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AS - N929 Pharmacology II > Autonomic Pharmacology > Flashcards

Autonomic Pharmacology Flashcards

1
Q

SNS

A 
Sympathetic
Thoracolumbar
Ganglia in perivertebral chain
Short pre-ganglion
Long post-ganglion
ACh Nicotinic receptor
Target tissue Adrenergic receptor
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2
Q

PSNS

A 
Parasympathetic
Cranial nerves III, VII, IX, X
Cervical & sacral S2-4
Ganglia in end organ tissue
Long pre-ganglion
Short post-ganglion
ACh Nicotinic receptor
Target tissue Muscarinic receptor
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3
Q

Adrenal Medulla

A

Hormone release 80% Epi 20% NE
Only one neuron
Pre-ganglion to adrenal medulla
Chromaffin cell

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4
Q

Neurotransmission Steps

A 
Synthesis
Storage
Release
Action at receptor
Termination - reuptake, enzyme degradation, diffusion
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5
Q

Nicotinic Cholinergic Receptor

A

Ligand-gated Na+/K+ depolarizing channel
Subtypes: Nn & Nm
Nn located in all ANS ganglia, adrenal medulla, CNS (nerve)
Nm located at skeletal NMJ (muscle)

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6
Q

Muscarinic Cholinergic Receptor

A

GPCR
Subtypes: M1, M2, M3, M4, M5

Stimulatory = M1, M3 (smooth muscle, glands, endothelium, eye), M5 ↑ Ca2+ release
Inhibitory = M2 (heart) & M4 ↓cAMP
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7
Q

Alpha Adrenergic Receptors

A

α
GPCR
Epi, NE, dopamine

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8
Q

α1

A

Excitatory
↑ Ca2+ ↑ calmodulin activation ↑ actin-myosin interaction ↑ smooth muscle contraction
Vasoconstriction
Smooth muscle, GU sphincters, skin, GI

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9
Q

α2

A

Inihibitory
↓cAMP ↓NE release
Pre-synaptic nerve terminal
Ex: Precedex or Clonidine

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10
Q

Beta Adrenergic Receptors

A

β
GPCR
Adenyl cyclase activation ↑ cAMP ↑ kinase activation & phosphorylation

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11
Q

β1

A

ONE heart
Heart chronotropy (SA node) & inotropy (cardiomyocytes)
Renal JG cells → renin release RAAS activation

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12
Q

β2

A 
TWO lungs
Vasodilation
Bronchial & uterine smooth muscle 
Liver glycogenolysis & gluconeogenesis
Skeletal muscle
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13
Q

β3

A

Adipose fat cells

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14
Q

Phosphodiesterase 5

A

PDE5
Enzyme that breaks down cGMP 2nd messenger
Inhibitor drugs - Sildenafil, Viagra, Cialis

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15
Q

Adrenergic

A

Neurons or receptors that use NE

Drugs that mimic sympathetic nerve stimulation

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16
Q

Catecholamine

A

Molecule that contains catechol & amine group

Epi, NE, dopamine

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17
Q

Cholinergic

A

Neurons or receptors that use ACh

Drugs that mimic parasympathetic nerve stimulation

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18
Q

Epinephrine

A

Epi or adrenalin
Produced in the adrenal medulla
Neurotransmitter in CNS

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19
Q

Norepinephrine

A

NE or noradrenalin
Produced in the adrenal medulla
Neurotransmitter at sympathetic effector tissues in periphery & in CNS

20
Q

Muscarinic Agonists

A

Direct acting cholinergic
Acetylcholine

↑ACh

  • Salivation
  • Lacrimation
  • Urination
  • Diarrhea
  • GI upset
  • Emesis
21
Q

Nicotinic Agonists

A

Direct acting cholinergic
Acetylcholine
Succinylcholine

22
Q

Acetylcholinesterase Inhibitors (Reversible)

A

Indirect acting cholinergic
Edrophonium (short-acting)
Neostigmine (intermediate)
Donepezil (Alzheimer’s)

23
Q

AChEi (Irreversible)

A

Indirect acting cholinergic
Organophosphates
Insecticides

24
Q

Succinylcholine

A

Cholinergic nicotinic agonist
Depolarizing skeletal muscle paralysis

Contraindications:

  • GI/GU obstruction
  • CV disease
  • Respiratory disorder (asthma or COPD)
25
Q

Edrophonium

A

Short-acting polar alcohol
Onset 30-60sec
Duration 10min
Admin w/ Atropine

26
Q

Neostigmine

A

Intermediate-acting moderately polar carbamate
Onset 10-30min
Duration 2-4hr
Admin w/ Glycopyrrolate

27
Q

Physostigmine

A 
Parasympathomimetic
Intermediate-acting 
Non-polar
Crosses blood-brain barrier
Onset 3-8min
Duration 1hr
28
Q

Anticholinergics

A

Muscarinic & nicotinic antagonists

↓ACh

  • ↓secretions
  • Urinary retention
  • Hyperthermia
  • ↑HR
  • Flushed skin
  • Mydriasis (dilation)
  • Confusion/delirium
  • Tremors
  • Absent bowel sounds
29
Q

Muscarinic Antagonists

A 
Non-selective muscarinic antagonist
- Atropine
- Glycopyrrolate
- Scopolamine
Selective M3 antagonist
30
Q

Nicotine Antagonists

A

NicotinicN (neuron)

NicotinicM
Non-depolarizing neuromuscular blocking drugs
Atracurium, Cisatracurium, Vecuronium, Rocuronium, Pancuronium

31
Q

Atropine

A 
Non-selective muscarinic antagonist
Lipophilic tertiary amine
Crosses blood-brain barrier
Half-life 4hr (prolonged in elderly)
↑HR ↑demand → cardiovascular concerns

Contraindications:

  • Glaucoma d/t ↑IOP
  • Prostate hypertrophy
  • GU obstruction
32
Q

Glycopyrrolate

A

Non-selective muscarinic antagonist
Quaternary amine
Less CNS effects (unable to cross blood-brain barrier)

Onset 1min
Duration 7hr
Half-life 1hr

Contraindications:

  • Glaucoma d/t ↑IOP
  • Prostate hypertrophy
  • GU obstruction
33
Q

Scopolamine

A 
Non-selective muscarinic antagonist
More lipophilic than Atropine
Tertiary amine
Crosses blood-brain barrier
CNS effects (amnesia)
\+++ sedation

Onset 10min
Duration 2hr
Half-life 2hr

Contraindications:

  • Glaucoma d/t ↑IOP
  • Prostate hypertrophy
  • GU obstruction
34
Q

Direct Acting Adrenergic Agonists

A 
α agonist
Norepinephrine α1,2
Phenylephrine α1
Clonidine α2
Dexmedetomidine α2

β
Isoproterenol β1,2
Dobutamine β1
Albuterol β2

α/β
Epinephrine α1 β1,2
NE α1 β1

35
Q

Indirect Acting Adrenergic Agonists

A

NT releaser

  • Amphetamine
  • Ephedrine

NE reuptake inhibitor

  • Cocaine
  • SNRI

MAO inhibitor

  • Tranylcypromine (non-selective)
  • Selegiline (selective MAO-B)
36
Q

α1

A

Vasoconstriction
Smooth muscle contraction
GI/GU sphincters contract
Mydriasis

37
Q

α2

A

↓NE release (pre-synaptic)
CNS inhibition
Platelet aggregation
↓insulin secretion

38
Q

β1

A

↑HR/contractility

↑renin release

39
Q

β2

A 
Bronchodilation
Vasodilation (skeletal muscle)
Smooth muscle relaxation
- Uterine
- GI/GU 
Glycogenolysis ↑glucose
40
Q

α Adrenergic Blockers

A 
α receptor blockers
Non-selective (phen...amine)
- Phenoxybenzamine α1 > α2
- Phentolamine α1 = α2
α1 Prazosin
α2 Yohimbine

Used to treat HTN (later agent), BPH, & pheochromocytoma (non-selective)
Cause smooth muscle relaxation, ↓SVR, ↓BP

41
Q

β Adrenergic Blockers

A

Non-selective Propranolol
β1
- Metoprolol
- Esmolol

↓MVO2

42
Q

Epinephrine

A 
α1,2 β1,2 agonist
↑β receptor affinity
1-20mcg/min
Hepatic CYP450 metabolism w/ renal excretion
Elimination 1/2 life <5min
43
Q

Norepinephrine

A 
α1 β1 (minimal effect on β2)
1-20mcg/min
Hepatic, renal, & plasma metabolism via CYP450
Renal excretion
Elimination 1/2 life 1min
44
Q

Isoproterenol

A

Non-selective β1,2
2-20mcg/min
Hepatic CYP450 metabolism w/ renal excretion

45
Q

Dopamine

A

Low dose D1 (renal) vasodilation 1-4mcg/kg/min
Moderate dose β1 inotrope 5-10mcg/kg/min
High dose α1 vasoconstriction 11-20mcg/kg/min

Hepatic, renal, & plasma metabolism via CYP450
25% metabolized to NE
Renal excretion
Elimination 1/2 life 2min

46
Q

Dobutamine

A 
β1
1-20mcg/kg/min
Hepatic metabolism via CYP450
Renal excretion
Elimination 1/2 life 2min

AS - N929 Pharmacology II (10 decks)

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