1.

Introduction Organization of the nervous system

2. Drugs Act on Autonomic nervous system

Drugs that produce Parasympathetic like actions = Parasympathomimetics =

Cholinergics
Drugs that oppose Parasympathetic = Parasympatholytic = Anticholinergics
Drugs that produce sympathetic like action = Sympathomimetics =
Adrenergics
Drugs that oppose sympathetic = Sympatholytics = Antiadrenergics

3. Cholinergic transmission
4. Cholinoceptors
Muscarinic receptors: 3 subtypes are well defined pharmalogically M1, M2 M3
found on ganglia of the peripheral nervous system and on the autonomic effector
organs, such as the heart, smooth muscle, brain, and exocrine glands
Nicotinic receptors (N) present in: autonomic ganglia, adrenal medulla,
neuromuscular junction
5. Parasympathomimetics Cholinergics
Drugs that stimulate muscarinic receptors

Direct Parasympathomimetics
Indirect Parasympathomimetics (Anti-cholinesterases)

Mechanism of action

Direct Parasympathomimetics: They stimulate the muscarinic receptors

directly.
Indirect Parasympathomimetics (Anti-cholinesterases): They inhibit
cholinesterase enzyme leading to accumulation of endogenous
acetylcholine at both muscarinic and nicotinic receptors

7. Direct cholinergic agents

Acetyl-choline is It is a natural direct parasympathomimetic. stimulates

directly both muscarinic & nicotinic receptors important physiologically, it is
not used clinically because its actions are very brief because of rapid
hydrolysis
Methacholine more selective on cardiovascular system .Weak nicotinic effect.
Carbachol : has muscarinic and nicotinic but it is mainly selective on EYE,
gastrointestinal tract and urinary tract
Bethanichol Actions: No nicotinic action, but only muscarinic action which is
mainly selective on gastrointestinal tract , and urinary system.

Pilocarpine Direct muscarinic agonist specific on eye and secretions . Very

weak nicotinic action

8. Reversible anticholinesterases

Physostigmine has muscarinic action most specific on eye and CNS

stimulation
Neostigmine It produces both nicotinic and muscarinic actions but it is more
active on the nicotinic receptors of the N-M junction. Its muscarinic actions
are more specific on the gastrointestinal and urinary tracts. No CNS action

9. Indications

Methacholine paroxysmal atrial tachycardia and peripheral vascular disease

Carbachol Glucoma Post-operative paralytic ileus Post- operative retention of
urine Bethanechol Post-operative paralytic ileus Post- operative retention of
urine
Pilocarpine Glucoma physostigmine Glucoma Anti-cholinergic poisoning
Neostigmin Myasthenia gravis Reversal of neuromuscular blockade Urine
retention

10. cholinergic agents Adverse effects

Muscarinic: Miosis, lacrymation, salivation, sweating Urgency and
spontaneous micturition Bronchospasm and increased bronchial secretion.
Bradycardia and hypotension. Colic, vomiting, diarrhea, hyperacidity & peptic
ulcer
Nicotinic: skeletal muscle twitches followed by paralysis Contraindication
Bronchial asthma Peptic ulcer Coronary insufficiency Thyrotoxicosis
Mechanical obstruction of the GIT and urinary bladder

DRUGS:
Bethanechol (Uriflow)
Therapeutic Categories

Drug acting on the gastrointestinal system

Urological
Muscarinic receptor agonist (parasympathomimetic agent, direct acting)
Choline ester