Drugs affecting the

Autonomic
Nervous System Unit 11:
Pharmacolo
gy
Chap 14: Sedative –
Hypnotic
1
Nervous System

 Drugs that affect the nervous system act upon the:

1. Central Nervous System (CNS)

2. Autonomic Nervous System (ANS)

2
Autonomic Nervous System

 Regulatory and self-

governing
 Without conscious thought

 Maintains internal
environment

3
Autonomic Nervous System: Divisions

1. Sympathetic System
 Fight or flight
 under stress

3. Parasympathetic System
 Rest and digest

4
Innervation

 Most organs are innervated

by BOTH Sympathetic and
Parasympathetic
 Keeps a balance of
function

 For example:
 Heart

 Eyes
5
Sympathetic Nervous System Drugs
 Adrenergic (Sympathomimetic) Drugs
 Mimic the action of sympathetic nervous system
 For example, Epinephrine (Adrenalin)

 Anti-Adrenergic (Sympatholytic) Drugs

 Block the action of sympathetic nervous system
 Division:

1. Alpha adrenergic blockers

2. Beta blockers 6
Parasympathetic Nervous System Drugs

 Cholinergic (Cholinomimetic) drugs

 Stimulate the Parasympathetic Nervous System

 Anti-Cholinergic (Cholinolytic) drugs

 Inhibit the Parasympathetic Nervous System

7
Adrenergic (Sympathomimetic)

 Mimic the action of the

Sympathetic Nervous
System

 Therapeutic uses and

adverse effects targets:
 Heart, lungs, and blood
vessels

8
Adrenergic (Sympathomimetic): Receptors

Receptor Location Stimulation

vasoconstrictions,

↑ BP,
Alpha blood vessels ↓ nasal congestion,

contraction of GIT and urinary

bladder sphincter

↑ HR
Beta 1 heart
(+) contraction

lungs bronchodilator
Beta 2
peripheral blood vessels vasodilation 9
Adrenergic (Sympathomimetic): Drugs
1. Cathecholamines
 Cannot cross Blood Brain Barrier
 Endogenous: Epinephrine, NE, Dopamine
 Exogenous (synthetic): Dobutamine (post-heart failure)
and Isoproterenol (Bronchodilators)

3. Non-Cathecholamines
 Cross the Blood Brain Barrier
 Ephedrine (Metabolife – diet pills), albuterol (anti-asthma),
and phenylephrine (decongestant) 10
Adrenergic (Sympathomimetic): Uses

Primarily used for emergency drugs

1. Cardiac arrest – stimulates the heart
2. Hypotension – increase BP
3. CHF – increase force and contraction of heart
4. Asthma – bronchodilator
5. URT Congestion – decongestant
6. Allergic reaction – vasoconstriction and decongestant
7. Hypoglycemia – glycogenolysis
8. Local bleeding – vasoconstriction
9. Obstetrics – uterine relaxant
10. Eye disorder – vasoconstriction
11
Adrenergic (Sympathomimetic): Adverse Effects
1. Cathecholamines 1. Non-Cathecholamines
 Nervousness and  Severe anxiety and
restlessness insonmia

 Angina  Tachycardia and

palpitations
 Hypertension
 Dysrhythmias
 Tachycardia
 Muscular weakness
 Hyperglycemia and cramps
 Nausea and vomiting
12
Adrenergic (Sympathomimetic): Contraindications

 Cardiac dysrythmia

 Angina

 Hypertension

 Glaucoma

 Pregnant women

 Caution with children !!

13
Adrenergic (Sympathomimetic): Cathecholamine Drugs
 Epinephrine hydrochloride
(Adrenalin Chloride)
 Drug of choice for
Anaphylaxis
 Active ingredient in OTC
asthma preparation
 Effects: (+) Alpha and Beta
recepts
 ↑ BP and ↑ HR

 ↑ blood flow to brain,

heart, and skeletal muscle
 Peripheral vasoconstriction

 (-) GIT motility 14

Adrenergic (Sympathomimetic): Cathecholamine Drugs

 Norepinephrine (Levophed)
 Strong vasoconstrictor
 Used for Hypotension and Cardiac
Arrest

 Dopamine Hydrochloride
(Intropin)
 Precursor to NE
 Dosage effects:
 Low dose – causes renal
perfusion
 Low to moderate dose –
causes increased CO
 Higher doses – increased
peripheral resistance and BP
15
Adrenergic (Sympathomimetic): Cathecholamine Drugs

 Dobutamine hydrochloride
(Dobutrex)
 Synthetic cathecholamine

 Acts directly on heart muscle

to increase the contraction

 Isoproterenol hydrochloride
(Isuprel)
 Synthetic cathecholamine

 Bronchodilator

 (+) Beta1 and Beta2 receptors

16
Adrenergic (Sympathomimetic): Anti-Cathecholamine Drugs

 Ephedrine and Pseudoephedrine

(Sudafed)
 Less potent but longer acting than
epinephrine
 Bronchodilator and Nasal
decongestant (allergic reaction)

 Phenylephrine hydrochloride
(Neo-Synephrine)
 (+) Alpha receptor
 Vasoconstrictor, decongestant,
and bronchodilator

 Albuterol (Proventil)
 Bronchodilator
17
Anti-Adrenergic (Sympatholytic)

 Block the effect of sympathetic nervous system

 Treatment goal is to reduce pathologic response to

activity, stress, and other stimuli

 Two major types:

1. Alpha-adrenergic blocking agent

2. Beta-adrenergic blocking agent 18

Anti-Adrenergic (Alpha-adrenergic): Uses

 Mild to moderate hypertension

 Benign prostatic hypertrophy (BPH)
 Migraine headaches
 Pheochromocytoma – tumor of the adrenal glands
 Increased secretion of Epinephrine and NE
 CHF with diuretics
 Peripheral vascular disorders (frostbites)
19
Anti-Adrenergic (Alpha-adrenergic): Adverse Effects

 Nasal congestion

 Nausea

 Vomiting

 Postural hypotension

20
Anti-Adrenergic (Alpha-adrenergic): Contraindications

 Hypersensitivity
 Sepsis
 Vascular disease
 Hepatic or renal disease
 Atherosclerosis
 Hypertension
 Anemia
 Pregnancy and lactating

 Caution to children and elderly 21

Anti-Adrenergic (Alpha-adrenergic): Important Drugs

 Phentolamine mesylate (Regitine)

 Prevents tissue necrosis after extravasation of IV NE
 Prevents and controls hypertension caused by Pheochromocytoma

 Doxazosin (Cardura), Prozosin (Minipress), and Terazosin (Hytrin)

 Acts on the periphery
 Treats hypertension or BPH

 Sumatriptan (Imitrex)
 Vascular headache suppressant to treat migraines
22
Anti-Adrenergic (Beta-Adrenergic)
 Block the effect of Adrenergic stimulation of Beta1 or Beta2

 Competes with NE receptor site

 Beta blockers
 Decrease in BP, heart contraction, and CO

 Beta2 blockers causes vasodilation in skeletal muscles

 Treatment for Angina pectoris and decrease BP 23

Anti-Adrenergic (Beta-Adrenergic): Uses

 Angina – decrease in O2 demand, heart contraction, HR, BP

 Dysrhythmias – slow sinus node, prolongs AV conduction

 Hypertension – lowers BP

 MI – to decrease Cathecholamin-induced dysrhythmias

 Glaucoma – decreases IOP

 Migraine – unclear

 Palpitation and Tremor – unapproved anti-anxiety

24
Anti-Adrenergic (Beta-Adrenergic): Adverse Effects
 Bradycardia  Fatigue

 Shortness of breath  Nausea

 Edema  Vomiting

 Reduced tolerance to  Bronchospasm

exercise
 Impotence
 Hypoglycemia
 Depression
 CHF
 Sleep disorders
 Orthostatic hypotension

25
Anti-Adrenergic (Beta-Adrenergic): Contraindication

 Diabetes with insulin

 Kidney and liver disease (metabolism and excretion)

 Alcohol, CNS depressant, and OTC decongestant

 Not affective for African-Americas

26
Anti-Adrenergic (Beta-Adrenergic): Important Drugs
 Propranolol hydrochloride (Inderal)
 Treats hypertrophic subaortic
stenosis, hypertension, angina,
dysrythmias, and MI

 Metoprolol tartrate (Lopressor)

 Treats hypertension and
dysrythmias

 Atenolol (Tenormin)
 Treats hypertension, angina, and
MI

 Timolol maleate (Timoptic)

 Eye drop for treatment of 27
Glaucoma
Parasympathetic Nervous System

 75% of all parasympathetic

fiber are in the Vagus Nerve

 Functions in Rest and

Repair

 Found in Digestion,
Excretion, Cardiac
deceleration, and
Anabolism
28
Parasympathetic Nervous System

 Acetylcholine is the
neurotransmitter

 Stimulation
 Constricted pupils

 Contraction of GIT smooth

muscle
 Bronchoconstrictor

 Bradycardia

 Increased glandular secretion

(except sweat)
29
Cholinergic (Parasympathomimetic): Receptors
1. Nicotinic (resembles nicotine)
 Tachycardia
 Hypertension
 Peripheral vasosconstriction

3. Muscarinic
 Bradycardia
 Hypotension
 Increase salivation 30
Cholinergic (Direct-acting): Effects

 Decreased heart rate

 Increased GIT muscle

and secretion
 Relaxation of sphincters

 Increased respiratory
secretions
 Constriction of pupils
31
Cholinergic (Direct-acting): Uses

 Glaucoma

 Gastric reflux

 Prevention of nausea & vomiting

 Related to chemotherapy

32
Cholinergic (Direct-acting): Adverse Effects
 Nausea and Vomiting  Increased sweating

 Diarrhea  Impaired vision

 Wheezing & shortness  Poor night vision
or breath
 Anxiety and restlessness
 Bradycardia
 Sleep disturbance
 Hypotension
 Convulsion
 Headache
 coma
 Increased salivation
33
Cholinergic (Direct-acting): Contraindication

 Diabetes mellitus

 Coronary artery disease (bradycardia)

 MI

 Heart block

 Intestinal obstruction

 Peptic ulcer

 Asthma (increased secretion)

34
Cholinergic (Direct-acting): Drugs
 Bethanechol chloride (Urecholine)
 Treats urinary retention and
glaucoma

 Pilocarpine hydrochloride (Pilocar)

 Decreases IOP in Glaucoma

 Carbachol intraocular (Miostat)

 Treats Glaucoma

 Metoclopramide hydrochloride
(Reglan)
 Prevents chemotherapy-induced
nausea and vomiting
 Treats Acid-reflux disease 35
Cholinergic (Indirect-acting):

 Inhibit the action of

Acetylcholinesterase
 Enzyme that breaks down
acetylcholine.
 Prolongs the effects of
Ach

36
Cholinergic (Indirect-acting): Uses

 Myasthemia gravis – autoimmune

 Decreased neuromuscular transmission

 muscle weakness

 Glaucoma

 Bladder emptying

37
Cholinergic (Indirect-acting): Adverse Effects

 Hypotension

 Miosis – constriction of the pupils

 Vasodilation

 Bradycardia

 Intestinal spasm

 Increased salivation

 diaphoresis
38
Cholinergic (Indirect-acting): Contraindications

 Diabetes mellitus

 Coronary artery disease

 Heart block

 Urinary tract obstruction

 asthma

39
Cholinergic (Indirect-acting): Important drugs

 Neostigmine bromide
(Prostigmin)
 Treats urinary retention

 Edrophonium chloride (Tensilon)

 Diagnoses Myasthenia gravis

 Pyridostigmine bromide
(mestinon)
 Drug of choice for Myasthenia
gravis
40
Anti-cholinergic (Parasympatholytic):
 Sometimes called
Muscarinic antagonist
(blocker)
 Competes with Ach at the
receptor site
X

 Depresses the CNS X

 Targets the skin, eyes, GIT,

urinary bladder, bronchi, and
heart 41
Anti-cholinergic (Parasympatholytic): Uses

 Widespread effects on the body. Thus, limits the use

 Treats GIT disorders by increasing motility, secretion, with

accompanying pain.

 Urinary disorder – antispasm

 Respiratory disorder – causes bronchodilation

 Cardiac disease – treats bradycardia

 Parkinson’s – decreases salivation and tremors

42
Anti-cholinergic (Parasympatholytic): Adverse Effects

 Dry mouth

 Constipation

 Difficulty urination

 Tachycardia

 Intolerance to heat

43
Anti-cholinergic (Parasympatholytic): Contraindication

 Glaucoma – drugs causes dilatation of pupil

 Hypersensitivity to drug

 Chronic lung, renal, and liver disease

 Myasthenia gravis

 Heart disease

44
Anti-cholinergic (Parasympatholytic): Drugs
 Atropine sulfate
 Used to pre-operatively to dry secretions
 Treats bradycardia

 Belladonna tincture
 Treats GIT disorders

 Hemoatropine (spectro-homatropine)
 Eye drops to produce Mydriasis (pupil dilation) and
cycloplegia (paralysis of ciliary muscle) 45