ANS Part 2

Sudan International
University
Faculty of Dentistry
Drugs Acting on Autonomic

Nervous System
Sara Abdalla
M.Sc. Cancer and Therapeutics, Queen Mary University of London
M.Sc. Clinical Pharmacy, Queen’s University Belfast
Anticholinergic Agents
(Cholinergic Receptor
Blockers)
1. Antimuscrinic Agents
• These drugs competitively block the binding of Ach to muscarinic
receptors, producing an anticholinergic response.
• Classification of antimuscarinic agents:

• Natural alkaloids: Atropine, scopolamine (hyoscine).
• Semisynthetic derivatives: Ipratropium bromide.
• Synthetic compounds: Pirenzepine
Effects of muscarinic Antagonists
1. CNS: atropine reduces the cholinergic overactivity in the

basal ganglia and suppresses vestibular disturbances
associated with the movement. However, large doses can
produce excitement, restlessness, agitation, hallucinations,
medullary paralysis, coma, and death.
2. CVS: At low doses, atropine causes initial bradycardia due

to the blockade of presynaptic muscarinic receptors (M1)
on vagal nerve endings. In therapeutic doses, tachycardia
is seen due to the blockade of M2 receptors of the heart; it
also improves A–V conduction. In high doses, flushing of
the face and hypotension may occur due to cutaneous
vasodilatation. Arterial blood pressure is unaffected
because most resistance vessels have no cholinergic
3. Exocrine Glands: All secretions under cholinergic influence are
reduced due to blockade of M3 receptors, i.e. sweat, salivary,
nasal, throat, bronchial, gastric, lacrimal, etc. The skin and
mucous membranes become dry.
4. Eye: Mydriasis and rise in IOP can occur in patients with narrow-angle
glaucoma
5. Smooth muscle: Antimuscrinic agensts exert inhibitory effects on smooth

muscle and cause relaxation of the bronchial, biliary and urinary tract smooth
muscles.
Actions of Atropine
Clinical Uses of Antimuscrinic
Agents
• Treatment of sinus bradycardia e.g. after mysocardial infraction (Atropine).
• To dilate pupile (topical Tropicamide or Cyclopentolate).
• Neurological prevention of motion sickness (Scopolamine).
• Hypersalivation: decrease salivary secretion e.g. during dental
procedures.
Clinical Uses of Antimuscrinic
Agents
• Asthma and COPD (Ipratropium or Tiotropium).
• As antispasmodics in dysmenorrhoea, intestinal and
renal colic.
• As preanathesia medication to prevent vagal bradycardia
during anaesthesia and laryngospasm by decreasing
respiratory secretions (atropine or scopolamine).
• Treatment of Parkinsonism (Benzhexol or Benztropone).
Adverse Effects and
Contraindications
1. CNS: With large doses produce restlessness, excitement,
delirium and hallucinations.
2. CVS: Tachycardia, palpitation and hypotension.
3. GIT: Dryness of mouth and throat, difficulty in swallowing,
constipation, etc.
4. Eye: Photophobia, headache, blurring of vision; in elderly
persons with shallow anterior chamber, they may precipitate
acute congestive glaucoma.
5. Urinary tract: Difficulty in micturition and urinary retention,
especially in elderly men with enlarged prostate.
2. Ganglionic Blockers
• Act at neuronal-type nicotinic receptors of the autonomic ganglia
(block para-sympathetic and sympathetic ganglia) and produce
widespread complex effects.
Figure: Sites of action of Ganglionic Blockers
• The ganglionic blockers have ‘atropine-like’ action on the heart

(palpitation and tachycardia), eye (mydriasis and cycloplegia), GIT
(constipation and dryness of mouth), bladder (urinary retention),
Clinical Applications of
Ganglionic Blockers
• No selective ganglion blockers are available till now. Hence,
they are rarely used in therapy.
• Nicotine: is of no value in clinical practice except in the form

of transdermal patches and chewing gum for the treatment
of tobacco addiction.
Key Points for Dentists
• Patients on anticholinergics should be advised to maintain good oral
hygiene because they can cause dry mouth (Xerostomia).
• Anticholinergic drugs should not be used in patients with glaucoma, and

elderly males with benign prostatic hyperplasia.
3. Skeletal muscle relaxlants
• Physiology of skeletal muscle contration
Skeletal Muscle Relaxants
Centrally Acting Skeletal Muscle
Relaxants
• Baclofen, benzodiazepines, Gabapentin, Methocarbamol, etc.
• They are used to reduce spasms associated with temporomandibular

joint pain, cerebral pain, cerebral palsy, trauma, muscular stain, and
tetanus.
Neuromuscular Blockers
1.Depolarizing Blockers
• Mechanism of action: They act as a partial agonist at the receptors,
hence causing initial fasciculations and later paralysis due to
prolonged depolarization. With continuous exposure to the drug, the
membrane becomes desensitized and the muscle becomes relaxed.
• They can be classified according to their duration of action into:

• A) Long-acting: Pancuronium, Doxacurium.
• B) Intermediate-acting: Vecuronium, Atracurium.
• C) Short-acting: Mivacurium.
Adverse Effects
1. Muscle pain due to initial fasciculations.
2. Increased IOP due to contraction of external ocular muscles.
3. Aspiration of gastric contents may occur due to increased gastric
pressure.
4. Hyperkalaemia due to K+ released into the blood.
5. Sinus bradycardia due to vagal stimulation.
2. Non-depolarizing Blockers
(Competitive Blockers)
• They function by competitively antagonizing the actions of ACh at
the neuromuscular junction.
• Uses:
1. Adjuvant to general anesthesia.
2. In dental procedures to allow manipulation of bone fragments in
fracture of mandible and to facilitate opening of the mouth.
3. Tetanus and status epilepticus not controlled by other drugs.
Adverse Effects
1. Hypotension.
2. Respiratory paralysis.
3. Bronchospasm.
4. Aspiration of gastric contents.
• Indirectly acting chominomimetics (anticholinesterases) are used to

reverse the effects of competitive blockers by increasing the
concentration of ACh.
3. Botulinum Toxin A
• The toxin prevents the release of ACh into the synaptic cleft by
inhibiting the proteins necessary for the release of ACh. Thus it
normalises the tone in hyperreactive or spastic muscles when given
locally.
• Adverse effects are pain at the site of injection, muscle paralysis,

myalgia and occaionally rashes.
Directly Acting Agents
Dantrolene
• Dantrolene inhibits depolarization-induced Ca2+ release (decreasing

the intracellular calcium) concentration and produces skeletal muscle
relaxation.
• Used in malignant hyperthermia and reduce spasm in multiple
sclerosis, cerebral palsy, and spinal injuries.
• Side effects are drowsiness, diarrhea, dizziness, headache, fatigue,
and rarely hepatotoxicity.

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Sudan International

Drugs Acting on Autonomic

• Classification of antimuscarinic agents:

1. CNS: atropine reduces the cholinergic overactivity in the

2. CVS: At low doses, atropine causes initial bradycardia due

5. Smooth muscle: Antimuscrinic agensts exert inhibitory effects on smooth

Figure: Sites of action of Ganglionic Blockers

• The ganglionic blockers have ‘atropine-like’ action on the heart

• Nicotine: is of no value in clinical practice except in the form

• Anticholinergic drugs should not be used in patients with glaucoma, and

• They are used to reduce spasms associated with temporomandibular

• They can be classified according to their duration of action into:

• Indirectly acting chominomimetics (anticholinesterases) are used to

• Adverse effects are pain at the site of injection, muscle paralysis,

• Dantrolene inhibits depolarization-induced Ca2+ release (decreasing

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