Intro to Autonomic Pharm Flashcards

1
Q

The ANS is not influenced by voluntary control and it regulates:

A
  • contraction and relaxation of smooth muscle
  • all exocrine and certain endocrine secretions
  • heartbeat
  • certain steps in intermediary metabolism
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2
Q

In the heart the CNS/PNS dominates

A

PNS (parasympathetic nervous system)

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3
Q

The control of blood pressure is mainly sympathetic/parasympathetic

A

Sympathetic

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4
Q

Sweat glands, kidney and the adrenal medulla are innervated only by _________

A

Sympathetic

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5
Q

What are the cholinergic fibers?

A
  • ALL preganglionic autonomic fibers
  • all parasympathetic post ganglionic fibers
  • all somatic motor fibers to skeletal muscle
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6
Q

Example of a sympathetic chilinergic fiber?

A

Sweat glands; they are sympathetic fibers that release acetylcholine

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7
Q

The ______________ fibers in the kidney release ____________ that act on the renal vascular smooth muscle

A

Sympathetic; dopamine

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8
Q

What is the rate limiting step in the synthesis of acetylcholine?

A

Bringing in choline into the neuron via the CHT1 transporter that also requires sodium (symport)

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9
Q

M2 muscarinic receptor is found on __________________ and is ___________

A

Presynaptic neuron; inhibitory in action by binding and inactivating acetylcholine

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10
Q

Where is dopamine converted into NE?

A

Inside the vesicle

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11
Q

The α 2 adrenergic receptor on the _________ neuron causes ________

A

Presynaptic;

↓ further release of NE

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12
Q

What are the two types of cholinergic receptors?

A
  • nicotinic (ion channel linked) : neuronal and muscle type

- muscarinic (G protein linked)

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13
Q

Neuronal nicotinic receptors are found on ________

A

Plasma membranes of the cell bodies of POST ganglionic parasympathetic and sympathetic receptors

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14
Q

Where can muscarinic receptors be found?

A
  • organs innervated by parasympathetic nerves
  • can be found in tissues that are NOT innervated by parasympathetic nerves BUT have these receptors but can get activate (endothelial cells)
  • tissues innervated by cholinergic postganglionic nerves (sweat glands which are sympathetic)
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15
Q

Where can M1 receptors be found and what are the effects

A
  • ganglia, CNS and vomiting center

- causes: depolarization, ↑ cognitive function, and emesis

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16
Q

Where can M2 receptors be found and what are the effects?

A
  • heart (atria), presynaptic Nerve terminal s

- cardiac inhibition and inhibition of acetylcholine release

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17
Q

Where are M3 receptors located and what are the effects

A
  • smooth muscles, secretory glands, vascular endothelium
  • contraction of smooth muscle
  • secretion
  • vasodilation of vascular endothelium (only receptors are found here)
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18
Q

Endothelial cells that line blood vessels have uninnervated M3 receptors contain the enzyme __________ which catalyzes: _________

A

NO synthase; formation of NO from arginine

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19
Q

What is the effect of NO on the smooth muscle cells?

A

NO activates guanylyl sh last which causes the formation of cGMP from GTP
- cGMP activates a kinase which then phosphorylates proteins → relaxation of smooth muscle → vasodilation

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20
Q

All___________ receptors are G protein coupled receptors

A

Adrenergic

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21
Q

All β adrenergic receptors activate __________ via interaction with ______

A

Adenylyl cyclase; Gs

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22
Q

_______ and_______ of the β adrenergic receptors have equal affinity for _________ and ______

A

β1 and β3; NE and epinephrine

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23
Q

β2 has higher affinity for ________

A

epinephrine

24
Q

Tissues with ________ receptors such as the vasculature of skeletal muscle are responsive to circulating ____________ released by the adrenal medulla

A

Β2; epinephrine

25
Q

Where are α1 and β1 receptors found and what is the importance of their location

A

Found near the adrenergic nerve terminals so they can be activated when the nerves are stimulated

26
Q

Where are α2 and β2 receptors located? What is the effect of their location on their activation?

A
  • Located at sites remote form the nerve terminals

- they are activated preferentially by circulating epinephrine

27
Q

Α2 and β2 receptors are activated preferentially by __________

A

Circulating epinephrine

28
Q

What it the signaling method of β1 receptors?

A

↑ cAMP; Gs

29
Q

What are the specific locations of the β1 receptor

A
  • heart
  • Juxtaglomerular (JG) cells
  • adipocytes
30
Q

What are the effects on the heart when the β1 receptors are activated?

A

↑ Heart rate
↑ Heart force
↑ AV conduction velocity

31
Q

What is the effect on the JG cells when the _____ receptors are activated

A

β1;

↑ renin release

32
Q

What is the effect of β1 receptor activation on adipocytes?

A

↑ lipolysis

33
Q

What is the effect on the activation of ______ receptors on the pancreatic cells?

A

β2;

  • pancreatic β cells: ↑ insulin secretion
  • pancreatic α cells: ↑ glucagon secretion
34
Q

Where can you find β2 receptors? (6)

A
  • smooth muscle
  • skeletal muscle
  • pancreatic α cells
  • pancreatic β cells
  • liver
  • adipocytes
35
Q

What is the effect of activation of β2 receptors on skeletal muscle?

A

↑ glycogenolysis

↑ K+ uptake

36
Q

What is the signaling mechanism of β receptors?

A

Gs coupled; ↑ cAMP etc

37
Q

What is the signaling mechanism for α1 receptors and where are they located?

A

↑ IP3 and DAG ↑ Calcium; Gq

Located at: vascular and genitourinary SM and the liver

38
Q

What is the effect of α1 receptors at the smooth muscles?

A

Vascular and genitourinary SM → contraction

39
Q

What is the signaling mechanism for α2 receptors?

A

↓ cAMP through Gi → inhibition of NE release, inhibition of lipolysis

40
Q

What is the effect of α2 receptors on platelets, pancreatic ____ cells and the vascular smooth muscle?

A
  • platelet aggregation
  • ↓ insulin secretion
  • contraction
41
Q

Where can the α2 receptors be found?

A
  • presynaptic nerve terminals
  • platelets
  • adipocytes
  • pancreatic β cells
  • vascular SM
42
Q

____ and _____ receptors act on the pancreatic β cells but _____ has more power and leads to a net effect of _____

A

α2 and β2 receptors;

α2 has more effect leading to an over effect of ↓ insulin secretion

43
Q

What do you have more of in the vascular smooth muscle: α1 or α2 receptors?

A

α1

44
Q

Dopamine receptors are predominately found in _______________ causing _________

A

Smooth muscle of renal vascular bed; relaxation and thus improving blood flow to the kidney

45
Q

The receptor found in the salivary glands are ______

A

Parasympathetic cholinergic M3 receptors

46
Q

The primary controlled variable in the cardiovascular function is the __________

A

Mean arterial pressure

47
Q

What is the net effect of NE on the heart when accounting of the negative feed back baroeceptor response (homeostasis)?

A
  • ↑ peripheral vascular resistance (contraction of SM)
  • moderate ↑ in MAP
  • BRADYCARDIA (opposite of drugs direct action)
48
Q

The cells of the medulla are modified __________ ___________ neurons

A

Post ganglionic sympathetic

49
Q

Describe the uniqueness of the innervation of sweat glands

A

They have sympathetic fibers that release acetylcholine and act on muscarinic receptors

(all other post ganglionic sympathetic fibers act on either α or β adrenoreceptors aka they are noradrenergic and act by releasing NE)

50
Q

Dopamine is released by some peripheral _________ fibers

A

Sympathetic

51
Q

What is the enzyme that synthesizes acetylcholine from acetyl CoA and choline?

A

Choline acetyltransferase (ChAT)

52
Q

Synthesis of all catecholamines in the nervous systems originates from the amino acid ____________

A

Tyrosine

53
Q

What is the rate limiting step in the creating of dopamine?

A

Tyrosine → L-DOPA which is done by the enzyme tyrosine hydroxylase

54
Q

________ receptor actuation are response for the vagal inhibition fo the heart and the CNS and periphery

A

M2

55
Q

________ activates endothelial nitric oxide synthase leading to the formation of NO from _________

A

Calcium;

Arginine

56
Q

How does the release of NO lead to vasodilation?

A

NO binds to and activates guanylyl cyclase which catalyzes the formation of cGMP which ten acres the cGMP dependent protein kinase → phosphorylates proteins → vasodilation

57
Q

NE stimulates renin secretion by directly acting on juxtaglomerular cells of the kidney as is mediated by _________ receptors

A

β1 adrenergic receptors