Autonomic: Anticholine Estrases (Parasympathomimetic) Flashcards
general mechanism of Anticholine esterases
inhibit choline esterase enzyme —> Accumulation of Acetylcholine
enumerate reversible anti-choline esterases
- Physostigmine
- neostigmine
- Neostigmine substitutes (Edrophonium & Pyridostigmine, Ambenonium)
Action of Physostigmine & Neostigmine can be summarised as:
- Physostgmine = (🤓) is CNS stimulant
- Neostigmine = (💪🏼) is a powerful Muscle Stimulant
Compare between Source, Chemistry & distribution of Physostigmine & Neostigmine
- Physostigmine is Natural, Neostigmine is synthetic
- Physostigmine is Tertiary amine structure, Neostigmine is Quaternary structure
- Physostigmine Crosses BBB (avoided in parkinsonism), Neostigmine doesn’t cross BBB
Uses of Physostigmine
Eyes:
* Glaucoma
* Counteract Mydratics
treatment of Atropine poisoning
Uses of Neostigmine
- Glaucoma
- Paralytic ileus
- post-op urine retention
- Diagnosis & Treatment of Myasthenia gravis
- Antidote to atropine toxicity
- Antidote to neuromuscular blockers given during surgeory
from Edrophonium & Pyrostigmine/Ambenonium, which one has longer duration & more specific in treating Myasthenia gravis
Pyrostigmine/Ambenonium
edrophonium for diagnosis of Mysthenia gravis
Uses of Edrophonium
- Diagnosis of myasthenia gravis
- Treatment of Myasthenia crisis
- Diagnosis of cholinergic crisis
- Curare poisoning
uses of Pyrostigmine/Ambenonium
treatment of Myasthenia gravis
Use of Rivastigmine
treatment of Alzheimer’s
Clinical Manifestations of Organophosphorus compounds poisoning
- Miosis
- Bradycardia
- Hypotension
- bronchospam
- Increase in secretion (salivary, bronchial, lacrimal, sweat)
- Skeletal muscle twitches —> prolonged depolarisation —> Paralysis
- Central inhibition
- Convulsions
- Collapse
- Coma
Enumerte drugs used in treatment of OPC posioning
- Atropine
- Oximes (pralidoxime & obidoxime)
- Benzodiazepines (Diazipam)
target end-points in Atropine therapy in treatment of OPC posioning
- HR less than 80 bpm
- Systolic bp more than 80 mmHg
- dry mouth & axilla (decreased sweat & salivary secretion)
- Clear chest with absence of wheeze (no bronchial secretion)
- Dilated pupils (Mydrasis)
why do we use Oximes (pralidoxime & obidoxime) in treatment of OPC posioning
- reactivates choline esterase
- Restores muscle power
when do Oximes (pralidoxime & obidoxime) become ineffective in treating OPC poisoning
in late cases —> Aging of choline esterase (complete irrevesible inactivation)