Cholinergic agents

Question 1

Group and action of NICOTINE

Answer 1

N cholinoreceptor agonist, Acute biphasic effect, Phase 1 : N cholino stimulation:
phase 2 : Suppression of PNS

Question 2

Group, action and indication of CYSTEIN

Answer 2

N cholinoreceptor agonist, Smoking cessation agent,
Less toxicity, Higher therapeutic index
Competes
=>Tabacism, nicotine addiction therapy

Question 3

Group, action and indication of VARENICLINE

Answer 3

N cholinoreceptor agonist, Smoking cessation agent,
Selective partial agonist, Effect depends on nicotine,
Decreases rewarding effects of dopamine
=>Tabacism, nicotine addiction therapy

Question 4

Group, action and indication of SUXAMETHONIUM

Answer 4

N cholinoreceptor agonist, depolarising muscle relaxant
Biphasic action: In phase 1, analogous depolarization of ACh
In phase 2, the membrane polarization does not recover and a cholinolytic effect occurs - myorelaxation
=> Intubation of the trachea, short surgical manipulations

Question 5

Group, action and indication of PILOCARPINE

Answer 5

M cholinoreceptor agonist,
Miotic effect of eyes, accomodation, reduces intraocular pressure
Secretory effect, salivation
=> Glaucoma, glaucoma attack, xerostomia

Question 6

Neostigmine

Piridostigmine

Answer 6

Acetylcholinesterase inhibitor
Peripheral acting non selective AceI
doesn't cross BBB
=> Myasthenia
=> GIT atony
=> Urinary bladder atony
=> Overdose of peripheral muscle
relaxants

Question 7

DONEPEZIL

RIVASTIGMINE

Answer 7

Acetylcholinesterases
D: centrally acting selective
R: centrally acting non selective, Increases cognitive function
=> Alzheimer’s disease, dementia

Question 8

Toxicology of Acetylcholinesterases

Answer 8

D diarrhea, defecation
U urination
M myosis
B brochial spasms
B bradycardia
E excitation 
L lacrimation 
S salivation
S sweating

Therapy - AcHE reactivators (-oximes):Blocked enzyme dephosphorylation +
symptomatic therapy
Pralidoxime or Trimedoxime + Atropine

Question 9

TUBOCURARINE

TRIMETAPHAN

Answer 9

N cholinoreceptor antagonist
Localization: neuromuscular synapsis
Affects depolarization of the synaptic membrane

N cholinoreceptor antagonist
Localization - ganglia

Question 10

ROCURONIUM

Answer 10

N cholinoreceptor antagonist
Non-depol muscle relaxants
=>Muscle relaxation during surgical procedures

Question 11

ATROPINE

Answer 11

M cholinoreceptor antagonist 
Non-selective mACh receptor blocker
Antisecretory (reduces glandular secretion),
Long term mydriasis,
Cycloplegic (** accommodation
paralysis),
Antispasmodic (relaxes smooth
muscles),
Increases heart rate («+» chrono-, dromotropic effect)
Dose increases leads to CNS excitement

=>Symptomatic sinus bradycardia
(AV block)
=> Preoperatively, suppression of hypersecretion
=> Antidote – poisoning with insecticides
=> *GIT spasms

Question 12

Toxicology of Cholinoblockers

Answer 12

Delirium with visual hallucinations
Sedation / coma
Cramps
Dry mouth
Dry and hot skin
Mydriasis
Hyperthermia
Paralytic ileus

Therapy - mainly symptomatic,
In case of severe tachycardia, physostigmine

Question 13

Dysport

botox

Answer 13

Local ACh release inhibitors
in presynaptic vesicles of peripheral motor neurons-myorelaxation

=>Post-stroke hand spasticity,
cerebral palsy spasticity, spastic
cervical spine, blepharospasm
=> Hyperhidrosis in the armpit
=> Cosmetic surgery