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Chapter 5 of TH IUSM Pharmacology Notes
35
Pharmacology
Professional
09/13/2010

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Term
Clonidine
Definition
Antihypertensive
Stimulates Adrenergic receptors in the CNS
Lowers SNS tone--decreases BP
likely stimulates inhibitory center
Term
Sweat Gland SNS Postganglion Signal
Definition
Acetylcholine
Term
What stimulates dilation of skeletal muscle vasculature?
Definition
Beta 2 receptors from circulating epinephrine
Term
Pathway from Tyrosine to Epinephrine
Definition
Tyrosine-->DOPA-->Dopamine-->NE-->Epinephrine
Term
What is the RLS of EPI synthesis from Tyrosine?
Definition
Tyrosine-->DOPA via dopamine hydroxylase
Term
Metyrosine
Definition
Competitive inhibitor of tyrosine hydroxylase
Treats pheochromacytoma (catecholamine producing tumor of the adrenal medulla)
Term
Dopa Decarboxylase
Definition
Enzyme catalyzing conversion of DOPA to Dopamine
Aromatic AA decarboxylase enzyme
Term
Dopamine-Beta-Hydroxylase
Definition
Enzyme for Dopamine to Norepinephrine conversion
Term
Phenylethanolamine-N-methyltransferase
Definition
Converts NE to EPI
In Adrenal Medulla
Term
False Transmitter
Definition
A compound that enters presynaptic storage vesicles and replaces the normal neurotransmitter.
Term
2 druges which interferewith storage and release of norepinephrine release from nerve terminals
Definition
Guanethidine and Reserpine
Term
Guanethidine's effect on BP
Definition
Initially short term increase (Not seen clinically, however, because it only occurs via IV bolus, and that's not done with Guanethidine)
Then long term decrease
Term
Guanethidine Side Effects: (5)
Definition
Orthostatic Hypotension
Excessive GI stim (unopposed PSNS)
Inhibition of Ejaculation
Pheochromocytoma especially sensitive
No CNS effect (can't cross BBB because too polar)
Term
Reserpine
Definition
Decreases Blood Pressure via inhibition of ATP dependent NE/Dopamine uptake carrier in vesicles
NE can't get into the vesicles--not displaced, it just runs out
Term
Is Reserpine Lipid or Water soluble? Side effects? (4)
Definition
Lipid soluble--enters CNS:
Sedation
Lethargy
Nightmares
Depression
Term
How does cocaine function to stop adrenergic nerve terminals?
Definition
It blocks reuptake of NE into presynaptic terminal.
Term
How do Tricyclic Antidepressants (TCAs) work?
Definition
It blocks reuptake of NE into presynaptic terminal.
Term
What is the primary mechanism of termination of the adrenergic signal?
Definition
Reuptake of catecholamines by the presynaptic nerve terminal.
Term
MAO MonoAmine Oxidase
Definition
Enzyme that metabolizes catecholamines after uptake.
Mitochondrial enzyme that is widely distributed in body tissues.
Term
COMT Catechol-O-methyltransferase
Definition
Widely distributed Cytoplasmic enzyme. High concentrations in kidney and liver.
Term
Dopamine's metabolite in urine
Definition
homovanillic acid
Term
Epi and NE urinary metabolites
Definition
3-methoxy-4-hydroxyphenylglycol (MHPG) and
3-methoxy-4-hydroxy-mandelic acid (VMA)
Term
Wine and Cheese Syndrome
Definition
From use of MAO inhibitors
from foods high in tyramine
tyramine is normally broken down by MAO, but with the inhibitor present, it can't be broken, down, so the tyramine acts as a sympathomimetic. 15-20 documented deaths.
Term
Alpha receptors
Definition
EPI>NE>>ISO
Vasoconstriction
Contraction of Uterus
Contraction of Nictitating Membrane
Pupillary Dilation
GI Inhibition
Term
Beta Receptors--order of epinephrine, NE, and ISO strengths
Definition
ISO>EPI>NE
Term
Beta-1 actions
Definition
Cardiac Stimulation
Renin Secretion by JG cells. NE, EPI and ISO all utilized.
Term
Beta-2 Receptor actions
Definition
Vascular Dilation
Bronchiolar Relaxation
Iso and Epi: NO NE!
Term
Beta-phenylethylamine
Definition
Parent compound from which sympathomimetic drugs are derived
Term
Oxymetazoline
Definition
Direct alpha sympathomimetic
Term
Phenylephrine
Definition
Direct alpha sympathomimetic
Term
Methoxamine
Definition
Direct alpha sympathomimetic
Term
Dobutamine
Definition
Beta-1 Agonist
Term
Metaproterenol
Definition
Beta 2 agonist (bronchodilator)
Term
Terbutaline
Definition
Beta 2 agonist (bronchodilator)
Term
Salbutamol/Albuterol
Definition
Beta 2 agonist (bronchodilator)
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