Autonomic Nervous System (Cholinergic) Flashcards

1
Q

What are the cholinergic receptors?

A

Muscarinic (M1-M5) -Nicotinic (Nn or Nm)

Think acetylcholine binding to these receptors, can be either sympathetic or parasympathetic. But parasympathetic is the postganglionic receptor at the target site so it will have more of a response.

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2
Q

What do heteroreceptor on the presynaptic neuron do?

A

Hetero = different

Heteroreceptors respond to neurotransmitters, neuromodulators, or neurohormones released from adjacent neurons or cells; they are opposite to autoreceptors, which are sensitive only to neurotransmitters or hormones released by the cell in whose wall they areembedded.

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3
Q

What are the function of autoreceptors?

A

An autoreceptor is a type of receptor located in the membranes of presynaptic nerve cells. It serves as part of a negative feedback loop in signal transduction. It is only sensitive to the neurotransmitters or hormones released by the neuron on which the autoreceptor sits.

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4
Q

Blood vessels are mainly controlled by what receptors?

A

Sympathetic control

a1, a2 - Constriction

B2 - Dilation

Location: systemic veins, smooth muscles, arterioles in: skin, splanchnic nerves, skeletal muscle

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5
Q

The eye is mainly controlled by what receptors and systems?

A

Sympathetic control

a1 - Contraction (mydriasis)

B2 - Relaxation to far vision

Parasympathetic control

M3 - Contraction (miosis)/near vision

M - Tear secretion

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6
Q

Receptors in the genitourinary smooth muscle?

A

Sympathetic control

B2/B3 - Relaxation of bladder wall

a1 - Contraction trigone and sphincter/ uterus, pregnant

Parasympathetic control

M3 - Contraction of bladder/Relaxation of sphincter

M - Erection of penis

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7
Q

Receptors in the heart?

A

Sympathetic control

B1 - Increase heart rate at SA node/Increase conduction at AV node/purkinje

B1/B2 - Increase in contractility in atria and ventricles

Parasympathetic control

M2 - Decreae heart rate in SA node/Decrease conduction at AV node/purkinje/Decrease atrial contractility

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8
Q

Receptors in the stomach and intestines?

A

Sympathetic control

a2/B2 - Decrease motility and tone

a1 - Contraction of sphincter

Parasympathetic control

M3 - Increase motility/tone, relax sphincter, stimulate secretion

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9
Q

Receptors in lungs?

A

Sympathetic control

B2 - Relaxation

a1 - Decreased secretion

B2 - Increased secretion

Parasympathetic control

M3 - Contraction/stimulation

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10
Q

Receptors in the skin?

A

Sympathetic control

a1 - Contraction pilomotor smooth muscle

M - Increase sweat secretion (Ach)

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11
Q

Receptors in the liver?

A

Sympathetic control

a1/B2 - glycogenolysis and gluconeogenesis

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12
Q

What are the effects of muscarinic agonists?

A
  • effects may be blocked by a muscarinic receptor antagonist
  • Alkaloids
  • Mimic Ach at muscarinic/nicotinic receptors to generate parasympathetic responses
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13
Q

Direct acting cholinergic/muscarinic agonists?

A

Acetylcholine (cholinergic) -> Very susceptible to AchE and nictotinic receptors

Methacholine (muscarinic) -> less susceptible to AchE and more cardiac effects than Ach. Does not affect skeletal muscle. Used for diagnosis of asthma.

Bethanechol (muscarinic) -> not susceptible to AchE, more GI effects (urination) and eye effects. Does not affect skeletal muscle. Stimulates urination.

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14
Q

Nicotinic receptor agonists?

A

Nicotine -> tobacco use or smoking cesation/dose related effect

Succinylcholine -> Depolarizing muscular blocker that causes depolarization and eventually blocks the nicotinic receptor becoming an antagonist

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15
Q

Indirect acting cholinergic agonists?

A

Endrophonium (Reversible) -> has alcohol group, and is short lived (2-10 min), very fast acting and can be used to reverse MR quickly

Neostigmine/Prostigmine (Reversible) -> carbamic acid ester, longer duration of action (30min to 6hrs) used to reverse MR

Physostigmine (Reversible) -> tertiary NH, can cross BBbarrier so is used as atropine overdose reversal where CNS was affected

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16
Q

What are reversible AchE inhibitors used for?

A

Myasthenia gravis, Alzheimer’s Disease, glaucoma, reversal of NM agents, antidote for antimuscarinic CNS toxicity

17
Q

What is an example of an Acetylcholinesterase regenerator?

A

Pralidoxime (2PAM) -> may reverse organophosphates if administered prior to “aging”. High affinity for phosphorus atom of the organophosphate and reactivates the enzyme

18
Q

What is a irreversible AchE agent?

A

Malathion, parathion -> Insecticides

19
Q

What are the muscarinic antagonists?

A

Glycopyrrolate -> antimuscarinic

Atropine -> more potent heart effects

Tolterodine -> think toilet, helps to treat urinary incontinence

Ipratropium -> used to open up the airways, treats asthma

20
Q

What receptor does NM blockers act on?

A

Selective for nicotinic receptors at NMJ (Nm)

21
Q

How are NM blockers metabolized?

A
  • Plasma esterases
  • Hofmann elimination
  • Hepatic metabolism
22
Q

How are NMBs eliminated?

A

Renal/hepatic/other

Plasma cholinesterases - short DOA

Metabolism - longer DOA

23
Q

How is atracurium eliminated?

A

Spontaneous (Hoffman degradation)

24
Q

How is pancuronicum eliminated?

A

Kidney (80%)

25
Q

How is rocuronium eliminated?

A

Liver (75-90%) and kidney

26
Q

Phase 1 Block

A

Membrane depolarizes resulting in an initial discharge which produces transient fasciculations followed by flaccid paralysis

27
Q

Phase 2 Block

A

Membrane repolarizes but receptor is desensitized to effect of acetylcholine

28
Q

What are the nicotinic antagonists?

A

atracurium

pancuronium

rocuronium

29
Q

What is an example of an indirect acting cholinergic antagonist?

A

Botox, blocks the release of Ach vesicles by interacting with SNARE proteins. Produces flaccid paralysis of selected skeletal muscle and diminished activity to local parasympathetic and sympathetic cholinergic synapses

30
Q

What are the muscarinic antagonists?

A

Glycopyrrolate

Atropine

Tolterodine

Ipratropium