Drug Flaschards 13.08.26 Epi and Norepi Flashcards
Norepi Other Names?
noradrenaline, Levophed
Norepi Drug Class…
Pharmacologic Class?
Therapeutic Class?
- pharmacologic class—direct-acting adrenergic agonist
* therapeutic class—vasopressor, vasoconstrictor
Norepi Pharmacodynamics?
What is the major action?
What is the minor action?
What are the main effects?
- Major action is to stimulate peripheral alpha-1 adrenoceptors, thereby leading to vasoconstriction (resistance arterioles, increase SVR) and venoconstriction (in capacitance vessels, increase preload).
- This increases CO, SVR, and MAP, but decreases blood flow to vulnerable tissues like skin, muscle, and kidney.
- Minor action stimulates beta-1 receptors in the heart, increasing HR and contractility
- Main effects are vasoconstriction and cardiac stimulation.
Norepi stimulates peripheral _____ receptors which leads to increases CO, SVR, and MAP.
Norepi stimulates heart _____ receptors which increases HR and Contractility
Alpha-1
Beta-1
Norepi Pharmacokinetics?
What is F %?
How is it administered?
What enzyme metabolizes Norepi and in what organ?
Where are metabolites of Norepi excreted?
What is the half-life of Norepi?
What Blood-Tissue barriers can Norepi cross and not cross?
- F ~100%.
- Given IV only.
- Metabolized by COMT and MAO, mostly in liver.
- Metabolites are excreted in urine.
- Half-life 1-2 minutes (e.g. can be titrated quickly IV).
- Can cross the placenta, but not the blood/brain barrier.
Norepi…
What is F%?
How is it administered?
- F ~100%.
* Given IV only
Norepi…
What enzymes metabolizes Norepi and in what organ?
How are the metabolites excreted?
- Metabolized by COMT and MAO, mostly in liver.
* Metabolites are excreted in urine.
What is the Half-Life of Norepi?
- Half-life 1-2 minutes (e.g. can be titrated quickly IV)
What Blood-Tissue barriers can Norepit cross and not cross?
- Can cross the placenta, but not the blood/brain barrier.
Norepi Toxicity
What physiologic events occur with Norepi Toxicity?
- excessive vasoconstriction in mesenteric vessels
- peripheral arterioles causing ischemia, infarction, and gangrene
- reflex bradycardia
Norepi…
Which drug interactions are a concern?
MAO inhibitors (phenelzine) [use lower doses of norepi] Propranolol [risk of causing hypertension]
Norepi…
What special considerations are there?
- correct volume depletion with IV fluids BEFORE giving NE infusion
- select infusion site carefully—extravasation is a major problem
- monitor patient and BP continuously in ICU setting
- use cautiously in pediatric and geriatric patients
Norepi…
What are indications and dose/route?
- for adults with acute hypotension and shock (related to low SVR)
- infuse 2-12 mcg/min
Norepi…
How should the patient be monitored if given norepi?
BP, HR, infusion site, evidence of extravasation
Epi…
Other names?
Adrenaline
EpiPen
Epi…
Pharmacologic class?
Therapeutic Class?
- pharmacologic class—direct-acting adrenergic agonist
- therapeutic class—vasopressor, cardiac stimulant, bronchodilator, adjunct to local anesthetics, treatment for anaphylaxis
Epi…
What are the pharmacodynamics…
Major actions (3)?
(Comprehensive flashcard)
- major action is to stimulate peripheral alpha-1 adrenoceptors, thereby leading to vasoconstriction (resistance arterioles, increase SVR) and venoconstriction (in capacitance vessels, increase preload)
- beta-1 receptors leading to tachycardia and increased contractility
- beta-2 receptors leading to bronchodilation these actions are also helpful in severe allergic reactions (e.g. anaphylaxis) by stabilizing mast cells
Epi… which receptors?
- major action is to stimulate peripheral ____ adrenoceptors, thereby leading to vasoconstriction (resistance arterioles, increase SVR) and venoconstriction (in capacitance vessels, increase preload)
- ____ receptors leading to tachycardia and increased contractility
- ____ receptors leading to bronchodilation these actions are also helpful in severe allergic reactions (e.g. anaphylaxis) by stabilizing mast cells
Alpha-1
Beta-1
Beta-2
Epi again…
What do Alpha-1 receptors do in peripheral vessels?
What do Beta-1 receptors do to the heart?
What do Beta-2 receptors do to the lungs and to mast cells?
- peripheral alpha-1 adrenoceptors, thereby leading to vasoconstriction (resistance arterioles, increase SVR) and venoconstriction (in capacitance vessels, increase preload)
- beta-1 receptors leading to tachycardia and increased contractility
- beta-2 receptors leading to bronchodilation these actions are also helpful in severe allergic reactions (e.g. anaphylaxis) by stabilizing mast cells
Epi Pharmacokinetics…
What are routes of administration?
What enzyme metabolizes epi?
How are the metabolites excreted?
can be given iv (immediate), IM (variable), SC 5-15 min), inhalation (1-5 min onset), ophthalmic topical
metabolized by COMT and then renally excreted
Epi…
What are syptoms of toxicity?
excessive vasoconstriction, HTN, hemorrhagic stroke, angina, arrhythmias
Epi…
What are special considerations (ie, when is it used)?
- utility with local anesthetics
* drug of choice in severe anaphylactic reactions (along with others)
Epi…
What are indications for use?
Anaphylaxis
Cardiac arrest
Epi... What are the dosages and route of administration for Anaphylaxis? Cardiac Arrest? Infusion of epi?
anaphylaxis, 0.1-0.5 mg SC or IM
cardiac arrest, 1-5 mg IV push
infusion, 1-4 mcg/min