Parasympatholytic or

Cholinergic antagonist
Dr. Mozna Talpur
Classififation
Cholinergi
c
antagonist
s

Muscarini Nicotinic
c blockers blockers
Classification
Anti cholinergic
Atropine Cyclopentolate
ScopolamineTertiary amide Darifenacin
alkaloid
Benztropine Fesoterodine
Oxybutynin
Ipratropium Solifenacin
Tritropium Quaternary Tolterodine
Amide derivatives
Trospium chloride
Atropine is the prototype drug used as poison, cosmetic
and medicine.
Tertiary amine alkaloid ester of tropic acid found in atropa
belladonna and datura stramonium.
Absorption

Natural alkaloid and most tertiary amines are well

absorbed from Gut and conjunctival membranes.
Distribution

Widely distributed in body and in CNS.

Quaternary amines can not reach CNS.
Metabolism and excretion
50% of dose is excreted unchanged.
Mostly appears in Urine as hydrolysis and conjugation
products.
Effects in eye and ciliary muscles lasts for 72 hrs.
Mechanism of action
Atropine causes competitive reversible blockage of
muscarinic receptors.
Atropine acts both centrally and peripherally. Its
general actions last about 4 hours, except when placed
topically in the eye, where the action may last for days.
Neuroeffector organs have varying sensitivity to
atropine. The greatest inhibitory effects are on
bronchial tissue and the secretion of sweat and saliva.
 Organs End organ effect
Excitation, agitation, Hallucinations
CNS
and coma
Mydriasis(Dilatation of pupil)
Circular part of pupilary muscles
Loss of light reflex
Ciliary muscles Loss of accommodation
lacrimal gland ↓ secretion
Heart Low dose bradycardia, Tachycardia
Bronchioles Bronchodilation
GIT ↓peristalsis
Relaxes smooth muscles of ureters and
Bladder
bladder wall.
Cutaneous vasodialatation(un known
Blood vessels
mechanism)
Sweat glands, salivary glands and other
↓ secretion
exocrine glands of body
 Clinical uses
CNS:
Anti-psychotic induced parkinsonism.
Parkinsons disease (Benztropine mesylate)
Motion sickness (scopolamine)
Eye:
Measurement of refractory error.(Cyclopentolate)
Retinoscopy, fundoscopy
Prevention of synechia in uveitis, iritis.
Respiratory disorders:
Asthma and COPD (ipratropium)
GIT:
Travelers diarrhea.
Peptic ulcer(pirenzipine)
Urinary disorder: (darifenacin)
Urinary urgency, bed wetting, over reacting bladder
Can be given in urolithiasis associated pain.
Pre operative:
Decrease bronchial secretions.
Cholinergic poisoning.
Hyperhydrosis.
Side effects
Mydriasis, cycloplegia.
Retention of urine.
Dry mouth, hot flushed skin, no sweating.
Agitation, delirium.
Children are very sensitive to hyperthermia
Toxicity
Mydriasis, cycloplegia, dry sandy eyes, corneal ulcers.
Dryness of mouth, dysphagia.
Hot flushed skin, decreased sweating, hyperthermia.
Agitation, delirium, coma and death.
“dry as bone, blind as bat, red as beet, mad as hatter”
Treatment of toxicity
Symptomatic:
Choline estrase inhibitors (neostigmine).
Cold sponging.
Diazepam.
Contra indications
Glaucoma.
BPH.
Cardiac patient.
Neonates.