Cholinergic Agents
Drugs that stimulate the
parasympathetic nervous system (PSNS)
The PSNS is the opposing system to
the SNS
Cholinergic Agents
Also known as
cholinergic agonists
or
parasympathomimetics
Cholinergic Agents
Mimic the effects of the PSNS
neurotransmitter
Acetylcholine (ACh)
Direct-acting (agonist)
Bind to cholinergic receptors, causing
stimulation
Indirect-acting
Inhibit the enzyme “cholinesterase”
Result: more ACh is available at the
receptors
Cholinergic Agents
Cholinergic Agents
Cholinergic Receptors
Two types, determined by:
Location
Action once stimulated
Nicotinic receptors and Muscarinic receptors
Nicotinic Receptors
Located in the ganglia of both the
PSNS and SNS
Named “nicotinic” because can be
stimulated by the alkaloid nicotine
Muscarinic Receptors
Located postsynaptically:
Smooth muscle
Cardiac muscle
Glands of parasympathetic fibers
Effector organs of cholinergic sympathetic fibers
(Sweat gland)
Named “Muscarinic” because can be
stimulated by the alkaloid Muscarine
Drug Effects of Cholinergic
Agents
Stimulate pupil
Constriction (miosis)
Reduced intraocular pressure
Cardiovascular effects
Decreased heart rate
Vasodilation (not direct but through release of
(EDRF)
Respiratory effects
Bronchial constriction, narrowed airways
Drug Effects of Cholinergic
Agents
Stimulate intestine and bladder
Increased gastrointestinal motility
Increased gastric secretions
Increased urinary frequency
Increased salivation and sweating
Bethenechol
It is not hydrolyzed by acetylcholinestrase
It lacks nicotinic activity
Its major action on smooth muscles of GIT
and urinary bladder
Mostly used for the urologic conditions
Carbachol
Having both muscarinic and nicotinic actions
Having long duration of action
Produce effects on CVS & GIT
Mostly it is used for opthalmic coditions
Pilocarpine
Tertiary amine and stable to hydrolysis by
acetylcholineserase.
Having muscarinic activity
It is mostly used for eye problems
Acute glaucoma
Sjogren syndrome
Side Effects of Cholinergic Agents
“SLUDGE”
Salivation
Lacrimation
Urinary incontinence
Diarrhea
Gastrointestinal cramps
Emesis