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Therapeutics > Lecture 6: Adrenergic Agonsists > Flashcards

Lecture 6: Adrenergic Agonsists Flashcards

1
Q

monoamines

A

-contain one amino group connected to aromactic ring by two-carbon chain
-serotonin, dopamine, norepinephrine, epinephrine, (histamine)

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2
Q

Catecholamines

A

-monoamines with catechol group (benzene with 2 hydroxyl groups)
-dopamine, norepinephrine, epinephrine

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3
Q

derivatives of trytophan

A

-serotonin

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4
Q

Derivatives of tyrosine

A

-norepinephrine
-epinephrine
-dopamine

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5
Q

NE transmission

A
  1. tyrosine transported to noradrenergic ending by sodium-dependent carrier
  2. tyrosine to dopamine
  3. Dopamine transported to vesicle by VMAT
  4. dopamine to NE
  5. release NE when action potential opens Ca+ channels and fusion of vesicle with surface membrane
  6. NE binds adrenergic receptors on postsynaptic cell
  7. NE binds to regulatory receptors present on presynaptic terminal
  8. NE diffuses
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6
Q

Tyrosine to dopamine

A
  1. tyrosine to dopa by tyrosine hydroxylase
  2. dopa to dopamine by dopa decarboxylase
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7
Q

VMAT

A

-vesicular monoamine transporter
-transport NE and dopamine

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8
Q

dopamine-B-hydroxylase

A

-dopamine to NE
-happens in vesicle

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9
Q

NE diffusion from synapse

A

-out of cleft
-reuptaken into cytoplasm by NET (NE transporter) where it is metabolized by MAO or taken back to vesicles by VMAT
-can also be degraded by COMT

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10
Q

monoamine oxidase (MAO)

A

-metabolizes NE in cytoplasm

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11
Q

COMT

A

-catechol-O-methyltransferase
-degrade NE released from synapse

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12
Q

Biosynthesis of Catecholamines

A
  1. L tyrosine (hydroxylase)
  2. L-Dopa (decarboxylase)
  3. Dopamine (hydroxylase in vesicle)
  4. NE (PNM in adrenal medulla)
  5. Epinephrine
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13
Q

Metyrosine

A

-can inhibit L-tyrosine to L-Dopa step

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14
Q

Carbidopa

A

-can inhibit L-dopa to dopamine step
-parkinson’s disease

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15
Q

Metabolism of catecholamines

A

-COMT and MAO enzymes

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16
Q

Epinephrine + COMT

A

-metanephrine

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17
Q

metanephrine or normetanephrine + MAO

A

VMA

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18
Q

NE or epinephrine + MAO

A

-dihydroxymandelic acid

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19
Q

dihydroxymandelic acid + COMT

A

VMA

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20
Q

NE + COMT

A

Normetanephrine

21
Q

Dopamine + MAO

A

dihydroxyphenylacetic acid

22
Q

Dopamine + COMT

A

-3-methoxtyramine

23
Q

Homovanillic acid

A

-from dihydroxyphenylacetic acid + COMT
-from 3-methoxytyramine + MAO

24
Q

Direct acting adrenergic receptor agonists

A

-norepinephrine
-epinephrine

25
Q

Sterochemistry of Adrenergic receptor agonists

A
26
Q

a1 agonist

A

-Gq
-vasoconstriction
-rise in BP
-pupil dilation
-ejaculation
-inhibition of GI

27
Q

a2 agonist

A

-Gi
-vasoconstriction
-inhibit NE release
-decrease CV SNS input

28
Q

B1 agonist

A

-Gs
-cardiac stimulation
-increase force and conduction
-secrete renin

29
Q

B2 agonist

A

-cardiac stimulation
-bronchodilation
-uterine relaxation
-GI inhibition
-vasodilation
-fall in BP

30
Q

Epinephrine receptor preference

A

-B1, B2, a1, a2

31
Q

NE receptor preference

A

-a1, a2, B1

32
Q

Norepinephrine activates

A

-a and B1 receptors

33
Q

Epinephrine activates

A

a and B receptors

34
Q

Dopamine activates

A

-D1
-B1
-a1

35
Q

D1 agonist

A

-vasodilation in renal, mesenteric, coronary arteries
=increase blood flow

36
Q

Sodium bisulfate

A

-used in NE and epinephrine preparations to prevent oxidation

-uhhh slide 20-21

37
Q

Epinephrine Beta activity

A

-stronger than alpha activity

38
Q

Epinephrine action at lower concentrations

A

-B1 and B2 effects predominate

39
Q

Epinephrine action at higher concentrations

A

-a1 effects prefominate

40
Q

Epinephrine clinical use

A

-treat anaphylaxis or cardiac arrest
-adjunct with local anesthetics

41
Q

Epinephrine problems

A

-not orally active due to COMT and MAO in liver
-can produce unwanted effects through broad activation of adrenergic receptors

42
Q

Epinephrine counters hypoglycemia

A

-B2: glycogenolysis, gluconeogenesis
= INCREASE glucose
-a2: inhibit insulin secretion

43
Q

Dipiveferin

A

-epinephrine
-treat infant glaucoma
-lipophilic
-activated by esterase

44
Q

Dopamine (intropin)

A

-D1 agonist
-renal dilation
-B1 and a1 agonist
-SNS activity
-cardio stimulate and systemic vasoconstrictor outside the kidney

45
Q

Dopamine clinical use

A

-shock
-acute congestive heart failure
-must be given as IV

46
Q

selective D1 agonist

A

-Fenoldopam
-severe HTN in hospitalized patients

47
Q

Phenylephrine

A

-a1 agonist
-nasal decongestant (not that good tho most gets metabolized in liver)
-mydriasis without cycloplegia
-pressor
-vasoconstrictor in regional anesthesia

48
Q

Phenylephrine administration

A

-parenteral
-oral
-local
-substrate for MAO

Therapeutics (78 decks)

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