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Sympathomimetics
PHAR340
24
Pharmacology
Undergraduate 3
12/06/2012

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Cards

Term
N-alkyl group
Definition
β activity
Term
β hydroxyl
Definition
Polar, decreased CNS activity
Term
Catechol OH
Definition
Metabolism by catechol-O-methyl transferase (-OH → -OCH3)
Term
ɑ carbon bulky group
Definition
No metabolism by monoamine oxidase (-NH → -N-OH)
Term
Epinephrine
Structure?
Definition
N-alkyl group: β activity
β hydroxyl: polar, decreased CNS activity
Catechol OH: metabolism by catechol-O-methyl transferase (-OH → -OCH3)
Metabolism by monoamine oxidase (-NH → -N-OH)
No steric hindrance by ɑ carbon bulky group
Term
Epinephrine
Low dose?
Definition
β2 dilation
Term
Epinephrine
High dose?
Definition
ɑ1 constriction
Term
Epinephrine
Blood pressure tracing
Definition
Increase (β1)
Decrease (β2)
Increase (ɑ1)
Term
Epinephrine
Anti-asthmatic effect?
Definition
Vasoconstriction and bronchiolar dilation to relieve anaphylactic shock
Term
Epinephrine
Metabolism? Administration?
Definition
Rapidly metabolized in liver
Intravenous injection usually
Term
Ephedrine
Adrenergic activity? Structure?
Definition
ɑβ
No catechol –OH groups
No CMT metabolism
β-OH and ɑ-CH3
Decreased CNS activity, no MAO metabolism
Longer acting
Release of NE at adrenergic receptors
Term
Methamphetamine
Structure?
Definition
No catechol –OH groups
No CMT metabolism
ɑ-CH3
No MAO metabolism
No β-OH
Lipophilic, CNS activity
Term
Ergot
Definition
Uterine contractions via ɑ receptors
Premature labour
Term
Norepinephrine
Adrenergic activity?
Definition
(ɑ, β1)
No β2 activity
Smooth muscle constriction & increase in B.P.
Term
Norepinephrine
Blood pressure tracing?
Definition
Increase
Smooth muscle constriction & increase in B.P.
Term
Isopropyl norepinephrine (INE)
Definition
β1, β2
No ɑ activity
Term
Isopropyl norepinephrine (INE)
Blood pressure tracing?
Definition
Acute increase in B.P. via β1
Decrease in B.P. via β2
Term
Phenylephrine
Activity?
Definition
ɑ1 only
Increase
Term
Dopamine
Adrenergic activity?
Definition
β1
Acts on dopamine and beta receptor
Increase in B.P. via activation of RAAS
Term
Salbutamol
Adrenergic activity?
Definition
β2
Bronchiolar relaxation to treat asthma
Usually inhaled
Term
Tyramine
Definition
Tyrosine → tyramine via decarboxylation
Release NE into synaptic cleft
Constriction of blood vessels within skull
Term
Amphetamine
Adrenergic activity? Structure? Adverse Effects?
Definition
Release NE from storage sites
ɑ and β1 actions
Peripheral and CNS effect, no β-OH group
Lack of polarity → lipid soluble
Prevent sleep, reduce appetite
Sympathetic stimulation in CNS
Impact on growth
Term
Cocaine
Adrenergic activity? Adverse effects?
Definition
Inhibits reuptake of NE
Increases potency of NE peripherally and centrally
Left-shift in dose/response curve
Vasoconstriction → heart attack
Term
Methylphenidate
Definition
CNS stimulant
Less impact on growth than amphetamine
ADHD
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