates and is due to the fact that nitrites associate with Hb to form methemoglobin (molecule w low O2 affinity)?

A

Pseudocyanosis

25
Q

Overdose of Nitrovasodilators may lead to generation of ____

A

ROS

26
Q

How does excess levels of Reactive Oxidative Species affect NO and peroxynitrite levels?

A

Excess ROS can down regulate NO by converting NO to Peroxynitrite

27
Q

DDI with nitrites?

A

PDE-5 Inhibitors

28
Q

True or False: Nitroglycerin is known to prevent first pass metabolism of Ergotamine.

A

True

29
Q

True or False: Excess ergot alkaloids can precipitate angina, should be avoided in patients on nitrites

A

True

30
Q

What drug is an inward sodium current/channel inhibitor?

A

*Ranexa/Ranolazine

31
Q

Myocardial Ischemia is accompanied by an increase in inward ____and ____in myocardial tissues

A

sodium current; sodium overload

32
Q

How does increase inward sodium current and sodium overload in myocardial tissues, as seen in Myocardial Ischemia, affect calcium entry?

A

Increase Na causes increase Ca entry via Na/Ca2+ Exchanger

33
Q

True or False: Enhanced calcium overload may increase contractility followed by a DECREASE myocardial oxygen demand

A

False - Enhanced calcium overload may increase contractility followed by a INCREASE myocardial oxygen demand

34
Q

How does Ranolazine affect:
- myocardial O2 demand?
- ca2+ overload?
- sodium load?

A
  • REDUCED myocardial O2 demand
  • indirectly PREVENTS excess ca2+ overload
  • DECREASES excess sodium load
35
Q

What drugs can Ranolazine be co-administered with?

A

Other anti-anginal drugs

36
Q

Which anti-anginal drug is contraindicated in patients with QT prolongations? Why is it contraindicated?

A

Ranolazine
- can lead to torsade de pointes and ventricular tachycardia

37
Q

How does increase SA Nodal Activity affect contractility and myocardial O2 demand?

A

Increased SA Nodal Activity increases contractility and enhances myocardial O2 demand

38
Q

True or False: Ivabradine is a HCN channel blocker

A

True

39
Q

___ inhibits sodium entry (inward funny current_ through HCN in the SA Node with reduction in HR, leading to reduced myocardial ___ demand

A

Ivabradine; HCN

40
Q

Bradycardia, A-Fib, and Visual disturbances are associated with which anti-anginal?

A

Ivabradine

41
Q

In angina, calcium channel blockers bind to which subunit of the L-Type Calcium Channel?

How does this affect HR, force of contraction, and vasodilation?

A

Alpha 1 subunit
(this is the MAIN pore-forming unit of the calcium channel)

  • HR/force of contraction: decreases
    -Increased vasodilation
42
Q

Which anti-anginal is associated with the AE of: bradycardia, asystole, and WORSENING of heart failure?

A

Calcium channel blockers

43
Q

True or False: Taking anti-retroviral drugs or grapefruit with CCB’s can enhance CCB toxicity

A

True

44
Q

What three beta-1 blockers that are most commonly prescribed for exertional angina, prior MI, or stable/unstable angina?

A

1) Atenolol
2) Metoprolol
3) Bisoprolol

45
Q

AE associated with beta-1 blockers used to treat angina?

A

1) Left Ventricular Dysfunction

46
Q

True or False: Cholestyramine and Colestipol decrease absorption of beta blockers, resulting in reduced bioavailability of beta blockers

A

True

47
Q

By specifically blocking beta-1 receptors in CV tissue, beta blockers lead to ____ chronotropic and inotropic effects. As a result, myocardial O2 demand and use is ____

A

negative; decreased

48
Q

True or False: B1 receptors are known to regulate HCN channel activity in SA Node, along with their direct stimulatory effects on cardiac muscle

A

True

49
Q

Which drugs decrease oxygen demands?
A. Vasodilators
B. Ranolazine
C. Ivabradine

A

B. Ranolazine
C. Ivabradine (decreases myocardial sodium levels)

Pharmacology (53 decks)

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