1 Anticholinergic Drugs

Muscarinic
Anticholinergic Drugs
Neuromuscular
Ganglionic
Ganglionicblockers
Ach
Nn
blockers
blockerNm
MNn
Ach
AchNn
Learninig Outcomes
Classify anticholinergic drugs
Outline pharmacodynamic
actions of anticholinergic drugs
Discuss their pharmacokinetic

properties
Define their clinical uses
List their ADRs & contraindications

Antimuscarinic Drugs
According to source
Natural Atropine Hyoscine
According to
structure
According
Semisynthetic
to selectivity
Homatropine
Tertiary amines
Non-selective
Synthetic Ipratropium, tropicamide
Quaternary ammonium Ipratropium
Selective Pirenzepine(M1) Darifenacin(M3)
Mechanism of action
Competitively block
muscarinic receptors
Smooth
Salivary,
Gastric muscle and and
bronchial,
glands and gastric heart
smoothare
intermediate
sweat glands
muscles are most
are the least.
sensitive
Pharmacodynamic Actions
CNS:-
Atropine at clinical dose, initial stimulation
followed by slower longer –lasting sedative effect
Hyoscine sedative effect

Atropine stimulates many medullary
centers,
vagal, respiratory, and vasоmotor.
High doses of atropine cause cortical excitation,
restlessness, disorientation, hallucinations, and
delirium followed by respiratory depression and
CVS:-
Atropine causes tachycardia in isolated
heart, due to blockade of M2-receptors on SA
node
In intact animals, initial bradycardia
Atropine shortens the refractory period of AV conduction
followed by tachycardia
Atropine does not influence BP. It blocks the
vasodepressor action of cholinergic agonists
Eye:-
Relaxes
Relaxescilliary muscle
pupillae abolitionmydriasis
constrictor of light reflex
& [cycloplagia].
Increase intraocular pressure
 Lachrymal secretions
Respiratory system
Atropine bronchodilation & of secretion

GIT:-
Motility
 Secretion.
Genitourinary tract:-
Atropine has relaxant action on the uriters & bladder

wall
Urinary retention can occur in older men with

prostatic hyperplasia.
Summary of Effects
Sweat glands:-
Atropine decreases sweat secretion (M3-blockade)
In children modest doses ”atropine fever”
Pharmacokinetics
Atropine and hyoscine are rapidly absorbed
from the GIT
When applied to the eyes they penetrate the
cornea.
Passage of atropine across BBB is restricted.
50% of atropine is metabolized in the liver and
excreted unchanged in urine.
Atropine has t1/2 of 3–4 h

Hyoscine is more completely metabolized and
has better BBB penetration.
Clinical Uses
CNS:-
i-Parkinsonism:-
Benzhexol,sickness
ii-Motion benztropine
Hyoscine
Clinical Uses
Ophthalmic disorders:-
Ophthalmoscopic examination of retina
Clinical uses
GIT:-
Biliary & renal colic.
Ulcer Pirenzepine
Irritable
Urinary urgency
bowel syndrome,
caused bycolonic
minor diverticular
disease
inflammatory
e.g. dicyclomine,
bladder disorders.
glycopyrrolate
Urinary incontinence
(Oxybutynin
Traveler's , Darifenacin(M3)
diarrhoea with opioid [Atropine +
diphenoxylate ]
Clinical Uses
Respiratory disorders:-
Bronchial
Pre- operative
asthmamedication
& chronicwhen
obstructive
anaesthetic
secretion
pulmonary disease
& laryngospasm
(COPD)
Ipratropium(inhalation)
Hyoscine amnesia,
Clinical Uses
Cardiovascular effects:-
Pain of myocardial infarction  depression of
SA, AV node
Sinus bradycardia
Clinical Uses
Cholinergic poisoning:-
Cholinesterase
Mushroom poisoning.
inhibitors “insecticides”.
Clinical Uses
Hyperhydrosis:-
Adverse Effects
Mydriasis, blured vision

Confusion, agitation, delirium
Dry mouth , hot flushed skin,
Constipation, urinary retention
Tachycardia
 Body temperature
The Mnemonic
Red
Mad
Dry
Full
Blind
Hot as
as
as
asaasabone
abeet
aHell
hen
Flask
bat
fire
Contra-indications
Glaucoma
Elderly people with prostatic hypertrophy
Tachycardias secondary to thyrotoxicosis or

cardiac insufficiency
Paralytic ileus.
Non selective M blockers →ulcer

Quiz 1?
A patient is brought into the emergency room. Upon
examination you find the following: a high fever,
rapid pulse, no bowel sounds and dilated pupils that
do not respond to light. His lungs are clear. His face
is flushed and his skin is dry. He is confused,
disorientated and reports 'seeing monsters'. Based
on these symptoms, you suspect he has been
'poisoned'. Which of the following, is the MOST
obvious cause of poisoning?
A. Neostigimine
B. Physostigmine
C. Atropine sulfate
D. Acetylcholine
Quiz 2?
You are working in the post anesthesia care unit

of a hospital. You have just received a patient
back from surgery and you are monitoring his
status. Knowing that the patient has received
atropine, which of the following
statements/observations is UNEXPECTED?
A. The patient is complaining of extreme thirst.
B. The patient complains he is unable to clearly see
the clock located just across from him.
C. The patient's heart rate is elevated.
D. The patient reports he has cramping and diarrhea.

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Muscarinic

Discuss their pharmacokinetic

Define their clinical uses

List their ADRs & contraindications

Hyoscine sedative effect

Atropine bronchodilation & of secretion

Atropine has relaxant action on the uriters & bladder

Urinary retention can occur in older men with

Atropine has t1/2 of 3–4 h

Mydriasis, blured vision

Dry mouth , hot flushed skin,

Constipation, urinary retention

Elderly people with prostatic hypertrophy

Tachycardias secondary to thyrotoxicosis or

Non selective M blockers →ulcer

You are working in the post anesthesia care unit

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