Antianginal drugs Flashcards

1
Q

Organic Nitrates: MOA

Once in cells, molecules releases NO through enzymatic action. NO increases intracellular cGMP which leads to dephosphorylation of myosin light chain smooth muscle _______.

A

relaxation

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2
Q

how do organic nitrates work?

A

These drugs work by reducing the work of the heart through systemic vasodilation

(Drops total peripheral resistance in systemic circulation and puts less work on heart to pump against higher pressure)

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3
Q

Is nitro’s primary action through coronary dilation? why?

A

NO.

The primary action is NOT coronary artery dilation.diseased arteries do not dilate well)

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4
Q

Nitroglycerin different routes of administration

A

o IV
o Ointment (Nitro-BID)
o Spray (Nitrolingual, NitroMist)
o Sublingual tablets (Nitrostat, NitroQuick)
o Transdermal (Nitro-Dur, Minitran, Transderm-Nitro)

PO Formulations
o Isosorbide mononitrate (Imdur, ISMO)
o Isosorbide dinitrate (Isordil, Dilatrate-SR)

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5
Q

What formulations of nitro are considered short acting?

A

IV, OINTMENT, SPRAY, AND SUBLINGUAL IS SHORT ACTING- USED FOR ACUTE CHEST PAIN

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6
Q

What formulations of nitro are considered long acting?

A

PO Formulations, Transdermal is long acting.

ointment- old use was long acting

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7
Q

Are the short acting or long acting nitro drugs used for prophylaxis?

A

long acting

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8
Q

uses for IV nitro

A

acute angina, acute MI, perioperative/emergency HTN

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9
Q

uses for sublingual nitro

A

acute angina treatment

(sometimes also prophylaxis- VERY SPECIFIC SITUATIONS- if someone knows they are about to do something that will cause chest pain they can take this, like push mowing lawn, etc.)

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10
Q

uses for transdermal nitro

A

prophylaxis

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11
Q

uses for ointment nitro

A

prophylaxis

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12
Q

Organic Nitrates: ADR

3

A

Headache
Facial flushing
Hypotension

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13
Q

why does nitro induce migraines?

A

It dilates blood vessels in head and you get throbbing headache

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14
Q

What is the main DDI you need to be concerned about with NITRO?

A

Main DDI is with PDE-5 Inhibitors- erectile dysfunction drugs.

Avoid concurrent use with PDE-5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)

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15
Q

When nitrate administration becomes medically necessary, you may administer nitrates only if ___hours have elapsed after use of sildenafil or vardenafil (48 hours after tadalafil use)

A

24

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16
Q

If you use nitro with someone who has taken PDE-5 inhibitors in last 24 hours, what can happen?

A

they can have a dangerous drop in BP.

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17
Q

when can organic nitrate tolerance develop?

A

Can develop if dosed continuously or too often

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18
Q

You MUST provide________ on nitrate-free intervals (typically at least 12 hours)

A

pt education

  • Use of various products requires specific education
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19
Q

When using sublingual nitrate, why can’t the patient just swallow it?

A

• It won’t work because it gets rapidly inactivated in stomach and won’t be able to get into system and cause vasodilation.

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20
Q

What are the two forms of sublingual nitro?

A

SL tablets/spray

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21
Q

are SL nitro tablets or spray more effective?

A

Both just as effective

22
Q

When should you call 911 after use of nitro?

A

Call 911 if no pain relief after 5 min

23
Q

how often can you give sublingual nitro for acute angina?

A

Can repeat q5 min

Typically max 3 doses

24
Q

nitro tablets are sensitive to what?

A

light/heat sensitive

25
Q

when patients take nitro, they should feel what type of sensation?

A

tingling

Patients should feel tingling sensation when taking nitro, this should show patient that It is active and working. If they don’t feel it then nitro Is probably expired.

26
Q

If you have angina once a month is the nitro spray or tablet better?

A

spray

Spray is sealed, bottle gets exposed to air more often so it doesn’t last as long. If you have angina only once a month then spray would be better. If pt gets pain multiple times a week then the bottle is fine.

27
Q

BBs: Use in Angina

A

First-line in all patients with chronic, stable angina unless CI

28
Q

Which BBs are preferred for patients with angina?

A

o Cardio-selective BBs are preferred

29
Q

Can BBs be used alone in variant angina?

A

NO

NOT used alone for variant angina

30
Q

warnings/ CIs for using BBs for angina

A

asthma/COPD, severe bradycardia, DPV/heart block,/vasospastic disease, DM, depression

31
Q

Why give BB in angina?

A

Decrease oxidative stress on heart and decrease oxygen demand. It does this by negative inotropy and chronotropy.

32
Q

If stopping BB, you should taper dose over several weeks to prevent rebound ___,___, AND/or ___?

A

HTN, MI, worsening angina

(Receptor adaptation- if pt is on BB for long time the body has more beta receptors, when we discontinue abruptly pt will start to have symptoms like nervousness, tachy, insomnia- epinephrine overdrive. If you have underlying CAD then it can put pt into MI.)

33
Q

BB goal resting heart rate and exercise heart rate?

A

Often titrated to resting HR 55-60, exercise HR max 75 bpm

34
Q

CCBs: Use in Angina

A
  • Can be used as add-on therapy if symptoms not controlled on BB, nitrate, or combo
  • Can be used first-line if CI/intolerance to BB and/or nitrate (Like severe lung disease, COPD, etc.)
35
Q

If BP is high, but HR is low and the pt has chest pain, what type of calcium channel blockers should you give?

A

DHP

36
Q

If BP is not very high but the pt is tachy, what type of calcium channel blocker should you give?

A

verapamil or diltiazem.

37
Q

Calcium-channel Blockers can be used to treat what types of angina?

A
  • Used for stable and variant angina
38
Q

what calcium channel blockers are preferred to use in patients with angina because of improved mortality?

A

Long-acting diltiazem or verapamil or a second generation dihydropyridine (amlodipine or felodipine) are preferred due to improved mortality

39
Q

what calcium channel blocker has a CI in AV conduction abnormalities or depressed cardiac function

A

Verapamil

40
Q

Ranolazine (Ranexa) belongs to what class of drugs?

A

Sodium-channel Blocker

41
Q

What is the MOA for Ranolazine (Ranexa) (sodium channel blockers)?

A

MOA (exact mechanism of angina control is unknown):

Inhibits sodium influx in myocytes during repolarization which reduces intracellular levels. This leads to less calcium influx.
Less Ca = less ventricular tension and oxygen consumption

42
Q

Clinical Use for Ranolazine (Ranexa) (sodium channel blockers)?

A

Chronic angina in patients who have failed other therapies, PO formulation

43
Q

Ranolazine (Ranexa) (sodium channel blockers) is metabolized via what substrates?

A

o CYP3A4/2D6 metabolism

o Many DDI: dose adjustments needed for select medications

44
Q

Warning in use of Ranolazine (Ranexa) (sodium channel blockers) because of?

A

Cardiac conduction abnormalities (prolonged QT)

45
Q

what diseases can you not use Ranolazine (Ranexa) (sodium channel blockers)?

A

o Not for acute coronary syndrome

o Liver/kidney disease

46
Q

UA, NSTEMI, or STEMI all types of ____ ____ syndrome

A

Acute Coronary Syndrome

47
Q

If dx with ACS then you should address each of the following IMMEDIATELY:
(6 things)

A
o	Hemodynamic status: HTN, HR
o	Risk stratification
o	Invasive v. medical therapy
o	Antithrombotic therapy (platelet and coag.)
o	Beta-adrenergic blockade
o	Pain
48
Q

Once acute management of ACS is complete, THEN address what?

4 things

A

o Long-term antiplatelet therapy (aspirin)
o Statins
o Long-term anticoagulant if needed (a.fib., thrombus)
o ACEI

49
Q

Chronic Stable Angina Meds/treatments?

A
  • Lifestyle
  • Exercise
  • Antiplatelet agents (ASA)
  • Cholesterol meds- STATINS
  • Antianginal drugs- NITRO (SA +/- LA), BB, CCB, Na+ channel blocker
50
Q

Drug Options for Chronic Stable Angina?

A
  • Short-acting nitrates for all to be used PRN (Sublingual- spray or tablet under tongue every 5 min)
  • Beta-blockers: first-line
  • Long-acting nitrates added when first-line drug doesn’t control symptoms (i.e., BB or CCB)
  • CCB preferred for add-on unless CI for BB