ANS & Cholinergic Drugs

Toxins Interfere Cholinergic Transmission.
MISCELLANEOUS
Tre-morine
Oxo-tre-morine
Cevi-meline
Tre-morine and Oxo-tre-morine are synthetic tertiary

amines. These are not used therapeutically but used
only as investigative research tool, to stimulate
parkinsonism-like symptoms in animal models.
Skeletal muscles
Activates pre- junctional fibers repetitive firing twitching and
fasciculation.
Higher doses cause persistent depolarization of endplates resulting in blockade
of neuromuscular transmission- weakness and paralysis.
CNS
Cognitive function may be improved in Alzheimer’s disease.
Higher doses produce excitement, mental confuse, disorientation, tremors and
convulsions followed by coma.
Other effects.
Stimulations of smooth muscles and glands of the gastrointestinal, respiratory,
urinary tracts and in the eye.
THERAPEUTIC USES
1. Ophthalamic
a. Glaucoma
b. Counteracts mydriatics after eye tests
c. Prevents adhesions between iris and lens or cornea
d. To break or prevent adhesions formed between iris and cornea and iris and lens
iritis. (miotic are used alternating with mydriatic )
2. MYASTHENIA GRAVIS
3. POST OPERATIVE
e. Paralytic ileus/ urinary retention
f. Post op decurarisation
4. Poisoning
a. Cobra bite
b. Belladonna poisoning- physostigmine
THERAPEUTIC USES
5. CNS
a. Alzheimer’s Disease
6. MISCELLANEOUS
b. Edrophonium is used for diagnostic purpose to differentiate between
cholinergic and myasthenic crisis.
Overtreatment with anti-ChEs-
Overdose persistent depolarization of muscle endplate
weakness Cholinergic crisis.
Edrophonium test to differentiate cholinergic crisis and myasthenic crisis.
Improvement
Edrophonium 2mg IV Myasthenic crisis
No Improvement/worsening-
cholinergic crisis
Myasthenia Gravis-Diagnosis
• Edrophonium 2-10 mg injected slowly i.v.

Improve muscle strength only in myasthenia gravis and not in other
muscular dystrophins.
Treatment
• There are 4 basic therapies:
Symptomatic treatment-acetylcholinesterase inhibitors

Rapid short term plasmapheresis and intravenous immunoglobulin
 chronic long term-immunomodulating treatment- glucocorticoids &
immunosuppressive drugs
Surgical treatment
IRREVESIBLE
ANTICHOLINESTERASES
ORGANOPHOSPHORUS (OP) INSECTICIDES
• All OP compounds except Echothiopate have no therapeutic
applications.
• It is used in resistant cases of glaucoma.
• Op poisoning is one of the most common poisoning all over the
world. Common OP compounds are
• parathion, malathion, dyflos, etc
• They irreversibly inhibit cholinesterase's & cause a accumulation of
Ach at muscarinic & Nicotinic sites
Pharmacotherapy of Organophosphate poisoning
• Signs & symptoms:

1. Irritation of eye, lacrimation, salivation, trachea-bronchial secretions, colic, blurring
of vision, defaecation & urination
2. Fall in BP, tachy or bradycardia and CVS collapse
3. Muscular fasciculations, weakness and respiratory paralysis
4. Excitement, tremor, convulsions and coma
• TREATMENT:
◊ Decontamination-gastric lavage if needed
◊ Airway maintenance
◊ Supportive measures- for BP/fluid & electrolyte
◊ Specific antidote-Atropine-2mg IV every 10 min
CHOLINESTERASE till dryness of mouth or
REACTIVATORS
atropinization (upto 200mg/day).
(A)ATROPINE
 It is high effective in counteracting the muscarinic symptoms, but higher
doses are required to antagonize the central effects
 It does not reverse peripheral muscular paralysis which is in a nicotinic
action.
 All cases of anti-ChE(carbamate or organophosphate) poisoning must
be promptly given ATROPINE 2 mg I.V REPEATED EVERY 10 MIN till
dryness of mouth or other signs of atropinization appear
 Continued treatment with maintenance dosed may be required for 1-2
weeks
(B) CHOLINESTERASE REACTIVATORS
 Oximes are used to restore neuromuscular transmission only in case of
organophosphate anti Che poisoning.
 The phosphorylated CHE reacts very slowly or not at all with water.
However, if more reactive OH groups in the form of oximes are provided,
reactivation occurs more that a million times faster.
 Pralidoximes 1-2 mg (30mg/kg), IV as 15-30 min infusion [max 12g]
 Oximes improve action at nicotinic sites.
 It should be administered within 48 hours of organophosphorus poisoning;
otherwise when ageing occurs; the phosphorylated enzyme becomes
resistant to hydrolysis (following loss of an alkyl group)
A man age 45 years presented with gradual onset complaints of
double vision, drooping eyelids, difficulty in chewing food and
weakness of limbs which is accentuated by exercise. The
symptoms fluctuate in intensity over time. A provisional
diagnosis of myasthenia gravis is made.
a) Can a pharmacological test be performed to confirm/refute

diagnosis?
b) In case the diagnosis is confirmed, can this disease be cured
by medication?
c) Is there a surgical solution for this illness?
CASE STUDY
In mid-afternoon, a coworker brings 43-years old men to the emergency
department because he is unable to continue picking vegetables. His gait is
unsteady and he walks with support form his colleague. He has difficulty
speaking and swallowing, his vision is blurred, and his eyes are filled with tears.
His coworker notes that’s he was working in afield that has been sprayed early in
the morning with a material that had the odor of sulfur. Within 3hours after
starting his work, he complained of tightness in this chest that made breathing
difficult, and he called for help before becoming disoriented.
How would you proceed to evaluate and treat the patient?

What should be done for his coworker?
1. Botulinum toxin blocks the release of
acetylcholine from cholinergic nerve
terminals. Which is a possible effect of
botulinum toxin?
a) Skeletal muscle paralysis

b) Improvement of myasthenia gravis symptoms
c) Increased salivation
d) Reduced hear rate
2. A patient develops urinary retention after an
abdominal surgery. Urinary obstruction was ruled
out in this patient. Which strategy would be
helpful in promoting urination?
a) Activating nicotinic receptors

b) Inhibiting the release of acetylcholine
c) Inhibiting cholinesterase enzyme
d) Blocking muscarinic receptors
3. If an ophthalmologist wants to dilate the pupils
for an eye examination, which durg/class of drugs
is theoretically useful?
a) Muscarinic receptor activator (agonist)

b) Muscarinic receptor inhibitor (antagonist)
c) Pilocarpine
d) Neostigmine
4.In Alzheimer disease, there is a deficiency of
cholinergic neuronal function in the brain. Theoretically,
which strategy is useful in treating symptoms of
Alzheimer disease?
a) Inhibiting cholinergic receptors in the brain

b) Inhibiting the release of acetylcholine in the brain
c) Inhibiting the acetylcholinesterase enzyme in the brain
d) Activating the acetylcholinesterase enzyme in the brain
5. An elderly female who lives in a farmhouse was brought to the
emergency room in serious condition after ingesting a liquid from an
unlabeled bottle found near her bed, apparently is a suicide
attempt. She presented with diarrhea, frequent urination,
convulsions, breathing difficulties, constricted pupils (miosis), and
excessive salivation. Which of the following is correct regarding this
patient?
a) She most likely consumed an organophosphate pesticide.

b) The symptoms are consistent with sympathetic activation.
c) Her symptoms can be treated using anticholinesterase agent.
d) Her symptoms can be treated using a cholinergic agonist.
6. A patient who had received a nondepolarizing
neuromuscular blocker (NMB) for skeletal muscle
relaxation during surgery is experiencing mild
skeletal muscle paralysis after surgery. Which
drug could reverse this effect of NMBs?
a) Pilocarpine
b) Bethanechol
c) Neostigmine
d) Atropine
7. A 60 years old female who had a cancerous
growth in her neck region underwent radiation
therapy. Her salivary secretion was reduced due to
radiation and she suffers from dry mouth
(xerostomia). Which drug would be useful in
treating xerostomia in this patient?
a) Acetylcholine
b) Pilocarpine
c) Echothiopate
d) Atropine
8. A 40 years old male presents to his family physician
with drooping eyelids, difficulty chewing and
swallowing, and muscle fatigue on mild exertion.
Which agent could be used to diagnose myasthenia
gravis in this patient?
a) Atropine
b) Edrophonium
c) Pralidoxime
d) Echothiopate
9. Atropa belladonna is a plant that contains atropine
(a muscarinic antagonist). Which of the following
drugs of classes of drugs will be most useful in treating
poisoning with belladonna?
a) Malathion
b) Physostigmine
c) Muscarinic antagonists
d) Nicotinic antagonists
10. Which of the following cholinomimetic agent
is used for acute congestive glaucoma?
a) Muscarine
b) Pilocarpine
c) Arecoline
d) Edrophonium
11. The preferred agent for the treatment of
belladonna poisoning is
a) Physostigmine
b) Neostigmine
c) Pralidoxime
d) Pyridostigmine
12. How the following agents can be used to
differentiate the cholinergic and myasthenic crisis
a) D-Tubocurarine as it will aggravate the weakness due to

cholinergic crisis
b) Edrophonium as it will aggravate the weakness due to
myasthenia gravis
c) Edrophonium as it will relieve the weakness due to
myasthenia gravis
d) Ipratropium as it will relieve the weakness due to
cholinergic crisis
13. Which of the following statement is correct with
regard to treatment of acute organophosphate
poisoning?
a) Physostigmine is preferred due to its central as well as

peripheral effects
b) Neostigmine is preferred because of direct action on
receptors
c) Atropine is administered together with pralidoxime as
early as possible
d) Atropine is contraindicated but pralidoxime is used

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Toxins Interfere Cholinergic Transmission.

Tre-morine and Oxo-tre-morine are synthetic tertiary

• Edrophonium 2-10 mg injected slowly i.v.

Symptomatic treatment-acetylcholinesterase inhibitors

• Signs & symptoms:

a) Can a pharmacological test be performed to confirm/refute

How would you proceed to evaluate and treat the patient?

a) Skeletal muscle paralysis

a) Activating nicotinic receptors

a) Muscarinic receptor activator (agonist)

a) Inhibiting cholinergic receptors in the brain

a) She most likely consumed an organophosphate pesticide.

a) D-Tubocurarine as it will aggravate the weakness due to

a) Physostigmine is preferred due to its central as well as

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