Autonomics Flashcards
What part of sympathetic nervous system
is innervated by cholinergic fibers?
(2 places)
Adrenal medulla
Sweat glands
What prevents release of NT at all cholinergic terminals?
Botulinum toxin
System, receptor, G-protein?
Increases:
VSM contraction, pupillary dilation (mydriasis), intestinal and bladder sphincter contraction
Sympathetic
Alpha 1
Gq
System, receptor, G-protein?
Increases:
Platelet aggregation
Decreases:
Sympathetic outflow, insulin release, lipolysis
Sympathetic
Alpha 2
Gi
System, receptor, G-protein?
Increases:
HR, contractility, renin release, lipolysis
Sympathetic
Beta 1
Gs
System, receptor, G-protein?
Increases:
HR, contractility, lipolysis, insuline release, aqueous humor production
Decreases:
VSM tone, bronchial SM tone, uterine tone (tocolysis), ciliary muscle tone
Sympathetic
Beta 2
Gs
System, receptor, G-protein?
Effects in CNS, eneteric nervous system
Parasympathetic
M1
Gq
System, receptor, G-protein?
Decrease:
HR, contractility of atria
Parasympathetic
M2
Gi
System, receptor, G-protein?
Increases:
Exocrine gland secretions, gut peristalsis, bladder contraction, broncial SM tone, pupillary sphincter tone (miosis), ciliary muscle tone (accommodation)
Parasympathetic
M3
Gq
System, receptor, G-protein?
Decreases:
Renal VSM tone
Dopamine
D1
Gs
System, receptor, G-protein?
Modulates transmitter release, esp. in brain
Dopamine
D2
Gi
System, receptor, G-protein?
Increases:
Nasal and bronchial mucus production, bronchial SM tone, pruritis, pain
Histamine
H1
Gq
System, receptor, G-protein?
Increases:
Gastric acid secretion
Histamine
H2
Gs
System, receptor, G-protein?
Increases:
VSM tone
Vasopressin
V1
Gq
System, receptor, G-protein?
Increases:
H2O permeability, reabsoption in collecting duct
Vasopressin
V2
Gs
Which enzyme, which second messenger?
Gq
Gs
Gi
Gq- phospholipase C, protein kinase C
Gs- adenylyl cyclase, protein kinase A
Gi- adenylyl cyclase, protein kinase A
Modulates NE release
by acting on
alpha-2, M2, angiotensin II
presynaptic autoreceptors
Norepinephrine
Activated bowel, bladder smooth muscle
Postoperative ileus, neurogenic ileus
Urinary retention
Direct cholinergic agonist
AChE resistant
Bethanechol
Glaucoma, pupillary contraction
Direct cholinergic agonist
Carbachol
Potent stimulator of sweat, tears, saliva
Open and closed-angle glaucoma
(What does it contract?)
Direct cholinergic agonist
Resistant to AChE
Pilocarpine
Contracts:
ciliary muscle (open-angle glaucoma)
pupillary sphincter (closed-angle glaucoma)
Challenge test for asthma diagnosis
Stimulates muscaric receptors in airway when inhaled
Direct cholinergic agonist
Methacholine
Postoperative and neurogenic ileus, urinary retention
Myasthenia gravis
Reversal of NMJ blockade (post-op)
Anticholinesterase (AChE-i)
No CNS penetration
Neostigmine
increases endogenous ACh
Myasthenia gravis (long-acting)
Anticholinesterase (AChE-i)
No CNS penetration
Pyridostigmine
Diagnosis of myasthenia gravis
(extremely short acting)
Anticholinesterase (AChE-i)
Edrophonium
Anticholinergic toxicity
(atropine OD)
Crosses BBB
Physostigmine
“Phyxes” atropine OD
Alzheimer’s disease
Anticholinesterase (AChE-i)
Donepezil
Side effects of cholinomimetics
COPD exarcerbation, asthma, peptic ulcers
AChE-i poisoning
(due to organophosphates, i.e. parathion)
Irreversibly inhibit AChE
Symptoms:
Diarrhea, urination, miosis, bronchospasm, excitation of skeletal muscle and CNS, lacrimation, sweating, salivation
Treatment for AChE-i poisoning =
Atropine
+
Pralidoxime
(regenerates active AChE)
Mydriasis, cycloplegia (no accommodation)
Muscarinic antagonists (3)
Atropine, homatropine, tropicamide
Parkinson’s disease
Muscarinic antagonist
Benztropine
Park my Benz
Motion sickness
Muscarinic antagonist
Scopolamine
COPD, asthma
Muscarinic antagonists (2)
Ipratropium, tiotropium
I pray I can breathe soon
Reduce urgency in mild cystitis, reduce bladder spasms
Muscarinic antagonist
Oxybutynin
Reduce airway secretions (post-op)
Oral: drooling, peptic ulcers
Muscarinic antagonist
Glycopyrrolate
Bradycardia, eye exams
Increases:
Pupil dilation (mydriasis), cycloplegia (no accommodation)
Decreases:
Airway secretions, gastric acid secretion, gut motility, bladder urgency in cystitis
Muscarinic antagonist
Atropine
Dry mouth, dry, flushed skin, increased body temperature, cycloplegia, mydriasis, disorientation
Acute closed-angle glaucoma (elderly)
Urinary retention (BPH)
Hyperthermia (infants)
Atropine overdose
(HOT as a hare
DRY as a bone
RED as a beet
BLIND as a bat
MAD as a hatter)
(Tx: physostigmine)
alpha-1, alpha-2, beta-1, beta-2
Anaphylaxis, open-angle glaucoma, asthma, hypotension
Epinephrine
alpha-1, alpha-2, > beta-1
Hypotension
Norepinephrine
beta-1, beta-2
Torsade de pointes, bradyarrhythmias
Isoproterenol
(May worsen ischemia by causing tachycardia)
High doses: alpha-1, alpha-2
Medium doses: beta-1, beta-2
Low doses: D1
Shock (renal perfusion), heart failure
inotropic and chronotropic
Dopamine
beta-1 > alpha-1, alpha-2, beta-2
Heartfailure, cardiac stess test
inotropic and chronotropic
Dobutamine
alpha-1, alpha-2
Hypotension, eye exams, rhinitis
Phenylephrine
beta-2 > beta-1
Asthma, COPD, premature uterine contractions
(3)
Albuterol- acute asthma
Salmeterol- long-term asthma, COPD
Terbutaline- premature uterine contractions
beta-2
Premature uterine contractions
Ritodrine
Releases stored catecholamines
Narcolepsy, obesity, ADD
Amphetamine
Releases stored catecholamines
Nasal decongestion, urinary incontinence, hypotension
Ephedrine
Catecholamine reuptake inhibitor
Vasoconstriction, local anesthesia
No beta-blockers!
Cocaine
beta-blockers = unopposed alpha-1 activation
= extreme hypertension
Centrally acting alpha-2 agonists
Decrease sympathetic outflow
Hypertension, esp. with renal disease
Clonidine, alpha-methyldopa
(No decrease in blood flow to kidney)
Non-selective alpha blocker
Irreversible
Pheochromocytoma
SE: orthostatic hypotension, reflex tachycardia
Phenoxybenzamine
Non-selective alpha blocker
Reversible
Pt on MAO-I who eats tyramine foods
Phentolamine
Alpha-1 blockers
Hypertension
Urinary retention in BPH
1st dose orthostatic hypotension, dizziness, headache
Prazosin, terazosin, doxazosin, tamsulosin
Alpha-2 blocker
Depression
SE: sedation, increased serum cholesterol, appetite
Mirtazapine
Beta-1 blockers
Angina pectoris, MI, SVT (2), HTN, CHF
_Ace_butolol, _bet_axolol, esmolol, atenolol, metoprolol
SVT- metoprolol, esmolol
Esmolol is short acting
Acebutolol is partial agonist
“Muck A TEN, BET ACEs ESpecially”
Nonselective beta blockers
Angina pectoris, MI, HTN, CHF, glaucoma (1)
Propranolol, timolol, nadolol, pindalol
Glaucoma- timolol
decreases secretion of aqueous humor
Nonselective alpha and beta antagonists
Carvedilol, labetalol
Vasodilatory effects
Partial beta agonists
Pindolol, acebutolol
Impotence, exacerbation of asthma
Adverse CV effects, CNS effects
Use with caution in diabetics
Beta blocker toxicities
How do beta blockers reverse SVT?
Decreased AV conduction velocity
(class II antiarrhythmics)
How do beta blockers reverse HTN?
Decreased CO
and
Decreased renin secretion
(B-1 receptor block on JGA cells)