Drugs for Aortic Dissection (Stuadinger) Flashcards

1
Q

How do Beta Blockers work for treating Aortic Dissection?

A
  1. Block Epinephrine’s effects
  2. Cause heart to beat slower and with less force, lowering BP
  3. Opens arteries/veins to improve flow
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2
Q

What are four common Beta Blockers used for aortic dissection?

A

Labetalol

Esmolol

Nitroprusside

Nicardipine

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3
Q

What is the MOA for Labetalol?

A

alpha and beta blocker

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4
Q

What are the indications for Labetalol?

A

treatment for arterial hypertension

used alone or in combo with other antihypertensives

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5
Q

What are contraindications for Labetalol?

A

HYPERSENSITIVITY

cardiac failure

2-3’ AV block

severe bradycardia

cardiogenic shock

severe hyptension

obstructive airway disease (Asthma)

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6
Q

What are the adverse effects of Labetalol?

A

Dizziness, tingling, fatigue, HA

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7
Q

What are the warnings and precautions for Labetalol?

A

hepatic injury

cardiac failure

worsening ischemic heart disease

bronchospasm

pheochromocytoma

DM, hypoglycemia

major surgery

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8
Q

What are some drug interactions of Labetalol?

A

Tricyclic antidepressants

Beta-Receptor agonists

Cimetidine

Halothane Anesthesia

NTG

Calcium antagonists (verapamil)

Digitalis

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9
Q

What are the pregnancy/lactation warnings for Labetaloll?

A

Cat. C in pregnancy

Small amount excreted in milk

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10
Q

What are the pediatric and geriatric indications for Labetalol?

A

Peds: Nothing established

Geratrics: caution, lower dose, concern for orthostatic hypotension

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11
Q

What percentage of Labetalol dose appears in urine as a conjugate or unchanged drug within the first 24 hours of dosing?

A

55-65%

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12
Q

How does pregnancy hormones effect Labetalol metabolism?

A

increase in progesterone causes an increase in labetalol glucoronidation, thereby allowing labetalol concentration to fall below the therapeutic value

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13
Q

What is the MOA of Esmolol?

A

Class II Antiarrhythmic

Blocks B1 adrenergic with no effect on B2 (except at high doses)

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14
Q

What are the indications for Esmolol?

A

Control rapid heartbeats or abnormal rhythms

used to treat fast heart rate and HTN during/after surgery or during other procedures

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15
Q

What are the contraindications for Esmolol?

A

Asthma

cardiac failure

shock

bradycardia

hypersensitivity

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16
Q

What are the pregnancy/lactation concerns for Esmolol?

A

Fetal bradycardia

may be used in hypertensive emergencies

unknown if present in milk

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17
Q

What are adverse reactions to Esmolol?

A

Anaphylactic reactions

*giving epinephrine to pt’s on beta-blockers may promote undesirable effects or be uneffective (Big Yikes)*

Extravasation with skin necrosis

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18
Q

Esmolol carris a concerning risk for what associated with serum K?

A

Hyperkalemia leading to renal impairment

*monitor serum K during therapy

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19
Q

Esmolol can cause what effect in BP?

A

Hypotension

reduce dose or D/C to reverse BP drop usually within 30 min.

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20
Q

What is the metabolism of Emsolol like?

A

“soft drug” that is metabolized rapidly to an inactive form by the hydrolysis if ester linkages

21
Q

What is the MOA for Nitropursside?

A

Na Nitroprusside breaks down in circulation to release NO

(Mechanism similar to Cialis-elevates cGMP)

22
Q

What are the indications for Nitroprusside?

A

Lower BP immediately via injection

Reduce bleeding during surgery

treat acute HF/CHF

23
Q

What are some contraindications for Nitroprusside?

A

Do not use for:

Compensatory HTN (AV stent/Coarctation of aorta)

Pt’s with inadequate cerebral circulation

Pt’s nearing death

24
Q

What are common Adverse Reactions to Nitroprusside?

A

Bradyarrhthymia/Tachyrrhytmia

Hypotension

Palpitations

Ileus

Hemorrhage

CN poisoning

25
Q

What is a concerning toxicity of Nitroprusside?

How to avoid this?

A

When more than 500mcg/kg is given faster than 2mcg/kg/min CN is generated faster than it can be eliminated

Giving with Na Thiosulfate can increase the rate of CN processing and reduce the hazard of CN toxicity

26
Q

Pt’s receiving more than 10mg/kg of Nitroprusside will develop what?

Those with impaired renal function will predictably develop what?

A

Methemoglobinemia (rare)

Thiocyanate toxicity after prolonged rapid transfusions

27
Q

What is the Black Box warning for Nitroprusside?

A

Excessive Hypotension

Cyanide Toxicity

28
Q

What is Nitroprusside metabolized to? (thus contributing to it’s toxic effects)

A

One molecule of Nitroprusside is metabolized to Cyanomethemoglobin and four CN- ions

Thiosulfate reacts with CN to form thiocyanate which is eliminated in the urine

29
Q

What is the MOA of Nicardipine?

A

Ca entry blocker

inhibits the transmembrane influx of Ca into cardiac muscle and smooth muscle without changing serum Ca concentration

*more selective to vascular than to cardiac muscle

30
Q

What are the indications for Nicardipine?

A

short term injectable for HTN

oral medication for long term HTN control

31
Q

What are the contraindications for Nicardipine?

A

advanced aortic stenosis

32
Q

What are the adverse effects of Nicardipine

A

HA

Hypotension

tachycardia

N/V

33
Q

What are the warnings of Nicardipine based on pharmacodynamic effects?

A

monitor for hypotension/tachycardia and avoid use in patients who have had cerebral ischemia or hemorrhage

34
Q

What are the precautions of nicardipine in patient’s with angina?

A

can see increase in frequency, duration or severity of angina

35
Q

What are the warnings of nicardipine in patients with heart failure?

A

titrate slowly when using IV nicardipine esp. in combo with beta-blockers in patients with heart failure due to negative inotropic effects

36
Q

What are the warnings of nicardipine in patients with impaired renal function?

A

there is lower systemic clearance and higher AUC in those with moderate renal impairment when given IV or oral nicardipine

*titrate gradually in these patients*

37
Q

Are there fertility, carcinogenesis or mutagenesis concerns in humans with Nicardipine?

A

unlikely

38
Q

What are some reproductive/developmental toxicity concerns for nicardipine?

A

embryotoxic in white rabbits at higher doses but not at 16mg/kg/day-8x the max human dose

39
Q

What is the pregnancy category for nicardipine?

A

Cat. C

40
Q

What are the effects on pregnancy in animal studies of Nicardipine

A

IV on rats/rabbits during organogenesis only showed toxic effects at high doses

organogenesis issues only happened at really high doses

41
Q

What are the Lactation concerns for nicardipine?

A

minimally excreted in milk

no adverse effects seen in infants

No pediatric effects studied

42
Q

What are the concerns of Nicardipine in geratric populations?

A

Use a low dose initially

43
Q

What are the greatest precautions for Nicardipine?

A

excessive pharmacodynamic effects

-closely monitor BP and heart rate

44
Q

What are the four drug-drug interactions with Nicardipine?

A

B-Blockers

Cimetidine

Cyclosporine

Tacrolimus

45
Q

What happens when Nicardipine and B-Blockers are mixed?

A

usually okay, but titrate slowly with Iv Nicardipine and B-blockers in heart failure patients

46
Q

What happens when Nicardipine and Cimetidine are mixed?

A

increases nicardipine concentrations in plasma

47
Q

What happens when cyclosporine and nicardipine are mixed?

A

elevates cyclosporine concentration through nicardipine inhibition of CYP3A4

48
Q

What happens when nicardipine and tacrolimus are mixed?

A

elevated tacrlimus levels thorugh nicardipine inhibition at the CYP3A4

49
Q

How is Nicardipine metabolized?

A

Mainly via CYP3A4

transported via P-Gp