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Parasympathetic (Cholinergic Agonist (Indirect Acting (reversible)…

- - - - has nicotinic and muscarinic actions
      - poor substrate of AchE
      - action
        
        cause miosis and spasm of accommodation
        
        decrease intraocular pressure, treat glaucoma
    - - strong muscarinic activity (M3)
        
        stimulate atonic urinary bladder
        
        increase intestinal motility
      - 1 hour duration of action
      - not hydrolyzed by AchE
      - sweating, salivation, nausea, diarrhea,bronchospasm
    - - lacks therapeutic importance
        
        action is too diverse
        
        rapid inactivation by cholinisterases
      - quaternary ammonium compound
    - - uncharged (tertiary amine), can penetrate CNS
      - can be hydrolyzed by AchE
      - has muscarinic activity
      - same action as carbachol
        
        also stimulate secretion of sweat, tears, saliva
      - adverse effect
        
        blurred vision
        
        night blindness
  - - - tertiary amine, intermediate acting (30 mins-2 hrs),
      - actions at muscarinic and nicotinic sites
      - increase intestinal & bladder motility, treatment of overdoses of drugs
      - adverse effect
        
        high doses lead to convulsion (sawan)
        
        bradycardia
        
        paralysis of skeletal muscle
    - - stimulate bladder & GIT, antidote for competitive neuromuscular blocker
      - effect on skeletal muscle is greater than physostigmine
      - quaternary nitrogen, cannot enter CNS
      - adverse effect
        
        general cholinergic stimulation
        
        conta-indicated when bladder obstruction is present (remove obstruction first)
    - - used for chronic management of myasthenia gravis
      - intermediate acting (3-6 hours)
    - - delay progression of Alzheimer's disease
      - adverse effect
        
        GI distress (bloating, cramping,abdominal distention & pain)
    - - used in diagnosis of myasthenia gravis and reversing effect of neuromuscular blockers after surgery
      - quaternary amine, rapidly absorbed, short duration of action (10-20 mins)
  - - - covalently binds via phosphate group at AChE active site
      - AChE permanently deactivated (inactive)
      - synthetic organophosphate
      - loss of alkyl group (aging)
- - - - overall response: summation of stimulatory and inhibitory effects
      - at low dose, increase BP. at high dose, decrease BP
      - at low conc will stimulate the receptors, at high conc will block the receptors
  - - - used as bronchodilators (delivered via inhalation)
      - do not enter CNS, only to pulmonary system
    - - treat Parkinson's disease & other parkinsonian syndromes
    - - tertiary amine, has greater action on CNS, longer duration of action than atropine
      - anti-motion sickness drug, produce sedation
      - at higher dose, can cause euphoria & excitement
    - - side effect: dry mouth, constipation, blurred vision
      - treat overactive bladder
    - - used as anti-spasmodic to reduce activity of GIT, low dose cause slight decrease in HR, high dose cause increase HR (block M2)
      - treat mydriasis and cycloplegia at longer time (7-14 days), replaced by cyclopentolate & tropicamide
      - cause xerostomia, elevated body temperature, mydriasis, cyclopegia, raise in intraocular pressure
      - tertiary amine, acts both centrally and peripherally, action last for 4 hrs, binds competitively to ACh
      - antispasmodic agent, treat bradycardia, anti-secretory agent to block secretions prior to surgery, antidote for cholinergic agonist
      - adverse effect
        
        CNS effect (restlessness, confusion, hallucination, delirium)
        
        tachycardia, urinary retention
        
        dry mouth, blurred vision
- - - - bladder, exocrine glands & smooth muscles
    - - cardiac cells & smooth muscles
    - - gastric parietal cells
  - - - adrenal medulla
      - autonomic ganglia
      - CNS
    - - NMJ in skeletal muscle