Anti-cholinergic Drugs

Atropine , Scopolamine and Glycopyrrolate

Cholinesterase
Neostigmine

inhibitors

Dr. Med. Khaled Radaideh, Facharzt

Department of Anesthesiology Jordan University of Science and Technology Irbid-Jordan
April 12 Dr. Med. Khaled Radaideh 1

Anticholinergic drugs and Cholinesterase inhibitors

Objectives:
1.Atropine 1.1. general about atropine (Origin, Mode of action, Dose..) 1.2. Effect of atropine on different organs 1.3. clinical uses and Contraindications 1.4. Side Effects (intoxication)
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Anticholinergic drugs and Cholinesterase inhibitors

Objectives:

Continue..

2. Scopolamine 2.1. general about scopolamine (Origin, difference to atropine, Dose..)

3. Glycopyrrolate: difference to atropine

April 12

Dr. Med. Khaled Radaideh

Anticholinergic drugs and Cholinesterase inhibitors

Objectives:

Continue..

4. Cholinesterase inhibitors 4.1. general about Cholinesterase inhibitors (Origin, Mode of action, Classification...)

4.2. Effect of Cholinesterase inhibitors on different Organs

April 12 Dr. Med. Khaled Radaideh 4

Anticholinergic drugs and Cholinesterase inhibitors

Objectives:

Continue..

4.3. Neostigmine 4.3.1. general about Neostigmine (Dose, clinical uses, side effects..)

4.4. Role f neostigmine & atropine in anesthesia

April 12

Dr. Med. Khaled Radaideh

Atropine
Atropine is an alkaloid found in atropa

belladona It is a competitive antagonist for the muscarinic acetylcholine receptor Because its a tertiary amine atropine is relatively lipid soluble and cross BBB and its well distributed through the CNS
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Atropine

continue

Duration of action is 4 to 8 hours except

in the eyes where it reaches 72 hours or longer initial single doses in adults vary from around 0.5 mg to 1 mg 40% metabolized in the liver,60% excreted un changed in the urine
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Effect of atropine on different organs:

CVS : bradycardia at low doses ,

tachycardia at high doses EYE : mydriasis, cycloplegia, increase IOP, reduce lacrimal secretion GIT : reduce the activity f GI Urinary system : relaxation of smooth muscles in urinary tract
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Effect of atropine on different organs:

continue.

Respiratory : bronchodilation ,reduction in

secretions
Salivary glands : xerostomia Sweat glands :inhibition of secretion can cause

hyperthermia
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Clinical uses:
Blocks the effect of acetylchline that result from

cholinesterase inhibitors like Neostigmine

Blocks secretions prior to surgery Ophthalmic: mydiasis and cycloplegia to

facilitate the examination of retina and optic disc

GIT:antispasmodic agents

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Dr. Med. Khaled Radaideh

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Clinical uses:

continue

Urinary: reduce hypermotility states f the

urinary bladder and occasionally used in enuresis

In CNS disorder: Parkinson and motion

sickness
Antidote for organophosphate and some types

of mushroom poisoning.
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Contraindication
Relatively contraindicated in glaucoma

especially closed angle

Men with prostatic hyperplasia

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Side Effects (intoxication)

Dry mouth ,blurred vision , tachycardia ,

constipation, confusion, delirium ,agitation ,collapse of the circulatory and respiratory systems

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Scopolamine
A belladona alkaloid Produces peripheral effects similar to atropine

but it has greater action on CNS Longer duration of action that atropine Dose 0.4 mg More effective in motion sickness Produce sedation but at higher doses can cause excitement
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Scopolamine

Continue..

The amnesic action of scopolamine makes it an

important adjunct drug in anesthetic procedures

Side effects same as atropine but with more

effect on CNS

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Glycopyrrolate
Doesnt cross BBB so no CNS effect It has longer duration of action in relation to

atropine
Produce less cardiovascular stimulation

than atropine
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Cholinesterase inhibitors
Cholinesterase is enzyme that cleaves

acetylcholine to acetate and choline to end its action

Its located in both pre and postsynapse

Cholinesterase inhibitors indirectly provide a

cholinergic action by prolonging the life time of acetylcholine

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Cholinesterase inhibitors

continue.

These drugs provoke a response at all

acetylcholine receptor in the body which include muscaranic , nicotinic and neuromuscular junction Classified to: Reversible: Neostigmine , physosigmine, pyridostigmine, Endrophnium Irreversible: Isoflurophate, Echothiphate
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Effect of cholinesterase inhibitors on different organs:

CVS : Bradycardia EYE : Miosis GIT : increase the activity of GI

Salivary glands : Hypersalivation

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Neostigmine
Reversible inhibition by making ester linkage with the enzyme
It is polar so it doesnt enter the CNS

Has moderate duration of action usually 30 min to 2 hours

Dose 2-150 mg/kg orally Dose 2.5 5 mg i.v. to reverse the muscle

blockade (non depolarizing MR)

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Clinical uses
In anesthesia at the end of an operation to

reverse the effect of non polarizing muscle relaxants

It can be used for urinary retention resulting

from general anesthesia

In the treatment of myasthenia gravis

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Side Effects
Salivation flushing Bradycardia, decrease blood pressure abdominal pain , nausea bronchospasm , urinary urgency Meiosis Sweaty skin
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Role f neostigmine & atropine in anesthesia

Neostigmine increase amount of Ach so Ach

competes with non depolarizing drugs and decrease their effect but leads to many side effects resulting from increased Ach concentration and activation of parasympathetic system leading to bradycardia ,meiosis, hypersalivation,intestinal hypermotility so we combine atropine with neostigmine in one syringe to counteract the side effects.
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Anti-cholinergic Drugs

Atropine , Scopolamine and Glycopyrrolate

Cholinesterase inhibitors

Neostigmine

Thank you
Dr. Med. Khaled Radaideh, Facharzt
Department of Anesthesiology, Faculty of medicine Jordan University of Science and Technology Irbid-Jordan
April 12 Dr. Med. Khaled Radaideh 24