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Autonomic System Pharmacology > Intro To Autonomic System > Flashcards

Intro To Autonomic System Flashcards

1
Q

Which presynaptic receptor provides feedback inhibition of NE

A

alpha2 receptors

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2
Q

Inhibition of alpha 2 receptor cause

A

Increase of NE

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3
Q

Location of alpha 1 receptors

A
  1. Blood vessels of skin, viscera, kidney , salivary glands

2. Most sympathetic organs (except heart)

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4
Q

Location of alpha 2 receptors

A 
Platelets
Vascular smooth muscles
Exocrine gland of pancreas
Never terminals
Fat cells
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5
Q

Beta 1 receptor location

A

Heart - + ve chronotrophic and inotrophic

kidney- increase renin production

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6
Q

Which adrenergic receptors are inhibitory(hyperpolarize)

A

Alpha 2

Beta 2

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7
Q

Which receptor binds only to epinephrine

A

Beta 2

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8
Q

Action of alpha 2 and G protein

A

G protein- Gi

  1. constriction of vasculature
  2. Inhibit lipolysis
  3. Inhibit insulin secretion
  4. Increase platelet aggregation
  5. Inhibit transmitter release
  6. Decrease secretions
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9
Q

Action of beta 2receptors G protein

A

G protein- Gs

  1. Dilation of bronchiole
  2. Dilation of blood vessels to lund and heart
  3. Lipolysis
  4. Glycogenolysis
  5. Decrease motility of GIT
  6. Tremors of skeletal muscles
  7. Relaxation of urinary bladder
  8. Increase HR and force
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10
Q

Where are beta 3 receptor found

A

Fat cells

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11
Q

Location and function of D1 receptors

A
  1. Splanchnic vessels-dilates

2. Renal vessels- dilate

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12
Q

D2 receptor location and function

A

Presynaptic nerve terminals- inhibit adenylyl cyclase

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13
Q

Mechanism of action of alpha 1

A
  1. Ligand binds
  2. Gq protein activated
  3. Activates PLC
  4. Hydeolyzes PIP2
  5. Form DAG and IP3
  6. IP3 cause increase in intracellular Ca2+
  7. Ca bind calmodulin cause phosphorylation
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14
Q

Mechanism of alpha 2

A
  1. Activation Gi
  2. Inhibits adenylyl cyclase - dec cAMP
  3. activate K+ channels or inhibit voltage gates Ca2+ channels
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15
Q

Beta receptor with least affinity

A

Beta 3 but is resistant to desensitization

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16
Q

G protein of D1

A

Gs - activates adenylyl cyclase-increase cAMP- vasodilation of renal and splanchnic vessels

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17
Q

Mechanism of D2

A

Activate Gi protein - inhibit adenylyl cyclase- dec cAMP- open K+ channels and Ca 2+ influx

18
Q

NE more potent at which receptors

A

alpha 1 and beta 3

19
Q

Phenylephrine and methoxamine have greater affinity at

A

Alpha1 more than alpha 2

20
Q

Clonidine and methylnorepinephrine greater affinity to which receptor

A

Alpha 2 greater than alpha 1

21
Q

Phenylephrine and methoxamine receptor, features, action

A
  1. Alpha 1
  2. Not a cathecol derivative
    not activated by COMPT
    Longer duration of action
  3. Vasoconstriction
22
Q

Treat hypotension, nasal congestion and cause local mydriasis

A

Phenylephrine and methoxamine

23
Q

Milodrine acts on

A

Selective alpha 1 receptor

24
Q

Effects if alpha 1 agonist

A
  1. mydriasis (ciliary muscle contact)
  2. Increased BP (arterioles and veins constrict)
  3. Piloerection
  4. Bladder sphincters contacted
25
Q

Hypertension treatment

A

Presynaptic Alpha 2 agonist- Clonidine, guanabenz, guanfacine, methyldopa, moxonidine

Feedback inhibition of NE release

26
Q

Side effects of presynaptic Alpha 1 agonist

A
  1. Drug withdrawn too quickly- withdrawal symptoms- rebound hypertension
  2. Dry mouth in 50%patient
  3. Sexual dysfunction in males
  4. Nausea
  5. Dizziness
  6. Sleep disturbances
27
Q

Clonidine acts on and effect

A
  1. Brain stem alpha 2 receptors
  2. Dec symp outflow to CVS
    - hypotension
    - bradycardia
28
Q

Clonidine acts on and effect

A
  1. Brain stem alpha 2 receptors
  2. Dec symp outflow to CVS
    - hypotension
    - bradycardia
29
Q

Fusion proteins

A

vSNARES- VAMPs ( synaptobrevin)

tSNARES- SNAPs (syntaxin, SNAP 25)

30
Q

Enzyme that converts Acetyl CoA +choline-> Ach

A

Choline acetyltransferase

31
Q

Where is Acetyl and choline got from

A

Acetyl CoA synthesised in mitochondria

Choline got from outside the cell transported by- choline transporter (CHT) Na dependent

32
Q

Drugs that act on CHT

A

HEMICHOLINIUMS

33
Q

Ach transported in to vesicle by

A

VAT (vesicle associated transport) driven by proton efflux

34
Q

VAT anther is blocked by

35
Q

Ach in the vesicle is bound to

A

Negatively charged vesicular proteoglycan ( VPG)

36
Q

Ca entering the cells interested with what protein to trigger fusion

A

Ca binds with VAMPs- synaptotagmin on vesicle never

37
Q

How is Ach vesicle release blocked

A

Botulinum toxin cleaves 2aa from one or more SNARE proteins

38
Q

Converts tyrosine to dopa

And drug that invite this process

A

Tyrosine hydroxylase

Metyrosin

39
Q

Catecholamine enter vesicle through

This protein is blocked by

A

VMAT (vesicle monoamine transporter)

Reserpine

40
Q
  1. Dopa is converted to dopamine by

2. Dopamine is converted to NE by

A
  1. Dopa decarboxylase

2. Dopamine-β - hydroxylase

Autonomic System Pharmacology (4 decks)

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