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General Functions of Metyrosine
Interfere with the synthesis of of adrenergic stimulents
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Blockade of uptake 1 at nerve terminal
Cocaine and Imipramine
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Blockage of storage in granule or granular uptake.
why dont we use this anymore?
- Reserpine
- decreases dopamine levels too low so that depressive effects occurs.
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Promotion of NE release.
Amphetamine and Ephedrine
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Prevention of Release of NE.
Bretylium, Guanethidine
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Where is MAO-A located?
What does it do?
What inhibits it?
Located in the Nerves/ intestines/ liver (really anywhere)
Metabolizes NE, 5-HT, Dopamine and tyramine
Inhibitors are: Phenelzine, and Tranylcypromine
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What is the Cheese reaction?
It is Caused when someone is on a MAO-A inhibitor and eating cheese (which has Tyramine in it). Tyrimine isn't brocken down--> tyrimine releases NE--> causes Severe hypertension.
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Where is MAO-B located?
What does it do?
What inhibits it?
Located in the Brain
Metabolizes Dopamine, NE, and serotonin.
Inhibited by: Selegiline, Rasagiline
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What are some COMT inhibitors?
Tolcapone, Entacapone
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What dont you give dopamine in the treatment of Parkasons?
What should you do?
Problem is there is not enough Dopamine, if you give dopamine, it is water soluble--> so it will not beable to cross the BBB--> it just creates systemic effects.
Should give a MAO-B inhibitor--> increase the activity of Dopamine.
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Agonist acting on Alpha 1 receptors
Phenylephrine, Mephenteramine, Methoxamine
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Agonist acting on Alpha 2 receptors.
Clonidine, Alpha Methyldopa
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Agonist acting on Beta 1 and 2 receptors
Isoproterenol
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Agonist acting on Beta 1 receptor
Dobutamine
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Agonist acting on Beta 2
Terbutaline, Albuterol, Ritodrine, Metaproterenol
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Dopamine 1 receptor agaonist
Fenoldopam
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What receptors does Epi act on?
What are its actions on CVS? and what receptor is that?
Acts on all adrenergic receptors.
- Beta 1 receptor.
- Incresases Contraction force
- Increases heart rate
- Increases conductions through AV node
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What is Epis Effect on Vascular Blood Vessels?
Constriction--> increasing BP High Dose--Alpha 2
- Dilation of Vessels of skeletal Muscle--> decreasing BP
- low dose --- Beta 2 (more sensative)
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Epinephrine in low doses on Beta 1
on Beta 2
----Increases HR, SV, CO, and Pulse Pressure
---- Decreases Peripheral Resistance, BP
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How do you calculate the Mean Arterial Pressure?
2/3 diastolic, and 1/3 systolic pressures
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what is the effect of Medium dose of Epi?
Slight increase in Mean arterial Pressure because Alpha 2s are activated (increase in TPR and BP)
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What is the Effect of High does of Epi?
Increase in HR, MAP, --> reflex --> bradycardia
Activation of Alpha 1 receptors ( increase TPR and BP).
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What happens when you give Epi before Alpha Blackade and After?
What does this Occur?
Before--- Increase in BP
After----- Decreases BP
Because all the Alpha Receptors are blocked and only Beta 2 receptors are active.
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What is Epis effects on Smooth Muscle?
GIT-- Peristalsis is reduced and sphinctors are consticted
Bladder-- Trigone and sphincter is contracted
Uterus-- Relaxation at term
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Epi Effects on the Eye. What receptors?
Causes Mydriasis (radial Muscle Constiction) but do NOT effect accomadation. (Alpha 1)
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Epi effects on Metabolic Actions?
1.Activation of Beta 2 receptors result in uptake of K into the cells--> may lead to hypokalemia
2.Renin increased by Epi (Beta 1)
3. Produces Glycogenolysis and lipolysis
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Locations of:
B1
B2
B3
D1
D2
- -Heart
- -Resp, Uterine, Vascular Smooth m, Skeletal m, Liver
- - Fat cells
- -smooth muscle
- - Nerve endings
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What is the effect of Alpha 2 receptors being activated in the Pancreas?
Inhibits insulin release.
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What is Fenoldopam
when is it used?
a dopamine agonist
used for Emergency Hypertension.
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What is Dobutamine?
When do you used it?
Why use it instead of dopamine?
Similar to dopamine, except it does not act on D1 and 2 receptors. It is predominantly a Beta 1 receptor.
Used in Heart failure and cardiac shock-- Increases force of contraction, but NOT heart rate.
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What is Ephedrine?
What does it act on?
Is it effective orally? Why or Why not?
When is it used?
it is a mixed Adrenergic agonist.
- Acts Directly on A and B receptors
- acts Indirectly by releasing NE.
Effective Orally-- resistant to MAO (not broken down).
Used in Bronchial asthma and hypertension.
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What is Amphetamine?
Is it orally active?
What are its effects?
When do you used it?
- it is an Indirectly acting adrenergic agonist.
- Orally active-- Resistant to MAO and COMT
Causes Alertness, increased concentration (CNS action)
Used in ADHD and Narcolepsy.
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