DH206: Pharmacology
Chapter 4: Autonomic Drugs
Lisa Mayo, RDH, BSDH
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Objectives
1.
2.
Review of nervous system
ANS
ANS Anatomy Review
4. ANS Drugs Overview
5. PANS Drugs
6. SANS Drugs
3.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Objective #1
Review of Nervous System
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Nervous System
Primary function: control & coordinate the activity of all the systems
in the body
 Elaborate system that functions in both conscious and unconscious
levels
 2 subdivisions
1) CNS
 Brain & spinal cord
oReceive information from afferent nerves
oInitiates appropriate responses via efferent nerves
2) PNS: Peripheral Nervous System (next slide)
 12 pairs cranial nerves, 31 pairs spinal nerves
 2 subdivisions: somatic & visceral based on the type of
muscle to which these nerves innervate

Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PNS

Subdivisions PNS
1. Somatic Division
 Branches of cranial & spinal motor nerves that innervate
skeletal muscle
 CONSCIOUS CONTROL
2. Visceral Division (ANS): this chapter covers
 Visceral nerves are the branches of the cranial and spinal
motor nerves that innervate cardiac & smooth muscle
(involuntary) internal organs & glands
 UNCONSCIOUS CONTROL
 Nerves regulated by hypothalamus & medulla oblongata
 Visceral nerves commonly called ANS
 2 subdivisions: Parasympathetic & Sympathetic
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Objective #2: ANS
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS
Function: regulate organs (either ↑ or ↓ their activity)
 ALL organs have PANS & SANS receptors
 Practice of medicine and dentistry greatly benefitted from the
understanding of the ANS
 Relies on neurotransmitters (NTs) & receptors to cause a response
 NT: synthesized in the neuron & stored in axon
 When an AP occurs – NT released into synapse – eventually bind
to target organs in the body
 Results in either excitation or inhibition of the organ
 NT removed: degradation by enzymes, or through “reuptake”
 NT used in ANS: Norepi, ACH
Referred to as
 Other NT’s: epi, dopamine, serotonin, GABA
catecholamines

Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS

Receptors
 Receive NTs from axon terminals
 Located on the dendrites of POSTganglionic neurons
or smooth muscle, cardiac muscle, glands
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS


Divisions
1. PANS: parasympathetic autonomic nervous system
 Also known as the craniosacral division
2. SANS: sympathetic autonomic nervous system
 Also known as the thoracolumbar division
Most organs receive a nerve from each division
 Exception: blood vessels do NOT receive PANS
○ Why BP is controlled by SANS drugs & not PANS
drugs
○ Decrease stimulation = vasodilation
○ Increase stimulation = vasoconstriction
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS: PANS



Active during periods of rest & restoration of body
energy stores
Increase body functions (ex: digestion, waste
elimination)
When PANS activated: only select nerves can be
stimulated (unlike SANS) and confined to particular
body systems
 Ex: urination
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS: SANS
Innervates blood vessels (PANS does not)
 When SANS engaged, the whole body is stimulated (unlike PANS)
 Fight-or-Flight
 Adrenal medulla releases epi, some norepi into blood
↓
 Catecholamines act as hormones
↓
 Travel to all sympathetic receptors
↓
 Produce intense stimulation

↓
 Increase activity: heart rate, bronchodilation
 Decrease activity: GI and urinary tracts
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS: PANS vs SANS
Majority of time: actions produced are opposites
 SANS stimulates radial smooth muscles → increase in
pupil size (dilation)
○ Dilated pupils are termed mydriasis
 PANS stimulates circular smooth muscles → decrease
in pupil size
○ Constricted pupils are termed myosis
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS
Body Effects in text found p.34, Table 4-1
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Objective #3
ANS Anatomy Review
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS: Anatomy Review
Peripheral motor (efferent) nerves
 Branches of nerves that travel from brain/spinal column
to organs
 Neurons that emerge from the spinal column are called
PREGANGLIONIC NERVE FIBERS
 Neurons that travel from the ganglion to the organs are
called POSTSYNAPTIC NERVE FIBERS
 SYNAPSE: space between the preganglionic and
postganglionic fibers
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Synapse
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS: Anatomy Review
Main pharmacological difference between
PANS & SANS is the NT released from nerve
endings
 PANS: ACH, ACH
 SANS: ACH, Norepinephrine
 Nerves that release ACH = cholinergic nerve
 Nerves that release Norepi = adrenergic nerve
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Cholinergic nerve
Cholinergic
nerve
Cholinergic
nerve
Adrenergic nerve
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS: Anatomy Review
Summary
 Effects of SANS produced by
Norepi released from adrenergic nerve endings
2) Epi released from the adrenal medulla
1)
○ Both norepi & epi stimulate adrenergic receptors
 Effects of PANS produced when ACH which binds to
cholinergic receptors
○ 2 main types of cholinergic receptors (both stimulated by
ACH)
1. Muscarinic: Located POSTganglionic junction PANS
2. Nicotinic: Located PREganglionic junction PANS & SANS
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS: Anatomy Review
Cholinergic Receptors
1. Muscarinic
 Located on cell membranes of visceral organs and
glands (PANS innervated) – stimulated by ACH
released from POSTGANGLIONIC nerve endings
2. Nicotinic: 2 types receptors (nerve & muscle)
1) Nn: on both PANS and SANS ganglion & stimulated
from ACH released from PREGANGLIONIC nerve
endings to conduct impulses across autonomic
ganglion to POSTGANGLIONIC fibers of both
divisions (see next slide)
2) Nm: Part of Somatic, not ANS (skeletal muscles)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS: Anatomy Review
Adrenergic Receptors (SANS): divided into alpha(α) &
beta (β) receptors
α
Receptor Locations
Action
Alpha-1 smooth muscles ( GI
system, sweat glands, eye)
Vasoconstriction arteries/veins
Contract eye muscles
Alpha-2 POSTganglionic neurons
↓ release norepi
↓ BP
↓ secretion insulin
↓ eye secretion
Called autoreceptors
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS: Anatomy Review
Adrenergic Receptors (SANS): divided into alpha(α) &
beta (β) receptors
β
Receptor Locations Action
Beta-1
Cardiac tissue
Positive chronotrophic effects (↑ heart rate)
Positive inotropic effects (↑ contractibility/strength)
Beta-2
Smooth muscle of
bronchioles, skeletal
muscles, blood
vessels of
heart/kidney
Bronchodilation
Vasodilation
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ANS: General Rules for α & β
1.
2.
3.
4.
5.
α-receptor activation = generally excitatory or
stimulating (vasoconstriction, uterine contraction)
EXCEPT intestinal relaxation
β-receptor activation generally inhibitory/relaxing
EXCEPT heart which stimulates
Epi released by adrenal medulla – activates both
α and β but more potent on β-2 (higher affinity for
those receptors)
Norepi acts on ALL α and only some β. Chiefly a
vasoconstrictor.
β-1 predominate in the heart & blood vessels
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following neurotransmitters is
released from sympathetic postganglionic
neurons?
a. Dopamine
b. Serotonin
c. Acetylcholine
d. Norepinephrine
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following neurotransmitters is
released from sympathetic postganglionic
neurons?
a. Dopamine
b. Serotonin
c. Acetylcholine
d. Norepinephrine
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following neurotransmitters is
released from sympathetic and
parasympathetic preganglionic neurons?
a. Dopamine
b. Serotonin
c. Acetylcholine
d. Norepinephrine
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following neurotransmitters is
released from sympathetic and
parasympathetic preganglionic neurons?
a. Dopamine
b. Serotonin
c. Acetylcholine
d. Norepinephrine
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Objective #4
ANS Drugs Overview
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Autonomic Drugs




All drugs are either agonist or antagonist @
cholinergic & adrenergic receptors
AGONIST
 Sympathomimetic / Parasympathomimetic
ANTAGONIST
 Sympatholytic / Parasympatholytic
Certain ANS drugs are used in dentistry
 Vasoconstrictors added to local anesthetic
 Drugs used to ↑ or ↓ salivary flow
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
AUTONOMIC DRUGS

PANS
 Cholinergic (Parasympathomimetic) Agents
P+
 Anticholinergic (Parasympatholytic/Cholinergic Pblockers) Agents

SANS
 Adrenergic (Sympathomimetic) Agents
 Adrenergic Blocking (Sympatholytic/
Sympathetic blockers) Agents
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
S+
S-
Autonomic Drugs: p.36-38
4 drug groups of the ANS
1. A drug that stimulates the PANS is called P+
(cholinergic or parasympathomimetic)
2. A drug that blocks the PANS is called P–
(anticholinergic, parasympatholytic, or
cholinergic blockers)
3. A drug that stimulates the SANS is called S+
(sympathomimetic or adrenergic)
4. A drug that blocks the SANS is called S–
(adrenergic blockers, sympathetic blockers, or
sympatholytic)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Objective #5
PANS Drugs
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS DRUGS: p.38-43
1.
Cholinergic (parasympathomimetic) agents
○ Produce the effects of PANS (see handout)
2.
Anticholinergic (parasympatholytic) agents
○ Produce effects opposite the PANS (see handout)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS: General

Inactivation of ACH
 Achieved through hydrolysis by certain enzymes (this
occurs quickly so the effects of ACH last only a few
seconds)
1. Enzyme located in the area of the cholinergic
receptor – ACETYLCHOLINESTERASE (yields
metabolites of choline & acetic acid)
2. Enzyme PSEUDOCHOLINESTERASE is located in
liver & plasma that can hydrolyze ACH
 Ex: Botox: inhibits the release of ACH from the
cholinergic nerve ending to produce paralysis of
skeletal muscle – only lasts 3mo
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
ACETYLCHOLINESTERASE
choline & acetic acid metabolites
PSEUDOCHOLINESTERASE
In plasma/liver
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS
1. Cholinergic Agents
p.36-38
Cholinergic agents are classified 2 ways:
1. Direct acting
 Bind to muscarinic/cholinergic receptor to produce
effects similar to those of ACH
2. Indirect acting (cholinesterase inhibitors)
 Inhibit enzyme acetylcholinesterase to produce effects
similar to those of ACH
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS
1. Cholinergic Agents
1. Direct acting

Not useful drugs because of its extremely short duration of
action
 Actions: see handout for heart, kidney, GI, eye effects
 Ex: Pilocarpine (stimulate saliva, decrease intraocular
pressure)
2. Indirect acting
 When cholinesterase enzyme deactivates in the synaptic gap
– then ACH can build up because the enzyme is not there to
destroy it = ↑ concentrations of ACH at the receptor site
 Subdivisions (based on duration of action)
1) Reversible inhibitors: NOT tightly bound to receptors
2) Irreversible inhibitors: bind irreversibly to receptors
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
p.36, Table 4-3
USE THESE TABLES FOR REFERENCE, NOT BOOK
CHOLINERGIC PARASYMPATHOMIMETIC DRUGS
TYPE
DRUG
USES
Direct Acting Bethanechol(Urecholine) Urinary retention
Pilocarpine (Salagen)
Glaucoma, Xerostomia
Myasthenia gravis
TYPE
CLASS
DRUG
Indirect Acting Irreversible
Chemical Warfare (sarin)
Reversible
Physostigmine(Antilirium)
Neostigimine(Prostigmin)
Pyridostigmine(Mestinon)
Donepezil(Aricept)
Tacrine(Cognex)
USES
Glaucoma
MG
MG
Alzheimer's
Alzheimer's
NEED TO KNOW WHOLE GRAPH: USES, DRUG NAMES,
CLASSIFICATION!
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS
1. Cholinergic Agents



Adverse reactions (excessive stimulation of PANS)
 SLUD (salivation, lacrimation, urination, defecation)
 Tx adverse rxns with pralidoxime or atropine
Tx reactions caused by several drugs: Physostigmine
Pharmacologic Effects (see handout)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS
1. Cholinergic Agents
Contraindications
1) Bronchial asthma: may cause asthma attack
2) Hyperthyroidism: may cause atrial fibrillation
3) Severe cardiac disease: reflex tachycardia may
exacerbate a severe cardiac condition
4) Peptic ulcer: cholinergic agents stimulate gastric
acid secretion and increase gastric motility
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS
2. Anticholinergic Agents

p.38-40
Prevent the action of ACH at POSTganglionic endings
 Release of ACH is not blocked, but the receptor site is
competitively blocked by the anticholinergic
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS
2. Anticholinergic Agents

Atropine, scopolamine
 Lipid soluble
 Low doses: cause dry mouth, inhibit sweating
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS
2. Anticholinergic (parasympatholytic) agents
Pharmacological Effects
1. CNS effects
○ Drowsiness & sedation
○ OTC doses: limited amts scopolamine & used as sleep aids
○ Used in tx Parkinson’s disease & motion sickness
2. Exocrine Glands
 ↓ sweating
 Dentistry: ↓salivation & create a dry field
3. Eye: mydriasis (dilation of the pupil) used during eye exams
4. Respiratory
 Relax smooth muscle
 Ipratropium is an anticholinergic inhaler used to treat asthma
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS
2. Anticholinergic Agents
Contraindications (see handout)
 Glaucoma (Only ANS class drug that is not safe to use
for pt’s with glaucoma)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
PANS
2. Anticholinergic Agents
Drug Interactions: Avoid using in drugs that also cause
same adverse effects
SEE HANDOUT
Adverse effects important to dentistry
 Xerostomia: provide education
If pt using anticholinergic inhaler to tx asthma – need education
on dry mouth
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following receptors is stimulated when
pilocarpine is taken?
Cholinergic nicotinic
b. Cholinergic muscarinic
c. Adrenergic alpha
d. Adrenergic beta
a.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following receptors is stimulated when
pilocarpine is taken?
Cholinergic nicotinic
b. Cholinergic muscarinic
c. Adrenergic alpha
d. Adrenergic beta
a.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following drugs may cause xerostomia?
Epinephrine
b. Dopamine
c. Cevimeline
d. Atropine
a.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following drugs may cause xerostomia?
Epinephrine
b. Dopamine
c. Cevimeline
d. Atropine
a.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
A patient has an extensive history. All of the following
drugs can cause xerostomia as an adverse effect
EXCEPT which one?
Scopolamine
b. Pilocarpine
c. Homatropine
d. Atropine
a.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
A patients has an extensive history. All of the following
drugs can cause xerostomia as an adverse effect
EXCEPT which one?
Scopolamine
b. Pilocarpine
c. Homatropine
d. Atropine
a.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Objective #6
SANS Drugs
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS DRUGS: p.40-45
1. Adrenergic (sympathomimetic) agents
2. Adrenergic blocking agents
3. Neuromuscular blocking drugs
Cholinergic nerve
Adrenergic nerve
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: General
NTs in SANS: norepi(NE) and epinephrine
 NE: released at terminal nerve endings of the
SANS
 Epinephrine: released from adrenal medulla &
distributed via the blood
 Both NTs stimulate many internal organs to ↑
sympathetic activity
 Epi will relax smooth muscle, NE does not
○ Ex: epi used for bronchodilation, NE is not
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: General
p.40
Adrenergic nerve ending takes up the amino acid tyrosine
↓
Then forms DOPA (dihdroxyphenylalanine) & dopamine
↓
Then converted to Norepi
↓
Norepi then stored within vesicles inside nerve endings
↓
When nerves are stimulated – NE released – travel to smooth &
cardiac muscle – attach to their receptors – produce sympathetic
response
↓
Then NE will reuptake back into nerve ending or destroyed by
MONOAMINE OXIDASE enzyme
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: General
α-Receptors
Alpha-1 adrenergic receptors
 When stimulated by NE or Epi = cause
vasoconstriction
○ Remember: PANS drugs have NO direct action
on arteries
 Alpha-2 adrenergic receptors
 Drugs used in this category tx hypertension

Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
α-1
Vasoconstriction
HBP
Cholinergic nerve
Adrenergic nerve
α-2
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
↓ NE
SANS: General
-Receptors


Beta-1 receptors (memory trick - 1 heart)
 When stimulated = ↑ heart rate & force of contraction
 Metabolic effects on glycogen formation
(glycogenolysis) (NBQ)
Beta-2 receptors (memory – 2 lungs)
 When stimulated = produce vasodilation (mainly
skeletal & cardiac) and bronchodilation
 Drugs used in tx asthma
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: General
Alpha & Beta Receptors
2 divisions of drugs
1. Sympathomimetics/Adrenergic S+
 Alpha & beta-agonists
2. Sympatholytics/Adrenergic Blocking S Alpha, beta-blockers
 Antagonize or ↓ sympathetic activity
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympathomimetic
Sympathomimetic/Agonist drugs divided by their mechanism
of action (just like PANS drugs)
1) Direct acting
 Bind to & activate α or β receptors
 Ex: catecholamines (Epi, NE, Dopamine,
Isoproterenol)
2) Indirect acting
 Not bind to receptor
 Cause release NE from nerve endings
 Ex: Amphetamines (Adderall) & Cocaine
3) Mixed-Acting
 Ephedrine & Pseudoephedrine(Sudafed) activate α1
& β2 receptors by direct & indirect methods
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympathomimetic
Direct-Acting Agonists (next slides)
1) α-adrenergic agonists
2) β-adrenergic agonists
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympathomimetic
Alpha-1 Agonist Drugs
α1 receptor drugs (cause contraction of smooth
muscle)
 Vasoconstrict blood vessels (can cause
xerostomia)
 Stimulate submax/subling salivary glands = thick,
viscous saliva produced
 Contract ocular muscles that cause dilation of the
pupil (mydriasis)
 Next slide for clinical indications
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympathomimetic
Alpha-1 Agonist Drugs

Clinical Indications α1 receptor drugs
 IV in hypotensive states
 Dilate pupils for eye exams
 Ocular decongestants
 Open nasal passages = ↑breathing
○ Used as nose drops & nasal sprays for their
decongestant effect
○ Ex: phenylephrine(Neo-Synephrine),
oxymetazoline(Afrin)
○ Should not use more than 3-5 days due to re-bound
swelling & congestion that will occur
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
DIRECT ACTING α1-agonists
α1-agonist
Clinical Use
phenylephrine(Neo-Synephrine)
Nasal decongestant
oxymetazoline(Afrin)
Nasal decongestant
Tetrahydrozoline(Visine)
Ocular decongestant
Dipivefrin(Propine)
Glaucoma
Norepinephrine(Levarterenol, Levophed)
Hypotension, Shock
Epinephrine
Prolong action local anesthetics
Levonordefrin
Prolong action local anesthetics (not as
potent as epi)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympathomimetic
Alpha-2 Agonist Drugs

α2 receptor drugs
 Used to tx hypertension by decreasing heart rate
 Protype drug = Catapres
 Adverse effects
○ Xerostomia
○ Orthostatic hypotension
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
DIRECT ACTING α2-agonists
α2-agonist
Clinical Use
Clonidine(Catapres)
Hypertension
Withdrawal from alcohol
Methydopa(Aldomet)
Hypertension
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympathomimetic
Direct-Acting Agonists (next slides)
1) α-adrenergic agonists
2) β-adrenergic agonists
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympathomimetic
Beta Drugs
Most beta drugs have VERY FEW alpha effects
(EXCEPT EPI)
 Isoproterenol: Protype drug
 Non-selective drug
 Produce effects on heart (↑BP) & lungs
(bronchodilation) @ same time
 New drugs are selective – now can cause an
effect on the lungs & not the heart

Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
DIRECT ACTING Non-Selective β-agonists
Non-Selective β-agonist
Clinical Use
Isoproterenol(Isuprel)
Asthma
Isoetharine(Bronkosol)
Asthma
Epinephrine(Adrenaline)
Anaphylactic shock
Bronchodilator
Vasoconstrictor
Increase BP
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympathomimetic
Beta Drugs


β1 selective drugs
 Dobutamine (Dobutrex): ↑ myocardial contractility,
main use is in heart failure (IV)
β2 selective drugs
 Tx asthma through bronchodilation
 Vasodilation of skeletal muscle
 Can inhibit uterine contractions (how preterm labor is
stopped) Terbutaline
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
DIRECT ACTING Selective β1-agonists
β1-agonist
Clinical Use
Dobutamine (Dobutrex)
Stimulates heart
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
DIRECT ACTING Selective β2-agonists
β2-agonist
Clinical Use
Albuterol(Ventolin, Proventil)
Asthma
Terbutaline(Brethine)
Asthma, Pre-term labor
Metaproterenol(Alupent, Metaprel)
Asthma
Salmeterol(Serevent)
Asthma
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympathomimetic
Epinephrine
Possess alpha & beta effects (β effects greater than α)
 Cannot give orally: enzymes would destroy it too quickly
 Alpha effects: vasoconstriction
 Mydriasis, ↑BP, ↑heart rate, palpitations
 Beta effects
 β1 stimulation: Tachycardia, cardiac arrhythmias
 β2 stimulation: Bronchodilator
○ Why is the drug of choice for anaphylaxis
(bronchoconstriction)
 Increases glycogenolysis (β-receptor)
○ ↑ glucose production, release insulin = hyperglycemia

Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympathomimetic
Epinephrine


Epi in dental local anesthetic typically causes β2 responses
If use over 3-4 carpules = α1 responses will begin to occur
 Ex: increase systolic BP (not diastolic, just systolic)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following receptors does epi in low dose
primarily stimulate?
a. Alpha-1
b. Alpha-2
c. Beta-1
d. Beta-2
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following receptors does epi in low dose
primarily stimulate?
a. Alpha-1
b. Alpha-2
c. Beta-1
d. Beta-2
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Epinephrine goes through biphasic response
concerning BP. After the initial increase in BP,
there is a decrease. This decrease in blood
pressure is due to stimulation of which of the
following receptors?
a. α1
b. α2
c. β1
d. β2
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Epinephrine goes through biphasic response
concerning BP. After the initial increase in BP,
there is a decrease. This decrease in blood
pressure is due to stimulation of which of the
following receptors?
a. α1
b. α2
c. β1
d. β2
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
In high doses that are used in anaphylactic
shock, which of the following receptors
does epi primarily stimulate?
a. α1
b. α2
c. β1
d. β2
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
In high doses that are used in anaphylactic
shock, which of the following receptors
does epi primarily stimulate?
a. α1
b. α2
c. β1
d. β2
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: General
Alpha & Beta Receptors

2 divisions of drugs
1. Sympathomimetics/Adrenergic S+
 Alpha & beta-agonists
2. Sympatholytics/Adrenergic Blocking S Alpha, beta-blockers
 Antagonize or ↓ sympathetic activity
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympatholytics



Used in tx of:
 HBP
 Urinary retention
 Migraine headaches
 Glaucoma
Therapeutic effects & adverse effects due to the blocking of
alpha or beta receptors
Most all drugs are SELECTIVE – eliminate potential adverse
effects
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympatholytics
Alpha-Blockers
Bind to alpha receptors to block actions of NE and Epi
 Pharmacological effects
1) Relaxation of smooth muscle bladder & prostate
2) Vasodilation
3) Decrease BP: can ↑ risk orthostatic hypotension
 Clinical Indications
1) Hypertension
2) Raynaud’s disease (poor blood flow to skin & extremities)
3) Prostate hyperplasia (enlarged prostate which interferes
w/urinary flow through ureter)
4) Penile erectile dysfunction (α2)

Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
DIRECT ACTING Selective α1-antagonists
α1-antagonist
Clinical Use
prazosin (Minipress)
Hypertension
doxazosin (Cardura)
Hypertension
terazosin (Hytrin)
Hypertension, prostate hypertrophy,
urinary retention
Tamsulosin(Flomax)
Prostate hypertrophy
phenoxybenzamine, phentolamine
Raynaud's
DIRECT ACTING Selective α2-antagonists
α2-antaonist
Clinical Use
Yohimbine(Aphrodyne)
Penile erectile dysfunction
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympatholytics
Alpha-Blockers

Adverse Effects: complete opposite of alpha effects
 Instead of pupil dilation, will see constriction (miosis)
 Nasal congestion instead of decongestion
 Increase GI activity
 Reflex tachycardia will occur if the BP is lowered too
much
 Orthostatic hypotension
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympatholytics
Beta-Blockers
There are no therapeutic uses for blocking beta-2 receptors
 General names end in olol so it is easy to recognize them
 β1 blockers = most widely prescribed autonomic drugs!
 Clinical Indications
1) Hypertension
2) Angina
3) Heart arrhythmias
4) Panic attacks
5) Migraine headaches
6) Glaucoma

Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympatholytics
Beta-Blockers


Antagonize the beta actions of NE and Epi
Patients with HBP, angina, arrhythmias have
increased sympathetic activity
↓
If you can block the beta receptors with these drugs
↓
Then you reduce the effects Epi & NE
↓
Thus improve the patient’s heart issues by
decreasing heart activity
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympatholytics
Beta-Blockers
1. Selective β-1 (best choice for asthmatic patients who
have heart conditions) (NBQ)
 Protype drug: Atenolol (Tenormin)
 Fewer side effects, only affect heart, not lungs =
lower chance of drug interactions
2. Non-Selective (will block beta-1&2)
NEXT SLIDE
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympatholytics
Beta-Blockers
1. Selective Beta-1
2. Non-Selective (will block beta-1&2)





Protype drug: Propranolol (Inderal)
Block β1 & β2 (NBQ-never give to asthmatic!)
Block β1
 Effect on heart: Reduce cardiac output & BP
 Effect on eye: Reduce secretions & intraocular pressure
Block β2
 Effect on lungs: Bronchoconstriction in asthmatics
 Effect on liver: inhibit glycogenolysis, may cause
hypoglycemia in diabetics
Contraindicated: asthma, diabetes
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
DIRECT ACTING Selective β1-antagonists
β1-antagonist/blocker
Clinical Use
Metoprolol(Lopressor)
Hypertension
Atenolol(Tenormin)
Hypertension
Esmolol(Brevibloc)
Hypertension
Bisoprolol fumerate(Zebeta)
Hypertension
All end in ~olol
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
DIRECT ACTING Non-Selective β-antagonists
Non-selective β-antagonist/blocker
Clinical Use
Naldolol(Corgard)
Hypertension
Propranolol(Inderal)
Hypertension
Timolol(Blocadren)
Hypertension, migraines, MVP, tremors
All end in ~olol
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
SANS: Sympatholytics
Beta-Blockers

Metabolism
 Atenolol is NOT lipid-soluble
○ Does NOT pass blood-brain barrier
○ Excreted unmetabolized by kidney
 Propranolol is the most lipid-soluble β -blocker
○ Passes into the brain easily where it can exert pharmacological
effects
○ CNS sedation, mental depression, decreased central
sympathetic activity which may contribute to the lowering of
BP in tx of hypertension
○ Can tx secondary tachycardia associated w/ hyperthyroidism
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
What is the best choice medication to use for a patient with
angina pectoris and asthma?
a. Proanolol
b. Timolol
c. Labectalol
d. Atenolol
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
What is the best choice medication to use for a patient with
angina pectoris and asthma?
a. Proanolol
b. Timolol
c. Labectalol
d. Atenolol
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following types of drugs is used in
the treatment of nasal congestion?
a. B1-agonist
b. Selective B2-antagonist
c. Alpha-1-agonist
d. Alpha-2-agonist
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following types of drugs is used in
the treatment of nasal congestion?
a. B1-agonist
b. Selective B2-antagonist
c. Alpha-1-agonist
d. Alpha-2-agonist
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following pathways is
activated in a “fight-or-flight” situation?
a. Adrenergic
b. Cholinergic
c. Adrenergic antagonist
d. Somatic nervous system
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
NBQ
Which of the following pathways is
activated in a “fight-or-flight” situation?
a. Adrenergic
b. Cholinergic
c. Adrenergic antagonist
d. Somatic nervous system
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.