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PARASYMPATHOLYTICS
Dr. Rukhsana Anwar
Assistant Professor
University College of Pharmacy
University of the Punjab
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Parasympatholytics
• Cholinergic antagonists/ Cholinergic blockers/
Anticholinergics
• Bind to cholinergic receptors i.e. muscarinic
receptors (M1, M2 and M3 receptors) and
nicotinic receptors but do not trigger and
produce receptor mediated intracellular effects.
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Classification
1. Anti muscarinic Drugs
Atropine, Scopolamine (Hyoscine): Natural Alkaloid
Glycopyrrolate, Ipratropium, Tiotropium,
Benztropine: Quaternary amines
Pirenzipine, Dicyclomine, Tropicamide: Tertiary
amines
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2. Anti nicotinic Drugs
a. Ganglion Blockers (Hexamethonium)
b. Neuromuscular blockers (Tubocurarine)
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ANTI MUSCARINIC DRUGS
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Atropine (Non selective
Mucarinic blocker)
• Natural source: Atropa belladonna
Datura stramonium
• An alkaloid having tertiary amine
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Pharmacokinetics
• well absorbed through gut, blood brain barrier
and conjunctival membrane.
• Half life: 2hrs
• 60% of the dose is excreted unchanged in urine
• Effect on eye iris and ciliary muscles persists for
72 hours or longer other effects decline rapidly.
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Pharmacodynamics
Mechanism: Binds to muscarinic receptors and causes
blockade of effects of cholinomimetics as it competes with
acetylcholine for muscarinic receptors.
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Effect on Organ systems
1. Eye
• Mydriasis (Dilation of pupil)
• Diminished light reflex
• Cycloplegia (inability to focus for near vision due to
weakening of contraction of ciliary muscles of eye)
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2. GIT
• Decrease salivary secretions / dry mouth
• Spasmolytic/ temporary intestinal paralysis
• Used in the past to reduce acid secretions but now obsolete.
3. Urinary System:
• Reduces urinary bladder motility
4. Cardiovascular:
• Moderate to high doses cause tachycardia
• Little effect on blood pressure 11
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5. Secretions
• Salivary glands: reduced secretions and dry mouth
(xerostomia)
• Sweat glands: suppression of thermoregulatory
sweating process leading to high body temperature
(Atropine Fever)
• Lacrimal glands: Dry, sandy eyes
The tissues most sensitive to atropine are salivary,
bronchial and sweat glands. Secretion of acid by gastric
parietal cells is least sensitive.
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6. CNS
In therapeutic doses, atropine has minimal stimulant
effects on CNS
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Clinical Uses
• For ophthalmoscopic examination of retina and accurate
measurement of refractive errors
• Antispasmodic
• Antidote for cholinergic agonists (Physostigmine)
• Preoperatively to block respiratory secretions
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Adverse Effects
• Blurred vision
• Sandy eyes
• Urinary retention
• Constipation
• Tachycardia
• Restlessness, confusion and hallucinations
• Atropine fever/ Hyperthermia
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Atropine Toxicity
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Other Antimuscrinics
Scopolamine (Hyoscine)
• Produces similar peripheral effects as atropine but has
marked effect on CNS causing drowsiness and amnesia
• Vestibular disturbances like Motion sickness appear to
involve muscarinic cholinergic transmission so it is
effective in preventing or reversing these disturbances
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Ipratropium & Tiotropium
• Quaternary amines, because of positive charges, do
not enter systemic circulation or CNS.
• Given by inhalation
• Act as bronchodilator for maintenance treatment of
chronic pulmonary obstructive disease
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Benztropine, Trihexphenidyl
• Parkinson’s disease results from relative excess of
cholinergic nerves and deficiency of dopaminergic
activity in basal ganglia-striatum system.
• Combination of Antimuscrinic agent and dopamine
precursor is suitable therapy for Parkinson’s disease.
• Benztropine, Trihexphenidyl are centrally acting
Antimuscrinic agents that are used as adjunctive therapy
in treatment of Parkinson’s disease.
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Oxbutynin, Tolterodine
• By blocking muscarinic receptors in bladder intravesicular
pressure is lowered, bladder capacity is decreased and
frequency of bladder contractions is reduced.
• Oxbutynin used to relieve bladder spasm after surgery and to
reduce involuntary voiding in patients with neurologic
disease.
• Tolterodine is used in adults to treat urinary incontinence.
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References
• Basic and clinical pharmacology, by Bertram G. Katzung
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