AUTONOMIC SYSTEMS

AND DRUGS-2
Epinephrine
Adrenergic
Norepinephrine
Acetyl choline Cholinergic
 HR Contractility Transmitter(s)

Sympathetic Norepinephrine
Epinephrine

Parasympathetic Acetyl Choline

 Vascular smooth muscle

Sympathetic only (or nearly so)

Synthesized from: Tyrosine

Rate limiting reaction: Tyrosine hydroxylase

COMT - catechol-O-methyltransferase
MAO - monoamine oxidase
Reuptake into the nerve ending by
an active transport system
Reserpine Inhibits storage in vesicles

-Methyldopa False transmitter

Guanethidine Inhibits NE release

Amphetamine Stimulates NE release

Imipramine Inhibits NE reuptake

Fluoxetine Inhibits serotonin reuptake

 Alpha Beta
Generally excitatory Generally inhibitory
Exception: Exception: beta1 in
intestinal smooth the heart
muscle
Muscarinic Nicotinic
Acetylcholinesterase
Cholinergic agonists
•Bethanechol
•Pilocarpine
•Carbachol
Antimuscarinics
•Atropine
•Scopolamine
Anticholinesterases
•Neostigmine
•Organophosphates (e.g. DFP)
Neuromuscular blockers
•Tubocurarine
•Pancuronium
•Succinyl Choline
Parasympathomimetics: limited uses
•Glaucoma
•Pupillary constriction (meiosis)
Not used for:
•Bronchial Asthma
•Coronary Insufficiency
•Peptic Ulcer
•Hyperthyroidism
Atropine; Scopalamine
Therapeutic uses:
•Motion sickness
•Pupillary dilation
•Parkinson’s Disease
Side effects:
•Dry mouth
•Blurred vision
•Tachycardia
•Urinary retention
•Constipation
Reversible Irreversible
Neostigmine Organophosphates
Physostigmine (e.g. DFP)

Predict effects on:

• Eye
• GI tract
• Urinary tract
• Skeletal muscle
 • Atropine
• Pralodoxime

Reversal of atropine poisoning:

• Physostigmine
• Glaucoma
• Paralytic ileus
• Mysathenia gravis
 Pancuronium Succinylcholine

Mechanism Competitive Depolarizing

Onset 1-2 min 20-40 sec

Duration 30-60 min 2-5 min

Side BP tendency Cardiac arrhythmia

Effects Prolonged apnea
Malignant
hyperthermia
Autonomic reflexes modulate drug responses

BP SNS PSNS

BP SNS PSNS
What is the treatment of choice
for anaphylactic shock?
Epinephrine

Why?
It is the only drug that addresses the
most serious manifestations:
• increases cardiac output
•  relaxes constricted bronchioles
• 1 constricts capillaries
2-Selective Adrenergic Agonists

• Albuterol
• Terbutaline

Bronchial dilators
Uterine relaxant (ritodrine)
1 Adrenergic Agonists
•Phenylephrine
•Ephedrine

Therapeutic uses:
•Nasal decongestants
•Used with local anesthetics
•Local hemostasis
•Mydriatic
•Glaucoma
•Vasopressor
•Appetite suppressant
Alpha blockers
• Prazosin (1)
• Phenoxybenzamine (12)
• Phentolamine (12)

Hypertension
Beta blockers:
•Propranolol (1 2)
•Metoprolol (1 )
•Atenolol (1 )
•Timolol (1 2)
Therapeutic uses:
•Arrhythmia
•Angina pectoris
•Hypertension
Alpha blockers
• Postural hypotension
• Tachycardia
• First dose (prazosin)
Beta blockers
• Cardiac depression
• Asthma attack
• Nightmares, lassitude, depression
• Angina pectoris (abrupt withdrawal)
 Tolcapone

Carbidopa Selegiline
Reduced GI - nausea and vomiting
with
carbidopa Hypotension
Dyskinesias
Psychiatric reactions
 Drugs to Know

Levodopa
used in combination
Carbidopa
Amantidine DA reuptake inhibitor (?)

Bromocryptine DA receptor agonist

Selegiline MAO-B inhibitor
Tolcapone COMT inhibitor