CHOLINERGIC ANTAGONIST

Prof. Dr Awal sir

Pharmacology
• The drug that blocks or inhibit the action of Ach/Cholinergic drug is called Anticholinergic
drug.
CLASSIFICATION OF CHOLINERGIC DRUG
A. Anti-Muscarinic/ Muscarinic blocker/Muscarinic action blocker
According to the sources
1. NATURAL
Atropine- Atropa Belladona ( Datura plant)
Hyoscine/ scopolamine - hyosinamus Nigra
2. SEMI-SYNTHETIC
Homotropin (eye drop) – Used in corneal ulcer / Glaucoma/ Conjunctivitis
Hyoscynamine(N- Butyl Bromide)
Ipratropium Bromide
3. SYNTHETIC
Dicyclomine
Propantheline
Oxyphenonium
According to Clinical Use
1.Anti-spasmatic/ smooth muscles relaxant : (GIT, URINARY, BILIARY
SPASM)
• Hyoscyamine N butyl bromide
• Propantheline
• Dicyclomine
*** NOTE : Anticholinergic but Anti-spasmatic drug : Tiotropium methal
Sulphate
2.MYDRIATIC DRUGS:
• Atropine sulphate
• Narcotine
• Tropicamide
3.Anti- Asthmatic drugs
• Ipratropium bromide
• Tiotropium bromide
4.Anti- Parkinsonium Drugs
• Procyclidine
• Dextropine
• Biperidine
• Benzhexol
5.Vesicle selective drugs
• Oxybutynin
• famoxine
B. ANTI – NICOTINIC DRUGS
• On the basis of mechanism of action:
1.Ganglion blocker:
Trimethoprim
Hexamethorium
2. Neuromuscular blocker/ Muscle relaxant:
Non- depolarizing/ Competitive: Gallamine , Atracuronium
Depolarizing/ Non- Competitive: Succinyl choline
ACCORDING TO DURATION OF ACTION

1. Long acting (30 – 60 min) :

D- tubocurarine
Pancuronium
2. Intermediate acting ( 20- 40 min):
Atracuronium
Rocuronium
3. Short acting (15 -30 min) :
Mivacurium
Succinyl choline/ suxamethonium ( very short acting)
Muscle relaxant:
Smooth muscle relaxant: Drotaverine , Dicyclomine
Skeletal muscle relaxant :
• Central
• Peripheral
Smooth muscle relaxant ( Anti – Spasmatic):
Mechanism:
Drotaverine

inihibits PDE – 4 (phosphodiesterase enzyme)

inhibits cAMP or cGMP

Causes muscle relaxation (Thus inhibiting the spasm)

***Note : Other drugs act by inhibiting the M3 receptor of smooth muscle
INDICATION OF SMOOTH MUSCLE RELAXANT
1. All colic : like intestine , renal , Biliary , uteric
2. Abdominal cramps
3. Gastric hypermotility
4. Gastritis
5. Irritable bowel syndrome (IBS)
6. Urinary Frequency and Urgency
7. Nervous and Drug induced Diarrhoea
8. Dysmenorrhoea
9. Spasmotic pain
10. Anurosis in children
SKELETAL MUSCLE RELAXANT
a) Neuro-muscular blocker:
I. Depolarizing: Succinyl choline
II. Non – Depolarizing: Gallamine , Atracuronium
b) Anti – Spasmatic Drug/ Spasmolytic Drugs:
Mechanism: Increase tone or spasticity due to impairment of descending tract.
1. Centrally Acting: Diazepam, baclofen, GABA, pentin( most frequently used)
these drugs selectively depress the spinal and supraspinal reflexes.
Indication of centrally acting anti – spasmatic drug:
1. Acute muscle spasm (sprain, bursitis ,dislocation , rupture tendon and ligaments)
2. Backache
3. Neuralgia
4. Enzyme retention
5. ETC ( Electro compulsive Therapy)
6. Tetanus
7. Orthopedic Manupulation
2. Directly acting :
• Mechanism:
Acts on Sarcoplasmic reticulum of skeletal muscle

prevents ca++ releases

interfere with excitation contraction coupling

relaxation of skeletal muscle

INDICATION :
1. hemiplegia and paraplegia
2. Cerebral palsy
3. Multiple sclerosis
4. Sapasticity due to upper motor neuron (UMN Disorder)
5. Malignant Hyperthermia
a) Neuromuscular Blocker
I. Depolarizing: Succinyl choline
II. Non – Depolarizing: Gallamine , Atracuronium
INDICATION OF NEURO MUSCULAR BLOCKER:
1. As surgical adjuvant GA – for skeletal muscle relaxant
2. For the treatment of Convulsion like Epilepsy , tetanus
3. Electro compulsive Therapy(ETC) in severe depressed condition to
prevent trauma
4. To facilitate bronchoscopy, laryngoscopy, Esophagopscopy, Endotracheal
intubation
ATROPINE
• EFFECT OF ATROPINE:
1. ON EYE:
• Mydriasis (Dilatation of pupil )
• Cycloplegia – paralysis of ciliary muscle, loss of accommodation of near vision
• increase of IOP ( intra ocular pressure) / ocular hypertension
 Relaxation of ciliary muscle and iris
Close the cannal of schlem
Decrease outflow of aqueous humour
Increase IOP
Glaucoma
• Decrease lacrimation
• Loss of light reflex
2. ON GIT:
• tone and motility decreases
• Smooth muscle relax Causes constipation
• Decrease gastric Secretion
3. ON RESPIRATORY SYSTEM:
• Relax the bronchial smooth muscle
• Decrease bronchial Secretion
4. ON GASTRO- URINARY SYSTEM:
• Detrusor muscle relax and sphincter contraction causes urinary retention
• Ureteric smooth muscle relaxation
5. ON EXOCRINE GLAND:
• secretion of all exocrine gland decrease except milk
• Sweat gland : decrease dry hot skin, increase temp(upto 106-108 degree
Celsius)
• Salivary Gland : dry mouth, difficulty in speech and deglutition
• Lacrimal gland: decrease secretion
• Bronchial Secretion decreases
6. ON CNS
• Excitement
• Restlessness
• Hallucination
• Delirium
• Respiratory and circulatory collapse
CONTRAINDICATION OF ATROPINE
• Close angled glaucoma
• Benign enlargement of prostrate
• Paralytic ileus
ADVERSE EFFECT OF ATROPINE:
• Dry mouth( difficulty in speech and deglutition)
• Constipation
• Urinary Retention
• Dry and hot skin
• Dry eye
• Excitement , hesitation and delirium
ATROPINE POISONING:
SIGN AND SYMPTOMS:
• Convulsion
• Confusion
• Blurred vision
• Hyperthermia
• Dry mouth
• Constipation
MANAGEMENT:
• Gastric lavage by KmnO4
• Ice bag (sponging)
• Diazepam (if excited)
**SPECIFIC TREATMENT: Physostigmine (1mg/ml)I/V repeated until sign and
symptoms disappear