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Drugs Affecting the Autonomic Nervous System

Nervous System Review:
Divisions of the Nervous System

Central NS
Peripheral NS

Somatic
Autonomic
(voluntary) (involuntary)

Sympathetic and
Parasympathetic NS

Neurotransmitters of the Autonomic NS

1) Sympathetic NS Nor-epinephrine and Epinephrine (Adrenalin)
2) Parasympathetic NS
Acetylcholine
The release of neurotransmitters (AKA neurohormones) is controlled by
the bodys feedback mechanism, in an attempt to maintain homeostasis.
Receptors = a reactive site on the cell surface that responds to specific
chemical substances (lock and key analogy)
These circulating chemicals (neurohormones) attach to the receptor site
and send a message to the cell to create a specific response.
The Sympathetic NS and Para-Sympathetic NS each have their own specific
receptors.
Adrenergic Receptors:
1 increase cardiac contractility, increased BP, increased
HR, increased renin secretion

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2 decrease GI tone and motility, bronchodilitation,
relaxation of smooth muscle.
1 increased cardiac contractility, vasoconstriction,dilates
pupils, decreased salivation.
2 promotes vasodilataion and decreases BP, decrease GI
motility and tone.
Cholinergic receptors:
Muscarinic smooth muscle
Nicotinic skeletal muscle
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Sympathetic NS Fight or Flight Release of epinephrine
and nor-epinephrine from adrenergic (sympathetic) nerve fibers
HR, BP, CO
Pupil dilation = mydriasis
Brochodilation
GI Motility
Bladder Relaxation
CNS - Alertness
Parasympathetic NS Rest and Digest
HR, BP
Pupil constriction = miosis
Bronchconstriction
GI motility digest
Bladder contraction
watery secretion in saliva
Relaxed, calm

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Drug Therapy
Antagonist = blocks affect at receptor
Agonist = causes affect at receptor
Classification of Drugs of the Autonomic NS (terminology)
Sympathomimetic, Parasympathomimetic = agonist
Sympatholytic,

or Blocker
(alpha or beta)

Parasympatholytic = antagonist opposite effect

Anti-Cholinergic

The perfect drug would exert its action only on the target organ or cell;
however despite major advances in drug therapy, this is not always
possible Side Effects
Drugs affecting the Sympathetic NS
1 adrenergic antagonists = Beta-blockers Revolutionary drugs in the
field of Cardiology
Mechanism of Action: Blocks the effects of epinephrine and
nor-epi at the receptor site HR, BP
*Reduces myocardial O2 demand
Indications:
Tachycardia, high blood pressure
Potential side effects: bronchoconstriction = bronchospasm (wheezing)
Why?
Non selective

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Use Beta-blockers cautiously in Diabetic patients, especially Insulin
dependent Diabetics can mask the signs and symptoms of hypoglycemia
Drugs: Metoprolol (Lopressor)
Metoprolol XL (Toprol XL)
Atenolol (Tenormin)
Carvedilol (Coreg)
Propanolol (Inderal)
*Beta-Blockers can not be stopped abruptly. Taper over 14 days if
possible. Can cause rebound tachycardia
Common side effects: fatigue, sexual dysfunction in males
Beta-Agonists ( adrenergic agonists) these drugs are Sympathomimetic
From a cardiac perspective: Beta-Agonists are used as Emergency Drugs to
HR and/or BP
Epi-pen administered for acute allergic response, given SC
Catecholemines: Endogenous neurohormones produced by the
Sympathetic NS:
1) Epinephrine
2) Nor-epinephrine
3) Dopamine
1 Antagonists = Alpha blockers
Alpha 1 receptors are densely located on blood vessels (arteries,
arterioles)
If 1 receptors blocked decrease cardiac contractility/vasodilation
Conversely: If 1 receptors stimulated increase cardiac
contractility/vasoconstriction

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Mechanism of action of Blockers: lower BP by blocking 1 receptors on blood
vessels relaxation of the vessel, vasodilation
Indication: Hypertension mostly for hypertension
Drugs:
Terazosin (Hytrin)
Doxazosin) Cardura
1 receptors are also located on bladder and prostate: symptoms of BPH
in men (Benign Prostatic Hyperplasia)

1 Agonist
Indicated for the treatment of Orthostatic Hypotension
Orthostatic Hypotension = decrease BP with standing or changing position.
MOA: Stimulate Alpha 1 receptors on blood vessels vasoconstriction
Remember: Epinephrine Fight or Flight
EX: Midodrine (Pro-Amantine)
Very selective for 1, therefor does not affect HR
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1 Agonist Drugs also used as Decongestants:
Pseudoephedrine, Ephedrine, Phenylephrine, Neo-Synephrine
By what mechanism of action do these sympathomimetic drugs
congestion? Cause vasoconstriction of the capillaries and decrease
secretions. Vo consctriction, decreases the tissue. Histamine allergy reaction-

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increases capillary permabilty, vessels become leaky. Steroids wil close the
vessels. Decrease edema.
Preventing leakage into the nose and sinuses and causing the fluid to be
reabsorbed into the bloodstream and lymphatic system
Side Effects of Decongestants:
Hypertension
Tachycardia (effect on 1)
Insomnia-unable to sleep
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Drugs Affecting the Parasympathetic NS
Anti-Cholinergic Drugs (Cholenerigic antagonist/Parasympatholytics)
Interrupt parasympathetic nerve impulses in the CNS and ANS and prevents
acetylcholine from stimulating cholinergic receptors.
Uses:
1. Reduce oral, gastric, and respiratory secretions.
2. Reverse heart block
3. Paralyze ciliary muscles in the eye (dilates pupil)
Atropine (know this drug)
Given IV to HR in cases of extreme bradycardia (an
Emergency drug)
Anti-cholinergic eye drops used to dilate pupils at the
Ophthalmologist office for eye exam
GI:
Anti-Cholinergic drugs are used to treat diarrhea and intestinal spasm
seen w/ IBS
*Remember: Acetylcholine Rest and Digest Anti-Cholinergics
block these effects: resulting in GI motility diarrhea,
intestinal spasm

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Anti-cholinergics affecting the GI tract
Lomotil: anti-diarrheal
dicyclomine (Bentyl): TX for IBS (relaxes smooth muscle of the GI
tract and GI motility
GU: (Genito-urinary)
Drugs used to treat urinary frequency and incontinence
Mechanism of Action: Minimizes bladder contraction.
EX: oxybutynin (Ditropan)

*Most common side effects of Anti-Cholinergic: (As a class)

Dry mouth, constipation, urinary retention, tachycardia, sedation

MEMORIZE THE LIST!

Cant Pee
Cant See
Cant Spit
Cant Sh**
Sedation
Confusion
Especially in the Elderly
Do not use in:
1. acute angle glaucoma

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2.
3.
4.
5.
6.
7.
8.
9.

uncontrolled tachycardia
urinary or GI obstruction
COPD
Severe ulcerative colitis
Myasthenia gravis
Acute or severe hemorrhage
Unstable cardiovascular status
Breast feeding women

Reversal agent: Physostigmine

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Cholinergic Drugs (cholenerigic agonist/Parasympathomimetics)
Enhance the effects of Acetylcholine at the receptor site OR by inhibiting
cholinesterase.
Used for:
1. Glaucoma
2. Atonic bladder (urinary retention
3. Salivary gland hypofunction
Do not use in:
1.
2.
3.
4.
5.
6.

Prostate enlargement (BPH)

Urinary or GI obstruction
Hyperthyroidism
Bradycardia or AV conduction issues
Asthma
CAD

Never give these meds IV or IM (only PO or SQ)

EX: 1) Bethanachol (urocholine) Targets the detrusor muscle of the
bladder, stimulates the receptor enhances bladder contraction
Indication: Urinary Retention, Neurogenic Bladder promotes complete
bladder emptying

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EX: 2) Prostigmin (neostigmine) inhibits cholinesterase
Indication: Myasthenia Gravis
MYASTHENIA GRAVIS: An autoimmune disease characterized by
acetylcholine receptor antibodies. The body attacks its own acetylcholine
receptors, interfering with neuromuscular transmission of impulses.
Symptoms of myasthenia gravis: Diplopia (double vision), ptosis (eyelid
drooping), fatigable muscle weakness improved by rest, dysphagia
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Effects and Side Effects of cholinergic drugs:

DUMBELS

Diarrhea, Urination, Miosis, Bradycardia and Bronchoconstriction,

Excitation, Lacrimation, Salivation
Also remembered as: SLUDGE
Salivation, Lacrimation, Urination, Defecation, Gastric upset, Emisis
This is seen in organophosphate poisonings or nerve gas exposure

Reversed with atropine and pralidoxime (2-pam)

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