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16 Cards in this Set

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  • Back
  • 3rd side (hint)
What is the receptor affinity for NE? Tx?
NE: mixed ∂ß: ∂1=∂2, ß1>ß2… Tx: endogenous NT…
What is the receptor affinity for Epinephrine? Action? Tx?
(1) mixed ∂ß agonist: ∂1=∂2, ß1=ß2…

(2) Action:
(a) ß1: increase --> inotrope, and chronotrope --> increase in BP…

(b) ∂: vasoconstriction of capilary beds… ß2: skeletal muscle vessel dilation --> may cause fall in TPR --> fall in Diastolic pressure (leads to increased blood flow during exercise)

(c) dose dependent:
High dose: shows increase in BP, due to ∂1 effect on vasoconstriction and ß1ß2 effect on inotropy and chronotropy.

Low Dose: show decrease in BP because ß2 have a lower threshold than ∂1, thus it cause vasodilation at skeletal muscle BV.

(3) Tx: (endogenous NT) restore cardiac rhythms after arrest (heart block), AV block, cardiac arrest, relieve hypersensitivity (anaphylaxis
What is the receptor affinity for Isoproterenol? Action? Tx?
(1) Affinity: Selective ß agonist: ß>>>∂…

(2) Action:
(a) ß1: +inotrope, +chronotrope… --> --> increase in CO... small increase in SV

(b) ß2: potent vasodilator -->decrease DBP, lesser decrease in SBP, decrease MAP…

(3) Tx: bradycardia, heart block, cardiac arrest, cardiogenic shock where blood flow/pressure is low), bronchospams caused by anesthesia

TAKE HOME: Increases heart function w/DECREASE in BP
What is the receptor affinity for Dobutamine? Action? Tx? (hint?)
(1) Affinity: Partial Agonist: Selective ß1 agonist: ß1>ß2>>>∂… [+isomer is a ∂1-antagonis and -isomer is an ∂1-agonist] …

(2) Action:
(a) ß1 --> Increases inotrope, and chronotrope --> increase in CO.

(b) No ß2 --> so no skel mus dilation and no reflexive tachycardia.

(c) Since dobutamine does not bind dopamine receptors --> no ∂ adrenergic response --> less likely to cause an increase in BP

(3) Tx: short term treatment for cardiac decompensation and CHF (short term because of intolerance of direct acting catacholamine = poor outcome in heart patients)
Hint: "Doh!"
What is the half-life and tolerance consideration for Dobutamine?
Dobutamine has a short half life and tolerance can develop.
What is the receptor affinity for Phenylephrine? Action? Tx? Contraindication?
(1) Affinity: Poor selective ∂1 agonist (∂1>∂2>>>>>ß…

(2) Action: ∂ effects…

(3) Tx: mydratic (dilates pupils), decongestant, raises blood pressure

(4) Narrow angle Glaucoma is a contraindication... NOTE: ∂2 leads to decreasing aqueous production and increasing uveo-scleral outflow... HOWEVER, Phenylephrine is primarily ∂1
Is Phenylephrine a catacholamine? What is the significance of this?
Phenylephrine is not a catacholamine, thus it is not metabolized by COMT --> leading to an increase in half-life
What is the receptor affinity for Ephedrine? Action? Tx?
Ephedrine: (1) Affinity: Weak Mixed ∂ß agonist -->

(2) Action:
(a) Direct:
- ß1ß2 --> inotropy, + chronotropy, w/ increased in BP

- ∂ --> vasoconstriction --> increase in BP

(b) Indirect: displaces NE from vesicles --> so it sort of acts like an amphetamine.

(3) Tx: decongestant, bronchiodilator (ß2), urinary incontinance, weight loss
(1) What are the ADR for Ephedrine?…
(2) Where is Ephedrine derived…
(3) what is Ephedrine used to make?…
(4) why does Ephedrine have a long half life?
(1) arrythmias, increased HR&BP, death… don't use if involved in strenuous exercise or hx of heart disease or HTN…
(2) Chinese Ma Huang…
(3) "Meth"…
(4) non-catacholamine --> long half-life.
What is Pseudoephedrine? What is it used for?
Pseudoephedrine is an enantiomer of Ephedrine… used as a decongestant… it's also used to make "meth"
What is the receptor affinity for Dopamine? Action? Tx?
"Dopamine: (1) Affinity: D1=D2>>ß>>∂…

(2) Action:
D1--> vascular beds in Renal, mesenteric, coronary vascular beds --> Dilation

D2 --> suppresses NE release (by decreasing adenylate cyclase --> decreasing Ca+ influx --> NE efflux is decreased)

ß1 --> receptors in heart --> + inotrope and chronotrope.

Dose Dep:
Low Dose: → ↓ TPP
High Dose: → ↑ BP due to activation of ∂ receptors (similar to Epinephrine:

(3) Tx: CHF, cardogenic, septic shock
Is Dopamine metabolized by MAO and COMT?

What are the ADR for Dopamine?
Dopamine is metabolized by COMT and MAO…

ADR: Dopamine causes excess sympathetic activity
(1)What is the mechanism of action for Amphetamine?

(2) What are Amphetamines used for?

(3) Are Amphetamines catacholamines?
(1) Mechanism: Indirect adrenergic agonist --> releases catacholamines…

(2) Amphetamines are used in CNS stimulant abuse, enter the brain, elevates mood, and is an appetite suppressant…

(3) Amphetamines are not catacholamines
What is the receptor affinity for Clonidine? Action? Tx? ADR?
(1) Affinity: Selective ∂2 direct agonist…

(2) Action: decreases sympathetic outflow from the CNS, by fooling the brain into thinking there are excess catacholamines…

(3) Tx: HTN

(4) ADR: if Clonidine is removed suddenly it can cause rebound hypertension
What is the receptor affinity for Terbutaline? Action? Tx?
Terbutaline: (1) Affinity: Selective ß2 agonist… (2) Action: bronchodilation w/o tachycardia… (3) Tx: Asthma
What is Tyramine's mechanism of action? Tx? Is Tyramine metabolized by MAO? What effect do aged cheeses or fermented foods have on Tyramine?
(1) Tyramine's mech of action is it causes the relase of NE, thus it is an indirect sympathomimetic… (2) Tx: ? … (3) Yes, thus MAOI's (as well as aged cheeses or fermented foods) can increase Tyramine's availability --> increase in BP