Anticholinergic

Drugs
• Drugs that block or inhibit the actions of
acetylcholine (ACh) in the parasympathetic
nervous system (PSNS)
• Also called cholinergic blocking agents or
parasympatholytics
 Mechanism of
Action
• Competitive antagonists
• Compete with acetylcholine
• Block acetylcholine at the
muscarinic receptors in the PSNS
• Reversible blockade of acetylcholine at
muscarinic receptors by competitive
binding
• (reversal by increasing acetylcholine or
agonist ----> decreased blockade)
• Once these drugs bind to receptors, they
inhibit nerve transmission at these receptors.
 Atropine
• Prototype antimuscarinic drug - derived
from Atropa belladonna (deadly nightshade)
and Datura stramonium (thorn apple)
• History:
• during the Italian renaissance dilated
pupils were considered desirable
• plant extracts were used as cosmetic eye
drops
• hence the name belladonna or "beautiful
lady" in Italian
 Actions
Cardiovascular effects-
• Decreased cardiovascular response to vagal
stimulation resulting in tachycardia
• Mainly, tachycardia due to antagonism of
the vagal affect.

• Vascular
– no (direct) effect
– except, dilate cutaneous vessels (red as a
beet)
– block hypotensive effect of muscarinic
 Actions
CNS –
• At normal doses atropine stimulates medullary
centers, However, at higher doses produce
excitement, agitation, hallucinations and
coma.
• Depresses vestibular excitation and has
anti motion sickness properties
• Supresses tremor and rigidity of
parkinsonism by blocking cholinergic
overactivity in basal ganglia.
 Actions
Eye:
• Dilated pupils (mydriasis)
• Blocks muscarenic innervations on the circular
muscles (Mydriasis) and relaxes cilairy muscles
(Cycloplegia)
• worsens glaucoma

Gastrointestinal:
• Relax smooth muscles of GI tract
• Decrease intestinal and gastric secretions
• Decrease motility and peristalsis
• antispasmodic effect
•  Sphincter contraction
 Actions
Respiratory system -
• Decreases bronchial secretion (used as
preanesthetic Medication,COPD)
• Dilated bronchial airways (used for treatment of
Asthma)
Genitourinary -
• Relaxes detrusor muscle
• Increased constriction of internal sphincter
• Result: urinary retention
• Relaxation of smooth muscles of ureters.
• Therefore, they are contraindicated for prostate
hypertrophy patients.
Glandular –
•  Salivary secretion (Dry mouth)
•  gastric Acid (used for Peptic Ulcer )
•  Sweating  Dry skin  Fever in infants and
children.
•  Bronchial Secretion (used for COPD)
 Therapeutic Uses
Central Nervous System Disorders-
• Parkinson’s disease – Benztropine,
Trihexyphenidyl
• Those who cannot take Levodopa
• Helpful in decreasing salivation, spasticity
and tremors
• Motion Sickness (Scopolamine)
• Drug-induced extrapyramidal reactions(due
to antipsychotics)
 Therapeutic Uses
CVS –
• Atropine is used to increase heart rate
in symptomatic bradycardias.
• Sinus node dysfunction
• Symptomatic second-degree heart block
• Sinus or nodal bradycardia (due to
myocardial infarction)
 Therapeutic Uses
Respiratory system-
• Decreased secretions from nose, mouth,
pharynx, bronchi
• Relaxed smooth muscles in bronchi
and bronchioles
• Decreased airway resistance
• Bronchodilation
Respiratory agents are used to
treat:
• Exercise-induced
bronchospasms
• Chronic bronchitis
• Asthma
• Chronic obstructive
 Therapeutic Uses
Gastrointestinal:
• Blockade of PSNS results in:
• Decreased secretions
• Relaxation of smooth muscle
• Decreased GI motility and peristalsis
Gastrointestinal agents are used to
treat:
• Peptic Ulcer: Pirenzepine
• As antispasmodic :Butylscopolamine
• Irritable bowel disease: Propantheline
• GI hypersecretory states
 Therapeutic Uses
Urologic disorders-
• Antispasmodic effects seen in overactive
bladder and in urinary incontinence -
Oxybutynin
• Detrusor hyper-reflexia,
• Enuresis
-Increase bladder capacity
-Decrease bladder pressure
 Therapeutic Uses
Opthalmological Disorders-
• Homatropine,tropicamide
• Accurate measurement of refractive error
in uncooperative patients (e.g, children)
• Examination of retina (Mydriasis)
 Side Effects of anticholinergics
Body System Side/Adverse Effects
Cardiovascular Increased heart
rate, dysrhythmias

CNS CNS excitation,

restlessness, irritability,
disorientation,
hallucinations,delirium
 Side Effects of anticholinergics
Body System Side/Adverse Effects
Eye Dilated pupils, decreased
visual accommodation,
increased intraocular pressure

Gastrointestinal Decreased salivation,

decreased gastric secretions,
decreased motility
 Side Effects of anticholinergics
Body System Side/Adverse Effects
Genitourinary Urinary retention

Glandular Decreased sweating

Respiratory Decreased bronchial

secretions
 Toxicity of Anticholinergics
• Anticholinergic overdose syndrome
(Belladona poisoning- consumption of seeds
or berries of belladona or dhatura plant) is
characterized by: Hyperthermia, delirium, dry
mouth, tacycardia, ileus, urinary retention.
Seizures, coma and respiratory arrest may
occur.
• Treatment – Gastric lavage with tannic acid,
cold sponging or ice bags, Physostigmine s.c.
or i.v., diazepam to control convulsions.
 Contraindications
• Glaucoma
• Prostatic hypertrophy
• Urinary tract obstruction
• Gastrointestinal tract obstruction
• Infectious diarrhea
• Reflux esophagitis
• Tachyarrhythmias
• Angina
• Hyperthyroidism
• Pregnancy
 Individual Drugs
• Atropine - prototype. Antidote in
OP Poisoning.
• Ipratropium - Useful in rhinorrhea.
Also excellent bronchodilator.
• Scopolamine - depresses CNS and causes
amnesia, drowsiness, euphoria, relaxation
and sleep. Also good for motion sickness.
Given parenterally, orally and transdermally.
• Benztropine - temporary use in Parkinson’s
disease. Useful for dystonic reactions
caused by antipsychotics.
 Individual Drugs
• Trihexyphenidyl - also used for treating EPS by
some antipsychotics. Contraindicated in
glaucoma.
• Flavoxate - relieves dysuria, urgency,
frequency, and pain with GU infections
• Oxybutynin - has direct antispasmodic effects
on smooth muscle and anticholinergic
effects. Decreases frequency of voiding.
 References

1) Slides by Dr. Mohit Kulmi.

2) Tripathi KD, Essential of Medical
Pharmacology 8th Edition
Thank you!