AGENTS THAT DONT LIKE CHOLINERGIC RECEPTOR - CHOLINERGIC ANATAGONISTS

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Cholinergic anatagonist/ cholinergic blocker/Parasympathetolytic/Anticholinergic 
/Antimuscarinic 

These agents selectively block muscarinic receptors of parasympathomimetic nerves 

Atropine= tertiary amine…Belladona alkaloid…Hyocyamine active isomer

MOA:

bind competitively prevent Ach from binding to those receptor act both centrally and peripherally

PHARMACOLGY, PHARMACOKINETICS, PHARMACODYNAMICS, AUTONOMIC NERVOUS SYSTEM, ANTICHOLINERGIC, CHOLINOCEPTORS. LIPINCOTT, SCREENIG TEST, AKUH,

Effects 

Produce Cycloplegia; inability to focus near vision….unresponsive to light

Mydriasis : dilation of pupil by contracting radial muscle & dilating ciliary muscle 

Antispadmodic: reduce activity of GIT 

Tachycardia, reduce the hypermotility of urinary bladder, secretions increase temp.of 

body can be dangerous in childern and elderly 

T.E:

measurement of Refractive error 

Antispasmodic

antidote for cholinergic agonist 

Antisecretery

healing of peptic ulcer

S.E

blurred vision, sandy eyes, Dilirium, hallucination.. 

PHARMACOLGY, PHARMACOKINETICS, PHARMACODYNAMICS, AUTONOMIC NERVOUS SYSTEM, ANTICHOLINERGIC, CHOLINOCEPTORS. LIPINCOTT, SCREENIG TEST, AKUH,PHARMACOLGY, PHARMACOKINETICS, PHARMACODYNAMICS, AUTONOMIC NERVOUS SYSTEM, ANTICHOLINERGIC, CHOLINOCEPTORS. LIPINCOTT, SCREENIG TEST, AKUH,

Classification: 

Antimuscarinic agents Atropine, Benztropine, Cyclopentolate 

Darifenacin, Solifenacin, 

Fesoterodine, Tolterodine 

Ipratropium, Tiotropium, tropicamide, 

Trihexyphenidyl, Trospium chloride

SCOPOLAMINE, Oxybutynin, 

Ganglionic blockers Mecamylamine,Nicotine 

Neuromuscular blocker Atracurium, Cistracurium, Pancrunium,

Rocuronium, Vecuronium,

Tiotropium used O.D….Ipratropium 4 times a day

Tropicamide & Cyclopentolate= ophthalmic soln. for mydriasis & cycloplegic…

Benztropine & Trihexyphenidyl= treatment of Parkinson disease

Darifenacin, Fesoterodine,Oxybutynin, Solifenacin, Tolterodine, Trospium chloride

Used in overactive bladder oxybutynin available as transdermal patch..

GANGLIONIC BLOCKERS

Act on Nicotinic receptors of both Parasympathetic & Sympathetic autonomic ganglia

Nicotine at lower dose, stimulate the receptor…at higher dose, block the receptor

cause paralysis…increased release of neurotransmitter (Dopamine & Norepinephrine )

Increased peristalsis secretions…suppress appetite..

Mecamylamine competitive blocker of ganglia…

NEUROMUSCULAR BLOCKING DRUGS

These drugs block the transmission of Ach b/w motor nerve endings and nicotinic receptors on the neuromuscular end plate of skeletal muscle

Non-depolarising (competitive) blocker

Include Tubocurarine, Atracurium, Vancronium, Rocuronium

MOA: 

interact with nicotinic receptor prevent the binding of Ach..

depolarization. muscle contraction . At higher dose they block the ion channel of the endplate..

Can overcome by increasing conc. Of Ach.

Blockade of skeletal muscle of 1st Face,eye,Limb,Neck,Trunk,Diphragm at last

T.E:

As Adjuvant in Anaesthesia during surgery..in orthopedic surgery..in intubation

S.E:

Atracurium releases Histamine and metabolite Laudanosine which can provoke

Seizure….Hyperkalemia..Increased intraocular pressure..Hyperthermia

Cisatracurium =metabolite Atracurium..suitable in renal failure..useful in mechanical

ventilation

Depolarizing Agents

Succinylcholine

Scopolamine is Antimotion sickness…block short-term memory…susceptible to abuse 

…with morphine in obstetrics to produce Amnesia & sedation 

Ipratropium & Tiotropium:

 Quaternary derivative of atropine..used in inhaled form.. 

Bronchodilators for brochospasm…in COPD

MOA:

bind with receptor instead of Ach…causes opening of Na+

channels...depolarization..twitching of muscles (Fasciculation)..continuous 

depolarization weakened the muscle...followed by flaccid paralysis..PHASE I

Memb.repolarize...but receptor desensitized..no response toAch..PHASE II

T.E:

 in anaesthesia.. in electroconvulsive shock treatment 

S.E

Hyperthermia ( muscle rigidity, tachycardia, metabolic acidosis, hyperpyrexia).. 

Treated by Dantrolene ..it block Ca++ ions..ϴheat production 

Apnea due to paralysis of diaphragm muscles..Hyperkalemia

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