Dr.

Jagan
Associate Professor of Pharmacology
HOD – Para clinical Department
Texila American University
 Learning Objectives
• Classify Muscarinic Receptor Antagonist.
• List the major clinical indications and Side effects of
muscarinic receptor antagonist.
• Contraindications for the use of muscarinic receptor
antagonists.
• List one antimuscarinic agent promoted for each of the
following uses: to produce mydriasis and cycloplegia; to
treat parkinsonism; asthma; bladder spasm and OP
poisoning.
• List the signs, symptom and treatment of atropine
overdose.
 Parasympatholytics
 Anticholinergic drugs
 Competitive antagonists.
 Classification:
1.Natural Alkaloids
2.Semi -synthetic Derivatives
3.Synthetic Compounds
1. Natural Alkaloids:
•Atropine, Hyoscine (Scopolamine)
2. Semisynthetic Derivatives:
•Homatropine,
•Atropine metho nitrate,
•Hyoscine butyl bromide
•Ipratropium bromide
•Tiotropium bromide.
3.Synthetic Compounds:
a) Mydriatic – Cyclopentolate,Tropicamide
b) Antisecretory – Antispasmodic
i) Quaternary Compounds
Propantheline,Oxyphenonium,Clidinium
Pipenzolate , Glyclopyrrolate
ii) Tertiary Amines
Dicyclomine,Oxybutynin,Flavoxate,
Pirenzepine, Telenzepine
c) Antiparkinsonism Drugs
Benztropine
Trihexyphenidyl or Benzhexol
Procyclidine
Biperiden
1. Natural Alkaloids:
1) Atropine
Atropa belladonna
(Deadly night shade)
Datura stramonium

2) Hyoscine
(Scopolamine)
Hyoscyamus niger
 Pharmacokinetics
1. Absorption:
• Well absorbed orally & cross the
conjunctival membrane
• Scopalamine Transdermal.
2. Distribution:
• Widely distributed
• Scopalamine CNS
3. Metabolism:
• 50% Atropine & 80% Scopalamine
Conjugation (Phase-II).
• Black rabbits atropine esterase.
4. Excretion:
• 50% unchanged in urine
• Plasma t1/2 : 3 hr
• Effect on eye persists for 72 hrs
 Mechanism of Action
• Competitive blockade of Muscarinic
receptors (M1- M3).
• IP3- DAG M1 – M3.

• CAMP M2
 Pharmacological actions
1.CNS :
High dose atropine CNS stimulation
Therapeutic doses Scopalamine
drowsiness, Amnesia
a. Depression of vestibular
excitation - motion sickness
b. Blocks cholinergic activity in
basal ganglia: tremor and
rigidity of parkinsonism
2. Cardiovascular System
 Heart Rate:
• M2 receptor blockade Tachycardia.
• Shortens refractory period and facilitates AV
conduction.
 BP:
• BP : Tachycardia and Vasomotor

• BP : Release of histamine and Vasodilatation

3.Eye:
• Passive mydriasis
• Abolition of light reflex
• Cycloplegia – 7 days
• Decrease lacrimal secretion
Cycloplegia – 7 days
4.Smooth Muscle:
a)GIT:
• M3 Blockade
• Constipation
b) Urinary bladder :
• M3 Blockade
• Hinder the micturation
C) Respiratory System:
• M3 Blockade
• Broncho-dilatation
• Reduce secretions
6.Glands:
• M3 Blockade
• Sweating , Salivary, Lacrimal, Gastric
 Therapeutic Uses
1.Central Nervous System
A. Parkinson’s Disease
Trihexyphenidyl (Benzhexol) : 1-5 mg/day o.p
Procyclidine : 5-15mg/day o.p
Benztropine: 1-5 mg/day o.p
• Useful in improving tremor and rigidity
• Used alone in mild cases or with Levodopa
B. Motion sickness: Scopalamine
• 0.6-1.0 mg s.c
• Transdermal patch 0.5 mg/ 3 days
C. Preanesthetic medication:
• Antisecretory, vagolytic
• Glycopyrrolate – 0.1- 0.3 mg/ I.M
F. Amnesia with Twilight sleep
2.Ophthalmological Uses:
a)As mydriatic: To test refraction errors Tropicamide,
cyclopentolate, Homatropine
b) Adhesions between Iris – lens
3. CVS:
• A-V block
4. Respiratory disorders: (B.A & COPD)
Atropine methonitrate, Ipratropium, Tiotropium
5.Gastro intestinal Disorders
a) Peptic Ulcer :Pirenzepine, Telenzepine
 
b) As antispasmodics:
Abdominal cramps, Hypermotility
Intestinal and renalcolic
Oxyphenonium, Propantheline, Clidinium
bromide
 
6.Urinary Disorders
Urinary urgency, incontinence:
Neurogenic bladder, Spinabifida,
Nocturnal enuresis
Oxybutynin, Tolterodine,
Flavoxate, Propiverine
7. Treatment of Ops poisoning:
• Atropine - specific antidote
• 1-2 mg/i.v/ every 15 min till dilatation of pupil (or)
atropinisation
8.Mushroom poisoning:
• 1-2mg/i.v atropine
9. Hyperhidrosis:
 
 Adverse Drug Reactions

• Broad range of actions. Hence, side effects are

inevitable .
Most common side effects:
• Dryness of mouth
• Blurred vision and photophobia
• Constipation
• Urinary retention
• Decrease all secretion
 Atropine poisoning
 Symptoms
1. CNS: Restlessness, Hallucination
2. CVS: Hypotension , Tachycardia
3. EYE: Dilated pupil, Photophobia, Blurred vision
4. GLANDS: Difficulty in swallowing and taking,
Flushed and hot skin ( face and neck)
4. Urinary: Difficulty in micturation
5. GIT: Constipation
High doses:
CVS collapse, respiratory depression,
convulsions, coma
Diagnosis:
Methacholine 5 mg or Neostigmine 1 mg.
Treatment:
1.Gastric lavage with tannic acid
2. Dark quiet room, Ice bag
3. General supportive measures,
4. Diazepam, - seizure control
5. Physostigmine: 1-3 mg s.c / i.v 4 hr
Contra Indications:
1.Narrow angle Glaucoma
2.BPH
 Drug interaction
Delayed gastric emptying
Antihistamine,
Tricyclic antidepressants
Phenothiazines.
MAO inhibitors
 1
In Ophthalmology OPD doctors are used to
administered following drug for routine
examination of EYE. That drug should be mydriatic
and cycloplegic. Which one of the following drugs
has that property:
a) Tropicamide
b) Pilocarpine
c) Phenylephrine
d) Dipivefrine
 2
An 80-year-old man is increasingly forgetful, and his wife
is afraid he is developing Alzheimer’s disease. You are
considering prescribing an anti- AChE drug to see if this
will decrease his forgetfulness. Before making this
prescription, you want to be sure that these drugs are
suitable given the patient’s medical history. Of the
possible pre-existing conditions listed below, you should
be least concerned about
A) Asthma
B) Weak atrioventricular conduction
C) Glaucoma
D) Obstruction of the GI tract
 3
You have successfully prescribed neostigmine to a young
patient with myasthenia gravis, and her muscle strength
has improved markedly. However, she also exhibits
cardiovascular and gastrointestinal signs of excessive
vagal tone, which you would like to block with atropine.
Which of the following risk factors in prescribing
atropine is most important to you?
A) Dry mouth
B) Ocular disturbances
C) Paralysis of the respiratory muscles
D) CNS Excitement
 4
Antimuscarinic mydriatics, such as tropicamide,
are useful in ophthalmological examinations.
Prior to administering tropicamide, it would be
most important to know
A) If the patient has angle-closure glaucoma
B) If the patient has open-angle glaucoma
C) If the patient is taking a cholinomimetic
miotic drug
D) If the patient is taking alcohol
 5
Which of the following antimuscarinic drug is
often effective in preventing or reversing
vestibular disturbances, especially motion
sickness?
a) Atropine
b) Ipratropium
c) Scopolamine
d) Homatropine
 6
A young man broke his leg in an accident, causing
severe muscular spasm that necessitated relaxation of
the muscle with a competitive nicotinic receptor
antagonist before the fracture could be set. At the end
of the orthopaedic procedure, the doctor restored
neuromuscular transmission by administering:
A) Succinylcholine
B) Carbachol
C) Physostigmine
D) Neostigmine
 7
Accepted therapeutic indications for the use of
antimuscarinic drugs include all of the
following except

A. OP poisoning
B. Motion sickness
C. Parkinson’s disease
D. Postoperative bladder spasm
 8
A 38-year-old farmer is brought to the ER by his wife with symptoms
of sudden difficulty breathing, sweatiness, and anxiety. He was
spraying insecticide when this happened. It has been 25 minutes
since the symptoms started. The patient is emergently intubated and
given atropine and another medication that acts to reactivate
acetylcholinesterase. What medication is it?
A) Physostigmine
B) Propranolol
C) Pralidoxime
D) Phenylephrine
E) Pancuronium
 9
A 78-year-old man with Parkinson disease experiences
worsening of his symptoms. He is already taking levodopa.
Since the disease is characterized by degeneration of
dopaminergic neurons, leading to the lack of inhibition of
cholinergic neurons, the addition of which medication is
likely to help alleviate the patient’s symptoms?
A) Benztropine
B) Reserpine
C) Doxazocin
D) Timolol
E) Tubocurarine
 10
Receptor actions of acetylcholine are mimicked by nicotine at
which one of the following sites?
A) Adrenal medullary chromaffin cells
B) Urinary bladder smooth muscle cells
C) Iris circular (constrictor) muscle
D) Heart sinoatrial pacemaker cells
 11
Which one of the following agents, when applied topically to
the eye, would cause both mydriasis and cycloplegia?
A) Phenylephrine
B) Carbachol
C) Prazosin
D) Atropine