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Sympathetic Nervous system Functions
maintain blood flow to the brain
redistribute blood flow during exercise
compensate for blood loss via vasoconstriction
Regulating body temperature
ex. increase HR, increase BP, decrease GI motility, dilation of the bronchi, dilation of the pupils
Parasympathetic Nervous system
slowing HR
increasing GI secretions
pupil constricition
emptying the bowels and bladder
contracting smooth bronchial muscle
PNS Transmitters
Acetylcholine
Norepinephrine
epinephrine
Acetylcholine
all preganglionic nuerons of the PNS have this
all postganglionic neurons have this in the PNS
all motor neurons to skeletal muscles have this
Norephinephrine
all postganlionic neurons of the SNS have this transmitter except sweat glands
Epinephrine
released by the adrenal medulla
cholinergic receptors
mediate the response of acetylcholine
Adrenergic recpetors
mediatate the response to EP and NorEP
Cholinergic subtypes
NicotinicN, NicotinicM, and Muscarinic
Adrenergic subtype
Alpha1, Alpha2, Beta1, and Beta2
Dopamine
receptor drug subtypes are,,,
important to drug selectivity
PNS
brain—> Preg neuron—> Ach, Nn—> postg neuron—> Ach M
SNS with alpha and beta
brain—→preg nueron—> ach—→Nn—→postg, NE alpha or beta
sweat glands
ACH, NN, ACH, M
SNS adrenal Medulla alpha or beta
ACH, NN, EPI
Skeletal muscle
no pre or post g, ACH, NM
NN receptors
NicotinicN Receptors
Promote ganglionic transmission at all ganglia of the sympathetic and parasympathetic nervous system.
Promote release of epinephrine from the adrenal medulla
NicotinicM Receptor
Causes skeletal muscle contraction
Muscarinic Receptor
Elicits responses from the target organ – i.e. glandular secretion, contraction of smooth muscle, decreased
HR, pupillary constriction,
alpha 1 receptors
Located in the eye, blood vessels, male sex organs, prostatic capsule and bladder
Causes contraction of the radial muscle of the eye (pupillary dilation), constriction of veins and arterioles, contraction
of the prostatic capsule and bladder trigone and sphincter and ejaculation
alpha 2 receptors
Drug effects from stimulation of peripheral nervous system Alpha2 receptors are of minimal significance.
Beta1 Receptors
Located in the heart and the kidneys.
• Activation of Beta1 cardiac receptors has an important therapeutic response to increase HR, force of contraction, and velocity of impulse
conduction.
• Activation of Beta1 receptors in the kidneys stimulates the release of renin
Beta2 Receptors
Located in the heart, lungs, skeletal muscle, bronchi, uterus, liver.
• Activation in the lungs facilitates bronchial dilation, uterine activation causes uterine smooth muscle relaxation. Effects of activation on
arterioles of the heart, lungs, and skeletal muscle is vasodilation – the opposite effect of what we see with alpha1 activation
Dopamine Receptors
• The only clinically significant dopamine receptors are located in the kidneys where activation causes dilation of renal
blood vessels and improve renal perfusion.
Bethanechol (Urecholine, Duvoid)
Muscarinic cholinergic agonist
Bethanechol (Urecholine, Duvoid
MOA:Direct-acting muscarinic agonist that binds reversibly to
muscarinic cholinergic receptors. Selective activation on muscarinic receptors.
Bethanechol (Urecholine, Duvoid
used for urinary retention and off label use for GERD and dysmobility disorders of the GI tract
ADEs of Bethencol
Cardiovascular – Bradycardia and hypotension (2/2 vasodilation)
GI – Excessive salivation, increased gastric acid, abdominal cramps, diarrhea
Urinary Tract – Increases bladder pressure, could cause bladder rupture if there is obstruction
or weakness of the bladder wall.
Pulmonary – Bronchoconstriction – CONTRAINDICATED for asthmatic patients.
Dysrhythmias – Dysrhythmias and tachycardia only in those with hyperthyroid –
CONTRAINDICATED for patients with hyperthyroidism.
Cevimeline (muscarinic agonist)
used for dry mouth
used in patients with autoimmune disorder that causes attack on the salivary gland cells
moa - increases salvation
Pilocarpine (muscarinic Agonist)
for glaucoma
moa: pupillary constriction of the iris sphincter which causes contraction of the detrusor muscles
decreases intraocular pressure
Acetylcholine (muscarinic agonist)
pupillary constriction
used after cardiac surgery
Atropine M antagonist
Classification: Anticholinergic
Mechanism of Action: Competitive blockade at muscarinic receptors; has no
direct effect on its own all responses are a result of preventing muscarinic
receptor activation
Atropine (M antagonist)
Therapeutic Uses: Pre-anesthetic medication, eye disorders, symptomatic
bradycardia, intestinal hypermotility, and muscarinic agonist poisoning.
Atropine ADEs
Xerostomia (dry mouth), blurred vision and photophobia, elevation of intraocular
pressure, urinary retention, constipation, anhidrosis (decreased sweating),
tachycardia
Scopolamine ( M antagonist)
o Similar to atropine with 2 important exceptions:
1. Can produce CNS sedation at therapeutic doses.
2. Suppresses emesis and motion sickness.
Ipratropium bromide (Atrovent) ( M antagonist)
o Muscarinic antagonism results in bronchial dilation
o Therapeutic uses include asthma, COPD, and rhinitis
icyclomine (Bentyl) ( M antagonist)
o Muscarinic antagonism results in decreased intestinal tone and motility
o IBS, functional bowel disorders
Another M antagonist
Urinary Antispasmodics
o Anticholinergic medications used to treat overactive bladder.
Oxybutynin (Ditropan,
Oxytrol) Anticholinergic, urinary antispasmodic agent
Mechanism of Action: Acts primarily on muscarinic M3 subtype receptors.
Therapeutic Uses: Only approved for treatment of OAB
Routes: PO (long & short-acting), transdermal patch, topical gel
Oxybutynin (Ditropan,
Oxytrol) ADEs
Dry mouth, constipation, tachycardia, urinary retention, mydriasis, blurred vision, and dry eyes. Can
also see CNS effects – sedation, hallucinations and confusion