Clinical Implications

of Drugs
that act on
Cholinoceptors
Cholinergic Agents
 Muscarinic Receptors
Receptors Location Pharmacological effect
Muscarinic 1.CNS Multiple effects
M1
2.stomach Inc HCL secretion
M2 1.Myocardium Dec heart rate

2.Smooth muscle contraction

M3 1.Smooth muscles: -Contraction

-Eye -Contraction
-GIT -Relaxation
walls -Contraction
sphincters -Relaxation
-Genitourinary -Contraction
Bladder wall
Sphincters
uterus

2.Glands -Increase secretion

-M4 and M5 are somewhere in CNS.
 Nicotinic Receptors
Receptors Location Pharmacological effect

Nm Neuromuscular junction Contraction of skeletal muscles

Nn Postganglionic cell body, Effects on cardiovascular system:

Dendrites -vasoconstriction
-tachycardia
-inc in BP

Effects on GIT:
-inc in tone and motility
 Cholinergic Drugs
Direct acting drugs Indirect acting drugs

1. ESTERS 1. Reversible

• Acetylcholine • Short acting

• Methacholine Edrophonium
• Carbacol • Longer acting
• Bethanechol Pyridostigmine,Neostigmine,
• Cevemeline physostigmine

2. Alkaloids 2. Irreversible

• Muscarine • Organophosphatase
• Nicotine Ecothiopate, Isofluropate,
• Pilocarpine Prathion, Melathion
• Oxytremorine
 Anti-Muscarinic Drugs
Groups Drugs
1)Natural Alkaloids Atropine
Hyoscine(Scopolomine)
2)Semisynthetic derivatives Homatropine
Ipratropium bromide
Tiotropium bromide
3)Synthetic compounds
a)Mydriatics Cyclopentolate
Tropicamide
b)Antisecretory
i,Quaternary Amines Clinidium
Glycopyrolate
Mepenzolate
ii,Tertiary Amines Tolterodine
oxybutynin
c)Antiparkinsonian Benztropine mesylate
Biperiden
Orphenadrin
 Anti Nicotinic Drugs
Ganglion Blocking Drugs Neuromuscular junction blocking drugs
•Tetraethyl Ammonium Depolarizers
•Hexamethonium •succinylcholine
•Trimethaphan •Decamethonium
•Mecamylamine Non Depolarizers
•Tubocurarine
•Pencruronium
•Atracurium
 Diseases cured by
Cholinergic Drugs
Disease Drug
Urinary Retention -Bethanechol

-Neostigmine
Clinical Implications Drug

Glaucoma 1. Pilocarpine (drug of first choice)

Type of glucoma:
•Open angle glaucoma 2. Carbachol (in pt. who have become
•Closed angle glaucoma tolerant to pilocarpine)

3. Physostigmine
(antidote for atropine overdose)

4. Ecothiophate (open angle glucoma)

Clinical Implications Drug
Alzheimer’s disease (dementia) Memantine
Clinical Implications Drug
Myasthenia gravis 1. Edrophonium
(differentiates between
myasthenia gravis and cholinergic
crisis)

2. Neostigmine(antidote for
tubocurarine)

3. Pyridostigmine (longer duration

of action)
Clinical Implications Drug
Sjogren’s Syndrome (Xerostomia) Cevimeline
General Adverse Effects of
Cholinergic Drugs
-Diarrhea
-Hypotension
-Nausea
-Headache
-Urinary urgency
-Salivations
-blurredness
-dizziness
-asthma
-bradycardia
-seizures
-Sweating
-Insomnia
-Abdominal cramp
 Diseases cured by
Anti-Cholinergic Drugs
Clinical Implications Drug

1. To measure refractive errors -Atropine

2. To cure urinary urgency (prototype drug)
3. Antidote for cholinergic agonist
4. Before surgery (reduces secretions) -Tropicamide

-Cyclopentolate
Clinical Implications Drug

1.Motion Sickness Hyoscine (scopolamine)

2.Anesthetic procedures (blocks

short term memory)
Clinical Implications Drug

Asthma -Ipratropium
-Tiotropium (longer
duration of action)
Clinical Implications Drug

Bowel syndrome -Glycopyrolate

-Dicycloamine
Clinical Implications Drug
1. Post-operative bladder spasm or 1.Oxybutynin
incontinence
2. Tolterodine
Clinical Implications Drug
Manifestations of 1. Benztropine Mesylate
Parkinson’s Disease
2. Biperiden
General Adverse Effects of
Anti-Cholinergic Drugs
-dental caries
-decreased bronchial secretion
-Hyperthermia
-photophobia
-blurred vision
-angina
-myocardial
-infarction
-urinary retention
-constipation
-confusion
-attention deficit
-memory impairment
 Ganglion Blockers
Clinical Manifestation Drug Adverse and Toxic
Effects

1. Hypertensive Trimethaphan -Excessive hypotension

Emergency -Urinary retention
-Dry mouth
2. Dissecting aortic -Impotency
aneurysm
Clinical Implications Drug Adverse and Toxic
Efects
Nicotine Addiction Mecamylamine -Weakness
-Fatigue
-Constipation
-Nausea
 Neuromuscular
Blocking Agents
Clinical Implications Drug Adverse and toxic effects

Muscular Succinylcholine -Respiratory paralysis

contractions -Muscle twitching
-Muscle pain
-Allergic reactions
Clinical Drug Adverse and toxic effects
Implications
1. Used for Mivacurium -Allergic reactions
complications of -Chest tightness
facial-cranial -Dizziness
surgery -Uneven heartbeat
-Fainting
2. Adjunct to
general anesthesia
Clinical Implications Drug Adverse and toxic effects

1. Treating spasm of Baclofen -Muscle weakness

skeletal muscles -Vomiting
-Drowsiness
2. Multiple sclerosis -Weak or shallow breathing
Presented By: (2nd Year BDS)
Ameerzeb Pirzada
Masooma Fizza
Nakia Mansoor
Hammad Athar