Autonomic Nervous

System Agents
Autonomic Nervous Systems: Sympathetic and Parasympathetic

Sympathetic Stimulants Parasympathetic Stimulants

Direct-Acting
Sympathomimetics (adrenergics, adrenomimetics, or adrenergic Parasympathomimetics (cholinergics or cholinergic agonists)
agonists) Action:
Action: Decrease blood pressure
Increase blood pressure Decrease pulse rate
Increase pulse rate Constrict bronchioles
Relax bronchioles Constrict pupils of eyes
Dilate pupils of eyes Increase urinary contraction
Relax uterine muscles Increase peristalsis
Increase blood sugar
Indirect-Acting
Cholinesterase inhibitors (anticholinesterase)
Action:
Increase muscle tone
Sympathetic Depressants Parasympathetic Depressants

Sympatholytics (adrenergic blockers, adrenolytics, or adrenergic Parasympatholytics (anticholinergics, cholinergic antagonists, or

antagonists) antispasmodics)
Action: Action:
Decrease pulse rate Increase pulse rate
Decrease blood pressure Decrease mucous secretions
Constrict bronchioles Decrease gastrointestinal motility
Increase urinary retention
Dilate pupils of eyes
 Adrenergics and Adrenergic Blockers

 Adrenergics – drugs that

stimulate the sympathetic
nervous system
 Adrenergic agonists,
sympathomimetics, or
adrenomimetics – mimic the
sympathetic neurotransmitters
(norepinephrine, epinephrine)
 Inactivation of neurotransmitters:
 Reuptake of the transmitter back into
the neuron
 Enzymatic transformation or
degradation
 Monoamine oxidase (MAO) – inside the
neuron
 Cathechol-O-methyltransferase (COMT)
– outside the neuron
 Classification of Sympathomimetics:
 Diffusion away from the receptor
 Drugs can stop the termination of the
neurotransmitter:
 Inhibiting the norepinephrine reuptake,
which prolongs the action of the
transmitter
 Inhibiting the degradation of
norepinephrine by enzyme action
 Direct-acting sympathomimetics
 Indirect-acting sympathomimetics
 Mixed-acting sympathomimetics
EPINEPHRINE
 Nonselective
 Acts on alpha1-, beta1- and beta 2-
adrenergic receptors
 Responses: increase BP, pupil dilation,
tachycardia, and bronchodilation
 Uses: treat allergic reactions, anaphylaxis,
bronchospasm, cardiac arrest
 S/E: anorexia, nausea, vomiting,
nervousness, tremors, agitation, headache,
pallor, insomnia, syncope, dizziness
ALBUTEROL
 Selective
 Beta2-adrenergic receptor
 Response: bronchodilation
 Uses: treat bronchospasm, asthma,
bronchitis, and other COPD
 S/E: tremor, dizziness, nervousness,
restlessness
CLONIDINE and METHYLDOPA

 Selective
 Alpha2-adrenergic drugs
 Tx: hypertension
 S/E: hypotension, tachycardia,
palpitations, dysrhythmias,
tremors, dizziness, urinary difficulty,
nausea, and vomiting.
Adrenergic Drugs (Alpha1, Beta1, and Beta2)
Generic (Brand)
Ephedrine HCl, Ephedrine sulphate
(Ephedsol, Ectasule)
(alpha1, beta1, and beta2)
Norepinephrine bitartrate
(Levarterenol, Levophed)
Alpha 1 and Beta 1
Dopamine HCl (Intropin)
Alpha 1 and Beta 1
Midodrine (proAmatine) Alpha1
Phenylephrine HCl 12-hour
spray/oxymetazoline HCl (Neo-
Synephrine) Alpha
Pseudoephedrine HCl (Sudafed,
Actifed, Co-Tylenol, PediaCare)
Alpha1 and Beta1
Uses and Considerations
Hypotensive states, bronchospasm, nasal congestion, orthostatic
hypotension.
Effective for relief of symptoms of hay fever, sinusitis, allergic
rhinitis. May also be used for mild cases of asthma.
Drug resistance may occur with prolonged use: stop drug for 3-5 d
then resume
For shock. Potent vasoconstrictor. Increase BP and CO.
BP should be closely monitored every 2-5 min during infusion.
IV flow titrated according to BP
To correct hypotension.
To treat symptomatic orthostatic hypotension.
Nasal decongestant.
To treat nasal decongestion. OTC drug. Avoid taking with history
of hypotension, cardiac disease, diabetes mellitus
Adrenergic Drugs (Alpha1, Beta1, and Beta2)
Generic (Brand)
Phenylpropanolamine HCl
(Dimetapp, Dristan)
Dexatrim, Dietac, Control
Alpha 1 and Beta 1
Metaproterenol sulphate (Alupent,
Metaprel) Beta 1 (some) and Beta 2
Dobutamine HCl (Dobutrex)
Beta 1
Isoetharine HCl (Bronkosol)
Beta 2
Terbutaline sulphate (Brethrine,
Bethaire, Bricanyl)
Beta 2
Ritodrine HCl (Yutopar)
Beta 2 and some Beta 1
Uses and Considerations
To treat nasal congestion; acts as OTC drugs
Appetite suppressant
Treatment of bronchospasm, acute heart block
To treat cardiac decompensation by enhancing myocardial
contractility, stroke volume, and cardiac output which may result
from cardiogenic shock or cardiac surgery.
To control asthma and COPD by dilating bronchial tubes
Primary use is to correct bronchospasm.
Unofficial: use during premature labor to prevent premature birth.
Used to decrease and/or stop uterine contraction.
 Adrenergics and Adrenergic Blockers

 Adrenergic Blockers – drugs that block the effects of the adrenergic neurotransmitters
 Adrenergic antagonist, or sympatholytics
 Act as antagonists to adrenergic agonists by blocking the alpha- and beta-receptor sites

Effects of Adrenergic Blockers at Receptors

Alpha 1 Vasodilation: decreases blood pressure; reflex
tachycardia might result; miosis; suppresses ejaculation;
reduces contraction of smooth muscle in bladder neck
and prostate gland
Beta 1 Decreases heart rate; reduces force of contractions
Beta 2 Constricts bronchioles; contracts uterus; inhibits
glycogenolysis, which can decrease blood sugar

Alpha-Adrenergic Blockers
 Alpha-blockers
 Drugs that block the response at alpha
adrenergic receptor site2
 groups:
 Selective (block alpha1)
 Nonselective
 Helpful in decreasing symptoms of BPH
 Promote vasodilation, causing decrease
in BP
 Can be used to treat peripheral vascular
disease (e.g., Raynaud’s disease)
Beta-Adrenergic Blockers
 Beta-blockers – decrease heart rate followed by
decrease in BP;
 Nonselective (beta1 and beta2) – can aslo cause
bronchoconstriction; extreme caution in client with COPD
 Selective adrenergic blockers has greater affinity for certain
receptors (Metoprolol tartrate)
 Intrinsic sympathomimetic activity (ISA) – causes
partial stimulation of beta receptors
 Carteolol, carvedilol, penbutolol, and pindolol –
nonselective beta-blockers that have ISA
 Acebutolol – selective blocker that has ISA
 Propranolol HCl (Inderal) – was the first beta
blocker prescribe to treat angina, cardiac
dysrhythmias, hypertension and HF; migraine
prophylaxis
 PK: well absorbed from the GIT; crosses BBB and placenta and
is excreted in breast milk; highly metabolized by the liver anf
t1/2 of 3 to 6h
 DI: phenytoin, isoproterenol, NSAIDs, barbiturates and
xanthines (caffeine, theophylline)-decrease drug effect
 DI: heart block if given together with digoxin or calcium
channel blocker
 S/E: bradycardia, palpitations, hypotension, headache,
dizziness, hyperglycemia, hypoglycaemia, bronchospasm
and agranulocytosis
Adrenergic Neuron Blockers

 Drugs that block the release of NE

from the sympathetic terminal
neurons
 Decrease BP
 Cholinergics

 Parasympathomimetics – drugs that stimulate

the parasympathetic nervous system; mimic
the parasympathetic neurotransmitter ACh
 Cholinomimetics, cholinergic stimulants, or
cholinergic agonists
 ACh – neurotransmitter located at the
ganglions and the parasympathetic terminal
nerve endings
 2 types of cholinergic receptors:
 Muscarinic receptors – stimulate smooth
muscle and slow the HR
 Nicotinic receptors – affect skeletal muscles
 Cholinergics

 Direct-acting cholinergic drugs – act on the

receptors to activate a tissue response
 Indirect-acting cholinergic drugs – inhibit the
action of enzyme cholinesterase (ChE) by
forming a chemical complex, thus permitting
acetylcholine to persist to attach to the
receptor
 Cholinesterase inhibitor/acetylcholinesterase
inhibitor (AChE)/anticholinesterases – are
drugs that inhibit cholinesterase
 Reversible
 Irreversible
Cholinergics
Effects of Cholinergic Drugs
Cardiovascular Decreases HR, lowers BP because of vasodilation, and slows
conduction of AV node
Gastrointestinal Increases tone and motility of smooth muscles of stomach and
intestine. Peristalsis in increased and sphincter muscles are
relaxed
Genitourinary Contracts muscles of urinary bladder, increases tone of ureters,
and relaxes bladder’s sphincter muscle. Stimulates urination
Ocular Increases pupillary constriction, or miosis, and increase
accommodation
Glandular Increases salivation, perspiration, and tears
Bronchial Stimulates bronchial smooth muscle contraction and increases
bronchial secretions
Striated muscle Increases neuromuscular transmission and maintains muscle
strength and tone
 Anti-Cholinergics

 Drugs that inhibit the actions of acetylcholine

by occupying the acetylcholine receptors
 Parasympatholytics, cholinergic blocking
agents, cholinergic or muscarinic
antagonists, antiparasympathetic agents,
antimuscarinic agents and antispasmodics