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16 Cards in this Set
- Front
- Back
- 3rd side (hint)
What is the receptor affinity for NE? Tx?
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NE: mixed ∂ß: ∂1=∂2, ß1>ß2… Tx: endogenous NT…
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What is the receptor affinity for Epinephrine? Action? Tx?
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Epinephrine:
(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 |
None
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What is the receptor affinity for Isoproterenol? Action? Tx?
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Isoproterenol
(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 |
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What is the receptor affinity for Dobutamine? Action? Tx? (hint?)
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Dobutamine:
(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!"
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What is the half-life and tolerance consideration for Dobutamine?
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Dobutamine has a short half life and tolerance can develop.
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What is the receptor affinity for Phenylephrine? Action? Tx? Contraindication?
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Phenylephrine:
(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 |
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Is Phenylephrine a catacholamine? What is the significance of this?
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Phenylephrine is not a catacholamine, thus it is not metabolized by COMT --> leading to an increase in half-life
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What is the receptor affinity for Ephedrine? Action? Tx?
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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 |
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Ephedrine:
(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. |
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What is Pseudoephedrine? What is it used for?
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Pseudoephedrine is an enantiomer of Ephedrine… used as a decongestant… it's also used to make "meth"
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What is the receptor affinity for Dopamine? Action? Tx?
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"Dopamine: (1) Affinity: D1=D2>>ß>>∂…
(2) Action: Direct: 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 |
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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 |
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(1)What is the mechanism of action for Amphetamine?
(2) What are Amphetamines used for? (3) Are Amphetamines catacholamines? |
Amphetamines:
(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 |
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What is the receptor affinity for Clonidine? Action? Tx? ADR?
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Clonidine:
(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 |
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What is the receptor affinity for Terbutaline? Action? Tx?
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Terbutaline: (1) Affinity: Selective ß2 agonist… (2) Action: bronchodilation w/o tachycardia… (3) Tx: Asthma
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What is Tyramine's mechanism of action? Tx? Is Tyramine metabolized by MAO? What effect do aged cheeses or fermented foods have on Tyramine?
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(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
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