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Sympatholytics
PHAR340
15
Pharmacology
Undergraduate 3
12/06/2012

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Cards

Term
ɑ-methylparatyrosine
Definition
NE synthesis inhibitor
Term
Bretylium
Definition
NE release inhibitor
Term
Reserpine
Definition
NE depletion
Term
Prazosin
Definition
ɑ1 antagonist
Term
Phentolamine
Adrenergic activity? Blood pressure tracing before and after epinephrine?
Definition
ɑ1, ɑ2 antagonist
Blood pressure tracing: phentolamine
Vasodilation, decrease in B.P.
Blocks constriction by ɑ receptors maintained by E
Blood pressure tracing: epinephrine, phentolamine
Initial rise (?), decrease in blood pressure
Treatment for hypertension by vasodilation
Term

Phentolamine

Adverse effects?

Definition
Orthohypotension Increased GI motility Nasal stuffiness
Term
Propanolol
Adrenergic effects?
Definition
Decrease in contractile force and heart rate
β1
Increase in blood pressure retained after epinephrine administration
ɑ1 vasoconstriction
Term
Propanolol
ADME?
Definition
β1, β2 antagonist
Highly susceptible to first pass effect, t1/2 = 4 hrs
Lipid soluble, plasma protein bound
Eliminated by hepatic metabolism
Term
Propanolol
Treatment?
Definition
Hypertension by decreased heart rate and contractility and renin release
Arrhythmias, when used in combo with a vasodilator
Ischemic heart disease
Term
Propanolol
Effects?
Definition
Bronchoconstriction (β2 receptor block)
Congestive heart failure
Bradycardia
Rebound hypertension
Term
Metoprolol
Definition
β1 antagonist
Cardiac effect only
Term
Pindolol
Definition
Partial β antagonist
Lesser bronchoconstriction
Less rebound hypertension
Less bradycardia
Term
Nadolol
Definition
Renal elimination
t1/2 = 14-24 hrs
Term
Esmolol
Definition
β1 antagonist
t1/2 = 10 mins
Term
ɑ-methylparatyrosine
Definition
NE synthesis inhibitor (competitive)
Tyrosine hydroxylase
Tyr → DOPA → dopamine → NE
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