I. Vasopresser & Inotropes Flashcards
(84 cards)
_____ & ____ were the first vasopressors synthesized.
Dopamine & Vaspopressin
Most sympathomimetics are derived from the parent compound ____.
Beta-Phenylethylalamine
Catecholamine have a hydroxyl substitution on the ____.
Benzene ring
The most basic catecholamine ____, is the precursor for both NE & Epi.
Dopamine
A lack of N-substitution indicates a lack of ____. However, bulky side chains indicates the opposite.
Beta activity
No N-substitution: Phenylephrine and NE = No Beta
Side-Chains: Isoproterenol & Dobutamine = Beta
End result of inotropes is to:
Positively influence the interaction (influx) of Calcium with actin and myosin in the cardiac myocyte
Beta 1 receptor MOA IOT increase INOTROPY:
- Gs membrane protein activated
- Activates Adenylyl Cyclase
- Activates cAMP
- Activates Protein Kinase A
- Increases probability Calcium channels open
- Calcium leaves SR & enters mycocardial/muscle cell
- Increased force of contraction (inotropy) & speed of contraction (chronotropy)
The vasodilation from PDEI is due to ____ .
.cAMP promoting vascular smooth muscle relaxation
reflex VD to accommodate increase in HR - per Weirich
*PDEI inhibit the breakdown of cAMP by PDE3. Increased cAMP enhances Calcium release from the SR and increases the force generated by actin-myosin.
Digoxin increases ____ by inhibiting ____.
- cytosolic Calcium
-Na/K ATPase on the cell membrane
Most vasopressors exert their effects via ____ receptors.
Alpha 1
What is common vasopressor that does not work on alpha 1?
Vasopressin (VA receptors)
All vasopressor drugs work by what MOA:
- Gq cell membrane activated
- Activates Phospholipase C
- Hydrolyzes PIP2 to IP3 & DAG
- IP3 increases Calcium release from SR & DAG activates Protein Kinase C to increase Calcium influx
- More calcium influx leads to increase in vascular smooth muscle tone
What does Phospholipase C do?
Hydrolyzes PIP2 to IP3 & DAG
What does IP3 do?
Increases Calcium release from SR
What does DAG do?
Activates protein kinase c to increase Calcium influx
What does protein kinase c do
Increases calcium influx
Generally vasopressors & intropes have a short/long half-life.
Short
T/F: Generally vasopressors/inotropes are rapidly metabolized.
True
usually run as infusions/titrated
Two compounds that metabolize (by methylation) catecholamines:
- COMT
- MOA
Epinephrine is secreted by
Adrenal medulla
Epinephrine Clinical uses
Epi clinical considerations (causes):
- Cardio: Increase BP, HR, CO, PP, MAP
- CNS: Increase CBF
- Resp: Bronchodilation
- Other: Hyperglycemia, Hyperlipidemia, Arrhythmias, Increase CMRO2
Catecholamines are broken down into:
Sugars (hyperglycemia)
Epinephrine concentration & dosing
1 mg/cc Epi hydrochloride
100 mcg/cc cardiac Epi
500 mcg auto-injector (Epi Pen)
ACLS: 1 mg IVP
HR/BP IVP: 10 mcg
Anaphylaxis: 0.3-1mg
Infusion: 0.05 - 0.2 mcg/kg/min