ANTICHOLINESTERASE

AGENTS
by :
dr.Ratna Dewi Puspita Sari
FAKULTAS KEDOKTERAN
UNIVERSITAS MALAHAYATI

 INTRODUCTION

Agents that prolong the existence of

acetylcholin after it is released from
cholinergic nerve terminal.

Agents inhibit acetylcholinesterase,

concentrated in synaptic regions
and use for catalysis of the
hydrolysis of acetylcholine.

 INTRODUCTION
Cross the blood-brain barrier.
Facillitation of gastrointestinal and
bladder motility, activity of
neuromuscular junction of skeletal
muscle.

 PHARMACOLOGICAL
PROPERTIES

Anticholinesterase (anti-ChE) effects :

1.stimulation of muscarinic reseptor.
2.stimulation & depression autonomic
ganglia and nicotinic action.
3.stimulation cholinergic reseptor.
The actions of anti-ChE are blocked by
atropine.
Anti-ChE increase peristaltic activity
smooth muscle at bronchioles,auerbachs
plexus & uterter.

Derivat of anti-ChE like physostigmine &

neostigmine :
- absorbed readly from the gastro
intestinal tract, subcutaneous tissue &
mucous membrans.
- administered parenterally,poorly in
oral administration.
- renal excretion.
Neostigmine enhances gastric contaction
& increase secretion of gastric acid.
Anti-ChE cannot againts skeletal muscle
paralysis caused by succinilcholine.

 TOXICOLOGY

Frequently it have been used for homicidal

& suicidal purposes by dermal & pulmonary
routes.
Acute intoxication by anti-ChE manifes by
muscarinic & nicotinic signs :
Occular effects :
miosis,occular pain,conjunctival congestion,
ciliary spasm, lacrimation,disminished vision
and brow ache.

 Respiratory effects :
rhinorrhea, hyperemia upper tract,
wheezing respiration & paralysis muscle.
Gastrointestinal effects :
anorexia, nausea, salivation, vomiting,
abdominal cramps, diarrhea & involuntary
defecation.
Muscle skeletal effects :
fasciculation, weakness, paralysis,
fatigability & penile erection.

 CNS effects :
confusion,ataxia,slurred speech,loss of
reflexes,cheyne stokes respiraion & coma.
Cardiovascular effects:
bradycardia and hypotension.
Treatment :
- atropine antagonis the action at muscarinic
reseptor sites.
- anti-ChE effects can be reversed by prali
doxime (2-PAM), a cholinesterase
reactivatior.

 THERAPEUTIC USES

Anti-ChE agents recommeded for the

treatment of :
- atony of smooth muscle of the intestinal
tract and urinary bladder.
- glaucoma
- myastenia gravis
- termination effects of neuromuscular
blocking drugs
Long acting & hydrophobic cholinesterarase
inhibitors use in th/ for alzheimers disease.

Physostigmine is useful in the

treatment of intoxication by atropine &
several drugs with anticholinergic side
efffects, friedreichs or inherited
ataxias.

Edrophonium can be used for

terminating attacks of paroxysmal
supraventicular tachycardia.
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