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PHRX 3009: drug action > 33: Drug Action on Adrenergic Neurotransmitters > Flashcards

33: Drug Action on Adrenergic Neurotransmitters Flashcards

1
Q

Draw the structure of norepinephrine.

A
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2
Q

Draw the structure of epinephrine

A
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3
Q

Where is norepinephrine produced? What is it used for?

A

Produced in the **locus coeruleus **in the back of the pons and distibuted in various areas in the brain.
* released in response to stress

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4
Q

Explain the function of adrenergic neurotransmitters in the sympathetic nervous system.

A

Sympathetic activation of the adrenal glands –> adrenal medulla releases norepinephrine and epinephrine into the bloodstream –> functions as a hormone to further access to a wide variety of tissues.

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5
Q

What is the function of adrenergic neurotransmitters in the eyes?

A

An increase in production of tears –> making the eyes more moist and pupil dilation.

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6
Q

What is the function of adrenergic neurotransmitters in the lungs?

A

An increase in bronchodilation.

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7
Q

What is the function of adrenergic neurotransmitters in the heart?

A

An increase in the amount of blood pumped.

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8
Q

What is the function of adrenergic neurotransmitters in the arteries?

A

Constriction of blood vessels –> causing an increase in blood pressure

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9
Q

What is the function of adrenergic neurotransmitters in the stomach and intestines?

A

A reduction in digestive activity due to decreases in gastrointestinl mobility, blood flow, and secretion of digestive substances.

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10
Q

What is the function of adrenergic neurotransmitters in the stomach and intestines?

A

A reduction in digestive activity due to decreases in gastrointestinl mobility, blood flow, and secretion of digestive substances.

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11
Q

What is the function of adrenergic neurotransmitters in the liver?

A

An increase in production of glucose.

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12
Q

What is the function of adrenergic neurotransmitters in the kidneys?

A

Release of renin and retention of sodium in the bloodstream.

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13
Q

What is the function of adrenergic neurotransmitters in the pancreas?

A

Increased release of glucagon
* glucagon - a hormone that increases the production of glucose by the liver

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14
Q

What is the function of adrenergic neurotransmitters in the adipose tissue?

A

An increase in lipolysis
* lipolysis - conversion of fat to substances that can be used directly as energy sources by muscles and other tissues

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15
Q

What is the function of adrenergic neurotransmitters on the bladder?

A

Increase in contraction

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16
Q

What is the function of adrenergic neurotransmitters on the uterus?

A

Increase of activity

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17
Q

Explain the negative outcomes of reduced norepinephrine hormone levels.

A
  • depression
  • poor memory
  • lack of energy
  • lack of concentration
  • lack of motivation
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18
Q

Explain the consequences of increased norepinephrine hormone levels.

A
  • increased blood pressure
  • increased heart rate
  • hyperactive
  • anxiety and stress
  • irritability and insomnia
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19
Q

Describe the human diseases associated with high levels of norepinephrine and epinephrine.

A

Sympathetic hyperactivation: a distinctive set of symptoms including…
* aches and pains
* rapid heartbeat
* elevated blood pressure
* sweating
* palpitations
* anxiety

Stress: increases when increase of norepinephrine activity, which mobilizes the brain and body to meet the threat

Tumor of the adrenal medulla

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20
Q

Describe the human diseases associated with high levels of norepinephrine and epinephrine.

A

Sympathetic hyperactivation: a distinctive set of symptoms including…
* aches and pains
* rapid heartbeat
* elevated blood pressure
* sweating
* palpitations
* anxiety

Stress: increases when increase of norepinephrine activity, which mobilizes the brain and body to meet the threat

Tumor of the adrenal medulla

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21
Q

Describe the human diseases associated with low levels of norepinephrine and epinephrine.

A

ADHD: a psychiatric condition involving problems with attention, hyperactivity, and impulsiveness

22
Q

Explain the different effects of drug action on adrenergic neurotransmitters.

A

Altering..
* biosynthesis of presynaptic neuron
* release from a presynaptic neuron to a synaptic cleft
* uptake back to a presynaptic neuron
* removal in a synaptic cleft

23
Q

Explain where biosynthesis of adrenergic neurotransmitters begins.

A

Starts from tyrosine
* tyrosine is a natural amino acid in proteins

24
Q

Explain aderenergic neurotransmitter biosynthesis: step 1.

A

Tyrosine is taken into the presynaptic neuron by Na+-dependent tyrosine transporter.

25
Explain aderenergic neurotransmitter biosynthesis: step 2.
Tyrosine is hydroxylated into DOPA by tyrosine hydroxylase (TH) * a rate-limiting step
26
Explain aderenergic neurotransmitter biosynthesis: step 3.
DOPA is converted into dopamine by DOPA decarboxylase (DDC)
27
Explain aderenergic neurotransmitter biosynthesis: step 4 (storage).
Dopamine is taken into presynaptic vesicles by a H+-coupled vesicular monoamine transporter (VMAT).
28
Explain aderenergic neurotransmitter biosynthesis: step 5.
Dopamine is hydroxylated into norepinephrine (NE) by dopamine beta-hydroxylase (DBH).
29
Explain aderenergic neurotransmitter biosynthesis: step 6.
Norepinephrine is methylated into epinephrine by PNMT.
30
Explain aderenergic neurotransmitter biosynthesis: step 7 (release).
Vesicles move to the presynaptic terminal, which enforces Ca2+ channel to open and uptake of Ca2+ into the neuron.
31
Explain aderenergic neurotransmitter biosynthesis: step 8 (release)
Ca2+ ions activate the vesicles to fuse with the presynaptic membrane and release norepinephrine into the synaptic cleft. * fusion process and release of norepinephrine can be inhibited by bretylium and guanethidine.
32
Explain aderenergic neurotransmitter biosynthesis: step 9 (removal)
A part of norepinephrine is diffused out of the synaptic cleft.
33
Explain aderenergic neurotransmitter biosynthesis: step 10 (reuptake)
A part of norepinephrine is retaken by NaCl-dependent norepinephrine transporter (NET) * NET can be inhibited by cocaine and tricyclic antidepressants (TCAs)
34
Explain aderenergic neurotransmitter biosynthesis: step 11 (degradation)
A part of norepinephrine is metabolized into nometanephrine by COMT --> form inactive metabolite secreted into urine.
35
Explain aderenergic neurotransmitter biosynthesis: step 11 (degradation)
A part of norepinephrine is metabolized into nometanephrine by COMT --> form inactive metabolite secreted into urine.
36
Explain aderenergic neurotransmitter biosynthesis: step 12 (degradation)
A part of reuptake norepinephrine is metabolized into DOPGAL by MAO --> form inactive metabolite secreted into urine.
37
Explain the negative feedback mechanism of norepinephrine release.
A part of norepinephrine binds to the presynaptic neuron on the neuron membrane surface --> inhibits neurotransmitter release from the vesicles by a negative feedback mechanism.
38
Metirosine *drug action:* *target protein:* *therapeutic indication:*
*drug action:* inhibition of biosynthesis *target protein:* TH *therapeutic indication:* hypertension
39
Carbidopa *drug action:* *target protein:* *therapeutic indication:*
*drug action:* inhibition of biosynthesis *target protein:* DDC *therapeutic indication:* parkinson's
40
Reserpine *drug action:* *target protein:* *therapeutic indication:*
*drug action:* inhibition of storage *target protein:* VMAT *therapeutic indication:* hypertension
41
Guanethidine *drug action:* *target protein:* *therapeutic indication:*
*drug action:* inhibition of release *target protein:* fusion process *therapeutic indication:* hypertension
42
Bretylium *drug action:* *target protein:* *therapeutic indication:*
*drug action:* inhibition of release *target protein:* fusion process *therapeutic indication:* arrhythmic
43
Cocaine *drug action:* *target protein:* *therapeutic indication:*
*drug action:* inhibition of reuptake *target protein:* NET *therapeutic indication:* pain management
44
Tricyclic antidepressants *drug action:* *target protein:* *therapeutic indication:*
*drug action:* inhibition of reuptake *target protein:* NET *therapeutic indication:* antidepressant
45
Entacapone *drug action:* *target protein:* *therapeutic indication:*
*drug action:* inhibition of degradation *target protein:* COMT *therapeutic indication:* parkinson's disease
46
Selegiline *drug action:* *target protein:* *therapeutic indication:*
*drug action:* inhibition of degradation *target protein:* MAO *therapeutic indication:* antidepressant
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PHRX 3009: drug action (36 decks)

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