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Pharmacology 1 > Section 2b Adrenergic Agonists > Flashcards

Section 2b Adrenergic Agonists Flashcards

1
Q

what amino acid is DOPA made from?

A

Tyrosine

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2
Q

What part of the catecholamine biosynthesis happens in the cytoplasm?

A

Tyrosine –> DOPA –> Dopamine

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3
Q

Where does the majority (~90%) of catecholamines (NE) come from?

A

Presynaptic (re)uptake via NET

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4
Q

what blocks catecholamine synthesis?

A

methyltyrosine

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5
Q

what blocks catecholamine storage?

A

reserpine via VMAT - release empty vesicles

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6
Q

what increases catecholamine release?

A

tyramine, amphetamine (indirect action)

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7
Q

what blocks catechol. release?

A

guanethidine

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8
Q

what blocks chatechol. (re) uptake presynaptically?

A

cocaine, tricyclic antidepressants via NET (indirect action)

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9
Q

what blocks chatechol. metabolism?

A

MAO inhibitors

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10
Q

Where are VMAT 1 and 2 found?

A 
1 = peripheral
2 = CNS
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11
Q

What is a NET selective blocker?

A

Atomoxetine - treatment of ADHD

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12
Q

what has a mixed (direct and indirect) adrenergic agonist action?

A

ephedrine

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13
Q

What is the preference of Epi vs NE for B1 and B2?

A

B1 - Epi=NE

B2 - Epi>NE

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14
Q

What is the preference of Epi, NE, and Iso for a receptor?

A

Epi > NE > Iso

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15
Q

What is the preference of Epi, NE, and Iso for B receptor?

A

Iso > Epi > NE

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16
Q

What is the receptor preference for phenylephrine?

A

a1 > a2&raquo_space;> B

17
Q

What is the receptor preference for Clonidine?

A

a2 > a1&raquo_space;> B

18
Q

What is the receptor preference for NE and Epi?

A

NE: a1 = a2; B1&raquo_space; B2
Epi: a1 = a2; B1 = B2

19
Q

What is the receptor preference for Dobutamine? Isoproterenol? Terbutaline/Albuterol?

A

Dobutamine: B1 > B2&raquo_space; a
Isoproterenol: B1 = B2&raquo_space;a
Terbutaline/Albuterol: B2&raquo_space;> B1&raquo_space;» a

20
Q

What is the receptor preference for Fenoldopam?

A

D1&raquo_space;> D2

21
Q

What are the 4 major effects (in tissues) that a1 do?

A
  1. vascular smooth muscle = vasoconstriction (increased blood pressure)
  2. Pupillary dilator (radial) = contraction (pupil dilation)
  3. Urinary bladder (sphincter) = contraction
  4. Prostate = contraction
22
Q

What are the 2 major effects (in tissues) that a2 do?

A
  1. adrenergic nerve terminals = inhibit transmitter release

2. pancreatic = decrease insulin secretion

23
Q

What are the 2 major effects (in tissues) that B1 do?

A
  1. heart = increase rate and force of contraction

2. renal jux. cells = increase renin secretion

24
Q

What are the 6 major effects (in tissues) that B2 do?

A
  1. respiratory smooth muscle = bronchodilation
  2. uterine smooth muscle = relaxation (prego)
  3. vascular skeletal muscle = vasodilation
  4. urinary bladder (detrusor wall) = relaxation
  5. liver = glycogenolysis, gluconeogenesis
  6. pancreas = increase insulin secretion
25
Q

Major effects (in tissues) that B3 does?

A

adipose tissue = lipolysis

26
Q

What senses high blood pressure and responds with an increase in vagal tone which decreases heart rate? where is it located and how does it work?

A

baroreflex sensors/mechanism in the neck – it is fast acting with the release of ACh in the sinoatrial node which decreases BP

27
Q

what do NE, Isoproterenol, and Epi do to systolic pressure?

and of these 3 which decreases pulse rate?

A

Epi = decreases it
NE = increases it (decrease pulse rate)
Isoproterenol IV = markedly decreases it

28
Q

What are adrenergic receptors and effects in teh respiratory tract? (2)

A
  1. bronchodilation (B2)

2. decongestant (a1)

29
Q

What are the adrenergic receptors and effects in the genitourinary tract? (3)

A
  1. urinary continence (a1A, B2)
  2. ejaculation (a1)
  3. uterine relaxation in pregnant women near term (B2)
30
Q

What are the adrenergic receptors and effects in the eye? (3)

A
  1. mydriasis (dilation) (a)
  2. increased outflow of aqueous humor (a)
  3. decreased production of aqueous humor (B antagonists)
31
Q

What do B’s increase? (3)

A

lipolysis, insulin secretion, and renin secretion

32
Q

What do a2 decrease? (3)

A

lipolysis, insulin secretion, and renin secretion

Pharmacology 1 (10 decks)

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