Autonomic NS Pharmacology Flashcards

1
Q

What two types of nerves make up the peripheral NS?

A

Somatic Nerves

Autonomic Nerves

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2
Q

What is the function of somatic nerves?

A

Movement of skeletal muscles

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3
Q

What is the function of autonomic nerves?

A

Motor function of internal organs

  • Motility of GI tract, bladder
  • Dilation of pupils
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4
Q

What two systems make up the autonomic NS?

A

Sympathetic (Adrenergic)

Parasympathetic (Cholinergic)

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5
Q

What neurotransmitters and receptors are involved in the sympathetic NS?

A

Epinephrine 80% & NE 20% (adrenal medula)
Norepinephrine (nerves)
Ach (sweat glands - ONLY EXCEPTION)
Dopamine (renal, D1 receptors)

Adrenergic receptors

  • Alpha 1, Alpha 2
  • Beta 1, Beta 2, Beta 3 (not clinically significant)
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6
Q

What neurotransmitters and receptors are involved in the parasympathetic NS?

A

Acetylcholine

Muscarinic receptors
- M1, M2, M3

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7
Q

What is miosis and which NS is it involved in?

A

Constrict pupils

Parasympathetic autonomic NS

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8
Q

What is mydriasis and what NS is it involved in?

A

Dilate pupils

Sympathetic autonomic NS

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9
Q

What are 8 pharmacologically relevant functions of the PANS?

A
  1. Miosis (CN III)
  2. Lacrimation (CN VII)
  3. Salivation (CN IX)
  4. Decreased HR (CN X)
  5. Broncho-constriction
  6. Stimulates GI motility & secretion
  7. Contracts bladder & Relaxes sphincter
  8. Erection
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10
Q

What are 9 pharmacologically relevant functions of the SANS?

A
  1. Mydriasis
  2. Increased HR & Contractility
  3. Bronchodilation
  4. Arteriolo-constriction
  5. Inhibits GI motility & secretion
  6. Stimulates adrenals
  7. Stimulates glucose release
  8. Relaxes bladder & contracts sphincter
  9. Ejaculation
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11
Q

__________ is the neurotransmitter at the autonomic ganglia.

A

Acetylcholine

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12
Q

Where are a1 receptors found?

A

Blood vessels
Pupils dilators
Intestinal & bladder sphincters
Liver

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13
Q

What are the agonist actions of a1?

A
Vasoconstriction
Mydriasis
Increased intestinal & bladder tone
Increased glycogenolysis
Decreased renin
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14
Q

What are the antagonist actions of a1?

A

Relaxation of vascular smooth muscle
Vasodilation
Relaxation of the prostate capsule

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15
Q

Where are a2 receptors found?

A

Presynaptic sympathetic neurons

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16
Q

What are the agonist actions of a2?

A
Decreased sympathetic outflow
Decreased insulin release
Decreased lipolysis
Decreased aqueous humor production
Increased platelet aggregation
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17
Q

Where are B1 receptors found?

A

Heart

18
Q

What are the agonist actions of B1?

A

Increased HR & contractility
Increases renin release
Increased lipolysis

19
Q

What are the antagonist actions of B1?

A

Decreased HR & contractility

20
Q

Where are B2 receptors found?

A

Lungs
Blood vessels
Liver
Pancreas

21
Q

What are the 8 agonist actions of B2?

A
  1. Vasodilation
  2. Bronchodilation
  3. Increased lipolysis
  4. Increased insulin release
  5. Increased glycogenolysis
  6. Increased aqueous humor production
  7. Increased K+ cellular uptake
  8. Decreased uterine tone (tocolysis)
22
Q

What are the antagonist actions of B2?

A

Bronchoconstriction
Decreased K+ cellular uptake
Decrease aqueous humor production

23
Q

Sympathomimetic Drugs

A

Adrenergic Agonists

Drugs that MIMIC the activity of the SNS

24
Q

Define Direct-Acting Agonists.

A

Exert their effect by DIRECTLY BINDING to alpha, beta, or dopaminergic receptors and mimicking the effects of endogenous catecholamines.

25
Q

Define Indirect-Acting Agonists.

A

Enhance the effects of Epi & NE by inhibiting their reuptake or degradation.

26
Q

Define Mixed-Action Agonists.

A

Work by directly binding to receptors & releasing NE from its stores.

27
Q

What are non-selective adrenergic agonists?

A

Are mainly natural catecholamines (CA)
Only available as injections
Theoretically work on all adrenergic receptors

Epi
NE
Dopamine

28
Q

What are selective adrenergic agonists?

A

Are mainly synthetic CAs and non-CAs.

Selectivity is not absolute, it is lost with high doses.

a1-selective: Oxymetazoline & phenylephrine
a2-selective: Clonidine
B1-selective: Dobutamine
B2-selective: SABA (albuterol) & LABA (formoterol)
B3-selective: Mirabegron

29
Q

What are 2 examples of indirect-acting adrenergic agonists?

A

Cocaine

Amphetamines

30
Q

What are 2 examples of mixed-action adrenergic agonists?

A

Ephedrine

Pseudoephedrine

31
Q

Cathecholamines

  • Oral usability
  • Duration of action
  • CNS penetration
A

Cathecholamines

  • Oral usability: INEFFECTIVE
  • Duration of action: SHORT
  • CNS penetration: POOR
32
Q

Non-Cathecholamines

  • Oral usability
  • Duration of action
  • CNS penetration
A

Non-Cathecholamines

  • Oral usability: EFFECTIVE
  • Duration of action: LONG
  • CNS penetration: GOOD
33
Q

How does epinephrine interact with a1 receptors?

A

Can activate almost all adrenergic receptors hence, it is the treatment of choice for anaphylactic shock

a1 stimulation → vasoconstriction → ↑BP & ↓ edema

34
Q

How does epinephrine interact with B1 receptors?

A

B1 stimulation → ↑HR & contractility → ↑CO (used for cardiac arrest caused by asystole)

35
Q

How does epinephrine interact with B2 receptors?

A

B2 stimulation → Bronchodilation (sometimes used for emergency treatment of bronchospasms)

36
Q

How does NE interact with adrenergic receptors?

A

At therapeutic doses, NE mainly stimulates
a1 receptors → vasoconstriction → ↑BP

Its use is more limited than epi, helps in cases of profound hypotension & shock

37
Q

How does dopamine function in LOW DOSES?

A

In low doses, it stimulates

D1 receptors → renal vasodilation

38
Q

How does dopamine function in MODERATE DOSES?

A

In moderate doses, it stimulates

B1 receptors → cardiac stimulation

39
Q

How does dopamine function in HIGH DOSES?

A

In high doses, it simulates

a1 receptors → vasoconstriction

40
Q

When treating shock, which is preferred: Dopamine or NE?

A

Dopamine is preferred to NE because of its effect on renal vasculature when used in low doses

41
Q

What are 2 examples of a1-selective drugs?

A

Oxymetazoline: Used as eyedrops for red eye

Phenylephrine: Nasal decongestants, OTC old treatments; can ↑BP & precipitate angina