Drugs for Aortic Dissection (Stuadinger) Flashcards by Monika Eszterhazy

How do Beta Blockers work for treating Aortic Dissection?

Block Epinephrine’s effects
Cause heart to beat slower and with less force, lowering BP
Opens arteries/veins to improve flow

How well did you know this?

Not at all

Perfectly

What are four common Beta Blockers used for aortic dissection?

Labetalol

Esmolol

Nitroprusside

Nicardipine

How well did you know this?

Not at all

Perfectly

What is the MOA for Labetalol?

alpha and beta blocker

How well did you know this?

Not at all

Perfectly

What are the indications for Labetalol?

treatment for arterial hypertension

used alone or in combo with other antihypertensives

How well did you know this?

Not at all

Perfectly

What are contraindications for Labetalol?

HYPERSENSITIVITY

cardiac failure

2-3’ AV block

severe bradycardia

cardiogenic shock

severe hyptension

obstructive airway disease (Asthma)

How well did you know this?

Not at all

Perfectly

What are the adverse effects of Labetalol?

Dizziness, tingling, fatigue, HA

How well did you know this?

Not at all

Perfectly

What are the warnings and precautions for Labetalol?

hepatic injury

cardiac failure

worsening ischemic heart disease

bronchospasm

pheochromocytoma

DM, hypoglycemia

major surgery

How well did you know this?

Not at all

Perfectly

What are some drug interactions of Labetalol?

Tricyclic antidepressants

Beta-Receptor agonists

Cimetidine

Halothane Anesthesia

NTG

Calcium antagonists (verapamil)

Digitalis

How well did you know this?

Not at all

Perfectly

What are the pregnancy/lactation warnings for Labetaloll?

Cat. C in pregnancy

Small amount excreted in milk

How well did you know this?

Not at all

Perfectly

What are the pediatric and geriatric indications for Labetalol?

Peds: Nothing established

Geratrics: caution, lower dose, concern for orthostatic hypotension

How well did you know this?

Not at all

Perfectly

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

55-65%

How well did you know this?

Not at all

Perfectly

How does pregnancy hormones effect Labetalol metabolism?

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

How well did you know this?

Not at all

Perfectly

What is the MOA of Esmolol?

Class II Antiarrhythmic

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

How well did you know this?

Not at all

Perfectly

What are the indications for Esmolol?

Control rapid heartbeats or abnormal rhythms

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

How well did you know this?

Not at all

Perfectly

What are the contraindications for Esmolol?

Asthma

cardiac failure

shock

bradycardia

hypersensitivity

How well did you know this?

Not at all

Perfectly

What are the pregnancy/lactation concerns for Esmolol?

Fetal bradycardia

may be used in hypertensive emergencies

unknown if present in milk

How well did you know this?

Not at all

Perfectly

What are adverse reactions to Esmolol?

Anaphylactic reactions

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

Extravasation with skin necrosis

How well did you know this?

Not at all

Perfectly

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

Hyperkalemia leading to renal impairment

*monitor serum K during therapy

How well did you know this?

Not at all

Perfectly

Esmolol can cause what effect in BP?

Hypotension

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

How well did you know this?

Not at all

Perfectly

What is the metabolism of Emsolol like?

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

What is the MOA for Nitropursside?

Na Nitroprusside breaks down in circulation to release NO

(Mechanism similar to Cialis-elevates cGMP)

What are the indications for Nitroprusside?

Lower BP immediately via injection

Reduce bleeding during surgery

treat acute HF/CHF

What are some contraindications for Nitroprusside?

Do not use for:

Compensatory HTN (AV stent/Coarctation of aorta)

Pt’s with inadequate cerebral circulation

Pt’s nearing death

What are common Adverse Reactions to Nitroprusside?

Bradyarrhthymia/Tachyrrhytmia

Hypotension

Palpitations

Ileus

Hemorrhage

CN poisoning

What is a concerning toxicity of Nitroprusside? How to avoid this?

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

Pt's receiving more than 10mg/kg of Nitroprusside will develop what? Those with impaired renal function will predictably develop what?

Methemoglobinemia (rare) Thiocyanate toxicity after prolonged rapid transfusions

What is the Black Box warning for Nitroprusside?

Excessive Hypotension Cyanide Toxicity

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

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

What is the MOA of Nicardipine?

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

What are the indications for Nicardipine?

short term injectable for HTN oral medication for long term HTN control

What are the contraindications for Nicardipine?

advanced aortic stenosis

What are the adverse effects of Nicardipine

HA Hypotension tachycardia N/V

What are the warnings of Nicardipine based on pharmacodynamic effects?

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

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

can see increase in frequency, duration or severity of angina

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

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

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

there is lower systemic clearance and higher AUC in those with moderate renal impairment when given IV or oral nicardipine ## Footnote *\*titrate gradually in these patients\**

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

unlikely

What are some reproductive/developmental toxicity concerns for nicardipine?

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

What is the pregnancy category for nicardipine?

Cat. C

What are the effects on pregnancy in animal studies of Nicardipine

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

What are the Lactation concerns for nicardipine?

minimally excreted in milk no adverse effects seen in infants No pediatric effects studied

What are the concerns of Nicardipine in geratric populations?

**Use a low dose initially**

What are the greatest precautions for Nicardipine?

excessive pharmacodynamic effects -closely monitor BP and heart rate

What are the four drug-drug interactions with Nicardipine?

B-Blockers Cimetidine Cyclosporine Tacrolimus

What happens when Nicardipine and B-Blockers are mixed?

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

What happens when Nicardipine and Cimetidine are mixed?

increases nicardipine concentrations in plasma

What happens when cyclosporine and nicardipine are mixed?

elevates cyclosporine concentration through nicardipine inhibition of CYP3A4

What happens when nicardipine and tacrolimus are mixed?

elevated tacrlimus levels thorugh nicardipine inhibition at the CYP3A4

How is Nicardipine metabolized?

**Mainly via CYP3A4** **transported via P-Gp**