This document discusses cholinergic and anticholinergic drugs. Cholinergic drugs act on the neurotransmitter acetylcholine in the parasympathetic nervous system, stimulating activation. They inhibit the cholinesterase enzyme that breaks down acetylcholine. Common cholinergic drugs include acetylcholine, pilocarpine, and reversible cholinesterase inhibitors. Anticholinergic drugs block the action of acetylcholine, inhibiting the parasympathetic nervous system. They include natural alkaloids like atropine and synthetic drugs. Common uses are as mydriatics in eye exams, to reduce secretions before surgery, and to treat Parkinson's disease symptoms. Side effects include dry mouth, urinary retention,

1. CHOLINERGICS
ANTICHOLINERGIC
By:- Dr Rupesh Dalavi

2.  Cholinergic medicines are a category of pharmaceutical
agents that act upon the neurotransmitter acetylcholine.
 Acetylcholine is primary neurotransmitter within the
parasympathetic nervous system

3.  Cholinergic drugs stimulate the activation of the parasympathetic nervous
system by activating receptors for acetylcholine.
 These drugs inhibit cholinesterase enzyme that rapidly destroy
acetylcholine and so prevent the destruction of acetylcholine.
 Cholinergic drugs areAgonist of acetylcholine.

4. 1. Direct acting
2. Indirect acting
(Anti- cholineesterage / Cholineesterage
Inhibitor)
Synthetic esters of choline
eg. Acetylcholine
Bethonechol, Carbacol,
methacholine, Urecholine)
Cholinomimetic alkaloids
eg. Pilocarpine, Muscarine,
Reversible cholinesterase
inhibitors e.g Physiostigmine,
Neostigmine, Pyridostigmine, Rivastigmine,
Donepezil, Endrophonium, Galantamine
Irreversible cholinesterase
Inhibitors eg :- Malathione, parathione, serine,

5. Physostigmine
 0.5-2 mg IM or IV given slowly (not to exceed mg/minute IV)
Neostigmine
 Adults: 0.5-25 mg slow IV.

6. Topical (eye)
 Treatment of open angle glaucoma.
 Reverse cycloplegia and mydriasis due to atropine like agents.
Systemic
 Diagnosis and treatment of myasthenia gravis.
 Relief of postoperative abdominal distention and urinary distention
 Neostigmine is antidote to muscle relaxant.

7. Acetylcholine Accumulation at cholinergic synapses
Competitively blocks acetylcholine Hydrolysis by cholinesterase +
mimics acetylcholine
Increase Cholinergic stimulation
Eg.- Miosis and Ciliary muscle contraction increase aqueous
humor outflow and decrease intraocular pressure

8.  Bronchial asthma
 Deceased visual acuity, eyelid twitching, increased tearing, mild headache.
 Sweating
 Urinary urgency
 Excessive salivation.
 Nausea, diarrheas.
 Cramping, Muscle twitching.

9.  Inflammation of the iris or ciliary body, Narrow/Close angle glaucoma.
 Asthma
 cardiovascular disease.
 Intestinal or urinary obstruction
 Mega colon.
 Acute peptic ulcer.
 Hyperthyroidism.

10.  Explain about salivations, vomiting, urination and other side effects.
 Reduce dosage if excessive nausea or sweating occurs.
 Have atropine sulfate (Ant cholinergic) injection ready, in case of allergic
action or accidental overdose.
 Have emergency measures readily available (e.g. atropine, oxygen with
respiratory suction apparatus) in case if a breathing crisis.

12.  Anticholinergic drugs Also called cholinergic blocking
agents or parasympatholytics.
 They inhibit the parasympathetic nervous system by
blocking the action of acetylcholine.
OR
 Anticholinergics are substances that block the action of the
neurotransmitter acetylcholine at synapses in the central
and peripheral nervous system

13. 1. Natural alkaloids 2. Semisynthetic 3. Synthetic
Atropine
Scopolamine
Homatropine,
Ipratropium bromide
a) Mydriatics: Cyclopentonate.
b) Antisecretory / Antispasmodics: Dicyclomine,
oxybutynin.
c) Antiparkinsonian: Benztropine, Trihexyphenidyl
(pacitan)

14. Anticholinergic inhibit the muscarinic actions of acetylcholine by
blocking parasympathetic impulses.
It competes with acetylcholine for sites on muscarinic receptors

15.  Mydriatics and cycloplegia for ophthalmic examinations.
 Close Angle Glaucoma
 Preoperative medication to reduce excess salivation and prevent
bradycardia
 Decrease Gl motility and secretion.
 GI spasms
 Treatment enuresis in children.
 Treatment of sinus bradycardia and conduction (due to excessive vagal
tone)
 Antidote to overdose with cholinergic agents.
 Relief of symptoms of parkinsonism and control of extra pyramidal
disorders resulting antipsychotic treatment.
 Treatment of motion sickness – hyoscine (scopolamine)

16. 1. Cardiovascular
• Decreased heart rate in small
doses.
• Increased heart rate in large
doses.
• Vasodilatation.
2. Gastrointestinal Tract
• Decreased motility.
• Decreased muscle tones.
• Decreased secretions.
3. Urinary Tract
• Relaxation of detrusor muscles.
• Contraction of sphincter
muscles.
4. Eye
• Mydriatics.
• Cycloplegia.(paralysis of muscle that adjust shape of
eye lens )
5. Smooth Muscles
• Slight relaxation of non-vascular smooth muscles.
6. Exocrine Glands
• Decreased sweat glands secretions.
• Decreased salivation.
• Decreased mucous gland secretions
7. Central Nervous System
• Drowsiness, disorientation, hallucinations.
• Decreased tremors and rigidity of parkinsonism.

17. o Decreased mucus production.
o Xerostomia (Dry mouth)
o Pupil dilation.
o Urinary retention.
o Tachycardia.
o Disorientation & Agitation.
o Confusion.
o Diminished bowel movements.
o Respiratory depression.
o Increased intraocular pressure.

18. o Glaucoma.
o Chronic renal, lung or hepatic disease.
o Myasthenia gravis.
o Heart disease & Tachycardia.
o Paralytic ileus.
o Ulcerative colitis.
o Genitourinary (GU) obstruction.
o Severe hemorrhage.

19. This is not the END……. 
• Write Nursing responsibility as I discussed in
class………