Receptor Organ

SNS
1
Eye/HEENT
Blood vessel

Location

Blood vessel

Skin & splanchnic vessels (1&2)

Nassal Passage BV (1&2)

Heart

SA node
Ectopic pacemakers
Contractility
Kidney
Aqueous humor production
skeletal muscle vessels

Metabolism
EYE/HEENT
Blood vessels
Bronchiolar smooth muscle
GU Smooth muscle
Metabolism

Iris radial muscle

Skin & splanchnic vessels (1&2)
Nassal Passage BV (1&2)

3
M

Fat Cells
Skin

Pregnant uterus
Liver (Gluconeogenesis)
Liver (Glycogenolysis)
Lipolysis
Eccrine

PSNS
M1
M2

Brain
Heart

Inolved in memory, arousal, cortical activation

SA node

M3

Eye

Iris circular muscle

Ciliary muscle

Blood vessels
Respiratory
GI

GU smooth muscle

Smooth Muscle walls

Smooth muscle Sphincters
secretion
Bladder wall/Detrusor
Sphincter

Muscarinic

Located in eye, GI, Bladder, Salivary and sweat glands

Stimulation ~PSNS activity, dose depedent effects w/ blockage= glands/bronchial->hear
blockage - dry mouth, (-) sweating, bronchial secretions
Tachycardia and blurred vision
Constipation and urinary retention
ataxia, hallucinations, delirium, coma

Nicotinic

Located on autonomic ganglia, the brain, and skeletal muscle

Rapidly desensitized
Linked to Na & Ca channels -> Depol
Brain -> low doses= alert and attentive, high doses=termor,convulsions, vomitting
Peripheral-> +post-gang neurotransmitter release, and eppi release
Cardiac - +bp, Bradycadia-> tachycardia & (+) NE B(1) stimulation of heart. Noticed more w
GI/GU = vomiting nausea, diarrhera, urination
NMJ = initial stimulation and then flaccid paralysis if high dose

Action

Antagonist

Contracts (dilation)
Vasoconstriction
contracts

pup
Decongestion

Contracts
contracts
Accelerates
Accelerates
Increases
Renin release
Increases
Relazes
Relaxes
Relaxes
Increases
Increases
Increases
Increases

cal activation
Deccelerates
Contracts
Contracts
Vasodilation
Contracts
Contracts
Relaxes
Increases
Contracts
Relaxes

Clinical use

Decongestion
M2

M3

Inhibits adenylate cyclase, (-)cAMP

Contraction incr Increases IP3, DAG
Contraction increases aqueous humor clearance

2
2 2
1
1&2
1

glands/bronchial->heart and eye-> GI/GU->CNS

Toxicity=vomiting, convulsions, coma, respiratory arrest, H

T(x) = atropine, anticonvulsants, mechanical respiration

ulsions, vomitting

n of heart. Noticed more w/ high vagal tone (healthy adults)

cyclase, (-)cAMP

mor clearance

ma, respiratory arrest, HTN, paralysis, arrhythmia

mechanical respiration

Class

Drug

Acetylcholine (Miochol)
Carbachol (Isopto Carbachol)
Methacholine (provocholine)

Bethanechol (urecholine)
Pilocarpine (Salagen/pilocar)
Cevimeline (Evoxac)
Nicotine
Varenicline (Chantix)

Quaternary amine

Neostigmine (Prostigmin)

Tertiary amine

Physostigmine (Eserine)

CNS

tacrine
Donepezil (Aricept)
Rivastigmine (Exalon)
Galantamine (Reminyl)

Quaternary ammonium

Edrophonium (Tensilon)

Irreversible

Echiothiophate (Phospholine)
Organophosphates (DFP, Soman, Sarin)
Pralidoximine (2-PAM/Protopam)

Muscarinic Antagonist

Atropine

Scopolamine
Methscopolamine (Pamine)
Glycopyrrolate (Robinul
Dicyclomine (Bentyl)
Homatropine
Tropicamide (Myadriacil)
Diphenoxylate-atropine (Lotmotil)
Benztropine (Cogentin)
Trihexyphenidyl (Artane)
Tolterodine (Detrol
Fesoterodine (toviaz)
Solifenacin (vesicare)
Darifenacin (enablex)
Oxyvutynin (Ditropan)
Trospium (sanctura)
Umeclidinium (incrus ellipta)
Ipratropium (Atrovent)
Tiotropium (Spiriva)

Class

Drug

D-tubocuarine
Skeletal muscle paralysis,
utilize two ACh molecules 10 Pancuronium
carbons apart
Rocuronium (Zemuron)
Vecuronium (Norcuron)

utilize two ACh molecules 10

carbons apart
Cistracurium (Nimbex)
Atracurium (Tracium
Sugammadex (Bridion)

Succinycholine (Anectine)

utilize two ACh molecules 6

carbons apart

Hexamethonium

Eppinephrine (adrenalin)

Inactivated by intestinal
mucosa, MAO, COMT

NE (Levophed)

Isoproterenol (Isuprel)

Phenylephrine (neo-synephrine, Sudafed

PE)

Pseudoephedrine (Sudafed)
Xylometazoline (Otrivin)
Tetrahydrazoline (Visine), Naphazoline
(Privine)
Oxymetazoline (Afrin),

Methoxamine (Vasoxyl)
Midodrine (ProAmatine)

Clonidine (Catapres)
Methylodopa (Aldomet)
Guanabenz (wytensin), Guanfacine
(Tenex)
Apraclonidine (Iopidine), Brimonidine
(Alphagan)
Dobutamine (Dobutrex)

Albuterol (Bentikub(

Sakneterik (Serevent)
Terbutaline (Brethine)
Ritrodine(Yutopar)
Mirabegron (Myrbetriq)
Ephedrine
Amphetamine/meth
Methylphenidate (Ritalin)
Cocaine
Tyramine
Dopamine (Intropin)
Fendolpam (Corlopam)

Mechanism

Cholin
Direct C
Stimulates Muscarinic And Nicotinic receptors
Stimulates Muscarinic And Nicotinic receptors
Stimulates Muscarinic And Nicotinic receptors

Mus
Stimulates (M) receptors
Tertiary amine alkaloid, well absorbed into the brain
M3 receptor selective

Nic
Stimulates (N) receptors
Stimulates (N) {42 in the brain] receptors Partial
Agonist,

Cholin

Reversibly binds

Cholin
Competitive antagonist of (M) receptors

Selective M(3) antagonists

Mechanism

Neurom
Non-de

Competitive antagonist, close channel (non-depol), block

pre-junctional Na channels to (-) ACh release, reduce
endplate potential =no AP generation

pre-junctional Na channels to (-) ACh release, reduce

endplate potential =no AP generation

Direct Blo

Depolarizin

Bind n receptor -> open channel-> depol, (+) cardiac m

receptors, Ganglionic n receptors

Ga
non-depol competitve antagonists

Andre
Ca
All alpha, B1&B2 receptors

All alpha, only B1 Receptors

Essentially only a B-receptor agonist

A1 selective agonist

A1 selective agonist
A1 selective agonist

A1&2

Al
Presynaptics A2 receptors -> (-) NT release

Dop

Effects

Pharmacokinetics
Cholinerginic Stimulants
Direct Cholinergic Agonists

See receptors
See receptors
See receptors

Bladder and GI, +peristalsis

Choline Ester - long half

life than Ach
Choline Ester - long half
life than Ach
Muscarinic Agonists
, cannot penetrate BBB

Reduce intraocular pressure,

+salivation
Salivation
Nicotinic Agonists

dopamine release

Cholinesterase Inhibitors
Reverse post-surgery neuromuscular
Poor oral abs
blockers
Good oral abs, crosses
BBB, longer half life

Short half life, must be

injected
Long half life
lipid soluble, long
lasting bond, increases
w/ aging
Slow administration req,
no BBB crossing
Cholinergic Antagonists
No BBB unless toxic
dose

Sedation, amnesia, euphoria

Enters BBB/CNS

Shorter half life than

atropine

Not lipid soluble, no

BBB

Decrease bladder overactivity

Decrease bladder overactivity

Metabolized by
CYP2D6 & CYP3A4

Bronchiodilation

Low oral abs, no BBB,

Inhaled

Effects

Pharmacokinetics
Neuromuscular Antagonists
Non-depolarizing Blockers

Long lasting

Block ganglionic N and m receptors

Rapid Onset

Highly ionized, no oral

abs, BBB

Highly ionized, no oral

abs, BBB

Direct Blockade Reversal Agents

Depolarizing Neurmuscular Blocker

Rapid onset and

recovery, hydrolyzed by
BChE

ACh has no effect, Phase I & II

blockade,

Ganglion Blockers

Andrenergic Stimulants
Catecholamines
Dosage depedant A1>Vasoconstriction-> intial (+)BP->
(-)disatolic due to B2 vasodilation of
muscle BV, Vasoconstriction prevails
w/ high doses

>=NE>>Isoproterenol
for Alpha
Eppi=NE for B1 must
be injected

Vasoconstriction, (+)Dias &systolic BP

no change in Pulse pressure

(+)HR & contractility, vasodilation in

muscle BV-> (-)BP -> Reflexive (+)HR
Alpha Agonists

Vasoconstriction-> (+)BP, reflexive (-)

in HR

Vasoconstriction
Vasoconstriction

Nasal spray

Vasoconstriciton

Eye drop

Vasoconstriction

Nasal spray

Alpha 2 Agonists
Platlet aggregation, (-) insulin
In brain, transdermal
secretion, BP, HR, (+) aqueous humor
patch
clearance

Beta 1 Agonists
(+) CO, AV conduction, & renin
secretion
Beta 2 Agonists
Slightly (+) CO, AV conduction, &
renin secretion
Relaxes resp,
uterine, GI, & skeletal muscle BV
smooth muscle. (+) K uptake into
muscle, glycogenolysis and
gluconeogenesis in liver Slight
increase in Systolic, drop in
diastolic BP

Beta 3 Agonists
(+) Liplysis in fat cells, relax detrusor
Others

Dopamine Agonists

Side Effects/Toxicity

mulants
Agonists

nists
Sweating (m1), salivation,
diarrhea, abdominal cramps.
Mushroom toxicity possible, t(x)
w/ atropine and eppi

ists
Nausea, vomiting, vivd
nightmares, psychosis, anxiety,
suicidal

hibitors

Fast (n) desensitization ->

neuromuscular blockade,, High
doses->SLUDGE - salivation,
lacrimation, urination, efecation,
gastric distress, emesis

Muscle weakness, spasm,

tachcardia, HTN

gonists
CNS stim->depression

Sedation->stimulation, euphoria

Increase risk of alzheimers

Dry mouth, (-) bronchial

secretions, Tachcardia,
mydriasis/cyclopelgia, (-) GI/GU
activity, hot dry skin, memory
impairment, delirium, dementia
Toxicity -> Dry as a bone, blind
as abat, mad as a hatter, red as
a beet

Side Effects/Toxicity

agonists
Blockers
Histamine release ->
Hypotension & bronchospasm

Vagal blockade & tachycardia

Rapid onset

no hist. release
Histamine release & (+) toxicity

rsal Agents

ular Blocker
Genetic variances in metabolism,
Dibucain number diagnostic,
Hyperkalemia, muscle pain,
regurg w/ buff dudes or
esophageual dysfucntion/obesity,
+ inraocular pressure, maligant
hyperthermia w/ repeated doses
or halothane due to uncontrolled
SR Ca release
kers

ulants
es

ts

Rebound effect & mucosal

ischemia w/ excessive nasal
decongestion

sts

sts

sts

sts

nists

(+) Automaticity can lead to

spontaneous pacemakers

Interactions

Contraindication: Peptic ulcer, asthma

CI in narrow angle glaucoma, men w/ BPH, elderly w/ risk of

alzheimer's/dementia. Atropine blocks muscarinic agonist (-)
of BP,

Interactions

(+) w/ general anesthetics ( esp. Isoflurane), aminoglycosides

(streptomycin), Tetracylcines, Ca channel blockers/
antagonized by cholinesterase inhibitors (neostigmine) +
response w/ myasthenia gravis

Inactivated by Sugammadex

No reversbile by cholinesterase inhibiton, repeated doeses ->

bradycardia, dantrolene to tx malignant hyperthermia CI in pt
w/ extensive burns, soft tissue damage, rhabdo, spinal cord
injury, musc dystrophy, and children <8yrs

Trigger baroreceptor response w/ +BP -> (-)HR via vagal

response -> lost w/ atherosclerosis. CI w/ HTN

CI in HTN & narrow angle glaucoma

CI in HTN & narrow angle glaucoma

Clinical - Individual

Clincal - by
Group
resembles PSNS
activity, especially
in the Eye, GI,
Bladder, Salivary,

D(x) for asthma

Urinary Retention
Narrow angle glaucoma w/ a cholinesterase
inhibitor, Sjogrens sydrome
Glaucoma, dry mouth

Reduce intraocular
pressure

Nicotine cravings

Myasthenia gravis
Myasthenia gravis DOC, Atropine poisoning,
glaucoma
Alzheimers
Alzheimers
Alzheimers
Myasthenia gravis Dx
Emergent, long term decrease in intraocular
pressure
Tx w/ 2-PAM
Organophosphate poisioning, maybe carabamte
cholinesterase tx

Diarrhea w/ diphenoxylate, reverse reflex vagal

discharge, MI bradycadia/ AV block

Creates +PSNS Sx,

Tx of myasthenia
gravis

Motion sickness and nausea

Prevent vagal responses in surgery w/ visceral
organs, (-) GI side effects of cholinesterase
inhibitors
GI antispasmodic
Cause mydriasis, cycloplegia
Cause mydriasis, cycloplegia
Tx diarrhea
Parkinson's disease, Ach and dopamine
imbalances, (-) antipsychotic side effects
Overactive bladder

Cause mydriasis,
cycloplegia. Used in
Open angle
glaucoma, Tx for
cholinesterase
inhibitor poisoning
(no cure for (n)
receptors)

Post-surgery bladder spasm

COPD, Asthma -> bronchodilation

Clinical - Individual

Intubation

Clincal - by
Group

Surgery w/ gen
anesthetics,
ventilation,
orthopedics,
intubation,
convulsions

ventilation,
orthopedics,
intubation,
convulsions

Tacheotomy, intubation

Cycloplegia, mydriasis, orthostatic hypotension,

tachycardia, urinary retention, no reflex
responses to drugs

Causes Mydriasis w/o affecting accomodation. Tx

for Decongestion, Hypotensive emergencies

Decongestant
Decongestnat
Tx for red eyes
Decongestant

Tx for HypoTN
Midodrine - tx for postural HypoTN & autonomic
insufficiencies

HTN, anxiety w/ HTN, (-) nicotine addict cravings

Tx for Glaucoma, asthma, premature labor

contractions,

Pyridostigmine (Mestinon)
Ambenonium (mytelase)
Cevimeline

A1->G(q)-> IP3->Ca2 &DAG->PKC

Presynaptic A2-> G(i)->(-)cAMP & NT release
B>G(s) ->(+)adentylate cyclase&camp B2>eppi
lower affinity for B1

Alpha receptors in general

Vasoconstriction, (+) TPR, mydriasis, prostate

gland contraction, GU sm contraction (sphincters),
pilomotor hair erection, relax interstinal sm, (+)
Glycogenolysis & gluconeogenesis

ne (Mestinon)
m (mytelase)