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Sympathomimetic / Adrenergic Drug
Review
55
Medical
Professional
08/11/2011

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Cards

Term
Describe the action of adrenergic drugs
Definition
responses similar to those produced by activation of the sympathetic nervous system and/or its receptors
Term
What are direct action?
Definition
action on specific receptor
Term
Decribe the receptors in direct action
Definition

alpha 1: postsynaptic;  

alpha 2: mostly presynaptic, some postsynaptic;  

beta 1 and/or beta 2: postsynaptic

Term
Describe indirect action on receptors
Definition
effect on all receptors by releasing NE or preventing uptake of NE
Term
Describe mixed action a on receptor
Definition
effects all receptors that includes both direct and indirect actions
Term
What are the catecholamine drugs?
Definition
Norepinephrine (exog.), Epinephrine (exog.), Isoproterenol   Dopamine (exog.), Dobutamine
Term
What does norepinephrine direct on?
Definition
direct on a1 and a2, less on some b1
Term
What does epinephrine direct on?
Definition
direct on a1, a2, b1 and b2
Term
What does Isoproterenol direct on?
Definition
direct on b1 and b2
Term
What does Dopamine direct on?
Definition
direct on a1, b1, b2, and DA receptors (renal vessels)
Term
What does Dobutamine direct on?
Definition
direct b1, other
Term
What are the non-catecholamine drugs?
Definition
Phenylephrine, Tetrahydrozoline, Naphazoline, Oxymetazoline, Ritodrine, Metaproterenol, Albuterol,         Salbutamol, Salmeterol, Formoterol, Terbutaline
Term
What does Phenylephrine direct on?
Definition
a1
Term
What does Tetrahydrozoline direct on?
Definition
a1
Term
What does Naphazoline direct on?
Definition
a1
Term
What does Oxymetazoline direct on?
Definition
a1
Term
What does Ritodrine direct on? 
Definition
b2>b1
Term
What does Metaproterenol direct on?
Definition
 b2 > b1
Term
What does Albuterol direct on?
Definition
 b2 > b1
Term
What does Salbutamol direct on? 
Definition
b2 > b1
Term
What does Salmeterol direct on? 
Definition
b2 > b1
Term
What does Formoterol direct on? 
Definition
b2 > b1
Term
What does Terbutaline direct on? 
Definition
b2 > b1
Term
What does Clonidine direct on? 
Definition
a2
Term
What rec. does Ephedrine, pseudoephedrine have indirect on?
Definition
a & b (increase release)
Term
What rec. does Amphetamine have indirect effect on? 
Definition
a+b (increase release)
Term
What receptor does cocaine have indirect effect on? 
Definition
a+b (decrease uptake)
Term
What rec. does Tyramine have indirect effect on?
Definition
 a+b
Term
What does b2 agonist affect at higher dose?
Definition
b1
Term
How does blood vessel react with a & b agonist?
Definition

low conc. – beta response

high conc.- alpha response

Term
What effect does dopamine have on renal blood vessels?
Definition
Dilation
Term
What is the basic structure of catecholamine?
Definition

Phenylethylamine

greatest activity: 2 C atoms separate from N;         

3,4 HO: highest activity for alpha and beta; no or or poor penetration into CNS

Term
What happens when Phenylethylamine loses 1 or 2 OH?
Definition
decrease in a and b activities but still have indirect action
Term
What happens when Phenylethylamine has no OH?
Definition
BBB penetration
Term
Which isomer type of catecholamine is potent in the periphery?
Definition
L-isomer more potent than d in periphery
Term
Which isomer type of catecholamine is potent in CNS?
Definition
D-isomer more potent than L-isomer
Term
What effect does N-alkylation have on catecholamine?
Definition
Increase in alkyl groups on N results in increase in beta activity
Term
What are catecholamines usually metabolized by?
Definition
Monoamine oxidase 
Term
How are catecholamines introsuced inside patient's body?
Definition
injection, infusion, inhalation, topical; some drugs can deteriorate if solution is exposed to air
Term

True or False

Catecholamines can cross BBB VERY WELL!

Definition
False
Term
How are non-catecholamine introduced in pateint's body?
Definition
slower metabolism via various routes (one through MAO);  injection, oral, inhalation
Term
Which two non-catecholamines can cross BBB? Why?
Definition
Amphetamine and Ephedrine because they don't have OH groups; this produce CNS stimulation
Term
Describe cardiologic response when Epi is injected?
Definition

  1:  b1 - increase in contractility, heart rate 

       a1 - increase in PR (vessel constriction) 

         2:  metabolism, excretion lowers drug levels BP                                                                

       3:  b2 – low dose vasodilation, decrease in PR 

4:  metabolism, excretion eliminates drug

Term
In blood vessel, how does a1 affected PR and BP?
Definition
↑ peripheral resistance – ↑ diastolic pressure
Term
In blood vessel, how does b2 affect PR and BP?
Definition
↓ peripheral resistance - ↓ diastolic pressure
Term
How does b1 receptor affect the heart?
Definition
↑  cardiac output –  ↑ systolic pressure
Term
What is the overall effect on vascular with adrenergic Drug?
Definition
constriction of peripheral blood vessels
Term
What are the application of adrenergic drug in terms of vascular effect?
Definition
Decongest "stuffy" nose during cold, allergy, stop superficial bleeding, with local anesthetics
Term
What is the overall effect on cardiovascular with adrenergic drug?
Definition
vasoconstriction and/or heart stimulation
Term
What are the application for adrenergic drug in terms of cardiovascular?
Definition
Hypotension, Shock, Congestive heart failure, Cardiac arrest
Term
What are the application for adrenergic drug in terms of bronchodilation?
Definition
Asthma, Anaphylaxis
Term
What effect does adrenergic drug have on ocular?
Definition
dilation of pupils, vasoconstriction, lowering of  IOP
Term
What is the application of adrenergic drug in terms of ocular effect?
Definition
Eye examination, Blanching, irritation, Glaucoma
Term
What is the application of adrenergic effects on uterus?
Definition
Reduction of premature contractions
Term

What is the application of adrenergic drug on CNS?

Definition
Narcolepsy, Obesity, Attention Deficit Syndrome
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