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COM: Cardiopulm (Final) COPY > DSA: Autonomic Pharmacology > Flashcards

DSA: Autonomic Pharmacology Flashcards

1
Q

What are cholinomimetic agents?

A

Drugs that mimic Ach

  • AchR agonists
  • AchE inhibitors
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2
Q

What class of drugs are AchR antagonists?

A

Cholinoceptor-blocking drugs

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3
Q

What are sympathomimetic agents?

A

Drugs that mimic or enhance alpha and beta receptor stimulation

  • Agonists, drugs that enhance catecholamine release, drugs that block reuptake
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4
Q

What class of drugs are alpha and beta receptor antagonsists?

A

Adrenoceptor-blocking drugs

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5
Q

Where does Ach act as the primary NT?

A
  • major NT of the PNS
  • All preganglionic autonomic fibers
  • All postganglionic PNS fibers
  • Few postganglionic SNS fibers (sweat glands) **
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6
Q

Where is norepinephrine (NE) the major NT?

A
  • Major NT of the SNS

- vast majority of postganglionic SNS fibers

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7
Q

Where does synthesis of epinephrine occur?

A

In the adrenal medulla and in a few epinephrine-containing neuronal pathways in the brainstem

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8
Q

What is dopamine the precursor for and what does it act on?

A
  • Precursor for NE and epi

- Acts on the CNS and renal vascular smooth muscle

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9
Q

Where are nAChR receptors found?

A 
CNS
Autonomic ganglia (Nn)
Adrenal medulla (Nn)***
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10
Q

Where are mAChR receptors found?

A

CNS
Autonomic ganglia
Effector organs (cardiac and smooth muscle, gland cells and nerve terminals)
Swea glands***

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11
Q

What cholinergic receptors are coupled to Gq/11 GPCR’s?

A

M1, 3, and 5

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12
Q

What cholinergic receptors are coupled to Gi/o GPCR’s?

A

M2 and 4

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13
Q

What is the general effect of M2 and M4 receptors?

A

decreased cAMP production = decreased contraction

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14
Q

What is the general effect of M1, 3 and 4 receptors?

A

increase in IP3 = increased contraction

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15
Q

What type of receptor is found on the adrenal medulla?

A

nAChR (Nn) -> this is a sympathetic action but is found in the cholinergic signaling family

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16
Q

What type of receptor is found on sweat glands?

A

MAChR -> this is an exception to the rule that Ach is only involved in PNS signaling

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17
Q

What is the action of the parasympathetic and sympathetic systems on the bronchial?

A

Sympathetic causes relaxation and parasympathetic causes contraction

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18
Q

Give the steps of catecholamine synthesis

A

Tyr -> Dopa -> dopamine all in cytoplasm
Dopamine -> NE in the vesicle
NE -> Epi in the vesicle in the adrenal medulla

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19
Q

What is the function of the Na+-dependent Tyr transporter

A

Transports try into the nerve terminal for catecholamine synthesis

20
Q

What is the function of the vesicular monoamine transporter (VMAT-2)?

A

Transports NE, Epi, DA, and serotonin into vesicles

21
Q

What causes release of catecholamines into the synaptic cleft?

A

Ap and Ca2+ influx

22
Q

What is the role of the NE transporter (NET)?

A

Imports NE into the nerve terminal (reuptake)

  • There is also a DAT that imports DA into the nerve terminal
23
Q

What does cocaine effect in catecholamine signaling?

A

Inhibits the NE transporter (NET) -> causes an increase of catecholamines in the synapse so it causes an increase in sympathetic tone

24
Q

What is the major mechanism that terminates the actions of catecholamines versus a cholinergic signal?

A

Reuptake into nerve terminals terminates an adrenergic signal and destruction of NT terminates a cholinergic signal

25
Q

What are the 2 main enzymes for metabolism of catecholamines?

A 
Monoamine oxidase (MAO)
Catechol-O-methyltransferase (COMT)
26
Q

After reuptake, where are catecholamines stored?

A

In vesicles by the VMAT-2

27
Q

Where are alpha1 adrenergic receptors found?

A

In SM surrounding vasculature

28
Q

Where are beta1 adrenergic receptors found?

A

Heart

29
Q

Where are beta2 adrenergic receptors found?

A

Everywhere else

30
Q

What is the effect of activation of alpha1 adrenergic receptors?

A

Contraction of the smooth muscle surrounding the vasculature -> causes vasoconstriction

31
Q

What is the effect of activation of beta1 adrenergic receptors?

A

Increased force and rate of contraction of the heart

32
Q

What is the effect of activation of beta2 adrenergic receptors?

A

relaxation of SM

33
Q

What is the major agonist for alpha1 adrenergic receptors

A

epi and NE are about equal

34
Q

What is the major agonist for beta1 adrenergic receptors?

A

Epi and NE are equal

35
Q

What is the major agonist for beta2 adrenergic receptors?

A

epi is greater than NE

36
Q

What type of G protein are beta adrenergic receptors coupled to?

A

Gs -> causes increase in adenylyl cyclase

37
Q

What type of G protein are alpha1 adrenergic receptors coupled to?

A

Gq -> causes increase in phospholipase C and therefore an increase in IP3 and DAG

38
Q

Does NE have a greater effect on Beta1 or beta2 receptors?

A

Beta1

39
Q

T/F SM of blood vessels is NOT innervated by parasympathetic neurons

A

True!

- Vasodilation occurs due to decrease in sympathetic activity NOT an increase in parasympathetic activity

40
Q

Are mAChRs or nAChRs found on SM of blood vessels?

A

No neither of them!

**Blood vessels are innervated by adrenergic receptors, which cause constriction when activated (SNS)

41
Q

Activation of mAChRs on endothelial cells causes production and release of what?What causes this release?

A

Causes release of NO (AKA endothelium-derived relaxing factor (EDRF) -> stimulation of NO release can occur from Ach, vasoactive products and physical stimuli

42
Q

Epi and NE release is triggered by the release of ______ from the preganglionic fibers, which binds to ________ receptors and produces a localized depolarization

A

Ach; NnAChRs

43
Q

Where are NnAChR receptors located that bind to ACh causing the release of Epi and NE in the adrenal medulla?

A

Chromatin cells

44
Q

What is the function of reserpine?

A

Blocks dopamine from entering the vesicle and therefore decreases catecholamine storage

45
Q

A muscarinic Ach receptor antagonist on the bronchioles of the lungs would elicit what response?

A

Relaxation of the bronchiole SM bc muscarinic receptors usually cause contraction

46
Q

A 38 y/o, slightly obese male begins to walk briskly. As he continues to exercise, his HR and CO increase significantly. The key receptors on the heart that are responsible for this cardiac response are the ________ receptors

A

Beta1 adrenergic

COM: Cardiopulm (Final) COPY (20 decks)

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