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Pharmacology > Drugs Affecting Adrenergic Neurotransmission > Flashcards

Drugs Affecting Adrenergic Neurotransmission Flashcards

1
Q

General actions of sympathetic stimulation

A

increased rate + force of heart contraction, blood pressure, and blood glucose levels
shift of blood flow to skeletal muscles
dilation of bronchioles and pupils

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2
Q

Where is norepinephrine made?

A

within adrenergic neurons near the terminus of the axon near the junction with the effector cell

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3
Q

Where is epinephrine made?

A

the adrenal medulla

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4
Q

Which amino acid does epinephrine come from?

A

tyrosine

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5
Q

Alpha 1A receptor

A

causes contraction of smooth muscle, promotes cardiac growth and structure, vasoconstriction of large resistant arterials in skeletal muscle

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6
Q

Alpha 1 B receptor

A

promotes cardiac growth and structure

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7
Q

Alpha 1 C receptor

A

causes vasoconstriction in aorta and coronary artery

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8
Q

Alpha 2A receptor

A

predominant inhibitory receptor on sympathetic neurons
vasoconstriction of small procapillary vessels in skeletal muscle

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9
Q

Alpha 2B receptor

A

predominant receptor mediating alpha 2 vasoconstriction

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10
Q

Alpha 2c receptor

A

predominant receptor modulating dopamine neurotransmission
predominant receptor inhibiting hormone release from the adrenal medulla

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11
Q

Beta 1 receptor

A

predominant receptor in heart producing positive inotropic and chronotropic effects

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12
Q

Beta 2 receptors

A

predominant receptor in smooth muscle relaxation
skeletal muscle hypertrophy

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13
Q

beta 3 receptor

A

predominant receptor producing metabolic effects

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14
Q

How many transmembrane domains do adrenergic receptors have?

A

7

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15
Q

Which G protein are beta receptors coupled to ?

A

Gs

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16
Q

Which G protein is the alpha 2 receptor coupled to?

A

Gi

17
Q

Which G protein is the alpha 1 receptor coupled to?

A

Gq

18
Q

Direct acting agonists

A

norepinephrine
tetrahydrozoline
clonidine
dobutamine
albuterol

19
Q

indirect acting agonists

A

increase the availability of norepinephrine or epinephrine to stimulate adrenergic receptors

20
Q

Mixed Acting Agonists

A

indirectly release norepinephrine and also directly activate adrenergic receptors

21
Q

A nitro group will deactivate the catechol which inhibits ?

A

COMT

22
Q

Catechols are not recognized by ?

A

MAO

23
Q

COMT inhibitors

A

treatment for parkinson’s
prolong half life of levodopa

24
Q

MAO inhibitors

A

second line treatment for depression
may cause hypertensive crisis
increased norepinephrine leads to increased vasoconstriction

25
Q

Phenylethanolamines

A

direct/mixed/indirect agonists
primary/secondary aliphatic amine separated by 2 carbon atoms from a benzene ring
a secondary hydroxyl group at the benzylic carbon
primarily ionized at physiological pH
pKa 9-11

26
Q

What is significant about the N-CH3 on epinephrine?

A

it maximizes activity

27
Q

For phenylethanolamines what happens as you increase the size of the N group

A

greatly decrease alpha activity due to differences in the binding pockets

28
Q

What happens when you remove the 4’ OH on a phenylethanolamine

A

activity at the alpha receptor is reduced and almost eliminated at the beta receptors

29
Q

Why does ephedrine have a greater duration of action than epinephrine?

A

no catechol, therefore no COMT metabolism
alpha-CH3 means steric hindrance ands blockage from MAO

30
Q

Why does pseudoephedrine primarily act as an indirect mechanism?

A

has the wrong stereochemistry at OH group, overall too many changes for a direct mechanism

31
Q

Ephedrine, pseudoephedrine and phenylephrine are commonly used as ?

A

Decongestants

32
Q

What are the major therapeutic indications of selective alpha one receptor agonists?

A

nasal congestion
allergic and viral conjunctivitis
allergic/vasomotor rhinitis
conjunctival hypermedia
corneal abrasion
vernal keratoconjunctivitis
vasoconstriction

33
Q

Which receptor accommodates a more diverse assortment of structural changes?

A

alpha 1

34
Q

Oxymetazoline, Naphazoline, and Tetrahydrozoline are all available as ?

A

nasal sprays and ophthalmic solutions

Pharmacology (16 decks)

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