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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
Edrophonium
Short-acting polar alcohol Onset 30-60sec Duration 10min Admin w/ Atropine
26
Neostigmine
Intermediate-acting moderately polar carbamate Onset 10-30min Duration 2-4hr Admin w/ Glycopyrrolate
27
Physostigmine
``` Parasympathomimetic Intermediate-acting Non-polar Crosses blood-brain barrier Onset 3-8min Duration 1hr ```
28
Anticholinergics
Muscarinic & nicotinic antagonists ↓ACh - ↓secretions - Urinary retention - Hyperthermia - ↑HR - Flushed skin - Mydriasis (dilation) - Confusion/delirium - Tremors - Absent bowel sounds
29
Muscarinic Antagonists
``` Non-selective muscarinic antagonist - Atropine - Glycopyrrolate - Scopolamine Selective M3 antagonist ```
30
Nicotine Antagonists
NicotinicN (neuron) NicotinicM Non-depolarizing neuromuscular blocking drugs Atracurium, Cisatracurium, Vecuronium, Rocuronium, Pancuronium
31
Atropine
``` 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
Glycopyrrolate
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
Scopolamine
``` 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
Direct Acting Adrenergic Agonists
``` 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
Indirect Acting Adrenergic Agonists
NT releaser - Amphetamine - Ephedrine NE reuptake inhibitor - Cocaine - SNRI MAO inhibitor - Tranylcypromine (non-selective) - Selegiline (selective MAO-B)
36
α1
Vasoconstriction Smooth muscle contraction GI/GU sphincters contract Mydriasis
37
α2
↓NE release (pre-synaptic) CNS inhibition Platelet aggregation ↓insulin secretion
38
β1
↑HR/contractility | ↑renin release
39
β2
``` Bronchodilation Vasodilation (skeletal muscle) Smooth muscle relaxation - Uterine - GI/GU Glycogenolysis ↑glucose ```
40
α Adrenergic Blockers
``` 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
β Adrenergic Blockers
Non-selective Propranolol β1 - Metoprolol - Esmolol ↓MVO2
42
Epinephrine
``` α1,2 β1,2 agonist ↑β receptor affinity 1-20mcg/min Hepatic CYP450 metabolism w/ renal excretion Elimination 1/2 life <5min ```
43
Norepinephrine
``` α1 β1 (minimal effect on β2) 1-20mcg/min Hepatic, renal, & plasma metabolism via CYP450 Renal excretion Elimination 1/2 life 1min ```
44
Isoproterenol
Non-selective β1,2 2-20mcg/min Hepatic CYP450 metabolism w/ renal excretion
45
Dopamine
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
Dobutamine
``` 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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