Autonomic Nervous System (2) Flashcards

1
Q

Location of ACh receptors in the ANS

A

Parasympathetic System

Adrenal Medulla of Sympathetic System

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2
Q

Location of Nicotinic ACh receptors

A

NMJ

Sympathetic Ganglia

Parasympathetic ganglia

Central Nervous system

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3
Q

Location of Muscarinic ACh receptors

A

Parasympathetic target organs

Sweat glands (sympathetic)

Vascular smooth muscle

CNS

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4
Q

Nicotinic ACh receptor

A

Ionotropic

Muscle - (alpha1)2 Beta1 Delta(3backwards)

Ganglia - (alpha3)2(beta2)3

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5
Q

Muscarinic ACh receptor

A

G-protein linked receptor (metabotropic)

Gq - M1 and M3 –> Increase IP3 and DAG
Gi - M2 –> decrease cAMP

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6
Q

Can we differentiate muscle from ganglion Nicotinic ACh receptors ?

A

Differences in subunits may allows for some specificity

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7
Q

Predominate Tone

A

Tissues innervated by both branches of the ANS

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8
Q

Effects of anti-cholinesterase on the ANS

(SLUDGE)

A

Salivation
Lacrimation
Urination
Defecation
Gastrointestinal upset
Emesis

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9
Q

Effects of anti-cholinesterase on ANS

A

Parasympathetic

Bradycardia
Hypotension
Broncho-constriction
Pupillary constriction (MIOSIS)

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10
Q

How can nicotinic and muscarinic receptors be differentiated ?

A

Nicotine binds to Nicotinic receptors

Muscarine binds to Muscarinic receptors

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11
Q

What affects both nicotinic and muscarinic receptors ?

A

Anything that influences storage and release of ACh will affect both receptor types.

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12
Q

How can muscarinic receptors be classified ?

A

Classified by their tissue distribution and their cellular response.

Not all muscarinic receptors are in the ANS

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13
Q

What muscarinic receptors are found in the CNS ?

A

M1,2,4,5

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14
Q

Where is M3 found ?

A

On vascular endothelial and smooth muscle cells

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15
Q

State the 3 muscarinic receptors that are under parasympathetic control

A

M1(neural)
M2 (cardiac)
M3 (glandular / smooth muscle)

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16
Q

M1

A

GLANDS : gastric, salivary, lacrimal
Autonomic ganglia

Gastric secretion

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17
Q

M2

A

HEART: Atria

Cardiac inhibition

18
Q

M3

A

Gastric, salivary secretion
GI smooth muscle contraction
Ocular accommodation
Vasodilation

19
Q

What is atropine ?

A

Muscarinic Antagonist

20
Q

Muscarine receptor mediated effects

A

SLUDGE + Sweating

21
Q

Nicotinic receptors effects

A

Changing between sympathetic and parasympathetic effects

Muscle weakness

22
Q

Atropine effects

A

CNS mediated effects
Inhibition of muscarinic receptors

23
Q

Describe :

-pilocarpine
-bethanechol

A

Non-selective muscarinic agonists

Show little or no selectivity between the subtypes of muscarinic receptor

24
Q

Clinical uses of Pilocarpine

A

Constriction of pupils (Miosis)
Glaucoma (decrease IOP)
Xerostomia (following head/neck radiotherapy)

25
Q

Clinical uses of Bethanechol

A

Bladder and GI hypotonia

26
Q

How is selectivity of action with muscarinic agonists achieved ?

A

Achieved by a combination of choice of route of administration and the ionised state of the drug.

27
Q

State the muscarinic ACh receptor antagonists

A

Atropine
Glycopyrronium
Hyoscine Hydrobromide
Hyoscine butyl bromide
Ipratropium
Tropicamide

28
Q

Pharmacological properties of : Atropine

A

Non-selective antagonist
Well absorbed orally
CNS effects

29
Q

Pharmacological properties of : Glycopyrronium

A

Simliar to atropine
Doesn’t cross blood-brain barrier

30
Q

Pharmacological properties of : Hyoscine hydrobromide

A

Similar to atropine
CNS effects

31
Q

Pharmacological properties of : Hyoscine butyl bromide

A

Similar to Atropine but poorly absorbed
Doesn’t cross blood-brain barrier

32
Q

Pharmacological properties of : Ipratropium

A

Delivered via inhaler or nebuliser
Doesn’t cross blood-brain barrier

33
Q

Pharmacological properties of : Tropicamide

A

Similar to atropine but shorter acting

34
Q

Clinical uses of : Atropine

A

Adjunct for anaesthesia
Anticholinesterase poisoning
Bradycardia

35
Q

Clinical uses of : Glycopyrronium

A

Similar to atropine

36
Q

Clinical uses of : Hyoscine hydrobromide

A

Hyper-salivation
Motion sickness

37
Q

Clinical uses of : Hyoscine butyl bromide

A

GI spasms

38
Q

Clinical uses of : Ipratropium

A

Maintenance treatment of COPD

39
Q

Clinical uses of : Tropicamide

A

Ophthalmic use
(Mydriasis)

40
Q

Diseases cause muscarinic ACh

A

Increased PSNS activity

  • Little therapeutic uses for antagonists
41
Q

Problems of selectivity with antagonists

A

Few differentiate between subtypes effectively

Muscarinic ACh receptors widespread - side effects

Control by route of administration and distribution.

42
Q

Atropine use

A

Treats bradycardia