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CPR Pharm > Drugs to treat Aortic Dissection > Flashcards

Drugs to treat Aortic Dissection Flashcards

1
Q

What drugs can be used to treat Aortic dissection?

A
  1. Labetalol
  2. Esmolol
  3. Nitroprusside
  4. Nitrocardipine

old LENNy with that Aortic dissection amiright???

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2
Q

How do beta blockers treat Aortic Dissection?

A
  1. block the effects of epinephrine (aka; adrenaline)
  2. Cause heart to beat more slowly and with less force–> lowers blood pressure
  3. Vasodialate veins and arteries up to help improve blood flow
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3
Q

What is Labetalol MOA?

A

blocks alpha and beta receptors

-decreaes peripheral resistance w/o significantly altering HR or CO

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4
Q

When is labetalol indicated?

A
  • arterial hypertension

- can be used alone or with other antihypertensives

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5
Q

What are the contraindications of labetalol?`

A
  1. Overt cardiac failure
  2. Greater-than-first-degree heart block
  3. Severe bradycardia
  4. Cardiogenic shock
  5. Severe hypotension
  6. Anyone with a history of obstructive airway disease
    including asthma

7.Those with hypersensitivity to the drug

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6
Q

Who should be careful with labetalol/ what are precautions

A
  1. Cardiac failure
  2. Hepatic injury
  3. Can cause non allergic bronchospasm
  4. Take caution in pheochromocytoma, DM, and hypoglycemia

Can exacerbate ischemic heart disease if withdrawal is too fast*

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7
Q

What are drug interactions of labetelol?

A
  • antidepressants –> can cause tremor

- Halothane anesthesia–> tell anesthesiologist before surgery

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8
Q

Is labetelol safe in pregnancy?

A
  • Preg. Category Ct
  • adverse effects in animal studies but not known in humans
  • can cross the placenta
  • may be used if potential benefit outweighs the risk
  • be cautious in nursing mothers
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9
Q

Describe the metabolism of labetalol

A
  • Approximately 55% to 60% of a dose appears in the urine as conjugates or unchanged labetalol within the first 24 hours of dosing
  • Labetalol clearance goes up in pregnancy
  • The increase in reproductive hormones–>Causes an increase in labetalol glucuronidation –> allows labetalol concentration to fall below the therapeutic value
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10
Q

What are black box warnings of labetalol

A

NONE

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11
Q

How should you counsel pt on Labetalol?

A
  • take exactly as prescribed
  • don’t interrupt or discontinue meds
  • tell doc if sign/sx of impending cardiac failure or hepatic dysfunction
  • may have scalp tingling-
  • monitor for conditions over regular intervals
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12
Q

How does esmolol work?

A

Class II anti-arrhythmic:
- Competitively blocks response to b1-
adrenergic stimulation
- Little effect of b2-receptors, except at high doses

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13
Q

Esmolol Indications

A

fast heartbeat and high blood pressure during

  • surgery
  • after surgery
  • during other medical procedures

(such as rate control for Afib or during other medical procedures)

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14
Q

What effect does esmolol have on Potassium?

A

Hyperkalemia

  • esp in patients with risk such as renal impairment
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15
Q

What effect can esmolol on blood pressure?

A
  • commonly causes hypotension– need to monitor patients

- stop if drops BP too much

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16
Q

What type of metabolism does esmolol have?

A

Erythrocytic!

  • soft drug- short half life of 9 min
  • Rapidly metabolized by ester linkage hydrolysis by esterase’s in cytosol of RBC
17
Q

What is the mechanism of action of Nitroprusside?

A

NO activates Guanylate Cyclase Enzyme on vascular smooth muscle

  • increases cyclic GMP –> PKG–> inactivate myosin light chains
  • Causes smooth muscle relaxation and blood vessel dilation
18
Q

What is the mechanism of nitroprusside similar to?

A

-PDE5 inhibitors like viagra and Cialis that elevate cGMP by degrading PDE5

19
Q

What is the rxn and by product of nitroprusside?

A

Sodium nitroprusside breaks down and binds to oxyhemoglobin to release

  • Nitric oxide
  • Cyanide (Toxic!!)
  • Methaemoglobin
20
Q

What are contraindications of Nitroprusside?

A
  • don’t use for compensatory HTN
  • Careful in pts with a higher cyanide/thiocyante ration (Lebers optic atrophy and tobacco amblyopia
  • don’t use in acute congestive heart failure or hepatic impairment
21
Q

Is nitroprusside okay in pregnancy?

A

Idk…. just be careful and monitor maternal pH and cyaninde

22
Q

What is a serious adverse effect of Nitroprusside? (2)

A
  • cyanide poisoning

- Thiocyanate toxicity

23
Q

How can cyanide toxicity of nitroprusside be avoided?

A
  • administer sodium nitroprusside slowly ( slower than 2mcg/kg/min)
  • Administer sodium thiosulfate to increase the rate of toxic cyanide processing
24
Q

What should be monitored in patients on nitroprusside with head trauma, increased ICP, hyponatremia, hypothyroidism, severe hepatic/ renal impairment or the elderly

A
  1. Cyanide toxicity–> can develop within an hour
  2. Check thiocyanate levels
  3. Monitor pulse ox
25
Q

The sequestration of hemoglobin as methemoglobin in nitroprusside use can result as…?

A
  • Metheglobonemia

- Thiocyanate toxicity

26
Q

What are the black box warnings of nitroprusside?

A
  • do not directly inject, need to dilute first
  • Hypotension–> can lead to irreversible ischemic injury/ death
  • cyanide toxicity from the accumulation of cyanide ion through metabolic processing
27
Q

What is the metabolism of nitroprusside?

A
  • nitroprusside is metabolized in combo with hemoglobin to
    1. one cyan-methemoglobin
    2. four CN ions
  • Thiosulfate reacts with cyanide to produce thicyanate
  • thiocyanate is eliminated in urine
28
Q

What type of drug is nicardipine?

A

Calcium entry blocker –> Dihydropyridine class

  • Slow channel blocker
  • Calcium ion antagonist

inhibits Ca2+ influx without changing serum calcium

29
Q

What is Nicardipine MOA?

A
  • Inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle without changing serum calcium concentrations
  • effects are more selective to vascular smooth muscle than
    cardiac muscle
30
Q

What are indications of Nicardipine?

A
  • Short-term treatment of hypertension

- Prolonged control of blood pressure

31
Q

When is nicardipine contraindicated?

A

Patients with advanced aortic stenosis

32
Q

Adverse effects of Nicardipine?

A
  • Headache
  • Hypotension
  • Tachycardia
  • Nausea/vomiting
33
Q

What are warnings of Nicardpine?

A
  1. Excessive pharmacodynamic effects –> can cause hypotention/tachycardia; avoid in cerebral infarction or hemorrhage
  2. Exacerbates Angina
  3. titrate slowly in heart failure -> can have negative inotropic effects (force/speed of contraction)
  4. Metabolized in liver–> be careful
  5. Impaired renal function lowers clearance
34
Q

What should be considered in geriatric patients on Nicardipine?

A

Use lower dose to start!

35
Q

What drugs interact with Nicardipine?

A
  1. Beta blockers
  2. Cimetidine
  3. Cyclosporine–>nicardipine inhibits hepatic CYP3A4–> can increase plasma Cyclosporine levels
  4. Tacrolimus–> nicardipine inhibits hepatic CYP3A4–> can increase plasma tacrolimus levels
36
Q

is nicardipine used in pregnant mothers?

A

Maybe… Pregnancy category C

  • be carefule
37
Q

What enzyme is involved in nicardipine metabolism?

A

CYP450 –> CYP3A4 Substrate

38
Q

What transporter is involved in Nicardipine metabolism?

A

P-GP (MDR1) substrate

39
Q

What is the black box warning of Nicardipine?

A

None

CPR Pharm (5 decks)

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